Methsuximide (Celontin) - Uses, Dose, Side effects, MOA, Brands

Methsuximide (Celontin) is a succinimide like ethosuximide. It is used in the treatment of patients with absence seizures or petit mal seizures (in which the patient suddenly becomes blank and unresponsive for a brief period of time)

Methsuximide (Celontin) Uses:

  • Absence (petit mal) seizures, refractory:

    • This medicine is recommended to help with seizures called absence (petit mal) that don't get better with other medicines.

Methsuximide (Celontin) Dose in Adults:

Methsuximide (Celontin) Dose in refractory Absence (petit mal) seizures:

  • Take 300 mg by mouth every day for the first week.

  • The most you should take in one day is 30 mg for every kilogram of your weight, but it should not go over 1,200 mg per day, divided into separate doses.

  • Consider going slower when increasing the dose to prevent any harmful effects and the quick buildup of the active form of the medicine (N-desmethylmethsuximide).

     

Methsuximide (Celontin) Dose in childrens:

Methsuximide (Celontin) Dose in refractory Seizures; adjunct therapy:

There's not much information available for different types of seizures, except for absence seizures.

This medication has proven to be helpful, particularly in treating Lennox-Gastaut syndrome and symptomatic focal epilepsies.

There's not much information available for different types of seizures, except for absence seizures.

This medication has proven to be helpful, particularly in treating Lennox-Gastaut syndrome and symptomatic focal epilepsies.

  • Children and Adolescents:

    • Start with 5 mg for every kilogram of body weight per day, taken orally once a day.

    • Increase the dose gradually, by 3.2 to 5.5 mg for every kilogram per week, in three or four separate doses each day, as long as it is well-tolerated, until you achieve the desired response and reach the target levels in the blood.

    • The maximum daily dose is 30 mg for every kilogram of body weight, but it should not go over 1,200 mg per day, divided into separate doses.

    • It's recommended to maintain the active metabolite N-desmethylmethsuximide (NDMSM) in the blood within a therapeutic range of 25 to 45 micrograms per milliliter for pediatric patients.


Pregnancy Risk Category: C

  • Various factors, such as genetics and medications, make epileptic patients more prone to having birth defects.

  • It's typically advised to use a single medication (monotherapy) to minimize risks, and it's better to avoid using multiple drugs at higher doses (polytherapy).

  • When seizure control is optimized, individuals planning a pregnancy should undergo testing to check the levels of antiepileptic medications in their system before proceeding.

  • This precaution helps ensure a safer environment for pregnancy.

  • Various factors, such as genetics and medications, make epileptic patients more prone to having birth defects.

  • It's typically advised to use a single medication (monotherapy) to minimize risks, and it's better to avoid using multiple drugs at higher doses (polytherapy).

  • When seizure control is optimized, individuals planning a pregnancy should undergo testing to check the levels of antiepileptic medications in their system before proceeding.

  • This precaution helps ensure a safer environment for pregnancy.

Use of methsuximide during breastfeeding

  • We don't know if the drug can pass into breast milk.
  • It's crucial to carefully consider the advantages and disadvantages of treating the mother, taking into account the potential for the infant to be exposed to the medication.

Dose in Kidney Disease:

 

The manufacturer's instructions do not mention any specific changes to the dosage.

However, individuals with kidney issues should approach its use with caution.

Dose in Liver disease:

The manufacturer's instructions do not provide specific adjustments to the dosage.

 

Mechanism of action of Methsuximide (Celontin):

  • It works by decreasing the transmission of signals in the motor cortex of the brain and raises the threshold for experiencing seizures.
  • Additionally, it helps in reducing the spike and wave patterns associated with absence seizures in patients.

Metabolism:

  • In the liver, it undergoes rapid demethylation, transforming into N-desmethylmethsuximide, which is the active metabolite.

Half-life elimination:

  • The drug takes about 2 to 4 hours to reach peak concentration.

  • After conversion, the active metabolite N-desmethylmethsuximide stays in the system for different durations:

  • In children, it lasts for approximately 26 hours.
  • In adults, it has a wider range, lasting from 28 to 80 hours.

Time to peak, serum:

  • It reaches peak concentration within 1 to 3 hours.

Excretion:

  • Less than 1% of the drug is excreted unchanged in the urine.

International Brand Names of Methsuximide:

  • Celontin

Methsuximide Brand Names in Pakistan:

  • No Brands Available in Pakistan.