Cabergoline


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Inhibition of physiological lactation 1 mg as a single dose on 1st day postpartum. Lactation suppression 250 mcg 12 hrly for 2 days. Hyperprolactinaemia-associated disorders Initial: 0.5 mg/wk, gradually increase by 0.5 mg/wk at mthly interval until optimal response. Monotherapy or adjunct therapy in Parkinsons's disease Initial: 1 mg/day, gradually increase by 0.5-1 mg at 1 or 2 wk interval. Recommended dose: 2-3 mg/day.
Dosage Details
Oral
Adjunct to levodopa treatment in Parkinson's disease, Monotherapy in Parkinson's disease
Adult: Initially, 1 mg daily, gradually increase by 0.5-1 mg at 1 or 2 wk interval until optimal response. Recommended dose: 2-3 mg daily.

Oral
Inhibition of physiological lactation
Adult: 1 mg as a single dose on the 1st day postpartum.

Oral
Hyperprolactinaemia-associated disorders
Adult: Initially, 0.5 mg wkly, increase gradually, preferably in increments of 0.5 mg wkly at mthly intervals until optimal response. Wkly dose may be given in 1 or 2 divided doses on separate days. Usual dose: 1 mg wkly (range: 0.25-2 mg, up to 4.5 mg wkly).

Oral
Suppression of lactation
Adult: 250 mcg 12 hrly for 2 days.
Administration
Should be taken with food.
Contraindications
Uncontrolled HTN; history of pulmonary, pericardial, and retroperitoneal fibrotic disorders; cardiac valvular disorders. Toxaemia of pregnancy, history of puerperal psychosis. Concomitant use w/ dopamine antagonists.
Special Precautions
Patients w/ severe CV disease, Raynaud’s syndrome, peptic ulcer, GI bleeding. Renal or hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Abdominal pain, angina, breast pain, confusion, constipation, depression, dyspepsia, epigastric pain, gastritis, hallucinations, headache, nausea, syncope, postural hypotension, somnolence, allergic skin reactions, alopecia, cardiac valvulopathy, constrictive pericarditis, drowsiness, dyskinesia, erythromelalgia, hypersexuality, hypotension, increased libido, leg cramps, pericardial effusion, pathological gambling, peripheral oedema, pleural effusion/fibrosis, pleuritis, pulmonary/retroperitoneal fibrosis. Rarely, digital vasospasm, epistaxis, hot flushes, muscle weakness, palpitation, paraesthesia, transient hemianopia, vomiting.
Patient Counseling Information
May impair ability to drive or operate machinery.
MonitoringParameters
Monitor BP; serum prolactin level (mthly until normalised); echocardiogram (at baseline and 6-12 mthly); ESR, chest X-ray, and serum creatinine level; signs and symptoms of pleuropulmonary disease, ureteral/abdominal vascular obstruction. Perform pregnancy test prior to initiation of therapy.
Overdosage
Symptoms: Nausea, vomiting, gastric complaints, postural hypotension, confusion/psychosis or hallucinations. Management: Supportive treatment. Admin of dopamine antagonist may be advisable.
Drug Interactions
Increased risk of orthostatic hypotension when used w/ antihypertensives. Additive therapeutic effect w/ levodopa. Increased systemic bioavailability w/ macrolide antibiotics (e.g. erythromycin).
Potentially Fatal: Diminished therapeutic effect w/ dopamine antagonist (e.g. phenothiazines, butyrophenones, thioxanthines, metoclopramide).
Action
Description: Cabergoline is a long-acting dopamine D2-agonist. It inhibits prolactin secretion through hypothalamic inhibitory control exerted through the release of dopamine.
Duration: Prolactin-lowering effect: 14 days.
Pharmacokinetics:
Absorption: Absorbed from the GI tract. Time to peak plasma concentration: 2-3 hr.
Distribution: Extensively distributed throughout the body. Crosses the placenta and enters breast milk. Plasma protein binding: 40-42%.
Metabolism: Metabolised in the liver via hydrolysis of the acylurea bond (w/ minimal CYP involvement). Undergoes first-pass metabolism.
Excretion: Via faeces (approx 60%) and urine (approx 22%; <4% as unchanged drug). Elimination half-life: 63-69 hr.
Chemical Structure

Chemical Structure Image
Cabergoline

Source: National Center for Biotechnology Information. PubChem Database. Cabergoline, CID=54746, https://pubchem.ncbi.nlm.nih.gov/compound/Cabergoline (accessed on Jan. 21, 2020)

Storage
Store between 20-25°C.
ATC Classification
N04BC06 - cabergoline ; Belongs to the class of dopamine agonist. Used in the management of Parkinson's disease.
G02CB03 - cabergoline ; Belongs to the class of prolactine inhibitors. Used to suppress lactation.
References
Anon. Cabergoline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/10/2016.

Buckingham R (ed). Cabergoline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/10/2016.

Cabergoline Tablet (Greenstone LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/10/2016.

Joint Formulary Committee. Cabergoline. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/10/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Cabergoline. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/10/2016.

Disclaimer: This information is independently developed by MIMS based on Cabergoline from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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