Suxilep - instructions for use, dose, side effects, contraindications

Active substanceEthosuximideEthosuximide

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Suxilep

capsules inwards

Miebe GmbH Artsclimitel

Dosage form: & nbspcapsules

Composition:

Each capsule contains:

Active substances: ethosuximide 250 mg.

Excipients:

macrogol 400 - 25,00 mg, gelatin - 63,99 mg, water purified - 10,42 mg, titanium dioxide (E 171) - 1.52 mg, dye solar sunset yellow (E 110) -0.07 mg.

Description:

Hard gelatin capsules. Color capsule - the lid orange, body white. The size of the capsule number 1. The contents of the capsule are a white solidified mass.

Pharmacotherapeutic group:Antiepileptic remedy

ATX: & nbsp

N.03.A.D Derivatives of succinimide

N.03.A.D.01 Ethosuximide

Pharmacodynamics:

Ethosuximide is an anticonvulsant drug that belongs to succinimides. The mechanism of action is not definitively established; among other properties, an inhibitory effect on the degradation of GABA was found.

Pharmacokinetics:

Suction

After oral administration ethosuximide absorbed almost completely.

In adults, after taking ethosuximide in a single dose of 1 g, the maximum concentration in the blood plasma was determined after 2-4 hours and was 18-24 μg / ml.

In children aged 7 to 8.5 years with a body weight of 12.9-24.4 kg after taking ethosuximide in a single dose of 500 mg, the maximum concentration in the blood plasma was achieved in 3-7 hours and was 28-50.9 μg / ml.

Between the dose and the increase in the concentration in the blood plasma there is a linear dependence; with an increase in the oral dose by 1 mg / kg / day, an increase in plasma concentration of 2-3 μg / ml is assumed, in children - 1-2 μg / ml. Therefore, younger children require slightly higher doses than older children. The therapeutic concentrations of ethosuximide in plasma are in the range of 40 to 100 μg / ml. At concentrations in the plasma of more than 150 μg / ml, toxic effects may develop.

Distribution

In children with prolonged use of the drug at a dose of 20 mg / kg, the concentration in the blood plasma increased to almost 50 μg / ml. In adults, this concentration was achieved when taking the drug at a dose of 15 mg / kg.

The equilibrium state is expected to occur 8-10 days after the initiation of therapy. There are significant interindividual differences in plasma concentrations when the drug is administered in the same doses in the form of oral dosage forms. Ethosuximide slightly binds to plasma proteins.

Ethosuximide is found in liquor and in saliva at the same concentrations as in plasma. The apparent volume of distribution is 0.7 l / kg.

Penetrates through the placental barrier, excreted in breast milk (the ratio of concentrations of ethosuximide in plasma and in breast milk is 0.94 ± 0,06). Metabolism, excretion

In adults, after taking ethosuximide orally at a single dose of 13.1-18 mg / kg, the half-life from plasma was 38.3-66.6 hours. In children after ingestion of ethosuximide in a single dose of 500 mg, the half-life from plasma was 25.7 -35.9 h.

Ethosuximide undergoes significant oxidative metabolism in the liver. Several apparently pharmacologically inactive metabolites are formed, which are excreted by the kidneys, partly in the form of conjugates with glucuronic acid. The main metabolites formed are 2 diastereomers: 2- (1-hydroxyethyl) -2-methyl-succinimide and 2-ethyl-2-methyl-3-hydroxysuccinimide.

In the unchanged form, 10-20% are excreted by the kidneys.

Indications:

- Attacks piknolepticheskih absences, as well as complex and atypical convulsive seizures.

Note. To avoid the development of generalized tonic-clonic seizures, which often aggravate the course of complex and atypical seizures, a combination of ethosuximide with anticonvulsants (for example, primidon, phenobarbital) can be used.Additional prophylaxis of generalized tonic-clonic seizures can be carried out without exception in the case of attacks of pycnopletic absences in children of school age.

- Myoclonic-astatic small seizures (petit mal).

- Juvenile myoclonic seizures (impulsive small seizures).

Contraindications:

Hypersensitivity to the components of the drug.

It is not recommended to use in children under 6 years due to the inability to accurately dispense this dosage form.

