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Glossary of USMLE Pharmacoloy

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calcium channel blocker associated with accelerated progression of CHF?
verapamil
drug to slow ventricular response in Wolff-Parkinson White?
ibutilide
hypersensitivity angiitis or microscopic polyarteritis nodosa (can be caused by penicilin)
leukocytoclastic angiitis
in which part of the systemic circulation does the greatest decrease in blood pressure occur?
arterioles
vasodilator with lupus-like syndrome as side effect?
hydralazine
mechanism of hydralazine?
increases cGMP - smooth muscle relaxation; vasodilates arterioles > veins; reduces afterload
what calcium channel blocker is most selective for peripheral vasculature?
nifedipine
mechanism of calcium channel blockers?
block voltage-dependent L-type calcium channels of cardiac and SM and thereby reduce contractility
which calcium channel blocker is not used to treat arrhythmias?
nifedipine
what is the goal of antianginal therapy?
reduce myocardial O2 consumption by decreasing 1 or more of the determinants of MVO2: EDV, BP, HR, contractility, ejection time
what do nitrates affect in antianginal therapy?
preload
what happens to contractility and HR in nitrate therapy?
increase - reflex response
what do beta blockers affect in antianginal therapy?
afterload
how do nitrates affect ejection time and MVO2?
decrease
how do beta blockers affect ejection time?
increase it
what do beta blockers do to EDV?
increase it
what do beta blockers do to BP, contractility, and HR?
decrease them
what is digitoxin used for?
CHF (increases contractility) and atrial fibrillation (decreases conduciton at the AV node)
toxicities of digitoxin are increased by what?
renal failure, hpokalemia, and quinidine
blurry yellow vision is side effect of what?
digitoxin
what is the antidote for digitoxin?
slowly normalize K+, lidocaine, cardiac pacer, anti-dig Fab fragments
lupus-like syndrome is associated with what class IA antiarrythmic?
procainamide
what are the class IA antiarrythmics?
Na+ channel blockers: quinidine, amiodarone, procainamide, disopyramide (queen amy proclaims disco pyramids)
this class IA antiarrhythmic can cause cinchonism (headache, tinnitus, thrombocytopenia), torsades de pointes (due to increased QT interval)
quinidine
what class of antiarrhythmics are contraindicated post-MI
class IC - proarrhythmic
what beta blocker is very short acting?
esmolol
what is the antiarrhythmic action of beta blockers?
decrease cAMP and calcium currents; suppress abnormal pacemaker by decreasing slope of phase 4 - AV node particularly sensitive - increased PR interval
toxicity of amiodarone?
pulmonary fibrosis, hepatotoxicity, hypo/hyperthroidism;corneal deposits, skin deposits resulting in photodermatitis, neuro effects, constipation, bradycardia, heart block, CHF
K+ channel blockers that can cause torsades de pointes
soltalol, ibutilide
K+ channel blocker that can cause new arrhythmias and hypotension?
bretylium
wha type of cells do Ca2+ channel blockers primarily affect?
AV nodal cells
what type of antiarrhythmics are used for prevention of nodal arrhythmias?
class IV - Ca2+ channel blockers
what class IV antiarrhythmic can cause torsades de pointes?
bepridil
what is the drug of choice for diagnosing/abolishing AV nodal arrhythmias?
adenosine
what depresses ectopic pacemakers, especially in digitoxin toxicity?
K+
Mg+ is effective for treating what?
torsades de pointes and digitoxin toxicity
drug for hypertension in patient with PKD?
ACE inhibitor
anti-hypertesive for pregnant woman?
methyldopa
in patients with wolff parkinson white and atrial fibrillation, what can digitoxin do?
enhance transmission through accessory pathways that can predispose to v tac
when is mannitol contraindicated?
anuria, CHF
clinical use of mannitol?
shock, drug overdose, decrease intracranial/intraocular pressure
how does mannitol work?
increases tubular fluid osmolarity, producing increased urine flow
mechanism of acetazolamide?
carbonic anhydrase inhibitor - causes self-limited NaHCO3 diuresis and reduction in total body HCO3- stores
where does acetazolamide act?
proximal convoluted tubule
toxicity of acetazolamide?
hyperchloremic metabolic acidosis, neuropathy, NH3 toxicity, sulfa allergy
clinical use of acetazolamide?
glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness
mechanism of furosemide?
sulfonamide loop diuretic - inhibits NKCC of thick ascending limb; abolishes hypertonicity of medulla, preventing concentration of urine
what effect does furosemide have on calcium excretion?
increases it - Loops Lose calcium
clinical use of furosemide?
edematous states (CHF, cirrhosis, nephrotic syndrome, pulmonary edema), hypertension, hypercalcemia
toxicity of furosimide?
