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380 Cards in this Set
- Front
- Back
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what does a lower Km signify
|
the enzyme has increased affinity for that substrate
|
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differentiate what competitive and noncompetitive inhibitors do to Vmax, Km, and pharmacodynamics
|
competitive: unchanged Vmax, increased Km (decreased affinity), decreased potency (need more substrate for same effect)
noncompetitive: decreased Vmax = decreased efficacy, unchanged Km |
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a drug infused at a constant rate takes how long to reach steady state
|
4-5 half lifes
1 = 50% 2 = 75% 3 = 87.5% 4 = 93.75% |
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|
loading dose
|
(plasma concentration) x (volume of distibution) / bioavailability
|
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when does bioavailability = 1
|
drug is given IV
|
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Maintenance dose
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(plasma concentration) x (clearance) / bioavailability
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does loading dose and maintenance does change in renal or liver disease
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Only maintenance does changes, loading dose is unchanged
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zero-order elimination
|
rate of elimination is constant regardless of plasma concentration
|
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examples of zero-order elimination
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phenytoin
ethanol aspirin (high or toxin concentrations) |
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first-order elimination
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rate of elimination is proportional to the drug concentration
plasma concentration decreased exponentially with time |
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what form does the drug need to be in order to be "trapped" in the urine and cleared quickly
|
ionized species
|
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differentiate phase I and phase II metabolism
|
phase I - cytochrome P450, reduction, oxidation, hydrolysis - often still active
phase II - conjugation via acetylation, glucuronidation, sulfation - inactive metabolites |
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efficacy
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maximal effect a drug can produce
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potency
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amount of drug needed for a given effect
|
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partial agonists effects when added with agonist
|
acts at the same site with reduced maximal effect - decreases efficacy but the potency can be variable (increased or decreased)
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substance that produces the opposite physiologic by acting on a different receptor
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physiologic antagonism
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when stimulated do dopamine receptors on blood vessels cause vasoconstriction or vasodilation
|
vasodilation (D1 found in renal vascular smooth msucle)
|
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neurotransmitter receptor that's activated on smooth muscle
|
Nicotinic ACh receptor
|
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neurotransmitter receptor that's activated on sweat glands
|
Muscarinic ACh receptor
|
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what toxin prevents release of neurotransmitters at all cholinergic terminals, including those to sweat glands and adrenal medulla
|
botulinum toxin
|
|
|
differentiate vasopressin receptors V1 and V2
|
V1 - vascular smooth muscle contraction
V2 - increase H20 permeability in collecting tubules |
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where are H2 receptors found
|
stomach - increase gastric acid secretion
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receptor coupled with Gq activate what
|
phosphlipase C - IP3 and DAG
|
|
|
receptors coupled with Gs activate what
|
adenylyl cyclase - cAMP - protein kinase A
|
|
|
receptors coupled with Gi do what
|
inhibit adenylyl cyclase, therefore cAMP and protein kinase A as well
|
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receptor found in heart that decreases HR and contracility
|
M2
|
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|
what should you watch for in all patients given cholinomimetic agents
|
COPD exacerbation
Asthma Peptic ulcers |
|
|
causes mydriasis and cycloplegia
|
atropine
|
|
|
muscarinic antagonist used for Parkinson's Dz, parkinsonism, and dystonias
