All Drugs. All Units. Random Order. Wow. Flashcards
Mineral oil
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
Edrophonium
Indirect cholinergic agonist
Doesn’t last very long
Inhibit AChE
Muscarine
Direct muscarinic agonist
Dronedarone
Tx: arrytmhias (Class III)
Mech: K+ channel blocker
Analog of amiodarone
Fewer SE-less efficacious
High Ceiling diuretics mechanism
Mech of action:
- Inhibit Na and Cl resorbtion from Asc. loop of Henle
More efficacious than thiazides
Piperacillin
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
Thiazide diuretics
Chlorothiazide and hydrochlorothiazide
Tetrahydrozoline (Visine)
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
Paracalcitrol
Tx: Ca disorders
Mech: Vit D analog
Less potent than calcitriol
SE: Hypothyroidism
Ledipasvir
Antiviral agent
Tx: Hepatitis virus (esp Hep C)
Mech: Binds to and inh. protein thats necessary for HCV replication
Loratadine
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
Inhibitors of Na transport in DCT and collecting tubule
Triamterene
Amiloride
Morphine
Narcotic analgesic- narcotic analogs
Given parenterally due to first pass effect
Triamterene
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
Foscarnet
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
“-lukast”s
Zafirlukast
Montelukast
Tx: Asthma
Mech: Leukotriene receptor blocker
Metoprolol
Tx: arrythmias (Class II)
Mech: B1 blocker
More selective
SE:
- Bradycardia
- Hypotension
Mezlocillin
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
Valacyclovir
Antiviral drug
Tx: Herpes simplex and zoster
Mech: Prodrug converted to acyclovir
Must be given orally-prodrug metab. by 1st pass metab.
Tocilizumab
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*
Flax oil seeds
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
Calcium chelators
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
Erythromycin
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——
Which GCs used for IBS
Prednisone
Budesonide
ACE inhibitors
“-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
Perampanel
Tx: Partial seizures
Mech: Blocks glutamate
Second generation antidepressants
Fluoxetine
Fluvoxamine
Sertraline
Paroxetine
Citalopram
Escitalopram
Vilazodone
Mech: SSRIs
SE:
- GI upset
- Nausea
- Insomnia
- Headache
- Decreased libido
Saw Palmetto
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
Clarithromycin
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
Leflunomide
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)*
Ganciclovir
Antiviral agent
Tx: CMV (herpes virus)
CMV→retinitis+ blindness
Mech: Inhibits viral DNA pol
Prodrug-activated by viral kinase
SE:
- Neutropenia
- Thrombocytopenia
- Teratogen
High ceiling diuretics
Furosemide, ethacrynic acid, bumetanide, torsemide
- Orally or parenterally
Difenoxin
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
Methicillin
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
Tranylcypromine
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)
Psyllium
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Diphenoxylate
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
Ribavirin
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
Pyrazinamide
Antimycobacterial agent
Mech: Inh FA synth
Prodrug converted in macrophase where TB lives
SE:
- Gout
- Hepatitis
Nifedipine
Tx: Arrythmias except vent. arrythmias (class IV)
Mech: Ca channel blockers
Increase refractory period
Ethambutol
Antimycobacterial agent
Mech: Inh arabinosyl transferase
Necessary for CW synth
SE:
- Optic neuritis
- Impaired red/green discrimination
- Decreased vision
Clavulanic acid
Mech: Bind to and inh. B lactamase
Non antibiotic B-lactam ring compounds
5-fluorouracil
Tx: Cancer
Mech: Inh. thymidylate synthatase→inh. thymidine synth
Prodrug–Pyrimidine analog
Omega 3 fatty acids
Tx: Hyperlipidemia
Mech: Inhibit enzyme responsible for Trig synth
Not clear though
Clonidine
Adrenergic agonist
Activates alpha2 receptors
Decrease symp outflow from CNS
Tx: hypertension
Other analogs used for glaucoma (Decrease pressure)
Nedocromil
“-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
Fluoride
Tx: Ca disorders
Effects: Increase osteoblasts
Makes bone harder but more brittle
Not for osteoporosis
Inhibitors of Na transport in DCT and collecting tubule mech
K sparing diuretic
Prevent Na from getting into the exchanger by blocking Na ion channel
-Effects more rapid and predictable than spironolactone
Lamotrigine
Tx: Partial seizures
Mech: Inh. Na
Hirudin
Tx: Anticoagulant–found in leech saliva
Mech: Directly inhibits thrombin
Enzyme inhibitor
Budesonide
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
Eplerenone
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
Atgam
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
Cyclophosphamide
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
Misoprostole
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)*
Antifungals for candida+ ringworm
Miconazole
and other “conazoles”
Route: Topical and systemic
“-ergotamine”s
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
Cocaine pharmacodynamics
Acts on transport systems
Epinephrine
Works on all adrenergic receptors
Causes increased HR, etc. etc.
Tirofiban
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
Amiloride
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
Ethosuximide
Tx: DOC for petit mal seizures
Mech: Inhibit Ca channels in CNS
SE:
- GI upset
- Drowsiness
Metronidazole
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
Quinidine
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
-prazole
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
Phenytoin
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
Morphine pharmacodynamics
Agents that act on cell membrane receptors
Natamycin
Class: Antifungal
Polyene antibiotics
Route: Topical
Mech: Binds to ergosterol in fungal CM→pores→memb. leakage
Only one approved for use in eye
Diltiazem
Tx: Arrythmias except vent. arrythmias (class IV)
Mech: Ca channel blockers
Increase refractory period
Ampicillin
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
Carbapenems
Tx: Antibacterial–mixed infections
Penicillin analog
Small penicillinase resistant B lactam
Spectrum: Very broad
Route: IV
SE:
- Can enter CNS→Seizures
Aldosterone antagonists clinical use
- Used w/ other diuretics to prevent K loss
- To treat excess aldosterone production
What are the stool softeners?
