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Cardiovascular Drugs
L to Z

Go To Cardiovascular Drugs A to I

 Last Updated 04/10/00 12:26:51 PM

Labetalol (Normodyne, Trandate)
Class: b -blocker
Use: Treatment of mild to severe HTN. IV for hypertensive emergencies.
Action: Blocks a 1, b 1 and b 2 receptor sites with an a to b blockade ration of 1:3 (oral) and 1:7 (IV). Also inhibits neuronal reuptake of norepinephrine
Cardiac Effect:
Administration Routes: PO, IV
Onset Time: PO: 30-120 mins. IV 2-5 mins
½ Life: 6-8 hrs
Metabolism -- Excretion: Extensive first-pass liver conjugation -- <5% excreted in urine unchanged. Possible decreased clearance in neonates/infants.
Side Effects: Orthostatic hypotension, CHF, arrhythmias, reduced peripheral circulation, dyspnea, bradycardia, hepatotoxicity
Anesthesia Interactions:

Lidocaine (Xylocaine)
Class: Antiarrhythmic – Class I B (Na+ channel blocker)
Use: Local anesthetic for infiltration, peripheral nerve blocks, and epidural spinal anesthesia. Acute treatment of ventricular arrhythmias from myocardial infarction, cardiac manipulation, digitalis intoxication.
Action: Blocks both the initiation and conduction of nerve impulses by ¯ the neuronal membrane’s permeability to Na+ ions (Na+ channel blocker), which results in inhibition of depolarization with resultant blockade of conduction. Suppresses automaticity of conduction tissue, by ­ electrical stimulation threshold of ventricle, HIS-Purkinje system, and spontaneous depolarization of the ventricles during diastole by a direct action on the tissues.
Cardiac Effect: Blocks inactive and active channels. More selective to cells with long action potentials. ¯ APD.
Administration Routes: Topical, SC, Spinal, IV
Onset Time: 1.5-5 mins
½ Life: 2-10 mins. Terminal: 1.5-2 hrs
Metabolism -- Excretion: 90% in liver by CP450. --
Side Effects: Hypotension, heart block, arrhythmias, cardiovascular collapse, dyspnea, respiratory depression or arrest
Anesthesia Interactions: Effect of succinylcholine may be enhanced

Lisinopril (Prinivil, Zestril, Zestoretic)
Class: Angiotensin Converting Enzyme (ACE) Inhibitor
Use: Treatment of HTN, alone or in combination with other antihypertensive agents. Adjunctive therapy in treatment of CHF (afterload reduction)
Action: Competitive inhibitor of ACE. Prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. Results in lower levels of angiotensin II which causes an increase in plasma renin activity and a reduction in aldosterone secretion.
Cardiac Effect:
Administration Routes: PO
Onset Time:
½ Life: 11-12 hrs
Metabolism -- Excretion: Nearly none. -- Almost entirely excreted in urine as unchanged drug.
Side Effects: Hypotension, angina, tachycardia, peripheral edema, hepatitis
Anesthesia Interactions:

Losartan (Cozaar)
Class: Angiotensin II receptor blocker
Use: Antihypertensive
Action: An angiotensin II receptor antagonist that blocks the vasoconstriction and aldosterone secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to its receptor sites found in many tissues, including VSM.
Cardiac Effect:
Administration Routes: PO
Onset Time:
½ Life:
Metabolism -- Excretion: Extensive first pass metabolism (CP450) -- Mostly in feces. Some in urine.
Side Effects: Hypotension
Anesthesia Interactions:

Mannitol (Osmitrol)
Class: Osmotic Diuretic
Use: Reduction of increased intracranial pressure associated with cerebral edema. Promotion of diuresis in the prevention and/or treatment of oliguria or anuria r/t acute renal failure. Reduction of increased intraocular pressure.
Action: Increases the osmotic pressure of glomerular filtrate, which inhibits tubular reabsorption of water and electrolytes and increases urinary output. Does not cross the Blood brain barrier.
Cardiac Effect:
Administration Routes: IV
Onset Time: Diuresis: 1-3 hrs. ICP: 15 mins.
½ Life: 1.1-1.6 hrs.
Metabolism -- Excretion: Minimal in liver to glycogen -- Unchanged in urine
Side Effects: Circulatory overload, convulsions, hypovolemia, pulmonary edema
Anesthesia Interactions:

Metoprolol (Lopressor, Toprol SL)
Class: Antiarrhythmic – Class II (b -blocker -- Selective)
Use: Treatment of HTN and angina pectoris. Prevention of MI, atrial fibrillation, flutter, symptomatic treatment of hypertrophic subaortic stenosis.
Action: Selective inhibitor of b 1 receptors. Competitively blocks b 1 receptors, with little or no effect on b 2 receptors at doses <100 mg. Does not exhibit any membrane stabilizing or intrinsic sympathomimetic activity
Cardiac Effect:
Administration Routes: PO, IV
Onset Time: PO: 20-30 mins. IV: 5 mins
½ Life: 3-4 hrs. ESRD: 2.5-4.5 hrs.
Metabolism -- Excretion: Significant first-pass in liver. -- Urine (3-10% unchanged drug)
Side Effects: Bradycardia, arrhythmia
Anesthesia Interactions: If given IV in OR, can cause and increase in effect in propofol, ketamine, fentanyl, sufentanil, etomidate.