|
benztropine
|
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AChE drugs used to treat and diagnose myasthenia gravis
|
diagnose - edrophonium
treat - pyridostigmine |
|
|
used to treat organophosphate poisoning - parathion
|
atropine + pralidoxime (regenerates active AChE)
|
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|
DUMBBELSS
|
associated with cholinesterase inhibitor poisoning - organophosphates:
D - diarrhea U - urination M - miosis B - bronchospasm B - bradycardia E - excitation of skeletal muscle and CNS L - lacrimation S - sweating S - salivation |
|
|
adverse effects of atropine
|
increased body temperature due to decreased sweating
cycloplegia constipation disorientation rapid pulse |
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used in experimental models to prevent vagal reflex response change in BP
|
hexamethonium - ganglionic nicotonic antagonist
|
|
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Effects B1 > B2, inotropic but not chronotropic - useful in heart failure
|
dobutamine
|
|
|
useful in shock (increases renal perfusion) and heart failure - both chronotropic and inotropic
|
dopamine
|
|
|
chronotropic = affects heart rate
inotropic = affects contracility |
**
|
|
|
affects a > B, usefully in hypotension, but renal perfusion decreases
|
norepinephrine
|
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partial B-agonists
|
pindolol
acebutolol |
|
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drug that blocks choline from entering cholinergic neuron
|
hemicholinium
|
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drug that blocks ACh forming vesicles in cholinergic neurons
|
vesamicol
|
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toxin that blocks release of ACh at presynaptic terminal
|
botulinum
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drug that blocks the conversion of tyrosine to DOPA
|
metyrosine
|
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drug that blocks NE forming vesicles in noradrenergic neurons
|
reserpine
|
|
|
drug that blocks the release of NE from presynaptic terminal
|
guanethidine
|
|
|
drugs that inhibit the reuptake of NE at presynpatic adrenergic terminal
|
cocaine
TCA |
|
|
direct cholinergic agonist used in postoperative and neurogenic ileus and urinary retention
|
bethanechol
|
|
|
what is bethanechol resistant to
|
resistant to AChE because direct agonist
|
|
|
direct cholinergic agonist used in glaucoma to relieve intraocular pressure
|
carbachol
pilocarpine |
|
|
challenge test for diagnosis of asthma
|
methacholine - stimulates muscarinic receptors in airway
|
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used for management of myasthenia gravis
|
pyridostigmine
|
|
|
used for atropine overdose
|
physostigmine
|
|
|
what should you watch out for with all cholinomimetic agents (direct or indirect)
|
exacerbation of COPD, asthma, and peptic ulcers
|
|
|
muscarinic antagonist used for motion sickness
|
scopolamine
|
|
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muscarinic antagonist used for genitourinary system, reduces urgency in mild cystitis and reduces bladder spasms
|
oxybutynin
|
|
|
muscarinic antagonists used for peptic ulcer treatment
|
pirenzepine
propantheline |
|
|
side effects associated with atropine poisoning
|
hot as a hare - increased temp due to decreased sweating
dry as a bone - decreased secretions red as a beet - flushed skin blind as a bat - cycloplegia and mydriasis mad as a hatter - disorientation |
|
|
nicotinic antagonist
|
hexamethonium
|
|
|
used in experimental models to prevent vagal reflex responses to changes in BP
|
hexamthonium
|
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|
application for NE use
|
hypotension
|
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application for Dopamine use
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shock or heart failure
|
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|
differentiate what NE and dopamine do to renal perfusion
|
NE - decreases renal perfusion
dopamine - increases renal perfusion |
|
|
B1 and B2 agonist
|
isoproterenol
|
|
|
selective B2 agonists
|
metaproterenol - acute asthma
albuterol - acute asthma salmeterol - long-term treatment of asthma terbutaline - premature uterine contractions ritodrine - premature uterine contractions |
|
|
indirect sympathomimetics
|
amphetamine
ephedrine cocaine |
|
|
drug used for hypertension in patients with renal disease
|
clonidine, a-methyldopa
*a2-agonists |
|
|
differentiate phenoxybenzamine and phentolamine
|
phenoxybenzamine - irreversible a-blocker
phentolamine - reversible *both are nonselective a-blockers |
|
|
drug used before removing pheochromocytoma since there will be high levels of released catecholamines
|
phenoxybenzamine - cannot not overcome irreversible blockade