Dioctal sodium sulfosuccinate
Mineral oil
Methotrexate pharmacodynamics
Act on specific enzymes
Homatropine
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
Methotrexate
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
- Can be dealt w/ by giving leucovorin-THFA analog
Propranolol
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
Sulfisoxazole
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
Longer lasting relatively selective B2 agonists
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
Relatively selective B2 agonists
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
Calcium carbonate
CaCO3
Antacid
Speed-rapid
Duration-medium
Neutralizing-high
SE:
- Constipating
- Hypercalcemia
Nitrofurantoin
Mech: Reduced by bacteria to a highly reactive molecule
Concentrates in urine
Use: UTI
SE:
- Cough
- Chest pain
- Brown urine
Amitriptyline
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
Hydroxyurea
Mech: Increase formation of fetal Hb (does not sickle)
SE: Mutagenic
Pregnancy category D
Ibritumomab
Tx: Cancer
Mouse MAB
Severe infusion rxn
Bismuth subsalicylate
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
Rimantadine
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
Griseofulvin
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.
Indomethacin
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
Basiliximab
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
Dobutamine
Tx: CHF
Class: Inotropic agents
Mech: Beta1 agonist
Effects: Increase force of contraction
Tranylcypromine pharmacodynamics
Act on specific enzymes
Adalimumab
Ada-li-mu-mab
Tx: RA
Immunosuppressant
Mech: Binds TNF
Vincristine and vinblastine
Tx: Cancer
Mech: Bind to microtubules and block cell mitosis
Route: IV
Natural product
Naloxone
Narcotic analgesic antagonist
Opiate receptor blocker
Naloxone-oxycodone combinations exist to make withdrawl easier
Heroin
Narcotic analgesic- semisynthetic
Originally to cure morphine addiction
5x stronger than morphine
Tacrolimus
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*
“Poetin” and “Pegin”
Epoietin alfa
Darbepoietin
Peginesatide
Tx: Anemia due to chronic renal failure or chemotherapy
Toxicities: Due to excess RBCs
- Increase BP
- Increase clotting
- MI
- Stoke
Bacitracin
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
Ginseng
Uses: Increase energy
No clear effect
Glucocorticoids
Effects: Inh. osteoblasts
So bone loss
Soy
Uses:
- Hyperlipidemia
- Osteoporosis
- Menopause
Decreases LDL
Decreases Menopausal symptoms
Mech: Metab. to estrogen like compound
SE: Allergic rxns
“-rudin”s
Bivalirudin
Desirudin
Tx: Anticoagulant
Synthetic analogs of hirudin
Clinical use: when patient has HIT
Skin grafts and reattaching body parts
Route: Injection
Sodium Bicarbonate
NaHCO3
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
Promethazine
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
Bevacizumab
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
Heparin
Effects: Act. osteoclasts
So bone loss
Fluoxetine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Ezogabine
Tx: Partial seizures
Mech: Open K channel
Venlafaxine
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.
alpha-methyl NE
Adrenergic agonist
Activates alpha2 receptors
Decrease symp outflow from CNS
Tx: hypertension
Other analogs used for glaucoma (Decrease pressure)
Isoniazid
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.
Lamivudine
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
Discontinuation→Increase hepatitis symptoms
Telbivudine
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE:
- Lactic acidosis
- Hepatomegaly
Discontinuation→Increase hepatitis symptoms
Antimycoplasma agents
NO CELL WALL!
So use non CW inhibitors:
Erythromycin
Tetracycline
Polymixin B
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*
Varenicline
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
Cinecalcet
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
Etanercept
Tx: RA
Immunosuppressant
Mech: Binds TNF
Route: SubQ (in comb. w/ other immunosupp)
Synthesized molecule
eTaNercept-binds TNF
Eptifibatide
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
Tapentadol
Narcotic and SSRI
Azithromycin
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——
Pancuronium
Antinicotinic agent
non-depolarizing neuromuscular blockers
Nizatidine
H2 blocker
Does not cross BB barrier
Effects:
- Blockade of H2 receptors→Decrease H secretion
- Histamine required to stim. acid secretion from parietal cells
-previr
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
Vilazodone
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Simethicone
Tx: Diarrhea
Mech: Changes gas surface tension of gas pocket in gut
Vancomycin
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
Loperamide
Tx: Diarrhea
Narcotic agent
Narcotic DOC for diarrhea
Mech: act a specific receptor
Acts ONLY in gut–no CNS effects
-pristin
Quinupristin (A+P site)
Dalfopristin (P site)
Mech: Inh. A and P sites
Always used together–synergistic
SE: Muscle pain
Spectrum: G+
Etodolac
NSAID
Anastrazole
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
What are the long acting designer insulins?
