carvedilol,
carvedilol [kahr´vĕ-dil″ol]
carvedilol (kär´v
dil´ol),drug class: nonselective β-adrenergic blocking agent with α-blocking activity;
action: produces fall in blood pressure without reflex tachycardia or significant reduction in heart rate;
use: essential hypertension alone or with other antihypertensives.
carvedilol
Coreg, Eucardic (UK)
Pharmacologic class: Beta-adrenergic blocker (nonselective)
Therapeutic class: Antihypertensive
Pregnancy risk category C
Action
Blocks stimulation of cardiac beta1-adrenergic receptor sites and pulmonary beta2-adrenergic receptor sites. Shows intrinsic sympathomimetic activity, causing slowing of heart rate, decreased myocardial excitability, reduced cardiac output, and decreased renin release from kidney.
Availability
Capsules (extended-release): 10 mg, 20 mg, 40 mg, 80 mg
Tablets: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg
⊘Indications and dosages
➣ Hypertension
Adults: Initially, 6.25 mg P.O. b.i.d. (Coreg). May be increased q 7 to 14 days to a maximum dosage of 25 mg b.i.d. Or, 20 mg P.O. daily (Coreg CR). If tolerated, using standing systolic pressure about 1 hour after dosing, maintain dosage of Coreg CR for 7 to 14 days; then increase to 40 mg once daily if needed based on trough systolic standing blood pressure. Maintain this dosage for 7 to 14 days and adjust to 80 mg once daily if tolerated and needed. Total daily dose of Coreg CR shouldn't exceed 80 mg.
➣ Heart failure caused by ischemia or cardiomyopathy
Adults: Initially, 3.125 mg P.O. b.i.d. (Coreg) for 2 weeks. May increase to 6.25 mg b.i.d. Dosage may be doubled q 2 weeks as tolerated, not to exceed 25 mg b.i.d. in patients weighing less than 85 kg (187 lb) or 50 mg b.i.d. in patients weighing more than 85 kg. Or, 10 mg P.O. daily (Coreg CR) for 2 weeks. If tolerated, increase dosage to 20 mg, 40 mg, and 80 mg over successive intervals of at least 2 weeks.
➣ Left ventricular dysfunction following myocardial infarction
Adults: Initially, 6.25 mg P.O. b.i.d. (Coreg); increase after 3 to 10 days to 12.5 mg b.i.d. (based on tolerability), then increase to target dosage of 25 mg b.i.d. A lower starting dose (3.125 mg b.i.d.) or slower titration may be used if clinically indicated. Or, 20 mg P.O. once daily (Coreg CR); increase after 3 to 10 days to 40 mg daily (based on tolerability), then increase to target dose of 80 mg daily. A lower starting dose may be used (10 mg daily) or the rate of up titration may be slowed if clinically indicated.
Off-label uses
• Angina pectoris
• Idiopathic cardiomyopathy
Contraindications
• Hypersensitivity to drug
• Uncompensated heart failure
• Pulmonary edema
• Cardiogenic shock
• Bradycardia or heart block
• Severe hepatic impairment
• Bronchial asthma, bronchospasm
Precautions
Use cautiously in:
• renal or hepatic impairment, pulmonary disease, diabetes mellitus, hypoglycemia, thyrotoxicosis, peripheral vascular disease, hypotension, respiratory depression
• elderly patients
• pregnant or breastfeeding patients
• children.
Administration
• Ensure that patient is hemodynamically stable and fluid retention has been minimized before starting therapy.
• Give immediate-release form with food to slow absorption and minimize orthostatic hypotension.
• Give extended-release form in the morning with food and instruct patient to swallow capsule whole.
• For patients who can't swallow capsules whole, carefully open capsules and sprinkle contents on applesauce; have patient swallow contents immediately without chewing. Don't use warm applesauce; doing so could affect the modified-release properties of this formulation.
• When drug is used to treat heart failure, check apical pulse before administering. If it's below 60 beats/minute, withhold dosage and contact prescriber.
