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Pharm 3 > Drugs from every unit in random order > Flashcards

Drugs from every unit in random order Flashcards

1
Q

Methotrexate pharmacodynamics

A

Act on specific enzymes

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1
Q

Propranolol

A

Tx: arrythmias (Class II)

Mech: B1 blocker

Decreases pacemaker firing rate

SE:

  • Bradycardia
  • Hypotension
  • B2 effects-asthma
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2
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
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3
Q

Calcium channel blockers

A

“-ipine”s

Inhibit Ca influx into vascular smooth m

Prevent vasoconstriction

SE:

  • Heartburn
  • May worsen heart failure
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3
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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4
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
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4
Q

Infliximab pharmacodynamics

A

Act on specific enzymes

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4
Q

Anagrelide

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Platelet count reducer

Decreases platelet formation, maturation, and #

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4
Q

Antipsychotic drugs used to treat mania

A

Phenothiazine

Haloperitol

Benzos

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5
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
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7
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

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8
Q

Cyclopentolate

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

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8
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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9
Q

Minoxidil pharmacodynamics

A

Agents that act on ion channels

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9
Q

Phenobarbital

A

Tx: All seizures EXCEPT petit mal

Class: Barbituate

Mech: Act. GABA

SE:

  • Sedation
  • Induces P450
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10
Q

Topiramate

A

Tx: Partial seizures

Mech: Act. GABA

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11
Q

Sarin

A

Nerve gas-direct cholinergic agonist

Irreversible AChE inhibitors

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11
Q

Pralidoxime

A

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

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11
Q

Sotalol

A

Tx: arrytmhias (Class III)

Mech: K+ channel blocker

Also a beta blocker

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11
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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11
Q

Fomepizole

A

Specific inhibitor of alcDH

Prolongs effects of alcohol

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12
Q

Aldosterone antagonists

A

K sparing diuretics

Spironolactone

Eplerenone

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12
Q

Insulin

A

Agents that act on cell membrane receptors

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13
Q

Inhibitors of Na transport in DCT and collecting tubule

A

Triamterene

Amiloride

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13
Q

Other tx of bipolar

A

Most are antiseizure:

  • Valproic acid
  • Carbamazepine
  • Limotripene

Acetazolamide

Aripripazole-anti-psychotic

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14
Q

Lamotrigine

A

Tx: Partial seizures

Mech: Inh. Na

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15
Q

Diazoxide

A

Acts directly on smooth muscle

Opens K channels→hyperpolarization

Inhibits insulin release from B cells in pancreas

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16
Q

Aliskiren

A

Renin inhibitor

SE:

  • Fetal damage
  • Diarrhea
  • Cough
  • Angioedema
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17
Q

Procaine pharmacodynamics

A

Agents that act on ion channels

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17
Q

High ceiling diuretics

A

Furosemide, ethacrynic acid, bumetanide, torsemide

  • Orally or parenterally
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17
Q

Specific B1 receptor blockers

A

“olol”s

Metoprolol

Acebutolol

Alprenolol

Atenolol

Esmolol

Betaxolol

Nebivolol

These decrease HR

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17
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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17
Q

Mirtazapine

A

Antidepressant

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18
Q

Methylxanthines

A

Caffeine

increase glomerular filtration rate

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19
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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20
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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21
Q

Rocuronium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

Most common one

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21
Q

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

A

curare

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21
Q

Fluvoxamine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

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22
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.

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23
Q

Aldosterone antagonists mech

A

Blocks aldosterone receptor

Aldosterone is responsible for synth of Na-K exchanger

Takes days to be effective

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24
Q

Heroin

A

Narcotic analgesic- semisynthetic

Originally to cure morphine addiction

5x stronger than morphine

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25
Q

Agents that activate B2 receptors

A

“Nols and rols”

Metaproterenol

Terbutaline

Fenoterol

Albuterol

Tx: asthma

Causes bronchodilation

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25
Q

Olestra

A

Fake fat

SE: Butt leakage

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25
Q

Orlistat

A

Tx: Hyperlipidemia

Mech: Inh GI and pancreatic lipase

Decrease fat absorption from gut

SE: Loose stool

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26
Q

Vorapaxar

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Thrombin receptor blocker on platelet

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

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27
Q

Cocaine pharmacodynamics

A

Acts on transport systems

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29
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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30
Q

Paroxetine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

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30
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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31
Q

Lacosamide

A

Tx: Partial seizures

Mech: Inh. Na

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32
Q

Fenoldopam

A

Activate D1 receptors

Given IV for HT emergencies

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32
Q

Dobutamine

A

Tx: CHF

Class: Inotropic agents

Mech: Beta1 agonist

Effects: Increase force of contraction

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32
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)

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33
Q

Atropine

A

Antimuscarinic agent

Blocks muscarinic receptor

Lasts 7-10 days

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33
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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35
Q

Neostigmine

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

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36
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

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36
Q

Pregabalin

A

Tx: Partial seizures

Mech: Acts on Ca channels

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37
Q

Naphazoline

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

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37
Q
A
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38
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.

