Lacosamidum

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Lacosamidum
Cognitores
ChemSpider 189902
PubChem 219078
DrugBank DB06218
Natura chemica
Lacosamidum
Lacosamidum
Formula summarum C
13H
18N
2O
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)

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

Historia

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

Natura lacosamidi

Natura chemica

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
6H
5CH
2NH
2, quod est benzenum cum NH2. Pariter est derivatum aminoacidorum (—NH—CO—COOH).

  • Benzylamidum
    Benzylamidum

Natura pharmacologica

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

Pharmacodynamica

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

Pharmacocinetica

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

Effectus lacosamidi

Effectus adversarii

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

Usus lacosamidi

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

Methodus therapeutica

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.

Notae

  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