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Cabergoline information from DrugsUpdate  

See Available Brands of Cabergoline in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Cabergoline (brand names Dostinex and Cabaser), an ergot derivative, is a potent dopamine receptor agonist on D2 receptors. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It is frequently used as a second-line agent in the management of prolactinomas when bromocriptine is ineffective.

Pharmacodynamics

Dose response with inhibition of plasma prolactin, onset of maximal effect, and duration of effect has been documented following single Cabergoline doses to healthy volunteers (0.05 to 1.5 mg) and hyperprolactinemic patients (0.3 to 1 mg). In volunteers, prolactin inhibition was evident at doses >0.2 mg, while doses ≥0.5 mg caused maximal suppression in most subjects. Higher doses produce prolactin suppression in a greater proportion of subjects and with an earlier onset and longer duration of action. In 12 healthy volunteers, 0.5, 1, and 1.5 mg doses resulted in complete prolactin inhibition, with a maximum effect within 3 hours in 92% to 100% of subjects after the 1 and 1.5 mg doses compared with 50% of subjects after the 0.5 mg dose. In hyperprolactinemic patients (N=51), the maximal prolactin decrease after a 0.6 mg single dose of Cabergoline was comparable to 2.5 mg bromocriptine; however, the duration of effect was markedly longer (14 days vs. 24 hours). The time to maximal effect was shorter for bromocriptine than Cabergoline (6 hours vs. 48 hours). In 72 healthy volunteers, single or multiple doses (up to 2 mg) of Cabergoline resulted in selective inhibition of prolactin with no apparent effect on other anterior pituitary hormones (GH, FSH, LH, ACTH, and TSH) or cortisol.

Pharmacokinetics

Cabergoline is a long-acting dopamine D2-agonist. It inhibits prolactin secretion through hypothalamic inhibitory control exerted through the release of dopamine.


Absorption Absorbed from the GI tract. Undergoes 1st pass effect.


Distribution Plasma protein binding: about 40%.


Metabolism Extensively metabolised to inactive metabolites. Excretion Mainly via faeces.

Cabergoline Indications / Cabergoline Uses

Information Not Available

Cabergoline Adverse Reactions / Cabergoline Side Effects

Decrease in BP, dizziness, vertigo, headache, nausea, sleeplessness, abdominal pain, dyspepsia, gastritis, weakness, fatigue, constipation, vomiting, breast pain, hot flushes, depression, tingling, leg cramps, Raynaud's syndrome, psychosis with hallucinations, delusions and confusion. Potentially Fatal: Risk of serotinin syndrome with sibutramine; avoid combination.

Precautions

General Initial doses higher than 1.0 mg may produce orthostatic hypotension. Care should be exercised when administering Cabergoline with other medications known to lower blood pressure.


Postpartum Lactation Inhibition or Suppression Cabergoline is not indicated for the inhibition or suppression of physiologic lactation. Use of bromocriptine, another dopamine agonist for this purpose, has been associated with cases of hypertension, stroke, and seizures.


Hepatic Impairment Since Cabergoline is extensively metabolized by the liver, caution should be used, and careful monitoring exercised, when administering Cabergoline to patients with hepatic impairment. Fibrosis As with other ergot derivatives, pleural effusion or pulmonary fibrosis have been reported following long-term administration of Cabergoline. Some reports were in patients previously treated with ergotinic dopamine agonists. Cabergoline should not be used in patients with a history of, or current signs and or clinical symptoms of, respiratory or cardiac disorders linked to fibrotic tissue. Following diagnosis of pleural effusion or pulmonary fibrosis, the discontinuance of Cabergoline has been reported to result in improvement of signs and symptoms. Erythrocyte sedimentation rate (ESR) has been found to be abnormally increased in association with pleural effusion/fibrosis. Chest x-ray examination is recommended in cases of unexplained ESR increases to abnormal values. Serum creatinine measurements can also be used to help in the diagnosis of fibrotic disorder. Psychiatric Pathological gambling, increased libido, and hypersexuality have been reported in patients treated with dopamine agonists including Cabergoline. This has been generally reversible upon reduction of the dose or treatment discontinuation.


Information for Patients Patients should be instructed to notify their physician if they suspect they are pregnant, become pregnant, or intend to become pregnant during therapy. A pregnancy test should be done if there is any suspicion of pregnancy and continuation of treatment should be discussed with their physician. Patients should notify their physician if they develop shortness of breath, persistent cough, difficulty with breathing when lying down, or swelling in their extremities.


Overdosage Symptoms may include nasal congestion, syncope or hallucinations. Measures to support BP should be taken if necessary.

Special Precautions

CV disease, Raynaud's syndrome, renal or hepatic impairment, peptic ulcer, GI bleeding, history of psychosis, hypertension. May affect ability to drive or operate machinery. Pregnancy, lactation. Prolonged use and/or usage of high doses may lead to psychiatric disorders, pleural/retroperitoneal fibrosis or cardiac valvular fibrosis. Monitor serum prolactin level mthly until normalisation. Monitor hepatic function regularly in patients with hepatic impairment.

Other Drug Interactions

ncreased risk of orthostatic hypotension when used with antihypertensives. May increase vasoconstriction effect of dopamine. May reduce vasodilation effect of nitroglycerin. Concurrent use with SSRIs or TCAs may increase the risk of serotonin syndrome. Potentially Fatal: Risk of serotonin syndrome with sibutramine.

Other Interactions

Information Not Available

Dosage

Oral Inhibition of physiological lactation Adult: 1 mg as a single dose on the 1st day postpartum. Hepatic impairment: Dosage adjustments may be needed.


Oral Suppression of lactation Adult: 250 mcg every 12 hr for 2 days. Hepatic impairment: Dosage adjustments may be needed.


Oral Hyperprolactinemia-associated disorders Adult: Initially, 500 mcg/wk then increased at mthly intervals by 500 mcg/wk according to response. Wkly dose may be admin on a single occasion or in 2 divided doses on separate days; doses >1 mg should be given as divided doses. Usual dose: 1 mg (up to 4.5 mg)/wk. Hepatic impairment: Dosage adjustments may be needed.


Oral Adjunct to levodopa treatment in Parkinson's disease Adult: Initially, 0.5 mg daily in monotherapy and 1 mg daily as adjunct, may increase in increments of 0.5-1 mg at 7- or 14-day intervals. Max: 3 mg daily. Elderly: Start with lower doses. Hepatic impairment: Dosage adjustments may be needed.


Oral As monotherapy in Parkinson's disease Oral: Store at 20-25?C. Adult: Initially, 0.5 mg daily in monotherapy and 1 mg daily as adjunct, may increase in increments of 0.5-1 mg at 7- or 14-day intervals. Max: 3 mg daily. Elderly: Start with lower doses. Hepatic impairment: Dosage adjustments may be needed.

Food(before/after)

Should be taken with food

List of Contraindications

Cabergoline and Pregnancy

Caution when used during pregnancy

Cabergoline and Lactation

Caution when used during lactation

Cabergoline and Children

Studies of this medicine have been done only in adult patients, and there is no specific information comparing use of cabergoline in children with use in other age groups

Cabergoline and Geriatic

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults or if they cause different side effects or problems in older people. There is no specific information comparing use of cabergoline in the elderly with use in other age groups.

Cabergoline and Other Contraindications

Hypersensitivity to ergot derivatives. Uncontrolled hypertension

Storage

Oral: Store at 20-25 ℃

Lab interference

Oral: Store at 20-25 ℃

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