Levetiracetam Canon is an antiepileptic drug derived from pyrrolidone (the S-enantiomer of Î±-ethyl-2-oxo-1-pyrrolidine-acetamide). The chemical structure differs 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 intra-neuronal concentration of Ca2 + ions, partially inhibiting the flow of Ca2 + through N-type channels and decreasing the release of calcium from intra-neuronal depots. In addition, levetiracetam partially restores currents through the GABA- and glycine-dependent channels, reduced by zinc and Î²-carbolines.
One of the proposed mechanisms is based on the proven binding of the synaptic SV2A synaptic vesicles contained in the gray matter of the brain and spinal cord to the glycoprotein. It is believed that in this way an anticonvulsant effect is realized, which is expressed in counteracting hypersynchronization of neural activity. It does not alter normal neurotransmission, but suppresses epileptiform neuronal bursts induced by the GABA agonist biculin and excitation of glutamate receptors. Levetiracytam activity has been confirmed for both focal and generalized epileptic seizures (epileptiform manifestations / photoparoxysmal reaction).
As a monotherapy for the treatment of partial seizures, with or without secondary generalization, in patients from 16 years of age with a new diagnosis of epilepsy.
As adjuvant therapy: partial seizures with or without secondary generalization in patients with epilepsy from 4 years of age (for intravenous administration) or from 6 years of age (for oral administration) myoclonic seizures in patients with juvenile myoclonic epilepsy from 12 years of age primary generalized tonic-clonic seizures in patients with idiopathic generalized epilepsy in adults and adolescents over 12 years old.
Hypersensitivity. Precautions – advanced age (decreased cardiac output). children under 6 years of age (for oral administration) hypersensitivity to levetiracetam, hypersensitivity to other pyrrolidone derivatives.
Caution should be used in elderly patients (over 65 years old), with liver diseases in the stage of decompensation, renal failure.
Concomitant antiepileptic drugs (during the transfer of patients to levetiracetam) should preferably be withdrawn gradually.
Patients with kidney disease and decompensated liver disease are advised to study kidney function before starting treatment. Due to reported cases of suicide, suicidal intent, and suicide attempts in the treatment of levetiracetam, patients should be warned about the need to immediately inform the attending physician of any symptoms of depression or suicidal intent.
Use in pediatrics
Available information on the use of levetiracetam in children does not indicate any negative effect on development and puberty. However, the long-term effects of treatment on children’s learning ability, their intellectual development, growth, endocrine gland function, sexual development and fertility remain unknown.
Effect on the ability to drive vehicles and control mechanisms
Due to the different individual sensitivity to levetiracetam from the central nervous system during treatment, patients should refrain from driving vehicles and engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Dosage and administration of
Depending on the indications and age of the patient, a single dose is 250-750 mg. Multiplicity of use – 2 times a day.
From the hematopoietic system: infrequently – thrombocytopenia, rarely leukopenia – neutropenia, pancytopenia.
From the side of metabolism: often – anorexia infrequently – increase / decrease in body weight.
From the side of the central nervous system: very often – drowsiness, headache often – mood swings, emotional lability, depression, aggressiveness, insomnia, nervousness infrequently – behavior disorder, bitterness, anxiety, hallucinations, psychotic disorders, memory impairment, suicidal attempt. obsessions, amnesia, tactile sensitivity disorder, dizziness, headache, hyperkinesia, tremor, imbalance, distraction, paresthesia rarely – personality disorder, including impaired thinking, suicide, hyperkinesis, choreoathetosis.
From the sensory organs: often – dizziness infrequently – diplopia, blurred vision.
From the respiratory system: often – cough.
From the digestive system: often – nausea, vomiting, diarrhea, abdominal pain, dyspepsia infrequently – deviations of laboratory parameters of liver function from the norm rarely – pancreatitis, hepatitis, liver failure.
On the part of the skin and subcutaneous tissues: often – a skin rash infrequently – eczema, itchy skin rarely – alopecia (in some cases, occurring after discontinuation of levetiracetam), toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome.
From the musculoskeletal system: infrequently – myalgia, muscle weakness.
Other: often – general weakness, fatigue infrequently – nasopharyngitis, accidental trauma.
Most often in children: vomiting, agitation, mood swings, aggression, emotional lability, behavior disorder, lethargy.
In a dry, dark place, at a temperature not exceeding 25 ° C.