Wimpat pills 200 mg 56 pcs
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Active ingredients
Lacosamide
Release form
Pills
Composition
Lacosamide 200 mg; Excipients: microcrystalline cellulose, low substituted hyprolosis, prosolv (microcrystalline cellulose 98%, colloidal silicon dioxide 2%) HD 90, crospovidone, magnesium stearate, hyprolose.; , macrogol 3350, soy lecithin, titanium dioxide (E171), indigo carmine dye FD & C blue 2), opadry YS-3-7413 transparent (macrogol 400, macrogol 8000, hypromellose 3 cf, hypromellose 6 cf, hypromellose 50 cf).
Pharmacological effect
Antiepileptic drug.; The exact mechanism of the antiepileptic effect of lacosamide has not been established. Lacosamide selectively enhances the slow inactivation of voltage-dependent sodium channels, which leads to stabilization of hyper-excitable neuronal membranes. In addition, lacosamide binds to the phosphoprotein CRMP-2, which is expressed predominantly in the nervous system and is involved in regulating the differentiation of neurons and axon growth. It has been shown that lacosamide retards the development of increased seizure readiness. Lacosamide had a synergistic or additive anticonvulsant effect in combination with levetiracetam, carbamazepine, phenytoin, valproic acid, lamotrigine, topiramate or gabapentin.
Pharmacokinetics
Pharmacokinetic parameters are directly proportional to the dose used, do not change with time and are characterized by low individual variability.; Absorption; Lacosamide is quickly and completely absorbed after ingestion. The bioavailability of lacosamide pills is approximately 100%. After ingestion, the concentration of lacosamide in the plasma quickly increases, Cmax is reached in 0.5-4 hours. Eating does not affect the speed and extent of absorption. After the intravenous dose of 50-300 mg, the concentration of lacosamide in plasma increases proportionally to the dose.; Distribution ; Plasma protein binding of less than 15%. Vd is approximately 0.6 l / kg. When applied 2 times / day, plasma Css is achieved within 3 days. Metabolism; The formation of the O-desmethyl metabolite occurs mainly under the action of the CYP2C19 isoenzyme. 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 does not possess pharmacological activity.; Elimination; 95% of the dose is excreted in the urine, both in unchanged form (about 40% of the dose) and in the form of metabolites (O-desmethyl metabolite - less than 30%). The proportion of the polar fraction in urine (presumably serine derivatives) was approximately 20%. Other metabolites are determined in the urine in the amount of 0.5-2%; T1 / 2 is approximately 13 hours.
Indications
- as part of complex therapy of partial convulsive seizures, accompanied or not accompanied by secondary generalization, in patients with epilepsy aged 16 years and older.; Vimpat; in the form of infusions prescribed in those cases where it is temporarily impossible to take the drug inside.
Contraindications
- AV block II or III degree; - age up to 16 years; - hereditary intolerance of fructose, deficiency of sucrase-isomaltase, glucose-galactose malabsorption (since fructose is a part of the syrup); - Phenylketonuria (because aspartame is included in the syrup); - Hypersensitivity to the components of the drug, including soy (part of the shell of the tablet), as well as peanuts. With caution should use the drug in patients with severe renal insufficiency (CK≤30 ml / min), with conduction disorders, heart failure and myocardial infarction in history. Special care should be taken in elderly patients who have an increased risk of heart disease, as well as when using lacosamide in combination with drugs that cause prolonged PR interval.
Use during pregnancy and lactation
Clinical data on the use of lacosamide during pregnancy is not available. Lacosamide should not be used during pregnancy, unless the benefit to the mother clearly outweighs the possible risk to the fetus. If a woman is planning a pregnancy, then carefully consider the feasibility of using this drug. In experimental studies, no teratogenic effects have been reported, however embryotoxicity when used in high (toxic) doses.; There are no data on the release of lacosamide in human breast milk.In experimental studies, excretion of lacosamide with breast milk was observed. During breast cancer treatment, lacosamide should be stopped.
