Levenium coated tablets 1000 mg. № 50

Description

Levenium Composition
active substance: levetiracetam;

1 coated tablet contains levetiracetam 1000 mg;

Excipients:

1000 mg tablets: corn starch, croscarmellose sodium, colloidal silicon dioxide, talc, magnesium stearate, Opadry White YS-1-7003 coating titanium dioxide (E 171), hypromellose, macrogol 400, polysorbate 80.

Levenium Dosage form
Film-coated tablets.

Levenium Basic physical and chemical properties:

tablets of 1000 mg: oval, biconvex film-coated tablets of white color, smooth on one side and with a break line on the other.

Levenium Pharmacotherapeutic group
Antiepileptic drugs. Levetiracetam. ATX code N03A X14.

Pharmacodynamics
Levetiracetam is a derivative of pyrrolidone (S-enantiomer of alpha-ethyl-2-oxo-1-pyrrolidine-acetamide), differs in chemical structure from known antiepileptic drugs.

Mechanism of action.
The mechanism of action of levetiracetam is not well understood. Based on in vitro and in vivo studies, it is assumed that levetiracetam does not alter the basic characteristics of the nerve cell and normal neurotransmission. In vitro studies have shown that levetiracetam affects intra-neuronal Ca 2+ levels by partially suppressing the current through N-type Ca 2+ channels and decreasing Ca2 + release from intra-neuronal stores. It also partially neutralizes the inhibition of GABA and glycine-regulated current caused by the action of zinc and β-carboline. In addition, in in vitro studies, levetiracetam binds to specific sites in rodent brain tissues. The binding site is the synaptic vesicle protein 2A, which is involved in vesicle fusion and neurotransmitter release. The relationship (in rank order) of levetiracetam and the corresponding analogs with the synaptic vesicle protein 2A correlated with the potency of their anticonvulsant action in models of audiogenic epilepsy in mice. These results suggest that the interaction between levetiracetam and synaptic vesicle protein 2A may partially explain the mechanism of antiepileptic action of the drug.

Pharmacodynamic effects.
Levetiracetam provides protection against seizures in a wide range of animal models of partial and primary generalized attacks, without causing a prodome effect. The main metabolite is inactive.
In humans, the activity of the drug has been confirmed for both partial and generalized epileptic seizures (epileptiform manifestations / photoparoxysmal reaction), which indicates a wide spectrum of the pharmacological profile of levetiracetam.

Pharmacokinetics
Levetiracetam is characterized by high solubility and permeability. Pharmacokinetics is linear, does not depend on time and is characterized by low inter- and intrasubject variability. After repeated use of the drug, the clearance does not change. There were no signs of influence of gender, race or circadian rhythm on pharmacokinetics. The pharmacokinetic profile was similar in healthy volunteers and patients with epilepsy.

Due to complete and linear absorption, the plasma level of the drug can be predicted from the oral dose of levetiracetam, expressed in mg / kg body weight. Therefore, it is not necessary to monitor plasma levels for levetiracetam.

In adults and children, there was a significant correlation between the concentration of the drug in saliva and blood plasma (the concentration ratio in saliva / plasma ranged from 1 to 1.7 after taking oral tablets and 4 hours after taking oral solution).