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20-September-2008 09:55:51 - Pramipexole Pramipexole Systematic IUPAC name 6S-N6-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine Identifiers CAS number 104632-26-0 ATC code N04BC05 PubChem 59868 DrugBank APRD00156 Chemical data Formula C10H17N3S Mol. mass 211.324 g/mol Pharmacokinetic data Bioavailability 90% Protein binding 15% Metabolism Minimal Half life 8 hours Excretion Renal 90% and fecal 2% Therapeutic considerations Licence data EU, US Pregnancy cat. B3AU CUS Legal status ℞ Prescription only Routes Oral Pramipexole INN, trade names Mirapex and Sifrol is a medication indicated for treating Parkinson's disease and restless legs syndrome RLS. It is also sometimes used off-label as a treatment for cluster headache or to counteract the problems with low libido experienced by some users of SSRI antidepressant drugs. Pramipexole has shown robust effects on pilot studies in a placebo-controlled proof of concept study in bipolar disorder1. Pramipexole is classified as a non-ergoline dopamine agonist. Contents 1 Mechanism of action 2 Adverse effects 3 References 3.1 Notes 3.2 Sources 4 External links Mechanism of action Basal ganglia connectivity diagram showing glutamatergic pathways as red, dopaminergic as magenta and GABA pathways as blue. Basal ganglia connectivity diagram showing glutamatergic pathways as red, dopaminergic as magenta and GABA pathways as blue. The basal ganglia is a region of the human brain involved in the regulation of body movement; hence, when components of the basal ganglia are damaged, disorders of body movement may occur. Parkinson's disease is a neurodegenerative disease affecting the substantia nigra, a component of the basal ganglia. The substantia nigra has a high quantity of dopaminergic neurons, which are neurons that release the neurotransmitter known as dopamine. When dopamine is released, it may activate dopamine receptors in the striatum, which is another component of the basal ganglia. When neurons of the substantia nigra deteriorate in Parkinson's disease, the striatum no longer receives dopamine signals. As a result, the basal ganglia can no longer regulate body movement effectively and motor function becomes impaired. By acting as an agonist to the dopamine receptors, pramipexole may directly stimulate dopamine receptors in the striatum, thereby restoring the dopamine signals needed for proper functioning of the basal ganglia. Any depressant effects are most likely the result of pramipexole binding to the D2 receptor subtype, which exhibits inhibitory behavior. Pramipexole binds to dopamine receptors, with particularly high affinity for the D3 receptor subtype.2 Adverse effects Some of the more common side effects of pramipexole include:3 Dizziness, lightheadedness, or fainting, especially when standing up orthostatic hypotension Drowsiness Hallucinations seeing, hearing, or feeling things that are not there Weight gain Weight loss Nausea Trouble in sleeping Twitching, twisting, or other unusual body movements Unusual tiredness or weakness Several unusual adverse effects of this medication may include compulsive gambling, hypersexuality, and overeating. These side effects may be linked to the D3 receptor agonist activity of pramipexole. D3 receptors are located in brain regions involved in mood, behavior, and rewards.4 References Notes ^ Biol Psychiatry. 2004 Jul 1;561:54-60. Pramipexole for bipolar II depression: a placebo-controlled proof of concept study.Zarate CA Jr, Payne JL, Singh J, Quiroz JA, Luckenbaugh DA, Denicoff KD, Charney DS, Manji HK.PMID: 15219473 ^ Mierau J, Schneider F, Ensinger H, Chio C, Lajiness M, Huff R 1995. Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors.. Eur J Pharmacol 290 1: 29-36. doi:10.1016/0922-41069590013-6. PMID 7664822. ^ MedlinePlus Drug Information: Pramipexole Systemic. United States National Library of Medicine. Retrieved on 2006-09-27. ^ Mayo Clinic Staff; M. Leann Dodd July 15, 2005. Parkinson's drug can cause compulsive gambling. Mayo Clinic. Retrieved on 2006-09-27. Sources RxList.com - Pramipexole Mirapex External links Mirapex.com - Manufacturer's website 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/Pramipexole 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 Italiano Nederlands This page was last modified on 10 July 2008, at 01:52
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