cabergoline, Dostinex

 Indications

Treatment of hyperprolactinemia (idiopathic or pituitary

in origin).

Action

Inhibits secretion of prolactin by acting as a dopamine

agonist. Therapeutic Effects: Decreased secretion

of prolactin in hyperprolactinemia.

Pharmacokinetics

Absorption: Well absorbed but undergoes extensive

first-pass hepatic metabolism.

Distribution: Widely distributed; concentrates in pituitary.

Metabolism and Excretion: Extensively metabolized

by the liver; 4% excreted unchanged in urine.

Protein Binding: 40–42%.

Half-life: 63–69 hr.

TIME/ACTION PROFILE (effect on serum

prolactin levels)

ROUTE ONSET PEAK DURATION

PO unknown 2–3 hr unknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity to cabergoline

or ergot alkaloids; Uncontrolled hypertension; History

of pulmonary, pericardial, or retroperitoneal fibrotic

disorders; History of cardiac valvular disease; Lactation:

Has been associated with hypertension, stroke, and seizures.

Not to be used for suppression of physiologic

lactation.

Use Cautiously in: Hepatic impairment; Patients

who have received medications associated with valvular

disorders; OB: Use only if clearly needed; Pedi: Safety

not established.

Adverse Reactions/Side Effects

CNS: dizziness, headache, depression, drowsiness, fatigue,

impulse control disorders (gambling, sexual),

nervousness, vertigo, weakness. Resp: PULMONARY FIBROSIS,

pleural effusion. EENT: abnormal vision. CV:

PERICARDIAL FIBROSIS, VALVULAR DISORDERS, postural hypotension,

hot flashes. GI: RETROPERITONEAL FIBROSIS,

constipation, nausea, abdominal pain, dyspepsia, vomiting.

GU: dysmenorrhea. Endo: breast pain. Neuro:

paresthesia.

Interactions

Drug-Drug:qrisk of hypotension with antihypertensives.

Mayqthe effects of SSRIs and other

serotonin agonists (induces serotonin syndrome).

Effectiveness may bepby phenothiazines, butyrophenones

(haloperidol), thioxanthenes, or metoclopramide

(avoid concurrent use).

Route/Dosage

PO (Adults): 0.25 mg twice weekly; may beqat 4-wk

intervals up to 1 mg twice weekly.

Availability (generic available)

Tablets: 0.5 mg.