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11-SEPTEMBER-2008 12:20:15 - Pizotifen Pizotifen Systematic IUPAC name 4-1-methyl-4-piperidylidine-9,10-dihydro -4H-benzo-4,5cyclohepta1,2-thiophene Identifiers CAS number 15574-96-6 ATC code N02CX01 PubChem 27400 Chemical data Formula C19H21NS Mol. mass 295.443 g/mol Pharmacokinetic data Bioavailability 78% Protein binding 91% Metabolism Glucuronidation is the main route of biotransformation, the main metabolite is the N-glucuronide-conjugate,accounting for at least 50% of the plasma and 60-70% of urinary excreted drug. Half life 23h Excretion 18% feces, 55% urine both as metabolites. Therapeutic considerations Pregnancy cat. B1AU Legal status Routes Oral Pizotifen trade names Pizotyline, Sandomigran is a benzocycloheptane based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches.1 Contents 1 Uses 2 Adverse effects 3 Contraindications 4 Mechanism 5 References 6 External links Uses The main medical use for pizotifen is for the prevention of vascular headache including migraine and cluster headache. Pizotifen is one of a range of medications used for this purpose, other options include propranolol, topiramate, valproic acid and amitryptyline. While pizotifen is reasonably effective,2 its use is limited by side effects, principally drowsiness and weight gain, and it is usually not the first choice medicine for preventing migraines, instead being used as an alternative when other drugs have failed to be effective.3 Other applications for which pizotifen may be used include as an antidepressant, or for the treatment of anxiety or social phobia.45 Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome or MDMA overdose6 in a similar manner to the closely related antihistamine/antiserotonin drug cyproheptadine. Adverse effects Side effects include sedation, dry mouth, drowsiness, increased appetite and weight gain.7 Occasionally it may cause nausea or dizziness. In rare cases, anxiety, aggression and depression may also occur. Contraindications Pizotifen is contraindicated in patients who suffer from hypersensitivity to any of its components , also Pizotifen is contraindicated in gastric outlet obstruction, pregnancy, zakrytougolnoy glaucoma and difficulty urinating8. Mechanism Pizotifen is a serotonin antagonist acting mainly at the 5-HT1, 5-HT2A and 5HT2C receptors. It also has some activity as an antihistamine.9 References ^ Stark RJ, Valenti L, Miller GC. Management of migraine in Australian general practice. Medical Journal of Australia. 2007 Aug 6;1873:142-6. ^ Barnes N, Millman G. Do pizotifen or propranolol reduce the frequency of migraine headache? Archives of Disease in Childhood. 2004 Jul;897:684-5. ^ Pierangeli G, Cevoli S, Sancisi E, Grimaldi D, Zanigni S, Montagna P, Cortelli P. Which therapy for which patient? Neurological Sciences. 2006 May;27 Suppl 2:S153-8. ^ Standal JE. Pizotifen as an antidepressant. Acta Psychiatrica Scandinavica. 1977 Oct;564:276-9. ^ Banki CM. Clinical observations with pizotifene Sandomigran in the treatment of nonmigrainous depressed women. Archiv fur Psychiatrie und Nervenkrankheiten. 1978 Mar 7;2251:67-72. ^ Young R, Khorana N, Bondareva T, Glennon RA. Pizotyline effectively attenuates the stimulus effects of N-methyl-3,4-methylenedioxyamphetamine MDMA. Pharmacology, Biochemistry and Behavior. 2005 Oct;822:404-10. ^ Crowder D, Maclay WP. Pizotifen once daily in the prophylaxis of migraine: results of a multi-centre general practice study. Current Medical Research and Opinion. 1984;94:280-5. ^ Likarstwo.ru ^ Dixon AK, Hill RC, Roemer D, Scholtysik G. Pharmacological properties of 4-1-methyl-4-piperidylidine-9,10-dihydro-4H-benzo-4,5cyclohepta1,2-thiophene hydrogen maleate pizotifen. Arzneimittelforschung. 1977;2710:1968-79. External links Sandomigran drug data sheet v d e Antimigraine preparations N02C Ergot alkaloids Dihydroergotamine Ergotamine Methysergide Lisuride Corticosteroid derivatives Flumedroxone Selective serotonin 5-HT1 agonists Triptans Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan, Zolmitriptan Other antimigraine preparations Pizotifen Clonidine Topiramate Amidrine Iprazochrome Dimetotiazine Oxetorone Dotarizine Lomerizine v d e Serotonin antagonists 5-HT2 Melperone · Paliperidone · Risperidone · Sertindole · Ziprasidone · Quetiapine 5-HT3 Alosetron · Azasetron · Bemesetron · Cilansetron · Dolasetron · Granisetron · Lerisetron · Ondansetron · Palonosetron · Ramosetron · Tropisetron · Zacopride · Zatosetron Other/ungrouped Amperozide · Blonanserin · Bufotenin · Cianopramine · Cinanserin · Clozapine · Cyanopindolol · Cyproheptadine · Deramciclane · Dotarizine · Fananserin · Fenclonine · Ketanserin · Lysergic acid diethylamide · Metergoline · Methiothepin · Methysergide · Mianserin · N,N-Dimethyltryptamine · Nafronyl · Olanzapine · Pindolol · Pipamperone · Pizotyline · Quetiapine · Renzapride · Ritanserin · Sarpogrelate · Setoperone · Tolfenamic acid · Wortmannin · Xylamidine Retrieved from http://en..org/wiki/Pizotifen Categories: Anxiolytics | Serotonin antagonists | Thiophenes 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 This page was last modified on 14 August 2008, at 10:3
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