Tegretol: Stabilizing Seizures and Mood with Precision
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Tegretol (carbamazepine) is a first-line anticonvulsant and mood-stabilizing agent with a well-established efficacy profile in neurology and psychiatry. As a sodium channel blocker, it modulates neuronal excitability, making it a cornerstone therapy for partial and generalized tonic-clonic seizures, trigeminal neuralgia, and bipolar disorder. Its decades of clinical use are supported by extensive research, offering physicians a reliable option for long-term management. This detailed product card provides a comprehensive overview for healthcare professionals to support informed prescribing and patient counseling.
Features
- Active ingredient: Carbamazepine
- Available formulations: Immediate-release tablets (100 mg, 200 mg), chewable tablets (100 mg), extended-release tablets (100 mg, 200 mg, 400 mg), and oral suspension (100 mg/5 mL)
- Mechanism of action: Voltage-gated sodium channel blockade, reducing synaptic transmission and stabilizing neuronal membranes
- Half-life: Initial 25–65 hours; reduces to 12–17 hours with autoinduction (chronic dosing)
- Metabolism: Hepatic, primarily via CYP3A4, with active metabolite (carbamazepine-10,11-epoxide)
- Bioavailability: 75–85% for oral forms; extended-release provides smoother plasma concentrations
- Pregnancy category: D; known teratogenic risk (neural tube defects, craniofacial abnormalities)
Benefits
- Effectively reduces frequency and severity of focal and generalized seizures
- Provides significant pain relief in trigeminal neuralgia by dampening aberrant nerve signals
- Stabilizes mood episodes in bipolar disorder, particularly manic and mixed states
- Offers flexible dosing formulations to accommodate individual patient needs and adherence
- Backed by decades of real-world evidence demonstrating long-term tolerability and efficacy
- Generic availability enhances cost-effectiveness and accessibility
Common use
Tegretol is indicated for the treatment of epilepsy, specifically partial seizures with complex symptomatology, generalized tonic-clonic seizures, and mixed seizure patterns. It is also approved for the relief of pain associated with trigeminal neuralgia and as a mood stabilizer in bipolar I disorder to prevent or ameliorate manic or mixed episodes. Off-label uses include treatment for certain neuropathic pain conditions, restless legs syndrome, and alcohol withdrawal syndrome, though evidence varies.
Dosage and direction
Dosage must be individualized based on clinical response, tolerability, and plasma concentration monitoring. For adults with epilepsy, initial dose is 200 mg orally twice daily (immediate-release) or once daily (extended-release), increased gradually by 200 mg daily at weekly intervals. Maintenance dose typically ranges from 800–1200 mg/day divided into 2–4 doses (immediate-release) or 1–2 doses (extended-release). For trigeminal neuralgia, start with 100 mg twice daily, increasing by up to 200 mg/day until pain relief is achieved (max 1200 mg/day). In bipolar disorder, target doses are similar to epilepsy regimens. Always take with food to minimize gastrointestinal upset. Regular therapeutic drug monitoring (4–12 mcg/mL) is recommended, especially during dose titration.
Precautions
Monitor blood counts (including platelets) and liver function tests at baseline and periodically, due to risk of agranulocytosis, aplastic anemia, and hepatotoxicity. Use with caution in patients with cardiac conduction abnormalities, hepatic or renal impairment, glaucoma, or history of adverse hematologic reactions. Tegretol induces its own metabolism (autoinduction), often necessitating dose adjustments after several weeks. Avoid abrupt discontinuation to prevent seizure recurrence or withdrawal symptoms. Perform HLA-B*1502 screening in patients of Asian ancestry before initiation to assess risk of serious dermatologic reactions.
Contraindications
Tegretol is contraindicated in patients with known hypersensitivity to carbamazepine or tricyclic antidepressants, history of bone marrow depression, concomitant use of monoamine oxidase inhibitors (or within 14 days of discontinuation), and in those with porphyria. Do not use in patients with atrioventricular block or other significant conduction defects unless paced.
Possible side effect
Common adverse reactions (≥10%) include dizziness, drowsiness, unsteadiness, nausea, vomiting, and diplopia. Less frequently (1–10%), rash, hyponatremia, elevated liver enzymes, leukopenia, or blurred vision may occur. Rare (<1%) but serious effects include Stevens-Johnson syndrome, toxic epidermal necrolysis, agranulocytosis, aplastic anemia, hepatitis, pancreatitis, and cardiac conduction disturbances. Most side effects are dose-related and may diminish over time.
Drug interaction
Tegretol is a potent inducer of CYP3A4 and may reduce plasma levels of many drugs, including oral contraceptives, warfarin, certain statins, many antipsychotics, and other anticonvulsants. Conversely, drugs that inhibit CYP3A4 (e.g., fluconazole, erythromycin, verapamil) can increase carbamazepine levels. Avoid coadministration with nefazodone, delavirdine, or other non-nucleoside reverse transcriptase inhibitors. Use caution with other CNS depressants (alcohol, benzodiazepines, opioids) due to additive sedation.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next dose. In that case, skip the missed dose and resume the regular schedule. Do not double the dose to make up for a missed one, as this may increase the risk of adverse effects.
Overdose
Symptoms of overdose may include dizziness, ataxia, drowsiness, nausea, vomiting, urinary retention, tremor, agitation, nystagmus, seizures, respiratory depression, coma, and cardiac arrhythmias. Management includes gastric lavage (if recent ingestion), activated charcoal, and supportive care with monitoring of vital signs, electrolytes, and ECG. Hemodialysis is not effective due to high protein binding. Specific antidote is not available.
Storage
Store at room temperature (15–30°C or 59–86°F) in a tightly closed container, protected from light and moisture. Keep all medications out of reach of children and pets. Do not use oral suspension if it has been frozen. Discard any unused medication after the expiration date.
Disclaimer
This information is intended for healthcare professionals and is not a substitute for clinical judgment or official prescribing information. Always consult the full product monograph and relevant clinical guidelines before prescribing. Dosage, indications, and safety profiles may vary by region and patient-specific factors.
Reviews
Tegretol remains a widely respected agent in neurological and psychiatric therapeutics. Clinical studies and meta-analyses consistently affirm its efficacy in seizure control and mood stabilization, though its side effect profile and monitoring requirements are noted. Many clinicians appreciate its predictability after the autoinduction phase and its formulary availability. Patient experiences vary; some report significant improvement in quality of life, while others discontinue due to adverse effects such as drowsiness or cognitive blunting. Ongoing pharmacogenomic research continues to refine its risk-benefit profile.