Drug information of Ethosuximide

Mechanism of effect

Binds to T-type voltage sensitive calcium channels. Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death.

Pharmacodynamic

Used in the treatment of epilepsy. Ethosuximide suppresses the paroxysmal three cycle per second spike and wave activity associated with lapses of consciousness which is common in absence (petit mal) seizures.

The frequency of epileptiform attacks is reduced, apparently by depression of the motor cortex and elevation of the threshold of the central nervous system to convulsive stimuli.

Pharmacokinetics

Used in the treatment of epilepsy. Ethosuximide suppresses the paroxysmal three cycle per second spike and wave activity associated with lapses of consciousness which is common in absence (petit mal) seizures.

The frequency of epileptiform attacks is reduced, apparently by depression of the motor cortex and elevation of the threshold of the central nervous system to convulsive stimuli.

Drug indications

Epilepsy , control of absence (petit mal) epilepsy.

Dosage

Usual Adult Dose for Seizures

Initial dose: 500 mg (10 mL) orally daily

Maintenance dose: Dosage may be increased by small increments, for example 250 mg daily every 4 to 7 days, until optimal seizure control with minimal side effects is achieved. Dosages greater than 1.5 g per day, in divided doses, should be administered only under strict supervision of a physician.

Usual Pediatric Dose for Seizures

3 to 6 years:

Initial dose: 250 mg (5 mL) orally daily

Maintenance dose: Dosage may be increased by small increments, for example 250 mg daily every 4 to 7 days, until optimal seizure control with minimal side effects is achieved. For most pediatric patients the optimal dose is 20 mg/kg/day in divided doses. Dosages greater than 1.5 g per day, in divided doses, should be administered only under close supervision by a physician.

> 6 to 18 years:

Initial dose: 500 mg (10 mL) orally daily

Maintenance dose: Dosage may be increased by small increments, for example 250 mg daily every 4 to 7 days, until optimal seizure control with minimal side effects is achieved. For most pediatric patients the optimal dose is 20 mg/kg/day in divided doses. Dosages greater than 1.5 g per day, in divided doses, should be administered only under close supervision by a physician.

Drug contraindications

hypersensitivity to drug or its components.

Side effects

sleep disorder , nausea , Headache , abdominal pain , dizziness , vomiting , allergic reaction , vertigo , Depression , Diarrhea , urticaria , weight decrease , anorexia , somnolence , itching , hirsutism , Agranulocytosis , difficulty urinating , tiredness , swelling of the tongue , Abdominal pain , Leukopenia , Systemic Lupus Erythematosus , psychoses

Interactions

Aprepitant , Isoniazid , Bosentan , Paroxetine , Pramipexole , Thalidomide , orlistat , Fluconazole , Phenobarbital , Phenytoin , Lorazepam , Minocycline , Magnesium sulfate , Zolpidem , Valproate sodium , Disulfiram , Sodium Oxybate , brigatinib , lumacaftor and Ivacaftor , Lorlatinib , Glycerol Phenylbutyrate , secukinumab

Alerts

• Blood dyscrasias: Severe blood dyscrasias (some fatal) have been reported. Monitor blood counts periodically, especially if signs/symptoms of infection develop.
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Dermatologic reactions: Severe reactions, including Stevens-Johnson syndrome (SJS), have been reported with an onset usually within 28 days, but may be observed later. Drug should be discontinued if there are any signs of rash, unless the rash is clearly not drug-related. If SJS is suspected do not resume ethosuximide and consider alternative therapy.
• Hepatic effects: Changes in hepatic function have been reported. Monitor liver function studies periodically.
• Multiorgan hypersensitivity reactions: Potentially serious, sometimes fatal drug reaction with eosinophilia and systemic symptoms (DRESS), also known as multiorgan hypersensitivity reactions, have been reported. Monitor for signs and symptoms (eg, fever, rash, exfoliative dermatitis, lymphadenopathy, facial swelling, eosinophilia) in association with other organ system involvement (eg, hepatitis, nephritis, hematologic abnormalities, pneumonitis, myocarditis, myositis, pericarditis). If DRESS is suspected, discontinue therapy.
• Renal effects: Changes in renal function have been reported. Monitor urinalysis periodically.
• Systemic lupus erythematous: Cases of systemic lupus erythematosus (SLE) have been reported.
• Suicidal ideation: Pooled analysis of trials involving various antiepileptics (regardless of indication) showed an increased risk of suicidal thoughts/behavior (incidence rate: 0.43% treated patients compared to 0.24% of patients receiving placebo); risk observed as early as 1 week after initiation and continued through duration of trials (most trials ≤24 weeks). Monitor all patients for notable changes in behavior that might indicate suicidal thoughts or depression; notify healthcare provider immediately if symptoms occur.

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you have:

• If you have an allergy to ethosuximide or any other part of this medicine (ethosuximide capsules).

• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.

Avoid driving and doing other tasks or actions that call for you to be alert or have clear eyesight until you see how this medicine (ethosuximide capsules) affects you.

Do not stop taking this medicine (ethosuximide capsules) all of a sudden without calling your doctor. You may have a greater risk of side effects. If you need to stop this medicine (ethosuximide capsules), you will want to slowly stop it as ordered by your doctor.

Very bad and sometimes deadly blood cell problems may happen. You will need to have blood tests while you take this medicine (ethosuximide capsules). Talk with your doctor. Tell your doctor right away if you have any signs of infection.

Have blood work checked as you have been told by the doctor. Talk with the doctor.

Patients who take this medicine (ethosuximide capsules) may be at a greater risk of having thoughts or actions of suicide. The risk may be greater in people who have had these thoughts or actions in the past. Call the doctor right away if signs like low mood (depression), nervousness, restlessness, grouchiness, panic attacks, or changes in mood or actions are new or worse. Call the doctor right away if any thoughts or actions of suicide occur.

Talk with your doctor before you drink alcohol or use other drugs and natural products that slow your actions.

Take good care of your teeth. See a dentist often.

A very bad and sometimes deadly effect has happened in people taking drugs for seizures like this medicine (ethosuximide capsules). Call your doctor right away if you have swollen glands; fever; rash; chest pain; unable to pass urine or change in the amount of urine passed; or signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.

This medicine may cause harm to the unborn baby if you take it while you are pregnant. If you are pregnant or you get pregnant while taking this medicine (ethosuximide capsules), call your doctor right away.

Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Keep taking this medicine (ethosuximide capsules) as you have been told by your doctor or other health care provider, even if you feel well.

To gain the most benefit, do not miss doses.Do not change the dose or stop this medicine (ethosuximide capsules). This could cause seizures. Talk with your doctor.

Take with or without food.

Take a missed dose as soon as you think about it.If it is close to the time for your next dose, skip the missed dose and go back to your normal time.Do not take 2 doses at the same time or extra doses.

Pregnancy level

C