Carbamazepine

Oleh :

dr. DrRiawati MMedPH

Carbamazepine adalah suatu agonis reseptor GABA, derivat iminostilbene yang secara kimiawi berhubungan dengan trisiklik antidepresan. Obat ini bekerja dengan cara menurunkan impuls saraf yang menyebabkan kejang dan nyeri. Secara struktur carbamazepine mirip dengan fenitoin

Sinonim: Carbamazepine

Nama kimia: 5-carbamoyl-5H-dibenz[b,f]azepine atau 5H-Dibenz[b,f]azepine-5-carboxamide

Carbamazepine ditemukan pada tahun 1953, dan dipasarkan pertama kali pada tahun 1962.

Carbamazepine berupa bubuk berbentuk kristal putih hingga berwarna agak kekuningan atau keabu-abuan, hampir tidak berbau, tanpa rasa, atau dapat sedikit pahit. Bersifat lipofilik, tidak larut dalam air biasa dan eter, namun larut dalam alkohol, aseton, karbon tetraklorida, kloroform, dimetilformamid dioksan dan propilen glikol

Obat ini digunakan sebagai first-line therapy untuk epilepsi, umumnya tipe lobus temporal, dan trigeminal neuralgia. Efek terapi yang diberikan adalah anti kejang, baik yang bersifat grand mal, psikomotor, atau fokal, dan anti nyeri spesifik. [1-9]

TABEL 1 Deskripsi Singkat Carbamazepine

Perihal	Deskripsi
Kelas	Anti Epilepsi─Anti Konvulsi [1,2]
Sub-kelas	Nil [1,2]
Akses	Resep dokter [3]
Wanita hamil	Kategori D [4,5]
Wanita menyusui	Ekskresi kedalam air susu ibu [6]
Anak-anak	Bilamana perlu dan sesuai aturan
Infant	Bilamana perlu dan sesuai aturana
FDA	Black Box WarningCongenital malformationToxic Epidermal Necrolysis; sindrom Steven Johnson [6]

Referensi

1. Granger, P., et al., Modulation of the gamma-aminobutyric acid type A receptor by the antiepileptic drugs carbamazepine and phenytoin [Abstract]. Mol Pharmacol, 1995. 47(6): p. 1189-96

2. Liu, L., et al., The mechanism of carbamazepine aggravation of absence seizures. J Pharmacol Exp Ther, 2006. 319(2): p. 790-8

3. US National Library of Medicine: PubChem Database. Carbamazepine. May 2017; Available from: https://pubchem.ncbi.nlm.nih.gov/compound/2554#section=Top

4. Drugs.com. Carbamazepine. May 2017; Available from: https://www.drugs.com/pro/carbamazepine.html

5. US Food and Drug Administration. Tegretol® (Carbamazepine). 2009; Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/016608s101,018281s048lbl.pdf

6. Tomson, T., Clinical Pharmacokinetics of Carbamazepine. Cephalalgia, 1987. 7(4): p. 219-223

7. US National Library of Medicine: Dailymed Drugs. Carbamazepine. February 2016; Available from: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7a1e523a-b377-43dc-b231-7591c4c888ea

8. Remy, S., et al., A novel mechanism underlying drug resistance in chronic epilepsy. Ann Neurol, 2003. 53(4): p. 469-79

9. Kawata, Y., et al., Pharmacological discrimination between effects of carbamazepine on hippocampal basal, Ca2+- and K+-evoked serotonin release. British Journal of Pharmacology, 2001. 133(4): p. 557-567

10. Kementerian Kesehatan R.I. Daftar Obat Esensial Nasional 2013. 2014; Available from: http://binfar.kemkes.go.id/2014/02/daftar-obat-esensial-nasional-2013/#.WM-TUbVMRjo

11. WHO. Essential medicines. 2017; Available from: http://www.who.int/medicines/services/essmedicines_def/en/

12. BPOM: Badan Pengawas Obat dan Makanan. Carbamazepine. 2015; Available from: http://pionas.pom.go.id/obat/carbamazepine

13. BPOM: Badan Pengawas Obat dan Makanan. Karbamazepin. 2015; Available from: http://pionas.pom.go.id/monografi/karbamazepin-0

