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Glossary of pharm cardiovascular and ANS

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botulinum toxin: class
anti-cholinergic
carbidopa: class
anti-adrenergic
tyramine: class
adrenergic
phenylephrine: class
alpha agonist
methoxamine: class
alpha agonist
norepinephrine: class
alpha agonist
dopamine: class
alpha agonist
phentolamine: class
allpha antagonist
phenoxybenzamine: class
allpha antagonist
prazosin: class
allpha antagonist
clonidine: class
centrally acting alpha agonist
methyldopa: class
centrally acting alpha agonist
yohimbine: class
alpha 2 antagonist
isoproterenol: class
beta agonist
dobutamine: class
beta agonist
propranolol: class
beta blocker
metoprolol: class
beta blocker
atenolol: class
beta blocker
bromocriptine: class
dopamine agonist
ephedrine: class
indirectly acting pheylethylamine
phenylpropanolamine: class
indirectly acting pheylethylamine
pseudoephedrine: class
indirectly acting pheylethylamine
methacholine: class
muscarinic agonist
bethanechol: class
muscarinic agonist
pilocarpine: class
muscarinic agonist
atropine: class
muscarinic antagonist

(competitive inhibitor)
nicotine: class
nicotinic agonist
insecticides: class
cholinesterase inhibitor
physostigmine: class
cholinesterase inhibitor
neostigmine: class
cholinesterase inhibitor
organophosphates: class
cholinesterase inhibitor
tubocurarine: class
Nondepolarizing neuromuscular blocker
succinylcholine: class
depolarizing neuromuscular blocker
dantrolene: class
spasmolytic
botulinum toxin: administration
local injection
tubocurarine: administration
parenteral
succinylcholine: administration
parenteral
propranolol: administration
IV, oral (40x greater oral b/c 1st pass effect)
esmolol: administration
IV
methyldopa: administration
IV as its ethyl ester
phenoxybenzamine: administration
oral
phentolamine: administration
IV
Nitroglycerin: administration
orally, sublingual, transdermal, spray to buccal mucosa, IV
Isosorbide dinitrate: administration
oral
nitroprusside: administration
IV only, with glucose water solution
mannitol: administration
IV
quinidine: administration
oral
procainamide: administration
IV
lidocaine: administration
IV
mexiletine: administration
oral
tocainide: administration
oral
ibutilide: administration
IV
inamrinone: administration
IV
streptokinase: administration
IV
t-PA: administration
IV
reteplase: administration
IV, double bolus
TNK t-PA : administration
single bolus
Unfractionated Heparin: administration
never IM goddamit. IV and subq
Lepirudin: administration
IV
Agatroban: administration
IV
Warfarin: administration
oral, 100% absorption
lidocaine: distribution and elimination times
8 min dist, 108 min elim...elim t1/2 determines time to steady state and maintanence dosing
phenoxybenzamine: time to clinical effect
hours
methyldopa: time to clinical effect
six hours (must be metabolized)
Nitroglycerin: time to clinical effect
minutes
Isosorbide dinitrate: time to clinical effect
30-90 min
Isosorbide mononitrates: time to clinical effect
30-60 min
Losartan: time to clinical effect
3-4 hours
amiodarone: time to clinical effect
slow accumulation to steady state
Ticlopidine: time to clinical effect
delay in onset 5=10 dias
botulinum toxin: duration/half life
weeks/months
phentolamine: duration/half life
short acting
phenoxybenzamine: duration/half life
over a day
tubocurarine: duration/half life
60 min half life
succinylcholine: duration/half life
5-10 min half life
propranolol: duration/half life
3-6 hours
esmolol: duration/half life
9 min half life
terazosin: duration/half life
3-4 hours
Nitroglycerin: duration/half life
30 min-hrs
Isosorbide dinitrate: duration/half life
hrs
Isosorbide mononitrates: duration/half life
hrs
nitroprusside: duration/half life
short, minutes
nifedipine: duration/half life
long acting
verapamil: duration/half life
long acting
diltiazem: duration/half life
long acting
amiodarone: duration/half life