OH DANG: ototoxicity, hypokalemia, dehydration, allergy (sulfa), nephritis (interstitial), gout
drug for diuresis in patients allergic to sulfa drugs?
ethacrynic acid
diuretic that can be used in hyperuricemia, acute gout?
ethacrynic acid
mechanism of hydrochlorothiazide?
inhibits NaCl reabsorption in distal convoluted tubule, reducing diluting capacity of the nephron, decreases calcium excretion
clinical use of hydrochlorothiazide?
hypertension, CHF, idiopathic hypercalciuiria, nephrogenic diabetes insipidus
diuretic used in nephrogenic diabetes insipidus?
hydrochlorothiazide
toxicity of hydrochlorothiazide?
hypokalemic metabolic alkalosis, hyponatremia, hyperGlycemia, hyperLipidemia, hyperUricemia, and hyperCalcemia (sulfa alergy)
what are the potassium sparing diuretics?
Spironolactone, Triamterene, Amiloride, eplercone (the K+ STAys)
mechanism of spironolactone?
competitive aldosterone receptor antagonist in cortical collecting tubule
how do triamterene and amiloride act?
cortical collecting tubule - block Na+ channels
clinical use of K+ sparing diuretics?
hyperaldosteronism, K+ depletion, CHF
toxicity of K+ sparing diuretics?
hyperkalemia, endocrine effects (e.g. spironolactone causes gynecomastia, antiandrogen effects)
diuretics causing acidosis?
carbonic anhydrase inhibitors, K+ sparing diuretics
diuretics causing alkalosis?
loop diuretics, thiazides
diuretic that increases urine calcium?
loop diuretics
diuretics that decrease urine calcium?
thiazides
name 3 ACE inhibitors
captopril, enlapril, lisinopril
mechanism of Losartan?
AT II receptor antagonist - not ACE inhibitor and so doesn't cause cough
toxicity of ACE inhibitors?
CATOPRIL: cough, angioedema, proteinuria, taste changes, hypOtension, pregnancy problems (fetal renal damage), rash, increased renin, lower angiotensin II; hyperkalemia
serious cardiac arrhythmias/torsades de pointes can occur with erythromycin and what?
cisapride
what type of drug are omeprazole, lansoprazole?
proton pump inhibitors
action of misoprostol?
PGE1 analog - increases production and secretion of gastric mucous barrier, decreases acid production
drug that can be used to prevent NSAID-induced peptic ulcers, maintain a PDA, and induce labor
misoprostol
action of pirenzepine, propantheline?
muscarinic antagonists - block M1 receptors on ECL cells (decrease histamine secretion) and M3 receptors on parietal cells (decrease H+ secretion) - used for peptic ulcer
monoclonal antibody to TNF-alpha
infliximab
sulfasalazine?
combination of sulfapyradine (antibacterial) and mesalamine (antinflammatory) activated by colonic bacteria; Rx for Crohn's and UC
mechanism of ondansetron?
5-HT3 antagonist - powerful central-acting antiemetic
overuse of aluminum hydroxide?
constipation and hypophosphatemia
overuse of magnesium hydroxide?
diarrhea
overuse of calcium carbonate?
hypercalcemia, rebound acid increase
all antacids can cause what metabolic disturbance?
hypokalemia
antiemetic that can cause Parkinsonian symptoms?
metoclopramide
how does cimetidine impact P-450 system?
potent inhibitor
H2 blocker with antiandrogenic effect that can decrease renal excretion of creatinine?
cimetidine
A patient presents with HA, tinnitis, vomiting,and confusion … you are concerned about and overdose of what common medication?