Carefully:

With an indication in a history of mental illness (the risk of developing the relevant side effects - anxiety, hallucinatory symptoms); increased risk of myelotoxicity.

Hepatic and / or renal insufficiency.

Pregnancy and lactation:

- Pregnancy

Specific embryopathy in children whose mothers received ethosuximide as monotherapy, is not revealed.

Against the background of the use of antiepileptic drugs increases the risk of malformations. With combined therapy, this risk is higher, therefore, during pregnancy, monotherapy is recommended.

A minimum effective dose controlling seizures should be given, especially between the 20th and 40th days of pregnancy. It is necessary to regularly determine the concentration of ethosuximide in the mother's blood serum.

In the last trimester of pregnancy, a woman should take a vitamin preparation K1, This prevents the development of a newborn deficiency of vitamin K, which can lead to bleeding.

It is necessary to warn the patient about the need to immediately consult a doctor when pregnancy comes on the background of therapy.

- Lactation

Against the background of Suxilep® treatment, breastfeeding should be discarded. concentration in breast milk can reach up to 94% of the concentration in the blood plasma of the mother.

Dosing and Administration:

Single and daily doses

The dose of Suxilep® depends on the clinical picture of the disease, the patient's individual response to treatment and tolerability. Treatment starts with small initial doses. Doses gradually increase.

In both children and adults, treatment starts with a total daily dose of ethosuximide ranging from 5 to 10 mg / kg body weight.

The total daily dose of ethosuximide can be increased by 5 mg / kg at intervals of 4 to 7 days (or, depending on the achievement of the equilibrium state: 8-10 days).

For maintenance therapy, a daily dose of ethosuximide at a rate of 20 mg / kg in children and 15 mg / kg in adults is usually sufficient.

Do not exceed the maximum daily dose of ethosuximide 40 mg / kg body weight in children and 30 mg / kg - in adults.

The daily dose is taken in 2-3 divided doses. In connection with the long half-life of ethosuximide with good tolerability, the whole daily dose can be taken simultaneously.

The therapeutic concentration of ethosuximide in blood plasma is 40-100 μg / ml. Examples of calculating the daily dose for adults and children over 12 years with a maintenance dose of ethosuximide 15 mg / kg:

Weight	Average daily	The maximum daily
bodies	dose, mg (cap.)	dose, mg (cap.)
50 kg	750 (3)	1500 (6)
67 kg	1000(4)	2000 (8)
83 kg	1250(5)	2500(10)

Examples of calculating the daily dose for children under the age of 12 years with a maintenance dose of ethosuximide 20 mg / kg:

Weight bodies	Average daily dose, mg (cap.)	The maximum daily dose, mg (cap.)
13 kg	250(1)	500 (2)
25 kg	500 (2)	1000 (4)
38 kg	750 (3)	1500 (6)
50 kg	1000 (4)	2000 (8)

Note: ethosuximide undergoes dialysis. Therefore, patients on hemodialysis require an additional dose of or. change the dosage regimen. 39-52% of the administered dose is removed during the 4-hour period of hemodialysis.

Mode of application

Capsules should be swallowed whole with a sufficient amount of liquid (for example, a glass of water) during or after a meal.

Basically, antiepileptic therapy is carried out for a long time. The question of correction, duration and withdrawal of therapy by Suxilep® should be decided by a specialist with experience in the treatment of epilepsy.

Usually, a dose reduction, possibly with the subsequent cancellation of the drug, should not be taken until the period during which convulsions occur is 2 or 3 years. The dose reduction for the purpose of drug discontinuation should be carried out in several stages for a period of 1 to 2 years. For children, it is allowed to "grow" from its dose (the dose remains constant, while the body weight increases). However, there should be no worsening of the electroencephalogram.

Side effects:

Dose-dependent adverse effects

Often there is nausea, vomiting, hiccough and abdominal pain. Sometimes there is lethargy, withdrawal syndrome, severe headache, dizziness, anxiety, depression, sleep disorders, decreased ability to concentrate, unusual fatigue, loss of appetite, weight loss, diarrhea or constipation,in also ataxia. In rare cases, within a few days and weeks, hallucinatory-paranoid ideas may develop. In some cases dyskinesia is observed during the first 12 hours of treatment. They disappear after the removal of ethosuximide or are controlled by diphenhydramine. Undesirable effects not dose dependent

Skin allergic reactions, such as exanthema, can be observed; possibly the development of Stevens-Johnson syndrome. Rarely there are systemic lupus erythematosus of varying intensity, leukopenia, eosinophilia, thrombocytopenia or agranulocytosis. In isolated cases, aplastic anemia and pancytopenia can develop.

