CABERGOLINE

CABERGOLINE
(ka-ber'go-leen)
Dostinex
Classifications: ergot alkaloid; dopamine agonist;
Therapeutic: ergot alkaloid
; antiparkinson agent
Prototype: Ergotamine
Pregnancy Category: B

Availability

0.5 mg tablets

Action

Cabergoline is a synthetic ergot derivative, long-acting dopamine receptor agonist with a high affinity for D2 receptors in the anterior pituitary, suppresses prolactin secretion.

Therapeutic Effect

Cabergoline inhibits both puerperal lactation and pathologic hyperprolactinemia.

Uses

Treatment of hyperprolactinemia (idiopathic or secondary to pituitary adenomas).

Unlabeled Uses

Treatment of Parkinson's disease.

Contraindications

Uncontrolled hypertension and hypersensitivity to ergot derivatives; pregnancy-induced hypertension, preeclampsia, eclampsia, lactation.

Cautious Use

Hepatic function impairment; elderly, psychosis; pregnancy (category B). Safety and efficacy in pediatric patients are unknown.

Route & Dosage

Hyperprolactinemia
Adult: PO Start with 0.25 mg 2 times/wk, may increase by 0.25  mg 2 times/wk to a max of 1 mg 2 times/wk

Parkinson's Disease
Adult: PO Start with 0.5 mg q.d., may increase up to 2.5 mg q.d. (max: 5 mg/d)

Administration

Oral
  • Give on same days each week.

Adverse Effects (≥1%)

Body as a Whole: Asthenia, fatigue, hot flashes. CV: Postural hypotension. GI: Nausea, constipation, abdominal pain, dyspepsia, vomiting, dry mouth, diarrhea, flatulence. Endocrine: Breast pain, dysmenorrhea. CNS: Headache, dizziness, paresthesia, somnolence, depression, nervousness.

Interactions

Drug: Concurrent use with phenothiazines, butyrophenones, thioxanthines, and metoclopramide decreases therapeutic effects of both drugs.

Pharmacokinetics

Absorption: Rapidly absorbed GI tract, undergoes first-pass metabolism. Peak: 2–3 h. Distribution: 40–42% protein bound. Crosses placenta. Metabolism: Extensively metabolized. Elimination: Approximately 22% in urine, 60% in feces. Half-Life: 63–69 h.

Nursing Implications

Assessment & Drug Effects

  • Lab tests: Monitor serum prolactin levels to assess response to each dosing level.
  • Monitor for hypotension, especially when given with other drugs known to lower BP.

Patient & Family Education

  • Discontinue this drug once physician advises that serum prolactin level has been maintained for 6 mo.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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