Active substanceLacosamideLacosamide
Similar drugsTo uncover
  • Wimpat®
    syrup inwards 
    YUSB Farma S.A.     Belgium
  • Wimpat®
    pills inwards 
    YUSB Farma S.A.     Belgium
  • Wimpat®
    solution d / infusion 
    YUSB Farma S.A.     Belgium
  • Dosage form: & nbspsyrup
    Composition:1 ml of syrup contains: active substance: lacosamide 15.00 mg. Excipients: glycerol, sodium carmellose, liquid sorbitol (crystalline), macrogol 4000, sodium chloride, citric acid, anhydrous, potassium acesulfame, sodium propyl parahydroxybenzoate, sodium methyl parahydroxybenzoate, strawberry flavor 501440 T, masking flavor 501521 T, purified water.
    Description:A clear, slightly viscous liquid from colorless to a yellow or yellow-brown color with a characteristic fruity odor.
    Pharmacotherapeutic group:Antiepileptic remedy
    ATX: & nbsp

    N.03.A.X   Other antiepileptic drugs

    N.03.A.X.18   Lacosamide

    Pharmacodynamics:
    The exact mechanism of antiepileptic action of lacosamide is not established. Lacosamide selectively enhances slow inactivation of voltage-gated sodium channels, resulting in stabilization hyperexcitable neurons membranes. Besides, lacosamide associated phosphoprotein with CRMP-2, which is expressed predominantly in the nervous system and is involved in regulating neuronal differentiation and neurite outgrowth.
    Shown, that lacosamide delayed the development of increased convulsive readiness.
    Pharmacokinetics:

    Suction

    Lacosamid is quickly and completely absorbed after ingestion. Bioavailability of lacosamide in tablets is approximately 100%. After oral administration, the concentration of lacosamide in the plasma rapidly increases, the maximum concentration (Cmah) is achieved after 0.5-4 hours. Food intake does not affect the speed and degree of absorption.

    Distribution

    The volume of distribution is approximately 0.6 l / kg, the degree of binding to plasma proteins is less than 15%. When applied twice a day, equilibrium concentrations in the plasma are reached within 3 days. Cumulation is accompanied by an increase in the concentration in the plasma by about 2 times.

    Metabolism

    95% of the dose is excreted through the kidneys, both in unchanged form (about 40% of the dose), and in the form of metabolites (O-desmethyl metabolite - less than 30%). The formation of the O-desmethyl metabolite occurs mainly under the action of cytochrome isoenzymes CYP2C19, 2C9 and 3A4. Other enzymes involved in the metabolism of lacosamide have not been established. The concentration of O-desmethyl metabolite in plasma is approximately 15% of the concentration of lacosamide. This metabolite has no pharmacological activity.

    The proportion of the polar fraction in urine (presumably serine derivatives) was approximately 20%, but it was detected in the plasma only in small amounts (0 - 2%) in some patients. Other metabolites are determined in urine in an amount of 0.5-2%.

    Excretion

    Lacosamide is excreted by renal excretion and biotransformation. The half-life is approximately 13 hours. The pharmacokinetic parameters are directly proportional depend on the used dose, do not change with time and are characterized by low individual variability.

    Indications:In the complex therapy of partial convulsive seizures, accompanied or not accompanied by secondary generalization, in patients with epilepsy aged 16 years and older.
    Contraindications:
    Hypersensitivity to any of the components of the drug. Atrioventricular block of II or III degree. Age to 16 years.
    Hereditary fructose intolerance, sucrase-isomaltase deficiency, glucose-galactose malabsorption (as in the composition of the syrup is included fructose). Phenylketonuria (since the composition of the syrup is included aspartame).
    Carefully:
    In patients with severe renal failure (creatinine clearance ≤ 30 ml / min), with conduction disorders, heart failure and myocardial infarction in history. Particular care should be taken in elderly people who are at increased risk of heart disease, and when using lacosamides in combination with drugs that cause prolongation of the PR interval.
    Pregnancy and lactation:
    Pregnancy
    There are no clinical data on the use of lacosamide in pregnant women. In studies on animals, teratogenic effects were not recorded, but embryotoxicity was noted with the use of high (toxic) doses. Lacosamide Do not use during pregnancy, except when the benefit to the mother clearly outweighs the possible risk to the fetus. If a woman is planning a pregnancy, it is necessary to correlate the benefits of using the drug for the mother and the possible risk to the fetus.
    Lactation period
    Data on the excretion of lacoside with human breast milk are absent. In studies on animals, excretion of lacosamide with milk was noted. During lacosamide treatment, breastfeeding should be discontinued.
    Dosing and Administration:Inside. The daily dose is divided into 2 doses - in the morning and in the evening, regardless of the time of meal. The recommended starting dose is 50 mg 2 times a day. After 1 week, the dose is increased to 100 mg 2 times a day. Taking into account the effectiveness and tolerability, the maintenance dose can be increased by 50 mg 2 times a day every week to a maximum daily dose of 400 mg / day (200 mg twice daily). To abolish Wimpat® is recommended gradually, reducing the dose by 200 mg per week.

