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Pharm 6 > All Drugs. All Units. Random Order. Wow. > Flashcards

All Drugs. All Units. Random Order. Wow. Flashcards

1
Q

Mineral oil

A

GI Drug

Cathartic–Stool softener

Mech: Acts like a lubricant

Why mineral oil should NOT be used:

  • Prevents fat soluble vitamin absorption
  • Aspiration pnemonia →may damage lungs
  • May contain carcinogens
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1
Q

Edrophonium

A

Indirect cholinergic agonist

Doesn’t last very long

Inhibit AChE

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1
Q

Muscarine

A

Direct muscarinic agonist

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1
Q

Dronedarone

A

Tx: arrytmhias (Class III)

Mech: K+ channel blocker

Analog of amiodarone

Fewer SE-less efficacious

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2
Q

High Ceiling diuretics mechanism

A

Mech of action:

  • Inhibit Na and Cl resorbtion from Asc. loop of Henle

More efficacious than thiazides

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3
Q

Piperacillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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3
Q

Thiazide diuretics

A

Chlorothiazide and hydrochlorothiazide

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4
Q

Tetrahydrozoline (Visine)

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

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5
Q

Paracalcitrol

A

Tx: Ca disorders

Mech: Vit D analog

Less potent than calcitriol

SE: Hypothyroidism

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5
Q

Ledipasvir

A

Antiviral agent

Tx: Hepatitis virus (esp Hep C)

Mech: Binds to and inh. protein thats necessary for HCV replication

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5
Q

Loratadine

A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
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5
Q

Inhibitors of Na transport in DCT and collecting tubule

A

Triamterene

Amiloride

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5
Q

Morphine

A

Narcotic analgesic- narcotic analogs

Given parenterally due to first pass effect

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5
Q

Triamterene

A

K sparing diuretic

Inhibitors of Na transport in DCT and collecting tubule

Mech:

Prevent Na from getting into the exchanger by blocking Na ion channel

-Effects more rapid and predictable than spironolactone

SE:

Hyperkalemia

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6
Q

Foscarnet

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Not a prodrug–directly inh. DNA pol

Route: IV 3x/day

SE: Renal damage

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6
Q

“-lukast”s

A

Zafirlukast

Montelukast

Tx: Asthma

Mech: Leukotriene receptor blocker

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6
Q

Metoprolol

A

Tx: arrythmias (Class II)

Mech: B1 blocker

More selective

SE:

  • Bradycardia
  • Hypotension
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7
Q

Mezlocillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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7
Q

Valacyclovir

A

Antiviral drug

Tx: Herpes simplex and zoster

Mech: Prodrug converted to acyclovir

Must be given orally-prodrug metab. by 1st pass metab.

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7
Q

Tocilizumab

A

Toci-li-zu-mab

MAb affecting immune sys. from humanized source

Immunosuppressant

Tx: RA

Mech: Binds to IL-6 receptor

  • Football players get tackled so they have RA but all of the ladies want to have risque sex w/ them*
  • Football players get tocilizumab so they have RA but all the ladies want to have IL-6 receptor with them*
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8
Q

Flax oil seeds

A

Uses:

  • Constipation
  • Diarrhea
  • IBS
  • Diabetes
  • Arthritis
  • Atherosclerosis
  • Menopause

May slightly lower total cholesterol

May decrease hot flashes

Mech: Soluble fiber and phyto estrogens

SE:

  • Increase GI act.
  • Allergic rxns
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8
Q

Calcium chelators

A

Citric acid (in blood transfusion bags(

ADTA

EGTA

Tx: Anticoagulants

Mech: Chelate Ca

Remove Ca from clotting cascade (4 steps need Ca)

We don’t give these to people b/c Ca is involed w/ lots of mechanisms

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9
Q

Erythromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth

-static

Mech: Reversibly binds to 50s subunit and inh. translocation of mRNA

Inh binding of tRNA to P site

Spectrum: G+

SE:

  • GI upset, nausea, and heartburn
    • Increase in GI activity b/c activates motilin
  • Inh P450
  • Liver damage
  • Arrythmias

macROlides like erythROmycin inh. transLOcation

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

O——

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10
Q

Which GCs used for IBS

A

Prednisone

Budesonide

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11
Q

ACE inhibitors

A

“-pril”s

ACE responsible for A1→A2

ACE responsible for bradykinin breakdown

Leads to decreased aldosterone secretion

SE:

  • Rash
  • Dry cough that cant be treated with suppressants
  • Angioneurotic edema-swelling of nose, throat, resp tract
  • Taste alteration
  • Fetal damage
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11
Q

Perampanel

A

Tx: Partial seizures

Mech: Blocks glutamate

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11
Q

Second generation antidepressants

A

Fluoxetine

Fluvoxamine

Sertraline

Paroxetine

Citalopram

Escitalopram

Vilazodone

Mech: SSRIs

SE:

  • GI upset
  • Nausea
  • Insomnia
  • Headache
  • Decreased libido
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12
Q

Saw Palmetto

A

Use: BPH

May be eff. but not as eff. as existing drugs (azosins”

Mech: Inh test synth (enz inh)+Inh test binding to receptor

SE:

  • Minimal SE
  • Drug interactions due to hormone effects
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12
Q

Clarithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Oral stability

vs. Helicobacter Pylori
* macROlides like erythROmycin inh. transLOcation*

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Oral stability

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12
Q

Leflunomide

A

Immunosuppressant

Prodrug. Gets converted into Teriflunomide

Mech: Inhibits dihydroorotate DH

  • Rate limiting step in production of pyrimidine (so inh. pyr. production)
  • Decrease in UMP and TMP
  • More effect on lymphocytes

SE:

  • Diarrhea and abdominal pain (rapidly replicating GI cells)
    • Flu like symptoms w/ flunomides
  • Teratogenic
    • Must take bile acid binding agent to get rid of all of drug if pregnant

Inhibits P450

  • You no ride w/ me–get another Designated Driver*
  • “Flu-no-ride w/ me. Get another DD (inh. Dihydroorate DH)*
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13
Q

Ganciclovir

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Prodrug-activated by viral kinase

SE:

  • Neutropenia
  • Thrombocytopenia
  • Teratogen
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13
Q

High ceiling diuretics

A

Furosemide, ethacrynic acid, bumetanide, torsemide

  • Orally or parenterally
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14
Q

Difenoxin

A

Tx: Diarrhea

Narcotic agent

Active metabolite of diphenoxylate

Mech: act a specific receptor

Acts primarily in gut

Opiate like effects in CNS though too

Given in comb w/ atropine to avoid abuse

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14
Q

Methicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

B-lactamase resistant

Narrow spectrum: G+

Does not readily enter CNS

Do not use anymore-too toxic

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14
Q

Tranylcypromine

A

Antidepressant-MAO inhibitor

Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)

Kinetcs: Slow onset

Toxicity:

Insomnia
Agitation
Hallucination
Seizure
Liver toxicity
Weight gain
Hypotension
Great increase in likelihood of suicide in children

Drug interactions:

Indirect acting amines→Hypertensive crisis

Some foods contain tyramine (smoked foods, aged cheeses, wine)

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15
Q

Psyllium

A

GI Drug

Cathartic–Bulk adding agent

Mech: Like eating fiber

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16
Q

Diphenoxylate

A

Tx: Diarrhea

Narcotic agent

Mech: act a specific receptor

Acts primarily in gut

Opiate like effects in CNS though too

Given in comb w/ atropine to avoid abuse

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16
Q

Ribavirin

A

Antiviral agent

Tx: RNA virus (RSV)

Only for severe lower resp inf.

Mech: Inh RNA dep DNA pol

Phosphorylated in cell.

SE:

  • Preg cat X
  • Hemolytic anemia
  • Decrease pulmonary fxn in infants
  • Cardiac arrest

Not used much anymore. Very expensive

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17
Q

Pyrazinamide

A

Antimycobacterial agent

Mech: Inh FA synth

Prodrug converted in macrophase where TB lives

SE:

  • Gout
  • Hepatitis
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17
Q

Nifedipine

A

Tx: Arrythmias except vent. arrythmias (class IV)

Mech: Ca channel blockers

Increase refractory period

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18
Q

Ethambutol

A

Antimycobacterial agent

Mech: Inh arabinosyl transferase

Necessary for CW synth

SE:

  • Optic neuritis
  • Impaired red/green discrimination
  • Decreased vision
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18
Q

Clavulanic acid

A

Mech: Bind to and inh. B lactamase

Non antibiotic B-lactam ring compounds

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18
Q

5-fluorouracil

A

Tx: Cancer

Mech: Inh. thymidylate synthatase→inh. thymidine synth

Prodrug–Pyrimidine analog

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18
Q

Omega 3 fatty acids

A

Tx: Hyperlipidemia

Mech: Inhibit enzyme responsible for Trig synth

Not clear though

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18
Q

Clonidine

A

Adrenergic agonist

Activates alpha2 receptors

Decrease symp outflow from CNS

Tx: hypertension

Other analogs used for glaucoma (Decrease pressure)

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19
Q

Nedocromil

A

“-crom-“

Tx: Asthma

Anti-inflammatory agent

Mech:

  • Inhibit release of mediators from immune cells
  • Inhibits Cl channels
  • Inhibits Ca uptake (Ca necessary for secretion)

Not bronchodilators

Route: inhalation

Not used much anymore

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20
Q

Fluoride

A

Tx: Ca disorders

Effects: Increase osteoblasts

Makes bone harder but more brittle

Not for osteoporosis

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20
Q

Inhibitors of Na transport in DCT and collecting tubule mech

A

K sparing diuretic

Prevent Na from getting into the exchanger by blocking Na ion channel

-Effects more rapid and predictable than spironolactone

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21
Q

Lamotrigine

A

Tx: Partial seizures

Mech: Inh. Na

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21
Q

Hirudin

A

Tx: Anticoagulant–found in leech saliva

Mech: Directly inhibits thrombin

Enzyme inhibitor

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22
Q

Budesonide

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Inhalation

1st pass metabolism

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
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22
Q

Eplerenone

A

K sparing diuretic

Aldosterone antagonist

_Mech: _

Blocks aldosterone receptor

Aldosterone is responsible for synth of Na-K exchanger

Takes days to be effective

Clinical use

Used w/ other diuretics to prevent K loss
To treat excess aldosterone production

SE

hyperkalemia
Spironolactone is a steroid and can have anti-androgenic effect (breast growth,etc)
Eplerenone-fewer interactions w/ steroid receptors

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23
Q

Atgam

A

ATGam

Tx: Acute renal transplant injection

Immunosuppressant

Antithymocyte globulin (ATG)–Polyclonal antibodies

Effects: Reduces circulating T cells(Wikipedia)

_A_ffects _T_ cell activation

SE:

  • Polyclonal antibodies may lead to allergic rxn
    • From horse or rabbit
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23
Q

Cyclophosphamide

A

Tx: Cancer

Mech: Alkylating agent

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth

Nitrogen mustard

Developed from mustard gas-destroys everything it touches

Prodrug given orally or IV

Stops cell from replicating once it hits DNA

Lots of collateral damage

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25
Q

Misoprostole

A

GI drug-Enhance mucosal defense

Tx: Ulcers

Drop in PGs→Ulcer

Asprin (NSAIDs) and GCs can decrease PGs

Mech: Prostaglandin analog

SE:

  • Uterine contractility (abortifacient)
  • You eat miso soup when you have a stomach ache because it is prostagrandin anarog (say that w/ a strong asian accent)*
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25
Q

Antifungals for candida+ ringworm

A

Miconazole

and other “conazoles”

Route: Topical and systemic

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25
Q

“-ergotamine”s

A

Ergotamine

Dihydroergotamine

Tx: Migrane

Mech: Partial 5HT receptor agonist

Can affect adrenergic and dopaminergic receptors

Useful in initial stages

SE:

  • Ergotism=excess of ergot alkaloids→St. Anthony’s Fire
    • Hallucinations (these are the source of LSD)
    • Uterine contractions-_preg. category X_
    • Severe vasospasm→gangrene (loss of O2 to periphery
  • ​Not as safe as triptans
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25
Q

Cocaine pharmacodynamics

A

Acts on transport systems

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25
Q

Epinephrine

A

Works on all adrenergic receptors

Causes increased HR, etc. etc.

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25
Q

Tirofiban

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Fibrinogen receptor blocker on platelet (GPIIB/IIIA receptor)

Clinical use: Decrease white thrombi

Used for coronary operation

Route: IV

SE: Thromobocytopenia

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25
Q

Amiloride

A

K sparing diuretic

Inhibitors of Na transport in DCT and collecting tubule

Mech:

Prevent Na from getting into the exchanger by blocking Na ion channel

-Effects more rapid and predictable than spironolactone

SE:

Hyperkalemia

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25
Q

Ethosuximide

A

Tx: DOC for petit mal seizures

Mech: Inhibit Ca channels in CNS

SE:

  • GI upset
  • Drowsiness
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26
Q

Metronidazole

A

Mech: Prodrug-converted to a free radical active molecule by obligate anaerobic bacteria

Route: IV for severe anaerobic bacterial inf.

Use: Protozoal inf:

  • Trichoma (STD)
  • Giardia (from water)

SE:

  • Seizures
  • Peripheral neuropathy
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26
Q

Quinidine

A

Tx: All arrythmias (Class Ia)

Mech: Na channel blocker

  • Depresses all mm fxn
  • Anti-cholinergic effects (antivagal effects)
  • *Vagal innervation slows HR–Quinidine will speed it up

SE:

  • GI
    • Nausea and vomiting
  • Anorexia
  • CNS
    • Tinnitus
    • Alterted color vision
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28
Q

-prazole

A

GI drug

Decrease acid formation

Mech: ATPase inhibitor

Known as proton pump inhibitor (PPI) but actually irreversibly inhibit ATPase required to drive H+ pump

Best available class of GI drugs

Prodrug-activated by acid

They are weak bases though→ stay in parietal cell

SE:

  • Hypochlorhydria-lack of H+ production
  • Decrease Ca absorption→osteoporosis
  • Decrease Vit B12 absorption
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29
Q

Phenytoin

A

Tx: Gran mal and others NOT petit mal

Mech:

  • Inh. Na channels in brain
  • Slows recovery rate of neuron
  • Generally not a CNS depressant

Pharmakokinetics:

  • Low TI

Toxicity:

  • Acute
    • Resp. depression
    • Cardiovascular collapse
    • Nausea
    • Ataxia
  • Chronic
    • Gingival hyperplasia
    • Vestibular effects
      • Diplopia
      • Ataxia
      • Blurred Vision
  • Some sedation
  • Teratogenic-fetal hydantoin syndrome
  • Life threatening rash-Stevens Johnson syndrome
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29
Q

Morphine pharmacodynamics

A

Agents that act on cell membrane receptors

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30
Q

Natamycin

A

Class: Antifungal

Polyene antibiotics

Route: Topical

Mech: Binds to ergosterol in fungal CM→pores→memb. leakage

Only one approved for use in eye

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30
Q

Diltiazem

A

Tx: Arrythmias except vent. arrythmias (class IV)

Mech: Ca channel blockers

Increase refractory period

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31
Q

Ampicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Rash in pts who have mononucleosis +other viral inf.
  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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31
Q

Carbapenems

A

Tx: Antibacterial–mixed infections

Penicillin analog

Small penicillinase resistant B lactam

Spectrum: Very broad

Route: IV

SE:

  • Can enter CNS→Seizures
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31
Q

Aldosterone antagonists clinical use

A
  1. Used w/ other diuretics to prevent K loss
  2. To treat excess aldosterone production
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32
Q

What are the stool softeners?