14. FDA. FDA Approved Drug Products. 2017; Available from: http://www.accessdata.fda.gov/scripts/cder/daf/

15. FDA. Pregnancy and Lactation Labeling (Drugs) Final Rule. 12 March 2014; Available from: https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DevelopmentResources/Labeling/ucm093307.htm

16. US Food and Drug Administration. Tegretol® (Carbamazepine USP) by Novartis. 2013; Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/016608s105,018281s053,018927s046,020234s038lbl.pdf

17. TGA: Therapeutic Goods Administration Department of Health Australian Government. Definitions of the Australian categories for prescribing medicines in pregnancy. May 2011; Available from: https://www.tga.gov.au/australian-categorisation-system-prescribing-medicines-pregnancy

18. TGA: Therapeutic Goods Administration Department of Health Australian Government. The Australian categorisation system for prescribing medicines in pregnancy. December 2016; Available from: https://www.tga.gov.au/prescribing-medicines-pregnancy-database#searchname

19. Singh, B., et al., Treatment of neonatal seizures with carbamazepine [Abstract]. J Child Neurol, 1996. 11(5): p. 378-82

20. Hoppen, T., C.E. Elger, and P. Bartmann, Carbamazepine in phenobarbital-nonresponders: experience with ten preterm infants [Abstract]. Eur J Pediatr, 2001. 160(7): p. 444-7

21. Sánchez, M.B., et al., Genetic factors associated with drug-resistance of epilepsy: Relevance of stratification by patient age and aetiology of epilepsy. Seizure, 2010. 19(2): p. 93-101

22. Isojarvi, J.I., A.J. Pakarinen, and V.V. Myllyla, Serum lipid levels during carbamazepine medication. A prospective study [Abstract]. Arch Neurol, 1993. 50(6): p. 590-3

23. Wagner, M.L. and R. Preblick, The effect of carbamazepine on serum lipid levels. Archives of Neurology, 1994. 51(8): p. 748-749

24. Bourgeois, B.F. and N. Wad, Combined administration of carbamazepine and phenobarbital: effect on anticonvulsant activity and neurotoxicity [Abstract]. Epilepsia, 1988. 29(4): p. 482-7

25. Baethge, C., et al., Long-term combination therapy versus monotherapy with lithium and carbamazepine in 46 bipolar I patients. J Clin Psychiatry, 2005. 66(2): p. 174-82

26. Khaitan, A.K., A. Sengupta, and H. Lata, Neurotoxicity Following Lithium and Carbamazepine Interaction - A Case Report. Indian Journal of Psychiatry, 1985. 27(3): p. 265-266

27. Drugs.com. Nefazodone. May 2017; Available from: https://www.drugs.com/pro/nefazodone.html

28. Ornoy, A. and E. Cohen, Outcome of children born to epileptic mothers treated with carbamazepine during pregnancy. Archives of Disease in Childhood, 1996. 75(6): p. 517-520

29. Davanzo, R., et al., Antiepileptic drugs and breastfeeding. Italian Journal of Pediatrics, 2013. 39: p. 50-50

30. Bar-Oz, B., et al., Anticonvulsants and breast feeding: a critical review [Abstract]. Paediatr Drugs, 2000. 2(2): p. 113-26

31. Frey, B., C.P. Braegger, and D. Ghelfi, Neonatal cholestatic hepatitis from carbamazepine exposure during pregnancy and breast feeding [Abstract]. Ann Pharmacother, 2002. 36(4): p. 644-7

32. Soriano, S.G., et al., Pharmacokinetics and pharmacodynamics of vecuronium in children receiving phenytoin or carbamazepine for chronic anticonvulsant therapy. BJA: British Journal of Anaesthesia, 2001. 86(2): p. 223-229

33. Amstutz, U., et al., Recommendations for HLA-B*15:02 and HLA-A*31:01 genetic testing to reduce the risk of carbamazepine-induced hypersensitivity reactions. Epilepsia, 2014. 55(4): p. 496-506

34. Albani, F., R. Riva, and A. Baruzzi, Carbamazepine clinical pharmacology: a review. Pharmacopsychiatry, 1995. 28(6): p. 235-44

35. Kawata, Y., et al., Pharmacological discrimination between effects of carbamazepine on hippocampal basal, Ca(2+)- and K(+)-evoked serotonin release. British Journal of Pharmacology, 2001. 133(4): p. 557-567

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