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40
Q

Epinephrine

A

Works on all adrenergic receptors

Causes increased HR, etc. etc.

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40
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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40
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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41
Q

Icosapent

A

Tx: Hyperlipidemia

Mech: Inhibit enzyme responsible for Trig synth

Not clear though

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41
Q

Levetiracetam

A

Tx: Partial seizures

Mech: Unknown

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42
Q

Edrophonium

A

Indirect cholinergic agonist

Doesn’t last very long

Inhibit AChE

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43
Q

More selective B blockers

A

Metoprolol

Acebutolol

Atenolol

Betaxolol

Nebivolol

SE:

  • Fewer CNS effects
  • Bradycardia
  • Fatigue w/ exercise
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44
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

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45
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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46
Q

Acamprosate

A

Decreased craving for ethanol

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47
Q

Ipratropium

A

Antimuscarinic agent

Blocks muscarinic receptor

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47
Q

Hirudin

A

Tx: Anticoagulant–found in leech saliva

Mech: Directly inhibits thrombin

Enzyme inhibitor

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48
Q

Diltiazem

A

Tx: Arrythmias except vent. arrythmias (class IV)

Mech: Ca channel blockers

Increase refractory period

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49
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

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49
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

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50
Q

Cimetidine pharmacodynamics

A

Agents that act on cell membrane receptors

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51
Q

Methadone

A

Narcotic analgesic- synthetic

Orally effective-liquid

Less euphoric

Given to wean off morphine

Same strength as morphine

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52
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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53
Q

Sufentanil

A

Narcotic analgesic- synthetic

500-600x stronger than morphine

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55
Q

Malathion

A

Insecticide-cholinergic agonist

Irreversible AChE inhibitors

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56
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

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57
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

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58
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
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59
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

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60
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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61
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
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62
Q

Zonisamide

A

Tx: Partial seizures

Mech: Inh. Na

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64
Q

Acetazolamide

A

Tx: Seizures

Mech: May increase CO2 in brain→Decrease activity

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65
Q

Vortioxetine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

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66
Q

Hydromorphone

A

Narcotic analgesic- semisynthetic

10x stronger than morphine

“Dilaudid”

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68
Q

Clonidine

A

Central alpha-2 agonist

SE:

Depression

Drowsiness

Dry mouth

Impaired Ejac.

Unlabeled uses:

  • Fibromyalgia-unspecified neuronal pain
  • Insomnia
  • Tourettes
  • Opiate withdrawal
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70
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)
71
Q

Ticlopidine

A

Tx: Anticoagulant

Mech: Platelet inhibitor

ADP receptor blocker on platelet

SE:

  • Neutropenia-loss of neutrophils
  • Agranulocytosis
71
Q

Gabapentin

A

Tx: Partial seizures

Mech: Act GABA

GABApentin

72
Q

Verapamil

A

Tx: Arrythmias except vent. arrythmias (class IV)

Mech: Ca channel blockers

Increase refractory period

73
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
75
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

76
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

78
Q

Sitostanol

A

Tx: Hyperlipidemia

Mech: Looks like cholesterol–blocks uptake

79
Q

Muscarine

A

Direct muscarinic agonist

80
Q

Propranolol pharmacodynamics

A

Agents that act on cell membrane receptors

80
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
80
Q

Cilostazol

A

Tx: Anticoagulant

Mech: Platelet inhibitor

Inhibits phosphodiesterase

Inh. enzyme that breaks down cAMP

Increased cAMP→Decrease platelet agg.

82
Q

Vigabatrin

A

Tx: Partial seizures

Mech: Act GABA

ViGABAtrin

84
Q

Morphine pharmacodynamics

A

Agents that act on cell membrane receptors

86
Q

Bethanechol

A

Direct muscarinic agonist

87
Q

Combined alpha and beta blockers

A

Block alpha1, beta1, and beta2

Labetalol

Carvedilol

SE:

  • Postural hypotension
  • Dry mouth
88
Q

Oxycodone

A

Narcotic analgesic- semisynthetic

Partial agonist-available in oral form as oxycontin

0.5x as strong as morphine

89
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

91
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

92
Q

Non specific B1 and B2 blockers

A

Propanolol

Timolol

Levobunolol

Certeolol

Metipranolol

92
Q

What induces the release of NE from nerve terminals?