very long, 40-60 days
inamrinone: duration/half life
elimination half life 2.5 hours, but can be >12 hours in CHF pts
APSAC: duration/half life
stupid long, yo. 60 mins
t-PA: duration/half life
stupid short, yo. 6 minutes
Ticlopidine: duration/half life
effects persist several days
Lepirudin: duration/half life
slower clearance than heparin, can give sub q
digoxin: time to steady state after maintanance dosages started
1 week
digitoxin: time to steady state after maintanance dosages started
1 month
botulinum toxin: mechanism
blocks release of Ach
tyramine: mechanism
displaces norepinephrine into synaptic cleft
methyldopa: mechanism
metabolized to alphamethylnorepinephrine, which stimulates presynaptic alpha 2 receptors
ephedrine: mechanism
indirectly acting adrenergic
pseudoephedrine: mechanism
indirectly acting adrenergic
methacholine: mechanism
muscarinic agonist
bethanechol: mechanism
muscarinic agonist
pilocarpine: mechanism
muscarinic agonist
pralidoxime: mechanism
reactivates cholinesterase
organophosphates: mechanism
cholinesterase inhibition
tubocurarine: mechanism
nondepolarizing blockade at neuromuscular jnx
succinylcholine: mechanism
depolarizing neuromuscular blockade
dantrolene: mechanism
reduces release of Ca++ from sarcoplasmic reticulum
atenolol: mechanism
beta 1 selective blocker
metoprolol: mechanism
beta 1 selective blocker
labetalol: mechanism
alpha 1 antagonist; beta 1 antagonist; beta 2 agonist
labetalol RR stereoisomer: mechanism
beta 1 antabonist and partial beta 2 agonist
labetalol SR stereoisomer: mechanism
alpha 1 antagonist
carvedilol, R isomer: mechanism
alpha 1 blocker
carvedilol, S isomer: mechanism
beta blocker and alpha 1 blocker
NO dependent vasodialtors: mechanism
activates guanylate cyclase, inc cGMP, cGMP activates protein kinase -> dilation of veins (major) and coronary vessels (minor)
sildenafil: mechanism
inhibits cGMP phosphpodiesterase Type V
hydralazine: mechanism
who the fuck knows?
minoxidil: mechanism
opens ATP sensitve K+ channel in arterial smooth muscle, dilates arteries
Captopril: mechanism
block conversion of Ang I to Ang II, block degradation of bradykinin
mannitol: mechanism
filtered but not resorded, osmotically inspired diuresis
furosemide: mechanism
inhibit contransport of Na, Cl, and K at the luminal membrane of the thick ascending limb of Henle's loop
ethacrynic acid: mechanism
inhibit contransport of Na, Cl, and K at the luminal membrane of the thick ascending limb of Henle's loop
hydrochlorothiazide: mechanism
inhibit Na transport in distal convoluted tubule (Na-Cl cotransporter)
triamterene: mechanism
inhibit luminal Na channel in collecting tubules
amiloride: mechanism
inhibit luminal Na channel in collecting tubules
quinidine: mechanism
block Na and K currents, alpha block and vagal inhibition
procainamide: mechanism
blocks Na and K channels
sotalol: mechanism
non selective beta blocker, K channel blocker
ibutilide: mechanism
K blocker, Na opener
digitalis: mechanism
increases myocardial intracellular Ca++ by blocking Na-K ATPase...also anti-symp pro-vagal effects
digoxin: mechanism
increases myocardial intracellular Ca++ by blocking Na-K ATPase...also anti-symp pro-vagal effects
digitoxin: mechanism
increases myocardial intracellular Ca++ by blocking Na-K ATPase...also anti-symp pro-vagal effects
inamrinone: mechanism
inhibits phosphodiesterase Type III (cardiac), increased cAMP -> increased intracellular Ca++
streptokinase: mechanism
indirect plasminogen activator...binds w/ a plaminogen molecule, complex activates 2nd molecule
urokinase: mechanism
direct plasminogen activator
t-PA: mechanism
binds to fibrin, directly activates plasminogen
reteplase: mechanism
binds to fibrin, directly activates plasminogen
Aspirin: mechanism
inhibits cyclooxygenase, thereby decreasing thromboxane A2
Dipyridamole: mechanism
Inhibits phosphodiesterase to increase accumulation of cAMP, blocks adenosine uptake, prevents platelet activation