*would be able to overcome phentolamine |
|
|
selective a1-blockers
|
prazosin
terazosin doxazosin |
|
|
nonselective a-blockers
|
phenoxybenzamine
phentolamine |
|
|
class of drugs associated with first-dose hypotension
|
selective a1-blockers
|
|
|
mirtazapine
|
selective a2-blockers
|
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|
what happens to BP when a-blocker is given before administration of epinephrine
|
usually increased BP
however if given a-blocker before than decreased BP due to B2 effect of epinephrine |
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two effects of B-blockers
|
decreased cardiac output
decreased renin release |
|
|
B-blockers of choice in patients with comorbid pulmonary disease
|
B1-blockers
|
|
|
nonseelctive a and B antagonists
|
carvedilol
labetalol |
|
|
treatment of acetaminophen toxicity
|
N-acetylcysteine
|
|
|
treatment of salicylate toxicity
|
NaHCO3 and dialysis
|
|
|
do you get rid of amphetamines quicker
|
NH4Cl to acidify the urine
|
|
|
treatment for organophosphate poisoning
|
atropine
pralidoxime |
|
|
treatment for B-blocker toxicity
|
glucagon
|
|
|
treatment for digitalis toxicity
|
normalize K
lidocaine magnesium |
|
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treatment for iron toxicity
|
deferoxamine
|
|
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treatment for lead toxicity
|
Ca EDTA, dimercaprol, succimer
|
|
|
treatment for mercury and arsenic toxicities
|
dimercaprol
|
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treatment for copper toxicity
|
penicillamine
|
|
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treatment for cyanide toxicity
|
nitrite
hydroxocabalamin thiosulfate |
|
|
treatment for methemoglobin
|
methyelen blue
vitamin C |
|
|
treatment for methanol and ethylene glycol poisoning
|
ethanol
fomepizole |
|
|
treatment for opioid toxicity
|
naloxone
|
|
|
treatment for benzo toxicity
|
flumazenil
|
|
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treatment for heparin toxicity
|
protamine
|
|
|
treatment for warfarin toxicity
|
vitamin K
fresh frozen plasma |
|
|
treatment for tPA or streptkinase toxicity
|
aminocaproic acid
|
|
|
treatment for theophylline toxicity
|
B-blocker
|
|
|
drugs associated with torsades de pointes
|
sotalol (class III)
quinidine (class IA) |
|
|
drugs associated with cutaneous flushing
|
vancomycin
adenosine niacin |
|
|
drugs associated with agranulocytosis
|
clozapine
carbamazepine colchicine propylthiouracil methimazole |
|
|
drug associated with direct coombs-positive hemolytic anemia
|
methyldopa
|
|
|
drug associated with aplastic anemia
|
chloramphenicol
|
|
|
drug associated with gray baby syndrome
|
chloramphenicol
|
|
|
drugs associated with megalobld with aplastic anemia
|
phenytoin
methotrexate sulfa drugs |
|
|
drugs associated with pulmonary fibrosis
|
bleomycin
amiodarone busulfan |
|
|
drugs associated with pseudomembranous colitis
|
clindamycin
ampicillin |
|
|
drugs associated with focal massive hepatic necrosis
|
halothane
valproic acid acetaminophen |
|
|
drugs associated with adrenocortical insufficncy
|
glucocorticoid withdrawal
|
|
|
drugs associated with hypothyroidism
|
lithium
amiodarone |
|
|
drugs that cause SLE-like syndrome
|
hydralazine
procainamide INH phenytoin |
|
|
drugs that cause tendonitis and tendon rupture
|
fluoroquinolones
|
|
|
drugs that cause interstitial nephritis
|
methicillin
NSAIDs furosemide |
|
|
drug that causes hemorrhagic cystitis
|
cyclophosphamide
|
|
|
drugs that cause diabetes insipidus
|
lithium
demenclocycline |
|
|
drugs that cause parkinson-like syndrome
|
haloperidol
chlorpromazine reserpine metoclopramide |
|
|
drugs that are associated with causing seizures
|
bupropion
imipenem INH |
|
|
drugs that are associated with nephrotoxicity and neurtoxicity
|
polymyxins - amphotericin B and nystatin
|
|
|
P450 inducers
|
quinidine
barbiturates St. john's wart phenytoin rifampin griseofulvin carbamazepine chronic alcohol use |
|
|
P450 inhibitors
|
HIV protease inhibitors
ketoconazole erythromycin grapefruit juice acute alcohol use sulfonamides INH cimetidine |
|
|
what is ethylene glycol broken down to by alcohol dehydrogenase
|
oxalic acid
|
|
|
what is methanol broken down to by alcohol dehydrogenase
|
formic acid
|
|
|
what does disulfiram block
|
acetaldehyde dehydrogenase
|
|
|
what does fomepizole block
|
alcohol dehydrogenase
|
|
|
drugs ending with -azine
|
antipsychotics
*chlorpromazine, fluphenazine |
|
|
drugs ending with -navir
|
protease inhibitors
|
|
|
differentiate what nitrates and B-blockers due to the MVO2 determinants: end diastolic pressure, BP, HR, contractility, and ejection time
|
nitrates: decrease EDV, BP, and ejection time; increase contracility and HR due to reflex response
B-blocker: decrease BP, contracility, HR; increase EDV and ejection time |
|
|
