Topiramate

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Topiramate.png
Topiramate chemical structure


Topiramate

2,3:4,5-bis-O-(1-methylethylidene)-
β-D-Fructopyranose sulfamate
CAS number
97240-79-4
ATC code
N03AX11
Chemical formula C12H21NO8S
Molecular weight 339.363
Bioavailability  ?
Metabolism  ?
Elimination half-life  ?
Excretion  ?
Pregnancy category  ?
Legal status  ?
Routes of administration  ?

Topiramate (brand name: Topamax®) is an anticonvulsant drug that is used to treat epilepsy in both children and adults. It has also been used by psychiatrists to treat bipolar disorder. In addition, it is sometimes prescribed for treatment of cluster migraines. It is produced by Ortho-McNeil pharmaceutical. This drug was investigated for use in treatment of obesity-specifically to aid in the reduction of binge eating. However, that use is not actively promoted by the drug's manufacturer and is an "off-label" use.

Pharmacodynamics

It appears as though Topiramate enhances GABA through interfering with calcium and sodium channels. It is also a weak inhibitor of carbonic anhydrase. Mood Stabilizations seems to occur before anticonvulsant qualities at lower dosages.

Side effects

Feeling of pins and needles in the head and extremities, or feelings of electrical shock; cognitive deficiency (particularly word-finding difficulty); grogginess; lethargy; impairment of fine motor skills; vision abnormality and transient or permanent vision loss (see below for FDA warning); weight loss; breast pain; abdominal pain; menstrual disorder; taste changes; pharyngitis; sinusitis; diplopia; rash; leukopenia; fatigue; dizziness; insomnia; anxiety; depression; paresthesia; diarrhea; nausea; dyspepsia; constipation; dry-mouth; dysmenorrhea.

The Food and Drug Administration (FDA) has issued a notification alerting physicians who prescribe topiramate, and their patients, to the risk of vision loss (blindness). Acute myopia and secondary angle closure glaucoma, in a small subset of patients who take topiramate regularly, may cause transient (reversible), or permanent, loss of vision. The symptoms, which typically begin in the first month of use, include blurred vision and eye pain. If addressed early in its course, discontinuation of topiramate, along with other measures deemed prudent by the prescribing physician and/or ophthalmologist, may halt the progression of the ocular damage, and may reverse the visual impairment. Patients who take topiramate and who feel pain in or around their eyes, or notice a loss of vision, visual acuity, or blurred vision, are advised to seek consultation with their physician as soon as reasonably possibly. According to the FDA: "in more than 825,000 patients...As of August 17, 2001 there have been 23 reported cases: 22 in adults and 1 in pediatric patients. It is generally recognized that postmarketing data are subject to substantial under-reporting."

In other postmarketing research, a risk of decreased sweating and hyperthermia was discovered. Pediatric patients (children) are especially prone to this side-effect. It is recommended that children treated with topiramate should be monitored closely for evidence of decreased sweating and increased body temperature, especially in hot weather. All patients, particularly those with other predisposing factors, should be instructed to maintain an adequate fluid intake in order to minimize the risk of kidney stone formation.

These harmful side effects will be included on the drug's warning label in the future.

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