Bromocriptine
- Atc Codes:G02CB01#N04BC01
- CAS Codes:22260-51-1#25614-03-3
- PHARMGKB ID:22260-51-1#25614-03-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Broman, Bromed, Umprel; Belgium: Parlodel; Bulgaria: Bromocriptine, Medocriptine; Cyprus: Parlodel, Ronalin, Serocryptin; Czech Republic: Medocriptine, Parlodel; Denmark: Parlodel; Estonia: Bromocriptin; Finland: Parlodel; France: Bromo-Kin, Parlodel; Germany: Bromocriptin, Kirim, Parlodel, Pravidel; Hungary: Bromocriptin, Parlodel, Serocryptin; Ireland: Parlodel; Italy: Bromocriptina, Parlodel; Luxembourg: Pravidel; Lithuania: Bromocriptin; Netherlands: Parlodel; Poland: Bromergon, Bromocorn, Ergolaktyna, Parlodel; Portugal: Bromocriptina, Parlodel; Slovakia: Medocriptine, Parlodel; Spain: Parlodel; Sweden: Pravidel; UK: Parlodel.
North America
Canada: Bromocriptine, Parlodel; USA: Cycloset, Parlodel.
Latin America
Argentina: Parlodel; Brazil: Bagren, Parlodel; Mexico: Biodel, Broptín, Mesikén, Parlodel.
Asia
Japan: Corpadel, Deparo, Erenant, Melen, Padoparine, Palolactin, Parlodel, Parlomin, Parukizone, Prospeline, Upnol.
Drug combinations
Chemistry
Bromocriptine Mesylate: C~32~H~40~BrN~5~O~5~ CH~4~SO~3~. Mw: 750.70. (1) Ergotaman-3′,6′,18-trione, 2-bromo-12′-hydroxy-2′-(1-methylethyl)-5′-(2-methylpropyl)-, monomethanesulfonate, (5’α); (2) 2-Bromoergocryptine monomethanesulfonate. CAS-22260-51-1; CAS-25614-03-3 (bromocriptine)(1977).
Pharmacologic Category
Antiparkinsonian Agents; Ergot-derivative Dopamine Receptor Agonists. (ATC-Code: G02CB01; N04BC01).
Mechanism of action
Semisynthetic ergot alkaloid derivative and dopamine receptor agonist which activates postsynaptic dopamine receptors in the tuberoinfundibular (inhibiting pituitary prolactin secretion) and nigrostriatal pathways (enhancing coordinated motor control). Causes transient increases in growth hormone secretion in individuals with normal growth hormone concentrations. Paradoxically causes sustained suppression of growth hormone secretion in acromegaly. Dysregulation of brain serotonin activity may also occur.
Therapeutic use
Treatment of hyperprolactinemia associated with amenorrhea with or without galactorrhea, infertility, or hypogonadism. Treatment of prolactin-secreting adenomas (may be used prior to surgery in patients undergoing excision of the tumor). Treatment of acromegaly. Treatment of Parkinson’s disease (as an adjunct to levodopa).
Pregnancy and lactiation implications
In general, therapy should be discontinued if pregnancy is confirmed unless needed for treatment of macroprolactinoma. Since bromocriptine interferes with lactation, the drug should not be administered to women who elect to breast-feed.
Unlabeled use
Neuroleptic malignant syndrome. Initial symptomatic management of parkinsonian syndrome as monotherapy (in patients ≤70 years of age). To relieve premenstrual breast symptoms. Cushing’s disease. Chronic hepatic encephalopathy.
Contraindications
Hypersensitivity to bromocriptine, ergot alkaloids, or any component of the formulation. Ergot alkaloids are contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics). Uncontrolled hypertension. Severe ischemic heart disease or peripheral vascular disorders. Pregnancy. Concomitant use with serotonin agonists (includes buspirone, SSRIs, TCAs, nefazodone, sumatriptan, and trazodone) and sibutramine.
Warnings and precautions
Use with caution in cardiovascular disease (myocardial infarction, arrhythmia). Should not be used postpartum in women with coronary artery disease or other cardiovascular disease (its use to control or prevent lactation or in uncontrolled hypertension is not recommended). Ergot alkaloids and derivatives have been associated with fibrotic valve thickening (e.g. aortic, mitral, tricuspid), usually associated with long-term, chronic use. Symptomatic hypotension may occur. Concomitant use of bromocriptine and other ergot alkaloids is not recommended. Particular caution is indicated in patients who have recently received other drugs that can alter blood pressure. Associated with compulsive behaviors and/or loss of impulse control (pathological gambling, libido increases, and/or binge eating). May cause sudden sleep onset and somnolence, primarily in Parkinson’s disease. Confusion and mental disturbances may occur in patients with parkinsonian syndrome receiving high-dose therapy. Concurrent use with levodopa has been associated with an increased risk of hallucinations. Caution in dementia. Discontinuation of therapy in macroadenomas has been associated with rapid regrowth of tumor and increased prolactin serum levels. Digital vasospasm (cold-sensitive) may occur in some patients with acromegaly. Rare cases of pleural and/or retroperitoneal fibrosis reported with prolonged daily use. Use with caution in peptic ulcer disease. Use not recommended in galactose intolerance, severe lactase deficiency, or glucose-galactose malabsorption. Use with caution in hepatic/renal impairment. Bromocriptine therapy has caused transient increases in serum concentrations of AST (SGOT), ALT (SGPT), γ-glutamyl transferase (γ-glutamyltranspeptidase, GGT, GGTP), creatine kinase (CK, creatine phosphokinase, CPK), alkaline phosphatase, uric acid, and BUN. May interfere with TSH assay (false low TSH levels).