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carvedilol
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carvedilol

Non-selective beta blocker with alpha blockade – especially effective in heart failure.

Prescription required
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What is carvedilol?

Carvedilol is a third-generation beta blocker with a unique profile: it not only blocks beta-1 and beta-2 receptors, but also alpha-1 receptors. This triple block leads to a particularly effective reduction in blood pressure and a relief of the heart.

Carvedilol is particularly well studied in chronic heart failure and in large studies (COPERNICUS, COMET) has reduced mortality in heart failure. It is used in high blood pressure, chronic heart failure and coronary heart disease.

Carvedilol must be taken twice a day due to the additional alpha blockade. Available preparations include Carvedilol-ratiopharm® and Dilatrend®.

Active Ingredients & Mechanism of Action

Active ingredient: Carvedilol

Carvedilol has a threefold mechanism of action:

Beta-1 blockade (in the heart):

  • Lowers heart rate and impact strength
  • Reduces oxygen consumption
  • Inhibits renin release

Beta-2 blockade (on lungs and vessels):

  • Non cardioelective
  • Cave: Bronchospasmus at Asthma possible

Alpha-1 blockade (on the vessels):

  • Extends peripheral blood vessels
  • Lowers the vascular resistance
  • Reduces the back load of the heart
  • Improves blood circulation

Additional properties:

  • Antioxidant action
  • Stabilization of cell membranes
  • No negative influence on insulin sensitivity
  • Cheap effects on fat metabolism

Initiation of action: Maximum blood pressure reduction after 1-2 hours. Stable setting after 1-2 weeks.

Who is it suitable for?

Carvedilol is suitable for:

  • Adults with high blood pressure
  • Chronic stable heart failure (NYHA II-IV)
  • Chronic stable angina pectoris

Especially recommended at:

  • Heart failure (strong study documents)
  • High blood pressure with increased peripheral resistance
  • Patients after heart attack
  • Liver cirrhosis with portal hypertension (off-label)

Not suitable:

  • Heavy asthma bronchiale (not cardioselective!)
  • AV block II/III. Grades
  • Heavy bradycardia
  • Decompensated heart failure
  • Heavy liver failure
  • Cardiogenic shock

Available Dosages

High blood pressure:

  • start dose: 12.5 mg once a day (1 and 2 days)
  • Then 25 mg once or twice a day
  • Maximum dose: 50 mg daily (divided)

Sufficiency:

  • start dose: 3,125 mg twice a day
  • Increase every 2 weeks: 6.25 mg → 12.5 mg → 25 mg (each 2x)
  • Target dose: 25 mg twice a day (up to 85 kg) or 50 mg twice a day (over 85 kg)

Angina pectoris:

  • start dose: 12.5 mg twice a day
  • After 2 days: 25 mg twice a day

Available starches:

  • 3.125 mg, 6.25 mg, 12.5 mg, 25 mg tablets

How to Take

Intake:

  • twice a day (morning and evening)
  • Take meals (better compatibility, slower intake)
  • With sufficient water
  • Patients with heart failure: slowly rise (orthostatic hypotension)

For heart failure:

  • Very slow dose increase (all 2 weeks)
  • Start with stable heart failure
  • Medical supervision
  • In case of deterioration: reduce dose

Important notes:

  • Do not drop abruptly
  • Regular blood pressure, pulse and weight controls
  • Asthmatiker: Carvedilol is not suitable (not cardioselective)

Contraindications

**Carvedilol must not be taken at:* *

  • hypersensitivity to carvedilol
  • Decompensated heart failure (i.v. therapy necessary)
  • Heavy liver failure
  • AV-Block II./III. Grades (without pacemaker)
  • Heavy bradycardia (under 50/min)
  • Sick sine syndrome
  • Cardiogenic shock
  • Heavy hypotension (under 85 mmHg systolic)
  • Asthma bronchiale or heavy COPD
  • Untreated phenochromocytoma

Preview at:

  • Diabetes mellitus (can mask hypoglycemia symptoms)
  • Peripheral blood circulation disorders
  • Prince metal angina
  • Contact lens support (reduced tear fluid)
  • Psoriasis

pregnant: Contraindicated. Betablockers can lead to growth delay and bradycardia in newborns.

Possible Side Effects

Very common (over 10%):

  • Squeeze
  • Headaches
  • fatigue (especially at the beginning)

Acid (1-10%):

  • Bradykardie
  • Orthostatic hypotension (especially in heart failure)
  • Edema
  • Weight gain
  • Gastrointestinal complaints
  • visual disorders
  • Reduced tear fluid

** Occasionally (0,1-1%):* *

  • Depressive detunement
  • Sleep disorders
  • Potency disorders
  • Skin rash
  • Breath, bronchospasmus
  • Blocking

Selten:

  • Heavy allergic reactions
  • Deterioration of kidney function
  • thrombocytopenia
  • Reinforcement of Psoriasis

** Orthostatic dizziness occurs especially at the start of therapy and dose increase. Slow up is recommended.

Interactions

Contraint with:

  • MAO inhibitors (except MAO-B inhibitors)

Preview at:

  • Digoxin → increased digoxin level
  • Insulin and Antidiabetics → Hypoglycemia masking and strengthening
  • Rifampicin → reduced carvedilol mirror
  • Cyclosporin → increased cyclosporin levels
  • Clonidine → Rebound effect with simultaneous settling
  • Narcotics → increased hypotension and bradycardia
  • CYP2D6 inhibitors (fluoroxetin, paroxetin) → increased carvedilol levels

Important: Carvedilol is metabolized via CYP2D6 and CYP2C9. These enzymes can intensify the action of carvedilol.

Frequently Asked Questions

Similar Medications

Is carvedilol right for you?

A licensed doctor will review your information and issue a prescription if suitable. Discreet and secure.

Important Notice

This information does not replace medical advice. If you have questions about your health or the suitability of this medication, please consult a doctor or pharmacist.

Important Safety Information

This service operates under German pharmaceutical law (HWG). For risks and side effects, read the package leaflet and consult your doctor or pharmacist. All medications are dispensed from a licensed pharmacy in Germany.