Description

Simple

A medication used to treat a wide variety of seizures.

Clinical

An anticonvulsant used to treat various types of seizures and pain resulting from trigeminal neuralgia.

Overview

Carbamazepine, also known as Tegretol, is an anticonvulsant drug and analgesic drug used to control seizures and to treat pain resulting from trigeminal neuralgia. It was initially approved by the FDA in 1965.[3] Aside from the above uses, this drug is also given to control the symptoms of bipolar 1.[16] Interestingly, carbamazepine was the first anticonvulsant used to treat individuals with bipolar disorder.[6]

Pharmacology

Indication

Carbamazepine is indicated for the treatment of epilepsy and pain associated with true trigeminal neuralgia.[16] In particular, carbamazepine has shown efficacy in treating mixed seizures, partial seizures with comp... Read more

Pharmacodynamic

**General effects**

Carbamazepine treats seizures and the symptoms of trigeminal neuralgia by inhibiting sodium channels. In bipolar 1 disorder, carbamazepine has been found to decrease mania symptoms in a clinically significant manner according to the Young Mania Rating Scale (YMRS).[ Read more

Mechanism of action

Carbamazepine's mechanism of action is not fully elucidated and is widely debated.[ Read more

Absorption

The bioavailability of carbamazepine is in the range of 75-85% of an ingested dose.[ Read more

Protein binding

Carbamazepine is 75%-80% bound to plasma proteins.[3, Read more

Volume of distribution

The volume of distribution of carbamazepine was found to be 1.0 L/kg in one pharmacokinetic study.[ Read more

Clearance

In a pharmacokinetic study, the apparent oral clearance of carbamazepine was 25 ± 5 mL/min [ Read more

Half life

The mean elimination half-life of carbamazepine was 35 to 40 hours after one dose of carbamazepine extended-release formulations. The half-life ranged from 12-17 hours after several doses of carbamazepine.[16] One... Read more

Route of elimination

After an oral dose of radiolabeled carbamazepine, 72% of the administered radioactive dose was detected in the urine and the remainder of the ingested dose was found in the feces. Carbamazepine is mainly excreted as hydroxylated and conjugated metabolites, and minimal amounts of unchanged drug.[ Read more

Toxicity

Toxicity information
Oral LDLO (female): 1920 mg/kg/17W (intermittent); Oral LDLO (male): 54 mg/kg/9D (intermittent)[18]
Oral LD50 (rat): 1957 mg/kg [ Read more

Adverse Effects

Contraindications

  • Regions: Canada
  • With Drugs Coadmin:
      • Name: Delavirdine
      • Drugbank Id: DB00705
  • Regions: US
  • Patient Conditions:
      • Name: Hypersensitivity to carbamazepine
      • Drugbank Id: DBCOND0121213
  • Regions: US
  • With Categories Coadmin:
      • Name: Monoamine Oxidase Inhibitors
      • Drugbank Id: DBCAT001004
      • Mesh Id: D008996
  • Regions: US
  • With Drugs Coadmin:
      • Name: Nefazodone
      • Drugbank Id: DB01149
  • Hypersensitivity:
    • Antidepressive Agents, Tricyclic
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: History of previous bone marrow depression
      • Drugbank Id: DBCOND0107838

Food Interactions

  • Avoid alcohol.
  • Avoid grapefruit products.
  • Take with or without food.

