Description overdue on 09/18/2014

• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Synonyms
• Babies
• With alcohol
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

International Nonproprietary Name (INN) of the active substance - levetiracetam.

Concentrate for further manufacturing solution for infusion   It comprises 500 mg levetiracetam   - The active substance. Additional ingredients: 45 mg - sodium chloride 8, 2 mg - sodium acetate trihydrate and 5 ml - water for injection, 10% acetic acid (to pH 5, 5).

Oral solution   It comprises 100 mg levetiracetam   - The active substance. Additional ingredients: 0, 06 mg - citric acid monohydrate, 1, 05 mg - sodium citrate, 2, 7 mg - methyl parahydroxybenzoate, 1, 5 mg - ammonium glycyrrhizate, 0, 3 mg - propyl parahydroxybenzoate, 300 mg - maltitol, 235, 5 mg - glycerol 85%, 4, 5 mg - acesulfame potassium, 504 mg - purified water, 0, 3 mg - 501040A grape flavor.

Tablets are film coated   in its composition contains 250 mg / 500 mg / 1000 mg levetiracetam   - The active substance. Additional ingredients are present in different parts of the mass, respectively the content of active substance: magnesium stearate, macrogol 6000, croscarmellose sodium, and silicon dioxide.

Product form

The drug is available in three pharmaceutical forms:

• Keppra concentrate for infusion (Keppra) ;
• Syrup Keppra (Keppra) ;
• coated tablets Keppra (Keppra) .

Pharmacological action

Anticonvulsant, antiepileptic drug.

Pharmacodynamics and pharmacokinetics

Keppra medicament as an active substance which acts levetiracetam,   It relates to pyrrolidone   and its chemical structure is allocated among the known drugs used for the treatment of epilepsy Since it is obvious that its mechanism of action, although it is not explored to the end, the mechanism of action is different from other anti-epileptic drugs.

It is believed that one mechanism of action is proved by reacting synaptic vesicle protein SV2A, which are in the gray matter of the brain and spinal cord with levetiracetam That leads to the anticonvulsant effect in terms of antagonistic activity of neurons gipersinhronizatsii .

Another mechanism of action is considered to be effects of the active substance at glycine receptors and GABA receptors with modulation of these receptors by various endogenous agents. Levetiracetam It does not affect the activation of glutamate receptors and neurotransmission, however, inhibiting neuronal epileptiform flash caused by GABA-agonist bikukulikom.

The drug efficacy was proven with respect to focal and generalized epileptic seizures.

Intravenous administration of the dose levetiracetam   1500 mg correspondence with the same dose administered orally.

Following oral administration are well and rapidly absorbed from the gastrointestinal tract.

Suction total, linear, with the fullness of absorption is independent of the dose and the food (a bit rate of absorption is reduced when eating).

The bioavailability of approximately 100%.

Cmax following a single oral dose of 1000 mg of the drug observed after 80 minutes and equal to 31 mg / ml. Repeated dose - 43 mg / ml.

Cmax when administered intravenously 1500 mg levetiracetam It achieved after 15 min at 51 ± 19 pg / ml.

When applying a single dose twice daily equilibrium state is observed after 48 hours.

Pharmacokinetics in pediatric patients - linear character, a daily dose of from 20 mg to 60 mg per kilogram of body weight.

Cmax - 30-60 minutes.

Vd about 0, 5-0, 7 l / kg.

Communication with the plasma protein is less than 10%.

Metabolism occurs via the enzymatic hydrolysis .

T1 / 2 from the plasma in children 5-6 hours in adults about 7 hours, increasing by 40% in the elderly.

Excreted by the kidneys.

Indications

Keppra drug prescribed as monotherapy for the treatment of patients older than 16 years with partial seizures with secondary generalization or not, when re-diagnosed epilepsy .

In the treatment of the drug is shown:

• for partial seizures with or without generalization secondary generalization, manifested in adult patients and pediatric patients older than 4 years old suffering from the disease epilepsy   (for tablets);
• for partial seizures with or without generalization secondary generalization, manifested in adult patients and pediatric patients older than 1 month, suffering from disease epilepsy   (oral solution);
• in the development of myoclonic seizures   patients juvenile myoclonic epilepsy For the treatment of adult patients and adolescents over 12 years of age;
• at primary generalized seizures in patients idiopathic generalized epilepsy,   for the treatment of adult patients and adolescents over 12 years of age.

The drug is in the form of Keppra concentrate for infusion is prescribed as an alternative treatment, when it is impossible for the patient to take the oral form of the drug.

