Carvedilol Brand Name– Coreg | Coreg CR
What is Carvedilol
Carvedilol is a combined alpha- and nonselective beta-blocker. Although it has some pharmacologic similarities to labetalol, the ratio of beta to alpha-1 effects is much greater for carvedilol than for labetalol.
Carvedilol is a lipophilic beta-blocker, and lacks intrinsic sympathomimetic activity (ISA).
Carvedilol also possesses antioxidant properties. The commercial product is a racemic mixture of two enantiomers, R(+) and S(-), both of which are important for the desired clinical effect.
Carvedilol (Coreg®) was approved in the US in September 1995 for the treatment of hypertension, either alone or in combination with other antihypertensive agents. In comparative studies in elderly hypertensive patients, blood pressure lowering effects of carvedilol were similar to other antihypertensives.
Carvedilol is appropriate therapy for treating hypertension in patients with renal disease or diabetes mellitus. A study in the treatment of heart failure was prematurely stopped in April 1995 due to early evidence of a beneficial effect on morbidity and mortality; results revealed a 65% decrease in risk of death in patients assigned to carvedilol.
Only 1.6% of patients who were randomized had to discontinue carvedilol due to worsening heart failure.
The FDA granted final approval for carvedilol use in mild-moderate heart failure in May 1997. An indication for use in severe heart failure received approval in November 2001 based on the COPERNICUS trial findings; carvedilol reduced mortality and hospitalization rate in patients with severe chronic heart failure.
Subsequently, the COMET trial evaluated carvedilol vs. metoprolol in patients with chronic heart failure (NYHA Class II—IV), and demonstrated a significantly lower all-cause mortality for carvedilol (34% vs. 40% for metoprolol).
However, the COMET study has been criticized for utilizing the immediate-release form of metoprolol (tartrate) vs. the extended-release formulation (succinate), which has been FDA-approved for heart failure based on the favorable findings of the MERIT-HF trial.
The COMET trial has also been criticized for evaluating a substantially lower metoprolol target dosage (50 mg PO twice daily) than the FDA-approved target dosage for heart failure (200 mg PO once daily) supported by the MERIT-HF trial. In March 2003, carvedilol received approval for use to prevent cardiovascular mortality in stable patients with left ventricular dysfunction following acute myocardial infarction.
This approval was based on the results of the CAPRICORN trial.
Carvedilol has been studied in stable angina pectoris. The 2007 AHA guidelines for the management of hypertension state beta-blockers should not be used as first-line therapy for the treatment of hypertension, as several comparative clinical trials have shown beta blockers to be inferior to ACE inhibitors, angiotensin-receptor blockers, or calcium channel blockers for preventing both stroke and coronary artery disease complications.
These guidelines do, however, recommend the use of beta-blockers for the treatment of hypertension in patients with angina, prior myocardial infarction, or heart failure.
Carvedilol has been marketed in Europe since the 1980s under the trade name Kredex™.
Extended-release carvedilol tablets (Coreg CR™) were approved by the FDA in October 2006 for the same indications approved for regular-release carvedilol tablets (Coreg®).
Indications
- acute myocardial infarction
- angina
- atrial fibrillation
- atrial flutter
- cardiomyopathy
- heart failure
- hypertension
- reduction of cardiovascular mortality
- unstable angina
For the treatment of essential hypertension, either as a single agent or in combination with other antihypertensive agents
Side Effects
- abdominal pain
- alopecia
- amnesia
- anaphylactoid reactions
- anemia
- angina
- angioedema
- anxiety
- aplastic anemia
- arthralgia
- asthenia
- asthma-related death
- AV block
- blurred vision
- bradycardia
- bronchospasm
- bundle-branch block
- confusion
- cough
- depression
- diabetes mellitus
- diaphoresis
- diarrhea
- dizziness
- drowsiness
- dyskinesia
- dyspnea
- edema
- elevated hepatic enzymes
- emotional lability
- erythema
- erythema multiforme
- exfoliative dermatitis
- fatigue
- fever
- floppy iris syndrome
- GI bleeding
- glycosuria
- gout
- headache
- heart failure
- hematuria
- hyperbilirubinemia
- hypercholesterolemia
- hyperglycemia
- hyperhidrosis
- hyperkalemia
- hypertension
- hypertriglyceridemia
- hyperuricemia
- hypervolemia
- hypoesthesia
- hypoglycemia
- hypokalemia
- hyponatremia
- hypoprothrombinemia
- hypotension
- hypotonia
- hypovolemia
- impaired cognition
- impotence (erectile dysfunction)
- increased urinary frequency
- insomnia
- jaundice
- leukopenia
- libido decrease
- maculopapular rash
- malaise
- melena
- migraine
- muscle cramps
- myocardial infarction
- nasal congestion
- nausea
- neuropathic pain
- nightmares
- orthostatic hypotension
- palpitations
- pancytopenia
- paresis
- paresthesias
- peripheral edema
- peripheral vasoconstriction
- pharyngitis
- photosensitivity
- pneumonitis
- proteinuria
- pruritus
- psoriaform rash
- pulmonary edema
- purpura
- rash
- sinus tachycardia
- Stevens-Johnson syndrome
- stroke
- syncope
- thrombocytopenia
- tinnitus
- toxic epidermal necrolysis
- tremor
- urinary incontinence
- urticaria
- vertigo
- visual impairment
- vomiting
- weakness
- weight gain
- weight loss
- wheezing
- withdrawal
- xerostomia
Monitoring Parameters
- blood pressure
- heart rate
Contraindications
- abrupt discontinuation
- acute bronchospasm
- acute heart failure
- asthma
- AV block
- beta-blocker hypersensitivity
- bradycardia
- breast-feeding
- bronchitis
- cardiogenic shock
- cerebrovascular disease
- children
- chronic obstructive pulmonary disease (COPD)
- contact lenses
- depression
- diabetes mellitus
- driving or operating machinery
- emphysema
- geriatric
- hepatic disease
- history of angioedema
- hyperthyroidism
- hypoglycemia
- hypotension
- infants
- myasthenia gravis
- neonates
- orthostatic hypotension
- peripheral vascular disease
- pheochromocytoma
- pregnancy
- psoriasis
- pulmonary disease
- pulmonary edema
- renal disease
- renal failure
- renal impairment
- sick sinus syndrome
- surgery
- thyroid disease
- thyrotoxicosis
- vasospastic angina
- ventricular dysfunction
Interactions
- Abacavir; Dolutegravir; Lamivudine
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