Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C12H21NO8S |
Molecular Weight | 339.362 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CO[C@@]3(COS(N)(=O)=O)OC(C)(C)O[C@@]3([H])[C@]1([H])OC(C)(C)O2
InChI
InChIKey=KJADKKWYZYXHBB-XBWDGYHZSA-N
InChI=1S/C12H21NO8S/c1-10(2)18-7-5-16-12(6-17-22(13,14)15)9(8(7)19-10)20-11(3,4)21-12/h7-9H,5-6H2,1-4H3,(H2,13,14,15)/t7-,8-,9+,12+/m1/s1
Molecular Formula | C12H21NO8S |
Molecular Weight | 339.362 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.drugbank.ca/drugs/DB00273Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020505s055,020844s046lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB00273
Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020505s055,020844s046lbl.pdf
Topiramate is an anticonvulsant indicated in the treatment of epilepsy and migraine. Topiramate enhances GABA-activated chloride channels. In addition, topiramate inhibits excitatory neurotransmission, through actions on kainate and AMPA receptors. There is evidence that topiramate has a specific effect on GluR5 kainate receptors. It is also an inhibitor of carbonic anhydrase, particular subtypes II and IV, but this action is weak and unlikely to be related to its anticonvulsant actions, but may account for the bad taste and the development of renal stones seen during treatment. Its possible effect as a mood stabilizer seems to occur before anticonvulsant qualities at lower dosages. Topiramate inhibits maximal electroshock and pentylenetetrazol-induced seizures as well as partial and secundarily generalized tonic-clonic seizures in the kindling model, findings predective of a broad spectrum of antiseizure activities clinically. The precise mechanism of action of topiramate is not known. However, studies have shown that topiramate blocks the action potentials elicited repetitively by a sustained depolarization of the neurons in a time-dependent manner, suggesting a state-dependent sodium channel blocking action. Topiramate also augments the activity of the neurotransmitter gamma-aminobutyrate (GABA) at some subtypes of the GABAAreceptor (controls an integral chloride channel), indicating a possible mechanism through potentiation of the activity of GABA. Topiramate also demonstrates antagonism of the AMPA/kainate subtype of the glutamate excitatory amino acid receptor. It also inhibits carbonic anhydrase (particularly isozymes II and IV), but this action is weak and unlikely to be related to its anticonvulsant actions. Topiramate is used for the treatment and control of partial seizures and severe tonic-clonic (grand mal) seizures and also for the prevention of migraine headaches. In children it is also used for treatment of Lennox-Gastaut syndrome. Topiramate is sold under the brand name Topamax. A combination product containing phentermine and topiramate extended-release called QSYMIA® is indicated for the management of obesity.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL205 |
5.0 nM [Ki] | ||
Target ID: CHEMBL3729 |
4.9 µM [Ki] | ||
Target ID: CHEMBL2326 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26915563 |
0.9 nM [Ki] | ||
Target ID: CHEMBL3242 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15686894 |
3.8 nM [Ki] | ||
Target ID: CHEMBL1962 Sources: http://www.drugbank.ca/drugs/DB00273 |
|||
Target ID: CHEMBL4789 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18640037 |
63.0 nM [Ki] | ||
Target ID: CHEMBL3969 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18640037 |
30.0 nM [Ki] | ||
Target ID: CHEMBL3912 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18640037 |
47.0 nM [Ki] | ||
Target ID: CHEMBL1845 Sources: http://www.drugbank.ca/drugs/DB00273 |
|||
Target ID: CHEMBL2093872 |
|||
Target ID: CHEMBL2109241 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | TOPAMAX Approved UseTOPAMAX is indicated for:
Monotherapy epilepsy: Initial monotherapy in patients > 2 years of age with partial onset or primary generalized tonic-clonic seizures
Adjunctive therapy epilepsy: Adjunctive therapy for adults and pediatric patients (2 to 16 years of age) with partial onset seizures or primary generalized tonic-clonic seizures, and in patients >2 years of age with
seizures associated with Lennox-Gastaut syndrome (LGS)
Migraine: Treatment for adults and adolescents 12 years of age and older for prophylaxis of migraine headache Launch Date1996 |
|||
Preventing | TOPAMAX Approved UseTOPAMAX is indicated for:
Monotherapy epilepsy: Initial monotherapy in patients > 2 years of age with partial onset or primary generalized tonic-clonic seizures
Adjunctive therapy epilepsy: Adjunctive therapy for adults and pediatric patients (2 to 16 years of age) with partial onset seizures or primary generalized tonic-clonic seizures, and in patients >2 years of age with
seizures associated with Lennox-Gastaut syndrome (LGS)
Migraine: Treatment for adults and adolescents 12 years of age and older for prophylaxis of migraine headache Launch Date1996 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.98 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.46 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
1.63 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
18.38 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
28.73 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.68 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
350.3 mg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
311.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
57.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
59.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
18.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
22 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8930774 |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOPIRAMATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
59% |
unknown, unknown |
TOPIRAMATE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1200 mg 1 times / day steady, oral MTD Dose: 1200 mg, 1 times / day Route: oral Route: steady Dose: 1200 mg, 1 times / day Sources: |
healthy, 23.3 years (range: 20–26 years) n = 8 Health Status: healthy Age Group: 23.3 years (range: 20–26 years) Sex: M+F Population Size: 8 Sources: |
|
4000 mg single, oral Overdose |
unknown, 24 years n = 1 Health Status: unknown Age Group: 24 years Sex: F Population Size: 1 Sources: |
|
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 6-15 years n = 77 Health Status: unhealthy Condition: Epilepsy Age Group: 6-15 years Population Size: 77 Sources: |
Disc. AE: Attention concentration difficulty, Fever... AEs leading to discontinuation/dose reduction: Attention concentration difficulty (>=2) Sources: Fever (>=2) Flushing (>=2) Confusion (>=2) |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, >16 years n = 159 Health Status: unhealthy Condition: Epilepsy Age Group: >16 years Population Size: 159 Sources: |
Disc. AE: Memory impairment, Fatigue... AEs leading to discontinuation/dose reduction: Memory impairment (>=2) Sources: Fatigue (>=2) Asthenia (>=2) Insomnia (>=2) Somnolence (>=2) Paresthesia (>=2) |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Disc. AE: Psychomotor retardation, Memory impairment... AEs leading to discontinuation/dose reduction: Psychomotor retardation (4%) Sources: Memory impairment (3.2%) Fatigue (3.2%) Confusion (3.1%) Somnolence (3.2%) Attention concentration difficulty (2.9%) Anorexia (2.7%) Depression (2.6%) Dizziness (2.5%) Weight decrease (2.5%) Nervousness (2.3%) Ataxia (2.1%) Paresthesia (2%) |
30 mg/kg 1 times / day steady, oral Dose: 30 mg/kg, 1 times / day Route: oral Route: steady Dose: 30 mg/kg, 1 times / day Sources: |
unhealthy, pediatric (<16 years) n = 310 Health Status: unhealthy Condition: epilepsy Age Group: pediatric (<16 years) Population Size: 310 Sources: |
Disc. AE: Convulsions aggravated, Attention concentration difficulty... AEs leading to discontinuation/dose reduction: Convulsions aggravated (2.3%) Sources: Attention concentration difficulty (1.6%) Language disorder (1.3%) Personality disorder (1.3%) Somnolence (1.3%) |
96 g single, oral Overdose Dose: 96 g Route: oral Route: single Dose: 96 g Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
Other AEs: Coma... Other AEs: Coma (1 patient) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Attention concentration difficulty | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 6-15 years n = 77 Health Status: unhealthy Condition: Epilepsy Age Group: 6-15 years Population Size: 77 Sources: |
Confusion | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 6-15 years n = 77 Health Status: unhealthy Condition: Epilepsy Age Group: 6-15 years Population Size: 77 Sources: |
Fever | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 6-15 years n = 77 Health Status: unhealthy Condition: Epilepsy Age Group: 6-15 years Population Size: 77 Sources: |
Flushing | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 6-15 years n = 77 Health Status: unhealthy Condition: Epilepsy Age Group: 6-15 years Population Size: 77 Sources: |
Asthenia | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, >16 years n = 159 Health Status: unhealthy Condition: Epilepsy Age Group: >16 years Population Size: 159 Sources: |
Fatigue | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, >16 years n = 159 Health Status: unhealthy Condition: Epilepsy Age Group: >16 years Population Size: 159 Sources: |
Insomnia | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, >16 years n = 159 Health Status: unhealthy Condition: Epilepsy Age Group: >16 years Population Size: 159 Sources: |
Memory impairment | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, >16 years n = 159 Health Status: unhealthy Condition: Epilepsy Age Group: >16 years Population Size: 159 Sources: |
Paresthesia | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, >16 years n = 159 Health Status: unhealthy Condition: Epilepsy Age Group: >16 years Population Size: 159 Sources: |
Somnolence | >=2 Disc. AE |
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, >16 years n = 159 Health Status: unhealthy Condition: Epilepsy Age Group: >16 years Population Size: 159 Sources: |
Paresthesia | 2% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Ataxia | 2.1% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Nervousness | 2.3% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Dizziness | 2.5% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Weight decrease | 2.5% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Depression | 2.6% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Anorexia | 2.7% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Attention concentration difficulty | 2.9% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Confusion | 3.1% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Fatigue | 3.2% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Memory impairment | 3.2% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Somnolence | 3.2% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Psychomotor retardation | 4% Disc. AE |
1400 mg 1 times / day steady, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: steady Dose: 1400 mg, 1 times / day Sources: |
unhealthy, adult (>16 years) n = 1757 Health Status: unhealthy Condition: epilepsy Age Group: adult (>16 years) Sex: M+F Population Size: 1757 Sources: |
Language disorder | 1.3% Disc. AE |
30 mg/kg 1 times / day steady, oral Dose: 30 mg/kg, 1 times / day Route: oral Route: steady Dose: 30 mg/kg, 1 times / day Sources: |
unhealthy, pediatric (<16 years) n = 310 Health Status: unhealthy Condition: epilepsy Age Group: pediatric (<16 years) Population Size: 310 Sources: |
Personality disorder | 1.3% Disc. AE |
30 mg/kg 1 times / day steady, oral Dose: 30 mg/kg, 1 times / day Route: oral Route: steady Dose: 30 mg/kg, 1 times / day Sources: |
unhealthy, pediatric (<16 years) n = 310 Health Status: unhealthy Condition: epilepsy Age Group: pediatric (<16 years) Population Size: 310 Sources: |
Somnolence | 1.3% Disc. AE |
30 mg/kg 1 times / day steady, oral Dose: 30 mg/kg, 1 times / day Route: oral Route: steady Dose: 30 mg/kg, 1 times / day Sources: |
unhealthy, pediatric (<16 years) n = 310 Health Status: unhealthy Condition: epilepsy Age Group: pediatric (<16 years) Population Size: 310 Sources: |
Attention concentration difficulty | 1.6% Disc. AE |
30 mg/kg 1 times / day steady, oral Dose: 30 mg/kg, 1 times / day Route: oral Route: steady Dose: 30 mg/kg, 1 times / day Sources: |
unhealthy, pediatric (<16 years) n = 310 Health Status: unhealthy Condition: epilepsy Age Group: pediatric (<16 years) Population Size: 310 Sources: |
Convulsions aggravated | 2.3% Disc. AE |
30 mg/kg 1 times / day steady, oral Dose: 30 mg/kg, 1 times / day Route: oral Route: steady Dose: 30 mg/kg, 1 times / day Sources: |
unhealthy, pediatric (<16 years) n = 310 Health Status: unhealthy Condition: epilepsy Age Group: pediatric (<16 years) Population Size: 310 Sources: |
Coma | 1 patient | 96 g single, oral Overdose Dose: 96 g Route: oral Route: single Dose: 96 g Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Effects of anti-epileptic drugs on glutamine synthetase activity in mouse brain. | 1999 Apr |
|
Topiramate increases brain GABA, homocarnosine, and pyrrolidinone in patients with epilepsy. | 1999 Feb |
|
Acute psychotic symptoms induced by topiramate. | 1999 Jun |
|
Valproate-induced hyperammonemic encephalopathy in the presence of topiramate. | 2000 Jan 11 |
|
A comparison of topiramate and acetazolamide on seizure duration and paired-pulse inhibition in the dentate gyrus of the rat. | 2000 Jul |
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Cutaneous drug reaction case reports: from the world literature. | 2001 |
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The new generation of GABA enhancers. Potential in the treatment of epilepsy. | 2001 |
|
Cognitive side effects of anticonvulsants. | 2001 |
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Validation of liquid-liquid extraction followed by flow-injection negative ion electrospray mass spectrometry assay to Topiramate in human plasma. | 2001 |
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Topiramate rapidly raises brain GABA in epilepsy patients. | 2001 Apr |
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Novel treatments for bipolar disorder. | 2001 Apr |
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First break of mania associated with topiramate treatment. | 2001 Aug |
|
Topiramate in venlafaxine-induced visual hallucinations in an obese patient with a posterior cerebral artery infarction. | 2001 Aug |
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Pharmacological characterization of the 6 Hz psychomotor seizure model of partial epilepsy. | 2001 Dec |
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Topiramate selectively attenuates nicotine-induced increases in monoamine release. | 2001 Dec 1 |
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Treatment and management of cluster headache. | 2001 Feb |
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Effect of tiagabine and topiramate on porphyrin metabolism in an in vivo model of porphyria. | 2001 Jul |
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A pilot study of topiramate as monotherapy in the treatment of acute mania. | 2001 Jun |
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Control of Tourette's syndrome with topiramate. | 2001 Jun |
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Topiramate for clozapine-induced seizures. | 2001 Jun |
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Cognitive changes during topiramate therapy. | 2001 Mar |
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Topiramate in refractory partial-onset seizures in children, adolescents and young adults: a multicentric open trial. | 2001 Mar |
|
[Social and economic aspects of administration of new antiepileptic drugs]. | 2001 Mar-Apr |
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New anticonvulsants for use in pediatric patients (part I). | 2001 Mar-Apr |
|
National survey on West syndrome in Korea. | 2001 Nov |
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Review of treatment options for refractory epilepsy: new medications and vagal nerve stimulation. | 2001 Nov |
|
Topiramate-induced metabolic acidosis: report of two cases. | 2001 Oct |
|
Topiramate as a neuroprotectant in a rat model of global ischemia-induced neurodegeneration. | 2001 Sep 28 |
|
Treatment-resistant bipolar disorder. | 2001 Winter |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/topiramate.html
Recommended dose: 400 mg orally per day in 2 divided doses of 200 mg each
The dose should be achieved by titration:
Week 1: 25 mg orally in the morning and 25 mg orally in the evening
Week 2: 50 mg orally in the morning and 50 mg orally in the evening
Week 3: 75 mg orally in the morning and 75 mg orally in the evening
Week 4: 100 mg orally in the morning and 100 mg orally in the evening
Week 5: 150 mg orally in the morning and 150 mg orally in the evening
Week 6: 200 mg orally in the morning and 200 mg orally in the evening
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19417176
0.3 to 10 uM topiramate 1 inhibited ATPA-evoked postsynaptic currents recorded from rat basolateral amygdala (BLA) interneurons
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:06:17 GMT 2023
by
admin
on
Fri Dec 15 15:06:17 GMT 2023
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Record UNII |
0H73WJJ391
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C264
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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WHO-ATC |
N03AX11
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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FDA ORPHAN DRUG |
283909
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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NDF-RT |
N0000008486
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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NDF-RT |
N0000175753
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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WHO-VATC |
QN03AX11
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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LIVERTOX |
NBK548632
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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FDA ORPHAN DRUG |
70792
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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EMA ASSESSMENT REPORTS |
QSIVA (REFUSED: OBESITY)
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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Code System | Code | Type | Description | ||
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N0000182140
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | Cytochrome P450 2C19 Inhibitors [MoA] | ||
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97240-79-4
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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Y-25
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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7531
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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2706
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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0H73WJJ391
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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TOPIRAMATE
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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Topiramate
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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63631
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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CHEMBL220492
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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1672206
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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m10976
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | Merck Index | ||
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100000092536
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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0H73WJJ391
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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6849
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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N0000185506
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | Cytochrome P450 3A4 Inducers [MoA] | ||
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6099
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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DTXSID8023688
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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5284627
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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C47764
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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C052342
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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38404
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | RxNorm | ||
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SUB11190MIG
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY | |||
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DB00273
Created by
admin on Fri Dec 15 15:06:17 GMT 2023 , Edited by admin on Fri Dec 15 15:06:17 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
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METABOLIC ENZYME -> INHIBITOR |
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||
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BINDER->LIGAND |
decreases as concentration increases
BINDING
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||
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TARGET -> AGONIST |
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||
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OFF-TARGET->INHIBITOR |
Believed to be responsible for adverse events.
Ki
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TARGET -> INHIBITOR |
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OFF-TARGET->INHIBITOR |
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SALT/SOLVATE -> PARENT |
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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EXCRETED UNCHANGED |
URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
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METABOLITE -> PARENT |
MINOR
URINE
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||
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METABOLITE -> PARENT |
MINOR
URINE
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||
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METABOLITE -> PARENT |
MINOR
URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
|