Aspirin
Aspirin overdose will manifest as a respiratory _____ and a metabolic ______?
Aspirin overdose will manifest as a respiratory alkalosis and metabolic acidosis
At a [CO] of 30% a patient will experience HA, and SOB because of hypoxia of what area of the brain?
gray matter
at a [co] of 50% there is hypoxia of the globus pallidus leading to what symptoms and signs?
loss of conciousness, convulsions, and coma
which mushroom is typically lethal, amanita muscaria or amanita phalloides?
phalloides - the toxin inhibits RNA polymerase and can lead to ab pain, vomiting, diarrhea, and fulminant hepatitis with extensive liver necrosis
"garlic scented breath"
arsenic poisioning
what are Mees lines?
transverse band on fingernails that may indicate chronic arsenic poisioning
what are the long term complications of chronic arsenic poisioning?
squamous cell carcinoma of lungs and skin
what is the most common chrnoic metal poisioining in the united states?
lead
lead poisionign ALWAYS involves
CNS toxicity
what is the mechanism of lead toxicity?
lead interferes with heme production by inhibiting d-aminolevulinic acid dehydratase and ferrochelatase
A patient presents with wrist and foot drop, microcytic anemia with basophillic stippling, and dark lines on their gums … you suspect …
lead poisioning
"bitter almond" scented breath
cyanide poisioing
what is the mechanism of cyanide poisioning
blocks cellular respiration by binding cytocrhome oxidase
what are the top 3 causes of death in smokers
1. heard disease, 2. lung cancer, 3. copd
T or F: stopping smoking for 15 years will reduce the risk of dying to almost the level of a non-smoker
TRUE
a patient presents with a perforation in the nasal septum and dilated cardiomyopathy … you suspect chronic use of what chemical?
cocain
what causes "track marks" of a IVDU
the healing of skin abscesses
mechanism of amantadine?
blocks viral penetration/uncoating; may buffer pH of endosome. also causes the release of dopamine from intact nerve terminals
clinical use of amantadine?
prophylaxis and treatment for influenza A; Parkinson's disease
toxicity of amantadine?
ataxia, dizziness, slurred speech
mehcanism of zanamivir, oseltamivir?
inhibit influenza neuraminidase
clinical use of zanamivir & oseltamivir?
both influenza A & B
mechanism of ribavirin?
inhibits synthesis of gruanine nucleotides by competitively inhibiting IMP dehydrogenase
clinical use of ribavirin?
RSV, chronic hepatitis C
toxicity of ribavirin?
hemolytic anemia, severe teratogen
mechanism of acyclovir?
preferentially inhibits viral DNA polymerase when phosphorylated by viral thymidine kinase; guanine analog
clinical use of acyclovir?
HSV, VZV, EBV; mucocutaneous and genital herpes lesions; prophylaxis in immunocompromised patients
toxicity of acyclovir?
delerium, tremor, nephrotoxicity
mechanism of ganciclovir?
phosphorylation by viral kinase; preferentially inhibits CMV DNA polymerase
clinical use of ganciclovir?
CMV, especially in immunocompromised patients
toxicity of ganciclovir?
leukopenia, neutropenia, thrombocytopenia, renal toxicity; more toxic to host enzymes then acyclovir
mechanism of foscarnet?
viral DNA polymerase inhibitor that binds to the pyrophosphate binding site of the enzyme; does not require action by viral kinase
clinical use of foscarnet?
CMV retinitis in immunocompromised patients when ganciclovir fails; acyclovir-resistant HSV
toxicity of foscarnet?
nephrotoxicity, hypoglycemia, hypomagnesia
saquinavir, ritonavir, indinavir, nelfinavir, and amprenavir are what type of drugs?
protease inhibitors - used in HIV therapy
mechanism of protease inhibitors?
inhibit assembly of new virus by blocking protease enzyme
toxicity of protease inhibitors?
