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401 Cards in this Set
- Front
- Back
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How to find Km from a V/S plot?
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[S] at 1/2 Vmax
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how to find Km and Vmax from a 1/V / 1/S plot?
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x intercept is 1/-Km
y intercept is 1/Vmax slope is Km/Vmax |
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effect on Vmax and Km of competitive/noncompetitive inhibitors?
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competitive inhibitor: increases Km, no effect on Vmax
noncompetitive inhibitor: no change on Km, decreases Vmax |
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a drug infused at a constant rate takes _________ to reach steady state
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4-5 half lives
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zero order elimination?
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rate of elimination constant regardless of plasma concentration, Cp decreases linearly with time.
Examples: phenytoin, Ethanol, Aspirin |
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first order elimination?
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rate of elimination proportional to drug concentration; constant fraction of drug eliminated per unit time; Cp decreases exponentially with time
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Phase I metabolism
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reduction, oxidation, hydrolysis
uses cytochrome P-450 system usually yields slightly polar, water-soluble metabolites that are often still active |
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Phase II metabolism
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acetylation, glucuronidation, sulfation (all types of conjugation)
usually yields very polar, inactive metabolites that are renally excreted |
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Efficacy vs. Potency
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efficacy - maximal effect a drug can produce
potency - amount of drug needed for a given effect |
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therapeutic index formula?
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median lethal dose
----------------------- median effective dose |
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describe neurons/neurotransmitters of parasympathetic nervous system?
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two neurons: first using nicotinic ACh, second using muscarinic ACh
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describe neurons/neurotransmitters of sympathetic nervous system?
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two neurons: first using nicotinic ACh, second using:
•for sweat glands, muscarinic ACh •for renal vascular smooth muscle, D1 •everything else (cardiac, smooth muscle, glands, nerve terminals): alpha/beta NE |
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describe neurons/neurotransmitters of somatic nervous system?
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one neuron using nicotinic ACh
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structure of nicotinic ACh receptors?
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ligand-gated sodium/potassium channels
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structure of muscarinic ACh receptors?
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GPCRs (M1-M5)
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second messenger systems involved with Gq?
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phospholipase C -> PIP2 ->
•IP3 -> increased calcium •DAG -> protein kinase C |
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second messenger systems involved with Gs?
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adenylyl cyclase -> cAMP -> protein kinase A
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second messenger systems involved with Gi?
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inhibits adenylyl cyclase -> decreased cAMP -> decreased protein kinase A
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noradrenergic synthesis pathway?
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tyrosine -> DOPA -> dopamine -> NE
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bethanechol
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direct cholinergic agonist
used for postoperative and neurogenic ileus and urinary retention |
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carbachol
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direct cholinergic agonist
used for glaucoma, pupillary contraction, relief of intraocular pressure |
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pilocarpine
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direct cholinergic agonist
used to stimulate sweat, tears, saliva |
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methacholine
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direct cholinergic agonist
used in challenge test for diagnosis of asthma |
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neostigmine
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anticholinesterase; increases endogenous ACh; NO CNS penetration
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pyridostigmine
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anticholinesterase; used for myasthenia gravis
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edrophonium
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anticholinesterase; used to diagnose myasthenia gravis (very short half life)
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physostigmine
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anticholinesterase; used in glaucoma and atropine overdose
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echothiophate
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anticholinesterase; used in glaucoma and atropine overdose
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symptoms of cholinesterase inhibitor poisoning?
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(seen in organophosphate poisoning)
DUMBBELSS (Diarrhea, Urination, Miosis, Bronchospasm, Bradychardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation) antidote: atropine and pralidoxime |
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Atropine
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muscarinic antagonist; produces mydriasis and cycloplegia
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Benztropine
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muscarinic antagonist; used in Parkinson's
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Scopolamine
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muscarinic antagonist; used in motion sickness
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Ipratropium
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muscarinic antagonist; used in Asthma, COPD
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oxybutynin
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muscarinic antagonist; reduces bladder spasms
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methscopolamine
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muscarinic antagonist; used in peptic ulcer disease
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atropine toxodrome?
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(anticholinergic)
hot, dry, red, blind, mad, constipated can cause acute angle-closure glaucoma in elderly |
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hexamethonium
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nicotinic antagonist used to prevent vagal reflex responses to changes in blood pressure
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epinephrine
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alpha-1, alpha-2, beta-1, beta-2
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norepinephrine
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alpha-1 and alpha-2 > beta-1
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isoproterenol
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beta-1 = beta-2
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effect of dopamine on adrenergic receptors?
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D1 = D2 > beta > alpha
inotropic and chronotropic |
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dobutamine
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beta-1 > beta-2
inotropic but not chronotropic |
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phenylephrine
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alpha-1 > alpha-2
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albuterol
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selective beta-2 (beta-2 > beta-1)
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ritodrine
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beta-2 (reduces premature uterine contractions)
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amphetamine
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indirect general sympathomimetic; releases stored catecholamines
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ephedrine
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indirect general sympathomimetic; releases stored catecholamines
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mechanism of cocaine
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indirect general sympathomimetic; uptake inhibitor
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clonidine
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centrally acting alpha-2 agonist; causes decreased central adrenergic outflow
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phenoxybenzamine
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irreversible non-selective alpha blocker; use before removing pheochromocytoma
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phentolamine
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reversable non-selective alpha blocker
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prazosin
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selective alpha-1 blocker; use for hypertension, urinary retention in BPH
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mirtazapine
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selective alpha-2 blocker; use in depression
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why are beta blockers used in SVT?
