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Carvedilol; Uses, Dosage, Side Effects, Interactions, Pregnancy

Carvedilol is a synthetic antihypertensive methoxyphenoxy- 2-propanol derivative with no intrinsic sympathomimetic activity, Carvedilol acts as a nonselective beta-adrenoceptor blocking agent (S(-) enantiomer) and as an alpha 1-adrenoceptor blocker (R(+) and S(-) enantiomers). Its acts more strongly on beta-receptors than on alpha 1-receptors, reduces peripheral vascular resistance by vasodilation, and prevents reflex tachycardia (beta-blockade) so that heart rate is either unchanged or decreased. Carvedilol also reduces renin release through beta-blockade.

Carvedilol is only found in individuals that have used or taken this drug. It is a non-selective beta blocker indicated in the treatment of mild to moderate congestive heart failure (CHF). Carvedilol is a racemic mixture in which nonselective beta-adrenoreceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol’s beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Carvedilol also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Carvedilol and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca 2+ in OH - free radical-treated myocardium. Carvedilol and its metabolites also prevent OH - radical-induced decrease in sarcoplasmic reticulum Ca 2+ -ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by preventing free radical damage.

Mechanism of action of Carvedilol

Carvedilol is a racemic mixture in which nonselective beta-adrenoreceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol’s beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Carvedilol also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Carvedilol and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca²⁺ in OH^– free radical-treated myocardium. Carvedilol and its metabolites also prevent OH^– radical-induced decrease in sarcoplasmic reticulum Ca²⁺-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by preventing free radical damage.

Carvedilol is a nonselective beta-adrenergic blocking agent with selective alpha1-adrenergic blocking activity. The principal physiologic action of carvedilol is to competitively block adrenergic stimulation of beta-receptors within the myocardium (beta1-receptors) and within bronchial and vascular smooth muscle (beta2-receptors), and to a lesser extent alpha1-receptors within vascular smooth muscle. The beta1-antagonist activity of carvedilol is similar to that of propranolol and greater than that of labetalol, and the duration of carvedilol’s effect is longer than those of labetalol and propranolol.

Indications of Carvedilol

High Blood Pressure
Left Ventricular Dysfunction
Atrial Fibrillation
Heart Failure
Chronic Stable Angina Pectoris
High Blood Pressure (Hypertension)
LVEF ≤40% Left ventricular dysfunction
NYHA Class I or II heart failure
Nonvalvular Atrial Fibrillation
Chronic heart failure with reduced ejection fraction (NYHA Class III)
Chronic heart failure with reduced ejection fraction (NYHA Class IV)
Treatment of essential hypertension in adults.
Reduction of cardiovascular morbidity in adults with
Manifest atherothrombotic cardiovascular disease (history of coronary heart disease, stroke, or peripheral arterial disease)
Cardiovascular Risk Reduction
Prevention of Cardiovascular Disease

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Contra Indications of Carvedilol

Hypersensitivity to the carvedilol or to any of the excipients of Carvedilol
Heart failure belonging to NYHA Class IV of the heart failure classification with marked fluid retention or overload requiring intravenous inotropic treatment.
Chronic obstructive pulmonary disease with bronchial obstruction
Clinically significant hepatic dysfunction.
Bronchial asthma.
AV block, degree II or III (unless a permanent pacemaker is in place).
Severe bradycardia (<50 bpm).
Sick sinus syndrome (incl. sino-atrial block).
Cardiogenic shock.
Severe hypotension (systolic blood pressure below 85 mmHg).
Prinzmetal’s angina.
Untreated phaeochromocytoma.
Metabolic acidosis.
Severe peripheral arterial circulatory disturbances.
Concomitant intravenous treatment with verapamil or diltiazem

Dosage of Carvedilol

Strenghts : 3.125 mg; 6.25 mg; 12.5 mg; 25 mg; 10 mg; 20 mg; 40 mg; 80 mg;

High Blood Pressure

Initial dose: 6.25 mg orally twice a day (if this dose is tolerated, using standing systolic pressure measured about 1 hour after dosing as a guide) maintain for 7 to 14 days
Titration: Increase to 12.5 mg orally twice a day if needed for 10 to 14 days, then to 25 mg orally twice a day if needed
Maximum dose: 50 mg orally twice a day

Extended-release capsules

Initial dose: 20 mg orally once a day (if this dose is tolerated, using standing systolic pressure measured about 1 hour after dosing as a guide) maintain for 7 to 14 days
Titration: If tolerated, increase dose to 40 mg orally once a day for 7 to 14 days, then to 80 mg orally once a day if needed
Maximum dose: 80 mg orally once a day

For heart failure

For oral dosage form (extended-release capsules)

Adults—At first, 10 milligrams (mg) once a day for at least two weeks. Your doctor may adjust your dose as needed. However, the dose is usually not more than 80 mg once a day.
Children—Use and dose must be determined by your doctor.

For hypertension

Adults—At first, 20 milligrams (mg) once a day for 7 to 14 days. Your doctor may adjust your dose as needed. However, the dose is usually not more than 80 mg once a day.
Children—Use and dose must be determined by your doctor.

For left ventricular dysfunction after a heart attack

Adults—At first, 20 milligrams (mg) once a day for 3 to 10 days. Your doctor may adjust your dose as needed. However, the dose is usually not more than 80 mg once a day
Children—Use and dose must be determined by your doctor.

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For congestive heart failure

Adults—At first, 3.125 milligrams (mg) two times a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 25 or 50 mg two times a day.
Children—Use and dose must be determined by your doctor.

For high blood pressure (hypertension)

Adults—At first, 6.25 milligrams (mg) two times a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 25 mg two times a day.
Children—Use and dose must be determined by your doctor.

For left ventricular dysfunction after a heart attack

Adults—At first, 6.25 milligrams (mg) two times a day. Some patients may start at 3.125 mg two times a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 25 mg two times a day.
Children—Use and dose must be determined by your doctor.

Side Effects of Carvedilol

The most common

Common

chills or fever
headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in chest
excessive sweating
sudden drowsiness or need to sleep
coughing up blood
liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
decreased amount of urine

Rare

Anxiety
change in vision
chest pain or tightness
confusion
cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
hallucinations
headache
irritability
lightheadedness
cold and clammy skin
fast and shallow breathing
swelling of your feet, legs, or hands purple spot on your skin caused by internal bleeding
fast or abnormal heart rate or palpitations
loss of appetite
lower back, side, or stomach pain
mental depression
muscle pain or cramps

Drugs interactions of Carvedilol

Carvedilol may interact with following drugs, supplements, & may change the efficacy of drugs

antidiabetes medications (e.g., insulin, metformin, gliclazide)
beta-2 agonists (e.g., formoterol, salmeterol, salbutamol)
bosutinib
bupropion
calcium channel blocking agents (e.g., diltiazem, verapamil)
cimetidine
cyclosporine
fluoxetine
MAO inhibitors (e.g., phenelzine, tranylcypromine)
medications that affect heart rhythm
medications that lower blood pressure
nitroglycerin
paroxetine
rituximab
tricyclic antidepressants (e.g., amitriptyline, nortriptyline)

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Pregnancy & Lactation of Carvedilol

FDA Pregnancy Category C

Pregnancy

The medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if carvedilol passes into human breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.

Children

The safety and effectiveness of using this medication have not been established for children.