pharmacopeia
GET
/api/v1/drug/topiramate
2D structure
[(1R,2S,6S,9R)-4,4,11,11-tetramethyl-3,5,7,10,12-pentaoxatricyclo[7.3.0.02,6]dodecan-6-yl]methyl sulfamate
SMILES CC1(O[C@@H]2CO[C@@]3([C@H]([C@@H]2O1)OC(O3)(C)C)COS(=O)(=O)N)C
InChIKey KJADKKWYZYXHBB-XBWDGYHZSA-N

Mechanism of action

Sourced from openFDA

The precise mechanisms by which topiramate exerts its anticonvulsant and preventive migraine effects are unknown; however, preclinical studies have revealed four properties that may contribute to topiramate's efficacy for epilepsy and the preventive treatment of migraine. Electrophysiological and biochemical evidence suggests that topiramate, at pharmacologically relevant concentrations, blocks voltage-dependent sodium channels, augments the activity of the neurotransmitter gamma-aminobutyrate at some subtypes of the GABA-A receptor, antagonizes the AMPA/kainate subtype of the glutamate receptor, and inhibits the carbonic anhydrase enzyme, particularly isozymes II and IV.

Cytochrome P450 2C19

Indications

Sourced from openFDA
  • Topiramate is indicated for: Epilepsy: initial monotherapy for the treatment of partial-onset or primary generalized tonic-clonic seizures in patients 2 years of age and older (1.1); adjunctive therapy for the treatment of partial-onset seizures, primary generalized tonic-clonic seizures, or seizures associated with Lennox- Gastaut syndrome in patients 2 years of age and older (1.2) Preventive treatment of migraine in patients 12 years of age and older (1.3) 1.1 Monotherapy Epilepsy Topiramate tablets are indicated as initial monotherapy for the treatment of partial-onset or primary generalized tonic-clonic seizures in patients 2 years of age and older. 1.2 Adjunctive Therapy Epilepsy Topiramate tablets are indicated as adjunctive therapy for the treatment of partial-onset seizures, primary generalized tonic-clonic seizures, and seizures associated with Lennox-Gastaut syndrome in patients 2 years of age and older.ICD-10: G40.909, G43.909

Contraindications

Sourced from openFDA
  • Topiramate is contraindicated in patients with a history of hypersensitivity reaction to topiramate, topiramate tablet or any of the inactive ingredients of topiramate tablet.contraindicated

Dosage & administration

Sourced from openFDA

Topiramate initial dose, titration, and recommended maintenance dose varies by indication and age group. See Full Prescribing Information for recommended dosage, and dosing considerations in patients with renal impairment, geriatric patients, and patients undergoing hemodialysis (2.1, 2.2, 2.3, 2.4, 2.5, 2.6) 2.1 Dosing in Monotherapy Epilepsy Adults and Pediatric Patients 10 Years of Age and Older The recommended dose for topiramate monotherapy in adults and pediatric patients 10 years of age and older is 400 mg/day in two divided doses. The dose should be achieved by titration according to the following schedule (Table 1): Table 1: Monotherapy Titration Schedule for Adults and Pediatric Patients 10 years and older Morning Dose Evening Dose Week 1 25 mg 25 mg Week 2 50 mg 50 mg Week 3 75 mg 75 mg Week 4 100 mg 100 mg Week 5 150 mg 150 mg Week 6 200 mg 200 mg Pediatric Patients 2 to 9 Years of Age Dosing in patients 2 to 9 years of age is based on weight. During the titration period, the initial dose of topiramate is 25 mg/day nightly for the first week. Based upon tolerability, the dosage can be increased to 50 mg/day (25 mg twice daily) in the second week. Dosage can be increased by 25 to 50 mg/day each subsequent week as tolerated. Titration to the minimum maintenance dose should be attempted over 5 to 7 weeks of the total titration period. Based upon tolerability and clinical response, additional titration to a higher dose (up to the maximum maintenance dose) can be attempted at 25 to 50 mg/day weekly increments.

Warnings & precautions

Sourced from openFDA

Acute myopia and secondary angle closure glaucoma: can lead to permanent visual loss; discontinue topiramate as soon as possible (5.1) Visual field defects: consider discontinuation of topiramate (5.2) Oligohidrosis and hyperthermia: monitor decreased sweating and increased body temperature, especially in pediatric patients (5.3) Metabolic acidosis: baseline and periodic measurement of serum bicarbonate is recommended; consider dose reduction or discontinuation of topiramate if clinically appropriate (5.4) Suicidal behavior and ideation: antiepileptic drugs increase the risk of suicidal behavior or ideation (5.5) Cognitive/neuropsychiatric adverse reactions: use caution when operating machinery including cars; depression and mood problems may occur (5.6) Fetal Toxicity: use during pregnancy can cause major congenital malformations, including but not limited to cleft lip and/or palate, and being small for gestational age (5.7) Withdrawal of AEDs: withdraw topiramate gradually (5.8) Decrease in Bone Mineral Density: has been shown to decrease bone mineral density and bone mineral content in pediatric patients (5.9) Negative effects on growth (height and weight): may slow height increase and weight gain; carefully monitor children receiving prolonged therapy (5.10) Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)/ Multiorgan Hypersensitivity, serious skin reactions (SJS or TEN), anaphylaxis, and angioedema: Discontinue topiramate if an alternative etiology cannot be established (5.11, 5.12, 5.13) Hyperammonemia/encephalopathy: measure ammonia if encephalopathic sy…

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are discussed in more detail in other sections of the labeling: Acute Myopia and Secondary Angle Closure Glaucoma [see Warnings and Precautions (5.1)] Visual Field Defects [see Warnings and Precautions (5.2)] Oligohidrosis and Hyperthermia [see Warnings and Precautions (5.3)] Metabolic Acidosis [see Warnings and Precautions (5.4)] Suicidal Behavior and Ideation [see Warnings and Precautions (5.5)] Cognitive/Neuropsychiatric Adverse Reactions [see Warnings and Precautions (5.6)] Decrease of Bone Mineral Density [see Warnings and Precautions (5.9)] Negative Effects on Growth (Height and Weight) [see Warnings and Precautions (5.10)] Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)/Multiorgan Hypersensitivity Reactions [ see Warnings and Precautions (5.11) ] Serious Skin Reactions [see Warnings and Precautions (5.12)] Anaphylaxis and Angioedema [see Warnings and Precautions (5.13)] Hyperammonemia and Encephalopathy (Without and With Concomitant Valproic Acid [VPA] Use) [see Warnings and Precautions (5.14)] Kidney Stones [see Warnings and Precautions (5.15)] Hypothermia with Concomitant Valproic Acid (VPA) Use [see Warnings and Precautions (5.16)] The data described in the following sections were obtained using topiramate tablets.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to topiramate during pregnancy. Patients should be encouraged to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry if they become pregnant. This registry is collecting information about the safety of antiepileptic drugs during pregnancy. To enroll, patients can call the toll-free number 1-888-233-2334. Information about the North American Drug Pregnancy Registry can be found at http://www.aedpregnancyregistry.org/ . Risk Summary Topiramate can cause fetal harm when administered to a pregnant woman. Data from pregnancy registries indicate that infants exposed to topiramate in utero have an increased risk of major congenital malformations, including but not limited to cleft lip and/or cleft palate (oral clefts), and of being small for gestational age (SGA) [see Human Data] . SGA has been observed at all doses and appears to be dose-dependent. The prevalence of SGA is greater in infants of women who received higher doses of topiramate during pregnancy. In addition, the prevalence of SGA in infants of women who continued topiramate use until later in pregnancy is higher compared to the prevalence in infants of women who stopped topiramate use before the third trimester.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption of topiramate is rapid, with peak plasma concentrations occurring at approximately 2 hours following a 400 mg oral dose. The relative bioavailability of topiramate from the tablet formulation is about 80% compared to a solution.

Overdosage

Sourced from openFDA

Overdoses of topiramate have been reported. Signs and symptoms included convulsions, drowsiness, speech disturbance, blurred vision, diplopia, impaired mentation, lethargy, abnormal coordination, stupor, hypotension, abdominal pain, agitation, dizziness and depression. The clinical consequences were not severe in most cases, but deaths have been reported after overdoses involving topiramate. Topiramate overdose has resulted in severe metabolic acidosis [see Warnings and Precautions (5.4)]. A patient who ingested a dose of topiramate between 96 and 110 g was admitted to a hospital with a coma lasting 20 to 24 hours followed by full recovery after 3 to 4 days. In the event of overdose, topiramate should be discontinued and general supportive treatment given until clinical toxicity has been diminished or resolved. Hemodialysis is an effective means of removing topiramate from the body.