Dosage and administration
For oral administration; The daily dose is divided into 2 doses - in the morning and in the evening, regardless of the meal time. The recommended starting dose is 50 mg 2 times / day. After 1 week, the dose is increased to 100 mg 2 times / day. Taking into account the effectiveness and tolerability, the maintenance dose can be increased when taking the pills can be increased to 150 mg 2 times / day in the third week of administration, while taking the syrup - 50 mg 2 times / day every week, up to a maximum daily dose of 400 mg / day (200 mg 2 times / day) since the fourth week.; Cancel Wimpat; It is recommended gradually, reducing the dose to 200 mg per week. For intravenous administration, to intravenously, to be administered within 15-60 minutes 2 times / day. The recommended initial dose is 50 mg 2 times / day. After 1 week, the dose is increased to 100 mg 2 times / day. Taking into account the effectiveness and tolerability, the maintenance dose can be increased every week by 50 mg 2 times / day to a maximum daily dose of 400 mg (200 mg 2 times / day). Abolish Wimpat; recommended gradually (reducing the dose to 200 mg per week); The solution can be administered without additional dilution or diluted. There is experience in using the solution for infusions of up to 5 days. It is necessary to proceed to the drug intake as soon as it becomes possible.; Treatment with Wimpat; can be started with the ingestion of pills, and with a / in the introduction of the solution for infusion. If necessary, you can replace the intake of pills / in the introduction without re-titration of the dose and vice versa. You should not change the daily dose and frequency of use (2 times / day). When taken orally and with a / in the introduction of patients with mild and moderate renal impairment (CC> 30 ml / min) dose adjustment is not required. In patients with severe renal insufficiency (CC ≤ 30 ml / min), the maximum dose is 300 mg / day. Lacosamide is removed from the plasma during hemodialysis, within 4 hours after the AUC procedure is reduced by approximately 50%. Patients on hemodialysis, it is recommended to appoint an additional up to 50% of a single dose immediately after the procedure. Treatment of patients with severe renal failure should be carried out with caution, becauseclinical experience with the drug in these patients is small, and accumulation of a metabolite that does not have known pharmacological activity is possible. All patients with impaired renal function dose titration is recommended to be carried out with caution. When ingestion and with / in the introduction of patients with mild and moderately impaired liver function dose adjustment is not required. Titration dose such patients should be cautious, given that abnormal liver function is often accompanied by impaired renal function. The pharmacokinetics of lacosamide in patients with severe hepatic insufficiency has not been studied. When ingestion and with a / in the introduction of elderly patients dose reduction is not required. 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 plasma lacosamide concentration; Rules for preparing an infusion solution; Before the drug is introduced, make sure that the solution in the vial is clear, colorless and free of impurities. Otherwise, do not use this vial.; Wimpat; The solution for infusion is compatible with the following solvents: 0.9% sodium chloride solution, 5% dextrose solution, Ringer's lactate solution.; The prepared solution should be used within 24 hours after dissolution when stored in glass or polyvinyl chloride bottles at a temperature not exceeding 25 ° C. ; Unused solution should be disposed of in accordance with existing regulations.
Side effects
In the treatment with lacosamide, dizziness, headache, nausea and diplopia were the most frequent adverse reactions. As a rule, they were mild or moderately pronounced. The severity of some adverse reactions depended on the dose and decreased after its decrease. The frequency and severity of adverse reactions from the central nervous system and the digestive system usually decreased with time. The use of lacosamide is accompanied by a dose-dependent prolongation of the PR interval, as a result of which clinical conditions such as AV blockade, fainting and bradycardia are possible.; Adverse reactions noted more than in 1% of patients in clinical studies are listed below.Determination of the frequency of adverse reactions: very often (≥1 / 10); often (from ≥1 / 100 to <1/10); infrequently (from ≥1 / 1000 to <1/100); From the side of the central nervous system: very often - dizziness, headache; often - depression, irritability, imbalance, impaired motor coordination, impaired memory, impaired attention, cognitive impairment, hypesthesia, drowsiness, confusion, tremor, nystagmus, dysarthria. From the sense organs: very often - diplopia; often - blurred vision, vertigo, tinnitus. On the part of the digestive system: very often - nausea; often - vomiting, constipation, flatulence, dyspepsia, dry mouth.; Dermatological reactions: often - itching.; From the musculoskeletal system: often - muscle spasms.; Other: often - violation of gait, asthenia, fatigue, falls, increased risk of injury (due to incoordination and dizziness).
