Peringatan Keamanan

The LD50 of intraperitoneal topiramate in the rat is above 1500 mg/kg.L10547

Overdose information

In a study of 4 healthy adult women taking topiramate, the severity of clinical effects following an overdose ranged from asymptomatic to severe, with no deaths reported.A175258 According to the FDA prescribing information for topiramate, an overdose may cause hypotension, severe metabolic acidosis, coma, abdominal pain, visual disturbances, convulsions, drowsiness, speech abnormalities, impaired mentation and coordination, stupor, agitation, dizziness, as well as depression.L10544

In the case of a recent ingestion of topiramate, the stomach contents should be emptied through the induction of emesis or gastric lavage. Offer supportive treatment, including activated charcoal and hemodialysis.L10544

Topiramate

DB00273

small molecule approved

Deskripsi

Topiramate is a anti-epileptic drug used to manage seizures and prevent migraines.A175249 It was initially approved by the FDA in 1996. In 2004, topiramate was approved for the prevention of migraine in adults.A188309,L10544,L43478 Since 2012, the extended-release formulation has been approved in combination with phentermine for chronic weight management therapy in adults.L10550

Characteristics that distinguish topiramate from other antiepileptic drugs are a monosaccharide chemical structure containing a sulfamate, and 40% of its mass accounted for by oxygen.A175249 Interestingly, topiramate was discovered by chance when attempts were made to formulate a novel antidiabetic drug.A188330

Struktur Molekul 2D

Berat 339.362
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life is reported to be in the range of 19-23 hours.[A175246] If topiramate is given with enzyme-inducers, the half-life can be reduced to 12-15 hours because of increased metabolism.[A175246]
Volume Distribusi The mean apparent volume of distribution of topiramate ranges from 0.6-0.8 L/kg when doses of 100mg to 1200mg are given.[A175246] Topiramate readily crosses the blood-brain barrier.[A175249]
Klirens (Clearance) The mean oral plasma clearance of topiramate ranges from 22-36 mL/min while the renal clearance is 17-18 mL/min, according to one pharmacokinetic study.[A175246] The FDA label for topiramate indicates a similar oral plasma clearance of approximately 20 to 30 mL/min in adults.[L10544]

Absorpsi

After a 400mg dose in one clinical trial, topiramate reached maximal concentrations within 1.8-4.3 hours and ranged from 1.73-28.7 ug/mL. Food did not significantly affect the extent of absorption, despite delaying time to peak concentration. In patients with normal creatinine clearance, steady state concentrations are reached within 4 days.A175246 The bioavailability of topiramate in tablet form is about 80% compared to a topiramate solution.L10544

Metabolisme

The metabolites of topiramate are not known to be active.A175237 The metabolism of topiramate is characterized by reactions of glucuronidation, hydroxylation and hydrolysis that lead to the production of six minor metabolites.L10544 Some of topiramate's metabolites include 2,3-desisopropylidene topiramate, 4,5-desisopropylidene topiramate, 9-hydroxy topiramate, and 10-hydroxy topiramate.A175282

Rute Eliminasi

Topiramate is mainly eliminated through the kidneys.A175243 About 70-80% of the eliminated dose is found unchanged in the urine.A175246,L10544

Interaksi Makanan

2 Data
  • 1. Avoid a ketogenic diet. This type of diet increases the risk of kidney stones.
  • 2. Take with or without food. Food slightly alters absorption but not to any clinically significant extent.

Interaksi Obat

1616 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Topiramate.
Buprenorphine Topiramate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Hydrocodone Topiramate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Magnesium sulfate The therapeutic efficacy of Topiramate can be increased when used in combination with Magnesium sulfate.
Metyrosine Topiramate may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Mirtazapine Topiramate may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Paraldehyde Topiramate may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Pramipexole Topiramate may increase the sedative activities of Pramipexole.
Ropinirole Topiramate may increase the sedative activities of Ropinirole.
Rotigotine Topiramate may increase the sedative activities of Rotigotine.
Sodium oxybate Topiramate may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Topiramate may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
Thalidomide Topiramate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Topiramate may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Tramadol The risk or severity of hyperthermia and oligohydrosis can be increased when Tramadol is combined with Topiramate.
Trospium The risk or severity of hyperthermia and oligohydrosis can be increased when Trospium is combined with Topiramate.
Oxyphenonium The risk or severity of hyperthermia and oligohydrosis can be increased when Oxyphenonium is combined with Topiramate.
Benzatropine The risk or severity of hyperthermia and oligohydrosis can be increased when Benzatropine is combined with Topiramate.
Ziprasidone The risk or severity of hyperthermia and oligohydrosis can be increased when Ziprasidone is combined with Topiramate.
Disopyramide The risk or severity of hyperthermia and oligohydrosis can be increased when Disopyramide is combined with Topiramate.
Amitriptyline The risk or severity of hyperthermia and oligohydrosis can be increased when Amitriptyline is combined with Topiramate.
Ipratropium The risk or severity of hyperthermia and oligohydrosis can be increased when Ipratropium is combined with Topiramate.
Olanzapine The risk or severity of hyperthermia and oligohydrosis can be increased when Olanzapine is combined with Topiramate.
Metixene The risk or severity of hyperthermia and oligohydrosis can be increased when Metixene is combined with Topiramate.
Terfenadine The risk or severity of hyperthermia and oligohydrosis can be increased when Terfenadine is combined with Topiramate.
Buclizine The risk or severity of hyperthermia and oligohydrosis can be increased when Buclizine is combined with Topiramate.
Clozapine The risk or severity of hyperthermia and oligohydrosis can be increased when Clozapine is combined with Topiramate.
Trihexyphenidyl The risk or severity of hyperthermia and oligohydrosis can be increased when Trihexyphenidyl is combined with Topiramate.
Oxyphencyclimine The risk or severity of hyperthermia and oligohydrosis can be increased when Oxyphencyclimine is combined with Topiramate.
Procyclidine The risk or severity of hyperthermia and oligohydrosis can be increased when Procyclidine is combined with Topiramate.
Profenamine The risk or severity of hyperthermia and oligohydrosis can be increased when Profenamine is combined with Topiramate.
Promazine The risk or severity of hyperthermia and oligohydrosis can be increased when Promazine is combined with Topiramate.
Hyoscyamine The risk or severity of hyperthermia and oligohydrosis can be increased when Hyoscyamine is combined with Topiramate.
Cyproheptadine The risk or severity of hyperthermia and oligohydrosis can be increased when Cyproheptadine is combined with Topiramate.
Imipramine The risk or severity of hyperthermia and oligohydrosis can be increased when Imipramine is combined with Topiramate.
Methscopolamine bromide The risk or severity of hyperthermia and oligohydrosis can be increased when Methscopolamine bromide is combined with Topiramate.
Chlorpromazine The risk or severity of hyperthermia and oligohydrosis can be increased when Chlorpromazine is combined with Topiramate.
Gallamine triethiodide The risk or severity of hyperthermia and oligohydrosis can be increased when Gallamine triethiodide is combined with Topiramate.
Darifenacin The risk or severity of hyperthermia and oligohydrosis can be increased when Darifenacin is combined with Topiramate.
Tridihexethyl The risk or severity of hyperthermia and oligohydrosis can be increased when Tridihexethyl is combined with Topiramate.
Triflupromazine The risk or severity of hyperthermia and oligohydrosis can be increased when Triflupromazine is combined with Topiramate.
Anisotropine methylbromide The risk or severity of hyperthermia and oligohydrosis can be increased when Anisotropine methylbromide is combined with Topiramate.
Nortriptyline The risk or severity of hyperthermia and oligohydrosis can be increased when Nortriptyline is combined with Topiramate.
Amoxapine The risk or severity of hyperthermia and oligohydrosis can be increased when Amoxapine is combined with Topiramate.
Lamotrigine The risk or severity of CNS depression can be increased when Topiramate is combined with Lamotrigine.
Atropine The risk or severity of hyperthermia and oligohydrosis can be increased when Atropine is combined with Topiramate.
Nicardipine The risk or severity of hyperthermia and oligohydrosis can be increased when Nicardipine is combined with Topiramate.
Pirenzepine The risk or severity of hyperthermia and oligohydrosis can be increased when Pirenzepine is combined with Topiramate.
Paroxetine The risk or severity of hyperthermia and oligohydrosis can be increased when Paroxetine is combined with Topiramate.
Homatropine methylbromide The risk or severity of hyperthermia and oligohydrosis can be increased when Homatropine methylbromide is combined with Topiramate.
Rocuronium The risk or severity of hyperthermia and oligohydrosis can be increased when Rocuronium is combined with Topiramate.
Scopolamine The risk or severity of hyperthermia and oligohydrosis can be increased when Scopolamine is combined with Topiramate.
Benzquinamide The risk or severity of hyperthermia and oligohydrosis can be increased when Benzquinamide is combined with Topiramate.
Clidinium The risk or severity of hyperthermia and oligohydrosis can be increased when Clidinium is combined with Topiramate.
Propiomazine The risk or severity of hyperthermia and oligohydrosis can be increased when Propiomazine is combined with Topiramate.
Propantheline The risk or severity of hyperthermia and oligohydrosis can be increased when Propantheline is combined with Topiramate.
Dicyclomine The risk or severity of hyperthermia and oligohydrosis can be increased when Dicyclomine is combined with Topiramate.
Biperiden The risk or severity of hyperthermia and oligohydrosis can be increased when Biperiden is combined with Topiramate.
Brompheniramine The risk or severity of hyperthermia and oligohydrosis can be increased when Brompheniramine is combined with Topiramate.
Flupentixol The risk or severity of hyperthermia and oligohydrosis can be increased when Flupentixol is combined with Topiramate.
Cocaine The risk or severity of hyperthermia and oligohydrosis can be increased when Cocaine is combined with Topiramate.
Quinidine The risk or severity of hyperthermia and oligohydrosis can be increased when Quinidine is combined with Topiramate.
Maprotiline The risk or severity of hyperthermia and oligohydrosis can be increased when Maprotiline is combined with Topiramate.
Methantheline The risk or severity of hyperthermia and oligohydrosis can be increased when Methantheline is combined with Topiramate.
Cycrimine The risk or severity of hyperthermia and oligohydrosis can be increased when Cycrimine is combined with Topiramate.
Glycopyrronium The risk or severity of hyperthermia and oligohydrosis can be increased when Glycopyrronium is combined with Topiramate.
Tolterodine The risk or severity of hyperthermia and oligohydrosis can be increased when Tolterodine is combined with Topiramate.
Oxybutynin The risk or severity of hyperthermia and oligohydrosis can be increased when Oxybutynin is combined with Topiramate.
Promethazine The risk or severity of hyperthermia and oligohydrosis can be increased when Promethazine is combined with Topiramate.
Diphenhydramine The risk or severity of hyperthermia and oligohydrosis can be increased when Diphenhydramine is combined with Topiramate.
Doxacurium The risk or severity of hyperthermia and oligohydrosis can be increased when Doxacurium is combined with Topiramate.
Doxepin The risk or severity of hyperthermia and oligohydrosis can be increased when Doxepin is combined with Topiramate.
Flavoxate The risk or severity of hyperthermia and oligohydrosis can be increased when Flavoxate is combined with Topiramate.
Desipramine The risk or severity of hyperthermia and oligohydrosis can be increased when Desipramine is combined with Topiramate.
Orphenadrine The risk or severity of hyperthermia and oligohydrosis can be increased when Orphenadrine is combined with Topiramate.
Escitalopram The risk or severity of hyperthermia and oligohydrosis can be increased when Escitalopram is combined with Topiramate.
Quetiapine The risk or severity of hyperthermia and oligohydrosis can be increased when Quetiapine is combined with Topiramate.
Mivacurium The risk or severity of hyperthermia and oligohydrosis can be increased when Mivacurium is combined with Topiramate.
Diphenidol The risk or severity of hyperthermia and oligohydrosis can be increased when Diphenidol is combined with Topiramate.
Aripiprazole The risk or severity of hyperthermia and oligohydrosis can be increased when Aripiprazole is combined with Topiramate.
Chlorprothixene The risk or severity of hyperthermia and oligohydrosis can be increased when Chlorprothixene is combined with Topiramate.
Metocurine The risk or severity of hyperthermia and oligohydrosis can be increased when Metocurine is combined with Topiramate.
Pancuronium The risk or severity of hyperthermia and oligohydrosis can be increased when Pancuronium is combined with Topiramate.
Pipecuronium The risk or severity of hyperthermia and oligohydrosis can be increased when Pipecuronium is combined with Topiramate.
Methotrimeprazine The risk or severity of hyperthermia and oligohydrosis can be increased when Methotrimeprazine is combined with Topiramate.
Tiotropium The risk or severity of hyperthermia and oligohydrosis can be increased when Tiotropium is combined with Topiramate.
Solifenacin The risk or severity of hyperthermia and oligohydrosis can be increased when Solifenacin is combined with Topiramate.
Isopropamide The risk or severity of hyperthermia and oligohydrosis can be increased when Isopropamide is combined with Topiramate.
Rapacuronium The risk or severity of hyperthermia and oligohydrosis can be increased when Rapacuronium is combined with Topiramate.
Mepenzolate The risk or severity of hyperthermia and oligohydrosis can be increased when Mepenzolate is combined with Topiramate.
Pizotifen The risk or severity of hyperthermia and oligohydrosis can be increased when Pizotifen is combined with Topiramate.
Fesoterodine The risk or severity of hyperthermia and oligohydrosis can be increased when Fesoterodine is combined with Topiramate.

Target Protein

Glutamate receptor ionotropic, kainate 1 GRIK1
Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1
Voltage-gated sodium channel alpha subunit SCN1A
Kainate receptors GRIK1
Carbonic anhydrase 2 CA2
Carbonic anhydrase 4 CA4
Voltage gated L-type calcium channel CACNA1C
Carbonic anhydrase 1 CA1
Carbonic anhydrase 3 CA3
Voltage-dependent R-type calcium channel CACNA1E

Referensi & Sumber

Synthesis reference: Geza Arvai, Sandor Garaczi, Attila Mate, Ferenc Lukacs, Zsolt Viski, Geza Schneider.(2004).US20060040874A1.Retrieved from: https://patents.google.com/patent/US20060040874A1/en.
Artikel (PubMed)
  • PMID: 28579749
    Ford L, Goldberg JL, Selan F, Greenberg HE, Shi Y: Comprehensive review of visual defects reported with topiramate. Clin Ophthalmol. 2017 May 23;11:983-992. doi: 10.2147/OPTH.S125768. eCollection 2017.
  • PMID: 28004305
    Brigo F, Bragazzi NL, Igwe SC, Nardone R, Trinka E: Topiramate in the Treatment of Generalized Convulsive Status Epilepticus in Adults: A Systematic Review with Individual Patient Data Analysis. Drugs. 2017 Jan;77(1):67-74. doi: 10.1007/s40265-016-0672-2.
  • PMID: 10768303
    Garnett WR: Clinical pharmacology of topiramate: a review. Epilepsia. 2000;41 Suppl 1:S61-5.
  • PMID: 10768292
    Shank RP, Gardocki JF, Streeter AJ, Maryanoff BE: An overview of the preclinical aspects of topiramate: pharmacology, pharmacokinetics, and mechanism of action. Epilepsia. 2000;41 Suppl 1:S3-9.
  • PMID: 19514879
    Wisniewski M, Lukasik-Glebocka M, Anand JS: Acute topiramate overdose--clinical manifestations. Clin Toxicol (Phila). 2009 Apr;47(4):317-20. doi: 10.1080/15563650601117954.
  • PMID: 16503717
    Wenzel RG, Schwarz K, Padiyara RS: Topiramate for migraine prevention. Pharmacotherapy. 2006 Mar;26(3):375-87. doi: 10.1592/phco.26.3.375.
  • PMID: 15845141
    Arnone D: Review of the use of Topiramate for treatment of psychiatric disorders. Ann Gen Psychiatry. 2005 Feb 16;4(1):5. doi: 10.1186/1744-859X-4-5.
  • PMID: 19860705
    Maryanoff BE: Sugar sulfamates for seizure control: discovery and development of topiramate, a structurally unique antiepileptic drug. Curr Top Med Chem. 2009;9(11):1049-62. doi: 10.2174/156802609789630938.
Menampilkan 8 dari 15 artikel.
Textbook
  • Mary J. Allen; Sandeep Sharma (2019). GABA receptor. StatPearls.

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