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.
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.
Description: Mechanism of Action: 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
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)
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.
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