Carvedilol

Products

Carvedilol is commercially available in tablet form (Dilatrend, generic). It has been approved in many countries since 1995. Carvedilol is also combined with ivabradine fixed (Carivalan).

Structure and properties

Carvedilol (C₂₄H₂₆N₂O₄, M_r = 406.5 g/mol) is a racemate, with both enantiomers participating in the pharmacological effects. It exists as a white crystalline powder that is practically insoluble in water.

Effects

Carvedilol (ATC C07AG02) has antihypertensive, antiarrhythmic, antianginal, organoprotective, and antioxidant properties. The effects are due to antagonism at alpha- and beta-adrenoceptors (α1, β1, and β2). Carvedilol is a nonselective beta-blocker with no intrinsic sympathomimetic activity and with membrane-stabilizing activity.

Indications

• Mild to moderate essential hypertension (high blood pressure).
• Seizure prophylaxis in chronic angina.
• Mild to severe stable heart failure.

Dosage

According to the drug label. The tablets are taken once or twice a day, regardless of meals. In heart failure, the tablets should be taken with food.

Contraindications

For complete precautions, see the drug label.

Interactions

Carvediolo is a substrate of CYP450 isoenzymes (mainly CYP2D6, CYP2C9) as well as a substrate as well as an inhibitor of P-glycoprotein.

Adverse effects

The most common potential adverse effects include fatigue, dizziness, headache, and low blood pressure.