Detemir
Glargine
Penicillin G
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
Azathioprine
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
Denosumab
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
Cimetidine
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
Pyroxicam
NSAID
Fomepizole
Specific inhibitor of alcDH
Prolongs effects of alcohol
Mg(OH)2
GI Drug
Cathartic–Osmotic agent
AKA Milk of Magnesia
Beclomethasone
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
Amikacin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
Ipecac
Emetic–reflex stimulant
Mech: Act. receptors in GI mucosa
Instant severe vomiting
SE: Cardiotoxic
Fexofenadine
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
Hydralazine
Act directly on smooth muscle
Arterial vasodilator
Increase in cGMP→relaxes smooth m
SE:
- Slow acetylators→lupus like syndrome
Dipryridamole
Tx: Anticoagulant
Mech: Platelet inhibitor
Inhibits phosphodiesterase
Inh. enzyme that breaks down cAMP
Increased cAMP→Decrease platelet agg.
Furosemide
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
Kanamycin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
Pralidoxime
If given early can reduce any perm. damage caused by organophosphate AChE inhibitors
Warfarin
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
Castor oil
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Trimethoprim
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
Anakinra
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
Bedaquiline
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.
Abiraterone
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*
Valganciclovir
Antiviral agent
Tx: CMV (herpes virus)
CMV→retinitis+ blindness
Mech: Inhibits viral DNA pol
Prodrug-converted to ganciclovir by viral kinase
Alprostadil
Tx: ED
Injectable prostaglandin (PGE1) leads to vasodilation when injected directly into penis
Harvoni
DOC for HCV
Ledipasvir+sofosbuvir
Pramlintide
Tx: Diabetes
Amylin analogs
Mech: Activate amylin receptor→
Decrease gastric emptying
Decrease appetite
Route: SubQ before meals
SE:
- Severe hypoglycemia
- prAMLINtide=AMyLIN analog*
Cisplatin
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
Nabumetone
NSAID
Mycophenolate mofetil
Tx: Transplants and lupus
More specific replacement than azothioprine
Inh. enzyme inosine monophosphate DH→Inh. guanisine synth.
SE:
Bone marrow decrease
GI cell disruption
Anagrelide
Tx: Anticoagulant
Mech: Platelet inhibitor
Platelet count reducer
Decreases platelet formation, maturation, and #
Hydromorphone
Narcotic analgesic- semisynthetic
10x stronger than morphine
“Dilaudid”
Bisacodyl
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Cycloserine
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*
Spironolactone
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
Everolimus
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*
Tenofovir
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE:
- Lactic acidosis
- Hepatomegaly
Discontinuation→Increase hepatitis symptoms
Citalopram
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Isosorbide dinitrate
Tx: Angina
Slow release nitrate formulation
Can be given orally
Slow enough that effects occur before 1st pass metabolism
Bortezomib
and carfilzomib
Tx: Multiply myeloma
Mech: Proteasome/protease inh.
Enzyme inhibitors
Allows excess proteins to accumulate and kill myeloma
“Zomibs” inh. proteaZomes
Bleomycin
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)
Methadone
Narcotic analgesic- synthetic
Orally effective-liquid
Less euphoric
Given to wean off morphine
Same strength as morphine
Teriflunomide
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)*
Argatroban
Tx: Anticoagulant
Peptide from hirudin-diff structure, similar mech
Clinical use: when patient has HIT
Skin grafts and reattaching body parts
Route: Injection
Fulvestrant
Same as Tamoxifen
Tx: Cancer
Mech: Blocks estrogen receptor
SE:
- Cataracts
- Retinal changes
Ustekinumab
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.*
Dapsone
Antimycobacterial agent
Related to sulfonamides
Mech: Reversible inh. dihydropterate synthetase
Use: For mycobacterium leprae (leprosy
Famotidine
H2 blocker
Does not cross BB barrier
Effects:
- Blockade of H2 receptors→Decrease H secretion
- Histamine required to stim. acid secretion from parietal cells
Ticlopidine
Tx: Anticoagulant
Mech: Platelet inhibitor
ADP receptor blocker on platelet
SE:
- Neutropenia-loss of neutrophils
- Agranulocytosis
Polycarbophil
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Aspart
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
What agents bind TNF
Etanercept (RA)
Infliximab (RA,C)
Certolizumab (RA,C)
Adalimumab (RA)
Golimumab (RA, etc)
Think TNF=TNT (dynamite)
Explosions In Caves Affect Gollum
Procainamide
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
Yohimbe
Use: ED
Mech: Alpha 2 blocker in CNS
SE:
- Hypertension
- MAOI
- CNS excitation
- Tachycardia
- Tremor
Inhibitors of Na transport in DCT and collecting tubule SE
Hyperkalemia
Fenoldopam
Activate D1 receptors
Given IV for HT emergencies
Icosapent
Tx: Hyperlipidemia
Mech: Inhibit enzyme responsible for Trig synth
Not clear though
Maraviroc
Tx: HIV
Mech: Blocks binding site on macrophage preventing entry of virus
Fusion inhibitor
SE:
- Hepatotoxicity
- Allergies
- Increase MI
Glucocorticoids
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
Aldosterone antagonists SE
- hyperkalemia
- Spironolactone is a steroid and can have anti-androgenic effect (breast growth,etc)
- Eplerenone-fewer interactions w/ steroid receptors
Cromolyn sodium
“-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
Calcitonin
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
Sarin
Nerve gas-direct cholinergic agonist
Irreversible AChE inhibitors
MAO inhibitors
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)
Propranolol
Tx: arrythmias (Class II)
Mech: B1 blocker
Decreases pacemaker firing rate
SE:
- Bradycardia
- Hypotension
- B2 effects-asthma
Tramadol
Narcotic and SSRI
Exenatide
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
“Choles- or coles-“
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
Tolazamide
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
Bumetanide
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
Meperidine
Narcotic analgesic- synthetic
.5x as strong as morphine
No pupil constriction
Levetiracetam
Tx: Partial seizures
Mech: Unknown
Meropenem
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
Alkylating agents
Names and mech.
