Peringatan Keamanan

The oral LD50 in rats is 253 mg/kg.L49171

Dizziness, nausea, and seizures (generalized tonic-clonic seizures, status epilepticus) were observed at doses greater than 800 mg, which is twice the maximum recommended daily dose. Cardiac conduction disorders, confusion, decreased level of consciousness, cardiogenic shock, cardiac arrest, and coma have also been observed.L49191

Fatal overdoses have occurred with lacosamide. As there is no specific antidote for overdose with lacosamide, standard decontamination procedures should be followed. General supportive care of the patient is indicated including monitoring of vital signs and observation of the clinical status of patient. Standard hemodialysis procedures result in significant clearance of lacosamide (reduction of systemic exposure by 50% in four hours). Hemodialysis may be indicated based on the patient's clinical state or in patients with significant renal impairment.L49191

Lacosamide

DB06218

small molecule approved

Deskripsi

Lacosamide is an antiepileptic drug used to treat seizures. As a chiral functionalized amino acid, it works by blocking slowly inactivating components of voltage-gated sodium currents. Lacosamide exhibits a stereoselective mode of interaction with sodium channels.A262681 Lacosamide was first approved by the European Commission in August 2008 and was later approved by the FDA in October 2008.A262681 It was granted approval by Health Canada in September 2010.L49206

Struktur Molekul 2D

Berat 250.2936
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 of the unchanged drug is approximately 13 hours and is not altered by different doses, multiple dosing or intravenous administration. The major O-desmethyl metabolite of lacosamide has an elimination half-life ranging from 15 to 23 hours).[L49191]
Volume Distribusi The volume of distribution is approximately 0.6 L/kg and thus close to the volume of total body water.[L49191]
Klirens (Clearance) -

Absorpsi

Lacosamide is completely absorbed after oral administration with negligible first-pass effect. It has a high absolute bioavailability of approximately 100%. Food does not affect the rate and extent of absorption. The Tmax ranges from one to four hours. Steady-state plasma concentrations are achieved after three days of twice-daily repeated administration. The pharmacokinetics of lacosamide are dose-proportional over the dose range between 100 and 800 mg, and time-invariant, with low inter- and intra-subject variability. The major O-desmethyl metabolite of lacosamide has a longer Tmax that ranges from 0.5 to 12 hours.L49191 After intravenous administration, Cmax is reached at the end of infusion. The 30- and 60-minute intravenous infusions are bioequivalent to the oral tablet. For the 15-minute intravenous infusion, bioequivalence was met for AUC0-tz but not for Cmax. The point estimate of Cmax was 20% higher than Cmax for oral tablet and the 90% CI for Cmax exceeded the upper boundary of the bioequivalence range. In a trial comparing the oral tablet with an oral solution containing 10 mg/mL lacosamide, bioequivalence between both formulations was shown. A single loading dose of 200 mg approximates steady-state concentrations comparable to the 100 mg twice-daily oral administration.L49191

Metabolisme

Lacosamide is metabolized by CYP3A4, CYP2C9, and CYP2C19 to form O-desmethyl lacosamide, which is a major, pharmacologically inactive metabolite in humans. There is no enantiomeric interconversion of lacosamide.L49191

Rute Eliminasi

Lacosamide is primarily eliminated from the systemic circulation by renal excretion and biotransformation. After oral and intravenous administration of 100 mg radiolabeled lacosamide, approximately 95% of the radioactivity was recovered in the urine and less than 0.5 % in the feces. The major compounds excreted were unchanged lacosamide (approximately 40% of the dose), its O-desmethyl metabolite (approximately 30%), and a structurally unknown polar fraction (~20%).L49191

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food does not affect the rate and extent of absorption.