Ticlopidine: mechanism
inhibits ADP activation, inhibit glycoprotein Iib/IIIa receptor and vonWillebrand factor
Clopidogrel: mechanism
inhibits ADP activation, inhibit glycoprotein Iib/IIIa receptor and vonWillebrand factor
Abciximab: mechanism
antibody to glycoprotein Iib/IIIa
Unfractionated Heparin: mechanism
inactivates coag factors, most importantly II and X
Low-Molecular Weight Heparins: mechanism
bind antithrombin-III/thrombin (little effect on PTT)
Lepirudin: mechanism
direct thrombin inactivator
Agatroban: mechanism
directly reversibly inhibits thrombin
Warfarin: mechanism
inhibits vitamin K, thusinhibits II, VII, IX, X, protein C, and protein S
digitalis: electrophysiologic effects on His-Purkinje system
resting potential more positive; Action Potential duration shortens; enhanced phase 4 depolarization (automaticity) at higher concentrations
carbidopa: receptor, effect
inhibits dopa decarboxylase (dopa to dopamine)
phentolamine: receptor, effect
alpha 1; competitive antagonist
phenoxybenzamine: receptor, effect
alpha 1; noncompetitive antagonist
clonidine: receptor, effect
presynaptic alpha 2 stimulation, feedback inhibition of norepinephrine
yohimbine: receptor, effect
blocks alpha 2 receptors in medulla, increased sympathetic outflow
isoproterenol: receptor, effect
stimulates beta 1 and beta 2 receptors
dobutamine: receptor, effect
beta 1 agonist
propranolol: receptor, effect
competitive inhibitor at beta 1 and beta 2
metoprolol: receptor, effect
selective blocker of beta 1
atenolol: receptor, effect
beta 1 blocker
methacholine: receptor, effect
muscarinic agonist
bethanechol: receptor, effect
muscarinic agonist
pilocarpine: receptor, effect
muscarinic agonist
atropine: receptor, effect
muscarinic antagonist
nicotine: receptor, effect
nicotinic agonist
insecticides: receptor, effect
inhibits acetylcholinesterase and pseudocholinesterase
labetolol: receptor, effect
beta blocker and alpha 1 blocker (more pronounced when given orally)
carvedilol: receptor, effect
beta blocker and alpha 1 blocker
nifedipine: receptor, effect
block L-type C++ channel, vascular
verapamil: receptor, effect
block L-type C++ channel, cardio
diltiazem: receptor, effect
block L-type C++ channel, cardio adn vascular
acetazolamide: receptor, effect
noncompetitive inhibition of carbonic anhydrase in proximal tubule, prevents reabsorption of NaHCO3, net secretion of NaHCO3 with obligatory H2O
spironolactone: receptor, effect
competes with aldosterone for cytosolic receptor, prevents aldosterone inspired K excretion and Na reabsorption
amiodarone: lipophilicity
high
carbidopa: clinical use
decrease peripheral dopamine production in anti-parkinsons tx
phenylephrine: clinical use
tx hyptension, cause mydriasis, tx nasal congestions, tx paroxysmal atrial tachycardia
phentolamine: clinical use
dx of pheochromocytoma, emergent tx of pheochromocytoma
phenoxybenzamine: clinical use
tx of pheochromocytoma
clonidine: clinical use
tx htn
yohimbine: clinical use
aphrodisiac
isoproterenol: clinical use
tx gravid uterus, asthma
pseudoephedrine: clinical use
tx nasal congestion
methacholine: clinical use
provoke bronchoconstriction w/ methacholine challenge
bethanechol: clinical use
improving gastric emptying; tx urinary retention
pilocarpine: clinical use
induce salivation; tx open angle glaucoma
atropine: clinical use
tx vasovagal syncope, decrease respiratory secretions
physostigmine: clinical use
tx of anticholinergic syndrome
neostigmine: clinical use
tx atonly of detrusor, tx myasthenia gravis, tx glaucoma
organophosphates: clinical use
kill one's enemies
dantrolene: clinical use
tx of malignant hyperthermia (releave muscle contracture)
tx torsades de pointes
isoproterenol
methyldopa: clinical use
tx htn
Nitroglycerin: clinical use
angina
Isosorbide dinitrate: clinical use
angina
Isosorbide mononitrates: clinical use
angina
sildenafil: clinical use
stiff penis
nitroprusside: clinical use