A

Dioctal sodium sulfosuccinate

Mineral oil

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32
Q

Methotrexate pharmacodynamics

A

Act on specific enzymes

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32
Q

Homatropine

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

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33
Q

Methotrexate

A

Tx: Cancer (and RA and psoriasis)

Mech:

  • Analog of Folic Acid
  • Inh. enzyme: Dihydrofolate reductase
  • PABA→Folic acid⇒Dihydrofolic acid⇒tetrahydrofolic acid
    • ⇒ indicate where DHFR works

SE:

  • Myelosuppression-inh. of blood cells
    • Can be dealt w/ by giving leucovorin-THFA analog
      • Does not require DHFR
    • Will rescue “normal” cells, but not malignant cells
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33
Q

Propranolol

A

Tx of hypertension

Nonselective Beta blocker

Central and peripheral effects

Mech:

  • Blocks B1 receptors on heart, prevents rise in HR
  • Decreases renin secretion
    • Renin converts Angiotensinogen→A1

SE:

  • Into CNS→Depression
  • Bradycardia→fatigue
  • Impotence
  • Lowers HDL, raises triglycerides
  • Exacerbates asthma
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34
Q

Sulfisoxazole

A

PABA*→folic acid→DHFA**→THFA

*→=Dihydropterate synthetase

**→DHFR

Mech: Reversible inh. dihydropterate synthetase

For UTIs

SE:

  • Allergic whole body rash (Stevens Johnson syndrome)
  • Hemolytic anemia in G6PDH deficient pts
  • Megaloblastic anemia

Sulfa drugs have sulf or sul

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34
Q

Longer lasting relatively selective B2 agonists

A

Formoterol

Arformoterol

Salmeterol

Indicaterol

“rols” w/o any “b”s​

Tx: Asthma

Bronchodilator–DOC for short term relief

Mech: B2 agonist–not completely selective

Cause even more down regulation of B2 receptors

Not as effective for rapid relief

SE:

  • Tremors
  • Tachycardia
  • Heart palpitations
  • Indigo Salmon Asked For More*
  • Indigo Salmon Asked Fo mo’*

_Ind_icaterol _Salmo_eterol _A_r_formo_terol _Formo_terol

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34
Q

Relatively selective B2 agonists

A

Albuterol

Pirbuterol

Bitolterol

Levalbuterol

Tertbutaline

Relatively selective are the only B2 agonists with a “b” and a “rol” (and tertButaline)

Tx: Asthma

Bronchodilator–DOC for short term relief

Mech: More specific B2 agonist than isoproterenol

Kinetics: Longer T1/2=6hrs

Route: Inhalation–immediate onset

SE:

  • Tremors
  • Tachycardia
  • Heart palpitations
  • Fewer SE than isoproterenol but still some B1
  • Downregulation of receptor
    • Any receptor activators may do this
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35
Q

Calcium carbonate

CaCO3

A

Antacid

Speed-rapid

Duration-medium

Neutralizing-high

SE:

  • Constipating
  • Hypercalcemia
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35
Q

Nitrofurantoin

A

Mech: Reduced by bacteria to a highly reactive molecule

Concentrates in urine

Use: UTI

SE:

  • Cough
  • Chest pain
  • Brown urine
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37
Q

Amitriptyline

A

First generation antidepressant

Tricyclic antidepressants

Mech: Inhibit NE reuptake

Act on multiple receptors

SE:

Most likely to cause SE
Sedation
Weight gain
Anticholinergic effect (dry eyes, dry mouth, constipation)
Cardiovascular effects

Arrythmias
Drop in BP (alpha1 block)
Orthostatic hypotension

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37
Q

Hydroxyurea

A

Mech: Increase formation of fetal Hb (does not sickle)

SE: Mutagenic

Pregnancy category D

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38
Q

Ibritumomab

A

Tx: Cancer

Mouse MAB

Severe infusion rxn

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39
Q

Bismuth subsalicylate

A

GI drug-Enhance mucosal defense

Anti-diarrheal agent–absorbing agent

Mech: Increase mucous production in stomach

Inh. growth of H. pylori

Unpleasant taste+odor

SE:

  • Long term use→Darkening of feces, tongue, and teeth
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39
Q

Rimantadine

A

Antiviral agent

Tx: RNA virus (Influenza A virus)

Virus taken up by cell endosome→opens channel in endosome→H enters→virus can release genes

Mech: Blocks process by which H channel forms in endosome

Blocks transporter or ion channel

Used proph. or very early

Widespread resistance

SE: Fewer than amantidine but similar SE

  • Renal failure
  • Teratogen
  • CNS fx
    • Dizziness
    • Slurred speech
    • Confusion
    • Seizures
    • Nausea
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40
Q

Griseofulvin

A

Class: Antifungal

Tx: Nail inf.

Nail inf. must be treated systemically to avoid painful tx

Mech: Binds to fungal microtubules→inh. fungal mitosis

Taken up by growing human skin cells and concentrated in keratin

Route: Systemic

Not well absorbed on skin

Most excreted unchanged

SE:

  • Headache
  • Induction of P450
  • Allergies
    • Derived from penicillium mold
  • Eat greasy fries and you will get fat *
  • Eat grise microtubules (fries) and you will get PHAT*

Griseofulvin binds microtubules. P450 induction, Headache, Allergies, t_reats _Toenail inf.

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40
Q

Indomethacin

A

NSAID

Tx: Patent ductus arteriosus

  • Hole would not close due to excess PGs
  • Indomethacin would allow closure, but so does ibuprofen too

Mech: Very potent COX inh.

Acetic acid derivative

SE:

  • Thrombocytopenia
  • Aplastic anemia
  • Corneal opacity
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40
Q

Basiliximab

A

Immunosuppressant

Mech: IL-2 receptor blocker

Used w/ CSA

65% human (chimeric)

Hypersensitivity rxn

  • Hypotension
  • Bronchospasm
  • Pulmonary edema

Harry Potter is a hypersensitive bitch when he fights the basilisk in the Chamber of Secrets, which is the 2nd reading in the series

Hypotension + Pulmonary edema, hypersensitivity, bronchospasm, basiliximab, used w/ CSA. IL-_2_ receptor blocker

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41
Q

Dobutamine

A

Tx: CHF

Class: Inotropic agents

Mech: Beta1 agonist

Effects: Increase force of contraction

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42
Q

Tranylcypromine pharmacodynamics

A

Act on specific enzymes

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43
Q

Adalimumab

A

Ada-li-mu-mab

Tx: RA

Immunosuppressant

Mech: Binds TNF

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44
Q

Vincristine and vinblastine

A

Tx: Cancer

Mech: Bind to microtubules and block cell mitosis

Route: IV

Natural product

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45
Q

Naloxone

A

Narcotic analgesic antagonist

Opiate receptor blocker

Naloxone-oxycodone combinations exist to make withdrawl easier

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46
Q

Heroin

A

Narcotic analgesic- semisynthetic

Originally to cure morphine addiction

5x stronger than morphine

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47
Q

Tacrolimus

A

Tx: Transplantation

Immune suppression

Mech:

  • Binds to FK binding protein
  • _Inh. calcineurin phosphatase _
    • Like cyclosporin but binds to diff protein→inh. of cytokine synth

More eff. than cyclosporin A-Increase max inh. effect

SE:

  • Nephrotoxicity
  • Neurotoxicity
  • Alopecia (baldness)
    • Less cosmetic effects than cyclosporine
  • Diabetes

Metab by P450

  • Tacrolimus for transplantations*
  • What else binds to FK protein? Sirolimus/Everolimus*
  • Tacrolimus: Inh calcinuerin phosphatase*
  • Sirolimus: Inh kinase*
  • What else affects calcinuerin phosphatase? Cyclosporine*
  • Cyclosporine: Binds cyclophyllin*
  • Tacrolimus: Binds FK protein*
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48
Q

“Poetin” and “Pegin”

A

Epoietin alfa

Darbepoietin

Peginesatide

Tx: Anemia due to chronic renal failure or chemotherapy

Toxicities: Due to excess RBCs

  • Increase BP
  • Increase clotting
  • MI
  • Stoke
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49
Q

Bacitracin

A

Antibacterial

Class: Non B lactam CW inhibitors

Polypeptide

Mech: Inh. recycling of bactoprenol carrier

Spectrum: G+

Route: Topically–very toxic

SE:

  • Nephrotoxicity–if not given topically
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50
Q

Ginseng

A

Uses: Increase energy

No clear effect

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51
Q

Glucocorticoids

A

Effects: Inh. osteoblasts

So bone loss

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52
Q

Soy

A

Uses:

  • Hyperlipidemia
  • Osteoporosis
  • Menopause

Decreases LDL

Decreases Menopausal symptoms

Mech: Metab. to estrogen like compound

SE: Allergic rxns

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53
Q

“-rudin”s

A

Bivalirudin

Desirudin

Tx: Anticoagulant

Synthetic analogs of hirudin

Clinical use: when patient has HIT

Skin grafts and reattaching body parts

Route: Injection

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54
Q

Sodium Bicarbonate

NaHCO3

A

Antacid

Speed-rapid

Duration-short

Neutralizing-high

SE:

  • CO2 production
  • Belching
  • Na may compromise low sodium diets
  • Systemic absorption
    • Contains Na
    • Important in those w/ kidney dysfunction
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54
Q

Promethazine

A

First gen H1 blocker

Tx: Strong sedative, strong anti-emetic

Related to anti-psychotic drugs

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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55
Q

Bevacizumab

A

Tx: Cancer

Mech: blocks VEGF

Prevents Vascular epi. growth factor from binding to receptor

Tumor can only grow w/ blood supply-this blocks it

_Beave_rs are _veg_etarians

Beva-cizumab–VEGF

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56
Q

Heparin

A

Effects: Act. osteoclasts

So bone loss

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56
Q

Fluoxetine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

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56
Q

Ezogabine

A

Tx: Partial seizures

Mech: Open K channel

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57
Q

Venlafaxine

A

Third Generation Antidepressant

Mech: SNRIs

Inhibit reputake of 5HT and NE

*Third generations have the -faxine drugs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation

*SE same as 2nd gen +cardio stim.

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58
Q

alpha-methyl NE

A

Adrenergic agonist

Activates alpha2 receptors

Decrease symp outflow from CNS

Tx: hypertension

Other analogs used for glaucoma (Decrease pressure)

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59
Q

Isoniazid

A

Antimycobacterial agent

Mech: Produces inh. of multiply mycobacterial enzymes

Inh CW synth

Prodrug

Cidal, but static for dormant cells

Used alone for prophylaxis–in combo for active tx

Metabolized by acetylation–slow acetylators affected

SE:

  • Increase excretion of vit B6→pyroxidase deficiency→niacin deficiency
  • Pellegra
  • Peripheral neuropathy
  • Optic neuritis
  • Hepatotoxicity

Isoniazid is IHOPPIN

Inh. mycobacterial enz.

  • Hepatotox.
  • O**ptic neuritis.

*Peripheral neuropathy + Pellegra. *

Prodrug + Prophylaxis

Increase excretion of vit B6→→

Niacin def.

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60
Q

Lamivudine

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

Discontinuation→Increase hepatitis symptoms

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62
Q

Telbivudine

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE:

  • Lactic acidosis
  • Hepatomegaly

Discontinuation→Increase hepatitis symptoms

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64
Q

Antimycoplasma agents

A

NO CELL WALL!

So use non CW inhibitors:

Erythromycin

Tetracycline

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65
Q

Polymixin B

A

Antibacterial agent

Mech: Binds to negatively charged sites on LPS of G- bact

→to memb. permeability

Route: Topical

SE: (all reversible)

  • Nephrotoxic
  • Neurotoxic
  • Neuromuscular blockade
  • Ataxia
  • Perioral paresthesia
  • Poly mixes in her PANNNN*
  • Polymixin B. Perioral paresthesia. Ataxia. Neurotoxic. Nephrotoxic. Neuromuscular blockade. binds to Negatively charged sites on LPS*
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67
Q

Varenicline

A

Direct partial nicotinic agonist

Binds to receptor but does not fully activate it. Thus prevents others from binding.

Anti-smoking drug b/c binds but does not have effects of nicotine

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68
Q

Cinecalcet

A

Tx: Ca disorders + hyperparathyroidism

Mech: Calcium mimetic

Sensitizes parathyroid Ca receptors to Ca→Decrese PTH secretion

Like there is a lot of Ca around

SE

  • Hypocalcemia
  • Nausea
  • Diarrhea
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68
Q

Etanercept

A

Tx: RA

Immunosuppressant

Mech: Binds TNF

Route: SubQ (in comb. w/ other immunosupp)

Synthesized molecule

eTaNercept-binds TNF

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68
Q

Eptifibatide

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Fibrinogen receptor blocker on platelet (GPIIB/IIIA receptor)

Clinical use: Decrease white thrombi

Used for coronary operation

Route: IV

SE: Thromobocytopenia

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69
Q

Tapentadol

A

Narcotic and SSRI

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70
Q

Azithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Longer T1/2 (3 days)

macROlides like erythROmycin inh. transLOcation

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

O——

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71
Q

Pancuronium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

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73
Q

Nizatidine

A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
  • Histamine required to stim. acid secretion from parietal cells
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74
Q

-previr

A

Boceprevir

Telaprevir

Simeprevir

Antiviral agent

Tx: Hepatitis virus (esp Hep C)

Mech: HCV protease inh.

Virus makes proteins but cannot be processed to final stage

Used in comb. w/ interferon

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75
Q

Vilazodone

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

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76
Q

Simethicone

A

Tx: Diarrhea

Mech: Changes gas surface tension of gas pocket in gut

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77
Q

Vancomycin

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Binds to dialanine residue on CW and prevents cross linking

Use: Severe infection in which B lactams can’t be used

Primary alt. to penicillins for staph infections.

Spectrum: G+

Route: IV–unless target in gut (pseudomembranous colitis)

SE:

  • Nephrotoxicity
  • Ototoxicity
  • If given rapidly via IV→histamine release→Redman or red neck syndrome
    • Flushing
    • Rash
    • Itching

Resistance:

  • Target changed
  • Dialanine changed to lactic acid

Dr. Van Ron

Dialanine Residue. Vancomycin. Redman. Ototox. Nephrotox

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78
Q

Loperamide

A

Tx: Diarrhea

Narcotic agent

Narcotic DOC for diarrhea

Mech: act a specific receptor

Acts ONLY in gut–no CNS effects

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78
Q

-pristin

A

Quinupristin (A+P site)

Dalfopristin (P site)

Mech: Inh. A and P sites

Always used together–synergistic

SE: Muscle pain

Spectrum: G+

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78
Q

Etodolac

A

NSAID

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79
Q

Anastrazole

A

Tx: Cancer

Mech: Inh. aromatase

Aromatase converts test→estr.

  • Ana is strong b/c aromatase inh. so test can’t be converted to est. *
  • Ana-stro-zole. Aromatase Inh so no conversion to est.*
  • *Both of the estrogen blockers have a woman’s name and a reference to strength**

Tam-ox-ifen

Ana-stro-zole

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80
Q

What are the long acting designer insulins?

A

Detemir

Glargine

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82
Q

Penicillin G

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Narrow spectrum: G+

Natural penicillin

Route: IV or IM–hydrolyzed w/ stomach acid

Given w/ procaine to slow release

Destroyed by B lactamase

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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82
Q

Azathioprine

A

Tx: RA, Chron’s, trans

Prodrug

Mech:

  • Converted to 6-mercaptopurine
  • Inh. synth of purines (guanosine required for DNA synth)
  • Inh. several enzymes responsible for GMP synth
    • Non specific

SE:

  • Bone marrow suppression→
    • Megaloblastic anemia
    • Thrombocytopenia
    • Leukopenia

6-mercaptopurine is also an anti-cancer agent

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83
Q

Denosumab

A

Tx: Ca disorders

Mech: Blocks a receptor (RANKL)

RANKL required for osteoclast production, activity, and survival

Given every 6 mnths

SE:

  • Hypocalcemia
  • Osteonecrosis of jaw
  • Skin inf.

Deno- SHO

Skin inf.

Hypocalcemia

Osteonecrosis

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83
Q

Cimetidine

A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
    • Histamine required to stim. acid secretion from parietal cells

SE:

  • Anti-androgenic effect
    • Males: gynecomastia and reduced sperm count
    • Females: Lactation
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83
Q

Pyroxicam

A

NSAID

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83
Q

Fomepizole

A

Specific inhibitor of alcDH

Prolongs effects of alcohol

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84
Q

Mg(OH)2

A

GI Drug

Cathartic–Osmotic agent

AKA Milk of Magnesia

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85
Q

Beclomethasone

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Inhalation

1st pass metabolism

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
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86
Q

Amikacin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

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88
Q

Ipecac

A

Emetic–reflex stimulant

Mech: Act. receptors in GI mucosa

Instant severe vomiting

SE: Cardiotoxic

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88
Q

Fexofenadine

A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
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88
Q

Hydralazine

A

Act directly on smooth muscle

Arterial vasodilator

Increase in cGMP→relaxes smooth m

SE:

  • Slow acetylators→lupus like syndrome
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89
Q

Dipryridamole

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Inhibits phosphodiesterase

Inh. enzyme that breaks down cAMP

Increased cAMP→Decrease platelet agg.