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
Iomitapide
Tx: Hyperlipidemia
Mech: Inh assembly of VLDL in liver
Apolipoprotein+cholesterol→(X)→VLDL
Enzyme for assembly is also a transporter
SE: hepatotoxicity
Other NSAIDs
_Pyr_os _ne_ed _e_xcess _f_ire
_Pyr_oxicam _n_abumetone _e_todolac -_f_enac
Rituximab
Tx: Chronic lymphocytic leukemia and RA
Mech: vs CD20
Etoposide
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***
Clemastine
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
Succinylcholine
Direct nicotinic agonist
Antinicotinic agent-Depolarizing neuromuscular blocker
Long duration of action compared to acetylcholine
Initially activates receptor, eventually muscle hyperpolarization then paralysis
Vigabatrin
Tx: Partial seizures
Mech: Act GABA
ViGABAtrin
Linaclotide
GI Drug
Cathartic–Secretion enhancer
Mech: Activate guanylate cyclase
Increase Cl secretion in stomach
Methotrexate
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
- Inh. lots of folic acid dependent processes, especially in cells w/ rapid turnover (at high doses):
More selective B blockers
Metoprolol
Acebutolol
Atenolol
Betaxolol
Nebivolol
SE:
- Fewer CNS effects
- Bradycardia
- Fatigue w/ exercise
Prednisone
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
Penicillin V
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
Pregabalin
Tx: Partial seizures
Mech: Acts on Ca channels
Prednisone
Tx: Cancer-leukemias and lymphomas
Mech: Inh. immune system fxns (refer to other lecture)
SE: lots of them
Ranitidine
H2 blocker
Does not cross BB barrier
Effects:
- Blockade of H2 receptors→Decrease H secretion
- Histamine required to stim. acid secretion from parietal cells
Demecarium
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
-amivir
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
Dioctal sodium sulfosuccinate
GI Drug
Cathartic–Stool softener
Detergent
Mech: Emulsifies contents of colon
First Generation H1 blockers
Diphenhydramine
Clemastine
Chloropheniramine
Hydroxyzine
Promethazine
Tripelennamine
Acetic acid derived NSAIDs
Double A (Aaron) slobbers into titties
Acetic Acid: Sulindac indomethacin tolmetin
Recombinant interferon alpha
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.
Codeine
Narcotic analgesic- narcotic analogs
Partial agonist-low anti-nociceptive effects
Given orally
Greater effect on coughing-anti-tussive effect
Mometasone
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
Endothelin blockers
“-entan”s
Tx of pulmonary arterial hypertension
SE:
- Fetal damage
- Testicular atrophy
- Hepatic toxicity
“-fenac”s
diclofenac
bromfenac
Nepafenac
NSAID
Gramicidin
Antibacterial agent
Mixture of 3 diff peptide AB
Mech: forms pores in bacterial CM
Route: topical
NEVER give IV–toxic
Spectrum: G+
Cidofovir
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
Aspirin pharmacodynamics
Act on specific enzymes
Cilostazol
Tx: Anticoagulant
Mech: Platelet inhibitor
Inhibits phosphodiesterase
Inh. enzyme that breaks down cAMP
Increased cAMP→Decrease platelet agg.
(Apo)morphine
Emetic–central stimulant
Mech: Stimulates DA sites in CTZ
Diazepam
Tx: Seizures
Class: Benzos
Mech: GABA
IV to treat status epilepticus
Lithium
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
Mirtazapine
Antidepressant
Naphazoline
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
Nafcillin
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
Dronabinol
Anti-emetic–THC derivative
Mech: Bind cannabinoid receptor
SE: Increased appetite
Malathion
Insecticide-cholinergic agonist
Irreversible AChE inhibitors
Minoxidil pharmacodynamics
Agents that act on ion channels
“-kinase”s
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
Terbinafine
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*
Antipsychotic drugs used to treat mania
Phenothiazine
Haloperitol
Benzos
Lispro
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
-fungin
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
Sulindac
NSAID
Acetic acid derivative
Esmolol
Tx: arrythmias (Class II)
Mech: B1 blocker
More rapid onset of action
SE:
- Bradycardia
- Hypotension
- B2 effects-asthma
St Johns Wort
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
Olestra
Fake fat
SE: Butt leakage
Desvenlafaxine
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.
Gemfibrozil
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
-sala-
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
Itraconazole
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
atracurium
Antinicotinic agent
non-depolarizing neuromuscular blockers
Non specific B1 and B2 blockers
Propanolol
Timolol
Levobunolol
Certeolol
Metipranolol
Leuprolide
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
Imipramine
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
Minoxidil
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
Imitinib pharmacodynamics
Act on specific enzymes
Disulfiram
Inhibits acet.DH→buildup of acetaldehyde
Get severe hangover right away
Fondaparinux
Tx: Anticoagulant
Synthetic heparin like drug
T1/2=17 hrs
Acts only on Xa
Can cross placenta
Can’t bind protamine
Given SubQ
Protease inh.
-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
Omalizumab
Tx: Asthma
Mech: Blocks IgE receptor
Receptor blocker
Route: Injection–like all monoclonal antibodies
Rocuronium
Antinicotinic agent
non-depolarizing neuromuscular blockers
Most common one
Nifedipine pharmacodynamics
Agents that act on ion channels
What are the short acting designer insulins?