acute hypertension, perioperative hypertension control, heart failure
hydralazine: clinical use
hypertension (best w/ beta blocker) heart failure (combined w/ nitrates and diuretics)
minoxidil: clinical use
difficult hypertension (need beta blocker and diuretic) hair growth
nifedipine: clinical use
hypertension
acetazolamide: clinical use
tx of glaucoma, acute mountan sickness, metabolic alkalosis
furosemide: clinical use
acute pulmonary edema, severe edema; hypercalcemia
ethacrynic acid: clinical use
acute pulmonary edema, severe edema; hypercalcemia
hydrochlorothiazide: clinical use
tx of essential hypertension, nephrogenic diabetes insipidous, tx hypercalciuria
spironolactone: clinical use
tx of edema of cirrhosis, K sparing used in conjunction with k wasting diuretics, counteract aldosterone escape with ACEIs and ARBs
quinidine: clinical use
chronic oral therapy of atrial fib/flutter (and VT)
procainamide: clinical use
supraventricular and ventricular arrhythmias
amiodarone: clinical use
effective for most arrhythmias; refractory VT/VF
ibutilide: clinical use
atrial flutter, less effective w/ atrial fib
dofetilide: clinical use
Atrial fib/flutter, esp patients w/ left ventric dysfunction
digitalis: clinical use
relieve sx of CHF; supraventricular arrhythmias (but can block AV node completely and cause Atrial fib)
inamrinone: clinical use
short term CHF support
e-aminocaproic acid: clinical use
antifibrinolytic
tranexamic acid: clinical use
antifibrinolytic
prazosin: Problems
First dose effect: severe hypotension w/ first dose. Tachyphylaxis
methyldopa: Problems
high doses may stimulate peripheral alpha 2 receptors, causing hypertension
propranolol: Problems
avoid in asthmatics
nicotine: Problems
bexold jarisch reflex (bradycardia, hypotension, nausea)
clonidine: Problems
clonidine rebound if withdrawn quickly
hydralazine: Problems
drug induced lupus erythmatosis, ANA positive, anti-histone antibodies
minoxidil: Problems
hair growth (not always problem), bigger heart if no beta blocker
propranolol: crosses CNS barrier?
oh yeah
metoprolol: crosses CNS barrier?
yes
atenolol: crosses CNS barrier?
no
physostigmine: crosses CNS barrier?
yes
neostigmine: crosses CNS barrier?
no, charged quaternary amine
tubocurarine: crosses CNS barrier?
loss of ventilation, histamine release, ANS effects
succinylcholine: crosses CNS barrier?
loss of ventilation, histamine release, ANS effects
atropine: adverse effects
constipation, xerostomia, hypohidrosis, mydriasis, urinary retention, glaucoma, decreased lacrimation, tachycardia, decreased respiratory secretions
organophosphates: adverse effects
Salivation, Lacrimation, Urination, Defecation, GI, Emesis....departure of soul
methyldopa: adverse effects
sedation, depression; hepatic toxicity; hemolytic anemia w/ positvie coomb's test
clonidine: adverse effects
Clonidine rebound when discontinued; sedation, depression; dry mouth; lost libido
phenoxybenzamine: adverse effects
hypotension, can be corrected with volume expansion
phentolamine: adverse effects
hypotension can tx with volume expansion
DILATORS: adverse effects
dizziness, headache
hydralazine: adverse effects
Lupus, Na retention, ischemia (coronary steal), enlarge heart if no beta blocker
furosemide: adverse effects
hpokalemia, los of Ca++ and Mg++
ethacrynic acid: adverse effects
hpokalemia, los of Ca++ and Mg++
spironolactone: adverse effects
hyperkalemia, gynecomastia--steroid cross talk
quinidine: adverse effects
diarrhea/gi intolerance 50%, Torsade de Pointes
N-acetylprocainamide: adverse effects
Lupus syndrome, 0.2% marrow aplasia
lidocaine: adverse effects
CNS toxicity
mexiletine: adverse effects
CNS toxicity
tocainide: adverse effects
CNS toxicity
amiodarone: adverse effects
multiple toxicities, eye, lungs, skin, thyroid
bretylium: adverse effects
biphasic autonomic response: hypertension, then hypotension--causes side effects

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