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89
Q

Furosemide

A

High ceiling diuretics

Orally or parenterally

Mech of action:

Inhibit Na and Cl resorbtion from Asc. loop of Henle

More efficacious than thiazides

Clinical use:

Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn

Side effects:

Dehydration
Hypokalemia

—Used w/ K supplements or K sparing diuretics

Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents

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90
Q

Kanamycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

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90
Q

Pralidoxime

A

If given early can reduce any perm. damage caused by organophosphate AChE inhibitors

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90
Q

Warfarin

A

Tx: Anticoagulant

Mech:

  • Vit K analog–*Koagulation*
  • Inhibits enzyme that allows vit K to be recycled
    • Leads to vit K deficiency
  • Vit K is essential for factors 7, 9, 10 and prothrombin
  • Works indirectly-doesn’t directly block clotting cascade

Route: Oral

Pharmacokinetics:

  • Factor T1/2s (hrs)
    • VII–6
    • IX–24
    • X–40
    • II–60
  • So 5-6 T1/2s for 99% to be gone
    • 30-36 hrs
    • So initial onset is 24+ hours
  • Metabolism
    • P450
    • Lots of drug interactions
      • Phenytoin/barbituates vs grapefruit juice, etc.
    • Diet interactions
      • Lots of Vit K in green veggies

Toxicity:

  • Overdose-tx w/ Vit K
  • Hemorrhage
  • Can pass placenta-preg. category X
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91
Q

Castor oil

A

GI Drug

Cathartic–Gastric Irritants

Mech: Stimulate gastric nn

Increase motility

Decrease electrolyte secretion into gut

SE:

  • Nephritis
  • Liver damage
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91
Q

Trimethoprim

A

Antibacterial agent

Mech: Inh. DHFR (like methotrexate)

Specific for bact. enzyme

*Used in conj. w/ sulfamethoxazole *

SE:

  • Megaloblastic anemia
    • Can be avoided w/ leucovorin

Targets:

  • G- bacteria
  • UTIs
    • Concentrates in acidic prostate and vaginal tissue
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91
Q

Anakinra

A

Tx: RA

Mech: Blocks IL-1 receptor

Route: SubQ

Used w/ other immunosuppressants like methotrexate

Should NOT be used w/ TNF inh b/c may lead to serious infection (too much suppression)

anakinRA=RA=RAceptor blocker

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92
Q

Bedaquiline

A

Antimycobacterial agent

Mech: inh. mycobacterial ATP synthetase

Always used w/ 3 other anti-TB drugs

SE:

  • Arrythmias
  • Increase incidence of death

*You’re in your bed MASTurbating and you go too hard and have an arrythmia *

_Bed_aquiline. Mycobacterial Atp SyntheTase. Arrythmia.

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93
Q

Abiraterone

A

Tx: Cancer (prostate)

Mech: Inhibits 17-hydroxylase lyase (CYP 17)

Inhibits androgen synthesis

Inhibits P450

  • Get this man a beer, at least 17 sips, he can’t make any androgens.*
  • Get this men abir-aterone, 17 CYP, can’t make any androgens*
  • P450 inhibitors from this unit: Abiraterone and -flunomides*
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94
Q

Valganciclovir

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Prodrug-converted to ganciclovir by viral kinase

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95
Q

Alprostadil

A

Tx: ED

Injectable prostaglandin (PGE1) leads to vasodilation when injected directly into penis

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97
Q

Harvoni

A

DOC for HCV

Ledipasvir+sofosbuvir

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98
Q

Pramlintide

A

Tx: Diabetes

Amylin analogs

Mech: Activate amylin receptor→

Decrease gastric emptying

Decrease appetite

Route: SubQ before meals

SE:

  • Severe hypoglycemia
  • prAMLINtide=AMyLIN analog*
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99
Q

Cisplatin

A

Tx: Cancer

Mech: Alkylating agent

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth

Contains platinum (expensive)

Associated w/ renal damage and ototoxicity

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100
Q

Nabumetone

A

NSAID

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100
Q

Mycophenolate mofetil

A

Tx: Transplants and lupus

More specific replacement than azothioprine

Inh. enzyme inosine monophosphate DH→Inh. guanisine synth.

SE:

Bone marrow decrease

GI cell disruption

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101
Q

Anagrelide

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Platelet count reducer

Decreases platelet formation, maturation, and #

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102
Q

Hydromorphone

A

Narcotic analgesic- semisynthetic

10x stronger than morphine

“Dilaudid”

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103
Q

Bisacodyl

A

GI Drug

Cathartic–Gastric Irritants

Mech: Stimulate gastric nn

Increase motility

Decrease electrolyte secretion into gut

SE:

  • Nephritis
  • Liver damage
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103
Q

Cycloserine

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Inh. incorporation of alanine into NAM

Enzyme inhibitor

Used against mycobacterium TB

SE:

  • CNS
    • Sedation
    • Tremor
    • Psychosis
  • Cyclo- gives you psycho-*
  • Go to war in NAM, when you come back you have PTSd*
  • Psychosis*
  • Tremors*
  • Sedation*
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103
Q

Spironolactone

A

K sparing diuretic

Aldosterone antagonist

Mech:

Blocks aldosterone receptor

Aldosterone is responsible for synth of Na-K exchanger

Takes days to be effective

Clinical use

Used w/ other diuretics to prevent K loss
To treat excess aldosterone production

SE

hyperkalemia
Spironolactone is a steroid and can have anti-androgenic effect (breast growth,etc)
Eplerenone-fewer interactions w/ steroid receptors

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104
Q

Everolimus

A

Tx: Transplant, psoriasis

Mech: Bind to FK binding protein

inh. kinase required for binding of IL-2 induced transcription factors to DNA→decreased cytokine production

Often used in combination w/ glucocorticoids

SE:

  • Some renal toxicity
    • Less than tacrolimus
    • Synergistic effect w/ used in comb w/ many immunosupp.
  • Some lung toxicity

Metab by P450

…

  • What else binds to FK protein? Tacrolimus*
  • Tacrolimus: Inh calcinuerin phosphatase*
  • Everolimus/Sirolimus: Inh kinase*
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106
Q

Tenofovir

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE:

  • Lactic acidosis
  • Hepatomegaly

Discontinuation→Increase hepatitis symptoms

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107
Q

Citalopram

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

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109
Q

Isosorbide dinitrate

A

Tx: Angina

Slow release nitrate formulation

Can be given orally

Slow enough that effects occur before 1st pass metabolism

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110
Q

Bortezomib

and carfilzomib

A

Tx: Multiply myeloma

Mech: Proteasome/protease inh.

Enzyme inhibitors

Allows excess proteins to accumulate and kill myeloma

“Zomibs” inh. proteaZomes

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112
Q

Bleomycin

A

Tx: Cancer

Mech: Intercalates w/ DNA-causes DNA strand breakage

SE: pulmonary fibrosis

_Bl_eo_my_cin _bl_ows my DNA apart

_Bleo_mycin affects your ability to blow (Pulmonary fibrosis)

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113
Q

Methadone

A

Narcotic analgesic- synthetic

Orally effective-liquid

Less euphoric

Given to wean off morphine

Same strength as morphine

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114
Q

Teriflunomide

A

Immunosuppressant

Gets converted from prodrug Leflunomide

Mech: Inhibits dihydroorotate DH

  • Rate limiting step in production of pyrimidine (so inh. pyr. production)
  • Decrease in UMP and TMP
  • More effect on lymphocytes

SE:

  • Diarrhea and abdominal pain (rapidly replicating GI cells)
    • Flu-like symptoms w/ flunomides
  • Teratogenic
    • Must take bile acid binding agent to get rid of all of drug if pregnant

Inhibits P450

  • You no ride w/ me–get DD*
  • “Flu-no-ride w/ me. Get DD (dihydroorate DH)*
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114
Q

Argatroban

A

Tx: Anticoagulant

Peptide from hirudin-diff structure, similar mech

Clinical use: when patient has HIT

Skin grafts and reattaching body parts

Route: Injection

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115
Q

Fulvestrant

A

Same as Tamoxifen

Tx: Cancer

Mech: Blocks estrogen receptor

SE:

  • Cataracts
  • Retinal changes
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116
Q
A
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117
Q

Ustekinumab

A

Ustek-i-nu-mab

MAb affecting immune sys. from human source

Immunosuppressant

Tx: Psoriasis

Mech: Binds to IL-12, 23

  • Michael Jordan used to wear #23 until someone stole his jersey and he had to wear #12 (true story). Whoever stole it ought to be sorry.*
  • MJ uste-kinumab wear IL-23 then wore IL-12. They ought to be psoriases.*
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119
Q

Dapsone

A

Antimycobacterial agent

Related to sulfonamides

Mech: Reversible inh. dihydropterate synthetase

Use: For mycobacterium leprae (leprosy

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121
Q

Famotidine

A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
  • Histamine required to stim. acid secretion from parietal cells
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122
Q

Ticlopidine

A

Tx: Anticoagulant

Mech: Platelet inhibitor

ADP receptor blocker on platelet

SE:

  • Neutropenia-loss of neutrophils
  • Agranulocytosis
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123
Q

Polycarbophil

A

GI Drug

Cathartic–Bulk adding agent

Mech: Like eating fiber

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124
Q

Aspart

A

Tx: Diabetes

Designer insulin

Short acting (2-5 hrs)

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124
Q

What agents bind TNF

A

Etanercept (RA)

Infliximab (RA,C)

Certolizumab (RA,C)

Adalimumab (RA)

Golimumab (RA, etc)

Think TNF=TNT (dynamite)

Explosions In Caves Affect Gollum

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125
Q

Procainamide

A

Tx: All arrythmias (Class Ia)

  • Also LA

Mech: Na channel blocker

  • Like quinidine but does not get into CNS
  • Quinidine:*
  • Depresses all mm fxn
  • Anti-cholinergic effects (antivagal effects)
  • *Vagal innervation slows HR–Quinidine will speed it up

SE:

  • Lupus like syndrome in slow acetylators
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126
Q

Yohimbe

A

Use: ED

Mech: Alpha 2 blocker in CNS

SE:

  • Hypertension
  • MAOI
  • CNS excitation
  • Tachycardia
  • Tremor
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127
Q

Inhibitors of Na transport in DCT and collecting tubule SE

A

Hyperkalemia

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129
Q

Fenoldopam

A

Activate D1 receptors

Given IV for HT emergencies

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131
Q

Icosapent

A

Tx: Hyperlipidemia

Mech: Inhibit enzyme responsible for Trig synth

Not clear though

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132
Q

Maraviroc

A

Tx: HIV

Mech: Blocks binding site on macrophage preventing entry of virus

Fusion inhibitor

SE:

  • Hepatotoxicity
  • Allergies
  • Increase MI
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132
Q

Glucocorticoids

A

Tx: Inh. all immune processes

Immunosuppressant

Mech:

  • GC cross CM, bind to receptor and dimerize, then affect trans.
  • Decrease PGE and leukotrienes
  • Alter migration of immune cells

Often used in comb. w/ other immunosuppressants

SE: Sig SE w/ long term use. Refer to other lecture

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132
Q

Aldosterone antagonists SE

A
  • hyperkalemia
  • Spironolactone is a steroid and can have anti-androgenic effect (breast growth,etc)
  • Eplerenone-fewer interactions w/ steroid receptors
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134
Q

Cromolyn sodium

A

“-crom-“

Tx: Asthma

Anti-inflammatory agent

Mech:

  • Inhibit release of mediators from immune cells
  • Inhibits Cl channels
  • Inhibits Ca uptake (Ca necessary for secretion)

Not bronchodilators

Route: inhalation

Not used much anymore

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135
Q

Calcitonin

A

Tx: Ca disorders

Mech: Binds to and inh. osteoclasts

Effects opposite of PTH

Secreted by thyroid gland

1st line of defense for Paget’s disease

SE:

  • Increase risk of cancer
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137
Q

Sarin

A

Nerve gas-direct cholinergic agonist

Irreversible AChE inhibitors

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139
Q

MAO inhibitors

A

Tranylcypromine

Phenelzine

Isocarboxazid

Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)

Kinetcs: Slow onset

Toxicity:

  • Insomnia
  • Agitation
  • Hallucination
  • Seizure
  • Liver toxicity
  • Weight gain
  • Hypotension
  • Great increase in likelihood of suicide in children

Drug interactions:

  • Indirect acting amines→Hypertensive crisis
    • Some foods contain tyramine (smoked foods, aged cheeses, wine)
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141
Q

Propranolol

A

Tx: arrythmias (Class II)

Mech: B1 blocker

Decreases pacemaker firing rate

SE:

  • Bradycardia
  • Hypotension
  • B2 effects-asthma
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142
Q

Tramadol

A

Narcotic and SSRI

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143
Q

Exenatide

A

Tx: Diabetes

Incretin enhancer

Mech: Bind to and activate receptors on B cell

Analog of GLP-1 (incretin)

Not broken down by DPP-4

Injection 2x/day

SE:

  • Pancreatitis
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144
Q

“Choles- or coles-“

A

Cholestyramine

Colestipol

Coleselevam

Tx: Hyperlipidemia

Mech: Irreversibly binds bile acids in gut→choles. excreted

Effects:

  • Decrease circulating cholesterol
  • Increase LDL receptor

Combine w/ statins for additional decrease in LPs

SE:

  • No systemic SE-too big to be absorbed
  • Can bind drugs
    • Digoxin
    • Oral anti-coagulants
  • Decrease absorption of fat soluble vitamins
  • GI upset-nausea
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145
Q

Tolazamide

A

Tx: Diabetes

Oral hypoglycemic agents

First gen sulphonylureas

Mech: K channel blockers

Block K channels on B cells →Increase Ca→Insulin secretion

Duration: 12-60 hrs

Contra/Indications:

  • Do not use if you have renal or hepatic damage
  • Not overweight
  • Have some islet fxn

SE:

  • Hypoglycemia and hypoglycemia coma
    • More common in drugs w/ longer duration
  • Can be teratogenic
  • Can increase death due to cardiovascular problems
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146
Q

Bumetanide

A

High ceiling diuretics

Orally or parenterally

Mech of action:

Inhibit Na and Cl resorbtion from Asc. loop of Henle

More efficacious than thiazides

Clinical use:

Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn

Side effects:

Dehydration
Hypokalemia

—Used w/ K supplements or K sparing diuretics

Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents

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148
Q

Meperidine

A

Narcotic analgesic- synthetic

.5x as strong as morphine

No pupil constriction

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150
Q

Levetiracetam

A

Tx: Partial seizures

Mech: Unknown

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152
Q

Meropenem

A

Tx: Antibacterial–mixed infections

Class: Carbapenem

Penicillin analog

Small penicillinase resistant B lactam

Spectrum: Very broad-Better against G-

Route: IV

SE:

  • Can enter CNS→Seizures
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152
Q

Alkylating agents

Names and mech.