Ca channels blockers Nifedipine and Verapamil are similar to what respectively when looking at actions against MVO2 determinants
|
nifedipine - nitrates
verapamil - B-blockers |
|
|
inhibit cholesterol precursor, mevalonate
|
HMG-CoA reductase inhibitors
|
|
|
side effects of HMG-CoA reductase inhibitors
|
hepatotoxicity (increased LFTs)
rhabdomyolysis |
|
|
inhibits lipolysis in adipose tissue and hepatic VLDL secretion
|
niacin
|
|
|
what decreases the red, flushed face in patients taking niacin for lipid-lowering affects
|
aspirin
|
|
|
side effects associated with niacin
|
red, flushed face
hyperglycemia hyperuricemia |
|
|
prevents intestinal reabsorption of bile acids, liver must use cholesterol to make more
|
bile acid resins
|
|
|
side effects associated with bile acid resins
|
cholesterol gallstones
decreased absorption of fat soluble vitamins |
|
|
prevents cholesterol reabsorption at small intestine brush border
|
ezetimibe
|
|
|
upregulates lipoprotein lipase which increases TG clearance
|
fibrates
|
|
|
side effects associated with fibrates
|
myositis, hepatotoxicity, cholesterol gallstones
|
|
|
B1 receptors are Gs and activate PKA which phosphorylates L-type Ca channels and phospholamban, both of which increase intracellular Ca during contraction
|
**
|
|
|
which two drugs will block the effects of L-type Ca channels
|
Ca channel blockers
B-blockers |
|
|
ryanodine
|
poison that inactivates ryanodine receptors which release calcium from SR to sarcomere
|
|
|
direct inhibition of Na/K ATPase leads to indirect inhibition of Na/Ca exhanger - this leads to increased intracellular Ca and positive inotrophy
|
digoxin
|
|
|
cation that is an antidote for digoxin
|
Magnesium
|
|
|
Class IA antiarrhythmics
|
Quinidine
Procainamide Disopyramide |
|
|
Class IA antiarrhythmic associated with revesible SLE-like syndrome
|
procainamide
|
|
|
generally what do class I antiarrhythmics block
|
Na channel
|
|
|
Na channel blockers that increase AP duration, increase effective refractory period, and QT interval
|
Class IA antiarrhythmics
|
|
|
drugs used for atrial and ventricular arrhythmias, especially reentrant and ectopic supraventricular and ventricular tachycardia
|
Class IA
|
|
|
Na channel blockers that decrease AP duration, preferentially affect ischemic or depolarized prukinje and ventricular tissue
|
Class IB
|
|
|
Na channel blockers useful for acute ventricular arrhythmias (post-MI) and in digitalis-induced arrhythmias
|
Class IB
|
|
|
drugs in class IB antiarrhythmics
|
lidocain, tocainide, mexiletine
*phenytoin falls in as well |
|
|
Na channel blockers contraindicated in post-MI, associated with no affect on AP duration
|
Class IC
|
|
|
antiarrhythmic associated with pulmonary fibrosis, hepatotoxicity, and hyper/hypothyroidism
|
amiodarone
|
|
|
antiarrhythmic with Class I, II, III, and IV effects because it alters the lipid membrane
|
amiodarone
|
|
|
associated with increased toxicity for all class I antiarrhytmics
|
hyperkalemia
|
|
|
potassium channel blockers associated with increased AP duration, effective refractory period, and QT interval
|
Class III antiarrhythmics
|
|
|
two class of antiarrhytmics that increase PR interval
|
Class II (B-blockers)
Class IV (Ca channel blockers) |
|
|
what drug blocks the affects of adenosine
|
theophylline
|
|
|
this drug increases K out of cells leading to hyperpolarization and the DOC for abolishing supraventricular tachycardia
|
adenosine
|
|
|
cation effective in torsades de pointes and digoxin toxicity
|
Magnesium
|
|
|
antiarrhytmic class that suppresses abnormal pacemakers by decreasing the slope of phase 4; used in slowing ventricular rate
|
class III (B-blockers)
|
|
|
DOC for patients with DM and HTN
|
ACE inhibitors/ARBs
|
|
|
these drugs preferentially vasodilate arterioles > veins
|
hydralazine
nitrates |
|
|
first line therapy for hypertension in pregnancy
|
methyldopa
|
|
|
what HTN drug is contraindicated in angina/CAD due to compensatory tachycardia
|
hydralazine
|
|
|
Ca channel blocker with preferential predisposition toward vascular smooth muscle
|
nifedipine
|
|
|
Ca channel blocker with preferential predisposition toward the heart
|
verapamil
|
|
|
adverse effects of Ca channel blocker
|
AV block
cardiac depression peripheral edema flushing constipation |
|
|
differentiate how hydralazine and nitrates work
|
hydralazine direct increases cGMP
nitrates release NO in smooth muscle which causes increased cGMP |
|
|
Monday disease
|
loss of tolerance to nitrates over the weekend resulting in tachycardia, dizziness, and headache upon reexposure on Monday
|
|
|
mechanism of diazoxide
|
K channel opener leading to hyperpolarization and vascular smooth muscle relaxation
|
|
|
adverse effect of diazoxide
|
reduces insulin release due to blockade of K channel
|
|
|
dopamine D1 agonist
|
Fenoldopam
|
|
|
