Cabergoline

Trade names

• DOSTINEX

Actions

• Agonist of D2 dopamin receptors.

Route of Administration

Oral

Bioavailability

First-pass effect. Absolute bioavailability is not known

Plasma protein binding

40–42%

Half-life

63–69 hours

Metabolism

Hepatic

Elimination

Biliary 60%, renal 22%

Important side-effects

Cardiac Valvulopathy. All patients should undergo a cardiovascular evaluation, including echocardiogram to assess the potential presence of valvular disease. If valvular disease is detected, the patient should not be treated with cabergoline. Cabergoline should be discontinued if an echocardiogram reveals new valvular regurgitation, valvular restriction or valve leaflet thickening. The risk of developing valvular disease is dose dependent.

Extracardiac Fibrotic Reactions.

• Pleuro-pulmonary disease
• Renal insufficiency or ureteral/abdominal vascular obstruction.
• Pericardial fibrosis.

Nausea, vomiting.

Somnolence, depression.

Orthostatism.

Recommended dose

Start with 0.25 mg twice a week.

Increase by 0.25 mg twice weekly up to a maximum dosage of 1 mg twice a week at 4-week intervals.

Renal impairment

Limited data exist on the safety of cabergoline in patients with impaired renal function.

Hepatic impairment

Limited data exist on the safety of cabergoline in patients with impaired hepatic function.