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(propranolol and esmolol) class II antiarrhythmics, decrease AV conduction velocity
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nonselective beta blockers?
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propranolol, timolol, nadolol, pindolol
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beta-1 selective beta blockers?
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acebutolol, betaxolol, esmolol, atenolol, metoprolol
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non-selective alpha and beta antagonists?
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carvedilol, labetalol
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partial beta agonists?
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pindolol, acebutolol
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antidote for acetaminophen
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n-acetylcysteine
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antidote for salicylates
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sodium bicarb (alkanize urine), dialysis
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antidote for amphetamines
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ammonium chloride (acidify urine)
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antidote for acetylcholinesterase inhibitors, organophosphates
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atropine, pralidoxime
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antidote for antimuscarinic, anticholinergic agents
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physostigmine salicylate
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antidote for beta-blockers
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glucagon
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antidote for digitalis
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stop dig, normalize K+, lidocaine, anti-dig Fab fragments, Mg2+
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antidote for iron
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deferoxamine
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antidote for lead
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CaEDTA, dimercaprol, succimer, penicillamine
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antidote for mercury, arsenic, gold
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dimercaprol, succimer
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antidote for copper, arsenic, gold
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penicillamine
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antidote for cyanide
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nitrite, hydroxocobalamin, thiosulfate
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antidote for methemoglobin
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methylene blue, vitamin C
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antidote for carbon monoxide
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100% O2, hyperbaric O2
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antidote for methanol, ethylene glycol
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ethanol, dialysis, femepizole
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antidote for opiods
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naloxone/naltrexone
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antidote for benzodiazepines
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flumazenil
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antidote for TCAs
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sodium bicarb (alkalinize plasma)
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antidote for heparin
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protamine
|
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antidote for warfarin
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Vitamin K, fresh-frozen plasma
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antidote for tPA, streptokinase
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aminocaproic acid
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antidote for theophylline
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beta-blocker
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causes atropine-like side effects?
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TCAs
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causes coronary vasospasm?
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cocaine, sumatriptan
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causes cutaneous flushing?
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Vancomycin
Adenosine Niacin Ca2+ channel blockers |
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causes dilated cardiomyopathy?
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doxorubicin, daunorubicin
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causes Torsades de pointes
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class III antiarrhythmics (sotalol)
class IA (quinidine) |
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causes agranulocytosis
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clozapine, carbamazepine, colchicine, propylthiouracil, methimazole, dapsone
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causes aplastic anemia
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chloramphenicol, benzene, NSAIDs, propylthiouracil, methimazole
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causes direct Coombs-positive hemolytic anemia
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methyldopa
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causes gray baby syndrome
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chloramphenicol
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causes hemolysis in G6PD deficient patients?
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Isoniazid
Sulfonamides Primaquine Aspirin Ibuprofen Nitrofurantoin |
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causes megaloblastic anemia?
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Phenytoin, Methotrexate, Sulfa drugs
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causes thrombotic complications
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OCPs
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antihypertensive class that causes cough?
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ACE inhibitors
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causes pulmonary fibrosis?
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Bleomycin, Amiodarone, Busulfan
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meds that cause acute cholestatic hepatitis?
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macrolides
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causes focal to massive hapatic necrosis?
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halothane, valproic acid, acetaminophen, Amanita phalloides
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causes hepatitis
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INH
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causes pseudomembranous colitis
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clindamycin, ampicillin
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causes adrenocortical insufficiency
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glucocorticoid withdrawal
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causes gynecomastia?
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Spironolactone, Digitalis, Cimetidine, chronic Alcohol use, estrogens, Ketoconazole
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causes hot flashes?
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tamoxifen, clomiphene
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causes hypothyroidism?
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lithium, amiodarone
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causes gingival hyperplasia?
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phenytoin
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causes gout
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furosemide, thiazides
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medications that cause osteoporosis?
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corticosteroids, heparin
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medications that cause photosensitivity?
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Sulfonamides, Amiodarone, Tetracycline
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causes stevens-johnson syndrome?
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Ethosuximide, lamotrigine, carbamazepine, phenobarbital, phenytoin, sulfa drugs, penicillin, allopurinol
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causes SLE-like syndrome?
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Hydralazine, INH, Procainamide, Phenytoin
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causes tendonitis, tendon rupture, cartilage damage (in kids)
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fluoroquinolones
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causes fanconi's syndrome?
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expired tetracycline
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causes interstitial nephritis?
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methicillin, NSAIDs, furosemide
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causes hemorrhagic cystitis?
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cyclophosphamide, ifosfamide
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causes cinchonism?
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quinidine, quinine
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causes diabetes insipidus
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lithium, demeclocycline
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causes parkinson-like syndrome?
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haloperidol, chlorpromazine, reserpine, metoclopramide
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causes seizures?
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bupropion, imipenem/cilastatin, isoniazid
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causes tardive dyskinesia
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antipsychotics
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causes disulfiram-like reaction?
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metronidazole, certain cephalosporins, procarbazine, 1st gen sulfonylureas
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antimicrobial class that causes nephrotoxicity/neurotoxicity?
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polymyxins
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causes nephrotoxicity/ototoxicity?
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aminoglycosides, vancomycin, loop diuretics, cisplatin
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P450 inducers?
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Quinidine
Barbiturates St. John's wort Phenytoin Rifampin Griseofulvin Carbamazepine Chronic alcohol use |
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P450 inhibitors?