GI intolerance (nausea, diarrhea), hyperglycemia, lipid abnormalities
protease inhibitor that can cause thrombocytopenia?
indinavir
zidovudine, didanosine, zalcitabine, stavudine, lamivudine, and abacavir are what type of drug?
nucleoside RT inhibitors
nevirapine, delaviridine, and efavirenz are what type of drug?
non-nucleoside RT inhibitors
mechanism of reverse transcriptase inhibitors?
preferentially inhibit RT of HIV; prevent incorporation of viral genome into host DNA
toxicity of RT inhibitors?
bone marrow suppression (neutropenia, anemia), peripheral neuropathy
what type of reverse transcriptase inhibitors can cause lactic acidosis?
nucleosides - zidovudine, didanosine, zalcitabine, stavudine, lamivudine, and abacavir
what type of RT inhibitors can cause rash?
non-nucleosides -nevirapine, delaviridine, and efavirenz
nucleoside RT inhibitor that can cause megaloblastic anemia?
AZT (zidovudine)
what HIV drug is used during pregnancy to reduce the risk of fetal transmission?
AZT
interferon-alpha is used for what?
chronic hepatitis B andC, Kaposi's sarcoma
interferon beta is used in what disease?
MS
interferon gamma is used in what disease?
NADPH oxidase deficiency
toxicity of interferons?
neutropenia
these are glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis
interferons
drug used for giardiasis, amebic dysentery, bacterial vaginitis, trichomonas?
metronidazole
drug used for giant roundworm (asarcis), hookworm (necator/ancylostoma), and pinworm (enterobius)?
pyrantel pamoate
drug used for trematode/fluke (schistosomes, paragnimus, clornorchis), and cysticercosis?
praziquantel
drug used for cestode/tapeworm (e.g. diphyllobothrium latum, taenia species) infections except cysticercosis?
niclosamide
drug used for onchocerciasis?
ivermectin (rIVER blindness)
drug used for nematode/roundworm (e.g. pinworm, whipworm) infections?
mebendazole/thiabendazole
block cell wall synthesis by inhibition of peptidoglycan cross-linking
penicillin, ampicillin, ticarcillin, piperacillin, imipenem, aztreonam, cephalosporins
block peptidoglycan synthesis
bacitracin, vancomycin, cycloserine
disrupt bacterial/fungal cell membranes
polymyxins
disrupt fungal cell membranes
amphotericin B, nystatin, fluconazole/azoles
block nucleotide synthesis
sulfonamides, trimethoprim
block DNA topoisomerases
quinolones
block mRNA synthesis
rifampin
block protein synthesis at 50S ribosomal subunit
chloramphenicol, erythromycin/macrolides, lincomycin, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid
block protein synthesis at 30S ribosomal subunit
aminoglycosides, tetracyclines
bacteriacidal antibiotics (6)
penicilin, cephalosporins, vancomycin, aminoglycosides, fluoroquinolones, metronidazole
penicillin mechanism
bind PBPs, block transpeptidase cross-linking of cell wall; activate autolytic enzymes
penicillin toxicity
hypersensitivity reactions, hemolytic anemia
mechanism of methicillin, nafcillin, dicloxacillin
bind PBPs, block transpeptidase cross-linking of cell wall - penicillinase resistant because of bulkier R group
methicillin toxicity
interstitial nephritis
ampicillin, amoxicillin toxicity
hypersensitvity, ampicillin rash (esp. in pts. w/ mono), pseudomembranous colitis
ticarcillin, carbenicillin, piperacillin usage
pseudomonas (Takes Care of Pseudomonas)
mechanism of cephalosporins
beta-lactam drugs that inhibit cell wall synthesis - less susceptible to penicillinases
antibiotic for penicillin-allergic patients and patients w/ renal toxicity who can't tolerate aminoglycosides
aztreonam (synergistic w/ aminoglycosides)
drug of choice for enterobacter
imipenem/cilastin
antibiotic that can cause seizures at high plasma levels
imipenem/cilastin
mechanism of vancomycin
inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursors
mechanism of resistance to vancomycin
amino acid change of D-ala D-ala to D-ala D-lac
vancomycin toxicity
well tolerated in general - does NOT have many problems: nephrotoxicity, ototoxicity, thrombophlebitis
aminoglycosides
streptomycin, gentamicin, tobramycin, amikacin - bacteriacidal
mechanism of action of aminoglycosides
inhibit 30S subunit - inhibit formation of initiation complex and cause misreading of mRNA
are aminoglycosides effective agains anaerobes?
