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20-September-2008 09:55:50 - Bromocriptine Chemical structure of Bromocriptine Bromocriptine Systematic IUPAC name Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-1-methylethyl-5'alpha-2 -methylpropyl- Identifiers CAS number 25614-03-3 ATC code G02CB01 N04BC01 PubChem 31101 DrugBank APRD00622 Chemical data Formula C32H40BrN5O5 Mol. mass 654.595 Pharmacokinetic data Bioavailability 28% of oral dose absorbed Metabolism ? Half life 12-14 hours Excretion 85% bile faeces Therapeutic considerations Pregnancy cat. BUS Legal status ? Routes oral Bromocriptine brand names include Parlodel, an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors and Parkinson's disease. Contents 1 Uses 1.1 Parkinson's disease 2 Structure 3 See also 4 External links 5 References Uses Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated by this drug. It has also used in some countries to prevent lactation following childbirth if the mother does not wish to breastfeed; one of dopamine's effects on the pituitary is as an antagonist of prolactin production by lactotrophs. However, the FDA removed this indication in 1995, because of concerns with respect to an increased risk of heart attack, seizure and stroke. Because of prolactin's role in stimulating proliferation of the T-lymphocytes of the immune system, bromocriptine has also been used to suppress the immune system in organ transplant patients.1 Since bromocryptine acts as a dopamine agonist, it has potential use in treating cocaine addiction, as the addictive effects of cocaine are caused by it blocking dopamine reuptake. Although it has negligible subjective effects when administered alone, studies show it has the potential to significantly ease the cocaine withdrawal syndrome.23 There appear to be some connections between insulin insensitivity and dopamine. A company called Veroscience 4 is using bromocriptine to treat diabetes and obesity, and their website postulates a connection between neurotransmitters and seasonal variation in insulin sensitivity among vetebrate animals.5 There are also some connections between temperature and dopamine and serotonin production.6 In addition, new research indicates that patients with diabetes are more likely to develop Parkinson's disease, which is characterized by a dopamine deficiency in the brain. Parkinson's disease Bromocriptine is an agonist of D2 dopamine receptors and has therefore been used as a treatment for Parkinson's disease. Early studies suggested that treating patients with bromocriptine before levodopa would delay the onset of side effects such as dyskinesia.7 However, a recent Cochrane review found a lack of evidence to support this view. 8 Structure Like all ergopeptides, bromocriptine is a cyclol; two peptide groups of its tripeptide moiety shown in black at the upper left of the Figure are crosslinked, forming the N-COH juncture between the two rings with the amide functionality. See also Cabergoline External links MedlinePlus DrugInfo medmaster-a682079 http://www.drugs.com/pro/bromocriptine.html References ^ Clodi M, Kotzmann H, Riedl M, Schmidt A, Barnas U, Muhlbacher F, Mustafa G, Horl WH, Waldhausl W, Mayer G, Luger A., 1997. The long-acting dopamine agonist bromocriptine mesylate as additive immunosuppressive drug after kidney transplantation. Nephrol Dial Transplant. 1997 Apr;124:748-52. ^ Campbell A, Baldessarini RJ, Cremens C, Teicher MH, Marsh E, Kula NS, 1989. Bromocriptine antagonizes behavioral effects of cocaine in the rat. Neuropsychopharmacology 1989 Sep; 23:209-24. ^ KL Preston, JT Sullivan, EC Strain and GE Bigelow, 1992. Effects of cocaine alone and in combination with bromocriptine in human cocaine abusers. J Pharmacol Exp Ther. 1992 Jul;2621:279-91. ^ VeroScience ^ Bromocriptine improves glycaemic control and serum lipid profile in obese Type 2 diabetic subjects: a new approach in the treatment of diabetes. Expert Opin Investig Drugs. 1999 Oct;810:1683-1707. ^ http://sulcus.berkeley.edu/mcb/165_001/papers/manuscripts/_281.html ^ JL Montastruc, O Rascol, JM Senard and A Rascol, 1994. BA randomised controlled study comparing bromocriptine to which levodopa was later added, with levodopa alone in previously untreated patients with Parkinson's disease: a five year follow up. Journal of Neurology, Neurosurgery, and Psychiatry, 1994, Vol 57, 1034-1038 ^ van Hilten J, Ramaker C, Stowe R, Ives Nj., 2007. Bromocriptine/levodopa combined versus levodopa alone for early Parkinson's disease. Cochrane Database Syst Rev. 2007 Oct 17;4:CD003634. v d e Ergolines Lysergic acid derivatives Bromocriptine, Cabergoline, Ergine, Ergonovine, Ergotamine, Lysergic acid, Lysergol, LSD, D-Lysergic acid hydroxyethylamide, Lisuride, Methergine, Methysergide, Pergolide Hallucinogenic lysergamides AL-LAD, ALD-52, BU-LAD, CYP-LAD, DAL, DAM-57, Ergonovine, ETH-LAD, LAE-32, LSD, LPD-824, LSM-775, D-Lysergic acid N-α-hydroxyethylamide, Methylergonovine, MLD-41, PARGY-LAD, PRO-LAD Other ergolines Ergoline Natural sources Argyreia nervosa, Claviceps spp., Ipomoea tricolor, Ipomoea violacea, Rivea corymbosa v d e Other gynecologicals G02C Sympathomimetics, labour repressants Ritodrine - Buphenine - Fenoterol Prolactin inhibitors Bromocriptine - Lisuride - Cabergoline - Quinagolide - Metergoline Anti-inflammatory products for vaginal administration Ibuprofen - Naproxen - Benzydamine - Flunoxaprofen Other gynecologicals Atosiban v d e Anti-parkinson drugs: dopaminergic agents N04B Dopa and derivatives Droxidopa Levodopa Melevodopa Etilevodopa Adamantane derivatives Amantadine Dopamine agonists A-412,997 Apomorphine Bromocriptine Cabergoline Dihydrexidine Dihydroergocryptine mesylate Fenoldopam Lisuride Pergolide Piribedil Pramipexole Propylnorapomorphine Quinpirole Ropinirole Rotigotine SKF 38393 SKF 82958 MAOIs B Selegiline Rasagiline COMT inhibitors Entacapone Tolcapone Other Budipine dopa decarboxylase inhibitor Carbidopa Retrieved from http://en..org/wiki/Bromocriptine Categories: Dopamine agonists Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Español Français Italiano Magyar Polski РуÑ?Ñ?кий Svenska This page was last modified on 10 July 2008, at 04:08
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