A

Indirect acting amines:

Amphetamine, methamphetamine

Tyramine

Phenylpropanolamine

Pseudoephedrine

93
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

93
Q

Omega 3 fatty acids

A

Tx: Hyperlipidemia

Mech: Inhibit enzyme responsible for Trig synth

Not clear though

95
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.

95
Q

Naltrexone

A

Narcotic analgesic antagonist

Opiate receptor blocker

97
Q

Tranylcypromine pharmacodynamics

A

Act on specific enzymes

98
Q

Methylnaltrexone

A

Narcotic analgesic antagonist

Opiate receptor blocker

99
Q

Tramadol

A

Narcotic and SSRI

100
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
101
Q

Demecarium

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

103
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
104
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
105
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.

107
Q

Rufinamide

A

Tx: Partial seizures

Mech: Inh. Na

108
Q

Metoprolol

A

Tx: arrythmias (Class II)

Mech: B1 blocker

More selective

SE:

  • Bradycardia
  • Hypotension
110
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

111
Q

Prazosin

A

Adrenergic antagonist

alpha1 receptor blocker

Tx: hypertension

112
Q

Fluoxetine

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

113
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

114
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

115
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

116
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
116
Q
A
118
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
119
Q

Echothiophate

A

Indirect cholinergic agonist

Lasts for 100s hours

Phosphorylates AChE

120
Q

Heparin pharmacodynamics

A

Act on specific enzymes

122
Q

Pancuronium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

123
Q

Inhibitors of Na transport in DCT and collecting tubule SE

A

Hyperkalemia

124
Q

Nicotine

A

Direct nicotinic agonist

126
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

127
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

128
Q

Deferoxamine

A

Tx: Acute iron OD

Mech: Iron chelator

De-Fer-oxamine

_De_toxes _Fer_rous overdose

130
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

131
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

133
Q

How do anticancer drugs work?

A

Binds non-specifically to large molecules

135
Q

Perampanel

A

Tx: Partial seizures

Mech: Blocks glutamate

136
Q

Ethosuximide

A

Tx: DOC for petit mal seizures

Mech: Inhibit Ca channels in CNS

SE:

  • GI upset
  • Drowsiness
137
Q

Alprostadil

A

Tx: ED

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

138
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
139
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

140
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
141
Q

Tapentadol

A

Narcotic and SSRI

143
Q

Imitinib pharmacodynamics

A

Act on specific enzymes

144
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

145
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)

146
Q

Agents that activate beta1 receptors

A

NE

Dobutamine

147
Q

Aspirin pharmacodynamics

A

Act on specific enzymes

149
Q

Fluoxetine pharmacodynamics

A

Acts on transport systems

150
Q

Buproprion

A

Antidepressant

152
Q

Aminocaproic acid

A

Tx: Hemostatic agent (enhance clotting)

Mech: Inhibits plasminogen activation

Enzyme inhibitor

Binds to plasminogen in plasma

Route: Oral or injection

153
Q

How does ethanol work?

A

Binds non-specifically to large molecules

Protein denaturance

154
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
154
Q

Codeine

A

Narcotic analgesic- narcotic analogs

Partial agonist-low anti-nociceptive effects

Given orally

Greater effect on coughing-anti-tussive effect

156
Q

Nitroglycerin pharmacodynamics

A

Act on specific enzymes

157
Q

Nifedipine pharmacodynamics

A

Agents that act on ion channels

158
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
159
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

161
Q

Tranexamic acid

A

Tx: Hemostatic agent (enhance clotting)

Mech: Inhibits plasminogen activation

Enzyme inhibitor

Binds to plasminogen in plasma

162
Q

Naloxone

A

Narcotic analgesic antagonist

Opiate receptor blocker

Naloxone-oxycodone combinations exist to make withdrawl easier

164
Q

Alpha-methyl DOPA

A

Central alpha-2 agonist

Prodrug: metabolized to alpha-methyl NE

SE:

Depression

Drowsiness

Dry mouth

Impaired Ejac.