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HIV protease inhibitors
Ketoconazole Erythromycin Grapefruit juice Acute alcohol use Sulfonamides Isoniazid Cimetidine |
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alcohol metabolism depletes ______?
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NAD+
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-afil
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erectile dysfunction (sildenafil)
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-ane
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inhalational general anesthetic (halothane)
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-azepam
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benzodiazepine (diazepam)
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-azole
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antifungal (ketoconazole)
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-barbital
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barbituate (phenobarbital)
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-caine
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local anesthetic (lidocaine)
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-cillin
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penicillin
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-ipramine
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TCA (imipramine)
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-navir
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protease inhibitor (saquinavir)
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-olol
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beta-antagonist (propranolol)
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-operidol
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neurolepic (haloperidol)
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-oxin
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cardiac glycoside (digoxin)
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-phyllin
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methylxanthine (theophylline)
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-pril
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ACE inhibitor (captopril)
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-terol
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beta-2 agonist (albuterol)
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-tidine
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H2 antagonist (cimetidine)
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-triptan
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5-HT agonist for migraine (sumatriptan)
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-triptyline
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TCA (amitriptyline)
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-tropin
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pituitary hormone (somatotropin)
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-zolam
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benzodiazepine (alprazolam)
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-zosin
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alpha-1 antagonist (prazosin)
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antimicrobials that block cell wall synthesis by inhibition of peptidoglycan cross linking?
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beta-lacams:
penicillins, cephalosporins, monobactams (aztreonam), carbapenems |
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antimicrobials that block peptidoglycan synthesis?
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bacitracin, vancomycin
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antimicrobials that disrupt bacterial cell membranes?
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polymyxins
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antimicrobials that block nucleotide synthesis?
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sulfonamides, trimethoprim
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antimicrobials that block DNA topoisomerases?
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fluoroquinolones
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antimicrobials that block mRNA synthesis?
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rifampin
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antimicrobials that block protein synthesis at 30S ribosomal subunit?
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Aminoglycosides
Tetracyclines |
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antimicrobials that block protein synthesis at 50S ribosomal subunit?
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Chloramphenicol, Clindamycin
Erythromycin Lincomycin Linezolid |
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bacteriostatic antibiotics?
|
Erythromycin
Clindamycin Sulfamethoxazole Trimethoprim Tetracyclines Chloramphenicol |
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antibiotic for MSSA?
|
nafcillin (or other penicillinase-resistant penicillin… methicillin, dicloxacillin, etc)
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beta-lactamase inhibitors?
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clavulanic acid, sulbactam, tazobactam
inhibit penicillinase (beta-lactamase) |
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1st gen cephalosporins: eg. and use?
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cefazolin, cephalexin
Proteus, E coli, Klebsiella |
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2nd gen cephalosporins: eg and use?
|
cefoxitine, cefuroxime
Haemophilus influenzae, Enterobacter aerogenes, Neisseria, Proteus, E coli, Klebsiella, Serratia marcencens |
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3rd gen cephalosporins: eg and use?
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ceftriaxone, ceftazidime
use for serious gram-neg infections like meningitis and gonorrhea (ceftriaxone) or pseudomonas (ceftazidime) |
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4th gen cephalosporins: eg and use?
|
cefepime; incrased activity against pseudomonas and gram-pos organisms
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vitamin deficiency seen with cephalosporins?
|
vitamin K
|
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toxicities of carbapenems?
|
GI distress, skin rash, seizures
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MOA of vancomycin?
|
inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursors
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mechanism of resistance to vancomycin?
|
amino acid change of D-ala D-ala to D-ala D-lac
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mechanism of aminoglycosides?
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30S inhibitor; bactericidal
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mechanism of tetracycline?
|
30S inhibitor; bacteriostatic
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mechanism of chloramphenicol?
|
50S inhibitor; bacteriostatic
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mechanism of clindamycin?
|
50S inhibitor; bacteriostatic
|
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mechanism of erythromycin?
|
50S inhibitor; bacteriostatic
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mechanism of lincomycin?
|
50S inhibitor; bacteriostatic
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mechanism of linezolid?
|
50S inhibitor; bacteriostatic/bacteriocidal (variable)
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examples of aminoglycosides?
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gentamicin, neomycin, amikacin, tobramycin, streptomycin
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toxicities of aminoglycosides?
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nephrotoxic, ototoxic, teratogeneic
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mechanism of resistance to aminoglycosides?
|
transferase enzymes inactivate the drugs (acetylation, phosphorylation, adenylation)
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special notes on administration of doxycycline?
|
fecally eliminated, can be used in patients with renal failure; must avoid milk, antacids, iron-containing preparations because divalent cations will inhibit absorption in gut
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drug that accumulates intracellularly and is used for rickettsia and chlamydia?
|
tetracycline/doxycycline
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examples of macrolides?
|
erythromycin, azithromycin, clarithromycin
|
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clinical use of macrolides?
|
(erythromycin/azithromycin)
atypical pneumonias, URIs, STDs, gram-positive cocci, neisseria |
|
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toxicity of macrolides?
|
(erythromycin/azithromycin)
prolonged QT interval, GI discomfort, acute cholestatic hepatitis, eosinophila, skin rashes |
|
|
clinical use of clindamycin?
|
anaerobic infections above diaphragm
|
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treatment for anaerobic infections?
|
above diaphragm: clindamycin
below diaphragm: metronidazole |
|
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MOA of sulfonamides?
