The details of Topiramate

Topiramate is a white crystalline powder with a bitter taste. It is most soluble in alkaline solutions containing sodium hydroxide or sodium phosphate and having a pH of 9 to 10. It is freely soluble in acetone, chloroform, dimethylsulfoxide, and ethanol. The solubility in water is 9.8 mg/mL. Its saturated solution has a pH of 6.3. It has the molecular formula C12H21NO8S and a molecular weight of 339.36. 

Topiramate(CAS NO:97240-79-4) is an oral drug that is used to prevent the seizures of epilepsy. It is an anti-epileptic or anti-seizure drug. It is used primarily among patients who are not controlled by other anti-epileptic drugs. About 1 in 4 Americans diagnosed with epilepsy has seizures that resist treatment with other anti-epileptic drugs. It also prevents migraine headaches.

Before taking topiramate, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: a certain eye problem (narrow angle glaucoma), kidney problems (such as kidney stones), liver problems, mental/mood problems (such as depression, thoughts of suicide), lung/breathing problems, a certain metabolic imbalance (metabolic acidosis), long-term diarrhea, a diet high in fat and low in carbohydrates (ketogenic diet), brittle bones (osteoporosis).

Most commonly, topiramate is started in low doses, 25 or 50 mg per day, and then increased slowly by 25 to 50 mg per week until an effective daily dose is reached. For children 10 years or older and adults the dose may be increased by 100 mg in week 5 and 6 when it is used alone. This slow approach to treatment reduces side effects. The recommended final adult dose is 200-400 mg administered as two divided doses daily.

In children, the starting dose is up to 25 mg (1 to 3 mg/kg/day), taken nightly for the first week. The dose is then increased at 1 or 2 week intervals by 1 to 3 mg/kg/day administered in two divided doses. The target dose is 5 to 9 mg/kg per day in two divided doses.

Migraine is treated 25 mg nightly for the first week then increased by 25 mg weekly up to a maximum dose of 100 mg administered in two divided doses. Patients should maintain an adequate fluid intake in order to minimize the risk of kidney stones.

Topiramate is absorbed quickly by the body soon after you swallow it. The drug works by interacting with the neurotransmitter GABA which controls communication between brain cells. It helps GABA to reduce certain types of excitory neural impulses to prevent seizures and stabilize mood. Around 70 percent of the drug is excreted in the urine.

The half-life of a medication denotes how long it takes for the concentration of the drug in your plasma to reach half of its original concentration, in other words, how long it takes for half of the original dose to be eliminated from your blood stream. The half-life of topiramate is 19-23 hours.

You should seek medical advice immediately if you are using topiramate and experience any of the following side effects: depression, suicidal thoughts, hyperactivity, irritability, hostility or anxiety. Other possible side-effects include impaired vision. You should also avoid drinking alcohol as this can in crease the risk of seizures.

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Risk of Topiramate

Topiramate is a white crystalline powder with a bitter taste. It is most soluble in alkaline solutions containing sodium hydroxide or sodium phosphate and having a pH of 9 to 10. It is freely soluble in acetone, chloroform, dimethylsulfoxide, and ethanol. The solubility in water is 9.8 mg/mL. Its saturated solution has a pH of 6.3.

Topiramate has the molecular formula C12H21NO8S and a molecular weight of 339.36, the CAS NO. is 97240-79-4. It is designated chemically as 2,3:4,5Di-O-isopropyliden-β-D-fructopyranose sulfamate.

Topiramate is an oral drug that is used to prevent the seizures of epilepsy. It is an anti-epileptic or anti-seizure drug. It is used primarily among patients who are not controlled by other anti-epileptic drugs. About 1 in 4 Americans diagnosed with epilepsy has seizures that resist treatment with other anti-epileptic drugs. It also prevents migraine headaches.

A GlaxoSmithKline-sponsored Phase IV study suggested that cognitive side effects may be more common with topiramate than with lamotrigine. In studies of healthy volunteers, therapeutic doses of topiramate for bipolar disorder produced greater cognitive deficits than lamotrigine, including short term memory loss and word-finding difficulty.

Side-effects reported by > 10% of subjects in at least one clinical study (listed by prevalence):

paresthesia (numbness & tingling) (23.7%)
upper respiratory tract infection (17.5%)
diarrhea (16.8%)
nausea (15.4%)
anorexia (loss of appetite) (13.3%)
memory problems (11.2%)

Side-effects most frequently leading to discontinuation of therapy with topiramate:

psychomotor slowing (4.1%)
memory problems (3.3%)
fatigue (3.3%)
confusion (3.2%)
somnolence (3.2%)

That same study also reported that in adult patients with Bipolar 1 disorder who were already receiving either lithium or valproate, the addition of topiramate did not produce a statistically significant improvement versus placebo, while adding the above adverse reactions.

Rarely, the inhibition of carbonic anhydrase may be strong enough to cause metabolic acidosis of clinical importance.

The U.S. Food and Drug Administration (FDA) has notified prescribers that topiramate can cause acute myopia and secondary angle closure glaucoma in a small subset of people who take this medicine regularly. The symptoms, which typically begin in the first month of use, include blurred vision and eye pain. Discontinuation of this medicine may halt the progression of the ocular damage, and may reverse the visual impairment.

Preliminary data suggests that, as with several other anti-epileptic drugs, topiramate carries an increased risk of congenital malformations. This might be particularly important for women who take this medicine to prevent migraine attacks. In March 2011 the FDA notified healthcare professionals and patients of an increased risk of development of cleft lip and/or cleft palate (oral clefts) in infants born to women treated with topiramate during pregnancy and placed it in Pregnancy Category D.

Topiramate has been associated with a statistically significant increase in suicidality, and "suicidal thoughts or actions" is now listed as one of the possible side effects of the drug "in a very small number of people, about 1 in 500."

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