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213 Cards in this Set

  • Front
  • Back
seligilene
selective MAO-B inhibitor;
antidepressant agent
phenylzine
irreversible MAO-A and B inhibitor;
antidepressant agent
tranylcypromine
prolonged inhibitor of MAO-A but not irreversible;
antidepressant agent
amitriptyline
TCA
imipramine
TCA
trazodone
2nd/3rd gen antidepressant;
directly inhibit 5-HT2 receptors;
inhibit 5-HT > NE reuptake
nefazodone
2nd/3rd gen antidepressant;
directly inhibit 5-HT2 receptors;
inhibit 5-HT > NE reuptake
venlafaxine
2nd/3rd gen antidepressant;
5-HT >> NE reuptake inhibitor
buproprion
2nd/3rd gen antidepressant
mechanism unknown
weak inhibition of monoamine reuptake
amoxapine
2nd/3rd gen antidepressant
metabolite of antipsychotic (loxapine)
maprotiline
2nd/3rd gen antidepressant
potent NE reuptake inhibitor
mirtazipine
2nd/3rd gen antidepressant
block 5-HT and α2 receptors
fluoxetine
antidepressant
SSRI
chlorpromazine
less potent phenothiazine
block DA receptors in limbic system
antipsychotic
thioridazine
potent phenothiazine
block DA receptors in limbic system
antipsychotic
fluphenazine
more potent phenothiazine
block DA receptors in limbic system
antipsychotic
haloperidol
antipsychotic
resembles high potency phenothiazine
block D2 receptors
molindone
antipsychotic
resembles high potency phenothiazine
block D2 receptors
thiothixene
antipsychotic
resembles low potency phenothiazine
block D2 receptors
clozapine
atypical antipsychotic
weak D1, D2 blocker
may cause agranulocytosis
olanzipine
atypical antipsychotic
block D2, 5-HT2, ACh receptors
also used in mania
respiridone
atypical antipsychotic
potent blocker of D2, 5-HT2 receptors
contraindicated in ASCVD
1st line drug
quetiapine
atypical antipsychotic
block 5-HT2, D2 receptors
marked somnolence
ziprasidone
atypical antipsychotic
fatal cardiac arrythmias
aripiprazole
atypical antipsychotic
complex mechanism
NMDA superagonists
antipsychotic under development
d-cycloserine
antipsychotic
glycine partial agonist
glycine transporter inhibitor
antipsychotic under development
pentobarbital
short-intermediate acting (3-6 hr) barbiturate
potentiate action of GABA
directly stimulate GABA-A receptor
sedative-hypnotic
secobarbital
short-intermediate acting (3-6 hr) barbiturate
potentiate action of GABA
directly stimulate GABA-A receptor
sedative-hypnotic
amobarbital
short-intermediate acting (3-6 hr) barbiturate
potentiate action of GABA
directly stimulate GABA-A receptor
sedative-hypnotic
chloral hydrate
nonbarbiturate sedative-hypnotic
sedation in children
paraldehyde
nonbarbiturate sedative-hypnotic
ethchlorvinol
nonbarbiturate sedative-hypnotic
meprobamate
nonbarbiturate sedative-hypnotic
gastric bezoars
triazolam
short acting (<6 hr) benzodiazepine
enhance GABA mediated Cl flux
sedative-hypnotic
temazepam
intermediate acting (6<t1/2<24 hr) benzodiazepine
enhance GABA mediated Cl flux
sedative-hypnotic
diazepam
long acting (>24 hr) benzodiazepine
enhance GABA mediated Cl flux
sedative-hypnotic
flurazepam
long acting (>24 hr) benzodiazepine
enhance GABA mediated Cl flux
sedative-hypnotic
chlordiazepoxide
long acting (>24 hr) benzodiazepine
enhance GABA mediated Cl flux
sedative-hypnotic
rohypnol
sedative-hypnotic
date rape drug
zaleplon
novel benzodiazepine-receptor agonist
hypnotic agent
zolpidem
novel benzodiazepine-receptor agonist
hypnotic agent
eszopiclone
novel benzodiazepine-receptor agonist
hypnotic agent
flumazenil
benzodiazepine-receptor antagonist
reverse sedative effects
phenytoin
antiseizure
inhibit voltage gated Na channels
DO NOT use for absence seizures
fetal hydantoin syndrome
carbamazepine
antiseizure
inhibit voltage gated Na channels
potentiate GABA-A receptors
drug of choice for partial seizures
aplastic anemia
valproate
antiseizure
inhibit voltage gated Na channels
increase presynaptic GABA