Milrinone (Primacor)
Class: Positive inotropic agent – Phosphodiesterase (PDE) inhibitor
Use: Short-term IV therapy of CHF. Used for Ca2+ antagonist intoxication
Action: Inhibits PDE III, the major PDE in cardiac and vascular tissues. Inhibition of PDE increases cAMP potentiating delivery of Ca2+ to myocardial contractile systems resulting in a positive inotropic effect. Inhibition of PDE in vascular tissue results in vasodilation with no change in heart rate.
Cardiac Effect:
Administration Routes: IV
Onset Time:
½ Life: 136 mins – 2.7 hrs
Metabolism -- Excretion: 12% hepatic -- 85% unchanged in urine.
Side Effects: Ventricular arrhythmias, hypotension, DP, V-Fib
Anesthesia Interactions:

Minoxidil (Rogaine, Loniten)
Class: Vasodilator
Use: Management of severe HTN resistant to treatment with other antihypertensives. Treatment of baldness.
Action: Produces vasodilation by directly relaxing arteriolar smooth muscle, with little effect on veins. Effects may be mediated by cAMP. Stimulation of hair growth is secondary to vasodilation, increased cutaneous blood flow and stimulation of resting hair follicles. ­ K+ efflux by activating the K+/ATP channels.
Cardiac Effect:
Administration Routes: PO, Topical
Onset Time: 30 mins
½ Life: 3.5-4.2 hrs
Metabolism -- Excretion: 88% hepatic glucuronidation -- 12% excreted unchanged in urine.
Side Effects: EKG T-wave changes, tachycardia, CHF, edema
Anesthesia Interactions:

Nicardipine (Cardene)
Class: Ca2+ Channel blocker
Use: Dihydropyridines (DHP). Chronic stable angina. Management of essential HTN, migraine prophylaxis. CHF.
Action: Inhibits Ca2+ from entering the "slow channels" or select voltage-sensitive areas of VSM and myocardium during depolarization, producing peripheral and coronary vasodilation. Increases myocardial O2 delivery in patients with vasospastic angina. Closed channel blocker.
Cardiac Effect:
Administration Routes: PO, IV
Onset Time:
½ Life: 2-4 hrs
Metabolism -- Excretion: Extensive first-pass in liver. -- As metabolites in urine
Side Effects: Tachycardia, pedal edema
Anesthesia Interactions:

Nifedipine (Adalat, Procardia)
Class: Ca2+ Channel blocker
Use: Dihydropyridines (DHP). Angina, hypertrophic cardiomyopathy, HTN (sustained release only), pulmonary HTN
Action: Inhibits Ca2+ from entering the "slow channels" or select voltage-sensitive areas of VSM and myocardium during depolarization, producing peripheral and coronary vasodilation. Increases myocardial O2 delivery in patients with vasospastic angina. More vascular than Diltiazem. Closed channel blocker.
Cardiac Effect:
Administration Routes: PO, SL
Onset Time: PO: 20 mins. SL: 1-5 mins
½ Life: 2-5 hrs. Cirrhosis: 7 hrs
Metabolism -- Excretion: Liver to inactive metabolites -- Urine
Side Effects: Hypotension, peripheral edema, dyspnea, tachycardia
Anesthesia Interactions: Fentanyl may increase hypotension.

Nimodipine (Nimotop)
Class: Ca2+ channel blocker (Dihydropyridines – DHP)
Use: Improvement of neurological deficits due to spasm following subarachnoid hemorrhage from ruptured congenital intracranial aneurysms in patients who are in good neurological condition postictus
Action: Inhibits Ca2+ from entering the "slow channels" or select voltage-sensitive areas of VSM and myocardium during depolarization, producing peripheral and coronary vasodilation. Increases myocardial O2 delivery in patients with vasospastic angina. Has a greater effect on cerebral arteries than other arteries. Closed channel blocker.
Cardiac Effect:
Administration Routes: PO
Onset Time:
½ Life: 3 hrs
Metabolism -- Excretion: Liver -- 32% feces. 50% in urine.
Side Effects: Hypotension. Edema, tachycardia, bradycardia
Anesthesia Interactions: Fentanyl may increase hypotension.