|
PABA antimetabolites, inhibit dihydropteroate synthetase. Bacteriostatic.
|
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clinical use of TMP-SMX?
|
recurrent UTIs, Shigella, Salmonella, Pneumocystic jiroveci pneumonia
|
|
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mechanism of fluroquinolones?
|
(ciprofloxicin, etc)
inhibit DNA gyrase/topoisomerase II |
|
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mechanism of metronidazole?
|
forms free radical toxic metabolites in bacterial cell, damage DNA
|
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clinical uses of metronidazole?
|
Giardia
Entamoeba Trichomonas Gardnerella vaginalis Anaerobes (bacteroides, clostridium) h Pylori |
|
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metronidazole toxicity?
|
disulfiram-like reaction with alcohol, headache, metallic taste
|
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polymyxins - eg, MOA, clinical use, toxicity?
|
polymyxin B, colistimethate
acts like detergent, disrupts cell membranes of bacteria used for resistant gram-negative infections neurotoxic, renal ATN |
|
|
prophylaxis and treatment for M. tuberculosis?
|
ppx: isoniazid
tx: Rifampin, Isoniazid, Pyrazinamide, Ethambutol |
|
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prophylaxis and treatment for M. avium-intracellulare?
|
ppx: azithromycin
tx: Azithromycin, Rifampin, Ethambutol, Streptomycin |
|
|
treatment for M. leprae (leprosy)?
|
Dapsone, rifampin, clofazimine
|
|
|
anti-TB drug that causes red-green color blindness?
|
ethambutol
|
|
|
MOA of ethambutol?
|
(anti TB)
decreases carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase |
|
|
mechanism of pyrazinamide?
|
(anti TB)
effective in acidic pH of phagolysosomes where TB engulfed by macrophages is found |
|
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MOA of isoniazid (INH)
|
decreases synthesis of mycolic acids; bacteria catalase-peroxidase is needed to convert INH to active metabolite
|
|
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toxicity of isoniazid?
|
"INH Injures Neurons and Hepatocytes"
-neurotixicity, hepatotoxicity, lupus -pyridoxine (vitamin B6) can prevent neurotoxicity and lupus |
|
|
MOA of rifampin
|
inhibits DNA-dependent RNA polymerase
|
|
|
4 R's of rifampin?
|
RNA polymerase inhibitor
Revs up microsomal P-450 Red/orange body fluids Rapid resistance if used alone |
|
|
ppx against meningococcal infections?
|
rifampin, minocycline
|
|
|
ppx against gonorrhea?
|
ceftriaxone
|
|
|
ppx against syphilis?
|
Benzathine penicillin G
|
|
|
ppx against recurrent UTIs?
|
TMP-SMX
|
|
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ppx against pneumocystis jiroveci pneumonia
|
TMP-SMX, aerosolized pentamidine
|
|
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ppx against endocarditis during surgical/dental procedures?
|
penicillins
|
|
|
ppx against mycobacterium avium intracellulare?
|
azithromycin
|
|
|
tx of MRSA?
|
vancomycin
|
|
|
tx of VRE?
|
linezolid and streptogramins (quinupristin/dalfopristin)
|
|
|
MOA of amphotericin B?
|
(antifungal)
binds ergosterol; forms membrane pores that allow leakage of electrolytes |
|
|
MOA of -azoles?
|
inhibit fungal sterol synthesis by inhibiting P-450 enzyme that converst lanosterol to ergosterol
|
|
|
treatment for cryptococcal meningitis in AIDS patients?
|
fluconazole (can cross blood-brain barrier)
|
|
|
MOA of flucytosine?
|
(antifungal)
inhibits DNA synthesis by conversion to 5-fluorouracil |
|
|
MOA of caspofungin?
|
(antifungal)
inhibits cell wall synthesis by inhibiting synthesis of beta-glucan; used for invasive aspergillosis |
|
|
MOA of terbinafine?
|
(antifungal)
inhibits fungal enzyme squalene epoxidase |
|
|
MOA of griseofulvin?
|
(antifungal)
interferes with microtubule function, disrups mitosis |
|
|
mechanism of amantadine being used in parkinson's?
|
causes release of dopamine from intact nerve terminals
|
|
|
MOA of oseltamivir?
|
inhibits influenza neuraminidase, decreasing release of progeny virus
|
|
|
MOA of ribavirin?
|
inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase; used for RSV, chronic hepatitis C
|
|
|
clinical use of ganciclovir?
|
CMV
|
|
|
MOA and use of foscarnet?
|
viral DNA polymerase inhibitor, binds to pyrophosphate-binding site of enzyme; used in CMV retinitis
|
|
|
clinical use of interferon alpha?
|
chronic hepatitis B and C
kaposi's sarcoma |
|
|
clinical use of interferon beta?
|
MS
|
|
|
clinical use of interferon gamma?
|
NADPH oxidase deficiency
|
|
|
antibiotics to avoid in pregnancy
|
Sulfonamides
Aminoglycosides Fluoroquinolones Erythromycin Metronidazole Tetracyclines Ribavirin Griseofulvin Chloramphenicol |
|
|
hepatitis C medication that can cause hemolytic anemia?
|
ribavirin; note that ribavirin is also severe teratogen
|
|
|
mechanism of statins?
|
inhibit HMG-CoA, thereby inhibiting mevalonate
|
|
|
mechanism of Niacin (hyperlipidemia)?