inhibit voltage gated Ca channels
particularly helpful with myoclonic
hepatotoxicity
topiramate
antiseizure
inhibit voltage gated Na channels
potentiate GABA receptor
changes in visual acuity
lamotrigine
antiseizure
inhibit voltage gated Na channels
inhibit voltage gated Ca channels
stevens johnson/toxic epidermal necrolysis in <16 yo
zonisamide
antiseizure
inhibit voltage gated Na channels
inhibit voltage gated Ca channels
depression and psychosis reported
primidone
antiseizure
metabolized to phenobarbital
tiagabine
antiseizure
inhibit GABA reuptake
psychosis reported
gabapentin
antiseizure
enhance presynaptic GABA concentration
ethosuximide
antiseizure
inhibit voltage gated Ca channels
first line for absence seizures
levetiracetam
antiseizure
unknown mechanism
felbamate
antiseizure
unknown mechanism
aplastic anemia and hepatotoxicity
phenobarbital
long-acting (>6 hr) barbiturate
potentiate action of GABA
directly stimulate GABA-A receptor
sedative-hypnotic
antiseizure
buspirone
5-HT1 agonist
anxiolytic, smoking cessation
sumatryptan
triptan
5-HT1 agonist
antimigraine
ergotamine
ergot alkaloid
promiscious agonist: 5-HT, adrenergic, etc
formerly used as antimigraine
cardiac valvular lesions
retroperitoneal fibroplasias
lysergic acid diethylamide
5-HT agonist
recreational hallucinogen
ketanserin
5-HT1, 5-HT2 antagonist
also α1 and H1 antagonist
antihypertensive
ondansetron
5-HT3 antagonist
antiemetic for chemotherapy
cyproheptadine
5-HT2 antagonist
H2 receptor antagonist
control post-gastrectomy dumping syndrome
ritanserin
5-HT2 antagonist
antithrombotic
sevoflurane
volatile anesthetic
desflurane
volatile anesthetic
isoflurane
volatile anesthetic
nitrous oxide
volatile anesthetic
halothane
volatile anesthetic
etomidate
IV anesthetic
used for trauma or CHF
fentanyl
IV anesthetic
opioid
propofol
IV anesthetic
used for normal anesthesia
thiopental
ultra-short acting (15-30 min) barbiturate
potentiate action of GABA
directly stimulate GABA-A receptor
sedative-hypnotic
IV anesthetic
midazolam
short acting (<6 hr) benzodiazepine
enhance GABA mediated Cl flux
sedative-hypnotic
IV anesthetic
used for normal anesthesia
ketamine
NMDA receptor
IV anesthetic
used for trauma or CHF
aspirin
analgesic, antipyretic, antiinflammatory
irreversible acetylation of COX
contraindicated in ulcer, asthma, gout, influenza
diflunisal
analgesic, antipyretic, antiinflammatory
mesalamine
analgesic, antipyretic, antiinflammatory
use in IBD
acetaminophen
analgesic, antipyretic, weak antiinflammatory
indomethacin
analgesic, antipyretic, antiinflammatory
treatment of acute gouty arthritis
sulindac
analgesic, antipyretic, antiinflammatory
prodrug
treatment of acute gouty arthritis
tolmetin
analgesic, antipyretic, antiinflammatory
diclofenac
analgesic, antipyretic, antiinflammatory
inhibit lipoxygenase and COX
ketorolac
analgesic, antipyretic, antiinflammatory
short term management of moderately severe acute pain (at opioid level)
ibuprofen
analgesic, antipyretic, antiinflammatory
naproxen
analgesic, antipyretic, antiinflammatory
treatment of acute gouty arthritis
ketoprofen
analgesic, antipyretic, antiinflammatory
inhibits lipoxygenase and COXs
oxaprozin
analgesic, antipyretic, antiinflammatory
long half life
piroxicam
analgesic, antipyretic, antiinflammatory
extended half life
reversible inhibitor of COXs
meloxicam
analgesic, antipyretic, antiinflammatory
inhibit COX2 > COX1
nabumetone
analgesic, antipyretic, antiinflammatory
only nonacid NSAID
ketone prodrug
preferentially inhibits COX2 at low dose
celecoxib
analgesic, antipyretic, antiinflammatory
COX2 selective inhibitor
abatacept
disease modifying antirheumatic drug
inhibits T cell activation
IV injection
rituximab
disease modifying antirheumatic drug
Ab that bind to CD20 B cells
IV infusion
fatal infusion reactions
etanercept
disease modifying antirheumatic drug
TNFα blocking agent
SC administration