Interaksi Obat

985 Data
Ceritinib Lacosamide may increase the bradycardic activities of Ceritinib.
Ivabradine Lacosamide may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Lacosamide.
Buprenorphine The metabolism of Lacosamide can be decreased when combined with Buprenorphine.
Dronabinol The metabolism of Lacosamide can be decreased when combined with Dronabinol.
Magnesium sulfate The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Magnesium sulfate is combined with Lacosamide.
Mirtazapine The metabolism of Lacosamide can be decreased when combined with Mirtazapine.
Nabilone The metabolism of Lacosamide can be decreased when combined with Nabilone.
Orphenadrine The metabolism of Lacosamide can be decreased when combined with Orphenadrine.
Perampanel The metabolism of Lacosamide can be increased when combined with Perampanel.
Rufinamide The metabolism of Lacosamide can be increased when combined with Rufinamide.
Suvorexant The metabolism of Suvorexant can be decreased when combined with Lacosamide.
Thalidomide The metabolism of Lacosamide can be increased when combined with Thalidomide.
Zolpidem The metabolism of Lacosamide can be decreased when combined with Zolpidem.
Dabrafenib The serum concentration of Lacosamide can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Lacosamide can be increased when it is combined with Luliconazole.
Mefloquine The therapeutic efficacy of Lacosamide can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Lacosamide can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Lacosamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phenytoin The serum concentration of Lacosamide can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Lacosamide can be decreased when it is combined with Fosphenytoin.
Topotecan Lacosamide may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The metabolism of Lacosamide can be decreased when combined with Methadone.
Carbamazepine The serum concentration of Lacosamide can be decreased when it is combined with Carbamazepine.
Delavirdine The serum concentration of Lacosamide can be increased when it is combined with Delavirdine.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Lacosamide.
Primidone The metabolism of Lacosamide can be increased when combined with Primidone.
Methylphenobarbital The metabolism of Lacosamide can be increased when combined with Methylphenobarbital.
Phenobarbital The metabolism of Lacosamide can be increased when combined with Phenobarbital.
Ethanol The metabolism of Lacosamide can be increased when combined with Ethanol.
Azelastine The metabolism of Lacosamide can be decreased when combined with Azelastine.
Citalopram The metabolism of Lacosamide can be decreased when combined with Citalopram.
Duloxetine The metabolism of Lacosamide can be decreased when combined with Duloxetine.
Trazodone The therapeutic efficacy of Lacosamide can be decreased when used in combination with Trazodone.
Paroxetine The metabolism of Lacosamide can be decreased when combined with Paroxetine.
Sertraline The metabolism of Lacosamide can be decreased when combined with Sertraline.
Escitalopram The metabolism of Lacosamide can be decreased when combined with Escitalopram.
Zimelidine The metabolism of Lacosamide can be decreased when combined with Zimelidine.
Dapoxetine The metabolism of Lacosamide can be decreased when combined with Dapoxetine.
Milnacipran The metabolism of Lacosamide can be decreased when combined with Milnacipran.
Desvenlafaxine The metabolism of Lacosamide can be decreased when combined with Desvenlafaxine.
Seproxetine The metabolism of Lacosamide can be decreased when combined with Seproxetine.
Indalpine The metabolism of Lacosamide can be decreased when combined with Indalpine.
Lumacaftor The serum concentration of Lacosamide can be decreased when it is combined with Lumacaftor.
Cyproheptadine The therapeutic efficacy of Lacosamide can be decreased when used in combination with Cyproheptadine.
Amoxapine The therapeutic efficacy of Lacosamide can be decreased when used in combination with Amoxapine.
Cocaine The risk or severity of methemoglobinemia can be increased when Lacosamide is combined with Cocaine.
Maprotiline The therapeutic efficacy of Lacosamide can be decreased when used in combination with Maprotiline.
Tolterodine The metabolism of Lacosamide can be decreased when combined with Tolterodine.
Trimebutine The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Trimebutine is combined with Lacosamide.
Otilonium The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Otilonium is combined with Lacosamide.
Desipramine The metabolism of Lacosamide can be decreased when combined with Desipramine.
Amitriptyline The metabolism of Lacosamide can be decreased when combined with Amitriptyline.
Doxepin The metabolism of Lacosamide can be decreased when combined with Doxepin.
Clozapine The metabolism of Lacosamide can be decreased when combined with Clozapine.
Zopiclone The metabolism of Lacosamide can be decreased when combined with Zopiclone.
Bexarotene The metabolism of Lacosamide can be increased when combined with Bexarotene.
Nafcillin The metabolism of Lacosamide can be increased when combined with Nafcillin.
Echinacea The metabolism of Lacosamide can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Lacosamide can be increased when combined with Dexamethasone acetate.
Esmolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Esmolol is combined with Lacosamide.
Betaxolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Betaxolol is combined with Lacosamide.
Midodrine The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Midodrine is combined with Lacosamide.
Atenolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Atenolol is combined with Lacosamide.
Digoxin The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Digoxin is combined with Lacosamide.
Bendroflumethiazide The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Bendroflumethiazide is combined with Lacosamide.
Sotalol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Sotalol is combined with Lacosamide.
Methyldopa The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Methyldopa is combined with Lacosamide.
Rivastigmine The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Rivastigmine is combined with Lacosamide.
Bretylium The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Bretylium is combined with Lacosamide.
Acebutolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Acebutolol is combined with Lacosamide.
Nadolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Nadolol is combined with Lacosamide.
Bevantolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Bevantolol is combined with Lacosamide.
Practolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Practolol is combined with Lacosamide.
Celiprolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Celiprolol is combined with Lacosamide.
Lucinactant The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Lucinactant is combined with Lacosamide.
Calfactant The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Calfactant is combined with Lacosamide.
Pasireotide The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Pasireotide is combined with Lacosamide.
Bufuralol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Bufuralol is combined with Lacosamide.
Beractant The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Beractant is combined with Lacosamide.
Lanreotide The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Lanreotide is combined with Lacosamide.
Bopindolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Bopindolol is combined with Lacosamide.
Bupranolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Bupranolol is combined with Lacosamide.
Fingolimod The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Fingolimod is combined with Lacosamide.
Indenolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Indenolol is combined with Lacosamide.
Poractant alfa The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Poractant alfa is combined with Lacosamide.
Arotinolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Arotinolol is combined with Lacosamide.
Levobetaxolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Levobetaxolol is combined with Lacosamide.
Talinolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Talinolol is combined with Lacosamide.
Anisodamine The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Anisodamine is combined with Lacosamide.
Landiolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Landiolol is combined with Lacosamide.
Bucindolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Bucindolol is combined with Lacosamide.
Esatenolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Esatenolol is combined with Lacosamide.
Cloranolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Cloranolol is combined with Lacosamide.
Mepindolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Mepindolol is combined with Lacosamide.
Epanolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Epanolol is combined with Lacosamide.
Tertatolol The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Tertatolol is combined with Lacosamide.
Amlodipine The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Amlodipine is combined with Lacosamide.
Nimodipine The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Nimodipine is combined with Lacosamide.
Lercanidipine The risk or severity of ventricular arrhythmias, bradycardia, and heart block can be increased when Lercanidipine is combined with Lacosamide.