A

Cyclophosphamide

Lomustine

Cisplatin

Mech

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth
  • Non specific
  • Inhibit non-replicating tumor cells
  • Worry about extravasation-leakage into surrounding tissue
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154
Q

Iomitapide

A

Tx: Hyperlipidemia

Mech: Inh assembly of VLDL in liver

Apolipoprotein+cholesterol→(X)→VLDL

Enzyme for assembly is also a transporter

SE: hepatotoxicity

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155
Q

Other NSAIDs

A

_Pyr_os _ne_ed _e_xcess _f_ire

_Pyr_oxicam _n_abumetone _e_todolac -_f_enac

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156
Q

Rituximab

A

Tx: Chronic lymphocytic leukemia and RA

Mech: vs CD20

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156
Q

Etoposide

A

Tx: Cancer

Mech: Inhibits topoisomerase II→unrepairable DNA breaks

Natural product

  • You know its a topoisomerase inhibitor but which one?*
  • Add the first letter of one vs two to the front. If it makes sense it’s correct*
  • Tetoposide vs oetoposide*
  • **T-etoposide so topoisomerase Two***
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157
Q

Clemastine

A

First gen H1 blocker

Tx: Motion sickness, sedative

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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158
Q

Succinylcholine

A

Direct nicotinic agonist

Antinicotinic agent-Depolarizing neuromuscular blocker

Long duration of action compared to acetylcholine

Initially activates receptor, eventually muscle hyperpolarization then paralysis

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160
Q

Vigabatrin

A

Tx: Partial seizures

Mech: Act GABA

ViGABAtrin

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161
Q

Linaclotide

A

GI Drug

Cathartic–Secretion enhancer

Mech: Activate guanylate cyclase

Increase Cl secretion in stomach

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161
Q

Methotrexate

A

Tx: DOC early tx of RA

Used more as immunosuppressant than anti-cancer drug

DMARD-Disease modifying anti-rheumatic drug

Actually stops progression of RA rather than just treat symptoms

Mech:

  • Analog of Folic Acid
  • Inh. enzyme: Dihydrofolate reductase
  • PABA→Folic acid⇒Dihydrofolic acid⇒tetrahydrofolic acid
    • ⇒ indicate where DHFR works
  • Inh. mammalian cell division
    • Inh. lots of folic acid dependent processes, especially in cells w/ rapid turnover (at high doses):
      • GI
      • Fetal development
      • Blood cells
    • Immune cells more susceptible than above though
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161
Q

More selective B blockers

A

Metoprolol

Acebutolol

Atenolol

Betaxolol

Nebivolol

SE:

  • Fewer CNS effects
  • Bradycardia
  • Fatigue w/ exercise
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163
Q

Prednisone

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Not inhaled

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
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164
Q

Penicillin V

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Narrow spectrum: G+

Route: Oral

Natural penicillin

Absorption unpredictable

Destroyed by B lactamase

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • B lactam ring may inh. GABAergic neurons
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165
Q

Pregabalin

A

Tx: Partial seizures

Mech: Acts on Ca channels

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166
Q

Prednisone

A

Tx: Cancer-leukemias and lymphomas

Mech: Inh. immune system fxns (refer to other lecture)

SE: lots of them

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168
Q

Ranitidine

A

H2 blocker

Does not cross BB barrier

Effects:

  • Blockade of H2 receptors→Decrease H secretion
  • Histamine required to stim. acid secretion from parietal cells
168
Q

Demecarium

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

169
Q

-amivir

A

Zanamivir

Oseltamivir

Antiviral agent

Tx: Influenza A+B virus (RNA virus)

Virus leaves cell and is attached by tether of neuraminic acid

Release of virus requires neuraminidase

Mech: Neuraminidase inh.

So virus cannot be released from cell and spread

SE:

  • Nausea
  • Diarrhea
  • Psychosis
  • Hallucinations
  • Zanamivir is a powder that must be inhaled so asthma issues

Only shorten influenza by about a day

170
Q

Dioctal sodium sulfosuccinate

A

GI Drug

Cathartic–Stool softener

Detergent

Mech: Emulsifies contents of colon

171
Q

First Generation H1 blockers

A

Diphenhydramine

Clemastine

Chloropheniramine

Hydroxyzine

Promethazine

Tripelennamine

173
Q

Acetic acid derived NSAIDs

A

Double A (Aaron) slobbers into titties

Acetic Acid: Sulindac indomethacin tolmetin

175
Q

Recombinant interferon alpha

A

Antiviral agent

Tx: Hepatitis virus (esp Hep C)

Cytokine w/ multiple mech

Mech:

  • Immunostimulant
  • Inh. mRNA processing
  • Decrese viral synth

SE:

  • Fatigue
  • Flu-like symptoms
  • Depression
  • Hypertensino
  • Retinopathy
  • Myelosuppression→fewer platelets, granulocytes, etc.
177
Q

Codeine

A

Narcotic analgesic- narcotic analogs

Partial agonist-low anti-nociceptive effects

Given orally

Greater effect on coughing-anti-tussive effect

178
Q

Mometasone

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Inhalation

1st pass metabolism

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
179
Q

Endothelin blockers

A

“-entan”s

Tx of pulmonary arterial hypertension

SE:

  • Fetal damage
  • Testicular atrophy
  • Hepatic toxicity
180
Q

“-fenac”s

A

diclofenac

bromfenac

Nepafenac

NSAID

181
Q

Gramicidin

A

Antibacterial agent

Mixture of 3 diff peptide AB

Mech: forms pores in bacterial CM

Route: topical

NEVER give IV–toxic

Spectrum: G+

182
Q

Cidofovir

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Prodrug-converted by host kinase

Used if resistance has occured so that host cells convert prodrug

SE: Renal damage

183
Q

Aspirin pharmacodynamics

A

Act on specific enzymes

184
Q

Cilostazol

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Inhibits phosphodiesterase

Inh. enzyme that breaks down cAMP

Increased cAMP→Decrease platelet agg.

186
Q

(Apo)morphine

A

Emetic–central stimulant

Mech: Stimulates DA sites in CTZ

187
Q

Diazepam

A

Tx: Seizures

Class: Benzos

Mech: GABA

IV to treat status epilepticus

188
Q

Lithium

A

Tx: Mania

Used prophylactically–5-7 day onset

Cheap-can’t patent it

Given orally

Low TI=2

Mech:

  • Alter glutamate metabolism
  • Decrease NE release
  • May alter 5HT

SE:

  • Short term
    • Tremors
    • Increase thirst
    • Increase urine prod. (block effects of ADH)
    • Edema
    • Weight gain
    • Nystagmus
  • Long term
    • Renal damage
    • Hypothyroidism

Toxicity:

  • Nausea
  • Delirium
  • Coma
  • Dangerous w/ kidney disorders
190
Q

Mirtazapine

A

Antidepressant

192
Q

Naphazoline

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

194
Q

Nafcillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

B-lactamase resistant

Narrow spectrum: G+

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons

NAFcillin=Not AFfected by penicillinase

195
Q

Dronabinol

A

Anti-emetic–THC derivative

Mech: Bind cannabinoid receptor

SE: Increased appetite

196
Q

Malathion

A

Insecticide-cholinergic agonist

Irreversible AChE inhibitors

198
Q

Minoxidil pharmacodynamics

A

Agents that act on ion channels

198
Q

“-kinase”s

A

Streptokinase

Urokinase

Tx: Thrombolytic agent

(dissolve formed clots)

Mech:

  • Urine plasminogen activator=Enzyme activator
  • Plasminogen→plasmin
  • Plasmin:
    • hydrolyzes fibrin
    • degrades fibrinogen
    • degrades factors V and VII

Route: IV

SE: May prolong bleeding time

199
Q

Terbinafine

A

Class: Antifungal

Mech: Inh. squalene epoxidase→inh. ergosterol synth

Inh. ergosterol synth→Increase in sqalene

Route: Systemic

Not well absorbed on skin

Most excreted unchanged

Metabolized and inhibits P450

SE:

  • Headache
  • Inhibit P450
  • Allergies
    • Derived from penicillium mold
  • Liver damage
  • SquaTer*
  • inh. Squalene epoxidase TERbinfine*
200
Q

Antipsychotic drugs used to treat mania

A

Phenothiazine

Haloperitol

Benzos

201
Q

Lispro

A

Tx: Diabetes

Designer insulin

Short acting (2-5 hrs)

203
Q

-fungin

A

Caspofungin

Micafungin

Anidulafungin

Antifungal agent

-cidal

Mech: Inh. synth of fungal CW component

Enzyme inhibitor

Route: Slow IV

Not readily absorbed

SE:

  • Rash
  • Fever
  • Fetal Damage
204
Q

Sulindac

A

NSAID

Acetic acid derivative

206
Q

Esmolol

A

Tx: arrythmias (Class II)

Mech: B1 blocker

More rapid onset of action

SE:

  • Bradycardia
  • Hypotension
  • B2 effects-asthma
207
Q

St Johns Wort

A

Uses:

  • Mild depression
  • anxiety

As eff as standard anti-dep.

Mech: Inh. reuptake of NE, 5HT, DA

SE:

  • Phototoxicity
    • Other allergic rxns
  • In breast milk→lethargic baby
  • Induces P450
    • Wafarin
    • BC
  • Anti-depressant interactions
208
Q

Olestra

A

Fake fat

SE: Butt leakage

209
Q

Desvenlafaxine

A

Third Generation Antidepressant

Mech: SNRIs

Inhibit reputake of 5HT and NE

*Third generations have the -faxine drugs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation

*SE same as 2nd gen +cardio stim.

211
Q

Gemfibrozil

A

Tx: Hyperlipidemia

Mech: Bind to PPAR-peroxisome proliferation acting receptor

Effects

  • Increase transcription of LPLase
  • Decrease VLDL
  • Decrease Trig.

SE:

  • GI upset-nausea, vomiting
  • Can displace warfarin from plasma binding sites
212
Q

-sala-

A

Sulfasalazine

Mesalamine

Olsalazine

Balsalazide

Tx: IBS–Salicylates

Mech: Decrease PG synth

Online it says mech is unclear–may not be the same as aspirin

Not systemically absorbed-like a topical drug for the stomach

SE:

  • Diarrhea
  • Take 3-5 weeks to work
212
Q

Itraconazole

A

Antifungal triazole

-static

Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase

So inh. ergosterol synth

SE:

  • Strongest effect on human P450 of the triazoles
  • Worsen CHF or arrythmias

_I_traconazole is the strongest _I_nhibitor of P450

ItrAConazole→Arrythmias or CHF

213
Q

atracurium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

214
Q

Non specific B1 and B2 blockers

A

Propanolol

Timolol

Levobunolol

Certeolol

Metipranolol

215
Q

Leuprolide

A

Tx: Cancer (prostate)

Mech: Activates GnRH receptor

Initially increases test synth, but eventually down regulates it

Used in comb. w/ other drugs

Lou Ferrigno was a pro bodybuilder w/ _AR_nold–initially boosted test. synth but eventually downregulated it

Leu-pro-lide _A_ctivates GnRH _R_eceptor–initially boosted test. synth but eventually downregulated it

215
Q

Imipramine

A

First generation antidepressant

Tricyclic antidepressants

Mech: Inhibit NE reuptake

Act on multiple receptors

SE:

Most likely to cause SE
Sedation
Weight gain
Anticholinergic effect (dry eyes, dry mouth, constipation)
Cardiovascular effects

Arrythmias
Drop in BP (alpha1 block)
Orthostatic hypotension

217
Q

Minoxidil

A

Acts directly on smooth muscle

Prodrug

Opens K channels in arterial smooth m, increased efflux→hyperpolarization

Very refractory px

SE:

  • Hypertrichosis-hair growth
    • Rogaine
    • Discontinuation→hair loss
    • Edema and pericardial effusion→cardiac tamponade
      • Fluid in sac around heart
218
Q

Imitinib pharmacodynamics

A

Act on specific enzymes

218
Q

Disulfiram

A

Inhibits acet.DH→buildup of acetaldehyde

Get severe hangover right away

219
Q

Fondaparinux

A

Tx: Anticoagulant

Synthetic heparin like drug

T1/2=17 hrs

Acts only on Xa

Can cross placenta

Can’t bind protamine

Given SubQ

220
Q

Protease inh.

A

-navir

Antiviral agent

Tx: HIV

Mech: Protease inh.

Prevent formation of active viral proteins from their peptide precursor

Most inh. P450

Some are absorbed poorly via oral route and 18 capsules must be taken/day

Ritonavir is most potent known P450 inh so it is given w/ the poorly absorbed protease inh to avoid taking so many

Ritonavir given w/: SALTD

  • Saquinavir
  • Atazanavir
  • Lopinavir
  • Tipranavir
  • Darunavir

SE:

  • Alter fat distribution
    • Loss of fat in face and limbs
    • Gain fait in gut, chest, and back
  • Increase diabetes
  • Some have sulfur groups→allergies
    • Tipranavir
    • Fosamprenavir
222
Q

Omalizumab

A

Tx: Asthma

Mech: Blocks IgE receptor

Receptor blocker

Route: Injection–like all monoclonal antibodies

223
Q

Rocuronium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

Most common one

223
Q

Nifedipine pharmacodynamics

A

Agents that act on ion channels

224
Q

What are the short acting designer insulins?

A

Regular human insulin

Lispro

Aspart

Glulisine

2-5 hrs

225
Q

Nabilone

A

Anti-emetic–THC derivative

Mech: Bind cannabinoid receptor

SE: Increased appetite

226
Q

-methasone

A

Dexamethasone

Betamethasone

Immunosuppressive potency=15

Relative minerallocorticod activity=

Duration: 36-54hrs

227
Q

Enfuvirtide

A

Tx: HIV

Mech: binds to specific site on virus that binds to target

Fusion inhibitor

SE: Insomnia

228
Q

Disopyramide

A

Tx: Arrythmias (Class Ia)

Mech: Na channel blocker

  • Even stronger antivagal effects (than quinidine)

SE:

  • Antimuscarinic effects (opposite of DUMBBELS)
    • Wouldn’t use w/ glaucoma pts
229
Q

Prednisone

+

Prednisolone

A

Immunosuppressive potency=4

Relative minerallocorticod activity=.25

Duration: 18-36hrs

Prednisone is a prodrug:

  • Must be metab by P450 (in liver)
  • Not effective topically
231
Q

alpha-methyl tyrosine

A

Tx of pheochromocytoma

Central and peripheral effects

Inhibits tyrosine kinase–preventing synthesis NE and epi

232
Q

Adefovir

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE: Liver and renal damage

Discontinuation→Increase hepatitis symptoms

232
Q

Sotalol

A

Tx: arrytmhias (Class III)

Mech: K+ channel blocker

Also a beta blocker

232
Q

Methylnaltrexone

A

Narcotic analgesic antagonist

Opiate receptor blocker

233
Q

Deferoxamine

A

Tx: Acute iron OD

Mech: Iron chelator

De-Fer-oxamine

_De_toxes _Fer_rous overdose

234
Q

Amiodarone

A

Tx: arrytmhias (Class III)

DOC for cardiac arrest–most effective anti-arrythmic

Mech: K+ channel blocker

Acts like all 4 classes of anti-arrythmic

SE:

  • Potentially fatal pulmonary fibrosis
    • Replaces lung tissue w/ fiber composites
  • Liver damage
  • Corneal deposits-optic neuritis
  • Deposits in skin-blue/gray skin coloration
  • GI upset

*Iodine responsible for some deposits

236
Q

Meclizine

A

Anti-emetic–Antihistamine

Mech: Block H1 receptor

SE: Anticholinergic effects

237
Q

Which antihistamines are used as anti-emetics?

A

Diphenhydramine

Dimenhydramine

Meclizine

Cyclizine

238
Q

Valerian

A

Uses: Sedative

Mild sedative effect

Mech: Increase GABA

SE:

  • Hepatotoxicity
  • Dont use w/ anti-dep
238
Q

Other tx of bipolar

A

Most are antiseizure:

  • Valproic acid
  • Carbamazepine
  • Limotripene

Acetazolamide

Aripripazole-anti-psychotic

240
Q

Calcium channel blockers

A

“-ipine”s

Inhibit Ca influx into vascular smooth m

Prevent vasoconstriction

SE:

  • Heartburn
  • May worsen heart failure
241
Q

Ibuprofen

and other -pro-

A

Naproxyn

Fenoprofen

Ketoprofen

Flurbiprofen

Oxaprozin

Suprofen

Tx: Analgesic, anti-inflam

Mech: Inh COX

Propionic acid derivative

242
Q

Sofosbuvir

A

Antiviral agent

Tx: Hepatitis virus (esp Hep C)

Mech: Inh HCV RNA dep RNA pol

243
Q

Third Generation antidepressants

A

Venlafaxine

Desvenlafaxine

Duloxetine

Milnacipram

Mech: SNRIs

Inhibit reputake of 5HT and NE

*Third generations have the -faxine drugs

SE:

  • GI upset
  • Nausea
  • Insomnia
  • Headache
  • Decreased libido
  • Cardiovascular stimulation

*SE same as 2nd gen +cardio stim.