Overdose
Clinical data on the overdose of lacosamide are limited. Symptoms: after taking the drug at a dose of 1200 mg / day - mostly dizziness and nausea, which disappeared after reducing the dose. During the clinical trials, a single dose of lacosamide was registered at a dose of 12 g, which was taken along with the toxic doses of other antiepileptic drugs. The patient fell into a coma, but then fully recovered without consequences.; Treatment: there is no antidote to lacosamide; conduct symptomatic therapy; if necessary, hemodialysis can be used.
Interaction with other drugs
Research indicates a low likelihood of lacosamide interaction with other drugs. In preclinical studies, synergism or additive anticonvulsant action was observed in combination with levetiracetam, carbamazepine, phenytoin, valproic acid, lamotrigine, topiramate, gabapentin.; causing prolongation of the PR interval (for example, carbamazepine, lamotrigine, pregabalin) and class I antiarrhythmic drugs. However, in clinical studies, no additional lengthening of the PR interval was observed in patients who simultaneously took lacosamide in combination with carbamazepine or lamotrigine.; Lacosamide is a substrate of cytochrome P450 (CYP2C19); Powerful enzyme inducers such as rifampicin or St. John's wort (Hypericum pertow may cause a moderate decrease in systemic lacosamide concentration.In this regard, the appointment of such drugs or their cancellation should be careful.; Lacosamide in any therapeutic dose has no effect on plasma Css of anticonvulsant drugs, including levetiracetam, carbamazepine, carbamazepine , phenytoin, phenobarbital in various doses), reduced the overall systemic exposure of lacosamide by 25%. No evidence of significant interaction between lacosamide and p oral contraceptives with ethinyl estradiol and levonorgestrel. Lacosamide does not affect the concentration of progesterone.; Lacosamide does not affect the pharmacokinetics of digoxin.; There is no clinically significant interaction of lacosamide and metformin.; There is no data on the interaction of lacosamide with ethanol. % This effect may not have clinical significance. When taking a single dose, lacosamide did not affect the pharmacokinetics of omeprazole. The effect of other cytochrome P450 isoenzymes and other enzymes on the metabolism of lacosamide has not been precisely established. Lacosamide is not a substrate or inhibitor of R-glycoprotein.; The binding of lacosamide to plasma proteins is less than 15%. In this regard, a clinically significant interaction with other drugs that bind to proteins is unlikely.
special instructions
Treatment with lacosamide may be accompanied by dizziness, potentially resulting in injuries and falls. In this regard, patients should be careful. Analysis of data from clinical studies of anticonvulsants indicates a slight increase in the risk of suicidal thoughts and suicidal behavior. The mechanism to increase the risk is not clear, the 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 risks and the need to consult a specialist if suicidal behavior occurs.Patients receiving treatment with lacosamide should be carefully monitored and warned to consult a specialist if suicidal thoughts occur. Considering the possibility of extending the PR interval during treatment with Vimpat; a periodic ECG monitoring is recommended for patients. Syrup contains sodium auxiliaries propyl parahydroxybenzoate (E217) and sodium methyl parahydroxybenzoate (E219), which can cause allergic reactions (including those of a delayed type). 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 is on a diet restricting sodium intake.; Pediatric use; Lacosamide is not recommended for children and adolescents under the age of 16, because safety and efficacy of the drug in these age groups have not been studied.; Influence on the ability to drive vehicles and control mechanisms; The drug may affect the ability to drive a car or use sophisticated equipment. Treatment with this drug may be accompanied by the development of dizziness or blurred vision. Accordingly, patients are not recommended to drive a car or operate complex machinery.