adalimumab
disease modifying antirheumatic drug
TNFα blocking agent
SC administration
infliximab
disease modifying antirheumatic drug
TNFα blocking agent
IV infusion
colchicine
treatment for acute gouty arthritis
inhibit migration of leukocytes and phagocytes
inhibit formation of leukotrine B4
probenecid
uricosuric agent
increase uric acid reabsorption
treatment for underexcretor
sulfinpyrazone
uricosuric agent
increase uric acid reabsorption
treatment for underexcretor
allopurinol
inhibit xanthine oxidase
inhibit PPRP synthetase
treatment for overproducers
febuxostat
inhibit xanthine oxidase
nonpurine compound
treatment for overproducers
recombinant uricase
converts uric acid to allantoin
prevents hyperuricemia
morphine
prototype opioid narcotic
codeine
opioid
1/10 morphine potency
orally active
used as antitussant or analgesic with aspirin or acetaminophen
heroin
opioid
high lipid solubility
oxycodone
opioid
same effects/potency as morphine
higher oral activity
hydromorphone
opioid
same effects as morphine
10x morphine potency
higher oral activity
apomorphine
opioid
DA agonist activity
used to induce vomiting (direct effect on CTZ)
misoprostol
synthetic PGE1 analog
given with NSAIDs to protect GI mucosa
mucomyst (N-acetylcysteine)
acetaminophen overdose antidote
body able to make more glutathione and safely metabolize acetaminophen
dextromethorphan
opioid
little analgesic or addiction activity
used as antitussant
meperidine
opioid
shorter duration of action than morphine
1/10 morphine potency
orally active
fentanyl
opioid
80x morphine potency
anesthetic induction
sole anesthetic for cardiac surgeries
alfentanil
opioid
80x morphine potency
sufentanil
opioid
80x morphine potency
methadone
opioid
same actions and potency as morphine
orally active
half life = 15 hr
used in methadone maintenance
LAAM
opioid
long-acting congener of methadone
orally active
maintenance treatment in heroin addiction
propoxyphene
opioid
similar to codeine
diphenoxylate
opioid
oral administration
antidiarrheal
loperamide
opioid
oral administration
antidiarrheal
naloxone
pure competitive opioid antagonist
drug of choice for opioid overdose
naltrexone
pure competitive opioid antagonist
orally active
pentazocine
opioid
weak mu antagonist
kappa agonist
sigma agonist
analgesic for mild to moderate pain
nalbuphine
opioid
mu antagonist
kappa agonist
analgesic for moderate to severe pain
butorphanol
opioid
mu antagonist
kappa agonist
analgesic for moderate to severe pain
buprenorphine
partial mu agonist
kappa antagonist
analgesic for moderate to severe pain
phencyclidine
arylcyclohexylamine
abused drug
sigma agonist
disulfiram
inhibits aldehyde dehydrogenase
n/v with ethanol ingestion
mannitol
osmotic diuretic
useful in increased ICP
acetazolamide
CA inhibitor
decreased NaHCO3 reabsorption
treatment of glaucoma
furosemide
loop diuretic
block Na-K-2Cl symporter
decrease preload
increase urinary Ca excretion
bumetanide
loop diuretic
block Na-K-2Cl symporter
decrease preload
increase urinary Ca excretion
ethacrynic acid
loop diuretic
block Na-K-2Cl symporter
decrease preload
increase urinary Ca excretion
more commonly causes ototoxicity
torsemide
loop diuretic
block Na-K-2Cl symporter
decrease preload
increase urinary Ca excretion
hydrochlorothiazide
thiazide diuretic
block NaCl symporter
decrease PVR
increase Ca reabsorption
chlorthalidone
thiazide diuretic
block NaCl symporter
decrease PVR
increase Ca reabsorption
metolazone
thiazide diuretic
block NaCl symporter
decrease PVR
increase Ca reabsorption
chlorthiazide
thiazide diuretic
block NaCl symporter
decrease PVR
increase Ca reabsorption
available in IV preparation
triamterene
K sparing diuretic: Na channel blocker
decrease Na reabsorption
decrease K, H excretion
amiloride
K sparing diuretic: Na channel blocker
decrease Na reabsorption
decrease K, H excretion
spironolactone