Approval history

Sourced from openFDA
  • Dec 24, 1996NDANDA020505Janssen Pharms
  • Oct 26, 1998NDANDA020844Janssen Pharms
  • Mar 27, 2009ANDAANDA078462Aurobindo Pharma
  • Mar 27, 2009ANDAANDA077627Glenmark Pharms Ltd
  • Jul 17, 2012NDANDA022580Vivus Llc
  • Aug 16, 2013NDANDA201635Supernus Pharms
  • Mar 11, 2014NDANDA205122Upsher Smith Labs
  • Nov 5, 2021NDANDA214679Azurity

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
97,080 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective10,32411%
  2. 2Off Label Use7,4547.7%
  3. 3Headache6,9127.1%
  4. 4Nausea6,0446.2%
  5. 5Fatigue5,5935.8%
  6. 6Pain4,6074.7%
  7. 7Migraine4,5094.6%
  8. 8Dizziness4,4644.6%
  9. 9Seizure3,8504.0%
  10. 10Diarrhoea3,7583.9%
  11. 11Depression3,7553.9%
  12. 12Vomiting3,6843.8%
  13. 13Weight Increased3,2643.4%
  14. 14Paraesthesia3,2453.3%
  15. 15Product Use In Unapproved Indication3,1333.2%

Literature

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Recent PubMed references pinned to Topiramate as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 334 ClinicalTrials.gov registrations naming Topiramate as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Topiramate work?
The precise mechanisms by which topiramate exerts its anticonvulsant and preventive migraine effects are unknown; however, preclinical studies have revealed four properties that may contribute to topiramate's efficacy for epilepsy and the preventive treatment of migraine. Electrophysiological and biochemical evidence suggests that topiramate, at pharmacologically relevant concentrations, blocks voltage-dependent sodium channels, augments the activity of the neurotransmitter gamma-aminobutyrate at some subtypes of the GABA-A receptor, antagonizes the AMPA/kainate subtype of the glutamate receptor, and inhibits the carbonic anhydrase enzyme, particularly isozymes II and IV.
What is Topiramate used for?
According to FDA labeling, Topiramate carries indications including: Topiramate is indicated for: Epilepsy: initial monotherapy for the treatment of partial-onset or primary generalized tonic-clonic seizures in patients 2 years of age and older (1.1); adjunctive therapy for the treatment of partial-onset seizures, primary generalized tonic-clonic seizures, or seizures associated with Lennox- Gastaut syndrome in patients 2 years of age and older (1.2) Preventive treatment of migraine in patients 12 years of age and older (1.3) 1.1 Monotherapy Epilepsy Topiramate tablets are indicated as initial monotherapy for the treatment of partial-onset or primary generalized tonic-clonic seizures in patients 2 years of age and older. 1.2 Adjunctive Therapy Epilepsy Topiramate tablets are indicated as adjunctive therapy for the treatment of partial-onset seizures, primary generalized tonic-clonic seizures, and seizures associated with Lennox-Gastaut syndrome in patients 2 years of age and older.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Topiramate?
Topiramate is classified as Other antiepileptics, Cytochrome P450 2C19 Inhibitors, Cytochrome P450 3A4 Inducers, Sodium Channel Interactions, Decreased Central Nervous System Disorganized Electrical Activity, Decreased Glutamate Activity, Increased GABA Activity.
What are the brand names for Topiramate?
Topiramate is marketed under brand names including Eprontia, Qsymia, Qudexy, Topamax, Trokendi.
What are the contraindications for Topiramate?
Topiramate labeling lists contraindications including: Topiramate is contraindicated in patients with a history of hypersensitivity reaction to topiramate, topiramate tablet or any of the inactive ingredients of topiramate tablet.. Always consult the full prescribing information and a clinician.
Note. Data for topiramate is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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