no! require O2 or uptake
aminoglycosides cause nephrotoxicity especially when used in combination with _________
cephalosporins
aminoglycosides cause ototoxicity especially when used with_________
loop diuretics
are aminoglycosides safe to use in pregnancy?
no! teratogenic
which tetracycline can be used in patients with renal failure?
doxycycline because it is fecally eliminated
can you take tetracyclines with milk?
no! nor atacids or iron-containing preparations because divalent cations inhibit its absorption in the gut
tetracycline toxicity
discoloration of teeth and inhibition of bone growth in children, photosensitivity
mechanism of action of macrolides
inhibit protein synthesis by blocking translocation - bind to 23S rRNA of the 50S subunit
name 3 macrolides
erythromycin, azithromycin, clarithromycin
when can sulfonamides cause hemolysis?
G6PD deficiency
most common cause of noncompliance with macrolides
GI discomfort
macrolides increase the serum concentration of what drugs?
theophyllines, oral anticoagulants
acute cholestatic hepatitis & eosinophilia are toxicities of which class of antibiotics?
macrolides
clinical use of chloramphenicol
meningitis - H. flu, neisseria, strep pneumo
why does chloramphenicol cause gray baby syndrome?
because infants lack liver UDP-glucoronyl transferase
is the aplastic anemia seen with chloramphenicol dose dependent?
no! the anemia is, however
mechanism of action of chloramphenicol
inhibits 50S peptidyltransferase
what is the clinical use of clindamycin?
treatment of anaerobic infections - B. frag, C. perfringfens
clindamycin toxicity
pseudomembranous colitis - destroys normal GI flora
mechanism of action of sulfonamides (sulfamethoxazole, sulfisoxazole, triple sulfas, etc.)
PABA antimetabolites inhibit dihydropteroate synthase
what side effect can sulfonamides cause in infants?
kernicterus
mechanism of action of trimethoprim
inhibits bacterial dihydrofolate reductase
trimethoprim toxicity
megaloblastic anemia, leukopenia, granulocytopenia (may alleviate with supplemental folinic acid)
mechanism of action of fluoroquinolones
inhibit DNA gyrase (topoisomerase II)
what class of antibiotics can cause cartilage damage in kids?
fluoroquinolones
what drug is associated with a disulfiram-like reaction with alcohol and a metallic taste
metronidazole
what can prevent the neurotoxicity associated with INH?
pyridoxine (vitamin B6)
INH toxicity
hemolysis if G6PD deficient, neurotoxicity, hepatotoxicity, SLE-like syndrome
mechanism of action of rifampin
inhibits DNA-dependent RNA polymerase
what drug delays resistance to dapsone when used for leprosy?
rifampin
resistance mechanism for penicillins/cephalosporins
beta-lactamase cleavage of beta lactam ring
resistance mechanism for aminoglycosides
modification via acetylation, adenylation, or phosphorylation
resistance mechanism for chloramphenicol
modification via acetylation
resistance mechanism for macrolides
methylation of rRNA near erythromycin's ribosome binding site
resistance mechanism for tetracycline
decreased uptake or increased transport out of cell
resistance mechanism for sulfonamides
altered enzyme (bacterial dihydropteroate synthetase), decreased uptake, or increased PABA synthesis
mechanism of action of amphotericin B
binds ergosterol (unique to fungi); forms membrane pores that allow leakage of electrolytes and disrupt homeostasis
drug of choice for systemic mycoses
amphotericin B
amphotericin B toxicity
fever/chills, hypotension, nephrotoxicity, arrhythmias, hypochromic normocytic anemia
do ketoconazole and ampho B act synergistically?
no - they antagonize each other's actions, so should never be used together
which has greater oral availability - amoxicillin or ampicillin?
amOxicillin
spectrum of ampicillin, amoxicillin
HELPS kill enterococci: h. flu, e. coli, listeria, proteus, salmonella, enterococci
cefazolin and cephalexin are what generation cephalosporins?
