Pharmacology Flashcards
drug of choice = DOC
inhibitors of ACh synthesis, storage, release
hemicholinium-3, vesamicol, botulinum toxin
inhibitors of ACh degradation (AChE inhibitors)
edrophonium, neostigmine, pyridostigmine, ambenonium, physostigmine
diisopropyl flurophosphate
tacrine, donepezil, rivastigmine, galantamine
muscarinic receptor AGONISTS
methacholine (asthma challenge test)
carbachol, bethanechol, cevimeline, pilocarpine
nicotinic receptor AGONISTS
succinylcholine
muscarinic recept ANTAGONISTS
atropine
scopolamine
pirenzepine, methscopolamine, glycopyrrolate
ipratropium, tiotropium
oxybutynin, propantheline, terodiline, tolterodine, fesoterodine, trospium, darifenacin, solifenacin
nicotinic recept ANTAGONISTS
pancuronium, tubocurarine, vecuronium, rocuronium, mivacurium
trimethaphan, mecamylamine
sodium channel inhibitors (antiepileptics)
phenytoin
carbamezepine
lamotrigine
lacosamide
Ca channel inhibitors (antiepileptics)
ethosuxamide, valproic acid (inhib T-type Ca channel)
gabapentin, pregabalin (inhib HVA Ca channel)
GABA channel potentiators (antiepileptics)
Benzos (diazepam, lorazepam, midazolam, clonazepam) [increase amount of Cl influx]
barbiturates (phenobarbital) [increase duration of Cl influx]
vigabatrin (irrev inhibit GABA transaminase)
glutamate recept inhibitors (antiepileptics)
felbamate
rufinamide
other antiepileptic drugs under investigation
tiagabine
topiramate
levetiracetam
zonisamide
drug of choice for focal seizures
carbamazepine
drug of choice for idiopathic generalized seizures (and mixed seizures)
valproic acid
drugs of choice for absence seizures
ethosuxamide > valproic acid > lamotrigine > clonazepam
glucocorticoid receptor AGONISTS
prednisone (preggos), prednisolone, methylprednisolone, dexamethasone (fetal), hydrocortisone (replacement therapy)
fluticasone, beclomethasone, flunisolide, triamcinolone, budesonide [inhaled]
GC recept ANTAGONISTS
mifepristone (for ectopic ACTH synd)
Inhibitors of GC synthesis
mitotane (DDT) aminoglutethimide metyrapone (dx of hypo-pit-adrenal axis) trilostane ketoconazole (inhib P450 enzymes)
Minerocorticoid receptor AGONISTS
fludrocortisone
MC recept ANTAGONISTS
spironolactone
eplerenone
Adrenal sex steroid
Dehydroepiandrosterone (DHEA)
inhibitor of fungal nucleic acid synthesis
flucytosine
inhibitor of fungal MITOSIS
griseofulvin
inhibitors of squalene epoxidase
terbafine, naftinfine (allylamines)
butenafine (benzylamines)
inhibitors of 14-alpha sterol demethylase
Imidazoles:
ketoconazole
butoconazole, clotrimazole, econazole, miconazole, oxiconazole, sertaconazole, sulconazole [topical]
Triazoles:
fluconazole, itraconazole (inhibit P450)
posaconazole, terconazole, voriconazole
inhibitors of fungal membrane stability: polyenes
amophotericin B
nystatin
inhibitors of fungal wall synthesis: echinocandins
caspofungin, micafungin, anidulafungin
tx of acute cryptococcal meningitis in HIV-positive patient
flucytosine + amphotericin B
tx of fungal inf of hair, skin, nails
griseofulvin
drug of choice for tx of candidiasis and cryptococcal meningitis
fluconazole
drug of choice for tx of invasive aspergillosis
voriconazole
only triazole whose absorption NOT affected by gastric acid
fluconazole
drug of choice for vulvovaginal candidiasis
terconazole
prophylaxis tx of invasive fungal infection
posaconazole
tx of mucocutaneous candidiasis
nystatin
tx of esophageal candidiasis
caspofungin, (micafungin, anidulafungin)
inhib of viral attachment/entry (and mechanism)
maraviroc (only blocks CCR5, not CXCR4)
enfuvirtide (T-20) [inhib gp41-med fusion by binding HR1]
inhibitors of viral uncoating
block M2 channel proton
amantidine (also for Parkinson’s)
rimantidine
Antiherpesvirus nucleoside and nucleotide analogues (plus dz/tox if applicable)
phosphorylated by viral kinases:
acyclovir, valacylovir (HSV, VZV)
pencicyclovir, famcicyclovir (HSV, VZV - shingles)
ganciclovir, valganciclovir (CMV) (neutropenia)
phosphorylated by cellular kinase:
cidofovir - must be coadmin w/ probenicid (CMV retinitis in those w/ HIV) (NEPHROtox)
vidarabine, idoxuridine, trifluridine (HSV keratitis)
anti-HIV and -HBV nucleoside/nucleotide analogues/SE
zidovudine (AZT) stavudine (d4T) zalcitabine (ddC) Lamivudine (3TC) - [HBV] emtricitabine (FTC) - 1x daily didanosine (ddl) Abacivir ^^all these ass. w/ neutropenia, anemia
tenofovir (HIV) (hepatotoxicity)
adefovir (HBV) (renal toxicity)
entecavir (HBV) (dose adjust in pts w/ mod renal insuff)
nonnucleoside DNA polymerase inhibitors/SE
foscarnet (renal impairment = dose-limiting)
NNRTIs/SE
efavirenz (1x daily), nevirapine, delavirdine, etravirine [rash!!]