Regular human insulin
Lispro
Aspart
Glulisine
2-5 hrs
Nabilone
Anti-emetic–THC derivative
Mech: Bind cannabinoid receptor
SE: Increased appetite
-methasone
Dexamethasone
Betamethasone
Immunosuppressive potency=15
Relative minerallocorticod activity=
Duration: 36-54hrs
Enfuvirtide
Tx: HIV
Mech: binds to specific site on virus that binds to target
Fusion inhibitor
SE: Insomnia
Disopyramide
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
Prednisone
+
Prednisolone
Immunosuppressive potency=4
Relative minerallocorticod activity=.25
Duration: 18-36hrs
Prednisone is a prodrug:
- Must be metab by P450 (in liver)
- Not effective topically
alpha-methyl tyrosine
Tx of pheochromocytoma
Central and peripheral effects
Inhibits tyrosine kinase–preventing synthesis NE and epi
Adefovir
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE: Liver and renal damage
Discontinuation→Increase hepatitis symptoms
Sotalol
Tx: arrytmhias (Class III)
Mech: K+ channel blocker
Also a beta blocker
Methylnaltrexone
Narcotic analgesic antagonist
Opiate receptor blocker
Deferoxamine
Tx: Acute iron OD
Mech: Iron chelator
De-Fer-oxamine
_De_toxes _Fer_rous overdose
Amiodarone
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
Meclizine
Anti-emetic–Antihistamine
Mech: Block H1 receptor
SE: Anticholinergic effects
Which antihistamines are used as anti-emetics?
Diphenhydramine
Dimenhydramine
Meclizine
Cyclizine
Valerian
Uses: Sedative
Mild sedative effect
Mech: Increase GABA
SE:
- Hepatotoxicity
- Dont use w/ anti-dep
Other tx of bipolar
Most are antiseizure:
- Valproic acid
- Carbamazepine
- Limotripene
Acetazolamide
Aripripazole-anti-psychotic
Calcium channel blockers
“-ipine”s
Inhibit Ca influx into vascular smooth m
Prevent vasoconstriction
SE:
- Heartburn
- May worsen heart failure
Ibuprofen
and other -pro-
Naproxyn
Fenoprofen
Ketoprofen
Flurbiprofen
Oxaprozin
Suprofen
Tx: Analgesic, anti-inflam
Mech: Inh COX
Propionic acid derivative
Sofosbuvir
Antiviral agent
Tx: Hepatitis virus (esp Hep C)
Mech: Inh HCV RNA dep RNA pol
Third Generation antidepressants
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.
Lomustine
Tx: Cancer
Mech: Alkylating agent
- Add alkyl group to DNA
- Causes DNA cross linking, inhibits cell replication, and RNA synth
Prodrug given IV
Angina definition and general tx methods
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
Isoproterenol
“-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
Vorapaxar
Tx: Anticoagulant
Mech: Platelet inhibitor
Thrombin receptor blocker on platelet
SE: Use carefully w/ pts w/ history of intracranial bleeding
Ipratropium
*“-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
Doxorubicin
And other rubicins
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*
Ketoconazole
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_*
Gabapentin
Tx: Partial seizures
Mech: Act GABA
GABApentin
Tacrine
Indirect cholinergic agonist
Alzheimer’s tx
Verapamil
Tx: Arrythmias except vent. arrythmias (class IV)
Mech: Ca channel blockers
Increase refractory period
Imitinib
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)
Infliximab pharmacodynamics
Act on specific enzymes
Kola nut
Caffeine
Increased HR
Insomnia
Posaconazole
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
Imipenem
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
Abciximab
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
Phenoxybenzamine
Adrenergic antagonist
alpha1 receptor blocker
Tx: hypertension
Delavirdine
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.
Chlorpheniramine
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
Isocarboxazid
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)
Acarbose
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.*
Buproprion
Antidepressant
Aztreonam
Antibacterial
Class: Monobactam
Route: IV or IM
Not affected by lactamases
Spectrum: Aerobic G- organisms
Not cross reactive w/ allergic pts
SE:
- Seizures
Compazine
Anti-emetic
Mech: DA blocker
*Related to anti-psychotic drugs *(phenothiazine)
SE: Extrapyramidal effects
Thiazide diuretics mechanism
Inhibits Na+ transport out of the DCT. H20 follows and both are excreted
High TI
works w/in 2 hours
Angiotensin receptor blockers
“-Artan”s
SE:
- Decrease secretion of aldosterone
- Fetal abnormalities
- All agents that alter angiotensin system
- Pregnancy risk X
-floxacin
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
Bran
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Cascara
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Hydroxychloroquinone
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
Bethanechol
Direct muscarinic agonist
Antifungals for ringworm
Tolfnaftate
Ciclopirox
Terbinafines and other “fines”
Route: Topical
Echothiophate
Indirect cholinergic agonist
Lasts for 100s hours
Phosphorylates AChE
-glitazone
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
Atropine
Antimuscarinic agent
Blocks muscarinic receptor
Lasts 7-10 days
Clindamycin
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
Ciclesonide
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
Diphenhydramine
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
Alpha-methyl DOPA
Central alpha-2 agonist
Prodrug: metabolized to alpha-methyl NE
SE:
Depression
Drowsiness
Dry mouth
Impaired Ejac.