244
Q

Lomustine

A

Tx: Cancer

Mech: Alkylating agent

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth

Prodrug given IV

245
Q

Angina definition and general tx methods

A

Not enough BF to heart

Causes chest pain (m becomes anoxic)

We usually have chest pain after we work out b/c we need more O2

But if at rest it is unstable angina

Tx by increasing BF or decreasing O2 demand

Tx:

  • Behavioral
    • Diet
    • Exercise
      • Creates collateral circulation (more blood vessels) in heart
    • Stop smoking
  • Drugs
247
Q

Isoproterenol

A

“-nol”s and “-rol”s

Tx: Asthma

Bronchodilator–DOC for short term relief

Mech: More specific B2 agonist than epi. but B1 effects

Kinetics: Shorter T1/2

SE:

  • Tremors
  • Tachycardia
  • Heart palpitations

Has been supplanted by more specific B2 agonists

247
Q

Vorapaxar

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Thrombin receptor blocker on platelet

SE: Use carefully w/ pts w/ history of intracranial bleeding

249
Q

Ipratropium

A

*“-trop-“ like atropine *

Tx: Asthma

Bronchodilator

Mech: Cholinergic blocker

Analog of atropine

Clinical use: Mainly for COPD but some use for asthma

Kinetics:

  • Inhaled–slower onset though (10 min)
  • Not well absorbed
  • Peak effect in hours
  • Weaker than B-blockers

SE: Anti-cholinergic effects​

Contraindications:

  • Urinary retention
  • Open angle glaucoma
250
Q

Doxorubicin

And other rubicins

A

Tx: Cancer

Mech: Intercalates w/ DNA→blocks DNA and RNA synth

Produces free radicals→break down DNA strands

Class: Antibiotic (produced by microorganisms)

SE:

  • Can cause heart m. degeneration
    • Irr. due to free radicals
  • Fall in love w/ Ruby but she’s a free radical and breaks your heart.*
  • Rubicin. Causes free radicals–> heart damage. Breaks DNA*
252
Q

Ketoconazole

A

Antifungal imidazole

Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase

So inh. ergosterol synth

SE:

  • Nausea
  • GI upset
  • Hepatic toxicity
  • Inh. human P450-Strongest inh. of the conazoles
  • Decrease in adrenal and gonal steroid synth
    • Decrease cortisol (tx of Cushing’s)
    • Decrease test. (tx of prostate cancer)
  • Ket…ocon..azole*
  • Ket azole=cat asshole*
  • So GI, nausea, and prostate cancer tx*
  • And cat’s have 9 lives so they LIVEr forever…l_iver tox_*
252
Q

Gabapentin

A

Tx: Partial seizures

Mech: Act GABA

GABApentin

252
Q

Tacrine

A

Indirect cholinergic agonist

Alzheimer’s tx

254
Q

Verapamil

A

Tx: Arrythmias except vent. arrythmias (class IV)

Mech: Ca channel blockers

Increase refractory period

255
Q

Imitinib

A

Tx: Chronic myelogenous leukemia (CML)

Mech: Kinase inh.

In CML a gene codes for a kinase that shuts off apoptosis

So cells keep multiplying and don’t die=cancer

Imitinib inhibits the kinase so that apoptosis occurs again

Orally

SE: Edema (only a few SE)

257
Q

Infliximab pharmacodynamics

A

Act on specific enzymes

258
Q

Kola nut

A

Caffeine

Increased HR

Insomnia

260
Q

Posaconazole

A

Antifungal triazole

-static

Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase

So inh. ergosterol synth

SE:

  • Less effect on human P450 (triazole vs imidazole)

Posaconazole is sucha pussy, it hardly inhibits our P450

261
Q

Imipenem

A

Tx: Antibacterial–mixed infections

Class: Carbapenem

Penicillin analog

Small penicillinase resistant B lactam

Spectrum: Very broad-Better against G+

Route: IV

SE:

  • Can enter CNS→Seizures
  • Metabolized in kidney to nephrotoxic product
    • Given w/ cilastatin which inh. enzyme that produces toxic product
263
Q

Abciximab

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Fibrinogen receptor blocker on platelet (GPIIB/IIIA receptor)

Monoclonal antibody

Clinical use: Decrease white thrombi

Used for coronary operation

Route: IV

SE: Thromobocytopenia

264
Q

Phenoxybenzamine

A

Adrenergic antagonist

alpha1 receptor blocker

Tx: hypertension

265
Q

Delavirdine

A

Antiviral agent

Tx: HIV

Mech: bind to non active sites and Inh reverse trans

Not competetive inh.

Not as effective

1st gen NNRTI

SE

  • Hepatotoxicity
  • Stevens Johnson syndrome
  • P450 inh.
266
Q

Chlorpheniramine

A

First gen H1 blocker

Tx: Does not cause as much sedation

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
267
Q

Isocarboxazid

A

Antidepressant-MAO inhibitor

Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)

Kinetcs: Slow onset

Toxicity:

Insomnia
Agitation
Hallucination
Seizure
Liver toxicity
Weight gain
Hypotension
Great increase in likelihood of suicide in children

Drug interactions:

Indirect acting amines→Hypertensive crisis

Some foods contain tyramine (smoked foods, aged cheeses, wine)

268
Q

Acarbose

A

Rosiglitazone

Pioglitazone

Tx: Diabetes

Glucose abs. delayers

Mech: Inh. alpha glucosidase

Prevents breakdown of complex carbs in gut

SE:

  • Unabsorbed carbs ferment in gut
    • Cramps
    • Diarrhea
    • Flatulence
  • A-carb-ose*
  • No-carb-abs.*
270
Q

Buproprion

A

Antidepressant

271
Q

Aztreonam

A

Antibacterial

Class: Monobactam

Route: IV or IM

Not affected by lactamases

Spectrum: Aerobic G- organisms

Not cross reactive w/ allergic pts

SE:

  • Seizures
272
Q

Compazine

A

Anti-emetic

Mech: DA blocker

*Related to anti-psychotic drugs *(phenothiazine)

SE: Extrapyramidal effects

273
Q

Thiazide diuretics mechanism

A

Inhibits Na+ transport out of the DCT. H20 follows and both are excreted

High TI
works w/in 2 hours

274
Q

Angiotensin receptor blockers

A

“-Artan”s

SE:

  • Decrease secretion of aldosterone
  • Fetal abnormalities
    • All agents that alter angiotensin system
    • Pregnancy risk X
275
Q

-floxacin

A

Antibacterial agent

Mech:

  • Inh topoisomerase II (DNA gyrase)
  • Inh topoisomerase IV

No effect on mammalian topoisomerase

SE:

  • May damage developing cartilage
    • Not for children or pregnant women
  • Tendonitis–achilles tendon rupture
  • Phototoxicity (drug in skin responds to sunlight)
  • May worsen myasthenia gravis

Spectrum: Broad–G+,G-, Acid fast

276
Q

Bran

A

GI Drug

Cathartic–Bulk adding agent

Mech: Like eating fiber

277
Q

Cascara

A

GI Drug

Cathartic–Gastric Irritants

Mech: Stimulate gastric nn

Increase motility

Decrease electrolyte secretion into gut

SE:

  • Nephritis
  • Liver damage
278
Q

Hydroxychloroquinone

A

Immunosuppressant

Mech:

  • Taken up by macs and conc. in mac lysosomes
  • Interferes w/ mac. processing of antigens (1st step in immune process)

Toxicities:

  • GI fxn
  • Dermatitis
  • Irr. retinal damage
    • Retinal changes and visual disturbances may progress even after discontinuation
279
Q

Bethanechol

A

Direct muscarinic agonist

280
Q

Antifungals for ringworm

A

Tolfnaftate

Ciclopirox

Terbinafines and other “fines”

Route: Topical

282
Q

Echothiophate

A

Indirect cholinergic agonist

Lasts for 100s hours

Phosphorylates AChE

284
Q

-glitazone

A

Rosiglitazone

Pioglitazone

Tx: Diabetes

Insulin enhancers

Mech: Act. PPAR→

Increased insulin receptor response

Increased # insulin receptors

Increased glc uptake by cells

SE:

  • Wt gain
  • Edema
  • Fractures of arms and legs
  • Macular edema
  • Cardio problems
    • MI
285
Q

Atropine

A

Antimuscarinic agent

Blocks muscarinic receptor

Lasts 7-10 days

287
Q

Clindamycin

A

Antibacterial agent–lincosamide

Mech: like erythromycin-inh. translocation

SE: Severe superinf. w/ C. dificile

Targets:

  • Severe anaerobic infections (penetrating gut wound)
  • Dental prophylaxis in pts w/ heart valve problems
287
Q

Ciclesonide

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Inhalation

1st pass metabolism

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
288
Q

Diphenhydramine

A

First gen H1 blocker

Tx: Sedative, motion sickness

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
290
Q

Alpha-methyl DOPA

A

Central alpha-2 agonist

Prodrug: metabolized to alpha-methyl NE

SE:

Depression

Drowsiness

Dry mouth

Impaired Ejac.

Hepatic dysfunction

291
Q

Alfentanil

A

Narcotic analgesic- synthetic

500-600x stronger than morphine

292
Q

Sucralfate

A

GI drug-Enhance mucosal defense

Aluminum salt

Tx: Ulcers

Mech: Complex that becomes viscous and binds to damaged mucosa when exposed to acid

SE:

  • Constipation
  • Excess Al absorption

Contraindication: H+ depleters (PPI or antacids)

SucrALfate=ALuminum salt→Excess Al

Sucralfate=sucrose=sticky…so this sticks to damaged mucosa

293
Q

Aluminum hydroxide

Al(OH)3

A

Antacid

Speed-slow

Duration-long

Neutralizing-low

SE:

  • Constipation
  • Adsorbs drugs
  • Loss of phosphate
  • Al toxicity
293
Q

Tobramycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

295
Q

(Hydro)Chlorothiazide

A

Inhibits Na+ transport out of the DCT. H20 follows and both are excreted

High TI
works w/in 2 hours

Other effects:

Cause direct vasodilation
Often initial drugs for hypertension
Decrease Ca excretion

Side effects:

  • Hypokalemia
    • Lose K due to Na-K exchanger
  • Increase in serum LDL and triglycerides (atherosclerosis)
  • Decrease uric acid secretion→gout
  • Inhibit insulin secretion
  • Contain sulfur ions-may cause allergens
296
Q

Metformin

A

Tx: Diabetes

Insulin enhancers

Mech: Act. protein kinase→

Increased glc abs. by muscle

Decreased glc production by liver

SE:

  • Lactic acidosis (potentially fatal)
  • Weight loss due to anorexia
  • George Foreman was an American Professional (Kick)boxer *
  • Metformin Activates Protein Kinase*
  • He worked out so hard he had lactic acidosis and had to be anorexic to make his weight class*
298
Q

Cilastatin

A

Given w/ impenem

Prevents nephrotoxic product by inh. enzyme

299
Q

Sirolimus

A

Tx: Transplant, psoriasis

Mech: Bind to FK binding protein

inh. kinase required for binding of IL-2 induced transcription factors to DNA→decreased cytokine production

Often used in combination w/ glucocorticoids

SE:

  • Some renal toxicity
    • Less than tacrolimus
    • Synergistic effect w/ used in comb w/ many immunosupp.
  • Some lung toxicity

Metab by P450

  • What else binds to FK protein? Tacrolimus*
  • Tacrolimus: Inh calcinuerin phosphatase*
  • Sirolimus/Everolimus: Inh kinase*
300
Q

Agents that activate B2 receptors

A

“Nols and rols”

Metaproterenol

Terbutaline

Fenoterol

Albuterol

Tx: asthma

Causes bronchodilation

302
Q

Alvimopan

A

Tx: Gastroparesis

prokinetic agents–agents that increase stomach emptying rate

Mech: Blocks opiate receptor in gut but not anywhere else

Blocks constipation due to post op opioid use

303
Q

Flutamide

and other “lutamides”

A

Tx: Cancer (prostate)

Mech: Blocks androgen receptor

Androgen receptor inside cell

Some tumors are hormone dependent

  • Careful:*
  • Flunomides-inh dihydroorate DH*
  • Flutamides-block androgen receptor*
304
Q

What induces the release of NE from nerve terminals?

A

Indirect acting amines:

Amphetamine, methamphetamine

Tyramine

Phenylpropanolamine

Pseudoephedrine

305
Q

-tidine

A

GI drug

Decrease acid secretion

Mech: H2 receptor blockers

SE:

  • Confusion in elderly
  • Bradycardia

Cimetidine:

  • Inh. P450
    • Prevent synth of test.
    • Anti-androgenic
      • Cause gynecomastia
306
Q

Mipomersen

A

Tx: hyperlipidemia

Antisense oligonucleotide

Mech: Binds to mRNA of ApoB

Prevents Apo from being synth

*(Apolipoprotein)*+cholesterol→VLDL

Must be given by injection

307
Q

Duloxetine

A

Third Generation Antidepressant

Mech: SNRIs

Inhibit reputake of 5HT and NE

*Third generations have the -faxine drugs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation

*SE same as 2nd gen +cardio stim.

308
Q

Magnesium hydroxide

Milk of magnesia

A

Antacid

Speed-slow

Duration-medium

Neutralizing-high

SE:

  • Laxative
  • Some Mg toxicity
309
Q

Zonisamide

A

Tx: Partial seizures

Mech: Inh. Na

310
Q

Carbamazepine

A

Tx: DOC for partial seizures

Mech: Inhibits on Na channels

Toxicity:

  • Blurred vision + diplopia
  • Drowsiness
  • Fetal defects-spina bifida
  • Aplastic anemia (abnormality of RBC)
  • Induces P450
312
Q

Eribulin

A

Tx: Cancer

Mech: inh. microtubules-prevents mitosis, causes apoptosis

Fully synthetic

312
Q

Digoxin

A

Tx: CHF

Class: Cardiac glycoside

  • Naturally occuring (foxglove and milk weed)
  • Produced as protection for plant

Route: orally

Kinetics: long T1/2

Mech:

  • When m stimulated, small influx of Ca→causes release of Ca into cell from SR→contraction
  • In order for m to relax after contraction, Ca must be removed (Na and Ca pumped out, K pumped in)
  • Digoxin inhibits NaK-ATPase
    • Na remains high in cell→prevents loss of Ca
    • High conc of Na inhibits the Na-Ca exchanger
  • Net result: Ca remains high
    • High Ca→greater contractility

Effects:

  • Increases duration of contractile response
  • Stimulates vagus n
  • Anti-arrythmic effects

SE:

  • Cardiac arrythmias
  • CNS effects
    • Yellow-green tinting of vision
    • Hallucinations
    • Activation of chemoreceptor trigger zone→severe nausea
  • Effects enhanced in hypokalemia
    • Cardiac glycosides bind and K site
    • If less K outside of cell, more effective

Digoxin poisoning treated w/ anti-digoxin anti-bodies

314
Q

Lidocaine

A

Tx: arrythmias (Class Ib)

*also LA

Mech: Na channel blocker

Route: Given IV

Kinetics: First pass effect

Toxicity: Low

SE:

  • Less likely to cause arrythmias but can enter CNS
    • Tremors
    • Seizures
315
Q

MgSO4

A

GI Drug

Cathartic–Osmotic agent

316
Q

Neostigmine

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

317
Q

Rufinamide

A

Tx: Partial seizures

Mech: Inh. Na

318
Q
A
320
Q

“-xaban”s

A

Tx: Anticoagulant

Mech: Factor Xa inhibitor

Think -xaban=_Ban_s factor Xa

Route: Oral

Kinetics: Rapid onset

SE: Bleeding after spinal tap or spinal injurty

321
Q

Chloramphenicol

A

Antibacterial agent

Mech: inh. peptidyl transferase

SE:

  • Inh. P450
  • Can cause aplastic anemia
  • Gray baby syndrome
    • Metabolized by a phase II enzyme that is not active in newborns.
    • Can’t metabolize it→baby turns blue and circulatory system inhibited
322
Q

Aspirin

A

Tx: Anticoagulant

Mech: Platelet inhibitor

COX (enzyme) inhibitor

Inhibits TXA2 synth

Decreases platelet aggregation

324
Q

Infliximab

A

Tx: IBS

Mech: Binds TNF alpha

326
Q

High Ceiling diuretics clinical use

A
  • Pts who dont respond to thiazides
  • Life threatening edema (pulmonary or cerebral)
  • Compromised renal fxn
327
Q

Heparin pharmacodynamics

A

Act on specific enzymes

328
Q

Escitalopram

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

329
Q

Orlistat

A

Tx: Hyperlipidemia

Mech: Inh GI and pancreatic lipase

Decrease fat absorption from gut

SE: Loose stool

331
Q

Paclitaxel

and other “-taxel”s

A

Tx: Cancer

Mech: Forms abnormal microtubules

Natural-from western yew tree. But now purely synthetic

”-_t_axels” make _t_errible _t_ubules

332
Q

Acetazolamide

A

Carbonic anydrase inhibitors (enzyme inhibitor)

Inhibits HCO3- resorption in PCT

Short term effect

Not used primarily as diuretic

Other uses:

  • Treats open angle glaucoma
  • Mountain sickness (by lowering CSF volume)
  • Epilepsy
    • May be due to pH in CNS
333
Q

Rifampin

A

Antimycobacterial agent

Antibacterial agent

Mech: Inh DNA dep. RNA polymerase

-cidal

SE:

  • Hepatic toxicity
  • Red color in all body fluids
  • Induces P450–very strong
    • Can metabolize BC!

