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Description of the drug CARBAMAZEPINE PHARMLAND

With simultaneous use of inhibitors of the CYP3A4 isoenzyme, an increase in the concentration of carbamazepine in the blood plasma is possible.

With the simultaneous use of inducers of the CYP3A4 isoenzyme system, it is possible to accelerate the metabolism of carbamazepine, reduce its concentration in the blood plasma, and reduce the therapeutic effect.

With simultaneous use, carbamazepine stimulates the metabolism of anticoagulants and folic acid.

When used simultaneously with valproic acid, a decrease in the concentration of carbamazepine and a significant decrease in the concentration of valproic acid in the blood plasma is possible. At the same time, the concentration of carbamazepine metabolite, carbamazepine epoxide, increases (probably due to inhibition of its conversion to carbamazepine-10,11-trans-diol), which also has anticonvulsant activity, so the effects of this interaction can be neutralized, but more often adverse reactions occur - blurred vision, dizziness, vomiting, weakness, nystagmus. With the simultaneous use of valproic acid and carbamazepine, a hepatotoxic effect may develop (apparently due to the formation of a minor metabolite of valproic acid, which has a hepatotoxic effect).

With simultaneous use, valpromide reduces the metabolism in the liver of carbamazepine and its metabolite carbamazepine-epoxide due to inhibition of the enzyme epoxide hydrolase. This metabolite has anticonvulsant activity, but with a significant increase in plasma concentration it can have a toxic effect.

When used simultaneously with verapamil, diltiazem, isoniazid, dextropropoxyphene, viloxazine, fluoxetine, fluvoxamine, cimetidine, acetazolamide, danazol, desipramine, nicotinamide (in adults, only in high doses), erythromycin, troleandomycin, josamycin, clarithromycin; with azoles (including itraconazole, ketoconazole, fluconazole), terfenadine, loratadine, it is possible to increase the concentration of carbamazepine in the blood plasma with the risk of side effects (dizziness, drowsiness, ataxia, diplopia).

When used simultaneously with hexamidine, the anticonvulsant effect of carbamazepine is weakened; with hydrochlorothiazide, furosemide - a decrease in sodium content in the blood is possible; with hormonal contraceptives - the effect of contraceptives may weaken and acyclic bleeding may develop.

When used simultaneously with thyroid hormones, it is possible to increase the elimination of thyroid hormones; with clonazepam - it is possible to increase the clearance of clonazepam and decrease the clearance of carbamazepine; with lithium preparations - a mutual enhancement of the neurotoxic effect is possible.

When used simultaneously with primidone, a decrease in the concentration of carbamazepine in the blood plasma is possible. There are reports that primidone may increase plasma concentrations of the pharmacologically active metabolite, carbamazepine 10,11-epoxide.

When used simultaneously with ritonavir, the side effects of carbamazepine may increase; with sertraline - a decrease in the concentration of sertraline is possible; with theophylline, rifampicin, cisplatin, doxorubicin - a decrease in the concentration of carbamazepine in the blood plasma is possible; with tetracycline - the effects of carbamazepine may be weakened.

With simultaneous use with felbamate, a decrease in the concentration of carbamazepine in the blood plasma is possible, but an increase in the concentration of the active metabolite of carbamazepine-epoxide, while a decrease in the plasma concentration of felbamate is possible.

When used simultaneously with phenytoin and phenobarbital, the concentration of carbamazepine in the blood plasma decreases. A mutual weakening of the anticonvulsant effect is possible, and in rare cases, its strengthening.

Cautions and contraindications

You need to watch for bleeding, bruising, mouth ulcers, infections, and fever. Taking carbamazepine increases the risk of aplastic anemia and agranulocytosis by 5-8 times.
Use cautiously with MAOIs.
May cause exacerbation of angle-closure glaucoma.
Reduces the effectiveness of hormonal contraceptives.
Restriction of fluid intake may be necessary due to the risk of interfering with antidiuretic hormone production.
Cannot be used if the patient has a history of bone marrow suppression.
Do not use if the patient is allergic to any tricyclic compounds.