Hepatic dysfunction
Alfentanil
Narcotic analgesic- synthetic
500-600x stronger than morphine
Sucralfate
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
Aluminum hydroxide
Al(OH)3
Antacid
Speed-slow
Duration-long
Neutralizing-low
SE:
- Constipation
- Adsorbs drugs
- Loss of phosphate
- Al toxicity
Tobramycin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
(Hydro)Chlorothiazide
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
Metformin
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*
Cilastatin
Given w/ impenem
Prevents nephrotoxic product by inh. enzyme
Sirolimus
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*
Agents that activate B2 receptors
“Nols and rols”
Metaproterenol
Terbutaline
Fenoterol
Albuterol
Tx: asthma
Causes bronchodilation
Alvimopan
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
Flutamide
and other “lutamides”
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*
What induces the release of NE from nerve terminals?
Indirect acting amines:
Amphetamine, methamphetamine
Tyramine
Phenylpropanolamine
Pseudoephedrine
-tidine
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
Mipomersen
Tx: hyperlipidemia
Antisense oligonucleotide
Mech: Binds to mRNA of ApoB
Prevents Apo from being synth
*(Apolipoprotein)*+cholesterol→VLDL
Must be given by injection
Duloxetine
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.
Magnesium hydroxide
Milk of magnesia
Antacid
Speed-slow
Duration-medium
Neutralizing-high
SE:
- Laxative
- Some Mg toxicity
Zonisamide
Tx: Partial seizures
Mech: Inh. Na
Carbamazepine
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
Eribulin
Tx: Cancer
Mech: inh. microtubules-prevents mitosis, causes apoptosis
Fully synthetic
Digoxin
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
Lidocaine
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
MgSO4
GI Drug
Cathartic–Osmotic agent
Neostigmine
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
Rufinamide
Tx: Partial seizures
Mech: Inh. Na
“-xaban”s
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
Chloramphenicol
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
Aspirin
Tx: Anticoagulant
Mech: Platelet inhibitor
COX (enzyme) inhibitor
Inhibits TXA2 synth
Decreases platelet aggregation
Infliximab
Tx: IBS
Mech: Binds TNF alpha
High Ceiling diuretics clinical use
- Pts who dont respond to thiazides
- Life threatening edema (pulmonary or cerebral)
- Compromised renal fxn
Heparin pharmacodynamics
Act on specific enzymes
Escitalopram
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Orlistat
Tx: Hyperlipidemia
Mech: Inh GI and pancreatic lipase
Decrease fat absorption from gut
SE: Loose stool
Paclitaxel
and other “-taxel”s
Tx: Cancer
Mech: Forms abnormal microtubules
Natural-from western yew tree. But now purely synthetic
”-_t_axels” make _t_errible _t_ubules
Acetazolamide
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
Rifampin
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
Scopolamine
Anti-emetic–anti-cholinergic
Mech: Block muscarinic receptor
Route: Patch
SE:
- Dry
- Drowsy
- Etc.
Tiagabine
Tx: Partial seizures
Mech: Act GABA
Tiagabine
Golimumab
Tx: RA, Ulcerative colitis, psoriatic arthritis
Immunosuppressant
Mech: Binds TNF
Natalizumab
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
Torsemide
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
Dactinomycin
Tx: Cancer
Mech: Intercalates w/ DNA and interferes w/ mRNA synth
Oxycodone
Narcotic analgesic- semisynthetic
Partial agonist-available in oral form as oxycontin
0.5x as strong as morphine
“-parin” drugs excluding heparin
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.
Prazosin
Adrenergic antagonist
alpha1 receptor blocker
Tx: hypertension
Reserpine
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
Propranolol pharmacodynamics
Agents that act on cell membrane receptors
Ethacrynic acid
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
Methylcellulose
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Palivizumab
Antiviral agent
Tx: RNA virus (RSV)
Mech: vs antigenic site of RSV–blocks fusion of virus w/ target
Only used prophylactically
Tolmetin
NSAID
Acetic acid derivative
Acyclovir
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
Tiotropium
*“-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
Naltrexone
Narcotic analgesic antagonist
Opiate receptor blocker
“Osin”s
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
Vortioxetine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Non-depolarizing neuromuscular blockers that are antinicotinic agents are derived from?
curare
Omeprazole pharmacodynamics
Agents that act on transport systems
-zolid
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
Tripelennamine
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
Tissue plasminogen activator (TPA)
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
Detemir
Tx: Diabetes
Designer insulin
Long acting (24+ hrs)
Determined to get large (that a long time)
Detemir +glargine=long acting insulins
Tofacitinib
-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
Prazosin pharmacodynamics
Agents that act on cell membrane receptors
Erythromycin
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*
Fenofibrate
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
Nitroglycerin pharmacodynamics
Act on specific enzymes
Ethanol as a diuretic
Mech: decrease release of ADH
Tranexamic acid
Tx: Hemostatic agent (enhance clotting)
Mech: Inhibits plasminogen activation
Enzyme inhibitor
Binds to plasminogen in plasma
Cranberry
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
Cimetidine pharmacodynamics
Agents that act on cell membrane receptors
Famciclovir
Antiviral agent
Tx: herpes simplex and zoster
Mech: prodrug converted to acyclovir analog
Phenelzine
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)
Pilocarpine
Direct muscarinic agonist
Regular human insulin
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Afrezza is the inhaled form
Digoxin
Emetic–central stimulant
Mech: Stimulates DA sites in CTZ
Tamoxifen
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
Amphotericin B
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
Diazoxide
Acts directly on smooth muscle
Opens K channels→hyperpolarization
Inhibits insulin release from B cells in pancreas
Lubiprostone
GI Drug
Cathartic–Secretion enhancer
Mech: Acts on PGE receptor
PGE1 derivative
Also acts on Cl channel in intestine
Paroxetine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
cytarabine
Tx: Cancer
Mech: Inh. DNA polymerase
Prodrug–Pyrimidine analog
Ezetimibe
Tx: Hyperlipidemia
Mech: Blocks cholesterol transport
SE: Flatulence
“-oxacillin”s
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
Polyethylene glycol
GI Drug
Cathartic–Osmotic agent
DOC for colonoscopy
Efavirenz
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*
Phenobarbital
Tx: All seizures EXCEPT petit mal
Class: Barbituate
Mech: Act. GABA
SE:
- Sedation
- Induces P450
Belatacept
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.