|
inhibits lipolysis in adipose tissue, reduces hepatic VLDL secretion into circulation
|
|
|
bile acid resins: examples, MOA
|
cholestyramine, colestipol, colesevelam
prevent intestinal reabsorption of bile acids; liver must use cholesterol to make more |
|
|
MOA of ezetimibe?
|
prevents cholesterol reabsorption at small intestine brush border
|
|
|
MOA of fibrates?
|
upregulates lipoprotein lipase
|
|
|
statin effects on LDL/HDL/TGs?
|
decrease LDL
slight increase HDL slight decrease TG |
|
|
niacin effects on LDL/HDL/TGs?
|
decrease LDL
increase HDL slight decrease TG |
|
|
bile acid resin effects on LDL/HDL/TGs?
|
decrease LDL
slight increase HDL slight increase TG |
|
|
ezetimibe effects on LDL/HDL/TGs?
|
decrease LDL
no change HDL no changeTG |
|
|
fibrates effects on LDL/HDL/TGs?
|
slight decrease LDL
slight increase HDL decrease TG (major effect) |
|
|
which hyperlipidemia med has primary effect of decreasing TG?
|
fibrates
|
|
|
which hyperlipidemia med inhibits lipolysis in adipose tissue?
|
niacin
|
|
|
which hyperlipidemia med upregulates LPL?
|
fibrates
|
|
|
phenytoin toxicities (chronic use)?
|
gingival hyperplasia in children
peripheral neuropathy hirsuitism decreased folate absorption -> megaloblastic anemia note: teratogenic, cytochrome P-450 inducer |
|
|
effect of spironolactone on potassium?
|
"spares" potassium (ie retains it), so can lead to hyperkalemia
|
|
|
mechanism of vincristine, vinblastine?
|
bind to tubulin in M phase and blocks polymerization so that mitotic spinkle cannot form
|
|
|
mechanism of paclitaxel?
|
hyperstabilizes polymerized microtubules in M phase so that mitotic spindle cannot break down (blocks progression into anaphase)
|
|
|
gram positive bacilli in CSF?
|
Listeria monocytogenes meningitis; treat with ampicillin
|
|
|
clinical use for ampicillin?
|
Haemophilus influenzae
E coli Listeria monocytogenes Proteus mirabilis Salmonella Enterococci |
|
|
MOA of NO relieving angina?
|
venodilation (at low doses) causing decreased preload, decreased myocardial demand
|
|
|
treatment of atypical pneumonia?
|
Macrolides (Azithromycin)
|
|
|
MOA of azithromycin (macrolide)?
|
inhibits protein synthesis by blocking translocation of 23S rRNA during translation
|
|
|
increased fibrin split products?
|
DIC
|
|
|
treatment of TCA poisoning/overdose?
|
alkalinization of plasma (bicarb)
|
|
|
MOA of methotrexate
|
folic acid analog, inhibits dihydrofolate reductase -> decreased DNA and decreased protein synthesis
|
|
|
MOA of 5-fluorouracil (5-FU)
|
pyrimidine analog; inhibits tymidylate synthase and decreases DNA/protein synthesis
|
|
|
MOA of 6-mercaptopurine?
|
purine analog, decreases de novo purine synthesis; activated by HGPRTase
|
|
|
MOA of cytarabine?
|
pyrimidine antagonist, inhibits DNA polymerase
|
|
|
MOA of cyclophosphamide?
|
covalently X-links DNA at guanine N-7
requires bioactivation by liver |
|
|
MOA of busulfan
|
alkylates DNA; used in CML
|
|
|
MOPP regimin for Wilms' tumor?
|
Mechlorethamin
Oncovin (vincristine) Procarbazine Prednisone |
|
|
MOA of cholestyramine, colestipol?
|
bile acid sequestrants (bind and excrete bile acids in intestine, force liver to use plasma cholesterol to synthesize new bile acids)
|
|
|
risk/benefit of tamoxifen?
|
may increase risk of endometrial carcinoma via partial agonist effects; raloxifene is endometrial antagonist and does not have this risk
|
|
|
antitumor drugs that can cause cardiotoxicity?
|
doxorubicin and daunorubicin (noncovalently intercalate in DNA); used for Hodgkin's lymphomas, myelomas, sarcomas, solid tumors
|
|
|
MOA of acyclovir?
|
inactive precursor is monophosphorylated by HSV/VZV thymidine kinase leading to guanosine analog that preferentially inhibits viral DNA polymerase by chain termination
|
|
|
which classes of anti-cancer drugs act during S phase (DNA synthesis)?
|
antimetabolites
etoposide |
|
|
drug targetted to aberrant tyrosine kinase in CML?
|
imantinib
|
|
|
MOA of amantadine used vs. influenza A?
|
binds to M2 protein on influenza A virus, preventing viral uncoating
|
|
|
antitumor drug that causes pulmonary fibrosis and skin changes?
|
bleomycin
|
|
|
toxicities of aspirin?
|
gastric ulceration, bleeding, hyperventilation, Reye's syndrome, tinnitus
|
|
|
tumor-associated syndrome that presents with diarrhea, cutaneous flushing, asthmatic wheezing, right-sided valvular heart disease?
|
carcinoid syndrome, seen when neuroendocrine tumor secreting serotonin metastasizes to liver
|
|
|
common triple therapy regimens for H pylori?
|
bismuth, metronidazole, tetracycline/amoxicillin
omeprazole, metronidazole, clarithromycin |
|
|
early signs of lithium toxicity?
|
memory impairment/confusion, nausea and vomiting, dysarthria, lethargy, coarse hand tremors with hypothyroidism and DI
|
|
|
lab values seen in nephrogenic DI?