first
coverage of cefazolin and cephalexin?
proteus, e. coli, klebsiella and gram +
cefoxitin, cefaclor, cefuroxamine are what generation?
second
coverage of cefoxitin, cefaclor, cefuroxamine?
h. flu, enterobacter, neisseria, proteus, e. coli, klebsiella
ceftriaxone, cefotaxime, and ceftazidime are what generation?
third
use of ceftriaxone, cefotaxime, and ceftazidime?
serious gram-negative infections resistant to other beta lactams; meningitis; ex. ceftazidime for pseudomonas, ceftriaxone for gonorrhea
cefepime, cefpiramide belong to what generation?
fourth
use of cefepime, cefpiramide?
increased activity against pseudomonas and gram-positive organisms
serum-like sickness in infants and kids can be seen with what cephalosporin?
ceflacor (2nd generation)
this is an inhibitor of renal dihydropeptidase I
cilastin - decreases inactivation of imipenem in renal tubules
why are aminoglycosides ineffective against anaerobes?
require O2 for uptake
drug used for bowel surgery?
neomycin
this tetracycline is an ADH antagonist - acts as a diuretic in SIADH
demeclocylcine
clinical use of tetracyclines?
VACUUM THe BedRoom: vibrio cholerae, acne, chlamydia, ureaplasma urealyticum, mycoplasma, tularemia, h. pylori, borrelia burgdorferi, rickettsia
this drug treats anaerobes above the diaphragm
clindamycin
these drugs can cause leg cramps and myalgias in kids
fluoroquinolones
used for anaerobes below the diaphragm
metronidazole
how does nystatin work?
binds to ergosterol, disrupting fungal membranes (too toxic for systemic use)
mechanism of the -azoles?
inhibit fungal steriod (ergosterol) synthesis
toxicities of -azoles?
hormone synthesis inhibition (gynecomastia), liver dysfunction (inhibition of P450), fever, chills
this antifungal inhibits DNA synthesis by conversion to fluorouracil, which competes with uracil
flucytosine
toxicity of flucytosine
nausea, vomiting, diarrhea, bone marrow suppression
mechanism of caspofungin?
inhibits cell wall syntehsis
use of caspofungin?
invasive aspergillosis
toxicity of caspofungin?
GI upset, flushing
this antifungal inhibits the fungal enzyme squalene epoxidase
terbinafine
use of terbinafene?
used to treat dermatophytoses (especially onychomycosis)
mechanism of griseofulvin?
interferes with microtubule function; disrupts mitosis; depostis in keratin-containing tissues (e.g. nails)
clinical use of griseofulvin?
oral treatment of superficial infections; inhibits growth of dermatophytes (tinea, ringworm)
toxicity of griseofulvin?
teratogenic, carcinogenic, confusion, headaches, increases warfarin metabolism
actions of insulin/insulin-like drugs?
TK activity: liver (increase glucose stored as glycogen), muscle (increase glycogen and protein synthesis, K+ uptake), fat (aids TG storage)
what type of drug: tolbutamide & chlorpropamide?
first generation sulfonylureas
what type of drug: glyburide, glimepiride, glipizide?
second generation sulfonylureas
mechanism of action of sulfonylureas?
close K+ channel in beta cell membrane so cell depolarizes, triggering of insulin release via Ca2+ influx
what are sulfonylureas used for?
stimulate release of endogenous insulin in type 2 DM; require some islet function so useless in type 1
side effects of first generation sulfonylureas?
disulfiram-like reactions
side effect of second generation sulfonylureas?
hypoglycemia
what is the most grave side effect of metformin?
lacti acidosis
can metformin be used in patients without islet function?
yes
action of pioglitazone and rosiglitazone?
increase target cell response to insulin
action of acarbose and miglitol?
alpha glucosidase inhibitors - inhibit intestinal brush border alpha glucosidases; delayed sugar hydrolysis and glucose and glucose absorption lead to decreased postprandial hyperglycemia
mechanism of propylthiouracil, methimazaole?
inhibit organification and coupling of thyroid hormone synthesis - used for hyperthyroidism

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