Cabergoline

Oral
Adjunct to levodopa treatment in Parkinson's disease, Monotherapy in Parkinson's disease

Oral
Inhibition of physiological lactation

Oral
Hyperprolactinaemia-associated disorders

Oral
Suppression of lactation

Should be taken with food.

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.

Patients w/ severe CV disease, Raynaud’s syndrome, peptic ulcer, GI bleeding. Renal or hepatic impairment. Pregnancy and lactation.

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.

PO: B

May impair ability to drive or operate machinery.

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.

Symptoms: Nausea, vomiting, gastric complaints, postural hypotension, confusion/psychosis or hallucinations. Management: Supportive treatment. Admin of dopamine antagonist may be advisable.

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).

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.

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

Store between 20-25°C.

Antiparkinsonian Drugs / Other Drugs Affecting Hormonal Regulation

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.

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.