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Topiramate

Topiramate structure

CAS No:
97240-79-4
Formula:
C12H21NO8S
Chemical Name:
Topiramate
Synonyms:
β-D-Fructopyranose,2,3:4,5-bis-O-(1-methylethylidene)-,1-sulfamate;β-D-Fructopyranose,2,3:4,5-bis-O-(1-methylethylidene)-,sulfamate;5H-Bis[1,3]dioxolo[4,5-b:4′,5′-d]pyran,β-D-fructopyranose deriv.;Topiramate;McN 4853;RWJ 17021;2,3:4,5-Bis-O-(1-methylethylidene) β-D-fructopyranose sulfamate;Topomax;Topamax;Epitomax;Topimax;Topamac;TPM;Epitoma;Topina;Sincronil;Qudexy XR;Trokendi XR;Topiragen;1103510-60-6
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

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Description

White-to-Off-White Crystalline Powder

Topiramate Basic Attributes

Molecular Weight：

339.36

Exact Mass：

339.36

EC Number：

200-659-6

HScode：

29350090

Characteristics

PSA：

124

XLogP3：

-0.8

Appearance：

white solid

Density：

1.336±0.06 g/cm3(Predicted)

Melting Point：

125-126 °C

Boiling Point：

438.7°C at 760 mmHg

Flash Point：

9℃

Refractive Index：

1.497

Water Solubility：

DMSO: ~44 mg/mL

Storage Conditions：

2-8°C

Vapor Pressure：

7.0X10-8 mm Hg at 25 deg C (est)

Toxicity：

LD50 intraperitoneal in rat: > 1500mg/kg

Specific rotation：

D23 -34.0° (c = 0.4 in methanol)

Taste：

Bitter

PH：

pH= 6.3 (saturated solution)

PKA：

8.7None

Safety Information

Transport codes：

UN1230 - class 3 - PG 2 - Methanol, solution

wgk germany：

hazard class code：

36/37/38-39/23/24/25-23/24/25-11

safety instructions：

26-36-45-36/37-16-7

RTECS Number：

LS7083000

Marks：

Xi,T,F

Stability/Shelf Life：

Stable if stored as directed.

Precautionary statement(s)：

P201, P202, P260, P264, P270, P281, P308+P313, P309+P311, P314, P405, P501

Hazard Statements：

H351

Topiramate Use and Manufacturing

Used as an anticonvulsant

Drug Function and Efficacy

1. Block state-dependent sodium channels; 2. Enhance the ability of GABA to induce chloride influx, and may regulate GABA receptor subtypes that are insensitive to benzodiazepines; 3. Antagonize the excitatory amino acid Kainate/AMPA subtype initiated by kainic acid; 4. Inhibit the action of some carbonic anhydrase isoenzymes (non-primary anti-epileptic properties); 5. Show synergistic anticonvulsant effects when used in combination with carbamazepine or phenobarbital, and show additive anticonvulsant effects when used in combination with phenytoin; 6. No human tolerance has been observed.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Topiramate Capsules
Ingredients	Chemical name: 2,3:4,5-bis-0-(1-methylethylidene)-β-D-pyranose sulfamate, molecular formula: C12H21NO8S, molecular weight: 339.36.
Indication	Effect of Topiramate on Other Antiepileptic Drugs When topiramate is co-administered with other antiepileptic drugs (phenytoin, carbamazepine, valproic acid, phenobarbital, primidone), topiramate has no effect on the steady-state plasma concentrations of other drugs, except that in very few patients, topiramate and phenytoin co-administration may lead to increased phenytoin plasma concentrations. This may be due to the inhibition of a polymorphic isomer of a specific enzyme (CPY2Cmeph). Therefore, any patient taking phenytoin and developing clinical signs or symptoms of toxicity should have their plasma phenytoin concentration monitored. Effect of Other Antiepileptic Drugs on Topiramate Phenytoin and carbamazepine can reduce the plasma concentration of topiramate. During topiramate treatment, the addition or withdrawal of phenytoin or carbamazepine may require an adjustment of the topiramate dose, which should be based on clinical efficacy. The addition or withdrawal of valproic acid does not produce clinically significant changes in the plasma concentration of topiramate, so no adjustment of the topiramate dose is required.
Specifications	15 mg

Topiramate

Topiramate Capsules
Ingredients	Active ingredient: Topiramate. Molecular weight: C12H21NO8S
Indication	Effects of this product on other anti-epileptic drugs When topiramate is used in combination with other anti-epileptic drugs (phenytoin, carbamazepine, valproic acid, phenobarbital, primidone), topiramate has no effect on the steady-state plasma concentrations of other drugs, except that in a very small number of patients, topiramate and phenytoin co-administration may lead to increased phenytoin plasma concentrations. The effect on phenytoin may be due to the inhibition of polymorphic isomers of a certain enzyme (CYP2Cmeph). Therefore, any patient taking phenytoin who develops clinical toxic symptoms or abnormal signs should have their plasma phenytoin concentration monitored. A drug interaction pharmacokinetic study in epileptic patients showed that when taking lamotrigine, the addition of a daily dose of 100 mg to 400 mg of topiramate did not increase the effects of lamotrigine.
Specifications	25mg

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Registered Holders

UNIMARK REMEDIES LTD

United States
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ALIVUS LIFE SCIENCES LTD

United States
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APITORIA PHARMA PRIVATE LTD

United States
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