Carbamazepine

CHEMBL108 Phase 4 Đã phê duyệt Small molecule
Half-Life
25-65 hours
Bioavailability
Protein Binding
Molecular Weight
236.3 g/mol
LogP
2.5
Phase
4

Prescribed for epileptic seizures, trigeminal neuralgia, and bipolar disorder, carbamazepine quiets abnormal neuronal firing by blocking voltage-gated sodium channels and holding them in an inactivated state. This blunts the rapid, repetitive discharges that drive both seizures and certain forms of nerve pain, which also underlies its use as a mood stabilizer. It is a tricyclic compound (C15H12N2O) reported with a half-life in the range of 25 to 65 hours. Two features shape its clinical profile: a wide network of drug interactions, and a rare but potentially fatal skin reaction, Stevens-Johnson syndrome, that warrants careful attention during treatment. An approved, long-established antiepileptic, it remains a reference agent for focal seizures and for trigeminal neuralgia.

An anticonvulsant and mood-stabilizing drug used to treat epileptic seizures, trigeminal neuralgia, and bipolar disorder. It works by blocking voltage-gated sodium channels to reduce abnormal electrical activity in the brain. It requires monitoring due to drug interactions and a rare but potentially fatal skin reaction called Stevens-Johnson syndrome.

Khối lượng phân tử

236,2690 g/mol

LogP

2,50

TPSA

46,30 Ų

Lipinski RO5

Đạt

Lĩnh vực điều trị

Phân loại thuốc

Cơ chế tác dụng

Voltage-gated sodium channel blocker.

Pharmacokinetics (PK)

Half-Life 25-65 hours

Pharmacodynamics (PD)

Cơ chế

Voltage-gated sodium channel blocker.

Cấu trúc 2D

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SMILES

NC(=O)N1c2ccccc2C=Cc2ccccc21

InChI

InChI=1S/C15H12N2O/c16-15(18)17-13-7-3-1-5-11(13)9-10-12-6-2-4-8-14(12)17/h1-10H,(H2,16,18)

Molecular Formula

C15H12N2O

HBD / HBA

1 / 1

Liên kết có thể quay

0

Nguyên tử nặng

18

Major Carbamazepine + Tacrolimus

Carbamazepine, a potent CYP3A4 inducer, substantially decreases tacrolimus blood concentrations, risking acute rejection in transplant recipients.

Major Carbamazepine + Quetiapine

Carbamazepine dramatically reduces quetiapine plasma concentrations, potentially rendering antipsychotic treatment ineffective.

Major Carbamazepine + Warfarin

Carbamazepine markedly reduces warfarin plasma concentrations, potentially resulting in sub-therapeutic anticoagulation and increased thromboembolic risk.

Major Carbamazepine + Cyclosporine

Carbamazepine dramatically reduces cyclosporine plasma levels through potent CYP3A4 induction, placing transplant patients at severe rejection risk.

Minor Carbamazepine + Metformin

Carbamazepine may modestly affect glucose homeostasis and potentially interact with metformin's antidiabetic effect through metabolic mechanisms.

Moderate Carbamazepine + Phenytoin

Carbamazepine and phenytoin have complex bidirectional interactions that can alter plasma levels of either drug in unpredictable ways.

Moderate Carbamazepine + Valproic Acid

Carbamazepine reduces valproic acid levels through enzyme induction, while valproic acid inhibits epoxide hydrolase, increasing the toxic carbamazepine-10,11-epoxide metabolite.

Moderate Carbamazepine + Topiramate

Carbamazepine reduces topiramate plasma concentrations by approximately 40% through enzyme induction, potentially impairing seizure control.

Moderate Carbamazepine + Venlafaxine

Carbamazepine significantly reduces venlafaxine plasma concentrations through CYP3A4 induction, potentially reducing antidepressant efficacy.

Moderate Carbamazepine + Levodopa

Carbamazepine may reduce levodopa efficacy through enzyme induction and pharmacodynamic antagonism, potentially worsening Parkinson's disease control.

Moderate Carbamazepine + Omeprazole

Carbamazepine reduces omeprazole plasma concentrations through CYP3A4 induction, potentially reducing the efficacy of acid suppression therapy.

Moderate Carbamazepine + Dexamethasone

Carbamazepine is a potent CYP3A4 inducer that markedly increases dexamethasone clearance, reducing its plasma concentrations by 50–80% and risking loss of anti-inflammatory and immunosuppressive efficacy.

Moderate Carbamazepine + Sertraline

Carbamazepine, a potent enzyme inducer, significantly reduces sertraline plasma concentrations, potentially impairing antidepressant efficacy.

Moderate Carbamazepine + Duloxetine

Carbamazepine substantially reduces duloxetine plasma levels through CYP1A2 and CYP3A4 induction, risking loss of antidepressant efficacy.

Moderate Carbamazepine + Lamotrigine

Carbamazepine reduces lamotrigine plasma concentrations by approximately 50% through enzyme induction, requiring lamotrigine dose adjustment.

Moderate Carbamazepine + Levothyroxine

Carbamazepine induces hepatic CYP enzymes involved in thyroid hormone metabolism, increasing levothyroxine clearance and potentially causing hypothyroid relapse in patients on replacement therapy.

Major Carbamazepine + Aripiprazole

Carbamazepine dramatically reduces aripiprazole plasma levels through potent CYP3A4 induction, potentially rendering antipsychotic treatment ineffective.

Moderate Carbamazepine + Acetaminophen

Carbamazepine induces CYP enzymes that convert acetaminophen to its hepatotoxic metabolite NAPQI, increasing the risk of acetaminophen-induced liver injury even at therapeutic doses.

No side effects recorded

Side effect data is not yet available for this drug.

Câu hỏi thường gặp

An anticonvulsant and mood-stabilizing drug used to treat epileptic seizures, trigeminal neuralgia, and bipolar disorder. It works by blocking voltage-gated sodium channels to reduce abnormal electrical activity in the brain. It requires monitoring due to drug interactions and a rare but potentially fatal skin reaction called Stevens-Johnson syndrome.

Voltage-gated sodium channel blocker.

Key pharmacokinetic parameters for Carbamazepine: Half-life: 25-65 hours.

Yes, Carbamazepine is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

Related Drugs

{# References & Data Sources section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

References & Data Sources

  • ChEMBL — European Bioinformatics Institute (EBI). CHEMBL108. Open-access bioactivity database.
  • PubChem — National Center for Biotechnology Information (NCBI). CID 2554. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.

Tuyên bố miễn trách y tế

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.