|
high serum sodium, high serum osmolality, low urine osmolality
|
|
|
cardiac abnormality seen with use of lithium during pregnancy?
|
Ebstein's anomaly (downward displacement of tricuspid valve and atrial septal defect)
|
|
|
type of antiarrhythmics that cause torsades de pointes?
|
Class IA due to increased QT interval
|
|
|
Class I antiarrhythmics
|
Na+ channel blockers
|
|
|
Class IA antiarrhythmics?
|
quinidine, procainamide, disopyramide
|
|
|
Class IB antiarrhythmics?
|
Lidocaine, Mexiletine, Tocainide
|
|
|
Class IC antiarrhythmics?
|
Flecainide, Encainide, Propafenone
|
|
|
electrolyte abnormality that increases class I antiarrhythmic toxicity?
|
hyperkalemia
|
|
|
use of Class I antiarrhythmics after MI?
|
IB is "best"
IC is "contraindicated" |
|
|
adverse effects of clozapine?
|
(atypical antipsychotic used for refractory schizophrenia)
agranulocytosis, weight gain, hypotension, mild sedation |
|
|
pharmacologic treatment of gastroparesis?
|
metoclopramide: antiemetic that causes relaxation of pylorus
functions as D2-receptor antagonist, can cause EPS side effects |
|
|
treatment of neuroleptic malignant syndrome?
|
bromocriptine (dopamine agonist)
|
|
|
drugs of choice in treating type IIa and IIb familial hyperlipidemia?
|
bile acid binding resins to decrease plasma LDL cholesterol levels
|
|
|
treatment for neurogenic bladder?
|
cholinomimetic -> bethanechol (long duration of action)
|
|
|
lumbar puncture with elevated RBCs, negative xanthochromia?
|
possible herpes encephalitis/viral meningitis causing cerebral hemorrhage
|
|
|
mechanism and side effects of ondansetron?
|
(zofran)
5-HT3 antagonist side effects include headache and constipation |
|
|
first line treatment for bacterial meningitis in adults?
|
third-gen cephalosporin like ceftriaxone
|
|
|
treatment of neuroleptic induced acute dystonia?
|
anticholinergic agents (benztropine)
|
|
|
basic difference in MOA between typical and atypical antipsychotics?
|
typical: inhibit D2 receptors
atypical: inhibit serotonin AND dopamine receptors |
|
|
treatment of wilson's disease?
|
penicillamine
|
|
|
used to reverse tPA in case of excess bleeding?
|
aminocaproic acid
|
|
|
main effects of beta blockers in hypertensino?
|
•reduction in cardiac output
•reduction of renin release from juxtaglomerular apparatus •reduction of sympathetic activity |
|
|
mechanism of phenytoin?
|
blocks sodium channels
increases refractory period inhibits release of glutamate from excitatory presynaptic neurons |
|
|
where does beta-lactamase interact with penicillin?
|
in space around bacterium
|
|
|
MOA of penicillins?
|
1. binds penicillin-binding proteins
2. blocks transpeptidase cross-linking of cell wall 3. activates autolytic enzymes |
|
|
mechanism of resistance vs. penicillins/cephalosporins?
|
beta-lactamase cleavage of beta-lactam ring or altered PBP
|
|
|
mechanism of resistance vs. aminoglycosides?
|
modification via acetylation, adenylation, or phosphorylation
|
|
|
mechanism of resistance vs. vancomycin?
|
replaces d-ala d-ala with d-ala d-lac causing decreased affinity
|
|
|
mechanism of resistance vs. chloramphenicol
|
modification via acetylation
|
|
|
mechanism of resistance vs. macrolides?
|
methylation of rRNA near erythromycin's ribosome-binding side
|
|
|
mechanism of resistance vs. tetracycline?
|
decreased uptake or increased transport out of cell
|
|
|
mechanism of resistance vs. sulfonamides?
|
altered enzyme, decreased uptake, or increased PABA synthesis
|
|
|
mechanism of resistance vs. quinolones?
|
altered gyrase or reduced uptake
|
|
|
structure of acyclovir?
|
guanosine analog
|
|
|
negative Monospot mononucleosis?
|
CMV infection
|
|
|
clotting and dropping platelet levels while on heparin?
|
HIT; treatment is to stop heparin and start on direct thrombin inhibitor
|
|
|
MOA of lactulose to treat hepatic encephalopathy?
|
acidifies colonic contents, causing ammonia trapping in intestines
|
|
|
treatment for giardia lamblia?
|
metronidazole
|
|
|
treatment for entamoeba histolytica?
|
metronidazole and iodoquinol
|
|
|
treatment for toxoplasma gondii?
|
sulfadiazine and pyrimethamine
|
|
|
antimalarial with cardiac complications?
|
quinines can cause torsades de pointes
|
|
|
MOA of dactinomycin?
|
(antitumor antibiotic)
intercalates in DNA |
|
|
MOA of doxorubicin, daunorubicin?
|
(antitumor antibiotic)
noncovalently intercalates in DNA causing breaks in DNA |
|
|
MOA of bleomycin?
|
(antitumor antibiotic)
induces formation of free radicals |
|
|
MOA of etoposide, teniposide?
|
(antitumor antibiotic)
inhibits topoisomerase II leading to DNA degradation |
|
|
transplant medication known for nephrotoxic effects?
|
cyclosporine
|
|
|
MOA of cyclosporine?