Contraindications

For tablets:

• pediatric patients under 4 years of age.

For oral solution:

• hypersensitivity fructose ;
• pediatric patients up to 1 month.

All forms of release of the drug:

• hypersensitivity levetiracetam   or other ingredients of medicaments.

With extreme caution:

• Patients over the age of 65 years;
• renal insufficiency;
• liver pathology in the stage of decompensation.

Side effects

The bodies of:

• ccomodation;
• diplopia.

Respiratory system:

• increased cough.

Digestive system:

• abdominal pain;
• dyspepsia;
• diarrhea;
• nausea;
• vomiting;
• weight change in the smaller side;
• anorexia;
• pancreatitis;
• hepatitis;
• hepatic impairment;
• changes in liver function tests.

Central nervous system:

• asthenic syndrome;
• drowsiness;
• dizziness;
• ataxia;
• amnesia;
• convulsions;
• headache;
• tremor;
• hyperkinesia;
• imbalance;
• memory loss;
• decreased concentration;
• excessive excitement;
• emotional lability;
• depression;
• frequent changes of mood;
• sleeplessness;
• aggression and hostility;
• irritability;
• nervousness;
• abnormal thinking;
• personality disorders;
• paresthesia;
• anxiety;
• behavioral disorders;
• anxiety;
• hallucinations;
• confusion;
• psychotic disorders;
• suicidal thoughts.

Skin:

• eczema;
• a rash on the skin;
• itching;
• alopecia (possible to restore hair after discontinuation);
• erythema multiforme;
• Stevens-Johnson syndrome;
• toxic epidermal necrolysis.

Hematopoietic system:

• thrombocytopenia;
• neutropenia;
• leukopenia;
• pancytopenia   (Sometimes there is depression of bone marrow function).

Others:

• joining infections;
• myalgia;
• nasopharyngitis.

Instructions for use (method and dosage)

Instructions on Keppra in the form of a solution for infusions   It recommends two-single intravenous daily dose, in equal portions over 15 minutes.

One ampoule preparation contains 500 mg / 5ml levetiracetam.   Before use, the solution is diluted at least 100 ml of Ringer's solution, 5% dextrose, or 0 9% sodium chloride.

Spending the infusion should be immediately after the process of breeding. In extreme cases, if you can not conduct an immediate procedure, it is stored in the refrigerator for a day, if preparation of the solution was held under aseptic conditions.

The dosage of intravenous infusion is determined by the attending physician.

The transition from intravenous to oral administration and can be carried back to the conservation dosage and frequency of application.

Oral daily doses of the drug Keppra carried out regardless of the meal in two equal parts, preferably with a 12 hour break.

Pills   recommend to drink enough water.

Instructions on syrup   It assumes its dosing with 10 ml measuring syringe included in the package, which corresponds to 1000 mg levetiracetam .

For the syrup filling the syringe with the vial is necessary to remove the cover and inserting a syringe into the adapter, dial using the right amount of stretch piston solution (division on the syringe - 25 mg corresponds to 0, 25 ml).

Metered solution was added to a prepared beaker with 200 ml of water and drink completely.

After each new set should be thoroughly rinsed syringe and vial cap tightly resealed.

Monotherapy

Patients over the age of 16 years recommended initial daily dose - 500 mg, with the reception in two steps of 250 mg every 12 hours. After 14 days, the dose may be increased to an initial therapeutic dose of 1000 mg, with two reception times daily 500 mg. The maximum recommended daily dose of Keppra is equal to 3000 mg.

In the treatment of

Pediatric patients older than 4 years prescribed initial daily dose is 20 mg / kg of body weight, with a double reception in the day to 10 mg / kg body weight. Changing the dosage of 20 mg / kg body weight may occur every 14 days, until reaching the recommended dose is 60 mg / kg body weight, with the reception of two times a day to 30 mg / kg. In the case of untreated patient recommended dose is reduced to its minimum effective.

The attending physician shall designate a medicament Keppra most suitable for each patient, and the dosage form of the dosage unit, depending on the desired therapeutic dose, and taking into account body weight.

Pediatric patients weighing up to 20 kilograms recommend starting treatment with the reception in the form of Keppra oral solution.

Pediatric patients weighing more than 50 kg recommend carrying out treatment with regimens and dosages for adult patients.

Patients aged over 16 years with a body weight above 50 kg administered daily starting dose is 1000 mg, with reception in two steps of 500 mg. Depending on tolerability and clinical response of the patient, the daily dose can be increased up to the maximum recommended dosage of 3000 mg taken two times daily 1500 mg. Changing the dosage of 500 mg 2 times a day, may be performed every 14-28 days.