inhib of viral integration - inhib HIV INTEGRASE!
raltegravir
inhib of viral integration - inhib HIV PROTEASE!/SE
saquinavir, ritonavir, amprenavir, fosamprenavir, indinavir, nelfinavir, lopinavir, atazanavir, tipranavir, darunavir
SE = fat distrib and metabolic abnormalities
inhibitors of viral release
inhib neuraminidase!! - Flu A, B
zanamivir
oseltamivir (prophylaxis/tx)
antiviral drugs w/ UNKNOWN mech of action (+ dz)
fomivirsen (2nd line CMV retinitis)
Ribavirin (RSV, HCV w/ IFN-alpha)
docosanol (HSV) - lacks cytotoxicity
antiviral drugs that modulate immune system
IFN-alpha
IFN-beta (tx of MS)
Imiquimod (w/ TLR-7 + 8 to boost innate immunity)
alpha1 receptor functions
Gq
increase vasc SM contraction (vasoconstriction) –> increases systolic/diastolic BP –> reflex bradycardia (DECREASED HR)
increase pupillary dilator muscle contraction (mydriasis - dilation)
increase intestinal and bladder sphincter muscle contraction
alpha2 receptor functions
Gi decrease sympathetic outflow (inhib NE release) decrease insulin release decrease lipolysis increase platelet aggregation
beta1 receptor functions
Gs increase heart rate increase contractility and conductance increase renin release increase lipolysis
beta2 receptor functions
Gs vasodilation (decrease diastolic BP) bronchodilation increase HR increase contractility increase lipolysis increase insulin release decrease uterine tone (tocolysis) ciliary muscle relaxation increase aqueous humor production
M1 receptor functions
Gq
CNS, enteric NS
M2 receptor functions
Gi
decrease HR and contractility of atria at SA node (bradycardia)
M3 receptor functions
Gq
increase exocrine gland secretions (lacrimal, gastric gland, bronchial secretions, etc.)
increase gut peristalsis
increase bladder contraction
bronchoconstriction (increase airflow resistance)
increase pupillary sphincter muscle contraction (miosis)
ciliary muscle contraction (accomodation)
D1 receptor functions
Gs
relaxes renal vasc SM
D2 receptor functions
Gi
modulates transmitter release (esp in brain)
H1 receptor functions
Gq increase nasal and bronchial mucus prod (allergy symptoms) contraction of bronchioles pruritus pain
H2 receptor functions
Gs
increase gastric acid secretion
V1 receptor functions
Gq
increase vasc SM contraction
V2 receptor functions
Gs
increase water permeability and reabsorption in collecting tubules of kidney
CCB used on vasc SM
amlodipine, nifedipine
first line therapy for HTN in preg
hydralazine w/ methyldopa
can cause cyanide toxicity (releases cyanide)
nitroprusside
drugs of choice in pts w/ CAD and CHF w/ HTN
cardioselective beta blockers
A BEAM of beta-1 blockers
DOC in pts w/ isolated systolic HTN
CCB + thiazide diuretics (in non-diabetics)
ACE inhib or ARB (diabetics)
CCB used on heart
verapamil
partial beta agonists contraindicated in angina
pindolol, acebutolol
decrease GI absorption of statins
bile acid resins (cholestyramine, colestipol, colesevelam)
class IA antiarrhythmics
quinidine, procainamide, disopyramide
increases AP duration, ERP, QT interval
“the Queen Proclaims Diso’s Pyramid”
class IB antiarrhythmics
lidocaine, mexiletine, tocainide; (phenytoin can also fall into this class)
decreases AP duration
BEST POST-MI!! + in digitalis-induced arrhythmias
class IC antiarrhythmics
flecainide, propaferone
no change in AP duration
last-ditch drug
class II antiarrhythmics
metoprolol, propanolol, esmolol, atenolol, timolol
class III antiarrhythmics
amiodarone, ibutilde, dofetilide, sotalol
“AIDS”
class IV antiarrhythmics
verapamil, diltiazem
“other” antiarrhythmics
adenosine, Mg
does not presdisp to Torsades de Pointes even though prolongs QT interval
amiodarone (half life > 80 days)
DOC in dx/abolishing paroxysmal SVT
adenosine
effects blocked by theophylline and caffeine
adenosine
DM tx: no risk of hypoglycemia
