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Pronunciation:

(ca BER goe leen)

U.S. Brand Names:

Dostinex®

Generic Available:

Canadian Brand Names:

Dostinex®

Use:

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

Use - Unlabeled/Investigational:

Adjunct for the treatment of Parkinson's disease

Pregnancy Risk Factor:

Contraindications:

Hypersensitivity to cabergoline, any component of the formulation, or ergot derivatives; ergot alkaloids are contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics); uncontrolled hypertension

Warnings/Precautions:

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. Pleural and peritoneal fibrosis have been reported with prolonged daily use. Cardiac valvular fibrosis has also been associated with ergot alkaloids.

Adverse Reactions:

>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%), palpitation (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%), paresthesia (2%)

Ocular: Abnormal vision (1%)

Respiratory: Rhinitis (1%)

Overdosage/Toxicology:

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

Measures to support blood pressure should be taken if necessary

Drug Interactions:

Antipsychotics: May diminish the effects of cabergoline (due to dopamine antagonism); these combinations should generally be avoided.

Metoclopramide: May diminish the effects of cabergoline (due to dopamine antagonism); concurrent therapy should generally be avoided.

Serotonin agonists: Concurrent use with cabergoline may increase the risk of serotonin syndrome (includes buspirone, SSRIs, TCAs, nefazodone, sumatriptan, and trazodone).

Sibutramine: May cause serotonin syndrome; concurrent use with ergot alkaloids is contraindicated.

Mechanism of Action:

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

Pharmacodynamics/Kinetics:

Distribution: Extensive, particularly to the pituitary

Protein binding: 40% to 42%

Metabolism: Extensively hepatic; minimal CYP

Half-life elimination: 63-69 hours

Time to peak: 2-3 hours

Dosage:

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.

Elderly: No dosage recommendations suggested, but start at the low end of the dosage range

Patient Education:

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.

Additional Information:

Bromocriptine and cabergoline are the only drugs indicated for the treatment of hyperprolactinemia. In the largest comparative clinical trial, prolactin levels normalized in 77% of patients treated with cabergoline compared to 59% of patients treated with bromocriptine. In that trial, 3% of patients discontinued treatment due to adverse effects in the cabergoline group versus 12% of patients in the bromocriptine group. In addition to the improved safety and efficacy profile, cabergoline (administered twice weekly) is more convenient than bromocriptine (administered 1-3 times/day) for patients to take.

If the drug is used to prevent lactation, a single 1 mg dose is recommended on the first day after delivery. The drug is not approved for the inhibition of established lactation and should only be used to prevent lactation when there are medical reasons whereby which the potential benefits of therapy outweigh the risks, since it has been associated with cases of hypertension, stroke, and seizures.

Dental Health: Effects on Dental Treatment:

Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation), throat irritation, and toothache.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

Dizziness is common; may cause depression

Mental Health: Effects on Psychiatric Treatment:

Antipsychotics may decrease the therapeutic effects of cabergoline; avoid combination

Dosage Forms:

Tablet: 0.5 mg

International Brand Names:

Actualene® (IT); Cabaser® (AU, CH, DK, FI, GB, IE, IL, IT, NO, PL, SE, YU); Cabaseril® (AT, DE); Cabaseril Paranova® (DK); Cabergoline® (BE); Cabergoline-Pharmacia® (LU); Dostinex® (AR, AT, AU, BE, BG, CA, CH, CL, CO, CR, CZ, DE, DK, ES, FI, FR, GB, GT, HN, IE, IL, IT, LU, NL, NO, NZ, PA, PL, PT, RO, RU, SE, SG, SV, TR, YU); Lactamax® (AR); Sogilen® (ES); Sostilar® (BE); Triaspar® (AR)

References

"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.

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