short acting direct release of NO used in the treatment of malignant hypertension
|
nitroprusside
|
|
|
vasodilator associated with causing CN toxicity
|
nitroprusside
|
|
|
effect of HMG-CoA reductase inhibitors on LDL, HDL, and TG
|
decreases LDL alot
decreases TG increases HDL |
|
|
effect of Niacin on LDL, HDL, and TG
|
decreases LDL
increases HDL the most decreases TG |
|
|
effect of bile acid resins on LDL, HDL, and TG
|
decreases LDL
increases HDL slightly increases TG slightly |
|
|
effect of ezetimibe (cholesterol absorption blocker on LDL, HDL, and TG
|
decreases LDL
no effect on HDL or TG |
|
|
effect of fibrates on LDL, HDL, and TG
|
decreases LDL
increases HDL decreases TG a lot |
|
|
lipid-lowering drug associated with hepatotoxicity and increased cholesterol gallstones
|
fibrates
|
|
|
this drug both increases contractility and decreases AV conduction
|
digoxin
|
|
|
patients presents with nausea, vomiting, diarrhea, blurry vision after taking heart medication. ECG shows increased PR, decreased QT, and hyperkalmia
|
digoxin
|
|
|
adverse effect associated with quinidine
|
conchonism (headache and tinnitus)
thrombocytopenia torsades de pointes due to increased QT interval |
|
|
this class of drugs decreases the slope of phase 4, especially AV node, and increases the PR interval
|
class II (B-blockers)
|
|
|
mechanism of action of class III antiarrhythmics
|
decrease K influx which increases AP duration and QT interval
|
|
|
drugs in class III antiarrhythmics
|
sotalol
ibutilide dofetilide amiodarone |
|
|
this drug has both class II and III properties
|
sotalol
|
|
|
mechanism of class IV antiarrhythmics
|
Ca channel blockers
|
|
|
list the rapid-acting, intermediate, and long-acting insulins
|
rapid: lispro, aspart
regular intermediate: NPH long: glargine, determir |
|
|
sulfonylureas
|
glyburide
glipizide |
|
|
this class of drugs closes K channels in B-cell membranes leading to depolarization and release of insulin
|
sulfonylureas
|
|
|
why are sulfonylureas useless in type 1 DM
|
requires some islet function
|
|
|
adverse effect associated with metformin
|
lactic acidosis
|
|
|
what patients is metformin contraindicated in
|
renal failure
|
|
|
this class of drugs binds to PPAR-y nuclear transcription regular
|
thiazolidinediones
|
|
|
adverse affects associated with thiazolidinediones
|
weight gain, edema
hepatotoxicity |
|
|
inhibits intestinal brush border enzymes leading to delayed reabsorption of glucose
|
a-glucosidase inhibitors
|
|
|
exenatide
|
GLP-1 analog that increases insulin release and decreases glucagon release
|
|
|
adverse effect associated with exenatide
|
pancreatitis
|
|
|
analog of amylin used to decrease glucagon excretion
|
pramlintide
|
|
|
this class of drugs inhibits organification of iodide and coupling of thryoid hormone synthesis
|
thioamides
*propylthiouracil, methimazole |
|
|
toxicities associated with thioamides
|
aplastic anemia
|
|
|
this drug mimics natural somatostatin pharmacologically
|
octreotide
|
|
|
drug used for central DI, not nephrogenic
|
desmopressin
|
|
|
ADH antagonist that is a member of the tetracycline family
|
demeclocycline
|
|
|
mechanism of action of cimetidine
|
reversible blocker of H2 receptor
|
|
|
adverse effects of cimetidine
|
P450 inhibitor
antiadrogenic effects (increases prolactin release) decreases renal excretion of creatinine |
|
|
which two H2 blockers decrease renal excretion of creatinine
|
cimetidine
ranitidine |
|
|
proton pump inhibitors
|
omeprazole
lansoprazole |
|
|
mechanism of proton pump inhibitors
|
irreversibly inhibit H/K ATPase in stomach parietal cells
|
|
|
two drugs that bind to ulcer base and provides physical protection and allow HCO3 to reestablish pH gradient in mucous layer
|
bismuth
sucralfate |
|
|
triple therapy for H. pylori ulcers
|
metrnidazole
amoxicillin (tetracycline) bismuth |
|
|
PGE1 analog that increases production and secretion of gastric mucous barrier and decreases acid production
|
misoprostol
|
|
|
in whom is misoprostol contraindicated in
|
women of childbearing potential (abortifactent)
|
|
|
muscarinic antagonists used to block M1 receptors on ECL cells and M3 receptors on parietal cells
|
pirenzepine
propantheline |
|
|
clinical uses for octreotide
|
acute variceal bleed
acromegaly VIPoma carcinoid tumors |
|
|
monoclonal antibody to TNF-a
|
infliximab
|
|
|
adverse effects of infliximab
|
reactivation of latent TB
|
|
|
DOC for inflammatory bowel disease
|
sulfasalazine
*combination of antibacterial and anti-inflammatory |
|
|
5-HT3 antagonist used an antiemetic
|
ondansetron
|
|
|
D2 receptor antagonist used to increase bowel motility
|
metoclopramide
|
|
|
cofactor for the activation of antithrombin leading to decreased thrombin and Xa
|
heparin
|
|
|
enoxaparin
|
low-MW heparin act more on Xa
|
|
|
heparin-induced thrombocytopenia
|
