Peringatan Keamanan

Toxicity information
Oral LDLO (female): 1920 mg/kg/17W (intermittent); Oral LDLO (male): 54 mg/kg/9D (intermittent)L7156
Oral LD50 (rat): 1957 mg/kg L7156

Overdose information

The initial signs of carbamazepine overdose occur 1-3 hours post ingestion. These signs and symptoms may vary in case of an overdose between carbamazepine and other drugs. Carbamazepine may cause various cardiovascular, neurological, respiratory, urinary symptoms as well as laboratory abnormalities including leukocytosis, reduced leucocytes, acetonuria, and glycosuria.L1335

Neuromuscular symptoms may occur initially, followed by mild cardiac symptoms such as tachycardia, hypertension, or hypotension. Higher doses of carbamazepine may cause more severed cardiovascular effects. Restlessness, muscular twitching, tremor, dilated pupils, nystagmus, psychomotor disturbances, and other neurological symptoms may occur. Hyperreflexia in the initial stages of overdose may be followed by hyporeflexia. Nausea, vomiting, urinary retention, dizziness or drowsiness may also occur.L1335 In cases of overdose, contact the local poison control center. Ensure to provide supportive and symptomatic treatment, which may include monitoring and careful supervision by a medical professional. The possibility of overdose with multiple drugs must be considered in the case of carbamazepine overdose. Maintain an adequate airway, oxygen, in addition to ventilation. Vital signs should be monitored.L1335

Carbamazepine

DB00564

small molecule approved investigational

Deskripsi

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.A180301 Aside from the above uses, this drug is also given to control the symptoms of bipolar 1.L1335 Interestingly, carbamazepine was the first anticonvulsant used to treat individuals with bipolar disorder.A180319

Struktur Molekul 2D

Berat 236.2686
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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.[L1335] One pharmacokinetic study determined the elimination half-life of carbamazepine to range between 27 to 36.8 hours in healthy volunteers.[A180424]
Volume Distribusi The volume of distribution of carbamazepine was found to be 1.0 L/kg in one pharmacokinetic study.[A180304] Another study indicates that the volume of distribution of carbamazepine ranges between 0.7 to 1.4 L/kg.[A180424]. Carbamazepine crosses the placenta, and higher concentrations of this drug are found in the liver and kidney as opposed to lung and brain tissue.[L1335] Carbamazepine crosses variably through the blood-brain barrier.[A180436]
Klirens (Clearance) In a pharmacokinetic study, the apparent oral clearance of carbamazepine was 25 ± 5 mL/min [A180424,L1335] after one dose of carbamazepine and 80 ± 30 mL/min after several doses.[L1335]

Absorpsi

The bioavailability of carbamazepine is in the range of 75-85% of an ingested dose.A180301 After one 200 mg oral extended-release dose of carbamazepine in a pharmacokinetic study, the Cmax carbamazepine was measured to be 1.9 ± 0.3 mcg/mL. The Tmax was 19 ± 7 hours. After several doses of 800 mg every 12 hours, the peak concentrations of carbamazepine were measured to be 11.0 ± 2.5 mcg/mL. The Tmax was reduced to 5.9 ± 1.8 hours. Extended-release carbamazepine demonstrated linear pharmacokinetics over a range of 200–800 mg.L1335 Effect of food on absorption A meal containing high-fat content increased the rate of absorption of one 400 mg dose but not the AUC of carbamazepine.L1335 The elimination half-life remained unchanged between fed and fasting state. The pharmacokinetics of an extended-release carbamazepine dose was demonstrated to be similar when administered in the fasted state or with food.L1335 Based on these findings, food intake is unlikely to exert significant effects on carbamazepine absorption.

