Levetiratsetam

Леветирацетам Constitutional formula

The description is actual on 20.09.2015

  • Latin name: Levetiracetamum
  • ATH code: N03AX14
  • Chemical formula: C8H14N2O2
  • CAS code: 102767-28-2

Chemical name

(S)-2-(2-oxopyrrolidin-1-yl) butanamide

Chemical properties

Substance – derivative a pirrolidona. The molecular mass of Levetiratsetam = 170,2 grams on mol. This epilepsy medicine which is brought in the list of the vital and necessary drugs. On the structure this substance cardinally differs from other antiepileptic means.

Pharmacological action

Antiepileptic.

Pharmacodynamics and pharmacokinetics

Drug – an anticonvulsant which mechanism of impact on an organism is not studied yet. It is supposed that substance contacts a glycoprotein of synoptic vesicles which are located in gray matter back and a brain, and counteracts hyper synchronization of work of neurons.

Also means affects receptors of GAMK and glycine receptors, modulates them by means of specific endogenous agents. For drugs on the basis of this means it is not peculiar to change processes of normal synoptic transfer of nervous impulses. However medicine well suppresses the epileptiform neyronalny flashes caused bikukuliny and excites specific glutamate receptors.

Substance is rather effective both at focal, and at generalized epileptic attacks.

After reception of tablets active ingredient is well acquired by a gastrointestinal tract. There is a full absorption, concentration in a blood plasma and other pharmacokinetic parameters change linearly, depending on the accepted dose. Meal does not influence process of assimilation of medicine in any way. Biological availability of substance reaches 100%.

After reception of one gram of Levetiratsetam within an hour the maximum equilibrium concentration will be reached it. Substance badly contacts proteins of plasma, less than 10%.

In a liver means undergoes a metabolism by means of hydrolysis of atsetamidny group. Connection does not exert impact on work of system of P450 cytochrome, a glyukuroniltransferaza, an epoksidgidroksilaza or enzymatic activity of cells of a liver.

The elimination half-life differs depending on age of the patient and his weight. On average for the adult of T1/2 = to 7 hours. Substance and its active metabolite by means of kidneys is removed.

At elderly patients the elimination half-life makes from 10 to 11 hours. In the course of a dialysis (4-hour) about a half of substance is removed from an organism.

At a serious illness of a liver the clearance of substance decreases almost in a half.

Indications to use

As monotherapy medicine is used for treatment of partial spasms without or with secondary generalization at persons 16 years are more senior.

As a part of complex therapy drug is appointed:

  • inside or intravenously at patients with epilepsy aged from 4 flyings;
  • at juvenile myoclonic epilepsy to persons 12 years are more senior;
  • for treatment of initially generalizirovanny toniko-clonic spasms at idiopathic generalized epilepsy aged from 12 flyings.

Contraindications

Levetiratsetam's pricks do not appoint to children till 4 flyings, and a tablet – to 6.

Medicine is contraindicated:

  • in the presence of an allergy to active ingredient or other derivatives of a pirrolidon;
  • to pregnant women;
  • 16 years are aged younger.

Care recommends to observe:

  • during feeding by a breast;
  • with body weight less than 25 kg;
  • at heavy disturbances in work of a liver or kidneys;
  • to patients 65 years are more senior;
  • at a depression and tendency to suicide behavior.

Side effects

Levetiratsetam's drugs often cause:

At treatment of children most often arise:

  • agitation, aggression, weakness and apathy;
  • vomiting and nausea, behavioural frustration.

Are less often observed:

  • leukopenia, neutropenia, thrombocytopenia, pancytopenia;
  • weight loss or increase in weight;
  • aggression, embitternment, hallucinations, disturbance of processes of storing, obsessions;
  • tendency to a suicide, amnesia, tremor, absent-mindedness;
  • decrease in sharpness and misting of sight;
  • increase of level of liver enzymes, weakness in muscles;
  • nasopharyngitis, alopecia.

Seldom develop:

  • suicide, choreoathetosis, frustration of the personality, hyperkinesia;
  • hepatitis, pancreatitis, liver failure;
  • Stephens-Johnson's syndrome, mnogoformny erythema;
  • oppression of work of marrow.

Levetiratsetam, application instruction (Way and dosage)

Substance is accepted orally in the form of tablets or entered intravenously in the form of solution for injections.

Depending on a disease and age use various daily dosage. As a rule, it makes from 1 to 3 grams a day. The daily dose is distributed on 2 receptions (on 250-750 mg for time).

It is possible to combine peroral and intravenous drug intake, keeping a dosage and frequency rate of introduction.

Patients with a renal failure are recommended to correct a daily dosage. If KK falls lower than 50 ml a minute, then the dosage is reduced twice.

For children use a special dosage form (for example, syrup).

Overdose

At overdose are shown: concern, drowsiness, coma, oppression of respiratory functions, aggression, loss of consciousness.

It is recommended to wash out a stomach, to accept absorbent carbon, to support respiratory function, the hemodialysis is shown.

Medicine has no specific antidote.

Interaction

At a drug combination with topiramaty the probability of development of anorexia increases.

Meal does not influence completeness of absorption of means, however the speed of process decreases.

Terms of sale

The recipe is necessary.

Special instructions

In need of transfer of the patient on Levetiratsetam from other drugs it is recommended to cancel other antiepileptic means gradually.

During treatment the patient has to notify the attending physician on existence of symptoms of a depression or emergence of suicide thoughts.

If the patient has problems with a liver and kidneys before an initiation of treatment this substance, it is recommended to make inspection of these bodies.

Medicine does not influence process of puberty or development of the child.

During therapy drug is not recommended to be managed the car.

At pregnancy and a lactation

Adequate clinical trials of influence of medicine on the course of pregnancy were not conducted. It is possible to use this drug only in emergency cases.

During pregnancy there is a decrease in plasma concentration of substance. This effect is most obviously observed in 1 trimester of pregnancy.

Medicine is allocated with breast milk therefore feeding by a breast is recommended to stop risk advantage after careful weighing of a ratio.

Drugs in which contains (Levetiratsetam's Analogues)

Substance is a part of medicines: Levetiratsetam Kanon, Keppra, Levetinol, Letiram, Epikepran, Komviron, Levetiratsetam Lyupin, Tirapol, Epiterra.

About Levetiratsetam

About drug very good. Some patients refuse to accept substitutes and analogs of this means, write that improvements in a state at them happened only after an initiation of treatment Levetiratsetamom. From side effects most often complain of dizziness, drowsiness and weakness.

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance use Levetiratsetam surely consult with the attending physician.