Pizotifen: Difference between revisions
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==Dose== |
==Dose== |
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Typically adult |
Typically adult dose is 1.5mg at night or 500 micrograms 3 times daily, adjusted according to response. Max single does 3mg, max daily dose 4.5mg. |
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Child over 2 years and up, up to 1.5mg daily in divided dose; max single dose at night 1mg. |
Child over 2 years and up, up to 1.5mg daily in divided dose; max single dose at night 1mg. |
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Revision as of 07:40, 14 July 2008
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| Clinical data | |
|---|---|
| Pregnancy category |
|
| Routes of administration | Oral |
| ATC code | |
| 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. |
| Elimination half-life | 23h |
| Excretion | 18% feces, 55% urine (both as metabolites). |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.036.014 |
| Chemical and physical data | |
| Formula | C19H21NS |
| Molar mass | 295.443 g/mol g·mol−1 |
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]
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.[2]
Side effects
Side effects include sedation, dry mouth, drowsiness, increased appetite and weight gain.[3] Occasionally it may cause nausea or dizziness. In rare cases, anxiety, aggression and depression may also occur.
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,[4] 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.[5]
Other applications for which pizotifen may be used include as an antidepressant, or for the treatment of anxiety or social phobia.[6][7] Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome or MDMA overdose[8] in a similar manner to the closely related antihistamine/antiserotonin drug cyproheptadine.
Dose
Typically adult dose is 1.5mg at night or 500 micrograms 3 times daily, adjusted according to response. Max single does 3mg, max daily dose 4.5mg.
Child over 2 years and up, up to 1.5mg daily in divided dose; max single dose at night 1mg.
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.
- ^ 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.
- ^ 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.
- ^ 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.
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