pharm Flashcards
triptans mechanism
serotonin agonists
cause vasoconstriction
modulate neurotransmission in trigeminal nerve
should be taken as soon as the headache starts
contraindications to triptans
vasoconstricts; do not give in pregnancy or CAD, or prinzmetal angina
DUMBBELSS
Diarrhea, urination, miosis, bradycardia, bronchospasm, excitation of skeletal muscle (ACh at NMJ), lacrimation, salivation sweating (ACh despite being a SNS function)
Endogenous stim at mu receptor
beta endorphin
endogenous stim at delta receptor
enkephalin
endogenous stim at kappa receptor
dynorphin
anticholinergic effects: atropine
hot as a hare (hyperpyrexia), red as a beet (flushing), blind as a bat (mydriasis), dry as a bone (no salivation), mad as a hatter (delirium), bloated as a toad (constipation), tachycardia
on the darn toilet: drugs that treat urge incontinence
oxybutinin, tolterodine, darifenacin and solifenacin, trospium; anticholinergics
physostigmine
anticholinesterase (indirect cholinergic agonist)
pilocarpine
direct muscarinic agonist
oxybutynin
muscarinic antagonist for urge incontinence
donepezil
anticholinesterase
pralidoxime
regenerator of AChE
bethanecol
cholinergic agonist
neostigmine
anticholinesterase inhibitor
darifenacin
muscarinic antagonist
ipratropium
muscarinic antagonist
tropicamide
muscarinic antagonist
benztropine
muscarinic antagonist
scopolamine
muscarinic antagonist for motion sicknesss and decreased salivary secretion in ventilated patients
edrophonium
anticholinesterase
tolteridine
muscarinic antagonist
trospium
muscarinic antagonist
rivastigmine
anticholinesterase, used in AD
homatropine
muscarinic antagonist
pyridostigmine
anticholinesterase
carbachol
cholinergic agonist
nonselective beta blockers
propanolol, timolol, nadolol
selective beta1 blockers
metoprolol, atenolol
partial agonists
acebutol (beta-1 only), pindolol (alpha and beta)
alpha and beta blockers
carvedilol, labetalol
glaucoma drugs
timolol, nadolol
opioid cough suppressant commonly used with the expectorant guaifenesin
dextromethorphan (DM)
opioid used in the treatment of diarrhea
loperamide, diphenoxylate
opioid receptor antagonist
naloxone, naltrexone
non-addictive weak opiod agonist
tramadol
partial opioid agonist that causes less respiratory depression
butorphanol
hemicholinium
inhibits choline - sodium transport into cholinergic axons for ACh synthesis
Vesimacol
inhibits ACh packaging into vesicles
Botulinum
inhibits presynaptic ACh vesicle release for flaccid paralysis
Black widow spider toxin
promotes ACh release from presynaptic terminal for spastic paralysis
Metyrosine
tyrozine hydroxylase inhibitor
reserpine
inhibits DOPA decarboxylase (conversion of DOPA to DA)
Bretylium, guanethidine
inhibit NE release from presynapse
Tyramine, amphetamine, ephedrine
promotes NE release from presynapse
Cocaine, TCA, amphetamine
inhibits NE reuptake
ATII
promotes NE release
alpha2 agonists
inhibit NE release from presynapse
Disulfiram- like reaction
p. 95, 260
metronidazole, certain cephalosporins, procarbazine, 1st generation sulfonylureas
CYP450 inducers
Guiness, coronas, PBRs induce chronic alcoholism
griseofulvan, carbamazepine, phenytoin, barbiturates, rifampin, st. john’s wart, chronic alcoholism
CYP inhibitors
CRACK AMIGOS:
ciprofloxacin, ritonavir, amiodarone, cimetidine, ketoconazole, acute alcohol use, macrolides, isoniazid, grapefruit juice, omeprazole, sulfonamides
Flushing
vancomycin, niacin, adenosine, dihydropyridine CCBs
Coronary vasospasm
cocaine, amphetamines, triptans (sumatriptan), ergotamine
dilated cardiomyopathy
doxorubicin, daunorubicin
Torsades de pointes
potassium channel blockers (class III), sodium channel blockers (class IA), macrolides, haloperidol, chloroquine, protease inhibitors
thrombocytopenia after heparin
HIT. cimetidine can also cause thrombocytopenia
Agranulocytosis
clozapine, carbamazepine, colchicine, PTU, Methimazole, dapsone
Aplastic anemia
chloramphenicol, benzene, NSAIDs, PTU, methimazole
Gray baby
chloramphenicol 2/2 insufficient UDP- glucaronyl transferase
Hemolysis in G6PD deficient patients
isoniazid, sulfonamides, primaquine, high dose asa, ibuprofen, nitrofurantoin, dapsone, fava beans, naphthalene
thrombosis
oral contraceptives
pulmonary fibrosis
amiodarone, busulfan, bleomycin
cough
ACEI 2/2 bradykinins
pseudomembranous colitis
clindamycin, amoxacillin, ampicillin
hepatic necrosis
halothane, acetaminophen, valproic acid, amanita phalloides
hepatitis
INH
tertiary adrenal insufficiency
corticosteroid withdrawal
gynecomastia
spironolactone, digozin, estrogens, cimetidine, chronic alcohol use, ketoconazole, marijuana (some drugs cause awesome knockers, or stacked where THC)
hot flashes
tamoxifen, clomiphene SERMs
hypothyroidism
amiodarone, lithium, sulfonamides
gout
diuretics (loop and thiazide), niacin, cyclosporine, pyrazinamide
gingival hyperplasia
phenytoin, verapamil
osteoporosis
corticosteroids, heparin
photosensitivity
sulfonamides, amiodarone, tetracycline (SAT for photo)
SJS
seizure drugs and penicillin ethosuximide, carbamazepine, lamotragine, phenytoin, phenobarbital, sulfonamides, penicillins, allopurinol CLAPPPERS carbamazepine lamotragine allopurinol phenytoin phenobarbitol pcn ethosuximide RASH sulfa drugs
drug- induced lupus
SHIPP
sulfonamides, hydralazine, INH, phenytoin, procainamide
tendinitis, cartilage damage
fluoroquinolones
interstitial nephritis
NSAIDs, furosemide, antibiotics
DI
lithium, demeclocycline
treat with HCTZ, amiloride
Fanconi
expired tetracycline, heavy metal exposure, wilson
hemorrhagic cystitis
cyclophosphamide, ifosfamide
Parkinson- like syndrome
metaclopramide, antipsychotics, reserpine
cinchonism
dizziness, HA, vision changes, tinnitus
quinidine, quinine
seizures
buproprion, imipenem, cilastatin, INH, tramadol, metaclopramide, benzodiasepines, EtOH w/drawal
tardive dyskinesia
antipsychotics, metoclopramide
disulfiram- like reaction
metronidazole, cephalosporins, procarbazine, first- generation sulfonylureas, disulfiram
nephrotoxic and neurotoxic
aminoglycosides, cisplatin, polymyxins
nephrotoxic and ototoxic
aminoglycosides, vancomycin, loop diuretics, cisplatin
anticholinergic side effects
atropine, TCAs, H1 blockers (diphenhydramine), low- potency neuroleptics (thioridizine, chlorpromazine)
eliminated at a constant rate (zero order)
PEA:phenytoin, ethanol, aspirin
low therapeutic index
warfarin, digoxin, lithium, phenobarbital
how does sildenafil lead to erection?
inhibits cGMP phosphodiesterase> increase in cGMP> relaxation of smooth muscle in corpus cavernosum> increased bloodflow> erection
pseudomonas aeruginosa
fluoroquinolones (ciprofloxacin, levofloxacin ticarcillin piperacillin cefepime ceftazidime carbapenems (imipenem, meropenem)
Triple therapy H. Pylori
PPI
Clarithromycin
Amoxicillin or metronidazole (if allergic to PCN)
Quadruple therapy H Pylori
PPI
Bismuth
Metronidazole
Tetracycline
adenosine
increases outward potassium current, hyperpolarization of cells, decreases intracellular calcium (stops the heart transiently)
precursor of 6MP
azathioprine
ab that binds CD3 on T cells
muromonab
ab that binds IL2 receptor on activated T cells
daclizumab
inhibits inosine monophosphate dehydrogenase
mycophenolate mofetil
inhibits calcineurin leading to loss of IL2 production and blockage of T cell differentiation and activation
cyclosporing, tacrolimus, pimecrolimus
metabolized by xanthine oxidase, thereby increasing allopurinol toxicity
azathioprine, and 6MP
ACEI
inhibits angiotensin vasoconstrictor production thereby preventing vasoconstriction.