• When drug is used for hypertension, check standing systolic pressure about 1 hour after dosing for use as a guide for patient tolerance.
• Be aware that addition of diuretic may cause additive effects and may worsen orthostatic hypotension.
• Know that full antihypertensive effect takes 7 to 14 days.
☞ Don't withdraw drug abruptly, because this may lead to withdrawal phenomenon (angina exacerbation, myocardial infarction, ventricular arrhythmias, and even death).
| Route | Onset | Peak | Duration |
| P.O. | Within 1 hr | 1-2 hr | 12 hr |
Adverse reactions
CNS: dizziness, fatigue, anxiety, depression, insomnia, memory loss, nightmares, headache, pain
CV: orthostatic hypotension, peripheral vasoconstriction, angina pectoris, chest pain, hypertension, bradycardia, heart failure, atrioventricular block
EENT: blurred or abnormal vision, dry eyes, stuffy nose, rhinitis, sinusitis, pharyngitis
GI: nausea, diarrhea, constipation
GU: urinary tract infection, hematuria, albuminuria, decreased libido, erectile dysfunction, renal dysfunction
Hematologic: bleeding, purpura, thrombocytopenia
Metabolic: hypovolemia, hypervolemia, hyperglycemia, hyponatremia, hyperuricemia, glycosuria, gout, hypoglycemia
Musculoskeletal: arthralgia, back pain, muscle cramps
Respiratory: wheezing, upper respiratory tract infection, dyspnea, bronchitis, bronchospasm, pulmonary edema
Skin: pruritus, rash
Other: weight gain, lupuslike syndrome, viral infection, anaphylaxis
Interactions
Drug-drug. Antihypertensives: additive hypotension
Calcium channel blockers, general anesthetics, I.V. phenytoin: additive myocardial depression
Cimetidine: increased carvedilol toxicity
Clonidine: increased hypotension and bradycardia, exaggerated withdrawal phenomenon
Digoxin: additive bradycardia
Dobutamine, dopamine: decrease in beneficial cardiovascular effects
Insulin, oral hypoglycemics: altered efficacy of these drugs
MAO inhibitors: hypertension
Nonsteroidal anti-inflammatory drugs: decreased antihypertensive action
Rifampin, thyroid preparations: decreased carvedilol efficacy
Theophyllines: reduced theophylline elimination, antagonistic effect that decreases theophylline or carteolol efficacy
Drug-diagnostic tests. Antinuclear antibodies: increased titers
Blood urea nitrogen, glucose, lipoproteins, potassium, triglycerides, uric acid: increased levels
Drug-food. Any food: delayed drug absorption
Drug-behaviors. Acute alcohol ingestion: additive hypotension
Patient monitoring
• Watch for signs and symptoms of hypersensitivity reaction.
• Assess baseline CBC and kidney and liver function test results.
• Monitor vital signs (especially blood pressure), ECG, and exercise tolerance. Drug may alter cardiac output and cause ineffective airway clearance.
• Weigh patient daily and measure fluid intake and output to detect fluid retention.
• Measure blood glucose regularly if patient has diabetes mellitus. Drug may mask signs and symptoms of hypoglycemia.
Patient teaching
• Instruct patient to take drug with food exactly as prescribed.
• Tell patient to take extended-release capsule in the morning with food, to swallow capsule whole, and not to chew, crush, or divide its contents.
• Instruct patient who can't swallow capsule whole to carefully open capsule, sprinkle contents on cool or cold applesauce, and swallow contents immediately without chewing. Tell patient not to store mixture for future use.
☞ Caution patient not to stop taking drug abruptly, because serious reactions may result.
• Advise patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from sudden blood pressure drop.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Inform male patient that drug may cause erectile dysfunction. Advise him to discuss this issue with prescriber.
• Advise patient to use soft-bristled toothbrush and electric razor to avoid gum and skin injury.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.
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