No

Ergot Derivative

Treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas

B

Patients with uncontrolled hypertension or hypersensitivity to ergot derivatives

Initial doses >1 mg may cause orthostatic hypotension. Use caution when patients are receiving other medications which may reduce blood pressure. Not indicated for the inhibition or suppression of physiologic lactation since it has been associated with cases of hypertension, stroke, and seizures. Because cabergoline is extensively metabolized by the liver, careful monitoring in patients with hepatic impairment is warranted. Female patients should instruct the physician if they are pregnant, become pregnant, or intend to become pregnant. Should not be used in patients with pregnancy-induced hypertension unless benefit outweighs potential risk. Do not give to postpartum women who are breast-feeding or planning to breast-feed. In all patients, prolactin concentrations should be monitored monthly until normalized.

>10%:

Central nervous system: Headache (26%), dizziness (17%)

Gastrointestinal: Nausea (29%)

1% to 10%:

Body as whole: Asthenia (6%), fatigue (5%), syncope (1%), influenza-like symptoms (1%), malaise (1%), periorbital edema (1%), peripheral edema (1%)

Cardiovascular: Hot flashes (3%), hypotension (1%), dependent edema (1%), palpitations (1%)

Central nervous system: Vertigo (4%), depression (3%), somnolence (2%), anxiety (1%), insomnia (1%), impaired concentration (1%), nervousness (1%)

Dermatologic: Acne (1%), pruritus (1%)

Endocrine: Breast pain (2%), dysmenorrhea (1%)

Gastrointestinal: Constipation (7%), abdominal pain (5%), dyspepsia (5%), vomiting (4%), xerostomia (2%), diarrhea (2%), flatulence (2%), throat irritation (1%), toothache (1%), anorexia (1%)

Neuromuscular & skeletal: Pain (2%), arthralgia (1%), paresthesias (2%)

Ocular: Abnormal vision (1%)

Respiratory: Rhinitis (1%)

An overdose may produce nasal congestion, syncope, hallucinations, or hypotension

Measures to support blood pressure should be taken if necessary

Additive hypotensive effects may occur when cabergoline is administered with antihypertensive medications; dosage adjustment of the antihypertensive medication may be required

Decreased effect: Dopamine antagonists (eg, phenothiazines, butyrophenones, thioxanthenes, or metoclopramide) may reduce the therapeutic effects of cabergoline and should not be used concomitantly

Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D₂ receptors; prolactin secretion by the anterior pituitary is predominantly under hypothalamic inhibitory control exerted through the release of dopamine

Distribution: Extensive tissue distribution, particularly to the pituitary

Metabolism: Extensively metabolized by the liver; minimal cytochrome P-450 metabolism

Bioavailability: The absolute bioavailability of cabergoline is unknown

Protein binding: 40% to 42%

Half-life: 63-69 hours

Time to peak: 2-3 hours

Initial dose: Oral: 0.25 mg twice weekly; the dose may be increased by 0.25 mg twice weekly up to a maximum of 1 mg twice weekly according to the patient's serum prolactin level. Dosage increases should not occur more rapidly than every 4 weeks. Once a normal serum prolactin level is maintained for 6 months, the dose may be discontinued and prolactin levels monitored to determine if cabergoline is still required. The durability of efficacy beyond 24 months of therapy has not been established.

Dizziness is common; may cause depression

Antipsychotics may decrease the therapeutic effects of cabergoline; avoid combination

No information available to require special precautions

No effects or complications reported

Patient should be instructed to notify physician if she suspects she is pregnant, becomes pregnant, or intends to become pregnant during therapy with cabergoline. A pregnancy test should be done if there is any suspicion of pregnancy and continuation of treatment should be discussed with physician.

Tablet: 0.5 mg

"European Multicentre Study Group for Cabergoline in Lactation Inhibition. Single Dose Cabergoline Versus Bromocriptine in Inhibition of Puerperal Lactation: Randomised, Doubleblind, Multicentre Study," Br Med J, 1991, 302:136771.

Ferrari C, Paracchi A, Mattei AM, et al, "Cabergoline in the Long-Term Therapy of Hyperprolactinemic Disorders," Acta Endocrinol, 1992, 126:489-94.

Giusti M, Porcella E, Carraro A, et al, "A Cross-Over Study With the Two Novel Dopaminergic Drugs Cabergoline and Quinagolide in Hyperprolactinemic Patients," J Endocrinol Invest, 1994, 17:51-7.

Rains CP, Bryson HM, and Fitton A, "Cabergoline: A Review of Its Pharmacological Properties and Therapeutic Potential in the Treatment of Hyperprolactinemia and Inhibition of Lactation," Drugs, 1995, 49:255-79.

Webster J, Piscitelli G, Polli A, et al, "A Comparison of Cabergoline and Bromocriptine in the Treatment of Hyperprolactinemic Amenorrhea," N Engl J Med, 1994, 331:904-9.

Webster J, Piscitelli G, Polli A, et al, "Dose-Dependent Suppression of Serum Prolactin by Cabergoline in Hyperprolactinaemia: A Placebo Controlled, Double Blind, Multicentre Study," Clin Endocrinol, 1992, 68:1201-6.

Webster J, Piscitelli G, Polli A, et al, "The Efficacy and Tolerability of Long-Term Cabergoline Therapy in Hyperprolactinaemic Disorders: An Open, Uncontrolled, Multicentre Study," Clin Endocrinol, 1993, 39:323-9.