Dropping angiotensin keeps bradykinin around longer leading to more vasodilation
Used in HTN, CHF to prevent LV remodeling
Post MI
Diabetic kidney disease- reduced proteinuris, reduced progression of nephropathy
overall, well tolerated.
SE:
dry hacking cough
(due to bradykining)
angioedemia (complicated possibly by airway compromise)
cough
angioedema
kyperkalemia, especially if also on a potassium- sparing diuretic.
decreased GFR: renal insufficiency
BL renal artery stenosis is a contraindication
teratogenesis- pregnancy is a contraindication
ARB
candesartan, losartan
side effects: teratogenesis, hyperkalemia, renal insufficiency
NO cough (no bradykinin)
but can cause angioedema sometimes
if pt on ACEI gets angioedema then, you can’t just sweitch
Aliskerin
renin inhibitor
hyperkalemia, renal insufficiency, contraindicated in pregnancy
NOT indicated in CHF or MI.
ONLY FOR HTN
Calcium channel blockers- dihydropyridines
amlodipine, felodipine, nicardipine, nifedipine, nisoldipine
act on vascular smooth muscle to cause vasodilation.
indicated to treat HTN, angina, vasospasm (Prinzmetal’s angina, Raynaud), esophageal spasm, migraine prophylaxis, cluster HA
adverse effects: peripheral edema, flushing, dizziness, constipation, deflex tachycardia
CCB- non-dihydropyridine
acts on heart
diltiazem, verapamil
verapamil acts at calcium channels of pacemaker cells in the heart. no effect on systemic vasodilation
Diltiazem is less specific, acting at calcium channels of heart and vessels. commonly used in patients with angina to slow the heart and decrease o2 demand
also used to control HR in patients with ventricular fibrillation and other tachycardias
adverse effects: cardiac depression, AV block, flushing, dizziness, constipation
Hydralazine
increases cGMP inside of smooth muscle cells, dilating arterioles> veins, thereby decreasing afterload.
uses include hypertensive urgency and emergency. HTN in pregnancy
side effects: reflex tachycardia (don’t give if coronary disease), may need to give with beta blocker
fluid retention
nausea headache
drug- induced lupus
Hypertensive Moms Love Nifedipine (know these HTN drugs that are safe during pregnancy
Hydralazine
Methyldopa
Labetalol
Nifedipine
Minoxidil
another arterial vasodilator. Opens potassium channels and hyperpolarizes smooth muscle, resulting in relaxation of vascular smooth muscle
therapeutic for severe HTN
or, apply topically to induce hypertrichosis (hair growth)
adverse effects: hypertrichosis, hypotension, reflex tachycardia, fluid retention/edema
Nitrates
nitroglycerin
isosorbide dinitrate
nitroprusside
dilate veins, reducing preload
treats angina, acute pulmonary edema
side effects: reflex tachycardia, flushing, HA, nitroprusside, CN toxicity
decreases afterload only
hydralazine
decreases preload and afterload
ACEI/ARB
decreases nitrates
nitrates
lipid- lowering agent with side effect of facial flushing
niacin
lipid- lowering agent with SE of elevated LFTs, myositis
statins, fibrates
lipid lowering agent with SE of GI discomfort, bad taste
bile acid binding resins
Best effect on HDL
niacin
Best effect on TGs/ VLDL
fibrates, omega 3 fatty acids
best effect on LDL/cholesterol
statins
lipid- lowering agent that bind c. diff toxin
cholestyramine
lipid- lowering agent that causes rash, vasodilation, diarrhea
niacin
prevent at bedtime, pretreat with ASA or NSAID 30 min in advance, avoid alcohol