|
blocks T-lymphocyte production of IL-2, preventing differentiation and early activation of T lymphocytes
|
|
|
medication used in conjunction with NSAIDs to reduce incidence of peptic ulcers?
|
misoprostol (prostaglandin E1 analog)
|
|
|
clinical uses of misoprostol?
|
(prostaglandin E1 analog)
1. decreases incidence of NSAID-related peptic ulcers 2. medical termination of pregnancy <49 days 3. cervical ripening and labor induction (off label) |
|
|
anticoagulant of choice in pregnancy?
|
unfractionated heparin (does not cross placenta) but must be discontinued before delivery
|
|
|
MOA and clinical use of abciximab?
|
monoclonal antibody, binds to glycoprotein receptor IIb/IIIa on activated platelets
used in ACS, percutaneous transluminal coronary angioplasty |
|
|
hyperlipidemia medication that can cause cholesterol gallstones?
|
fibrates
|
|
|
effect of HCTZ on acid/base status?
|
causes metabolic alkalosis through loss of hydrogen ion into cells in exchange for potassium and loss of hydrogen in urine
|
|
|
new onset glucose intolerance, coarsening of facial features, joint pain, increased hand and foot size, macrogloassia?
|
acromegaly, likely caused by GH-secreting pituitary tumor
treated with octreotide |
|
|
MOA of benzodiazepines vs. barbituates?
|
benzodiazepines increase frequency of chloride channel opening, barbituates increase duration of opening
|
|
|
breast cancer med that targets HER-2 receptor?
|
trastuzumab
|
|
|
MOA of hydralazine?
|
increases cGMP leading to smooth muscle relaxation
vasodilates arterioles > veins causing afterload reduction |
|
|
medication with anti-steroid effect that can be used to inhibit effects of ectopic ACTH-secreting tumors?
|
ketoconazole
|
|
|
cause of cushing's syndrome?
|
increased cortisol
|
|
|
long-acting beta-2 agonist used for asthma prophylaxis?
|
salmeterol
|
|
|
MOA of tamoxifen, raloxifen?
|
SERMs: block binding of estrogen to estrogen receptor-positive cells
|
|
|
oral hypoglycemic associated with lactic acidosis?
|
metformin
|
|
|
oral hypoglycemic associated with disulfiram-like effects?
|
first gen sulfonylureas (tolbutamide, chlorpropamide)
|
|
|
oral hypoglycemic associated with weight gain, edema, CV toxicity?
|
glitazones (pioglitazone, rosiglitazone)
|
|
|
treatment for essential thrombocytosis?
|
hydroxyurea (interferes with DNA synthesis)
|
|
|
what mutations are commonly seen in polycythemia vera, essential thrombocytosis, and myelofibrosis?
|
JAK2 mutations (JAK2 involved in hematopoietic growth factor signaling)
|
|
|
site of action of furosemide?
|
loop diuretic: blocks co-transport system of Na+-K+-2Cl- in thick ascending limb of loop of Henle
note: also causes increased calcium excretion |
|
|
site of action of acetazolamide?
|
(diuretic)
proximal convoluted tubule |
|
|
site of action of thiazide diuretics?
|
distal convoluted tubule
|
|
|
site of action of potassium sparing diuretics?
|
distal convoluted tubule
|
|
|
site of action of ADH antagonists?
|
collecting tubule
|
|
|
HAART medications that cause lipdystrophy?
|
protease inhibitors (-navir)
|
|
|
protease inhibitors used in HAART?
|
-navir meds (ritonavir, saquinavir, etc)
|
|
|
MOA of protease inhibitors used in HAART?
|
inhibit maturation of new virus by blocking protease in progeny virions
|
|
|
gout medications that inhibit uric acid reabsorption in the proximal collecting tubule?
|
prebenecid and sulfinpyrazone
|
|
|
MOA of allopurinol?
|
blocks xanthine oxidase, preventing formation of uric acid from purines
|
|
|
medication class NOT to give in gout?
|
salicylates (all but highest doses depress uric acid clearance in kidney)
|
|
|
clearance of what medications is affected by allopurinol?
|
azathioprine and 6-MP (both normally metabolized by xanthine oxidase)
|
|
|
pulmonary function tests that indicate restrictive lung disease?
|
reduced FEV1 and FVC, but normal FEV1:FVC ratio
|
|
|
common amiodarone side effects?
|
pulmonary fibrosis, hepatotoxicity, hypo/hyperthyroidism
(check PFTs, LFTs, TFTs!) |
|
|
antiarrhythmic that causes skin deposits resulting in blue/gray color?
|
amiodarone
|
|
|
HIV associated infections at CD4<50?
|
CMV retinitis and esophagitis, disseminated MAI, cryptococcal meningoencephalitis
|
|
|
HIV associated infections at CD4<100?
|
candidal esophagitis toxoplasmosis, histoplasmosis
|
|
|
class of medications with similar action to cocaine?
|
any reuptake inhibitors (SSRIs etc)
|
|
|
MOA of sulfonylureas in type II diabetes?
|
bind to sulfonylrea receptor on beta-islet cells, leading to release of pre-formed insulin
|
|
|
illicit drug that acts as NMDA receptor antagonist?
|
phencyclidine
|
|
|
MOA of tacrolimus?
|
inhibits calcineurin, leading to inhibition of T-lymphocyte signaling
|
|
|
when is Coombs' test positive?
|
autoimmune hemolytic anemia
|
|
|
MOA of phenobarbital in seizure treatment?