Indications

Ministry of Health of Russia

E23.2 Diabetes insipidus
F10.3 Withdrawal state
F30 Manic episode
F31 Bipolar affective disorder
G35 Multiple sclerosis
G40 Epilepsy
G40.1 Localized (focal) (partial) symptomatic epilepsy and epileptic syndromes with simple partial seizures
G40.2 Localized (focal) (partial) symptomatic epilepsy and epileptic syndromes with complex partial seizures
G40.3 Generalized idiopathic epilepsy and epileptic syndromes
G50.0 Trigeminal neuralgia
G52.1 Lesions of the glossopharyngeal nerve
G63.2 Diabetic polyneuropathy (E10-E14+ with common fourth character .4)
R35 Polyuria
R52.9 Pain, unspecified
R63.1 Polydipsia

FDA recommendations

Partial seizures with complex symptoms
Generalized tonic-clonic seizures (grand mal)
Mixed seizures
Trigeminal neuralgia pain
Acute episode of mania/mixed mania

UK Medicines and Healthcare Products Regulatory Agency guidelines

Generalized tonic-clonic and partial seizures
Trigeminal neuralgia pain
Prevention of manic-depressive psychosis in patients not responding to lithium treatment

Indications for use of "Carbamazepine"

Narcologists prescribe Carbamazepine as a drug that has a psychotropic and anticonvulsant effect.

This drug has a pronounced anticonvulsant effect, inhibits voltage-sensitive sodium channels, has an inhibitory effect on excitatory amino acid transmission in the limbic system, inhibits GABA metabolism, suppresses the presynaptic activity of serotonin with a single intake of alcohol in the body and enhances it with chronic administration.

Carbamazepine has an antimanic effect, which is not directly related to the dopamine blocking effect. The antidepressant activity of the drug is determined by its effect on the GABAergic system. Carbamazepine also inhibits calcium channels. Therefore, the drug is very effective in the treatment of epileptic patients and patients with affective psychoses.

Carbamazepine is able to re-synchronize a disturbed bio-rhythmic organization. The purpose of this drug for the treatment of alcoholics is explained by the effect of the drug on sodium and potassium channels and the flow of calcium into cells, the suppression of the activity of the glutamatergic system and inhibition of GABA metabolism, and changes in the functioning of the serotonergic and dopaminergic systems.

Initially, Carbamazepine was used to relieve alcohol withdrawal syndrome, since the drug has an anticonvulsant effect and reduces the severity of vegetative and mental disorders.

The drug is widely used for its low frequency of side effects and the virtual absence of hepatotoxic and hypnotic effects.

Treatment regimen

Dosage and dose selection

400-1200 mg/day
Children under 6 years: 10-20 mg/kg per day

Bipolar disorder, seizures (adults, children over 13): Start with 200 mg twice daily; increase every week by 200 mg/day in several doses; maximum for adults 1200 mg/day; maximum for children 13-15 years old – 1000 mg/day; some patients may require doses up to 1600 mg/day.

Trigeminal neuralgia pain: start with 100 mg twice daily; increase every week by 200 mg/day in divided doses.

Best taken with food
Slowly increasing the dose delays the onset of the therapeutic effect, but increases tolerance to sedative side effects
If other sedatives are being taken, increase the dose slowly
Over time, after several weeks of treatment, dose adjustment is required

How quickly does it work?

Response to acute mania may occur within a few weeks.

It may take several months for your mood to stabilize.

Cramps should stop after 2 weeks.

Expected Result

Disappearance of symptoms.

Treatment can be continued indefinitely to prevent mania or seizures.

If it doesn't work

(for bipolar disorder)

Increase the dose;

Switch to another drug or add another drug;

Connect psychotherapy;

Determine if there is a comorbid condition

How to stop taking it

Reduce the dose gradually. Abruptly stopping use increases the risk of bipolar disorder relapse. In epilepsy, abrupt cessation can trigger seizures [1].

Treatment combinations

Lithium
Valproic acid
Atypical antipsychotics
Lamotrigine
Antidepressants (with caution, as there is a risk of mood destabilization) [1].

Special patient groups

Patients with kidney problems

The dose needs to be reduced [1].

Patients with liver disease

Use with caution [1].

Patients with heart disease

Use with caution [1].

Elderly patients

In older people, side effects are more pronounced.

Children and teenagers

Approved for use in epilepsy.
Children 6-12 years: initial dose 100 mg twice daily; increase every week by 100 mg/day in several doses; maximum dose 1000 mg/day; maintenance dose 400-800 mg/day.
Children 5 years and younger: initial dose 10-20 mg/kg per day 2-3 times daily; increase every week if there is a need; maximum dose 35 mg/kg/day.

Pregnant

In the first trimester, it increases the risk of fetal developmental abnormalities. If treatment continues, tests should be performed to identify pregnancy pathologies. To reduce the risk, you should start taking folic acid (1 mg/day) earlier than usual.
For bipolar disorder, carbamazepine should be discontinued until pregnancy occurs. During pregnancy, atypical antipsychotics are preferred.

Breast-feeding

It is recommended that you stop taking carbamazepine or stop breastfeeding.