Adult: For idiopathic cases or those caused by pituitary adenomas: As 0.5 mg tab: Initially, 0.5 mg weekly, increased gradually in increments of 0.5 mg weekly at monthly intervals until optimal response is reached. Usual therapeutic dose: 1 mg weekly (range: 0.25-2 mg weekly). Max: 4.5 mg weekly. The weekly dose may be given as a single dose or divided into ≥2 doses on separate days depending on patient tolerability (particularly for doses >1 mg weekly). Use the lowest effective dose. Dosage and treatment recommendations may vary among individual products or between countries (refer to detailed local product guidelines).
Oral Parkinson's disease
Adult: As 2nd-line treatment in patients who are intolerant or have failed therapy with a non-ergot compound: Monotherapy or adjunct to levodopa and dopa-decarboxylase inhibitor: As 1 mg or 2 mg tab: Initially, 0.5 mg daily (in monotherapy) or 1 mg daily (in adjunctive therapy), may be increased gradually in increments of 0.5-1 mg at 1 or 2 weeks interval until optimal response is reached. Recommended therapeutic dose: 2-3 mg daily. For adjunctive therapy, a gradual decrease in the dose of concurrent levodopa while increasing the dose of cabergoline may be required until the optimum balance is determined. Use the lowest effective dose. Treatment recommendations may vary among individual products or between countries (refer to detailed local product guidelines).
Oral Inhibition of physiological lactation
Adult: As 0.5 mg tab: 1 mg as a single dose on the 1st day postpartum. Treatment recommendations may vary between countries (refer to detailed local product guidelines).
Oral Suppression of lactation
Adult: As 0.5 mg tab: 0.25 mg 12 hourly for 2 days. Treatment recommendations may vary between countries (refer to detailed local product guidelines).
Hepatic Impairment
Severe (Child-Pugh class C): Dose reduction may be needed.
Administration
Should be taken with food.
Contraindications
History of pulmonary, pericardial, or retroperitoneal fibrotic disorders; cardiac valvular disorders (indicated by evidence of cardiac valvulopathy of any valve, valve leaflet thickening, valve restriction, or mixed valve restriction stenosis); uncontrolled hypertension; history of puerperal psychosis. Lactation. Concomitant use with dopamine antagonists (e.g. phenothiazines, butyrophenones, thioxanthenes, metoclopramide).
Special Precautions
Patient with severe CV disease, Raynaud's syndrome, peptic ulcer, gastrointestinal bleeding, pregnancy-induced hypertension (e.g. pre-eclampsia, eclampsia, postpartum hypertension); history of serious mental illness, particularly psychotic disorders. Concomitant use with antihypertensives. Renal and hepatic impairment. Pregnancy.
Adverse Reactions
Significant: Cardiac valvulopathy and related disorders (e.g. pericarditis, pericardial effusion); pleural, pericardial, or retroperitoneal fibrosis; pleural effusion, abnormally increased erythrocyte sedimentation rate (ESR); aggression, psychotic behaviour, and impulse control disorders (e.g. increased libido, hypersexuality, pathological gambling, compulsive spending or buying, binge-eating); somnolence and episodes of sudden sleep onset, orthostatic hypotension; hypertension, MI, seizures, stroke and psychiatric disorders, particularly in postpartum women (when used for lactation inhibition). Cardiac disorders: Angina pectoris, palpitation. Ear and labyrinth disorders: Vertigo. Eye disorders: Abnormal vision. Gastrointestinal disorders: Nausea, vomiting, constipation, dyspepsia, abdominal pain, gastritis, xerostomia. General disorders and administration site conditions: Asthenia, fatigue, peripheral oedema, influenza-like symptoms. Immune system disorders: Hypersensitivity reaction. Investigations: Decreased Hb, haematocrit, and RBC; abnormal LFTs. Musculoskeletal and connective tissue disorders: Leg cramps. Nervous system disorders: Headache, dizziness, paraesthesia, dyskinesia, hyperkinesia, tremor. Psychiatric disorders: Depression, hallucinations, sleep disturbances, insomnia, confusion. Reproductive system and breast disorders: Dysmenorrhoea, breast pain. Respiratory, thoracic and mediastinal disorders: Nasal congestion, epistaxis, dyspnoea. Skin and subcutaneous tissue disorders: Acne, pruritus, rash, alopecia. Vascular disorders: Hot flushes, syncope, digital vasospasm.
This drug may cause somnolence or sudden sleep onset, if affected, do not drive or operate machinery. Women of childbearing potential must use proven birth control methods during therapy and for at least 1 month after stopping the treatment.
Monitoring Parameters
Evaluate the pregnancy status in women of childbearing potential before treatment initiation and monthly in case of amenorrhoeic period. Perform echocardiogram (at baseline, within 3-6 months after initiation, every 6-12 months thereafter and as clinically indicated) and chest X-ray (at baseline and as necessary). Obtain ESR and serum creatinine levels at baseline and regularly during treatment. Monitor blood pressure and serum prolactin levels (monthly until normalised). Assess for signs and symptoms of pleuro-pulmonary disease, cardiac failure, renal insufficiency, ureteral or abdominal obstruction, hypotension, amenorrhoea, and mental status changes during therapy.
Overdosage
Symptoms: Nausea, vomiting, nasal congestion, gastric complaints, orthostatic hypotension, confusion, psychosis, or hallucinations. Management: Symptomatic and supportive treatment. Measures should be taken to maintain blood pressure, if necessary. Administration of activated charcoal within 1 hour of ingestion or giving dopamine antagonists may be considered.
Drug Interactions
Decreased prolactin-lowering effect with dopamine antagonists (e.g. phenothiazines, butyrophenones, thioxanthenes, metoclopramide). Enhanced risk of orthostatic hypotension with antihypertensives. Increased systemic bioavailability with macrolide antibiotics (e.g. erythromycin).
Action
Description: Mechanism of Action: Cabergoline, an ergot-derivative, is a long-acting dopamine agonist with a high binding affinity for dopamine D2 receptors. It inhibits prolactin secretion from the anterior pituitary gland through direct stimulation of the dopamine D2 receptors on pituitary lactotrophs. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: 2-3 hours. Distribution: Extensively distributed throughout the body (particularly to the pituitary). Plasma protein binding: 40-42%. Metabolism: Extensively metabolised in the liver via hydrolysis; minimal CYP450-mediated metabolism. Undergoes first-pass metabolism. Excretion: Mainly via faeces (approx 60%); urine (approx 22%; <4% as unchanged drug). Elimination half-life: 63-69 hours.
Chemical Structure
Cabergoline Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 54746, Cabergoline. https://pubchem.ncbi.nlm.nih.gov/compound/Cabergoline. Accessed Jan. 24, 2024.
Storage
Store below 30°C. Keep in the original package to protect from moisture.
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. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 14/09/2023.Anon. Cabergoline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/09/2023.Buckingham R (ed). Cabergoline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/09/2023.Cabergoline 0.5 mg Tablets (Teva UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 08/01/2024.Cabergoline 2 mg Tablets (Teva UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 14/09/2023.Cabergoline Tablet (A-S Medication Solutions). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 14/09/2023.Dostinex 0.5 mg Tablet (Pfizer [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 14/09/2023.Joint Formulary Committee. Cabergoline. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/09/2023.Pfizer New Zealand Limited. Dostinex 0.5 mg Tablet data sheet 14 July 2023. Medsafe. http://www.medsafe.govt.nz. Accessed 14/09/2023.
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