    Use in patients with renal insufficiency

    Patients with mild and moderate renal impairment (creatinine clearance> 30 ml / min) do not need dose adjustment. In patients with severe renal insufficiency (creatinine clearance 30 ml / min) the maximum dose is 300 mg / day. Jla- Kosamid is removed from the plasma during hemodialysis, within 4 hours after the procedure, the area under the "concentration-time" curve decreases by approximately 50%. Patients who are on hemodialysis, it is recommended to appoint an additional 50% of a single dose immediately after the procedure. Treatment of patients with severe renal failure should be conducted with caution,since the clinical experience of using the drug in such patients is small, and possibly the accumulation of a metabolite that does not have a pronounced pharmacological activity. All patients with impaired renal function should be titrated with caution.

    Use in patients with impaired liver function

    Patients with mild to moderate liver dysfunction do not need dose adjustment.

    Titrate the dose to such patients with caution, given that the violation of liver function is often accompanied by a violation of kidney function.

    The pharmacokinetics of lacoside in patients with severe hepatic insufficiency has not been studied.

    Application in the elderly

    Elderly, a dose reduction is not required. The experience with lacosamide in elderly patients with epilepsy is limited. In elderly people, it is necessary to take into account the possibility of an age-related decrease in renal clearance and, as a consequence, an increase in the concentration of lacosamide in blood plasma.

    Use in children

    Lacosamides are not recommended for children and adolescents under the age of 16 because the safety and efficacy of the drug in these age groups have not been studied.

    Side effects:

    In the treatment of lacosamides, the most frequent adverse reactions were dizziness (also the main cause of lacosamid abolition), headache, nausea and diplopia. As a rule, they were mild or moderate. The severity of some adverse reactions depended on the dose and decreased after its reduction. The frequency and severity of adverse reactions from the central nervous system (CNS) and gastrointestinal tract usually decreased with time. The use of lacosamide is accompanied by a dose-dependent lengthening of the interval PR, so that the development of clinical conditions such as atrioventricular blockade, fainting and bradycardia is possible.

    Adverse reactions noted in more than 1% of patients in clinical trials are listed below. Adverse reactions are classified by frequency according to the following categories:

    Often (>1/10);

    Often (more than 1/100 and less than 1/10);

    Infrequently (more 1/1000 and less than <1/100).

    From the central nervous system and psyche

    Very often: dizziness, headache.

    Often: depression, irritability, imbalance, impaired coordination of movements, memory impairment, attention impairment, cognitive impairment, hypoesthesia, drowsiness, confusion, tremor, nystagmus, dysarthria.

    From the side of the cardiovascular system

    Bradycardia (frequency not established).

    From the side of the organ of vision

    Very often: diplopia.

    Often: blurred vision.

    From the side of the hearing and vestibular organs

    Often: vertigo, noise in the ears.

    From the gastrointestinal tract

    Very often: nausea.

    Often: vomiting, constipation, flatulence, indigestion, dry mouth.

    From the skin and subcutaneous fat

    Often: itching.

    Rash (frequency not established).

    From the musculoskeletal system

    Often: muscle spasms.

    Other

    Often: gait disturbance, asthenia, fatigue, falls, increased risk of injury (due to impaired coordination of movements and dizziness).

    Overdose:Clinical data on the overdose of lacosamide are limited. After taking the drug at a dose of 1200 mg / day, the clinical symptoms were mainly represented by the central nervous system and the gastrointestinal tract (dizziness and nausea) and disappeared after a dose reduction. During the clinical trials, a one-time intake of 12 g of lacosamide was registered, which was taken together with toxic doses of other antiepileptic drugs.The patient fell into a coma, but then completely recovered without consequences. The antidote of lacosamide does not exist. Treatment of an overdose is symptomatic. If necessary, hemodialysis is possible.
    Interaction:
    The results of studies indicate a low probability of interaction of lacosamide with other drugs.
    In preclinical studies lacosamide had a synergistic or additive anticonvulsant effect in combination with levetiracetam, carbamazepine, phenytoin, valproic acid, lamotrigine, topiramate, or gabapentin. Lacosamide should be used cautiously in combination with drugs that cause prolongation of the PR interval (for example, carbamazepine, lamotrigine, pregabalin) and class I antiarrhythmics. However, in clinical trials, there was no additional prolongation of the PR interval in patients who simultaneously took lacosamide in combination with carbamazepine or lamotrigine. Lacosamide is a substrate of cytochrome P450 isoenzymes (CYP2C19). Powerful inducers of microsomal liver enzymes, such as rifampicin or St. John's wort (Hypericum perforatum), can cause a moderate decrease in the systemic concentration of lacoside. In this regard, when prescribing such drugs or their withdrawal should be careful.

