Carbamazepine

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Carbamazepine, sold under the brand name Tegretol among others, is an anticonvulsant medication used in the treatment of epilepsy and neuropathic pain.[1][2] It is used as an adjunctive treatment in schizophrenia along with other medications and as a second-line agent in bipolar disorder.[3][2] Carbamazepine appears to work as well as phenytoin and valproate for focal and generalized seizures.[4] It is not effective for absence or myoclonic seizures.[2] See also Carbamazepine.

Carbamazepine is a sodium channel blocker.[5] It binds preferentially to voltage-gated sodium channels (Nav) in their inactive conformation, which prevents repetitive and sustained firing of an action potential.

Nav1.7 with Carbamazepine (8s9c).

Carbamazepine binding site.

Caption for this structure

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References

  1. "Tegretol - carbamazepine suspension Tegretol - carbamazepine tablet Tegretol XR- carbamazepine tablet, extended release". DailyMed. 16 May 2022. Retrieved 3 January 2023.
  2. 2.0 2.1 2.2 "Carbamazepine". The American Society of Health-System Pharmacists. Archived from the original on 27 February 2015. Retrieved 28 March 2015.
  3. Nevitt SJ, Marson AG, Weston J, Tudur Smith C. Sodium valproate versus phenytoin monotherapy for epilepsy: an individual participant data review. Cochrane Database Syst Rev. 2018 Aug 9;8(8):CD001769. PMID:30091458 doi:10.1002/14651858.CD001769.pub4
  4. Nevitt SJ, Marson AG, Tudur Smith C. Carbamazepine versus phenytoin monotherapy for epilepsy: an individual participant data review. Cochrane Database Syst Rev. 2019 Jul 18;7(7):CD001911. PMID:31318037 doi:10.1002/14651858.CD001911.pub4
  5. Rogawski MA, Löscher W, Rho JM. Mechanisms of Action of Antiseizure Drugs and the Ketogenic Diet. Cold Spring Harb Perspect Med. 2016 May 2;6(5):a022780. PMID:26801895 doi:10.1101/cshperspect.a022780

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