Keppra pills 250 mg 30 pcs
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Active ingredients
Levetiracetam
Release form
Pills
Composition
Active ingredient: Levetiracetam (Levetiracetam) Active ingredient concentration (mg): 250
Pharmacological effect
The antiepileptic drug, a pyrrolidone derivative (S-enantiomer of α-ethyl-2-oxo-1-pyrrolidine-acetamide), differs in its chemical structure from the known antiepileptic drugs. The mechanism of action of levetiracetam is not fully understood, but it is obvious that it differs from the mechanism of action of known antiepileptic drugs. In vitro studies have shown that levetiracetam affects the intraneuronal concentration of Ca2 + ions, partially inhibiting Ca2 + current through N-type channels and reducing the release of calcium from intraneuronal depot In addition, levetiracetam partially restores currents through GABA- and glycine-dependent channels, reduced by zinc and β-carbolines. One of the alleged mechanisms is based on the proven binding of the synaptic vesicle SV2A to the glycoprotein contained in the gray matter of the brain and spinal cord. It is believed that in this way the anticonvulsant effect is realized, which is expressed in counteracting the hypersynchronization of neural activity. Does not alter normal neurotransmission, however, suppresses epileptiform neuronal outbursts induced by a GABA agonist biculin and stimulation of glutamate receptors. The activity of the drug is confirmed in relation to both focal and generalized epileptic seizures (epileptiform manifestations / photoparoxysmal reaction).
Pharmacokinetics
AbsorptionAfter ingestion, levetiracetam is well absorbed from the gastrointestinal tract. Absorption is complete and linear, therefore plasma concentration can be predicted on the basis of the applied dose of the drug in mg / kg body weight. The degree of absorption does not depend on the dose and time of eating. Bioavailability is about 100%. After taking the drug in a dose of 1 g Cmax in the blood plasma is reached after 1.3 hours and is 31 μg / ml, after repeated administration (2 times / day) - 43 μg / ml. The distribution of the equilibrium state is reached after 2 days at twice taking the drug. Binding to plasma proteins of levetiracetam and its main metabolite is less than 10%.Vd of levetiracetam is about 0.5-0.7 l / kg. MetabolismThe formation of the primary pharmacologically inactive metabolite (ucb L057) occurs without the participation of cytochrome P450 isoenzymes in the liver. Levetiracetam does not affect the enzymatic activity of hepatocytes. The release of adult T1 / 2 from blood plasma is 7 ± 1 h and does not change depending on the dose, the route of administration or the repeated administration. The average clearance is 0.96 ml / min / kg. 95% of the dose is excreted by the kidneys. The renal clearance of levetiracetam and its inactive metabolite is 0.6 ml / min / kg and 4.2 ml / min / kg, respectively. Pharmacokinetics in special clinical situations in elderly patients T1 / 2 increases by 40% and is 10-11 hours, which is associated with a decrease in renal function in this category of people. In patients with impaired renal function, the clearance of levetiracetam and its primary metabolite correlates with creatinine clearance. Therefore, patients with renal insufficiency are recommended to select the dose depending on the CC. In the terminal stage of renal failure in adult patients T1 / 2 is 25 hours during the period between dialysis sessions and 3.1 hours during dialysis. During the 4-hour dialysis session, up to 51% of levetiracetam is removed. During the 4-hour dialysis, 51% of levetiracetam is removed from the body. In patients with mild and moderate hepatic impairment, no significant changes in the clearance of levetiracetam occur. With severe violations of liver function with concomitant renal failure, the clearance of levetiracetam is reduced by more than 50%. The pharmacokinetics of levetiracetam in children is linear in the dose range from 20 to 60 mg / kg / day. Cmax is achieved in 0.5–1 h. T1 / 2 in children after a single oral administration at a dose of 20 mg / kg body weight is 5–6 h. The total clearance of levetiracetam in children is about 40% higher than in adults and is directly dependent from body weight.
Indications
As a monotherapy (drug of first choice) in the treatment of: partial seizures with secondary generalization or without it in adults and adolescents over 16 years old with newly diagnosed epilepsy. As part of complex therapy for treatment: partial seizures with secondary generalization or without it in adults and children older than 4 years old, suffering from epilepsy (for pills); partial seizures with or without secondary generalization in adults and children older than 1 month,suffering from epilepsy (for solution); myoclonic seizures in adults and adolescents over 12 years of age with juvenile myoclonic epilepsy; primary generalized convulsive (tonic-clonic) seizures in adults and adolescents over 12 years of age with idiopathic generalized epilepsy.