Rifampin=red

Will metabolize BC (induce P450) so the sperm will LIVEr

334
Q

Scopolamine

A

Anti-emetic–anti-cholinergic

Mech: Block muscarinic receptor

Route: Patch

SE:

  • Dry
  • Drowsy
  • Etc.
336
Q

Tiagabine

A

Tx: Partial seizures

Mech: Act GABA

Tiagabine

337
Q

Golimumab

A

Tx: RA, Ulcerative colitis, psoriatic arthritis

Immunosuppressant

Mech: Binds TNF

338
Q

Natalizumab

A

Nata-li-zu-mab

MAb affecting immune sys. from humanized source

Immunosuppressant

Tx: Chron’s + MS

Mech: Binds to alpha integrin binding site on CD4 (and other immune cells)

Not really a receptor but a “binding site”

SE:

  • Linked w/ progressive multifocal leukoencephalothopy (PML)
    • Fatal viral disease of CNS

_Nat_ty’s give you the beer shits

_Nat_alizumab=Chron’s

natALIzumab-binds ALpha Integrin binding site

339
Q

Torsemide

A

High ceiling diuretics

Orally or parenterally

Mech of action:

Inhibit Na and Cl resorbtion from Asc. loop of Henle

More efficacious than thiazides

Clinical use:

Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn

Side effects:

Dehydration
Hypokalemia

—Used w/ K supplements or K sparing diuretics

Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents

340
Q

Dactinomycin

A

Tx: Cancer

Mech: Intercalates w/ DNA and interferes w/ mRNA synth

341
Q

Oxycodone

A

Narcotic analgesic- semisynthetic

Partial agonist-available in oral form as oxycontin

0.5x as strong as morphine

342
Q

“-parin” drugs excluding heparin

A

Enoxaparin

Dalteparin

Tx: Anticoagulant

Low molecular wt heparins-Partially purified heparin

Longer T1/2=4 hrs

More effect on Xa than thrombin

Less osteoporosis and HIT

More predictable dose-response

(Smaller so don’t bind as readily to lots of proteins)

More expensive

Not readily reversed by protamine sulfate

SE: spinal hematoma in pts who have had spinal tap or anesth.

343
Q

Prazosin

A

Adrenergic antagonist

alpha1 receptor blocker

Tx: hypertension

345
Q

Reserpine

A

Tx of HT

Central and peripheral effects/effector of post-ganglionic neuron

Causes depletion of post ganglionic neuron nt (NE)→ No vasoconstriction

SE: depression, drowsiness, diarrhea

347
Q

Propranolol pharmacodynamics

A

Agents that act on cell membrane receptors

348
Q

Ethacrynic acid

A

High ceiling diuretics

Orally or parenterally

Mech of action:

Inhibit Na and Cl resorbtion from Asc. loop of Henle

More efficacious than thiazides

Clinical use:

Pts who dont respond to thiazides
Life threatening edema (pulmonary or cerebral)
Compromised renal fxn

Side effects:

Dehydration
Hypokalemia

—Used w/ K supplements or K sparing diuretics

Increased Ca excretion→Hypocalcemia
Decreased uric acid excretion→gout
Auditory nerve damage esp. if used w/ other ototoxic agents

349
Q

Methylcellulose

A

GI Drug

Cathartic–Bulk adding agent

Mech: Like eating fiber

349
Q

Palivizumab

A

Antiviral agent

Tx: RNA virus (RSV)

Mech: vs antigenic site of RSV–blocks fusion of virus w/ target

Only used prophylactically

349
Q

Tolmetin

A

NSAID

Acetic acid derivative

351
Q

Acyclovir

A

Antiviral drug

Tx: Herpes simplex and zoster

Mech: Incorporated into DNA and inh. viral DNA pol

Prodrug-must be phosphorylated by viral kinase

Only occurs in active cells

Much higher affinity for viral DNA pol

Route: IV and oral (not well absorbed though)

SE:

  • GI upset
  • Renal damage
  • CNS problems
    • Delerium when given IV
352
Q

Tiotropium

A

*“-trop-“ like atropine *

Tx: Asthma

Bronchodilator

Mech: Cholinergic blocker

Analog of atropine

Clinical use: Mainly for COPD but some use for asthma

Kinetics:

  • Inhaled–slower onset though (10 min)
  • Not well absorbed
  • Peak effect in hours
  • Weaker than B-blockers

SE: Anti-cholinergic effects​

Contraindications:

  • Urinary retention
  • Open angle glaucoma
353
Q

Naltrexone

A

Narcotic analgesic antagonist

Opiate receptor blocker

354
Q

“Osin”s

A

Alpha 1 blockers

Blocks alpha 1 receptor on vascular smooth m

Tx of hypertension and some specifically treat BPH

Based on the drugs he gave us:

**If it ends in -azosin its for hypertension**

**If it ends in just -osin its used for BPH**

SE

  • First dose effect-rapid drop in BP→orthostatic (postural) hypotension
    • Do not confuse w/ first pass effect
355
Q

Vortioxetine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

356
Q

Non-depolarizing neuromuscular blockers that are antinicotinic agents are derived from?

A

curare

356
Q

Omeprazole pharmacodynamics

A

Agents that act on transport systems

357
Q

-zolid

A

Linezolid

Tedizolid

Mech: Inh. binding of fmet (start codon) tRNA to P site

Prevents initiation of protein synth.

SE

  • Anemia
  • Pseudomembranous colitis
    • Will happen w/ any powerful AB b/c of C. dificile
359
Q

Tripelennamine

A

First gen H1 blocker

Tx: Sedative, local anesthetic effect

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
360
Q

Tissue plasminogen activator (TPA)

A

Tx: Thrombolytic agent

(dissolve formed clots)

Mech:

  • Urine plasminogen activator=Enzyme activator
  • Plasminogen→plasmin
  • Plasmin:
    • hydrolyzes fibrin
    • degrades fibrinogen
    • degrades factors V and VII

Route: IV

SE: May prolong bleeding time

361
Q

Detemir

A

Tx: Diabetes

Designer insulin

Long acting (24+ hrs)

Determined to get large (that a long time)

Detemir +glargine=long acting insulins

363
Q

Tofacitinib

A

-ib=inhibitor (often kinase inh)

Mech: Janus kinase inh.

  • Inh signal pathways of cytokines and ILs
  • Modifies effect of cytokines on gene exp
  • Prevents act. of signal transducers and activators of trans.

SE:

  • Increase infection
  • Increase malignancy
364
Q

Prazosin pharmacodynamics

A

Agents that act on cell membrane receptors

366
Q

Erythromycin

A

Tx: Gastroparesis

prokinetic agents–agents that increase stomach emptying rate

Mech: Acts directly on motilin receptor

Route: Oral but IV possible if oral is not

SE:

  • ototoxicity
  • pseudomemb. colitis
  • cardiac arrythmia
    • Especially if metabolism is inh by P450
  • Remember erythro is a macrolide*
  • Motiliy*
  • Arrythmias*
  • Cholesteric toxicity (liver tox)/Colitis*
  • Restricts P450*
  • Ototoxicity*
367
Q

Fenofibrate

A

Tx: Hyperlipidemia

Mech: Bind to PPAR-peroxisome proliferation acting receptor

Effects

  • Increase transcription of LPLase
  • Decrease VLDL
  • Decrease Trig.

SE:

  • GI upset-nausea, vomiting
  • Can displace warfarin from plasma binding sites
369
Q

Nitroglycerin pharmacodynamics

A

Act on specific enzymes

371
Q

Ethanol as a diuretic

A

Mech: decrease release of ADH

372
Q

Tranexamic acid

A

Tx: Hemostatic agent (enhance clotting)

Mech: Inhibits plasminogen activation

Enzyme inhibitor

Binds to plasminogen in plasma

374
Q

Cranberry

A

Uses: UTI

May inh. recurrent UTI

Not helpful for current inf.

Mech: Proanthrocyanadin prevents bact from binding to UT cells

May also acidify urine

SE:

  • Inh P450
375
Q

Cimetidine pharmacodynamics

A

Agents that act on cell membrane receptors

376
Q

Famciclovir

A

Antiviral agent

Tx: herpes simplex and zoster

Mech: prodrug converted to acyclovir analog

377
Q

Phenelzine

A

Antidepressant-MAO inhibitor

Mech: Irreversibly inhibits metab of NE and 5HT (via inhibition of MAO)

Kinetcs: Slow onset

Toxicity:

Insomnia
Agitation
Hallucination
Seizure
Liver toxicity
Weight gain
Hypotension
Great increase in likelihood of suicide in children

Drug interactions:

Indirect acting amines→Hypertensive crisis

Some foods contain tyramine (smoked foods, aged cheeses, wine)

378
Q

Pilocarpine

A

Direct muscarinic agonist

379
Q

Regular human insulin

A

Tx: Diabetes

Designer insulin

Short acting (2-5 hrs)

Afrezza is the inhaled form

380
Q

Digoxin

A

Emetic–central stimulant

Mech: Stimulates DA sites in CTZ

382
Q

Tamoxifen

A

Tx: Cancer

Mech: Blocks estrogen receptor

SE:

  • Cataracts
  • Retinal changes

Tammy is as big as an ox because her estrogen receptor is blocked. She’s obsessed w/ Ron Swanson and has CRazy eyes

Tamoxifen blocks estrogen receptor. Side effects associated w/ eyes: Cataracts and Retinal damage

383
Q

Amphotericin B

A

Class: Antifungal

  • Polyene antibiotic*
  • -cidal*

DOC of systemic mycotic inf.

Mech: Binds to ergosterol in fungal CM→pores→memb. leakage

Route: Slow IV (2-4 mnths) or intrathecal

Must be given w/ detergent b/c not soluble in H2O

Topical too

SE: “amphoterrible”

  • Impaired renal fxn
  • Fever, chills, vomiting, convulsions, severe headache
  • Anemia

Amph SE=ANF (sounds similar)

*Anemia, Nephro fxn impaired, Fever *

or

AMPHTERIC

Anemia

Muscular contractions

Pores in membrane

Headache

Temp increase

Emesis

Renal fxn impaired

IV or intrathecal

Chills

384
Q

Diazoxide

A

Acts directly on smooth muscle

Opens K channels→hyperpolarization

Inhibits insulin release from B cells in pancreas

385
Q

Lubiprostone

A

GI Drug

Cathartic–Secretion enhancer

Mech: Acts on PGE receptor

PGE1 derivative

Also acts on Cl channel in intestine

386
Q

Paroxetine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

388
Q

cytarabine

A

Tx: Cancer

Mech: Inh. DNA polymerase

Prodrug–Pyrimidine analog

389
Q

Ezetimibe

A

Tx: Hyperlipidemia

Mech: Blocks cholesterol transport

SE: Flatulence

391
Q

“-oxacillin”s

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

B-lactamase resistant

Narrow spectrum: G+

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons

OXacillin=OX is strong animal, resistant to penicillinase

392
Q

Polyethylene glycol

A

GI Drug

Cathartic–Osmotic agent

DOC for colonoscopy

394
Q

Efavirenz

A

Antiviral agent

Tx: HIV

Mech: bind to non active sites and Inh reverse trans

Not competetive inh.

1st gen NNRTI

SE

  • CNS- so some people crush it up and smoke it
    • hallucinations
    • memory loss
  • Rash
  • Smoke EFavirenz to get EFfed up*
  • hallucinations and mem loss*
395
Q

Phenobarbital

A

Tx: All seizures EXCEPT petit mal

Class: Barbituate

Mech: Act. GABA

SE:

  • Sedation
  • Induces P450
396
Q

Belatacept

A

Tx: Renal transplantation

Immunosuppressant

Mech: binds to CD80, CD86 receptor

Affects T cell activation

SE:

  • Increase malignancy

ABatacept CD80+86 receptors (Belatacept too)

Abatacept: RA Belatacept: Kidney trans.

397
Q

Fluticasone

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Inhalation

1st pass metabolism

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
398
Q

Miglitol

A

Tx: Diabetes

Glucose abs. delayers

Mech: Inh. alpha glucosidase

Prevents breakdown of complex carbs in gut

SE:

  • Unabsorbed carbs ferment in gut
    • Cramps
    • Diarrhea
    • Flatulence

Mig--litol

_Midg_ets (Mack) are little b/c they don’t absorb any carbs

399
Q

Chlorpropamide

A

Tx: Diabetes

Oral hypoglycemic agents

First gen sulphonylureas

Mech: K channel blockers

Block K channels on B cells →Increase Ca→Insulin secretion

Duration: 60+ hrs

Contra/Indications:

  • Do not use if you have renal or hepatic damage
  • Not overweight
  • Have some islet fxn

SE:

  • Hypoglycemia and hypoglycemia coma
    • More common in drugs w/ longer duration
  • Can be teratogenic
  • Can increase death due to cardiovascular problems
400
Q

Mannitol

A

Osmotic diuretic

Not metabolized

Given IV

Mech: Draws H20 into tuble and is excreted w/ H20

Clinical use: Used to maintain renal flow after renal damage

Decreases intracranial pressure

401
Q

Nefazodone

A

Antidepressant

402
Q

Fluconazole

A

Antifungal triazole

-static

Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase

So inh. ergosterol synth

SE:

  • Least effect on human P450
  • Teratogenic
  • Liver damage
  • Hallucinations

FLUCking may lead to birth defects (teratogenic)

LUCy in the sky with diamonds=LSD=Hallucinations

404
Q

Retapamulin

A

Antibacterial agent

Mech: inh. peptidyl transferase

Route: Topical

Use: skin staph or strep inf.

405
Q

What are the gastric irritants used as cathartics?

A

Cascara

Senna

Castor oil

Bisacodyl

407
Q

Fidaxomycin

A

Antibacterial agent

Mech: Inh. C. dificile RNA pol

Orally–Not systemically absorbed

Target: C. dificile

408
Q

Agents that activate beta1 receptors

A

NE

Dobutamine

409
Q

Clonidine

A

Central alpha-2 agonist

SE:

Depression

Drowsiness

Dry mouth

Impaired Ejac.