Fluticasone
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
Miglitol
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
Chlorpropamide
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
Mannitol
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
Nefazodone
Antidepressant
Fluconazole
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
Retapamulin
Antibacterial agent
Mech: inh. peptidyl transferase
Route: Topical
Use: skin staph or strep inf.
What are the gastric irritants used as cathartics?
Cascara
Senna
Castor oil
Bisacodyl
Fidaxomycin
Antibacterial agent
Mech: Inh. C. dificile RNA pol
Orally–Not systemically absorbed
Target: C. dificile
Agents that activate beta1 receptors
NE
Dobutamine
Clonidine
Central alpha-2 agonist
SE:
Depression
Drowsiness
Dry mouth
Impaired Ejac.
Unlabeled uses:
- Fibromyalgia-unspecified neuronal pain
- Insomnia
- Tourettes
- Opiate withdrawal
Lincomycin
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
Topiramate
Tx: Partial seizures
Mech: Act. GABA
Aspirin
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
Heparin
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
Theophylline
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
Gli–ide
or
Gly–ide
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
Sugammadex
Reverses block by rocuronium by binding directly
Topotecan
and irinotecan
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***
Combined alpha and beta blockers
Block alpha1, beta1, and beta2
Labetalol
Carvedilol
SE:
- Postural hypotension
- Dry mouth
Certolizumab
Tx: RA, Chron’s
Immunosuppressant
Mech: Binds TNF
Dexamethasone
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
-glinide
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
Bisphosphonates
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
Acamprosate
Decreased craving for ethanol
Adenosine
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
First Gen Antidepressants
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
Garlic
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.
Glargine
Tx: Diabetes
Designer insulin
Short acting (24+ hrs)
Determined to get large (that a long time)
Detemir +glargine=long acting insulins
Nystatin
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
Daptomycin
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
How does ethanol work?
Binds non-specifically to large molecules
Protein denaturance
Ergocalciferol (D2)
Tx: Ca disorders
Mech: Vit D analog
Less potent than calcitriol
SE: Hypothyroidism
Aminobisphosphonates
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
Flucytosine
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
Ipratropium
Antimuscarinic agent
Blocks muscarinic receptor
Methylxanthines
Caffeine
increase glomerular filtration rate
Glulisine
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Netilmicin
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
Acetazolamide
Tx: Seizures
Mech: May increase CO2 in brain→Decrease activity
Entecavir
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE:
- Lactic acidosis
- Hepatomegaly
Discontinuation→Increase hepatitis symptoms
Metoclopramide
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 *
“-grel”s
Tx: Anticoagulant
Mech: Platelet inhibitor
ADP receptor blocker on platelet
Same as ticlopidine-diff is pharmacokinetics: rapid onset, shorter T1/2
Epinephrine
Tx: Asthma
Bronchodilator–DOC for short term relief
Mech: Acts on all adrenergic receptors
SE
- Tons of them
- Increase HR+vasoconstriction→increase BP
Fluvoxamine
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Fosfomycin
Antibacterial
Class: Non B lactam CW inhibitors
Mech: Blocks synth of NAM
Spectrum: Aerobic G-
Use: Uncomplicated UTI
SE:
- Diarrhea–killing bacteria in gut
Hydroxyzine
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
Ginko
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
Atropine
Tx: Diarrhea
Anti-cholinergic agent
Mech: Blocks muscarinic receptor
SE: Many systemic
“-vancin”s
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
Acetaminophen
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
-glutide
**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*
Ticarcillin
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
Nicotine
Direct nicotinic agonist
Second generation H1 blockers
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
-gliflozin
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
Cyclopentolate
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
What are the bulk adding agents?
Bran
Methylcellulose
Polycarbophil
Psyllium
-gliptin
or
-glyptin
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.*
Nevirapine
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
Carbenicillin
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
Sumatriptan
and other “-triptan”s
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
Alpha galactosidase
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**
Milnacipram
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.
Sulbactam
Mech: Bind to and inh. B lactamase
Non antibiotic B-lactam ring compounds
Amantadine
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
Aminocaproic acid
Tx: Hemostatic agent (enhance clotting)
Mech: Inhibits plasminogen activation
Enzyme inhibitor
Binds to plasminogen in plasma
Route: Oral or injection
“-afils”
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
Teriparitide
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
Donepezil
Indirect cholinergic agonist
Alzheimer’s tx
What are the osmotic cathartics?