Due to levetiracetam   excreted in the urine, the dose, for administration to patients with renal failure, must be adjusted.

Below are the maximum dose Keppra in accordance with creatinine clearance QC (ml / min):

• CC & gt; 80 - 3000 mg;
• CC 50-79 - 2000 mg;
• CC 30-49 - 1500 mg.

Patients who are on Dialysis On the first day of therapy prescribed loading dose - 750 mg, after further dialysis treatment take 250 mg - 500 mg.

Duration of therapy using the drug Keppra determined by a physician.

Overdose

In overdose possible manifestation: drowsiness, aggression, anxiety, respiratory depression, depression of consciousness,   and coma.

Recommended treatment during the acute phase is artificially induce vomiting and gastric lavage with a further reception adsorbents. If necessary, designate symptomatic therapy in a hospital, a hemodialysis procedure.

Cooperation

There were no drug interaction with Keppra antiepileptic drugs ( Phenytoin, valproic acid, carbamazepine, phenobarbital, gabapentin, lamotrigine and Primidone).

Oral contraceptives Digoxin   and Warfarin   no effect on the pharmacokinetics of levetiracetam.

Levetiracetam   2000 mg per day did not affect the pharmacokinetics of Warfarin   and Digoxin   and a daily dose of 1000 mg on the pharmacokinetics of oral contraceptives.

When combined with the application Topiramate   increases the risk of anorexia.

Terms of sale

Prescription.

Storage conditions

Solution for infusion   It should be stored in a dark place at a temperature no higher than 25 ° C.

Pills   should be kept at a temperature no higher than 25 ° C, in a dry place.

Oral Solution   It should be stored in a dark place at a temperature no higher than 30 ° C.

Shelf life

To solution for infusion   - 2 years.

To tablets and syrup   - 3 years.

Cautions

Abolition of the drug was gradually Keppra, decreasing the dose of 500 mg every 14 to 28 days (in children decrease dose not exceed 10 mg / kg two times a day, every 14 days, in children younger than 6 months - 7 mg / kg, 2 times a day, every 14 days).

When transferring a patient to Keppra taken anti-epileptic drugs, it is desirable to cancel slowly.

Patients with kidney disease, and decompensated liver disease states is recommended to study the function of these organs before starting therapy with levetiracetam In order to dose adjustment.

Infusion solution contains sodium which must be considered when administered to patients, who are at nizkonatrievoy diet .

Due to the fact that when using the drug Keppra there is evidence suicides It is necessary to control the emotional and mental health of the patient. The patient is obliged to inform your doctor about any symptoms of depression or suicidal feelings.

Clinical experience with the infusion solution Keppra than 4 days there.

Do not use the syrup when changing its color or finding it odd inclusions.

Oral solution contains maltitol and therefore is contraindicated in patients with impaired tolerance to fructose.

The presence in syrup propyl parahydroxybenzoate   and methyl parahydroxybenzoate can cause symptoms of allergic reactions.

Analogs of Keppra

Analogs drug Keppra presented the following medications:

• Vimpat;
• Gabapeptin;
• Konvulsan;
• Lamictal;
• Lyrics;
• Lamotrigine;
• Topiramate;
• Tebantin   etc.

Synonyms

• Komviron;
• Epiterra;
• Lethyr;
• Levetinol.

Babies

Assign children the recommended dose instructions.

With alcohol

No reliable data on the effect of alcohol on treatment with levetiracetam   no.

During pregnancy and lactation

Due to the fact that the specific clinical studies on the effects and safety of the drug Keppra in pregnancy has not been, is not recommended for pregnant women to his appointment, except in cases of urgent need.

Levetiracetam is excreted in mother's milk, so you should stop breast-feeding while taking the drug.

Reviews for Keppra

Reviews of Keppra forums reduced to the fact that treatment with antiepileptic drugs should be selected purely individual. Given the large selection of drugs with a similar action, the selection of appropriate treatment for an experienced doctor is not a problem.

Subject to compliance with all the recommendations for application and individual positive response to the therapy, the drug Keppra has shown good results.

Price Keppra where to buy

In Russia, the average cost of solution for infusion   It is - 7500 rubles.

Cost Syrup   About - 3,500 rubles.

Price Keppra 500 mg in the form of tablets   №30 about - 1700 rubles.

Keppra drug you can buy in Moscow in the same price range.