Unlabeled uses:

  • Fibromyalgia-unspecified neuronal pain
  • Insomnia
  • Tourettes
  • Opiate withdrawal
410
Q

Lincomycin

A

Antibacterial agent–lincosamide

Mech: like erythromycin-inh. translocation

SE: Severe superinf. w/ C. dificile

Targets:

  • Severe anaerobic infections (penetrating gut wound)
  • Dental prophylaxis in pts w/ heart valve problems
410
Q

Topiramate

A

Tx: Partial seizures

Mech: Act. GABA

412
Q

Aspirin

A

Tx: Analgesic, antipyretic, anti-inflam, anticlotting

Mech: Inh. COX

Therefore inh. prostaglandin synth (and thromboxane)

Kinetics:

  • ASA is weak acid so absorbed in stomach
  • Dissociates in plasma to form salicylic acid strongly bound to plasma proteins
  • 325-500mg/tablet; 4-6/day for arthritis
  • Lethal dose
    • Children(and elderly): 4g (12 tablets)
    • Adults 20g (50-60 tablets)
    • Death due to pulmonary edema

SE:

  • GI
    • Slicylic acid is direct irritant
    • ASA decreases PG production by intestinal mucosa
      • Decrease mucous production
      • Decrease HCO3 production
  • CNS effects
    • Tinnitus (large doses)
    • Increase resp rates
  • Other effects
    • Don’t take aspirin w/ warfarin
    • Direct effect on iris-decrease miosis during eye surgery
    • Decrease kidney perfusion
    • Hypersensitivity
    • Bronchospasms-esp in pts w/ nasal polyps
    • Inh. labor (PGs involved)

…

Asthmatic bronchospasms

Severe pulmonary edema

Peptic ulcer

Inhibit labor

Reye’s syndrome/Renal perfusion decrease

Iris–Inhibit miosis

Noise

413
Q

Heparin

A

Tx: Anticoagulant

Mech: Heparin binds to anti-thrombin (protease inhib) and increases its affinity for clotting factors by 1000x

Low doses: inhibits Xa, decreasing formation of thrombin

High doses: inhibits thrombin and irreversibly binds to IXa, XIa, and XIIa

Heparin inhibits clotting in vivo and in vitro

Activates lipoprotein lipases in blood

Where we get it: located in mast cells

Harvest it from cow lung and pig intestines

Strong neg charge

Not synthetic-each batch tested individually

Pharmacokinetics: IV or subQ

Too large to be absorbed in GI tract or pass placenta

Not risk free in pregnancy though

Immediate onset–T1/2=1 hour

Degradation via heparinase

Can bind to variety of proteins so dose response in unpredictable

_Toxicity: _

  • Generally non toxic
  • Major danger is bleeding
  • Overdose treated w/ protamine sulfate
    • Strong pos charge binds w/ strong neg of heparin
  • Long term use can lead to
    • Osteoporosis-act. osteoclasts
    • Thrombocytopenia-loss of platelets
      • HIT-heparin induced thrombocytopenia
    • Hypersensitivity-rare but we are injecting animal products
415
Q

Theophylline

A

Tx: Asthma

Mech: Inh. cAMP PDE→bronchodilation

Enzyme inh.

So increase in cellular cAMP

Methyl xanthine like caffeine

Clinical use: Chronic asthma

Low TI but used now b/c very cheap

SE:

  • Cardiac stimulation-arrythmias
  • CNS stim-tremors, insomnia, seizures
  • GI upset
417
Q

Gli–ide

or

Gly–ide

A

Glipizide

Glyburide

**Glimepiride **(most potent)

Tx: Diabetes

Oral hypoglycemic agents

Second gen sulphonylureas

More rapid onset and longer duration

Mech: K channel blockers

Block K channels on B cells →Increase Ca→Insulin secretion

Contra/Indications:

  • Do not use if you have renal or hepatic damage
  • Not overweight
  • Have some islet fxn

SE: Less than 1st gen

  • Hypoglycemia and hypoglycemia coma
    • More common in drugs w/ longer duration
  • Can be teratogenic
  • Can increase death due to cardiovascular problems
418
Q

Sugammadex

A

Reverses block by rocuronium by binding directly

419
Q

Topotecan

and irinotecan

A

Tx: Cancer

Mech: inhibits topoisomerase 1

  • You know its a topoisomerase inhibitor but which one?*
  • Add the first letter of one vs two to the front. If it makes sense it’s correct*
  • ttopotecan vs otopotecan*
  • **O-topotecan so topoisomerase One***
420
Q

Combined alpha and beta blockers

A

Block alpha1, beta1, and beta2

Labetalol

Carvedilol

SE:

  • Postural hypotension
  • Dry mouth
421
Q

Certolizumab

A

Tx: RA, Chron’s

Immunosuppressant

Mech: Binds TNF

422
Q

Dexamethasone

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Not inhaled

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
423
Q

-glinide

A

Repaglinide

Nateglinide

Tx: Diabetes

Oral hypoglycemic agents

Sulphonylurea-like agents

Rapid onset, short duration

Mech: K channel blockers

Bind diff site on K channel

Block K channels on B cells →Increase Ca→Insulin secretion

Contra/Indications:

  • Do not use if you have renal or hepatic damage
  • Not overweight
  • Have some islet fxn

SE:

  • Hypoglycemia and hypoglycemia coma
    • More common in drugs w/ longer duration
  • Can be teratogenic
  • Can increase death due to cardiovascular problems
425
Q

Bisphosphonates

A

Tiludronate

Etidronate

Bisphosphonates are less potent

Tx: Ca disorder

Mech: Enzyme inhibitor

Cause formation of abnormal ATP→inh ATP requiring enzymes

Pyrophosphates have an affinity for Ca and are incorporated into bone

When ingested by osteoclasts→decrease activity and apoptosis

T1/2: Many years

Use: 1st line tx for osteoporosis and pagets

Used in tx of MM too

SE:

  • GI upset, peptic ulcers
  • Inflammation of eye
  • IV infusions cause 1st dose effect (flu-like symptoms)
  • Osteonecrosis of jaw
    • Decrease blood flow to area
    • Esp in pts w/ lost of dental disease/surgery
    • Bone w/ bisphosphonates may be more susceptible to infections

Belly ache and peptic ulcers

Infections/Infarcts

Swollen eye

First dose eff (IV)→Flu-like symptoms

Osteonecrosis of jaw

426
Q

Acamprosate

A

Decreased craving for ethanol

427
Q

Adenosine

A

Tx:

  • Arrythmias (Other class)
  • Atrial Tachycardia

Mech:

  • Binds to adenosine receptor
  • Decreases firing rate of AV node
  • Coronary vasodilator

Kinetics-Very short T1/2=10sec

428
Q

First Gen Antidepressants

A

Impiramine + Amitryptyline

Tricyclic antidepressants

Mech: Inhibit NE reuptake

Act on multiple receptors

SE:

  • Most likely to cause SE
  • Sedation
  • Weight gain
  • Anticholinergic effect (dry eyes, dry mouth, constipation)
  • Cardiovascular effects
    • Arrythmias
    • Drop in BP (alpha1 block)
    • Orthostatic hypotension
429
Q

Garlic

A

Uses: Decrease blood lipids

May slightly lower blood lipids

1 fresh clove/day

SE:

  • Induce P450
  • Bad breath
  • Decrease clotting
  • Decrease conc. of some reverse transcriptase inh.
430
Q

Glargine

A

Tx: Diabetes

Designer insulin

Short acting (24+ hrs)

Determined to get large (that a long time)

Detemir +glargine=long acting insulins

432
Q

Nystatin

A

Class: Antifungal

Polyene antibiotics

Mech: Binds to ergosterol in fungal CM→pores→memb. leakage

Route: Topical

Can give orally, but only for fungi in gut

Too toxic for parenteral use

434
Q

Daptomycin

A

Antibacterial agent–lipopeptide

Mech: Forms pores in bacterial CM

Targets: Aerobic G+ (staph, strep)

Skin and soft tissue inf. or severe blood inf w/ S. aureus

SE:

  • Muscle pain and weakness
    • careful w/ statins
  • Eosinophilic pneumonia
435
Q

How does ethanol work?

A

Binds non-specifically to large molecules

Protein denaturance

436
Q

Ergocalciferol (D2)

A

Tx: Ca disorders

Mech: Vit D analog

Less potent than calcitriol

SE: Hypothyroidism

437
Q

Aminobisphosphonates

A

other -dronates

Aminobisphosphonates are more potent

Tx: Ca disorder

Mech: Enzyme inhibitor (farnesyl pyrophosphate synthetase)

Inh. enzyme in mavalonic acid synthesis pathway→abnormal cytoskeletal structure in osteoclasts

Pyrophosphates have an affinity for Ca and are incorporated into bone

When ingested by osteoclasts→decrease activity and apoptosis

T1/2: Many years

Use: 1st line tx for osteoporosis and pagets

Used in tx of MM too

SE:

  • GI upset, peptic ulcers
  • Inflammation of eye
  • IV infusions cause 1st dose effect (flu-like symptoms)
  • Osteonecrosis of jaw
    • Decrease blood flow to area
    • Esp in pts w/ lost of dental disease/surgery
    • Bone w/ bisphosphonates may be more susceptible to infections

Belly ache and peptic ulcers

Infections/Infarcts

Swollen eye

First dose eff (IV)→Flu-like symptoms

Osteonecrosis of jaw

438
Q

Flucytosine

A

Antifungal agent

Pyrimidine analog

Mech: Inh thymidine synth. in fungi

Converted to 5-fluororacil→inh. thymidilate synthatase

So inh DNA and RNA synth

Prodrug-enters fungus by specific enzymes

Does not enter human

SE:

  • Bone marrow depression→anemia
  • Liver toxicity
  • GI upset
439
Q

Ipratropium

A

Antimuscarinic agent

Blocks muscarinic receptor

441
Q

Methylxanthines

A

Caffeine

increase glomerular filtration rate

442
Q

Glulisine

A

Tx: Diabetes

Designer insulin

Short acting (2-5 hrs)

443
Q

Netilmicin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

DROPPED in the US

444
Q

Acetazolamide

A

Tx: Seizures

Mech: May increase CO2 in brain→Decrease activity

445
Q

Entecavir

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE:

  • Lactic acidosis
  • Hepatomegaly

Discontinuation→Increase hepatitis symptoms

446
Q

Metoclopramide

A

Tx: Gastroparesis

prokinetic agent–agents that increase stomach emptying rate

Also used for hiccups

Mech: DA and possible 5HT antagonist

Route: Oral or IV

Increase motility w/o secretion (of H or gastrin)

SE:

  • Sedation
  • Depression
  • Parkinson like symptoms

Metoclopramide increases motility

  • All that motility→shakes (parkinson like symptoms)*
  • All those shakes →sedation *
  • All that sedation→depression *
447
Q

“-grel”s

A

Tx: Anticoagulant

Mech: Platelet inhibitor

ADP receptor blocker on platelet

Same as ticlopidine-diff is pharmacokinetics: rapid onset, shorter T1/2

448
Q

Epinephrine

A

Tx: Asthma

Bronchodilator–DOC for short term relief

Mech: Acts on all adrenergic receptors

SE

  • Tons of them
  • Increase HR+vasoconstriction→increase BP
449
Q

Fluvoxamine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

450
Q

Fosfomycin

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Blocks synth of NAM

Spectrum: Aerobic G-

Use: Uncomplicated UTI

SE:

  • Diarrhea–killing bacteria in gut
451
Q

Hydroxyzine

A

First gen H1 blocker

Tx: Sedative, anti-itch

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
452
Q

Ginko

A

Uses:

  • Dementia
  • Intermittent claudication–pain in leg

About as eff. as tacrine for tx of alzheimer’s

But tacrine isn’t really effective at all

SE:

  • Inh platelet activating factor
  • Decrease clotting
  • Interacts w/ warfarin
454
Q

Atropine

A

Tx: Diarrhea

Anti-cholinergic agent

Mech: Blocks muscarinic receptor

SE: Many systemic

456
Q

“-vancin”s

A

Televancin

Dalbavancin

Antibacterial

Class: Non B lactam CW inhibitors

Lipoglycopeptide

Mech: Binds to dialanine residue on CW and prevents cross linking + disrupt bacterial CM

SE:

  • Nephrotoxicity
  • Fetal damage
  • Metallic taste
458
Q

Acetaminophen

A

Tx: Analgesic

Not an NSAID–Non-narcotic analgesic

No anti-platelet effect

Not effective for arthritis

Mech: Inh COX

Toxicity:

  • less GI effects than ASA
  • OD=10-15g (20-30 tablets)-can cause irreversible liver damage
    • Feel bad, then better, then liver starts to fail in a few days
    • Decreased glutathione in liver-treat w/ reducing agent (N-acetyl cysteine)
  • Alcoholics and acetaminophen lead to decreased glutathione w/ smaller dose
459
Q

-glutide

A

**Liraglutide **(Inj 1x/day)

Albiglutide (Inj. 1x/week)

Tx: Diabetes

Incretin enhancer

Mech: Bind to and activate receptors on B cell

Incretin analog

SE:

  • Thyroid tumor
  • I want my glutes to be as hard as concrete*
  • -glutide to be as hard as incretin*
460
Q

Ticarcillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
461
Q

Nicotine

A

Direct nicotinic agonist

462
Q

Second generation H1 blockers

A

Loratadine

Fexofenadine

Desloratadine

Cetirizine

Don’t cause drowsiness

Fewer CNS effects

Ionized in blood

Not metab. by P450

  • What does the fox say?*
  • What des the fex ce?*

_Des_loratadine (+ loratadine) _fex_ofenadine _ce_tirizine

463
Q

-gliflozin

A

Canagliflozin

Dapagliflozin

Empagliflozin

Tx: Diabetes

Inh. of glc resorption by kidney

**Mech: **Inh. SGLT2 (Na-glc cotransporter)

in PCT–allows kidney to eliminate blood glc

SE:

  • Hypotension
  • Hypokalemia
    • Due to increased urine output
  • Gential fungal inf
    • Urine loaded w/ glc
464
Q

Cyclopentolate

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

465
Q

What are the bulk adding agents?

A

Bran

Methylcellulose

Polycarbophil

Psyllium

467
Q

-gliptin

or

-glyptin

A

Sitagliptin

Saxagliptin

Linaglyptin

Alogliptin

Tx: Diabetes

Incretin enhancer

Mech: Inh DPP-4 Enzyme →prevent incretin metab

Orally

Often used in combo w/ other drugs

  • Put a lip of dip in (oral). Dip comes in a tin*
  • G-_LIP_-TIN are DPP inh. Taken orally.*
468
Q

Nevirapine

A

Antiviral agent

Tx: HIV

Mech: bind to non active sites and Inh reverse trans

Not competetive inh.

1st gen NNRTI

SE

  • Hepatotoxicity
  • Stevens Johnson syndrome
469
Q

Carbenicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
471
Q

Sumatriptan

and other “-triptan”s

A

Rizatriptan

Zolmitriptan

Naratriptan

Almotriptan

Eletriptan

Frovatriptan

Tx: Migraine

Mech: 5HT receptor agonist

Route: Orally as spray

Not to be used w/ SSRIs or MAO inh–will lead to synergistic effect→5HT syndrome→malignant hyperthermia like syndrome

472
Q

Alpha galactosidase

A

Tx: Diarrhea

Mech: Increase metab. of oligosacc.→digestible sugars

Oligosacc. produce gas

  • Alpha GAlactoSidase inh. GAS production*
  • *Be careful there are alpha-glucosidase inh in the diabetes section**
473
Q

Milnacipram

A

Third Generation Antidepressant

Mech: SNRIs

Inhibit reputake of 5HT and NE

*Third generations have the -faxine drugs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido
Cardiovascular stimulation

*SE same as 2nd gen +cardio stim.

474
Q

Sulbactam

A

Mech: Bind to and inh. B lactamase

Non antibiotic B-lactam ring compounds

475
Q

Amantadine

A

Antiviral agent

Tx: RNA virus (Influenza A virus)

Virus taken up by cell endosome→opens channel in endosome→H enters→virus can release genes

Mech: Blocks process by which H channel forms in endosome

Blocks transporter or ion channel

Used proph. or very early

SE:

  • Renal failure
  • Teratogen
  • CNS fx
    • Dizziness
    • Slurred speech
    • Confusion
    • Seizures
    • Nausea
476
Q

Aminocaproic acid

A

Tx: Hemostatic agent (enhance clotting)

Mech: Inhibits plasminogen activation

Enzyme inhibitor

Binds to plasminogen in plasma

Route: Oral or injection

477
Q

“-afils”

A

Sildenafil

Vardenafil

Tadalafil

Avanafil

Tx: ED

Mech:

  • Inhibits type 5 cGMP phosphodiesterase
  • Nitrates→NO→cGMP→smooth m relax
  • cGMP degraded to 5’GMP via type 5 cGMP phosphodiesterase
  • Relaxes arteries in corpus cavernosum→increase BF

SE:

  • Slight drop in BP
    • Do not use w/ alpha 1 blockers or nitrates
    • Too much drop in BP
  • Stroke
  • MI (may be due to activity)
  • Visual disturbances
    • Impaired blue/green color discrimination
    • NAION-some potential for damage to retina induced by cGMP PDE inhibitors

Metabolism: P450

478
Q

Teriparitide

A

Tx: Ca disorders

Mech: PTH analog

Increase osteoblast activity

Daily subQ injections for short periods

High doses→osteoclast stimulation so only given in short bursts

SE-increase incidence of osteosarcoma

479
Q

Donepezil

A

Indirect cholinergic agonist

Alzheimer’s tx

480
Q

What are the osmotic cathartics?