Metabolisme

Carbamazepine is largely metabolized in the liver. CYP3A4 hepatic enzyme is the major enzyme that metabolizes carbamazepine to its active metabolite, carbamazepine-10,11-epoxideA180427, which is further metabolized to its trans-diol form by the enzyme epoxide hydrolase.L1335 Other hepatic cytochrome enzymes that contribute to the metabolism of carbamazepine are CYP2C8, CYP3A5, and CYP2B6.L7195 Carbamazepine also undergoes hepatic glucuronidation by UGT2B7 enzyme and several other metabolic reactions occur, resulting in the formation of minor hydroxy metabolites and quinone metabolites.L7195 Interestingly, carbamazepine induces its own metabolism.L1335 This leads to enhanced clearance, reduced half-life, and a reduction in serum levels of carbamazepine.A180301,L1335

Rute Eliminasi

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.L1335

Farmakogenomik

10 Varian
SCN1A (rs3812718)

Patients with this genotype have increased resistance to the anti-epileptic effects of carbamazepine.

HSPA1L (rs2227956)

Patients with this genotype have increased risk of cutaneous hypersensitivity reactions with carbamazepine.

HSPA1A (rs506770)

Patients with this genotype have increased risk of cutaneous hypersensitivity reactions with carbamazepine.

HLA-B (rs3130690)

Patients with this genotype have increased risk of cutaneous hypersensitivity reactions with carbamazepine.

HLA-A (rs1264511)

Patients with this genotype have increased risk of cutaneous hypersensitivity reactions with carbamazepine.

MLN (rs2894342)

Patients with this genotype have increased risk of cutaneous hypersensitivity reactions with carbamazepine.

FLOT1 (rs3909184)

Taiwanese, Chinese, Indians, and Chinese–American patients with this genotype have increased risk of Stevens-Johnson syndrome or toxic epidermal necrolysis with carbamazepine.

MUC21 (rs2844682)

Taiwanese, Chinese, Indians, and Chinese–American patients with this genotype have increased risk of Stevens-Johnson syndrome or toxic epidermal necrolysis with carbamazepine.

HLA-B (None)

Patients who carry this allele may be at an increased risk of Stevens-Johnson Syndrome and toxic epidermal necrolysis when treated with carbamazepine.

HLA-A (rs1061235)

Patients who carry this genotype in HLA-A are at a higher risk of experiencing a hypersensitivity reaction to carbamazepine.

Interaksi Makanan

4 Data
  • 1. Avoid alcohol. Ingesting alcohol may increase drowsiness and dizziness.
  • 2. Avoid grapefruit products.
  • 3. Exercise caution with St. John's Wort. This herb induces the CYP3A metabolism of carbamazepine and may reduce its serum concentration.
  • 4. Take with or without food.

