Bromocriptine
Clinical data | |
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Trade names | Originally Parlodel, subsequently many[1] |
Other names | 2-Bromoergocriptine; CB-154 |
AHFS/Drugs.com | Monograph, International Drug Names |
MedlinePlus | a682079 |
Pregnancy category |
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intravenous | |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 28% of oral dose absorbed |
Metabolism | Extensively liver-mediated |
Elimination half-life | 12–14 hours |
Excretion | 85% bile (feces), 2.5–5.5% urine |
Identifiers | |
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Bromocriptine, originally marketed as Parlodel and subsequently under many brand names,
It was patented in 1968 and approved for medical use in 1975.[2]
Medical uses
Bromocriptine is used to treat
Since the late 1980s it has been used, off-label, to reduce the symptoms of cocaine withdrawal but the evidence for this use is poor.[6] Bromocriptine has been successfully used in cases of galactorrhea precipitated by dopamine antagonists like risperidone.
A quick-release formulation of bromocriptine, Cycloset, is also used to treat type 2 diabetes.[7][8][9] When administered within 2 hours of awakening, it increases hypothalamic dopamine level. That results to a significant weight loss, decreases blood glucose levels and hepatic glucose production and also insulin resistance.[10] It therefore acts as an adjunct to diet and exercise to improve glycemic control and cardiovascular risk.[10][11]
Side effects
Most frequent side effects are nausea,
Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence estimated to range between 0.005% and 0.04%. Additional safety precautions and stricter prescribing rules were suggested based on the data.[17][18] It is a bile salt export pump inhibitor.[19]
After long-term use of
Pharmacology
Pharmacodynamics
Bromocriptine is a
As an
Site | Affinity (Ki [nM]) | Efficacy (Emax [%]) | Action |
---|---|---|---|
D1
|
692 | ? | ? |
D2S
|
5.0 | 41 | Partial agonist |
D2L
|
15 | 28 | Partial agonist |
D3
|
6.8 | 68 | Partial agonist |
D4
|
372 | 0 | Silent antagonist |
D5
|
537 | ? | ? |
5-HT1A | 13 | 72 | Partial agonist |
5-HT1B | 355 | 66 | Partial agonist |
5-HT1D | 11 | 86 | Partial agonist |
5-HT2A | 107 | 69 | Partial agonist |
5-HT2B | 56 | 0 | Silent antagonist |
5-HT2C | 741 | 79 | Partial agonist |
5-HT6 | 33 | ? | ? |
5-HT7 | 11–126 | ? | ? |
α1A
|
4.2 | 0 | Silent antagonist |
α1B
|
1.4 | ? | ? |
α1D
|
1.1 | ? | ? |
α2A
|
11 | 0 | Silent antagonist |
α2B
|
35 | 0 | Silent antagonist |
α2C
|
28 | 0 | Silent antagonist |
α2D
|
68 | ? | ? |
β1
|
589 | ? | ? |
β2
|
741 | ? | ? |
H1
|
>10,000 | – | – |
M1 | >10,000 | – | – |
Notes: All receptors are human except α2D-adrenergic, which is rat (no human counterpart), and 5-HT7, which is rat/mouse.[21][27] |
Chemistry
Like all ergopeptides, bromocriptine is a cyclol; two peptide groups of its tripeptide moiety are crosslinked, forming the >N-C(OH)< juncture between the two rings with the amide functionality.
Bromocriptine is a
History
Bromocriptine was discovered by scientists at Sandoz in 1965 and was first published in 1968; it was first marketed under the brand name Parlodel.[30][31]
A quick-release formulation of bromocriptine was approved by the FDA in 2009.[32]
Society and culture
Brand names
As of July 2017, bromocriptine was marketed under many brand names worldwide, including Abergin, Barlolin, Brameston, Brocriptin, Brom, Broma-Del, Bromergocryptine, Bromergon, Bromicon, Bromocorn, Bromocriptin, Bromocriptina, Bromocriptine, Bromocriptine mesilate, Bromocriptine mesylate, Bromocriptine methanesulfonate, Bromocriptini mesilas, Bromocriptinmesilat, Bromodel, Bromokriptin, Bromolac, Bromotine, Bromtine, Brotin, Butin, Corpadel, Cripsa, Criptine, Criten, Cycloset, Degala, Demil, Deparo, Deprolac, Diacriptin, Dopagon, Erenant, Grifocriptina, Gynodel, kirim, Kriptonal, Lactodel, Medocriptine, Melen, Padoparine, Palolactin, Parlodel, Pravidel, Proctinal, Ronalin, Semi-Brom, Serocriptin, Serocryptin, Suplac, Syntocriptine, Umprel, Unew, Updopa, Upnol B, and Volbro.[1]
As of July 2017 it was also marketed as a combination drug with metformin as Diacriptin-M, and as a veterinary drug under the brand Pseudogravin.[1]
References
- ^ a b c d "Bromocriptine international brand names". Drugs.com. Archived from the original on 6 August 2017. Retrieved 13 July 2017.
- ISBN 9783527607495.
- ^ a b "Bromocriptine mesylate tablets -- original uses" (PDF). FDA. January 2012. Archived (PDF) from the original on 2017-02-28. For label updates see FDA index page for NDA 017962 Archived 2017-06-29 at the Wayback Machine
- S2CID 205077946.
- PMID 33851429.
- PMID 26014366.
- ^ "Bromocriptine mesylate tablet label" (PDF). FDA. February 2017. Archived (PDF) from the original on 2018-05-13.. For label updates see FDA index page for NDA 020866 Archived 2017-06-28 at the Wayback Machine
- PMID 23337160.
- S2CID 423132.
- ^ PMID 37415177.
- PMID 21447659.
- PMID 3516579.
- PMID 8691994.
- S2CID 29539691.
- PMID 24463000.
- PMID 2129961.
- ^ "European Medicines Agency - News and Events - CMDh endorses restricted use of bromocriptine for stopping breast milk production". www.ema.europa.eu. 2018-09-17. Archived from the original on 2014-08-28.
- ^ "EMA rät vom Abstillmittel Bromocriptin ab". 2014-08-25. Archived from the original on 2015-06-09. Retrieved 2014-08-26. "EMA rät vom Abstillmittel Bromocriptin ab", article in Ärzteblatt
- S2CID 46496531.
- S2CID 207489653.
- ^ S2CID 6200455.
- ^ S2CID 35238120.
- PMID 20138024.
- ^ S2CID 19260572.
- PMID 20599932.
- ^ PMID 24361689.
- ^ a b National Institute of Mental Health. PDSP Ki Database (Internet). ChapelHill (NC): University of North Carolina. Available from: "PDSP Database - UNC". Archived from the original on 2021-04-13. Retrieved 2021-04-12.
- ^ E. Fluckiger, A. Hofmann, U.S. patent 3,752,814 (1973)
- Sandoz AG
- ISBN 9780471899792.
- doi:10.1071/CH13639.
- S2CID 22908831.