Topiramate (2, 3, 4, 5-bis-O-(1-methylethylidene)-beta-D-fructopyranose sulfamate) is an antiepileptic, gamma-aminobutyric acid antagonist with the ability to inhibit compulsive desire for food and en ...

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Topiramate (2, 3, 4, 5-bis-O-(1-methylethylidene)-beta-D-fructopyranose sulfamate) is an antiepileptic, gamma-aminobutyric acid antagonist with the ability to inhibit compulsive desire for food and engaging behavior.

It is also used to prevent migraine and in alcohol and drug dependence.

Bipolar disorder or manic-depressive psychosis, can increase the risk of obesity and weight gain. Topiramate and sibutramine may have comparable effects of weight loss in overweight or obese bipolar patients (1).

In patients with schizophrenia, weight gain associated with olanzapine is a major concern. In this study topiramate may prevent olanzapine-induced weight gain and adverse metabolic effects (2).

In elderly people with epilepsy there is a problem of difficulty in ingesting antiepileptic tablets that should not be cut, crushed or chewed. Topiramate can be mixed with soft foods (3).

In pediatrics, an effective dosage regime has been established for the approval by the U.S. Food and Drug Administration of topiramate for initial monotherapy in pediatric patients aged 2-9 years. This study indicated an effective dosing regime for the approval by the U.S. Food and Drug Administration of the topiramate concerning initial monotherapy in pediatric patients aged between 2 and 9 years with diagnosis of partial onset seizures and primary generalized tonic-clonic seizures with a pharmacometric bridge approach (4).

Topiramate studies

Molecular Formula: C₁₂H₂₁NO₈S

Molecular Weight: 339.36 g/mol

CAS: 97240-79-4

EC Number: 619-263-3

NSC Number: 759251

UNII: 0H73WJJ391

DSSTox Substance ID: DTXSID8023688

MDL number MFCD00865320

PubChem Substance ID 24724627

Sinonimi:

• (-)-BETA-D-FRUCTOPYRANOS-[(3AS,5AR,8AR,8BS)-2,2,7,7-TETRAMETHYLTETRAHYDRO-3AH-BIS[1,3]DIOXOLO[4,5-B:4',5'-D]PYRAN-3A-YL]METHYL SULFAMATE
• 2,3:4,5-Bis-O-(1-methylethylidene)-36-D-fructo-pyranose sulfamate
• Topamax
• Topimax
• Epitomax
• Topiramato
• Topamax Sprinkle
• Tipiramato
• Tipiramate
• RWJ 17021
• Topiramatum
• McN 4853

References________________________________________________

(1) A 24-week, randomized, controlled trial of adjunctive sibutramine versus topiramate in the treatment of weight gain in overweight or obese patients with bipolar disorders.  McElroy SL, Frye MA, Altshuler LL, Suppes T, Hellemann G, Black D, Mintz J, Kupka R, Nolen W, Leverich GS, Denicoff KD, Post RM, Keck PE Jr.  Bipolar Disord. 2007 Jun;9(4):426-34.

(2) Topiramate for prevention of olanzapine associated weight gain and metabolic dysfunction in schizophrenia: a double-blind, placebo-controlled trial.  Narula PK, Rehan HS, Unni KE, Gupta N. Schizophr Res. 2010 May;118(1-3):218-23. doi: 10.1016/j.schres.2010.02.001.

(3) Advances with extended and controlled release formulations of antiepileptics in the elderly.  Banach M, Miziak B, Borowicz-Reutt KK, Czuczwar SJ.  Expert Opin Pharmacother. 2019 Feb;20(3):333-341. doi: 10.1080/14656566.2018.1549543.

(4) Pharmacometric Bridging Approach for U.S. Food and Drug Administration Approval and Identification of Topiramate Dosing Regimen for Pediatric Patients 2-9 Years of Age With Epilepsy.  Marathe A, Liu C, Kapcala LP, Hershkowitz N, Men A, Uppoor R, Mehta M, Wang Y.  J Pharm Sci. 2019 Apr;108(4):1598-1603. doi: 10.1016/j.xphs.2018.11.027.

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