heparin binds to platelet factor IV causing antibody production that binds to and activates platelets resulting in thrombocytopenia
|
|
|
direct thrombin inhibitors, used as an alternative to heparin for HIT
|
lepirudin
bivalirudin |
|
|
how can warfarin cause skin/tissue necrosis
|
if patient is deficient in protein C and S, leads to paradoxical hypercoagulable state causing thrombus in skin
|
|
|
warfarin is teratogenic because it crosses the placenta
|
**
|
|
|
directly or indirectly aid conversion of plasminogen to plasmin
|
thrombolytics
|
|
|
PT, PTT, and BT in patients receiving thrombolytics
|
increased PT and PTT
no change in platelet count or BT |
|
|
treatment of thrombolytic toxicity
|
aminocaproic acid, inhibitor of fibrinolysis
|
|
|
PT, PTT, and BT seen in patient taking aspirin
|
increased BT
no change in PT or PTT |
|
|
this drug prevents conversion of arachidonic acid to thromboxane A2
|
NSAID
|
|
|
drugs that inhibit platelet aggregation by irreversibly blocking ADP receptors, this inhibits glycoprotein IIb/IIIa expression
|
clopidogrel
ticlopidine |
|
|
adverse effect of ticlopidine
|
neutropenia
|
|
|
monoclonal antibody that binds to glycoprotein receptor IIb/IIIa on activated platelets
|
abciximab
|
|
|
two anticancer drugs that work during M phase of cell cycle
|
vincrinstine
paclitaxel |
|
|
what part of the cell cycle do antimetabolites work
|
S phase
|
|
|
two drugs that decrease thymidine synthesis
|
methotrexate
5-fluorouracil |
|
|
these two drugs inhibit purine synthesis
|
6-mercaptopurine
6-thioguanine |
|
|
differentiate how alkylating agnets, dactinomycin/doxorubicin, and etoposide inhibit DNA
|
alkylating agents - cross-link DNA
dactinomycin/doxorubicin - intercalate DNA etoposide - inhibit topoisomerase II |
|
|
differentiate how vincristine and paclitaxel function
|
vincristine - inhibit microtubule formation
paclitaxel - inhibit microtubule disassembly |
|
|
folic acid analog that inhibits DHF
|
methotrexate
|
|
|
what can reverse meylosuppression during methotrexate therapy
|
folinic acid (leucovorin)
|
|
|
pyrimidine analog that covalently complexes folic acid inhibiting thymidylate synthase
|
5-FU
|
|
|
how do you overcome myelosuppression during 5-FU therapy
|
thymidine
|
|
|
this drug is metabolized by xanthine oxidase
|
6-mercaptopurine
|
|
|
pyrimidine antagonist leading to inhibition of DNA polymerase
|
cytarabine
|
|
|
antimetabolites
|
methotrexate
5-FU 6-MP 6-TG cytarabine |
|
|
what enzyme activates both 6-MP and 6-TG
|
HGPRTase
|
|
|
antitumor antibiotics
|
dactinomycin
doxorubicin bleomycin etoposide |
|
|
mechanism of action of bleomycin
|
induces free radical formation causing DNA strand breaks
|
|
|
covalently cross-links DNA at guanine N-7 positions
|
cyclophosphamide
|
|
|
drug that cross-links DNA, associated with nephrotoxicity and acoustic nerve damage
|
cisplatin
|
|
|
this drug inhibits ribonucleotide reductase leading to decreased DNA synthesis
|
hydroxyurea
*increases HbF production in sickle cell disease |
|
|
estrogen receptor antagonists in breast and agonists in bone; used in breast cancer and can prevent osteoporosis
|
tamoifen
raloxifene |
|
|
differentiate what tamoxifen and raloxifene does to endometrial tissue
|
tamoxifin - causes hyperplasia and increases risk for endometrial carcinoma
raloxifene - endometrial antagonist |
|
|
monoclonal antibody against HER-2
|
trastuzumab
|
|
|
tyrosine kinase inhibitor used in bcr-abl translocation
|
imatinib
|
|
|
monoclonal antibody against CD20
|
rituximab
|
|
|
action of leukotrienes
|
bronchiconstriction
vasoconstriction increased vascular permeability |
|
|
function of PGI2
|
inhibits platelet aggregation
promotes vasodilation |
|
|
inhibit phospholipase A2 and formation of COX-2
|
corticosteroids
|
|
|
inhibits lipoxygenase (formation of leukotrienes)
|
zileuton
|
|
|
leukotriene receptor antagonists
|
zafirlukast
montelukast |
|
|
used to close PDA
|
indomethacin
|
|
|
adverse effects seen in selective COX-2 inhibitors
|
increased risk of thrombosis
|
|
|
celecoxib
|
selective COX-2 inhibitor
|
|
|
in what patients should selective COX-2 inhibitors be used
|
those with inflammation and comorbid gastritis or ulcers
|
|
|
reversibly inhibits COX, most in CNS; inactivated peripherally
|
acetaminophen
|
|
|
this drug metabolite depletes glutathione and forms toxic tissue adducts in liver
|
acetaminophen
|
|
|
this drug class inhibits osteoclastic activity
|
bisphosphonates
*-onates: etidronate, pamidronate, alendronate |
|
|
this drugs inhibits tubulin polymerization imparing leukocyte chemotaxis and degranulation
|
colchicine
|
|
|
inhibits reabsorption of uric acid in PCT; also inhibits secretion of penicillin
|
probenecid
|
|
|
inhibits xanthine oxidase; leads to increased concentration of 6-MP
|
allopurinol
|
|
|
purines --> hypoxanthine --> xanthine --> uric acid
|
**
|
|
|
TNF-a inhibitors
|
