pharm cardiovascular and ANS
Terms
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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