Hepatic dysfunction

165
Q

Angiotensin receptor blockers

A

“-Artan”s

SE:

  • Decrease secretion of aldosterone
  • Fetal abnormalities
    • All agents that alter angiotensin system
    • Pregnancy risk X
167
Q

Meperidine

A

Narcotic analgesic- synthetic

.5x as strong as morphine

No pupil constriction

168
Q

Pilocarpine

A

Direct muscarinic agonist

169
Q

Phenoxybenzamine

A

Adrenergic antagonist

alpha1 receptor blocker

Tx: hypertension

170
Q

Citalopram

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

172
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
174
Q

Fentanyl

A

Narcotic analgesic- synthetic

80-100x stronger than morphine

175
Q

High Ceiling diuretics clinical use

A
  • Pts who dont respond to thiazides
  • Life threatening edema (pulmonary or cerebral)
  • Compromised renal fxn
176
Q

Isosorbide dinitrate

A

Tx: Angina

Slow release nitrate formulation

Can be given orally

Slow enough that effects occur before 1st pass metabolism

178
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

179
Q

Escitalopram

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

180
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
181
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

182
Q

Morphine

A

Narcotic analgesic- narcotic analogs

Given parenterally due to first pass effect

183
Q

Vilazodone

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

184
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
185
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

186
Q

Ezetimibe

A

Tx: Hyperlipidemia

Mech: Blocks cholesterol transport

SE: Flatulence

187
Q

Diazepam

A

Tx: Seizures

Class: Benzos

Mech: GABA

IV to treat status epilepticus

188
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.

189
Q

Tacrine

A

Indirect cholinergic agonist

Alzheimer’s tx

190
Q

Omeprazole pharmacodynamics

A

Agents that act on transport systems

192
Q

Tropicamide

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

193
Q

Scopolamine

A

Antimuscarinic agent

Blocks muscarinic receptor

Lasts 3-7 days

194
Q

Ezogabine

A

Tx: Partial seizures

Mech: Open K channel

195
Q

Esmolol

A

Tx: arrythmias (Class II)

Mech: B1 blocker

More rapid onset of action

SE:

  • Bradycardia
  • Hypotension
  • B2 effects-asthma
197
Q

Remifentanil

A

Narcotic analgesic- synthetic

500-600x stronger than morphine

198
Q

Thiazide diuretics

A

Chlorothiazide and hydrochlorothiazide

199
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
200
Q

Sugammadex

A

Reverses block by rocuronium by binding directly

201
Q

Phenylephrine

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

203
Q

Tiagabine

A

Tx: Partial seizures

Mech: Act GABA

Tiagabine

205
Q

Ethanol as a diuretic

A

Mech: decrease release of ADH

207
Q

Endothelin blockers

A

“-entan”s

Tx of pulmonary arterial hypertension

SE:

  • Fetal damage
  • Testicular atrophy
  • Hepatic toxicity
208
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

209
Q

Aspirin

A

Tx: Anticoagulant

Mech: Platelet inhibitor

COX (enzyme) inhibitor

Inhibits TXA2 synth

Decreases platelet aggregation

210
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

211
Q

Alfentanil

A

Narcotic analgesic- synthetic

500-600x stronger than morphine

212
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

213
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
214
Q

Nefazodone

A

Antidepressant

215
Q

Second generation antidepressants

A

Fluoxetine

Fluvoxamine

Sertraline

Paroxetine

Citalopram

Escitalopram

Vilazodone

Mech: SSRIs

SE:

  • GI upset
  • Nausea
  • Insomnia
  • Headache
  • Decreased libido
216
Q

Sertaline

A

2nd gen antidepressant

Mech: SSRIs

SE:

GI upset
Nausea
Insomnia
Headache
Decreased libido

217
Q

Prazosin pharmacodynamics

A

Agents that act on cell membrane receptors

218
Q

Nifedipine

A

Tx: Arrythmias except vent. arrythmias (class IV)

Mech: Ca channel blockers

Increase refractory period

219
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

220
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

221
Q

Disulfiram

A

Inhibits acet.DH→buildup of acetaldehyde

Get severe hangover right away

222
Q

Donepezil

A

Indirect cholinergic agonist

Alzheimer’s tx

223
Q

Clonidine

A

Adrenergic agonist

Activates alpha2 receptors

Decrease symp outflow from CNS

Tx: hypertension

Other analogs used for glaucoma (Decrease pressure)

224
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

225
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)

226
Q

alpha-methyl tyrosine

A

Tx of pheochromocytoma

Central and peripheral effects

Inhibits tyrosine kinase–preventing synthesis NE and epi

227
Q

atracurium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

228
Q

alpha-methyl NE

A

Adrenergic agonist

Activates alpha2 receptors

Decrease symp outflow from CNS

Tx: hypertension

Other analogs used for glaucoma (Decrease pressure)

229
Q

Hydroxyurea

A

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

SE: Mutagenic

Pregnancy category D

230
Q

Dronedarone

A

Tx: arrytmhias (Class III)

Mech: K+ channel blocker

Analog of amiodarone

Fewer SE-less efficacious

231
Q

Physostigmine

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

232
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

233
Q

Homatropine

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

234
Q

Tetrahydrozoline (Visine)

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

Pharm 3 (6 decks)

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