Generic Name: Carvedilol.

Trade Name    : Carvedilol/Coreg.

Drug Class      : Mixed Adrenoceptor Antagonist.

Forms of Drug

  1. Capsule, Extended Release: 10mg – 20mg – 40mg – 80mg.
  2. Tablet: 3.125mg – 6.25mg – 12.5mg – 25mg.

Mechanism of Action

Carvedilol exerts its therapeutic effects through its unique mechanism of action, which involves both non-selective beta-blocking activity and alpha1-blocking activity. This dual action sets it apart from other beta-blockers and contributes to its efficacy in managing various cardiovascular conditions.

  1. Beta-Blocking Activity: Carvedilol blocks beta-adrenergic receptors, specifically the beta-1 receptors found primarily in the heart and the beta-2 receptors found in the lungs and peripheral blood vessels. By inhibiting these receptors, Carvedilol reduces the effects of norepinephrine and epinephrine (stress hormones) on the heart, resulting in the following effects:
  2. Reduced Heart Rate: Carvedilol decreases the heart rate by slowing down the electrical conduction through the sinoatrial (SA) node, which regulates the heart’s rhythm.
  3. Decreased Contractility: Carvedilol decreases the force of contraction of the heart muscle, reducing its oxygen demands and workload.
  4. Lowered Blood Pressure: By blocking beta-1 receptors in the blood vessels, Carvedilol reduces peripheral vascular resistance, leading to a decrease in blood pressure.
  5. Alpha1-Blocking Activity: Carvedilol also blocks alpha1-adrenergic receptors, which are primarily found in peripheral blood vessels. This action causes the blood vessels to relax and dilate, further contributing to the antihypertensive effects of Carvedilol. The alpha1-blocking activity helps to counteract the vasoconstrictive effects of norepinephrine, thereby reducing peripheral vascular resistance and improving blood flow.

Indications

  1. Hypertension
  2. Heart failure
  3. Left ventricular dysfunction after myocardial infarction
  4. Heart rhythm disorders

Contraindications

  1. Hypersensitivity.
  2. Bronchial asthma or chronic obstructive pulmonary disease (COPD).
  3. Cardiogenic shock.
  4. Severe bradycardia or heart block.
  5. Liver dysfunction.
  6. Pregnancy and breastfeeding.

Side Effects

  1. Dizziness (2-32%).
  2. Fatigue (4-24%).
  3. Hypotension (9-20%).
  4. Weight gain (10-12%).
  5. Hyperglycemia (5-12%).
  6. Diarrhea (1-12%).
  7. Bradycardia (2-10%).
  8. Nausea (2-9%).
  9. Cough (5-8%).
  10. Headache (5-8%).
  11. Atrioventricular block, edema (1-7%).
  12. Angina (1-6%).
  13. Hpercholesterolemia (1-4%).
  14. Hypertriglyceredemia (1%).
  15. Vomiting (1-6%).
  16. Dyspnea (>3%).
  17. Syncope (3%).
  18. Rhinitis (2%).

Drug Interaction

Other drugs that can interact with it.

  1. Beta-blockers and calcium channel blockers.
  2. Digoxin.
  3. Insulin and oral antidiabetic agents.
  4. CYP2D6 inhibitors, such as certain antidepressants (e.g., fluoxetine, paroxetine) or antipsychotics (e.g., thioridazine).
  5. Alpha-blockers and vasodilators.
  6. NSAIDs, such as ibuprofen or naproxen.

Precautions

  1. Pregnancy: Category C.
  2. Lactation: Carvedilol is known to be excreted into breast milk. Therefore, caution should be exercised when considering the use of Carvedilol during lactation.

Leave a Reply

Your email address will not be published. Required fields are marked *