Lamotrigin

Lamotrigin
(IUPAC) ime
	6-(2,3-dihlorofenil)-1,2,4-triazin-3,5-diamin
Klinički podaci
Identifikatori
CAS broj	84057-84-1
ATC kod	N03AX09
PubChem	3878
DrugBank	APRD00570
ChemSpider	3741
UNII	U3H27498KS
KEGG	D00354
ChEMBL	CHEMBL741
Hemijski podaci
Formula	C9H7Cl2N5
Mol. masa	256.091 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C9H7Cl2N5/c10-5-3-1-2-4(6(5)11)7-8(12)14-9(13)16-15-7/h1-3H,(H4,12,13,14,16) ; Key: PYZRQGJRPPTADH-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	98%
Vezivanje za proteine plazme	55%
Metabolizam	Hepatički (uglavnom putem UGT1A4)
Poluvreme eliminacije	24–34 časa (zdrave odrasle osobe)
Izlučivanje	Renalno
Farmakoinformacioni podaci
Trudnoća	C(US)
Pravni status	POM (UK) ℞-only (SAD)
Način primene	Oralno

Lamotrigin (prodajni nazivi Lamiktal, Lamal) je antiepileptik. Koristi se u lečenju epilepsije i manično-depresivne psihoze.^[6]^[7] U slučaju epilepsije, on se koristi za tretman parcijalnih napada, primarnih i sekundarnih grand mala, i napada vezanih za Lenoks-Gastautov sindrom. Poput mnogih drugih antiepileptika, lamotrigin takođe deluje kao stabilizator raspoloženja. On je jedini lek odobren od strane FDA za tu svrhu nakon litijuma, leka odobrenog skor 30 godina ranije. On je odobren za dugotrajno lečenje manično-depresivne psihoze tipa I. Hemijski nije srodan sa drugim antiepilepticima (on je feniltriazin). Lamotrigin ima relativno mali broj nuspojava i ne uslovljava analize krvi u monoterapiji. Precizan način dejstva lamotrigina nije poznat. Smatra se da je bloker natrijumskog kanala, mada on ima veoma mali broj nuspojava karakterističnih za druge nevezane antikonvulzante za koje je poznato da inihiviraju natrijumske kanale, npr. okskarbazepin. Stoga je moguće da originalan ima različiti mehanizam dejstva.^[8] Lamotrigin se inaktivira hepatičkom glukuronidacijom.

Sinteza

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948863. edit
↑ Masters, Susan B.; Katzung, Bertram G.; Trevor, Anthony J. (2009). Basic and Clinical Pharmacology (11th Edition (LANGE Basic Science) izd.). McGraw-Hill Medical. ISBN 0-07-160405-7.
↑ „Lamictal (Lamotrigine) Drug Information: User Reviews, Side Effects, Drug Interactions and Dosage at RxList”. Pristupljeno 7. 5. 2011.
↑ Lees G, Leach MJ (May 1993). „Studies on the mechanism of action of the novel anticonvulsant lamotrigine (Lamictal) using primary neurological cultures from rat cortex”. Brain Research 612 (1-2): 190–9. PMID 7687190. Pristupljeno 2011-05-07.

Literatura

Masters, Susan B.; Katzung, Bertram G.; Trevor, Anthony J. (2009). Basic and Clinical Pharmacology (11th Edition (LANGE Basic Science) izd.). McGraw-Hill Medical. ISBN 0-07-160405-7.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Psihijatrijska upotreba
Lamiktal
Lekovi za epilepsiju Arhivirano 2007-12-27 na Wayback Machine-u
Nuspojave Arhivirano 2013-02-23 na Wayback Machine-u
Lamotrigin
Nuspojave lamiktala

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948863. edit

[isbn0-07-160405-7-6] Masters, Susan B.; Katzung, Bertram G.; Trevor, Anthony J. (2009). Basic and Clinical Pharmacology (11th Edition (LANGE Basic Science) izd.). McGraw-Hill Medical. ISBN 0-07-160405-7.

[urlLamictal-7] „Lamictal (Lamotrigine) Drug Information: User Reviews, Side Effects, Drug Interactions and Dosage at RxList”. Pristupljeno 7. 5. 2011.

[pmid7687190-8] Lees G, Leach MJ (May 1993). „Studies on the mechanism of action of the novel anticonvulsant lamotrigine (Lamictal) using primary neurological cultures from rat cortex”. Brain Research 612 (1-2): 190–9. PMID 7687190. Pristupljeno 2011-05-07.

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