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Namespace Prefixes

PrefixIRI
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n9http://linked.opendata.cz/resource/drugbank/dosage/
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n6http://linked.opendata.cz/resource/drugbank/patent/
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owlhttp://www.w3.org/2002/07/owl#
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n14http://linked.opendata.cz/resource/drugbank/drug/DB06218/identifier/wikipedia/
n13http://linked.opendata.cz/resource/atc/
n12http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB06218
rdf:type
n3:Drug
n3:description
Lacosamide is a functionalized amino acid that has activity in the maximal electroshock seizure test, and is indicated for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain. Recent studies indicate that Lacosamide only affects those neurons which are depolarized or active for long periods of time, typical of neurons at the focus of an epileptic seizure, as opposed to other antiepileptic drugs such as carbamazepine or lamotrigine which slow the recovery from inactivation and reduce the ability of neurons to fire action potentials.
n3:dosage
n9:271B4AC6-363D-11E5-9242-09173F13E4C5 n9:271B4AC7-363D-11E5-9242-09173F13E4C5 n9:271B4AC4-363D-11E5-9242-09173F13E4C5 n9:271B4AC5-363D-11E5-9242-09173F13E4C5 n9:271B4ACD-363D-11E5-9242-09173F13E4C5 n9:271B4ACE-363D-11E5-9242-09173F13E4C5 n9:271B4ACF-363D-11E5-9242-09173F13E4C5 n9:271B4AC9-363D-11E5-9242-09173F13E4C5 n9:271B4ACA-363D-11E5-9242-09173F13E4C5 n9:271B4ACB-363D-11E5-9242-09173F13E4C5 n9:271B4ACC-363D-11E5-9242-09173F13E4C5 n9:271B4AC8-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Sheets PL, Heers C, Stoehr T, Cummins TR: Differential block of sensory neuronal voltage-gated sodium channels by lacosamide, lidocaine and carbamazepine. J Pharmacol Exp Ther. 2008 Mar 31;. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18378801 # Jones GL, Popli GS, Silvia MT: Lacosamide-induced valproic Acid toxicity. Pediatr Neurol. 2013 Apr;48(4):308-10. doi: 10.1016/j.pediatrneurol.2012.12.039. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/ 23498565
n3:group
approved
n3:halfLife
13 Hours
n3:indication
Lacosamide is indicated for adjunctive therapy for partial onset seizures in patients with epilepsy over 17 years old. Injection is indicated for short term use when oral therapy is not feasible.
owl:sameAs
n8:DB06218
dcterms:title
Lacosamide
adms:identifier
n11:DB06218 n14:Lacosamide n15:D07299 n16:0091-2480-47
n3:mechanismOfAction
It is proposed that lacosamide's inhibition of sodium channels is responsible for analgesia. Lacosamide may be selective for inhibiting depolarized neurons rather than neurons with normal resting potentials. Pain and nociceptor hyperexcitability are associated with neural membrane depolarization. Lacosamide binds to collapsin response mediator protein-2 (CRMP-2), a phosphoprotein which is expressed primarily in the nervous system and is involved in neuronal differentiation and control of axonal outgrowth. The role CRMP-2 of binding in seizure control is hasn't been elucidated.
n3:patent
n6:5654301 n6:RE38551
n3:routeOfElimination
Lacosamide is eliminated primarily from the systemic circulation by biotransformation and renal excretion.
n3:synonym
Vimpat Erlosamide Harkoseride SPM 927
n3:volumeOfDistribution
approximately 0.6 L/kg; thus close to the volume of total body water.
n3:proteinBinding
<15%
n3:synthesisReference
http://www.google.com/patents?id=IIanAAAAEBAJ&pg=PA2&source=gbs_selected_pages&cad=3#v=onepage&q&f=false
n3:IUPAC-Name
n4:271B4AD4-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4ADA-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B4AD9-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4AD6-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4AD7-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B4AD8-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B4AEA-363D-11E5-9242-09173F13E4C5 n4:271B4AD2-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4AED-363D-11E5-9242-09173F13E4C5 n4:271B4AD0-363D-11E5-9242-09173F13E4C5 n4:271B4AD3-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B4AD1-363D-11E5-9242-09173F13E4C5
n12:hasATCCode
n13:N03AX18
n3:H-Bond-Acceptor-Count
n4:271B4AE0-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4AE1-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4ADB-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B4ADC-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4ADE-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B4ADD-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4ADF-363D-11E5-9242-09173F13E4C5
n3:absorption
Lacosamide has a negligible first pass effect with bioavailability of about 100%. The maximum Lacosamide plasma concentrations occur about 1-4 hours after oral administration, and the pharmacokinetics of Lacosamide are dose proportional. Food does not affect absorption.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
175481-36-4
n3:category
n3:clearance
95% recovered in the urine 0.5% in the feces
n3:Bioavailability
n4:271B4AE6-363D-11E5-9242-09173F13E4C5
n3:Boiling-Point
n4:271B4AEC-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B4AE8-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B4AE9-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B4AEB-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4AE5-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4AE4-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4AE7-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4AD5-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4AE2-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4AE3-363D-11E5-9242-09173F13E4C5