Nitroglycerin (Nitrostat)
Class: Nitrate. Vasodilator
Use: Treatment of angina pectoris. IV for CHF. Pulmonary HTN. Hypertensive emergencies. Control of blood pressure in perioperative HTN. Controlled hypotension during surgical procedures
Action: Reduces cardiac oxygen demand by decreasing left ventricular pressure and systemic vascular resistance. Dilates coronary arteries and improves collateral flow to ischemic regions.
Cardiac Effect:
Administration Routes: SL, PO, IV, Topical, Transdermal, Spray
Onset Time: IV: Immediate. SL: 1-3 mins. Transdermal: 40-60 mins.
½ Life: 1-4 mins
Metabolism -- Excretion: Extensive first-pass -- Inactive metabolites in urine.
Side Effects: Hypotension, reflex tachycardia, bradycardia
Anesthesia Interactions:

Nitrosprusside (Nipride, Nitropress, Sodium Nitrosprusside, SNP)
Class: Nitrate - Vasodilator
Use: Management of hypertensive crises. CHF. Used for controlled hypotension to reduce bleeding during surgery
Action: Causes vasodilation by action on VSM (by generation of NO), thus ¯ peripheral resistance. ­ CO by ¯ afterload. Has little effect on other smooth muscle. Produces a baroreceptor mediated reflex tachycardia. Alters pulmonary V/Q, promoting shunting
Cardiac Effect:
Administration Routes: IV
Onset Time: 30-60 seconds
½ Life: <10 minutes. Thiocyanate: 2.7-7 days
Metabolism -- Excretion: Converted to cyanide ions in bloodstream. -- Thiocyanate renally eliminated
Side Effects: Hypotension, cyanide poisoning, hypoxia
Anesthesia Interactions: To treat cyanide poisoning use 100% O2, NaCO3, Sodium nitrate (competes with SNP), Vitamin B12 (binds with Cn-)

Pindolol (Visken)
Class: b -blocker (Partial agonist)
Use: Management of HTN
Action: Blocks both b1 and b2 receptors and has mild intrinsic sympathomimetic activity. Has negative inotropic and chronotropic effects and can significantly slow AV nodal conduction. Partial agonist. Has ISA (Intrinsic sympathomimetic activity) properties.
Cardiac Effect:
Administration Routes: PO
Onset Time:
½ Life: 2.5-4 hrs
Metabolism -- Excretion: 60-65% liver -- 70% hepatic. 30% renal (35-50% unchanged drug)
Side Effects: CHF, arrhythmia, reduced peripheral circulation, bradycardia
Anesthesia Interactions:

Prazosin (Minipress)
Class: a -blocker (Peripherally acting)
Use: Treatment of HTN, severe CHF. Reduce mortality in post MI patients with left ventricular dysfunction. May reduce vasospasm. Decrease ventricular arrhythmias due to cardiac ischemia.
Action: Competitively inhibits postsynaptic a 1 receptors which results in dilation of arterioles and a decrease in TPR and BP. Also dilates veins and therefore decreases cardiac preload.
Cardiac Effect: Minor ¯ in contractility
Administration Routes: PO
Onset Time: 1-2 hrs
½ Life: 2-4 hrs
Metabolism -- Excretion: Primarily in liver. -- Primarily in bile and feces. 6-10% in urine as unchanged drug
Side Effects: Orthostatic hypotension, edema, no sympathetic response.
Anesthesia Interactions:

Procainamide (Procan, Promine)
Class: Antiarrhythmic – Class I A (Na+ channel blocker)
Use: Treatment of ventricular tachycardia, PVC’s PAT’s, and A-fib. Prevention of recurrence of VT, PSVT, A-fib or A-flutter.
Action: ¯ myocardial excitability and conduction velocity and may ¯ contractility, by ­ the electrical stimulation threshold of ventricle, HIS-Purkinje system and through direct cardiac effects. Open channel blocker (frequency drug block). ­ APD. ¯ rate of rise of AP.
Cardiac Effect:
Administration Routes: PO, IM, IV
Onset Time: IM 10-30 mins
½ Life: Procainamide: Children: 1.7 hrs. Adults: 2.5-4.7 hrs. NAPA: Children: 6 hrs. Adults: 6-8 hrs.
Metabolism -- Excretion: Acetylation in liver to produce N-acetyl procainamide (NAPA) (active metabolite) -- Urinary excretion (25% as NAPA)
Side Effects: Tachycardia, arrhythmias, AV block, QT prolongation, widening QRS, hypotension, pleural effusion
Anesthesia Interactions: Increased effect of skeletal muscle relaxants, quinidine and lidocaine and neuromuscular blockers (succinylcholine)