    Antiepileptic drugs

    Lacosamide at any therapeutic dose does not affect the equilibrium concentration of levetiracetam, carbamazepine, carbamazepine epoxide, lamotrigine, topiramate, oxcarbazepine, phenytoin, valproic acid, phenobarbital, gabapentin, clonazepam and zonisamide.

    Carbamazepine and valproic acid did not affect the concentration of lacosamide in plasma.

    Concomitant therapy with antiepileptic drugs that induce microsomal liver enzymes (carbamazepine, phenytoin, phenobarbital, in various doses), reduced the total system exposure of lacosamide by 25%.

    Oral contraceptives

    There were no signs of significant interaction between lacosamide and oral contraceptives: these are neither laestradiol and levonorgestrel. Lacosamide does not affect the concentration of progesterone.

    Other

    Lacosamide does not affect the pharmacokinetics of digoxin.Clinically significant interactions between lacosamide and metformin have not been identified. There is no data on the interaction of lacoside with alcohol.

    Omeprazole in a dose of 40 mg once a day increased the area under the curve "concentration-time" of lacosamide by 19%. This effect may not be of clinical significance. When taking a single dose lacosamide did not affect the pharmacokinetics of omeprazole. The effect of other isoenzymes of cytochrome P450 and other enzymes on the metabolism of lacosamide has not been accurately established. Lacosamide is not a substrate or an inhibitor of P-glycoprotein.

    The degree of binding of lacosamide to plasma proteins is less than 15%. In this regard, clinically significant interaction with other drugs that bind to proteins is unlikely.

    Special instructions:

    Treatment with lacosamide may be accompanied by dizziness, potentially leading to injuries and falls. In this regard, patients should be careful.

    Analysis of clinical trials of antiepileptic drugs suggests a slight increase in the risk of suicidal ideation and suicidal behavior.The mechanism of increasing risk is not clear, existing data do not allow to deny the existence of such a risk when taking lacosamide. Persons caring for patients should be warned about the existing risk and the need for specialist advice in the event of suicidal behavior. Patients treated with lacosamide should be carefully monitored and warned of the need for consultation with a specialist in the event of suicidal thoughts.

    Given the possibility of prolonging the PR interval against the background of therapy with Wimpat®, patients are advised to periodically monitor the ECG.

    The syrup contains sodium auxiliary substances propyl parahydroxybenzoate (E217) and sodium methyl parahydroxybenzoate (E219), which can cause allergic reactions (including delayed type). The syrup contains 3.7 g of sorbitol (E420) per 200 mg of lacosamide, which corresponds to 9.7 kcal. The syrup contains 1.06 mmol (or 25.2 mg) of sodium per 200 mg of lacosamide. This should be taken into account if the patient observes a diet with reduced sodium intake.

    Effect on the ability to drive transp. cf. and fur:The drug may affect the ability to drive a car or use sophisticated technology. Treatment with this drug may be accompanied by the development of dizziness, blurred vision and other side effects. Accordingly, patients are not advised to drive a car or operate complex equipment.
    Form release / dosage:Syrup 15 mg / ml.
    Packaging:200 ml of syrup in a glass bottle of dark glass or in a polyethylene terephthalate (PET) bottle with a screwed white cap made of polypropylene with a sealing membrane, with a first opening control (color ring) and child protection. For 1 bottle complete with a measuring cup along with instructions for use in a cardboard bundle.
    Storage conditions:List B. Store at a temperature not exceeding 30 ° C. Keep out of the reach of children.
    Shelf life:
    2 years. Do not use the drug after the expiration date. Use within 4 weeks of the first opening of the vial.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005993/10
    Date of registration:25.06.2010
    Expiration Date:Unlimited
    The owner of the registration certificate: YUSB Farma S.A. YUSB Farma S.A. Belgium
    Manufacturer: & nbsp
    Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia
    Information update date: & nbsp15.02.2017
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