A

MgSO4

Mg(OH)2

Polyethylene glycol

481
Q

Remifentanil

A

Narcotic analgesic- synthetic

500-600x stronger than morphine

482
Q

Sodium Valproate

A

Tx: All seizures including Petit mal seizures

Mech:

  • Decrease GABA breakdown
  • Increase GABA synth
  • Act on Na and Ca channels

Toxicity:

  • GI upset
  • CNS sedation-tremors
  • Potentially fatal hepatitis
  • Fetal damage-drop in IQ
483
Q

-gravir

A

Tx: HIV

Mech: Inh. HIV-1 integrase

Inh. insertion of viral genome into human

Prevents propagation

484
Q

Infliximab

A

Infli-xi-mab

Tx: RA, Chron’s

Immunosuppressant

Mech: Binds TNF

Route: IV

SE:

  • Infusion→itching, hypertension, fever
  • Concerned if pt has pre-existing infection like fungus or Tb b/c infection may become worse
  • If you are _inflex_ible (from sitting on the toilet=Chron’s) take _inflix_imab although it may lead to _i_tching*
  • May also lead to hyperTensioN and Fever–binds to TNF*
485
Q

Physostigmine

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

487
Q

Cyclizine

A

Anti-emetic–Antihistamine

Mech: Block H1 receptor

SE: Anticholinergic effects

488
Q

Glyceryl Trinitrate (nitroglycerin) (GTN)

A

Tx: Angina

Mech:

GTN→NO→Act. guanylate cyclase→cGMP→vasodilation

Rapidly dilates all blood vessels, including coronary art.

Route: Given sublingually–1st pass effect

Effects last 30-60min

Rapid tolerance so cannot take continuously

SE:

  • Hypotension
  • Skin flushing
  • Headache-opening blood vessels in brain, feel pulsing

*Nitroglycerin is unstable and explosive in some conditions

489
Q

Phenylephrine

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

490
Q

-virine

A

Etravirine

Rilpivirine

Antiviral agent

Tx: HIV

Mech: bind to non active sites and Inh reverse trans

Not competetive inh.

2nd gen NNRTI

Differ from first gen:

  • Higher potency
  • Longer T1/2
  • Fewer SE
491
Q

Isophane

A

Tx: Diabetes

Designer insulin

Protamine insulin

Intermediate acting

493
Q

Nitroprusside

A

Acts directly on smooth muscle

Drug of choice in hypertensive emergencies

Acts w/in seconds–given IV

Dilates art and veins→drop in BP

increases cGMP→relaxation

Rapidly degrades in soln into cyanide

495
Q

Antibiotic combo for H pylori infection

A

GI drug-Enhance mucosal defense

Metronidazole

+/-

Amoxicillin

+/-

Clarithromycin

+/-

Tetracycline

496
Q

Ixabepilone

A

Tx: Cancer

Mech: Binds to microtubules

Natural product

  • Ixabepilone *
  • Pixabepilone*
  • Pixy sticks=tube=microtubules*
  • Yeah this one is a stretch…*
498
Q

Immunosuppressants for IBS

A

Methotrexate

Cyclosporine

499
Q

Fentanyl

A

Narcotic analgesic- synthetic

80-100x stronger than morphine

501
Q

Senna

A

GI Drug

Cathartic–Gastric Irritants

Mech: Stimulate gastric nn

Increase motility

Decrease electrolyte secretion into gut

SE:

  • Nephritis
  • Liver damage
503
Q

Dabigatran

A

Tx: Anticoagulant

Mech: Direct thrombin inhibitor

Enzyme inhibitor

Route: Oral

Kinetics:

  • Prodrug
  • Onset w/in 1 hr
  • P450 inhibitor may impact

SE-hemorhhage

504
Q

Telithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Same sites as erythromycin (50s) but induces less resistance b/c not readily transported out of bacterial cell

SE:

  • GI upset, nausea, and heartburn
  • Increase in GI activity b/c activates motilin
  • Inh P450
  • Liver damage-_SEVERE liver toxicity_
  • Arrythmias
  • Block cholinergic receptor
    • Worsen myasthenia gravis
    • Inh long ciliary ganglion→Decrease visual accomodation

macROlides like erythROmycin inh. transLOcation

Motility/ Myasthenia gravis worsens

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Ocular inh.

505
Q

Lacosamide

A

Tx: Partial seizures

Mech: Inh. Na

506
Q

Tropicamide

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

507
Q

Niacin

aka Vit B3

aka Nicotinic acid

A

Tx: Hyperlipidemia

Mech:

  • Inh. enzyme essential for VLDL synth
  • May also bind to receptor that decreases VLDL synth

Effects:

  • Decrease VLDL
  • Increase HDL–strongest increase of any drug

SE:

  • Cutaneous flushing and itching (prevented by aspirin)
  • Increase uric acid–>gout
  • Increase incidence of diabetes
508
Q

Diphenhydramine

or

Dimenhydramine

A

Anti-emetic–Antihistamine

Mech: Block H1 receptor

SE: Anticholinergic effects

509
Q

Ma huang (ephedra)

A

Use:

  • Weight loss
  • Nasal congestion
  • Asthma
  • Increase athletic performance

Strong CNS stimulant

SE:

  • Stroke
  • Hypertension
  • MI
511
Q

Fluoxetine pharmacodynamics

A

Acts on transport systems

512
Q

Gentamycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

**Use: **Ointment for eye

513
Q

Scopolamine

A

Antimuscarinic agent

Blocks muscarinic receptor

Lasts 3-7 days

514
Q

Tetracycline

A

Tx:

  • Rickettsia
  • Spirochetes (lyme disease)
  • Helicobacter
  • Legionella

Mech: Reversibly bind to 30s.

Inhibits the binding of tRNA to the A site

-static

SE

  • Deposited in Ca storage sites-bones/teeth-esp fetus or child
    • Binds to cations, esp Ca, also Fe and Al.
    • Preg risk D
  • Renal and hepatic toxicity
  • Degrades to toxins–don’t use after expiration date
515
Q

Aliskiren

A

Renin inhibitor

SE:

  • Fetal damage
  • Diarrhea
  • Cough
  • Angioedema
517
Q

-setron

A

Ondansetron

Granisetron

Dolasetron

Palonosetron

Anti-emetic (for IBS+chemo)

Mech: 5HT receptor blocker

Affect CTZ +rec. in gut

SE: Constipation

_SE_lective _T_e_R_minators _O_f _N_ausea

-SETRON

-setron blocks serotonin

517
Q

Thiazide diuretics SE and other effects

A

Other effects:

  • Cause direct vasodilation
  • Often initial drugs for hypertension
  • Decrease Ca excretion

Side effects:

  • Hypokalemia
    • Lose K due to Na-K exchanger
  • Increase in serum LDL and triglycerides (atherosclerosis)
  • Decrease uric acid secretion→gout
  • Inhibit insulin secretion
  • Contain sulfur ions-may cause allergens
518
Q

Cortisone

+

Hydrocortisone

A

Immunosuppressive potency=1

Relative minerallocorticod activity=1

Duration: 8-12hrs

Cortisone is a prodrug:

  • Must be metab by P450 (in liver)
  • Not effective topically
519
Q

Scopolamine

A

Tx: Diarrhea

Anti-cholinergic agent

Mech: Blocks muscarinic receptor

SE: Many systemic

520
Q

Amoxicillin

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Broad spectrum

Route: Oral

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • B lactam ring may inh. GABAergic neurons
521
Q

Sitostanol

A

Tx: Hyperlipidemia

Mech: Looks like cholesterol–blocks uptake

522
Q

Sufentanil

A

Narcotic analgesic- synthetic

500-600x stronger than morphine

523
Q

Codeine

A

Tx: Diarrhea

Narcotic agent

Mech: act a specific receptor

Not generally used for obvious reasons

525
Q

Mupirocin

A

Mech: Binds to bacterial isoleucyl tRNA synthetase

Route: Topical

Use: Staph inf.

526
Q

Voriconazole

A

Antifungal triazole

-static

Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase

So inh. ergosterol synth

SE:

  • Less effect on human P450 (triazole vs imidazole)
  • Can cause visual disturbances

_V_oriconazole causes _V_isual disturbances

527
Q

“-statin”s

A

Lovastatin

Bunch of other -statins whose diff is pharmacokinetics

Tx: Hyperlipidemia

Mech:

  • Lovastatin is prodrug
  • HMG CoA reductase inhibitor
    • Rate limiting step in cell synth of their own cholesterol
  • When cells can’t make own cholesterol→increase in LDL receptors→increase LDL uptake

Effects:

  • Decrease LDL (25%)
  • Decrease VLDL synth

SE:

  • Myositis (muscle pain)
    • At worst→rhabdomyolysis (muscle breakdown)
  • Liver toxicity
  • Teratogenic–preg. category X
  • Some memory loss

Kinetics-metab by P450

528
Q

Sertaline

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

529
Q

Echinacea

A

Use:

  • Upper resp. inf.
  • Wound healing
  • Antifungal

Can decrease sympt. of flu if used early

SE:

  • Allergies
    • Related to ragweed
530
Q

Abatacept

A

Tx: RA

Immunosuppressant

Mech: binds to and inh. CD80, CD86 receptors

Affects T cell activation

ABatacept CD80+86 receptors

_A_batacept for _A_rthritis

531
Q

Cyclosporine

A

Tx: Transplants, psoriasis, dry eye (tear duct inflam)

Fungus derived

Route: Emulsion

Mech:

Binds to intracellular protein-cyclophyllin

Complex forms and _inh. enzyme-_calcineurin phosphatase

Enzyme inhibitor

Prevents act. of NFAT complex which then prevents act of gene that codes for IL2,3 and TNF alpha

T cell inhibited

Kinetics

  • Metabolized by P450
    • Lots of drug interactions-esp. antibiotics

SE:

  • Nephrotoxicity
  • Hepatotoxicity
  • Cosmetic changes
    • Hypertrichosis
    • Gingival hyperplasia
  • Increased cholesterol (reversible)
  • Mild hypertension (reversible)

Cyclosporin-binds to Cyclophyillin→inh. Calcinuerin, used for Crusty eyes and skin, may cause Cosmetic Changes, î Cholesterol, Cidney (kidney) damage

  • What else affects calcinuerin phosphatase? Tacrolimus*
  • Cyclosporine: Binds cyclophyllin*
  • Tacrolimus: Binds FK protein*
532
Q

Procaine pharmacodynamics

A

Agents that act on ion channels

533
Q

SE of cephalosporins

A

Allergic cross activity w/ penicillin sensitive pts

Possibility of superinfection

534
Q

Celecoxib

A

Cele-cox-ib

Selective cox(2) inhibitor

Tx: Analgesic and anti-inflam

535
Q

Cetirizine

A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
536
Q

H2 blockers

Names

A

“-tidine”s

Cimetidine

Ranitidine

Famotidine

Nizatidine

*Only diff amongst all is that cimetidine has anti-androgenic effects

537
Q

Tolbutamide

A

Tx: Diabetes

Oral hypoglycemic agents

First gen sulphonylureas

Mech: K channel blockers

Block K channels on B cells →Increase Ca→Insulin secretion

Duration: 6-12 hrs

Contra/Indications:

  • Do not use if you have renal or hepatic damage
  • Not overweight
  • Have some islet fxn

SE:

  • Hypoglycemia and hypoglycemia coma
    • More common in drugs w/ longer duration
  • Can be teratogenic
  • Can increase death due to cardiovascular problems
538
Q

Trastuzumab

A

Tx: Cancer

Mech: vs HER2

Human epidermal growth factor receptor

  • Don’t hook up w/ her too, that’s trashy*
  • Don’t hook up w/ HER2, thats tras-tuzumab*
539
Q

Specific B1 receptor blockers

A

“olol”s

Metoprolol

Acebutolol

Alprenolol

Atenolol

Esmolol

Betaxolol

Nebivolol

These decrease HR

540
Q

How do anticancer drugs work?

A

Binds non-specifically to large molecules

541
Q

Raloxifene

A

Tx: Ca disorders +estrogen dependent breast cancer

Mech: Activates estrogen receptors in bone

Blocks estrogen receptors in breasts

Estrogen analog

SERM-selective estrogen receptor modulator

Inh. osteoclast activity

SE

  • Pulmonary embolisms
  • Stroke
  • Preg. cat X
  • Raloxifene like Tamoxifene affect estrogen receptor*
  • SE=SEX*

Stroke

Embolism (pulmonary)

X (preg cat.)

542
Q

6-mercaptopurine

A

Tx: Cancer

Mech: Converted in cell to an analog that inhibits several enzymes needed for purine synth

Prodrug–purine analog

  • Azathioprine=immunosuppressant prodrug. *
  • Gets converted into 6-mercaptopurine.*
  • Used for Chron’s, RA, and transplants*
543
Q

High Ceiling diuretics SE

A
  • Dehydration
  • Hypokalemia
    • Used w/ K supplements or K sparing diuretics
  • Increased Ca excretion→Hypocalcemia
  • Decreased uric acid excretion→gout
  • Auditory nerve damage esp. if used w/ other ototoxic agents
544
Q

Aldosterone antagonists mech

A

Blocks aldosterone receptor

Aldosterone is responsible for synth of Na-K exchanger

Takes days to be effective

545
Q

Neomycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

Route: Topical or oral

**SE: **Very nephrotoxic–so only topically or orally

546
Q

Aldosterone antagonists

A

K sparing diuretics

Spironolactone

Eplerenone

547
Q

Insulin

A

Agents that act on cell membrane receptors

548
Q

Streptomycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

Spectrum: Aerobic G-

Must be absorbed by active transport

SE:

  • Ototoxicity
    • Hearing and balance affected
    • hearing loss may be permanent
  • Nephrotoxic
    • Most common cause of drug induced renal failure
    • Used very widely
  • High doses
    • Neuromuscular blockade
      • Decrease in ACh+ ACh receptors on mm
    • Fetal damage
      • Preg cat. D

​​​

  • Strippers fornicate*
  • Strep. FORNICAT*

Fetal damage

Ototox.

Renal tox

Negative (G-)

Irr. bind 30s

Cidal

*ACh block *

tRNA can’t bind to mRNA

  • *
549
Q

Triamcinolone

A

Immunosuppressive potency=4

Relative minerallocorticod activity=.25

Duration: 18-36hrs

550
Q

Mexiletine

A

Tx: arrythmias (Class Ib)

Mech: Na channel blocker

Clinical use:

  • Emergency tx of ventricular arrythmias
  • Tx of ventricular tachycardia

Like lidocaine but can be given orally

551
Q

Zileuton

A

Tx: Asthma

Mech: Inh. 5-lipoxygenase

Blocks leukotriene synthesis

Enzyme inh.

SE: increases liver enzymes

zileutoN for eNzyme inhibitor

552
Q

Desloratadine

A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
553
Q

Rilonacept

A

Tx: RA

Mech: Binds to IL-1

Route: SubQ

Used w/ other immunosuppressants like methotrexate

Should NOT be used w/ TNF inh b/c may lead to serious infection (too much suppression)

  • Anakinra-blocks IL1 receptor*
  • Rilonacept-binds to IL1*
554
Q

Crofelemer

A

Tx: Diarrhea

Mech: Blocks Cl channel in gut

Also decreases secretion of Na and H2O

CrofeLemer blocks CL channels

  • or *
  • CROws block the CLouds*
  • CROfelemer blocks CL channels*

Pharm 6 (7 decks)

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