Target Protein

Dihydropyrimidinase-related protein 2 DPYSL2
Sodium channel protein type 11 subunit alpha SCN11A
Sodium channel protein type 9 subunit alpha SCN9A
Sodium channel protein type 3 subunit alpha SCN3A
Sodium channel protein type 10 subunit alpha SCN10A

Referensi & Sumber

Synthesis reference: http://www.google.com/patents?id=IIanAAAAEBAJ&pg=PA2&source=gbsselectedpages&cad=3#v=onepage&q&f=false
Artikel (PubMed)
  • PMID: 18378801
    Sheets PL, Heers C, Stoehr T, Cummins TR: Differential block of sensory neuronal voltage-gated sodium channels by lacosamide (2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide, lidocaine, and carbamazepine. J Pharmacol Exp Ther. 2008 Jul;326(1):89-99. doi: 10.1124/jpet.107.133413. Epub 2008 Mar 31.
  • PMID: 19552484
    Curia G, Biagini G, Perucca E, Avoli M: Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68. doi: 10.2165/00023210-200923070-00002.
  • PMID: 19043448
    Perucca E, Yasothan U, Clincke G, Kirkpatrick P: Lacosamide. Nat Rev Drug Discov. 2008 Dec;7(12):973-4. doi: 10.1038/nrd2764.
  • PMID: 25616473
    Rogawski MA, Tofighy A, White HS, Matagne A, Wolff C: Current understanding of the mechanism of action of the antiepileptic drug lacosamide. Epilepsy Res. 2015 Feb;110:189-205. doi: 10.1016/j.eplepsyres.2014.11.021. Epub 2014 Dec 3.

Contoh Produk & Brand

Produk: 323 • International brands: 0
Produk
  • Ach-lacosamide
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Ach-lacosamide
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Ach-lacosamide
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Ach-lacosamide
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Ag-lacosamide
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Ag-lacosamide
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Ag-lacosamide
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Ag-lacosamide
    Tablet • 200 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 323 produk.

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