This MedLibrary.org supplementary page on Pizotifen is provided directly from the open source Wikipedia as a service to our readers. Please see the note below on authorship of this content, as well as the Wikipedia usage guidelines. To search for other content from our encyclopedia supplement, please use the form below:
Related Sponsors
 |
|
|
Pizotifen
|
|
| Systematic (IUPAC) name | |
| 4-(1-methyl-4-piperidylidine)-9,10-dihydro -4H-benzo-[4,5]cyclohepta[1,2]-thiophene | |
| Identifiers | |
| CAS number | |
| ATC code | N02 |
| PubChem | |
| 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. |
B1(AU) |
| 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 |
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.[4][5] Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome or MDMA overdose[6] 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 urinating[8].
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;187(3):142-6.
- ^ Barnes N, Millman G. Do pizotifen or propranolol reduce the frequency of migraine headache? Archives of Disease in Childhood. 2004 Jul;89(7):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;56(4):276-9.
- ^ Banki CM. Clinical observations with pizotifene (Sandomigran) in the treatment of nonmigrainous depressed women. Archiv fur Psychiatrie und Nervenkrankheiten. 1978 Mar 7;225(1):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;82(2):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;9(4):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-[4,5]cyclohepta[1,2]-thiophene hydrogen maleate (pizotifen). Arzneimittelforschung. 1977;27(10):1968-79.
External links
|
||||||||||||||
|
|||||||||||
Wikipedia content modification information:
- This page was last modified on 14 August 2008, at 10:30.
Wikipedia Authorship and Review
Wikipedia content provided here is not reviewed directly by MedLibrary.org. Wikipedia content is authored by an open community of volunteers and is not produced by or in any way affiliated with MedLibrary.org.
Wikipedia Usage Guidelines
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article on "Pizotifen".
The URL for this specific entry is:
All Wikipedia text is available under the terms of the GNU Free Documentation License. (See Copyrights for details). Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc.