Peringatan Keamanan

The oral TDLO of levetiracetam in humans is 10 mg/kg.L8612 Symptoms of levetiracetam overdose are consistent with its adverse effect profile and may include agitation, aggression, somnolence, decreased level of consciousness, respiratory depression, or coma.L8606,L8600 There is no antidote for levetiracetam overdose, therefore management should involve general supportive measures and symptomatic treatment. Hemodialysis results in significant clearance of plasma levetiracetam (approximately 50% within 4 hours) and should be considered in cases of overdose as indicated by the patient's status.L8606,L8600

Levetiracetam

DB01202

small molecule approved

Deskripsi

Levetiracetam is a drug within the pyrrolidine class that is used to treat various types of seizures stemming from epileptic disorders. It was first approved for use in the United States in 1999 and is structurally and mechanistically unrelated to other anti-epileptic drugs (AEDs).L8606,L8600,L8615 Levetiracetam possesses a wide therapeutic indexL8615,A185918 and little-to-no potential to produce, or be subject to, pharmacokinetic interactionsL8606,L8600,L8615 - these characteristics make it a desirable choice over other AEDs, a class of drugs notorious for having generally narrow therapeutic indexes and a propensity for involvement in drug interactions.A185927

Struktur Molekul 2D

Berat 170.212
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life of levetiracetam is 6-8 hours and is not affected by dose or repeat administration. Half-life is increased in the elderly (by about 40%)[L8615] and those with renal impairment.[L8606,L8600]
Volume Distribusi The volume of distribution of levetiracetam is approximately 0.5 to 0.7 L/kg.[L8600,L8615]
Klirens (Clearance) The total plasma clearance of levetiracetam is 0.96 mL/min/kg, with renal clearance comprising 0.6 mL/min/kg.[L8606] The primary inactive metabolite of levetiracetam, L057, has a renal clearance of 4 mL/min/kg. Given the relatively high proportion of drug undergoing renal clearance, overall clearance of levetiracetam is reduced in patients with renal impairment.[L8606,L8600]

Absorpsi

Levetiracetam is rapidly and nearly completely absorbed following oral administration, with a reported absolute oral bioavailability of essentially 100%.L8615,L8606,L8600 Tmax is approximately 1.3 hours after dosing, and Cmax is 31 ?g/mL following a single 1000mg dose and 43 ?g/mL following repeated dosing.L8600,L8615 Co-administration of levetiracetam with food delays Tmax by approximately 1.5 hours and decreases Cmax by 20%.L8606,L8600

Metabolisme

Levetiracetam is minimally metabolized within the body - the major metabolic pathway appears to be the enzymatic hydrolysis of its acetamide group which produces an inactive carboxylic acid metabolite, L057, which accounts for approximately 24% of the total administered dose.L8606,L8600 The specific enzyme(s) responsible for this reaction are unclear, but this pathway is known to be independent of hepatic CYP enzymes and has been proposed to be driven primarily by type B esterases in the blood and other tissues.A185864 Two minor metabolites involving modifications to the pyrrolidone ring have been identified, one involving hydroxylation of the ring (constituting 1.6% of the total dose) and the other involving opening of the ring structure (constituting 0.9% of the total dose).L8615,L8606,L8600

Rute Eliminasi

Approximately 66% of the administered dose of levetiracetam is excreted in the urine as unchanged drug,L8606,L8600 while only 0.3% of the total dose is excreted via the feces.L8615 The primary inactive metabolite of levetiracetam, L057, is also found in the urine as approximately 24% of the administered dose.L8615

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Interaksi Obat

810 Data
Buprenorphine Levetiracetam 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 Levetiracetam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Levetiracetam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Levetiracetam.
Hydrocodone Levetiracetam 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 Levetiracetam.
Magnesium sulfate The therapeutic efficacy of Levetiracetam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Levetiracetam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Levetiracetam.
Mirtazapine Levetiracetam 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 Levetiracetam.
Orphenadrine Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Levetiracetam 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 Levetiracetam.
Pramipexole Levetiracetam may increase the sedative activities of Pramipexole.
Ropinirole Levetiracetam may increase the sedative activities of Ropinirole.
Rotigotine Levetiracetam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Levetiracetam.
Sodium oxybate Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Levetiracetam 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 Levetiracetam.
Thalidomide Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Levetiracetam can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Levetiracetam can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Levetiracetam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Levetiracetam may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Levetiracetam.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Levetiracetam.
Ethanol Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Levetiracetam.
Fluvoxamine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Levetiracetam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Levetiracetam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Levetiracetam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Levetiracetam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Levetiracetam is combined with Alaproclate.
Citalopram The risk or severity of adverse effects can be increased when Levetiracetam is combined with Citalopram.
Escitalopram The risk or severity of adverse effects can be increased when Levetiracetam is combined with Escitalopram.
Trazodone The risk or severity of adverse effects can be increased when Levetiracetam is combined with Trazodone.
Nefazodone The risk or severity of adverse effects can be increased when Levetiracetam is combined with Nefazodone.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Levetiracetam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Levetiracetam.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Levetiracetam.
Pizotifen The risk or severity of CNS depression can be increased when Levetiracetam is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Levetiracetam is combined with Dosulepin.
Cocaine The risk or severity of methemoglobinemia can be increased when Levetiracetam is combined with Cocaine.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Levetiracetam.
Clozapine The risk or severity of CNS depression can be increased when Clozapine is combined with Levetiracetam.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Levetiracetam.
Chlorpromazine The risk or severity of CNS depression can be increased when Chlorpromazine is combined with Levetiracetam.
Triflupromazine The risk or severity of CNS depression can be increased when Triflupromazine is combined with Levetiracetam.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Levetiracetam.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Levetiracetam.
Scopolamine The risk or severity of CNS depression can be increased when Scopolamine is combined with Levetiracetam.
Flupentixol The risk or severity of CNS depression can be increased when Flupentixol is combined with Levetiracetam.
Quinidine The therapeutic efficacy of Levetiracetam can be decreased when used in combination with Quinidine.
Promethazine The risk or severity of CNS depression can be increased when Promethazine is combined with Levetiracetam.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Levetiracetam.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Levetiracetam.
Quetiapine The risk or severity of CNS depression can be increased when Levetiracetam is combined with Quetiapine.
Chlorprothixene The risk or severity of CNS depression can be increased when Levetiracetam is combined with Chlorprothixene.
Zopiclone The risk or severity of adverse effects can be increased when Levetiracetam is combined with Zopiclone.
Efavirenz The risk or severity of CNS depression can be increased when Efavirenz is combined with Levetiracetam.
Melatonin The risk or severity of CNS depression can be increased when Melatonin is combined with Levetiracetam.
Dantrolene The risk or severity of CNS depression can be increased when Levetiracetam is combined with Dantrolene.
Lithium cation The risk or severity of CNS depression can be increased when Levetiracetam is combined with Lithium cation.
Lithium carbonate The risk or severity of CNS depression can be increased when Levetiracetam is combined with Lithium carbonate.
Alprenolol The risk or severity of CNS depression can be increased when Alprenolol is combined with Levetiracetam.
Pindolol The risk or severity of CNS depression can be increased when Pindolol is combined with Levetiracetam.
Penbutolol The risk or severity of CNS depression can be increased when Levetiracetam is combined with Penbutolol.
Urapidil The risk or severity of CNS depression can be increased when Levetiracetam is combined with Urapidil.
Aripiprazole lauroxil The risk or severity of CNS depression can be increased when Levetiracetam is combined with Aripiprazole lauroxil.
Metocurine iodide The risk or severity of CNS depression can be increased when Metocurine iodide is combined with Levetiracetam.
Gallamine triethiodide The risk or severity of CNS depression can be increased when Gallamine triethiodide is combined with Levetiracetam.
Cisatracurium The risk or severity of CNS depression can be increased when Cisatracurium is combined with Levetiracetam.
Rocuronium The risk or severity of CNS depression can be increased when Rocuronium is combined with Levetiracetam.
Atracurium besylate The risk or severity of CNS depression can be increased when Atracurium besylate is combined with Levetiracetam.
Doxacurium The risk or severity of CNS depression can be increased when Doxacurium is combined with Levetiracetam.
Tubocurarine The risk or severity of CNS depression can be increased when Tubocurarine is combined with Levetiracetam.
Mivacurium The risk or severity of CNS depression can be increased when Levetiracetam is combined with Mivacurium.
Metocurine The risk or severity of CNS depression can be increased when Levetiracetam is combined with Metocurine.
Pancuronium The risk or severity of CNS depression can be increased when Levetiracetam is combined with Pancuronium.
Pipecuronium The risk or severity of CNS depression can be increased when Levetiracetam is combined with Pipecuronium.
Rapacuronium The risk or severity of CNS depression can be increased when Levetiracetam is combined with Rapacuronium.
Atracurium The risk or severity of CNS depression can be increased when Levetiracetam is combined with Atracurium.
Gallamine The risk or severity of CNS depression can be increased when Levetiracetam is combined with Gallamine.
Alcuronium The risk or severity of CNS depression can be increased when Levetiracetam is combined with Alcuronium.
Promazine The risk or severity of CNS depression can be increased when Promazine is combined with Levetiracetam.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Levetiracetam.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Levetiracetam.

