Lacosamidum est medicamentum pharmaceuticum cum virtutibus anticonvulsivis convulsionum partialium apud adultos[1].

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Lacosamidum
Cognitores
ChemSpider 189902
PubChem 219078
DrugBank DB06218
Natura chemica
Lacosamidum
Lacosamidum
Formula summarum C
13
H
18
N
2
O
3
Massa molaris 250.294 g/mol
Natura pharmacologica
Codex ATC N03AX18 (WHO)
Semivita biologica 13 horae
Metabolismus iecore (hepaticus):
Demethylatione
CYP2C19, CYP2C9,
CYP3A4
Excretio renibus
Ad usum therapeuticum
Applicatio per os, i.v.
MedlinePlus a609028 (Anglice)

Historia

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Substantia primum anno 1996 in Houstonia ex N-benzyl-2-acetamidopropionamido derivatum descripta est[2].

Natura lacosamidi

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Natura chemica

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Nomen IUPAC suum est (2R)-N-benzylo-2-acetamido-3-methoxy-propano-amidum, massa molaris sua 250.294 g/mol. Inest praecursor chemicus benzylamidum C
6
H
5
CH
2
NH
2
, quod est benzenum cum NH2. Pariter est derivatum aminoacidorum (—NH—CO—COOH).

Natura pharmacologica

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Lacosamidum est medicamentum cum virtutibus anticonvulsivis. Codex ATC est N03AX18 (WHO).

Pharmacodynamica

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Lacosamidum canales ionticos natrii tensione reclusos (VGSC) tarde inhibit[3].

Pharmacocinetica

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Tempus semivitae biologicum  [4] 13 horae sunt. Metabolismus per cytochromatum CYP2C19[5], CYP2C9, CYP3A4 fit. Excretio est per urinas.

Effectus lacosamidi

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Effectus adversarii

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Lacosamidum enzyma hepatica in sanguinem liberare potest, ut valores sanguinei eorum augeantur.

Usus lacosamidi

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Dosis diurna definita (DDD) est 300 mg per die p.o.[6]

Methodus therapeutica

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In morbum comitialem tractando dosis initialis sit a 50 mg ad 100 mg die, deinde hebdomade inter 50 et 100 mg die augenti, bis distributum[7], usque a 200 mg ad 400 mg die, commendatur.

  1. Ben-Menachem E., Biton V., Jatuzis D., Abou-Khalil B., Doty P., Rudd G. D. (2007). "Efficacy and safety of oral lacosamide as adjunctive therapy in adults with partial-onset seizures". Epilepsia 48 (7): 1308-17 
  2. Choi D., Stables J. P., Kohn H. (Apr 1996). "Synthesis and anticonvulsant activities of N-Benzyl-2-acetamidopropionamide derivatives". Journal of medicinal chemistry 39 (9): 1907-16 
  3. Errington A. C., Stöhr T., Heers C., Lees G. (Ian 2008). "The investigational anticonvulsant lacosamide selectively enhances slow inactivation of voltage-gated sodium channels". Molecular pharmacology 73 (1): 157-69 
  4. Goldbook
  5. Cawello W., Mueller-Voessing C., Fichtner A. (Mai 2014). "Pharmacokinetics of lacosamide and omeprazole coadministration in healthy volunteers: results from a phase I, randomized, crossover trial". Clinical drug investigation 34 (5): 317-25 doi:10.1007/s40261-014-0177-2
  6. Systema classificationis Anatomicum Therapeuticum Chemicumque, cap. N03AX cum Pregabalini referentia,
  7. Benkert O, Hippius H (2017). Kompendium der Psychiatrischen Pharmakotherapie, Springer  (Theodisce)

Nexus externi

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