etanercept - recombinant form of human TNF receptor that binds TNF
influximab - antibody adalimumab - antibody |
|
|
mechanism of a-agonists in glaucoma
|
decrease aqueous humor synthesis due to vasoconstriction
|
|
|
mechanism of B-blockers in glaucoma
|
decrease aqueous humor secretion in ciliary body
|
|
|
mechanis of acetazolamide in glaucoma
|
decreaes aqueous humor secretion due to decreased HCO3
|
|
|
mechanism of cholinomimetics in glaucoma
|
increase outflow of aqueous humor by contract ciliary muscle and open trabecular meshwork
|
|
|
mechanism of prostaglandin in glaucoma
|
increase outflow of aqueous humor
|
|
|
adverse effect in prostaglandin use in glaucoma
|
darkens color or iris
|
|
|
a2-agonist used in treatment of gluacoma
|
brimonidine
|
|
|
opioid used for cough suppression
|
dextrmethorphan
|
|
|
very weak opioid agonist that also inhibits serotonin and NE reuptake
|
tramadol
|
|
|
two drugs given to patients in status epilepticus
|
phenytoin
benzodiazpine |
|
|
two drugs that increase Na channel inactivation
|
phenytoin
carbamazpine |
|
|
drug that blocks voltage-gated Na channels
|
lamotrigine
|
|
|
drug that blocks Na channels and increases GABA action
|
topiramate
|
|
|
drug that increases Na channel inactivation and increases GABA concentration
|
valproic acid
|
|
|
drug that blocks thalamic T-type Ca channels
|
ethosuximide
|
|
|
3 1st line drugs for tonic-clonic seizures
|
phenytoin
carbamazepine valproic acid *all increase Na channel inactivation |
|
|
1st line anticonvulsant in pregnancy
|
phenobarbital
|
|
|
what is gabapentin (anticonvulsant) used for
|
peripheral neuropathy
bipolar disorder |
|
|
adverse effects associated with carbamazepine
|
agranulocytosis
P450 induction |
|
|
adverse effect associated with phenobarbital
|
P450 induction
|
|
|
adverse effects associated with phenytoin
|
gingival hyperplasia
induction of P450 |
|
|
adverse effects associated with valproic acid
|
hepatotoxicity
contraindicated in pregnancy |
|
|
differentiate what barbiturates and benzodiazepines do to Cl channels
|
barbiturates - increase duration of Cl channel opening
benzos - increase frequency of Cl channel opening |
|
|
this class of drugs decreases REM sleep
|
benzodiazepines
|
|
|
nonbenzodiazpine hypnotics
|
zolpidem
|
|
|
what does flumazenil reverse
|
nonbenzodiazepine hypnotic action via the BZ1 receptor subtype
|
|
|
potency and MAC are inversely related
|
**
|
|
|
what do anesthetic drugs with low blood solubility indicate
|
rapid induction and recovery times
|
|
|
what do highly lipid soluble anesthetics indicate
|
increased potency (decreased MAC because less is needed to saturate the blood)
|
|
|
what characteristics of anesthetics would be the most potent with rapid induction and recovery
|
low blood solubility (rapid induction and recovery)
high lipid solubility (high potency) |
|
|
adverse effects of inhaled anesthetics
|
myocardial depression
increased cerebral blood flow respiratory depression hepatotoxicity (halothane) malignant hyperthermia (halothane) |
|
|
IV anesthetic with high potency, rapid entry and recovery, with decreased cerebral blood flow
|
barbiturates (thiopental)
|
|
|
competitive antagonist GABA benzodizepine receptor
|
flumazenil
|
|
|
NMDA receptor blocker with increased cerebral blood flow
|
ketamine
|
|
|
used for rapid anesthesia induction and short procedures, less postoperative nausea
|
propofol
|
|
|
mechanism for local anesthetics
|
binds preferentially to activated Na channel, binds to inner portion of channel
|
|
|
order of nerve blockade in local anesthetics
|
small myelinated > small unmyelinated > large myelinated > large unmyelinated
|
|
|
local anesthetic associated with severe cardiovascular toxicity
|
bupivacaine
|
|
|
depolarizing NMJ blocking drug
-selective for motor nicotinic receptor |
succinylcholine
|
|
|
mechanism of nondepolarizing NMJ blocking drugs
|
competitive inhibitor that competes with ACh for receptors
|
|
|
used in the treatment of malignant hyperthermia, caused by inhalation anesthetics and succinylcholine
|
dantrolene
|
|
|
mechanism of dantrolene in treatment of malignant hyperthermia or neuroleptic malignant syndrome
|
prevents the release of Ca from SR of skeletal muscle
|
|
|
parkinson is due to loss of dopaminergic neurons and excess cholinergic activity
|
**
|
|
|
dopamine agonists used in parkinson's disease
|
bromocriptine
pramipexole ropinirole |
|
|
this antiviral drug increases dopamine release
|
amantadine
|
|
|
MAO and COMT inhibitors that prevent L-DOPA degradation
|
MAO inhibitor - selegiline
COMT inhibitors - entacapone, tolcapone |
|
|
antimuscarinic that improves tremor and ridigity in Parkinsonism
|
benztropine
|
|
|
DOC for essential/familial tremors
|
B-blocker
|
|
|
carbidopa
|
increases the CNS availability of L-DOPA by inhibiting peripheral degradation; also inhibits peripheral side effects
|
|
|