K sparing diuretic
competitive antagonist of aldosterone
gynecomastia as side effect
eplerenone
K sparing diuretic
selective aldosterone receptor blocker
vasopressin = AVP = ADH
insertion of aquaporins in collecting duct (V2)
vasoconstriction (V1)
desmopressin = DDAVP
mainly insertion of aquaporins in collecting duct (V2)
vasoconstriction (V1) to lesser extent
demeclocycline
ADH antagonist
decrease effect of ADH on renal collecting duct cells
conivaptan
ADH antagonist
V1, V2 antagonist
short term treatment of euvolemic hyponatremia
NOT approved for heart failure
lithium
antidepressant
mood stabilizing
decrease formation of postsynaptic second messengers (IP3 and DAG)
ADH antagonist
clonidine
sympatholytic
α2 agonist
decreased SNS outflow
hypertensive crisis if sudden withdrawal
methyldopa
sympatholytic
prodrug α2 agonist
reserpine
decrease neurotransmitter released
inhibit vesicular uptake pump
guanethidine
decrease neurotransmitter released
depletion of neurotransmitter
prazosin
α1 blocker
antihypertensive
first-dose phenomenon
labetalol
α1, β blocker
antihypertensive
possible hepatotoxicity
carvedilol
α1, β blocker
antihypertensive
used for HF in certain patients
hydralazine
antihypertensive
arterial dilator via NO release
possible drug induced lupus
minoxidil
antihypertensive
arterial dilator via K channel opening activity
possible pericardial effusion
fenoldopam
antihypertensive
arterial dilator via D1 receptor agonist activity
used for hypertensive emergencies
possible increased intraocular pressure
diazoxide
antihypertensive
arterial dilator via K channel opening activity
used for hypertensive emergencies
sodium nitroprusside
antihypertensive
arterial and venous dilator via guanylyl cyclase stimulation
cyanide and thiocyanate toxicity
-pril drugs
ACE inhibitor
antihypertensive prodrugs
decreased AII leading to less vasoconstriction and aldosterone
decreased bradykinin (vasodilator) breakdown
contraindicated in renal artery stenosis
cough, angioedema
losartan
AII receptor blocker
antihypertensive
decreased pressor response
aliskiren
renin inhibitor
antihypertensive
decreased plasma renin activity
nitroglycerin
organic nitrate
antianginal
release NO to stimulate vasodilation
isosorbide dinitrate (ISDN)
organic nitrate
antianginal
release NO to stimulate vasodilation
isosorbide-5-mononitrate (ISMN)
organic nitrate
antianginal
release NO to stimulate vasodilation
propranolol
β blocker
antihypertensive, antianginal
decreased HR, contractility
decreased renal renin release
β blocker withdrawal
nifedipine
dihydropyridine Ca channel blocker
antianginal, antihypertensive
higher vascular selectivity
mainly arterial vasodilation
decreased contractility
ranolazine
antianginal
newer drug approved for chronic angina
digoxin
cardiac glycoside
inhibits Na,K-ATPase
leads to increased intracellular Ca --> increased contractility
used for heart failure
dobutamine
β1 agonist
used for heart failure
milrinone
inhibit phosphodiesterase 3 --> increased cAMP --> increased contractility and vasodilation
used for acute HF or severe exacerbation of chronic HF
nesiritide
hBNP
stimulate guanylate cyclase --> increased cGMP --> smooth muscle relaxation
used for heart failure
propranolol
antiarrhythmic - class II
block β receptor
atrial fibrillation
amiodarone
antiarrhythmic - class III
block Na, K, Ca channels
block α, β, ACh receptors
t1/2 = weeks
serious ventricular arrhythmias
certain supraventricular arrhythmias
many adverse effects
dronedarone
antiarrhythmic - class III
atrial fibrillation or flutter in certain patients
sotalol
antiarrhythmic - class III
block K channel
block β receptor
serious ventricular arrhythmias
maintenance of sinus rhythm in patients with symptomatic AFIB/AFL who are currently in sinus rhythm
dofetilide
antiarrhythmic - class III
block K channel
conversion of atrial fibrillation