Contraindications
Children's age up to 4 years (for pills) (safety and efficacy of the drug have not been established)
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Adequate and strictly controlled clinical studies on the safety of levetiracetam in pregnant women have not been conducted, so the drug should not be prescribed during pregnancy, except in cases of extreme necessity. Physiological changes in the woman's body during pregnancy can affect the plasma concentration of levetiracetam, as well as and other antiepileptic drugs. During pregnancy, a decrease in plasma concentration of levetiracetam was observed. This decrease is more pronounced in the first trimester (up to 60% of the baseline concentration in the period preceding the pregnancy). The treatment of pregnant women with levetiracetam should be carried out under special control. It should be borne in mind that interruptions in antiepileptic therapy may worsen the course of the disease, which is harmful for both the mother and the fetus. Levetiracetam is excreted in breast milk, so breastfeeding is not recommended for drug treatment. However, if treatment with levetiracetam is necessary during lactation, then the risk / benefit ratio of treatment should be carefully weighed against the importance of breastfeeding.
Dosage and administration
Tablets should be taken orally, squeezed with a sufficient amount of liquid, regardless of the meal.
Side effects
Asthenia, fatigue; drowsiness; headache, amnesia, ataxia, convulsions, hyperkinesia, tremor, imbalance, confusion, memory impairment, paresthesia; excitement, depression, emotional instability, mood changes, hostility, aggressiveness, insomnia, nervousness, irritability, confusion, hallucinations, psychotic disorders, suicide,suicide attempts and suicidal thoughts; abdominal pain, diarrhea, dyspepsia, nausea, vomiting; pancreatitis; liver failure, hepatitis; anorexia; dizziness; diplopia, blurred vision; myalgia; infectious diseases, nasopharyngitis; cough; skin rash; alopecia; thrombocytopenia; leukopenia, neutropenia, pancytopenia.
Overdose
Symptoms: drowsiness, anxiety, aggressiveness, depression of consciousness, respiratory depression, coma. Treatment: in the acute period - an artificial challenge of vomiting and gastric lavage followed by the appointment of activated carbon. There is no specific antidote for levetiracetam. If necessary, symptomatic treatment is carried out in a hospital using hemodialysis (dialysis
Interaction with other drugs
Leveetera does not interact and digoxin. Digoxin, oral contraceptives and warfarin do not affect the pharmacokinetics of levetiracetam. When used together with topiramate, anorexia is more likely to develop. The extent of absorption of levetiracetam does not change under the influence of food, while the rate of absorption somewhat decreases. There are no data on the interaction of levetiracetam with alcohol.
special instructions
If you want to stop taking the drug, it is recommended to cancel, gradually, reducing a single dose of 500 mg every 2-4 weeks. In children, the dose reduction should not exceed 10 mg / kg of body weight 2 times / day every 2 weeks. It is advisable to abolish concomitant antiepileptic drugs (during the transfer of patients to levetiracetam) gradually. Renal function testing is recommended for patients with kidney disease and decompensated liver diseases before starting treatment. If kidney function is impaired, a dose adjustment may be required. Due to reports of suicide,suicidal intent and attempted suicide in the treatment with levetiracetam should warn patients about the need to immediately inform the doctor about the appearance of any symptoms of depression or suicidal intentions. The oral solution contains maltitol, therefore Keppra in an appropriate dosage form is contraindicated for patients with fructose tolerance. in pediatricsRelated information about the use of the drug in children does not indicate any of its negative effects on p zvitie and puberty. However, the long-term effects of treatment on children's ability to learn, their intellectual development, growth, endocrine gland functions, sexual development and fertility remain unknown. The effect on the ability to drive vehicles and control mechanisms The effect of Keppra on driving ability and control mechanisms has not been specifically studied. However, due to the varying individual sensitivity to the drug on the part of the central nervous system during the period of treatment, it is necessary to refrain from driving vehicles and practicing potentially hazardous activities that require high concentration of attention and quickness of psychomotor reactions.