Suximide (Capsules) Instructions for Use

ATC Code

N03AD01 (Ethosuximide)

Active Substance

Ethosuximide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Anticonvulsant drug

Pharmacotherapeutic Group

Antiepileptic agent

Pharmacological Action

An anticonvulsant agent of the succinimide group. The mechanism of action is not fully understood. It is believed that Ethosuximide raises the threshold for the occurrence of epileptic seizures by inhibiting synaptic transmission, apparently in the motor areas of the cerebral cortex. On the EEG, this reduces the frequency of the spike-wave complexes characteristic of petit mal seizures.

These effects may be the result of a direct change in neuronal membrane function or an influence on mediator processes. There is evidence that Ethosuximide at relatively low concentrations disrupts the function of T-type calcium channels.

Ethosuximide has an analgesic effect in trigeminal neuralgia, being less effective than carbamazepine.

Pharmacokinetics

When taken orally, absorption from the gastrointestinal tract is rapid and almost complete. The time to reach C_max in blood plasma in adults is 2-4 hours, in children – 3-7 hours. It is easily distributed to all body tissues except adipose tissue.

The concentrations of ethosuximide in saliva and tear fluid are equivalent to those in blood serum. Protein binding is insignificant. It is metabolized in the liver. T_1/2 in adults is 56-60 hours, in children – 30-36 hours. It is excreted by the kidneys, with up to 20% of ethosuximide excreted unchanged.

Indications

Treatment of petit mal epileptic seizures. Trigeminal neuralgia.

ICD codes

Dosage Regimen

Capsules

Orally for adults and children over 6 years old at a dose of 15-30 mg/kg/day, if necessary, the dose is gradually increased taking into account the clinical effect, frequency of administration is 2-4 times/day. For children under 6 years of age – 15-40 mg/kg/day, if necessary, the dose is gradually increased taking into account the clinical effect, frequency of administration is 2-4 times/day.

Maximum daily doses when taken orally for adults and children over 6 years old – 1.5 g; for children under 6 years old – 1 g.

Adverse Reactions

From the central nervous system ataxia, dizziness, drowsiness, headache, hiccups may occur; rarely – irritability, unusual fatigue, weakness, aggressiveness, decreased concentration, depression, nightmares, increased tonic-clonic seizures, paranoid psychosis.

Allergic reactions eosinophilia; rarely – itchy erythematous rash, Stevens-Johnson syndrome, lupus-like syndrome (skin rash and itching, swollen lymph nodes, sore throat and fever, muscle pain).

From the digestive system anorexia, nausea, vomiting, stomach cramps.

From the hematopoietic system agranulocytosis, aplastic anemia, leukopenia, pancytopenia.

Contraindications

Hypersensitivity to ethosuximide.

Use in Pregnancy and Lactation

Ethosuximide penetrates into breast milk, but no complications in humans have been reported. If it is necessary to use during pregnancy and lactation, the intended benefit of therapy for the mother and the potential risk to the fetus or child should be assessed; in such cases, the minimum effective doses should be used.

Use in Hepatic Impairment

Not recommended for use in patients with impaired liver function.

Use in Renal Impairment

Not recommended for use in patients with impaired renal function.

Pediatric Use

Use is possible according to the dosage regimen.

Special Precautions

Not recommended for use in patients with impaired liver and/or kidney function, with blood diseases, intermittent porphyria. If there is hypersensitivity to other anticonvulsants of the succinimide group, hypersensitivity reactions to ethosuximide may also develop.

Do not allow alcohol consumption during treatment.

Effect on ability to drive vehicles and operate machinery

Use with caution in patients engaged in potentially hazardous activities that require high concentration and rapid psychomotor reactions.

Drug Interactions

With simultaneous use with valproic acid, an increase in the concentration of ethosuximide and a decrease in the concentration of valproate in blood plasma is possible.

With simultaneous use with haloperidol, changes in the type and/or frequency of epileptic seizures and a significant decrease in the concentration of haloperidol in blood plasma are possible.

With simultaneous use with carbamazepine, primidone, phenytoin, phenobarbital, the concentration of ethosuximide in blood plasma decreases.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.