NMDA receptor antagonist used in Alzheimer's
|
memantine
|
|
|
AChE inhibitor used in Alzheimers
|
donepezil
|
|
|
what are dopamine and GABA levels in Huntington's disease
|
increased dopamine
decreased GABA |
|
|
5-HT agonist that causes vasoconstriction used in migraine and cluster headache attacks
|
sumatriptan
|
|
|
mood stabilizers
|
lithium
valproic acid carbamazepine |
|
|
DOC for patient with depression and insomnia
|
mertazapine (a2-blocker)
|
|
|
mechanism for typical antipsychotics
|
blocks dopamine D2 receptors
|
|
|
differentiate which typical antipsychotics are associated with corneal deposits vs. retinal deposits
|
corneal - chlorpormazine
retinal - thioridazine |
|
|
high potency antipsychotics
*associated with extrapyramidal symptoms |
haloperidol
trifluoperiazine fluphenzine |
|
|
low potency antipsychotics
*associated with antocholinergic, anthistamine, a blockade effects |
chlorpromazine
thioridazine |
|
|
neuroleptic malignant syndrome
|
rigidity, myoglobinuria, hyperpyrexia (fever) - adverse effect of antipsychotics
|
|
|
associated with long-term antipsychotic use
|
tardive dyskinesia
|
|
|
atypical antipsychotics
|
olanzapine
clozapine quetiapine resperidone aripiprazole ziprazsidone |
|
|
these drugs block both positive and negative symptoms of schizophrenia
|
atypical antipsychotics
*typical only help with positive symptoms |
|
|
atypical antipsychotic used for OCD
|
olanzapine
|
|
|
atypical antipsychotic associated with agrnulocytosis (requires weekly WBC monitoring)
|
clozapine
|
|
|
lithium side effects
|
tremor
nephrogenic DI hypothyroidism teratogenic (Ebstein anomaly) |
|
|
5-HT receptor agonist used for GAD
|
buspirone
|
|
|
DOC for fibromyalgia
|
TCA
|
|
|
treatment for TCA cardiovascular toxicity
|
NaHCO3
|
|
|
adverse effects of TCAs
|
arryhthmias
|
|
|
treatment of serotonin syndrome
|
cyproheptadine (5-HT2 antagonist)
|
|
|
adverse effects in SSRIs
|
sexual dysfunction
serotonin syndrome if combined with MAO inhibitor |
|
|
which opioid should be avoided with SSRIs or MAOIs
|
meperidine
|
|
|
MAOIs
|
phenelzine
selegiline |
|
|
a2-antagonist as well as 5-HT agonist
|
mirtazapine
|
|
|
serotonin reuptake inhibitor used for insomnia
|
trazadone
|
|
|
where in the nephron do osmotic diuretics work
|
descending limb
|
|
|
adverse effects associated with mannitol
|
pulmonary edema
contraindicated in CHF |
|
|
clinical uses for mannitol
|
shock
increased ICP |
|
|
differentiate furosemide and ethacrynic acid
|
furosemide is a sulfonamide loop diruretic
ethacrynic acid is loop diuretic used in patients with sulfa allergy |
|
|
adverse effects associated with furosemide
|
ototoxicity, hypokalemia, intersitial nephritis
|
|
|
adverse effects associated with hydrochlorothiazide
|
hyperglycemia
hyperlipidemia hyperuricemia hypercalcemia |
|
|
K+ sparing diuretics
differentiate mechanism |
spironolactone - aldosterone receptor antagonist
eplerenone - same triamterene - Na channel blocker in CCT amiloride - same |
|
|
differentiate Urinary Ca in loop vs. thiazide diuretics
|
loop - increased urinary Ca
thiazide - decreased urinary Ca |
|
|
inhibits aromatase
|
anastrozole
|
|
|
what do flutamide and spironolactone inhibit
|
androgen receptor complex
|
|
|
GnRH analog with agonist properties
|
leuprolide
|
|
|
treatment of prostate cancer
|
continuous leuprolide
flutamide |
|
|
useful in both BPH and male-pattern baldness
|
finasteride
|
|
|
two drugs used in the treatment of polycystic ovarian syndrome to prevent hirsutism
|
ketoconazole
spironolactone |
|
|
this drug inhibits steroid synthesis via P450 inhibition
|
ketoconazole
|
|
|
estrogen partial agonists
|
tamoxifen
raloxifene |
|
|
competitive inhibitor of progestins, used for termination of pregnancy
|
mifepristone
|
|
|
B2-agonists that relax the uterus
|
ritodrine
terbutaline |
|
|
cGMP PDE inhibitors causing increased cGMP
|
sildenafil
verdenafil |
|
|
1st generation H1 blockers
|
diphenhydramine
dimenhydrinate chlorpheniramine |
|
|
2nd generation H1 blockers
|
loratadine
fexofenadine |
|
|
causes bronchodilation by inhibiting PDE; associated with carditoxicity and neurotoxicity
|
theophylline
|
|
|
prevents release of mediators from mast cells, effecitve only for prophylaxis of asthma
|
cromolyn
|
|
|
treatment of asthma by inactivating NF-kB used to prevent late response inflammation
|
corticosteroids
|
|
|
5-lipoxygenase inhibitor
|
zileuton
|
|
|
salmeterol
|
long-acting B2 blocker used for prophylaxis
|
|
|
two processes need to treat in asthma
|
1. bronchoconstriction (B2 agonist, theophylline, muscarinic antagonist)
2. inflammatory process (corticosteroids) |
|
|
can loosen mucous plugs in CF patients
|
N-acetylcysteine
|
|
|
used to treat pulmonary HTN, competitively antagonizes endothelin-1 receptors
|
Bosentan
|
|
|
removes excesss sputum, but does not suppress cough reflex
|
guaifenesin
|