metformin, pioglitazone, rosiglitazone, acarbose, miglitol, voglibose
sulfa drugs
probenecid furosemide acetazolamide celecoxib thiazides sulfonamide AB sulfasalazine sulfonylureas
“Sulfa Pills Frequently Cause Terrible Acute Symptoms”
pts w/ sulfa allergies –> fever, UTI, pruritic rash, Stevens-Johnson synd, hemolytic anemia, thrombocytopenia, agranulocytosis, urticaria (hives)
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
dantrolene
DOC for Pneumocystis jirovecii, Toxoplasma gondii, Nocardia, Stenotrophomonas meltophilia
TMP-SMX
Vd =
amount of drug in body/plasma drug concentration
half life =
0.7 x Vd / CL
loading dose =
Css x Vd/F (F=1 for IV dose)
maintenance dose =
Css x CL/F
reduces pain by decreasing levels of substance P in PNS
capsaicin
DOC for type II DM
metformin
P450 inducers
Momma Bear Steals Phen-phen and Refuses Greasy Carbs Chronically
modafinil barbiturates St.John's wort phenytoin rifampin griseofulvin carbamezapine chronic alcohol use
P450 inhibitors
MAGIC RACKS in GQ
macrolides amiodarone grapefruit juice isoniazid cimetidine ritonavir acute alcohol abuse ciprofloxacin ketoconazole sulfonamides gemfibrozil quinidine
AB to avoid in preg
Sulfonamides - Kernicterus Aminoglycosides - otoxicity Fluoroquinolones - cartilage damage Clarithromycin - embryotoxic Tetracyclines - discolored teeth, inhibition of bone growth Ribavirin (antiviral) - teratogenic Griseofulvin (antifungal) - teratogenic Chloramphenicol - "gray baby"
“SAFe Children Take Really Good Care”
DOC for DVT and pulmonary thromboembolism
warfarin
DOC for Legionella
erythromycin
DOC for Treponema
penicillin
DOC for Mycoplasma
erythromycin or tetracyclines
drug infused at constant rate achieves steady state in?
4-5 half-lives
DOC for hairy cell leukemia
cladribine (adenosine analog that is resistant to adenosine deaminase)
best agent to increase HDL levels?
niacin
best tx for high LDL
statins + ezetimibe
best agent for hypertriglyceridemia
fibrates
SE = increases TG levels
cholestyramine, colestipol, colesevelam
bile acid resins
MOA of cromolyn
prevents mast cell degranulation
cromolyn used for?
PROPHYLAXIS of asthma, allergies, aspirin HST
anti-TB drug most effective in acidic environments + most useful against INTRAcellular organisms
pyrazinamide
pyrazinamide most effective against?
M.tuberculosis engulfed by macrophages
what is needed to convert INH to active metabolite?
KatG (bacterial catalase-peroxidase)
solo prophylaxis against TB?
INH
meningococcal prophylaxis and chemoprophylaxis in contacts of children w/ H.influenzae type B?
rifampin
toxicity = blurry yellow vision (think Van Gogh)
digoxin
thiazide diuretics cause what SE?
- hypokalemic metab alkalosis (bc increased aldost secretion)
- hyponatremia, hypomagenesemia
- sulfa allergy
hypergGlycemia hyperLipidemia hypercCalcemia hyperUricemia ("Hyper Girls Like Crushing Uppers")
mannitol (osmotic diuretic) can cause what SE?
hypernatremia, pulmonary edema
mannitol is CI in pts w/ what?
anuria, CHF
carbidopa decreases what SE of L-dopa?
nausea, vomiting
carbidopa increases what SE of L-dopa?
anxiety, agitation, insomnia, confusion, delusions, hallucinations
leucovorin is a?
tetrahydrofolate derivative that does NOT req activation by dihydrofolate before it can function as cofactor for thymidylate synthase
N5-formyl-tetrahydrofolate
drug whose chemo effects overcome by leucovorin
methotrexate
drug whose chemo effects potentiated by leucovorin
5-FU
bortezomib MOA and indications?
proteasome inhibitor
tx for multiple myeloma and Waldenstrom’s macroglobulinemia
tx for mod-severe allergic asthma?
omalizumab (anti-IgE Ab)
this drug has increased toxicity w/ allopurinol
azathioprine (6-MP, 6-TG)
bc both metab by xanthine oxidase
antimetabolite not S-phase specific
gemcitabine (pyramidine analog)
methotrexate inhibits
dihydrofolate reductase