Supportive in the treatment of partial onset seizures and secondary generalized seizures in patients from 16 years of age. The infusion solution replaces tablets and syrup in patients who are temporarily unavailable for oral use.
Composition:
1 ml of solution contains 10 mg of lacosamide.
Action:
The exact mechanism of action of anti-epileptic lacosamide has not been fully understood. Lacosamide selectively enhances the inactivation of voltage-dependent sodium channels, which leads to the stabilization of excessively excitable neuronal cell membranes. It binds to the 2-mediated collapsin response protein (CRMP-2) - a phosphoprotein that is expressed mainly in the nervous system and is involved in neuronal differentiation and regulation of axonal growth. When administered intravenously Cmax it is reached at the end of the infusion. Lacosamide binds to plasma proteins in less than 15%. 95% of the administered dose is excreted in urine unchanged and as metabolites. T0,5 is 13 hours. Lacosamide AUC is increased by approximately 30% in patients with mild to moderate renal impairment and by 60% in patients with severe renal impairment and end-stage renal disease who require hemodialysis. Lacosamide is effectively removed from plasma by hemodialysis. In patients with moderate hepatic impairment (Child-Pugh Class B), the blood level of lacosamide is increased by 50%.
Contraindications:
Hypersensitivity to the components of the preparation. Atrio-ventricular block IIst. or III ..
Precautions:
Thoughts and suicidal behaviors have been reported in patients treated with antiepileptic drugs in various indications - patients should be closely monitored for the possibility of suicidal thoughts and behavior during treatment. Particularly cautiously use in elderly patients (increased risk of heart disease). Use with caution in patients with conduction disorders or severe cardiac conditions, such as myocardial infarction or heart failure, in patients with end-stage renal disease (due to limited clinical experience and accumulation of a metabolite with unknown pharmacological effects). All patients with impaired renal function should be cautious when setting the dose. Use with caution in patients with impaired hepatic function. The pharmacokinetics of lacosamide have not been studied in patients with severe hepatic impairment. There is limited experience with the use of lacosamide in elderly patients with epilepsy. Due to the lack of data on safety and efficacy, the product is not recommended for use in children and adolescents under 16 years of age.
Pregnancy and lactation:
Taking anti-epileptic preparations during pregnancy increases 2-3 times the risk of developmental defects compared to children of non-epilepsy women. An increase in the frequency of malformations has been observed in the case of multi-drug therapy, however, the extent to which the treatment and / or disease are responsible for the occurrence of defects has not been elucidated. In addition, effective anti-epileptic treatment must not be interrupted, since exacerbation of the disease is harmful to the mother and the fetus. There are no adequate data on the use of lacosamide in pregnant women. Lactosamide should not be used during pregnancy unless clearly necessary (if the benefit to the mother definitely does not outweigh the potential risk to the fetus). If a woman decides to become pregnant, the further use of the preparation should be carefully considered. Breast-feeding should be discontinued during treatment with lacosamide.
Side effects:
Very common (≥1 / 10): headache and dizziness (of central origin), double vision, nausea. Common (≥1 / 100, <1/10): depression, confusional states, insomnia, balance disorders, impaired motor coordination, memory disorders, cognitive impairment, drowsiness, tremor, nystagmus, hypestasis, dysarthria, attention disorders, paresthesia, blurred vision dizziness, tinnitus, vomiting, constipation, bloating, indigestion, dry mouth, diarrhea, pruritus, rash, painful muscle cramps, gait disturbances, weakness, fatigue, irritability, falls, alcohol intoxication, pain or discomfort at the site of administration, irritation, falls, skin damage, bruises.Uncommon: hypersensitivity reactions, aggression, agitation, euphoric mood, psychotic disorders, suicidal thoughts or attempts, hallucinations, atrioventricular block, bradycardia, atrial fibrillation or flutter, abnormal liver function tests, angioneurotic edema, urticaria, erythema. In addition: agranulocytosis, drug erosion with eosinophilia and organ manifestations (DRESS syndrome), Stevens-Johnson syndrome, toxic epidermal necrolysis.
Dosage:
Intravenously. Adults and adolescents over 16 years of age: the starting dose is 50 mg 2 times a day, after a week the dose should be increased to 100 mg 2 times a day. Then, depending on the response and tolerability, the maintenance dose may be increased by 50 mg twice a day every week up to the maximum recommended daily dose of 400 mg (200 mg 2 times a day). If it is necessary to discontinue treatment, it is recommended to stop the treatment gradually (eg by reducing the daily dose by 200 mg / week). Treatment with the preparation can be started by administering the drug orally or intravenously. The infusion solution is administered 15-60 min. 2 times a day. Changing the oral route to intravenous or vice versa can be done directly without a gradual dose adjustment. Keep the total daily dose and administration twice daily. Current clinical experience concerns the use of infusions of the preparation twice daily for up to 5 days. In patients with severe renal impairment (creatinine clearance ≤ 30 ml / min) and in patients with end-stage renal disease, the maximum dose is 250 mg / day. In hemodialyzed patients it is recommended to administer up to 50% of the divided daily dose immediately after hemodialysis.
(C)