Interactions

Type in a drug name to check for interaction with Carbamazepine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(6R)-Folinic acid
The serum concentration of Carbamazepine can be decreased when it is combined with (6R)-Folinic acid.
(6S)-5,6,7,8-tetrahydrofolic acid
The serum concentration of Carbamazepine can be decreased when it is combined with (6S)-5,6,7,8-tetrahydrofolic acid.
(R)-warfarin
The metabolism of (R)-warfarin can be increased when combined with Carbamazepine.
(S)-Warfarin
The metabolism of (S)-Warfarin can be increased when combined with Carbamazepine.
2-Methoxyethanol
The risk or severity of adverse effects can be increased when Carbamazepine is combined with 2-Methoxyethanol.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when Carbamazepine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Carbamazepine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine
The serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be decreased when it is combined with Carbamazepine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Carbamazepine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be increased when combined with Carbamazepine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Carbamazepine is combined with 4-Methoxyamphetamine.
5-fluorouridine
The therapeutic efficacy of Carbamazepine can be decreased when used in combination with 5-fluorouridine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Carbamazepine is combined with 5-methoxy-N,N-dimethyltryptamine.
5-methyltetrahydrofolic acid
The serum concentration of Carbamazepine can be decreased when it is combined with 5-methyltetrahydrofolic acid.
6-Deoxyerythronolide B
The metabolism of Carbamazepine can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanine
The serum concentration of 6-O-benzylguanine can be decreased when it is combined with Carbamazepine.
7-Deazaguanine
The serum concentration of 7-Deazaguanine can be decreased when it is combined with Carbamazepine.
7-ethyl-10-hydroxycamptothecin
The metabolism of Carbamazepine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
7-Nitroindazole
Carbamazepine may increase the Change in thyroid function activities of 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Carbamazepine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
19 References
  1. 1 . Staines AG, Coughtrie MW, Burchell B: N-glucuronidation of carbamazepine in human tissues is mediated by UGT2B7. J Pharmacol Exp Ther. 2004 Dec;311(3):1131-7. Epub 2004 Aug 3.PubMed: 15292462
  2. 2 . Sisodiya SM, Goldstein DB: Drug resistance in epilepsy: more twists in the tale. Epilepsia. 2007 Dec;48(12):2369-70.PubMed: 18088268
  3. 3 . Tolou-Ghamari Z, Zare M, Habibabadi JM, Najafi MR: A quick review of carbamazepine pharmacokinetics in epilepsy from 1953 to 2012. J Res Med Sci. 2013 Mar;18(Suppl 1):S81-5.PubMed: 23961295
  4. 4 . Marino SE, Birnbaum AK, Leppik IE, Conway JM, Musib LC, Brundage RC, Ramsay RE, Pennell PB, White JR, Gross CR, Rarick JO, Mishra U, Cloyd JC: Steady-state carbamazepine pharmacokinetics following oral and stable-labeled intravenous administration in epilepsy patients: effects of race and sex. Clin Pharmacol Ther. 2012 Mar;91(3):483-8. doi: 10.1038/clpt.2011.251. Epub 2012 Jan 25.PubMed: 22278332
  5. 5 . Ambrosio AF, Soares-Da-Silva P, Carvalho CM, Carvalho AP: Mechanisms of action of carbamazepine and its derivatives, oxcarbazepine, BIA 2-093, and BIA 2-024. Neurochem Res. 2002 Feb;27(1-2):121-30.PubMed: 11926264
  6. 6 . Chen CH, Lin SK: Carbamazepine treatment of bipolar disorder: a retrospective evaluation of naturalistic long-term outcomes. BMC Psychiatry. 2012 May 23;12:47. doi: 10.1186/1471-244X-12-47.PubMed: 22620289
  7. 7 . Johnson DL, Gellman H, Waters RL, Tognella M: Brachioradialis transfer for wrist extension in tetraplegic patients who have fifth-cervical-level neurological function. J Bone Joint Surg Am. 1996 Jul;78(7):1063-7. doi: 10.2106/00004623-199607000-00011.PubMed: 8698724
  8. 8 . Kuo CC, Chen RS, Lu L, Chen RC: Carbamazepine inhibition of neuronal Na+ currents: quantitative distinction from phenytoin and possible therapeutic implications. Mol Pharmacol. 1997 Jun;51(6):1077-83. doi: 10.1124/mol.51.6.1077.PubMed: 9187275
  9. 9 . Barrons R, Roberts N: The role of carbamazepine and oxcarbazepine in alcohol withdrawal syndrome. J Clin Pharm Ther. 2010 Apr;35(2):153-67. doi: 10.1111/j.1365-2710.2009.01098.x.PubMed: 20456734
  10. 10 . Aurora RN, Kristo DA, Bista SR, Rowley JA, Zak RS, Casey KR, Lamm CI, Tracy SL, Rosenberg RS: The treatment of restless legs syndrome and periodic limb movement disorder in adults--an update for 2012: practice parameters with an evidence-based systematic review and meta-analyses: an American Academy of Sleep Medicine Clinical Practice Guideline. Sleep. 2012 Aug 1;35(8):1039-62. doi: 10.5665/sleep.1988.PubMed: 22851801
  11. 11 . Rawlins MD, Collste P, Bertilsson L, Palmer L: Distribution and elimination kinetics of carbamazepine in man. Eur J Clin Pharmacol. 1975 Feb 28;8(2):91-6.PubMed: 1233212
  12. 12 . Yoshimura R, Yanagihara N, Terao T, Minami K, Toyohira Y, Ueno S, Uezono Y, Abe K, Izumi F: An active metabolite of carbamazepine, carbamazepine-10,11-epoxide, inhibits ion channel-mediated catecholamine secretion in cultured bovine adrenal medullary cells. Psychopharmacology (Berl). 1998 Feb;135(4):368-73.PubMed: 9539261
  13. 13 . Thorn CF, Leckband SG, Kelsoe J, Leeder JS, Muller DJ, Klein TE, Altman RB: PharmGKB summary: carbamazepine pathway. Pharmacogenet Genomics. 2011 Dec;21(12):906-10. doi: 10.1097/FPC.0b013e328348c6f2.PubMed: 21738081
  14. 14 . Lv Y, Zheng X, Shi M, Wang Z, Cui L: Different EPHX1 methylation levels in promoter area between carbamazepine-resistant epilepsy group and carbamazepine-sensitive epilepsy group in Chinese population. BMC Neurol. 2019 Jun 4;19(1):114. doi: 10.1186/s12883-019-1308-4.PubMed: 31164100
  15. 15 . Jasdave S. Maan; Abdolreza Saadabadi (2019). Carbamazepine. Stat Pearls Publishing.
  16. 16 . Carbamazepine FDA Label Link
  17. 17 . Pharm KGB, carbamazepine pathway, pharmacokinetics Link
  18. 18 . Carbamazepine MSDS Link
  19. 19 . ipolar Disorders and Carbamazepine: Pharmacokinetics,Pharmacodynamics, Therapeutic Effects and Indications of Carbamazepine: Review of Articles Link