Propranolol (Inderal)
Class: Antiarrhythmic – Class II (b -blocker -- Non-selective)
Use: Management of HTN, angina and arrhythmias. Prevention of MI, migraine. Symptomatic treatment of hypertrophic subaortic stenosis.
Action: Nonselective b -blocker. Competitively blocks response to b 1 and b 2 stimulation which results in decreases in HR (by decreasing AV nodal conduction), myocardial contractility, blood pressure, and myocardial oxygen demand.
Cardiac Effect:
Administration Routes: PO, IV
Onset Time: 1-2 hrs.
½ Life: Children: 3.9-6.4 hrs. Adults: 4-6 hrs.
Metabolism -- Excretion: Extensive first-pass effect. Metabolized to active and inactive compounds. -- 96-99% in urine
Side Effects: Bradycardia, CHF, hypotension, bronchospasm
Anesthesia Interactions:

Spironolactone (Aldactone)
Class: K+ Sparing Diuretic
Use: Management of edema associated with excessive aldosterone excretion. HTN. Primary hyperaldosteronism. hypokalemia. Treatment of hirsutism. Cirrhosis of liver accompanied by edema or ascites.
Action: Competes with aldosterone for receptor sites in the distal renal tubules, increasing Na+, Cl- and H2O excretion while conserving K+ and H+ ions. May block the effect of aldosterone on arteriolar smooth muscle as well
Cardiac Effect:
Administration Routes: PO
Onset Time: Slow
½ Life: 78-84 minutes
Metabolism -- Excretion: In liver to multiple metabolites including canrenone (active) -- Urinary and biliary excretion
Side Effects: Hypotension, edema, bradycardia, CHF
Anesthesia Interactions:

Timolol (Timoptic, Blocadren)
Class: b -blocker
Use: Ophthalmic dosage form used in treatment of elevated intraocular pressure such as glaucoma or ocular hypertension. Orally for treatment of HTN and angina and reduce mortality following MI and prophylaxis of migraine.
Action: Blocks both b1 and b2 receptors, reduces intraocular pressure by reducing aqueous humor production or possibly outflow. Reduces blood pressure by blocking adrenergic receptors and decreasing sympathetic outflow, produces a negative chronotropic and inotropic activity through an unknown mechanism
Cardiac Effect:
Administration Routes: PO, Drops
Onset Time: 15-45 minutes
½ Life: 2-2.7 hrs
Metabolism -- Excretion: Extensive first pass in liver -- Urinary excretion (15-20% as unchanged drug)
Side Effects: Bradycardia, dyspnea, arrhythmia, CHF
Anesthesia Interactions:

Triamterene (Dyrenium)
Class: K+ Sparing Diuretic
Use: Alone or in combination with other diuretic in treatment of edema and HTN. Decreases K+ excretion caused by kaliuretic diuretics.
Action: Competes with aldosterone for receptor sites in the distal renal tubules, increasing Na+, Cl-, and H2O excretion while conserving K+ and H+ ions. May block the effect of aldosterone on arteriolar smooth muscle as well
Cardiac Effect:
Administration Routes: PO
Onset Time: 2-4 hrs
½ Life: 100-150 minutes
Metabolism -- Excretion: --
Side Effects: Hypotension, edema, CHF, bradycardia, dyspnea
Anesthesia Interactions:

Urea (Carbamide)
Class: Osmotic Diuretic
Use: Reduction of intracranial or intraocular pressure.
Action: Elevates plasma osmolality, enhancing the flow of H2O into extracellular fluid such as blood, and reducing intracranial and intraocular pressure.
Cardiac Effect:
Administration Routes: IV
Onset Time: 1-2 hrs
½ Life:
Metabolism -- Excretion: Hydrolyzed in GI by bacterial urease -- By kidneys.
Side Effects: Syncope, hypotension
Anesthesia Interactions:

Verapamil (Calan, Verelan)
Class: antiarrhythmic – Class IV (Ca2+ channel blocker) (Diphenylalkalamine)
Use: (Diphenylalkalamine) Treatment of angina pectoris and HTN, PSVT, atrial fibrillation, atrial flutter.
Action: Inhibits CA2+ from entering the "slow channels" or select voltage-sensitive areas of VSM and myocardium during depolarization, producing a relaxation of coronary VSM and coronary vasodilation. Increases myocardial O2 delivery in patients with vasospastic angina. Slows automaticity and conduction of AV node. Open channel blocker. Most cardio-selective.
Cardiac Effect: Most cardio-selective. Negative inotrope.
Administration Routes: IV, PO
Onset Time:
½ Life: Infants: 4.4-6.9 hrs. Adults: 2-12 hrs.
Metabolism -- Excretion: Extensive firs-pass in liver -- 70% excreted in urine (16% in feces.
Side Effects: Bradycardia, first, second or third degree AV block, CHF, hypotension, peripheral edema
Anesthesia Interactions: Fentanyl may increase hypotension. Will increase AV block because it increases [Dig].

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