Target Protein

5-hydroxytryptamine receptor 3A HTR3A
Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B
Synaptic vesicle glycoprotein 2A SV2A

Referensi & Sumber

Synthesis reference: Tooru Futagawa, Jean-Pierre Canvat, Emile Cavoy, Michel Deleers, Michel Hamende, Vincent Zimmermann, "Process for the preparation of levetiracetam." U.S. Patent US6107492, issued September, 1996.
Artikel (PubMed)
  • PMID: 15301575
    Patsalos PN: Clinical pharmacokinetics of levetiracetam. Clin Pharmacokinet. 2004;43(11):707-24. doi: 10.2165/00003088-200443110-00002.
  • PMID: 17045309
    Baltes S, Gastens AM, Fedrowitz M, Potschka H, Kaever V, Loscher W: Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. Neuropharmacology. 2007 Feb;52(2):333-46. Epub 2006 Oct 10.
  • PMID: 18824002
    Luna-Tortos C, Fedrowitz M, Loscher W: Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008 Dec;55(8):1364-75. doi: 10.1016/j.neuropharm.2008.08.032. Epub 2008 Sep 11.
  • PMID: 15210974
    Lynch BA, Lambeng N, Nocka K, Kensel-Hammes P, Bajjalieh SM, Matagne A, Fuks B: The synaptic vesicle protein SV2A is the binding site for the antiepileptic drug levetiracetam. Proc Natl Acad Sci U S A. 2004 Jun 29;101(26):9861-6. Epub 2004 Jun 21.
  • PMID: 15367040
    Stahl SM: Psychopharmacology of anticonvulsants: levetiracetam as a synaptic vesicle protein modulator. J Clin Psychiatry. 2004 Sep;65(9):1162-3.
  • PMID: 18072813
    Johannessen Landmark C: Antiepileptic drugs in non-epilepsy disorders: relations between mechanisms of action and clinical efficacy. CNS Drugs. 2008;22(1):27-47.
  • PMID: 17461889
    De Smedt T, Raedt R, Vonck K, Boon P: Levetiracetam: the profile of a novel anticonvulsant drug-part I: preclinical data. CNS Drug Rev. 2007 Spring;13(1):43-56.
  • PMID: 11879381
    Lukyanetz EA, Shkryl VM, Kostyuk PG: Selective blockade of N-type calcium channels by levetiracetam. Epilepsia. 2002 Jan;43(1):9-18.
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