maintenance of normal sinus rhythm is patients with atrial fibrillation
ibutilide
antiarrhythmic - class III
block K channel
increase Na channel flow
rapid conversion of atrial fibrillation or atrial flutter of recent onset to sinus rhythm
adenosine
antiarrhythmic - class IV
acts on adenosine receptor
t1/2 <10 sec
conversion of paroxysmal supraventricular tachycardia to sinus rhythm
methylxanthine
inhibit adenosine receptor
example is caffeine
UFH
derived from porcine gastric mucosa;
catalyzes antithrombin inhibition of IIa and Xa
LMWH
digested UFH
catalyzes antithrombin inhibition of Xa and to lesser extent IIa
fondaparinux
synthetic pentasaccharide binding sequence;
catalyzes antithrombin inhibition of Xa
enoxaparin
LMWH
lepirudin
irreversible direct thrombin inhibitor
recombinant derivative of hirudin (anticoagulant in leeches)
argatroban
reversible direct thrombin inhibitor
protamine
combines with UFH to form a stable salt;
neutralize anti-IIa activity of LMWH but only partially reverses the anti-Xa activity;
does not reverse fondaparinux
warfarin
inhibit regeneration of reduced vit K;
inhibit modification of factor II, VII, IX, X, protein C and S;
S-isomer is more potent than R-isomer
streptokinase
fibrinolytic
binds to plasminogen thereby converting plasminogen into a plasmin-like molecule capable of converting plasminogen to plasmin
alteplase
fibrinolytic
tPA produced by recombinant DNA technology;
requires fibrin for activity
reteplase
fibrinolytic;
nonglycosylated deletion mutant of wild type tPA;
fibrin specific;
resistance to Plasminogen Activator Inhibitor-1
tenecteplase
fibrinolytic;
6 aa substitued at 3 sites compared to wild type tPA;
fibrin specific
resistance to Plasminogen Activator Inhibitor-1;
single bolus administration
aminocaproic acid
hemostatic;
bind reversible to plasminogen to block binding to fibrin and its activation and transformation to plasmin;
enhancing hemostasis
clopidogrel
antiplatelet agent
irreversible ADP pathway inhibitor
prodrug requires 2 CYP-dependent oxidations
prasugrel
antiplatelet agent
irreversible ADP pathway inhibitor
prodrug requires hydrolysis and 1 CYP-dependent oxidation
abciximab
antiplatelet agent
GIIb/IIIa antagonist
Fab frag of monoclonal Ab
eptifibatide
antiplatelet agent
GIIb/IIIa antagonist
tirofiban
antiplatelet agent
GIIb/IIIa antagonist
phytonadione
oral vit K
antagonizes warfarin
bivalirudin
direct reversible thrombin inhibitor
derived from hirudin
inactivates platelet bound Xa and clot bound thrombin
dipyridamole
inhibition of phophodiesterase to increase platelet cAMP;
blockade of uptake of adenosine;
with aspirin for stroke prevention
verapamil
Ca channel blocker
antianginal, antihypertensive
antiarrhythmic - class IV
decrease sinus node pacemaker rate
decrease AV conduction
decrease contractility
diltiazem
Ca channel blocker
antianginal, antihypertensive
antiarrhythmic - class IV
decrease sinus node pacemaker rate
decrease AV conduction
decrease contractility
propafenone
antiarrhythmic - class IC
block Na channel
block β receptor
supraventricular arrhythmia
flecainide
antiarrhythmic - class IC
block Na, K channels
maintenance of sinus rhythm in certain supraventricular arrhythmias in patients without structural heart disease
mexiletine
antiarrhythmic - class IB
block Na channel
oral lidocaine-like drug
serious ventricular arrhythmias
lidocaine
antiarrhythmic - class IB
block Na channel
acute treatment of ventricular arrhythmias
disopyramide
antiarrhythmic - class IA
block Na, K channels
block ACh receptors
serious ventricular arrhythmias
procainamide
antiarrhythmic - class IA
block Na, K channels
serious ventricular arrhythmias
active metabolite (NAPA)
drug-induced lupus
agranulocytosis
quinidine
antiarrhythmic - class IA
block Na, K channels
block α, ACh receptors
atrial fibrillation and flutter
serious ventricular arrhythmias
thrombocytopenia