MgSO4
Mg(OH)2
Polyethylene glycol
Remifentanil
Narcotic analgesic- synthetic
500-600x stronger than morphine
Sodium Valproate
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
-gravir
Tx: HIV
Mech: Inh. HIV-1 integrase
Inh. insertion of viral genome into human
Prevents propagation
Infliximab
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*
Physostigmine
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
Cyclizine
Anti-emetic–Antihistamine
Mech: Block H1 receptor
SE: Anticholinergic effects
Glyceryl Trinitrate (nitroglycerin) (GTN)
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
Phenylephrine
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
-virine
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
Isophane
Tx: Diabetes
Designer insulin
Protamine insulin
Intermediate acting
Nitroprusside
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
Antibiotic combo for H pylori infection
GI drug-Enhance mucosal defense
Metronidazole
+/-
Amoxicillin
+/-
Clarithromycin
+/-
Tetracycline
Ixabepilone
Tx: Cancer
Mech: Binds to microtubules
Natural product
- Ixabepilone *
- Pixabepilone*
- Pixy sticks=tube=microtubules*
- Yeah this one is a stretch…*
Immunosuppressants for IBS
Methotrexate
Cyclosporine
Fentanyl
Narcotic analgesic- synthetic
80-100x stronger than morphine
Senna
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Dabigatran
Tx: Anticoagulant
Mech: Direct thrombin inhibitor
Enzyme inhibitor
Route: Oral
Kinetics:
- Prodrug
- Onset w/in 1 hr
- P450 inhibitor may impact
SE-hemorhhage
Telithromycin
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.
Lacosamide
Tx: Partial seizures
Mech: Inh. Na
Tropicamide
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
Niacin
aka Vit B3
aka Nicotinic acid
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
Diphenhydramine
or
Dimenhydramine
Anti-emetic–Antihistamine
Mech: Block H1 receptor
SE: Anticholinergic effects
Ma huang (ephedra)
Use:
- Weight loss
- Nasal congestion
- Asthma
- Increase athletic performance
Strong CNS stimulant
SE:
- Stroke
- Hypertension
- MI
Fluoxetine pharmacodynamics
Acts on transport systems
Gentamycin
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
Scopolamine
Antimuscarinic agent
Blocks muscarinic receptor
Lasts 3-7 days
Tetracycline
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
Aliskiren
Renin inhibitor
SE:
- Fetal damage
- Diarrhea
- Cough
- Angioedema
-setron
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
Thiazide diuretics SE and other effects
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
Cortisone
+
Hydrocortisone
Immunosuppressive potency=1
Relative minerallocorticod activity=1
Duration: 8-12hrs
Cortisone is a prodrug:
- Must be metab by P450 (in liver)
- Not effective topically
Scopolamine
Tx: Diarrhea
Anti-cholinergic agent
Mech: Blocks muscarinic receptor
SE: Many systemic
Amoxicillin
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
Sitostanol
Tx: Hyperlipidemia
Mech: Looks like cholesterol–blocks uptake
Sufentanil
Narcotic analgesic- synthetic
500-600x stronger than morphine
Codeine
Tx: Diarrhea
Narcotic agent
Mech: act a specific receptor
Not generally used for obvious reasons
Mupirocin
Mech: Binds to bacterial isoleucyl tRNA synthetase
Route: Topical
Use: Staph inf.
Voriconazole
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
“-statin”s
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
Sertaline
2nd gen antidepressant
Mech: SSRIs
SE:
GI upset
Nausea
Insomnia
Headache
Decreased libido
Echinacea
Use:
- Upper resp. inf.
- Wound healing
- Antifungal
Can decrease sympt. of flu if used early
SE:
- Allergies
- Related to ragweed
Abatacept
Tx: RA
Immunosuppressant
Mech: binds to and inh. CD80, CD86 receptors
Affects T cell activation
ABatacept CD80+86 receptors
_A_batacept for _A_rthritis
Cyclosporine
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*
Procaine pharmacodynamics
Agents that act on ion channels
SE of cephalosporins
Allergic cross activity w/ penicillin sensitive pts
Possibility of superinfection
Celecoxib
Cele-cox-ib
Selective cox(2) inhibitor
Tx: Analgesic and anti-inflam
Cetirizine
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
H2 blockers
Names
“-tidine”s
Cimetidine
Ranitidine
Famotidine
Nizatidine
*Only diff amongst all is that cimetidine has anti-androgenic effects
Tolbutamide
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
Trastuzumab
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*
Specific B1 receptor blockers
“olol”s
Metoprolol
Acebutolol
Alprenolol
Atenolol
Esmolol
Betaxolol
Nebivolol
These decrease HR
How do anticancer drugs work?
Binds non-specifically to large molecules
Raloxifene
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.)
6-mercaptopurine
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*
High Ceiling diuretics SE
- 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
Aldosterone antagonists mech
Blocks aldosterone receptor
Aldosterone is responsible for synth of Na-K exchanger
Takes days to be effective
Neomycin
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
Aldosterone antagonists
K sparing diuretics
Spironolactone
Eplerenone
Insulin
Agents that act on cell membrane receptors
Streptomycin
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
- Neuromuscular blockade
- Strippers fornicate*
- Strep. FORNICAT*
Fetal damage
Ototox.
Renal tox
Negative (G-)
Irr. bind 30s
Cidal
*ACh block *
tRNA can’t bind to mRNA
- *
Triamcinolone
Immunosuppressive potency=4
Relative minerallocorticod activity=.25
Duration: 18-36hrs
Mexiletine
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
Zileuton
Tx: Asthma
Mech: Inh. 5-lipoxygenase
Blocks leukotriene synthesis
Enzyme inh.
SE: increases liver enzymes
zileutoN for eNzyme inhibitor
Desloratadine
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
Rilonacept
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*
Crofelemer
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*
