carvedilol

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

• 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

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

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)

**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

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

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