Interaksi Obat

2385 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Carbamazepine.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Carbamazepine.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Carbamazepine.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Carbamazepine.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Carbamazepine.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Carbamazepine.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Carbamazepine.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Carbamazepine.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Carbamazepine.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Carbamazepine.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Carbamazepine.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Carbamazepine.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Carbamazepine.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Carbamazepine.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Carbamazepine.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Carbamazepine.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Carbamazepine.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Carbamazepine.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Carbamazepine.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Carbamazepine.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Carbamazepine.
Cladribine Carbamazepine may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Carbamazepine.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Carbamazepine.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Carbamazepine.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Carbamazepine.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Carbamazepine.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Carbamazepine.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Carbamazepine.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Carbamazepine.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Carbamazepine.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Carbamazepine.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Carbamazepine.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Carbamazepine.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Carbamazepine.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Carbamazepine.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Carbamazepine.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Carbamazepine.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Carbamazepine.
Clofarabine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Clofarabine.
Pemetrexed The risk or severity of adverse effects can be increased when Carbamazepine is combined with Pemetrexed.
Dacarbazine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Dacarbazine.
Penicillamine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Penicillamine.
Mechlorethamine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Azacitidine.
Azathioprine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Azathioprine.
Hydroxyurea The risk or severity of adverse effects can be increased when Carbamazepine is combined with Hydroxyurea.
Melphalan The risk or severity of adverse effects can be increased when Carbamazepine is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Flucytosine.
Idarubicin The risk or severity of adverse effects can be increased when Carbamazepine is combined with Idarubicin.
Eculizumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Carbamazepine is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Carbamazepine is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Carbamazepine is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Carbamazepine is combined with Brequinar.
Interferon alfa The risk or severity of adverse effects can be increased when Carbamazepine is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Carbamazepine is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Carbamazepine is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Carbamazepine is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Carbamazepine is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Carbamazepine is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Carbamazepine is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Carbamazepine is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Belimumab.
Carfilzomib The risk or severity of adverse effects can be increased when Carbamazepine is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Carbamazepine is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Carbamazepine is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Carbamazepine is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Carbamazepine is combined with Antilymphocyte immunoglobulin (horse).
Ixekizumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Carbamazepine is combined with Pirarubicin.
Peficitinib The risk or severity of adverse effects can be increased when Carbamazepine is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Brodalumab.
Sirukumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Sirukumab.
Guselkumab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Guselkumab.
Ozanimod The risk or severity of adverse effects can be increased when Carbamazepine is combined with Ozanimod.
Mizoribine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Mizoribine.
Gusperimus The risk or severity of adverse effects can be increased when Carbamazepine is combined with Gusperimus.
Cepeginterferon alfa-2B The risk or severity of adverse effects can be increased when Carbamazepine is combined with Cepeginterferon alfa-2B.
Trofosfamide The risk or severity of adverse effects can be increased when Carbamazepine is combined with Trofosfamide.
Doxifluridine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Doxifluridine.
Deoxyspergualin The risk or severity of adverse effects can be increased when Carbamazepine is combined with Deoxyspergualin.
Acteoside The risk or severity of adverse effects can be increased when Carbamazepine is combined with Acteoside.
9-(N-methyl-L-isoleucine)-cyclosporin A The risk or severity of adverse effects can be increased when Carbamazepine is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Fluocortin The risk or severity of adverse effects can be increased when Carbamazepine is combined with Fluocortin.
Begelomab The risk or severity of adverse effects can be increased when Carbamazepine is combined with Begelomab.
Fluperolone The risk or severity of adverse effects can be increased when Carbamazepine is combined with Fluperolone.
Fluclorolone The risk or severity of adverse effects can be increased when Carbamazepine is combined with Fluclorolone.
Monomethyl fumarate The risk or severity of adverse effects can be increased when Carbamazepine is combined with Monomethyl fumarate.

Target Protein

Voltage-gated sodium channel alpha subunit SCN1A
Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Synthesis reference: Ketan Dhansukhlal Vyas, Wajid Sajjad Jafri, Ashok Krishna Kulkarni, "Process for preparing carbamazepine from iminostilbene." U.S. Patent US6245908, issued February, 1998.
Artikel (PubMed)
  • PMID: 15292462
    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.
  • PMID: 18088268
    Sisodiya SM, Goldstein DB: Drug resistance in epilepsy: more twists in the tale. Epilepsia. 2007 Dec;48(12):2369-70.
  • PMID: 23961295
    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.
  • PMID: 22278332
    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.
  • PMID: 11926264
    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.
  • PMID: 22620289
    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.
  • PMID: 8698724
    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.
  • PMID: 9187275
    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.
Menampilkan 8 dari 14 artikel.
Textbook
  • Jasdave S. Maan; Abdolreza Saadabadi (2019). Carbamazepine. Stat Pearls Publishing.

Contoh Produk & Brand

Produk: 338 • International brands: 12
Produk
  • Apo-carbamazepine
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Apo-carbamazepine CR
    Tablet, extended release • 200 mg • Oral • Canada • Generic • Approved
  • Apo-carbamazepine CR
    Tablet, extended release • 400 mg • Oral • Canada • Generic • Approved
  • Bio-carbamazepine
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Carbamazepin
    Tablet, extended release • 200 mg/1 • Oral • US • Generic • Approved
  • Carbamazepine
    Tablet • 100 mg/1 • Oral • US • Approved
  • Carbamazepine
    Tablet • 200 mg/1 • Oral • US • Approved
  • Carbamazepine
    Tablet • 300 mg/1 • Oral • US • Approved
Menampilkan 8 dari 338 produk.
International Brands
  • Actebral — Sanofi-Aventis
  • Anleptic — Square
  • Biston — Zentiva
  • Carbamat — AstraZeneca
  • Neurotop — Gerot
  • TEGretol Chewtabs
  • TEGretol-CR — Novartis
  • TEGretol-XR — Novartis
  • Teril — Taro
  • Timonil — Desitin

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