Overdose:

Whenever a diagnosis of overdose is established, the possibility of multiple intoxication as a result of taking several medications should be considered (for example, with a suicidal attempt).

Symptoms of overdose significantly increased under the influence of alcohol and other drugs that depress the activity of the central nervous system.

Symptoms of intoxication

Fatigue, lethargy, depressive states and agitation conditions, sometimes irritability, as well as other dose-related undesirable effects are most pronounced after an overdose.

The existing symptoms can be regarded as an overdose if the concentration of ethosuximide in the blood plasma is more than 150 μg / ml.

Treatment of intoxication

With a severe overdose at the beginning, it shows gastric lavage and the introduction of activated charcoal. It is necessary to carry out resuscitation measures to maintain the functions of the cardiovascular and respiratory systems.

Interaction:

Ethosuximide usually does not cause changes in plasma concentrations of other antiepileptic drugs (eg, prymidone, phenobarbital, phenytoin), since is not an inducer of enzymes. However, in some cases, an increase in the concentration of phenytoin in the blood plasma is possible.

The intake of carbamazepine leads to an increase in the plasma clearance of ethosuximide.

On the background of valproic acid therapy, a change in the concentration of ethosuximide in the blood serum is possible.

It can not be ruled out that with simultaneous use of drugs that have a depressing effect on the activity of the central nervous system and Suxilep®, their sedative effects are enhanced.

Avoid drinking alcohol.

Special instructions:

Particular attention should be paid to any manifestations of myelotoxicity,(for example, fever, tonsillitis, adenoiditis, and a tendency to bleeding); in such cases, the patient may need to consult a doctor. To determine the possible myelotoxic effects, the blood cell count should be periodically analyzed (first monthly, 12 months later, at intervals of 6 months). If the number of white blood cells is less than 3500 / μL or the amount of granulocytes is less than 25%, a dose reduction of Suxilep® or its cancellation is indicated. Also, the liver and kidney function indicators should be monitored regularly.

The risk of dose-related adverse effects can be reduced if therapy is started slowly, the dose is gradually increased, and patients take ethosuximide during or after a meal.

If dose-related reversible side effects develop, Succilept® should be discontinued; if treatment with the drug is resumed, the possibility of their re-emergence should be considered.

With the development of dyskinesias ethosuximide should be canceled. In addition, iv injection of diphenhydramine may be required.

Mostly in patients with a history of mental illness,Possible development of appropriate side effects from the psyche (anxiety, hallucinatory symptoms). In this patient category Suxilep® should be used with extreme caution.

With prolonged therapy, the physical activity of the patient and the interest in the environment may be reduced (for example, in children and adolescents there may be a deterioration in the ability to learn in school).

Effect on the ability to drive transp. cf. and fur:

Even if Suxilep® is used in accordance with the instruction, the reactivity can be changed to such an extent that the ability to drive and work with machinery is disrupted. This manifests itself more strongly with simultaneous intake with alcohol. Therefore, patients receiving ethosuximide, one should refrain from driving vehicles, working with machinery and other hazardous activities, at least during the stabilization phase. In each case, the decision is made by the attending physician, taking into account the individual reaction and the appropriate dose.

Form release / dosage:

Capsules 250 mg.

Packaging:

For 100 capsules in plastic vial or bottle dark glass with a plastic cover.The bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

Store at temperatures below 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date shelf life.

Terms of leave from pharmacies:On prescription

Registration number:П N013730 / 01

Date of registration:15.05.2009

The owner of the registration certificate:Miebe GmbH ArtsclimitelMiebe GmbH Artsclimitel

Manufacturer: & nbsp

Miebe GmbH Artsclimitel Germany

Representation: & nbspFARMAGATE, LLCFARMAGATE, LLC

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Suxilep (Suxilep)