|
increases GABA action
|
|
|
MOA of gabapentin in seizure treatment?
|
designed as GABA analog, but primarily inhibits HVA calcium channels
|
|
|
MOA of isoniazid?
|
decreases synthesis of mycolic acids
|
|
|
MOA of rituximab?
|
monoclonal antibody specific for CD20
|
|
|
mechanism of MAO-Is?
|
inhibit monoamine oxidase, which degrades norpinephrine, dopamine, and serotonin
|
|
|
mechanism of hypertensize crisis associated with tyramine ingestion while taking MAO-I?
|
tyramine accumulates and leads to release of stored norepinephrine
|
|
|
examples of nonselective MAO-Is?
|
phenelzine, tranylcypromine, isocarboxazid
|
|
|
selective MAO-B inhibitor?
|
selegiline
|
|
|
examples of SSRIs?
|
fluoxetine, paroxetine, sertraline, citalopram
|
|
|
treatment for serotonin syndrome?
|
cyproheptadine (5-HT receptor antagonist)
|
|
|
lithium side effects?
|
Movement (tremor)
Nephrogenic diabetes insipidus hypOthyroidism Pregnancy problems |
|
|
antibiotic known for causing long QT syndrome?
|
erythromycin
|
|
|
examples of atypical antipsychics
|
olanzapine, clozapine, quetiapine, resperidone, aripiprazole, ziprasidone
|
|
|
atypical antipsychotic that can cause agranulocytosis?
|
clozapine
|
|
|
examples of short acting benzodiazepines?
|
trazolam, oxazepam, midazolam
|
|
|
MOA of glitazones?
|
(oral hypoglycemics)
increase insulin sensitivity in peripheral tissues by binding and modulating peroxisome proliferator-activated receptors |
|
|
second line treatment of CMV when ganciclovir is ineffective?
|
foscarnet
MOA: inhibits DNA polymerase at pyrophosphate binding site |
|
|
histology of crohns vs UC?
|
Crohns is transmural, UC is restricted to mucosal and submucosal layers
|
|
|
pharmacologic treatment of UC?
|
first line: aspirin treatments (sulfasalazine)
second line: infliximab |
|
|
pharmacologic treatment of crohns?
|
corticosteroids, infliximab
|
|
|
Hep C treatment that can cause hemolytic anemia?
|
ribavirin
note: NOT immune mediated; negative coomb's test |
|
|
antiseizure med associated with neural tube defects if taken during pregnancy?
|
valproic acid
|
|
|
valproic acid side effects?
|
hepatotoxicity (rare but fatal)
neural tube defects in fetus tremor, weight gain, GI distress |
|
|
anti-seizure meds associated with stevens-johnson syndrome?
|
carbamazepine, ethosuximide, lamotrigine
|
|
|
HAART med used to reduce vertical transmission during pregnancy?
|
zidovudine (AZT) monotherapy
|
|
|
mechanism of zidovudine (AZT)?
|
nucleoside reverse transcriptase inhibitor
|
|
|
quinidine MOA and toxicity?
|
Class IA sodium channel blocker
causes cinchonism, thrombocytopenia, torsades de pointes (due to increased QT interval) |
|
|
cinchonism?
|
headache and tinnitus, caused by quinidine (class IA sodium channel blockers)
|
|
|
antihypertensives that should not be used in conjunction with spironolactome?
|
ACE inhibitors (combo can cause hyperkalemia)
|
|
|
medication given with cyclophosphamide to prevent development of hemorrhagic cystitis?
|
mesna disulfide
|
|
|
pharmacologic treatment for Wolff-Parkinson-White syndrome?
|
amiodarone (potassium channel blockers)
|
|
|
fast acting inhaled anesthetic agent associated with increased incidence of seizures?
|
enflurane
|
|
|
common side effect of halothane?
|
hepatotoxicity
|
|
|
medication shown to decrease risk of suicide in bipolar disease?
|
lithium
|
|
|
recommended treatment for invasive aspergillus?
|
voriconazole
|
|
|
mechanism, toxicities of voriconazole?
|
blocks fungal cytochrome P450 enzyme 14-alpha demethylase
toxicities include visual disturbances and QTc prolongation |
|
|
hepatitis medication associated with flu-like reaction and periodic profound depression?
|
interferon (pegylated is long-acting form)
|
|
|
MOA of heroin and other opiates?
|
stimulates mu receptors
|
|
|
antitumor drug that inhibits topoisomerase II, thereby increasing DNA degradation?
|
etoposide
|
|
|
side effect seen with expired tetracycline?
|
fanconi's syndrome: disorder of proximal tubule function resulting in severe loss of protein, glucose, and essential minerals
|
|
|
MOA of macrolides?
|
bind to 23S ribosomal RNA of prokaryotic 50S ribosome, blocking translocation step of protein synthesis
|
|
|
HAART medication associated with crystal-induced nephropathy?
|
ininavir (protease inhibitor)
|
|
|
side effects of chloramphenicol?
|
anemia, aplastic anemia, gray baby syndrome
|
|
|
cephalosporins effective against pseudomonas?
|
cefoperazone, ceftazidime, cefepime
|
|
|
chronic industrial exposure that leads to weekend/monday morning headaches, dizziness, palpitations?
|
nitric oxide
|
|
|
ketoconazole is a cytochrome P450 inducer/inhibitor?
|
inhibitor
|
|
|
clinical use of griseofulvin?
|
antifungal used for topical infections (tinea or ringworm)
|
