Vimpat - Instructions For Use, Price, Reviews, Analogues, Tablets, Syrup

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Vimpat

Vimpat: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Vimpat

ATX code: N03AX18

Active ingredient: lacosamide (lacosamide)

Manufacturer: Ebeve Pharma (Austria), YUSB Pharma S. A. (Belgium), Eisica Pharmaceuticals GmbH (Germany), Schwartz Pharma Manufacturing Inc. (USA)

Description and photo update: 2019-26-08

Prices in pharmacies: from 434 rubles.

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Vimpat is a drug with antiepileptic action.

Release form and composition

Dosage forms of Vimpat release:

• film-coated tablets: oval, biconvex, SP on one side; the color of the tablet and the marking on the other side (depending on the dose of 50/100/150/200 mg) - pinkish / dark yellow / pale orange / blue, "50" / "100" / "150" / "200" (in blisters of 14 pcs., in a carton box 1 or 4 blisters);
• syrup: transparent, slightly viscous, from colorless to yellow or yellow-brown in color, has a characteristic fruity odor (200 ml in dark glass or polyethylene terephthalate bottles, 1 bottle in a cardboard box);
• solution: colorless, transparent (20 ml vials, 1 vial in a cardboard box).

Composition of 1 tablet:

• active substance: lacosamide - 50, 100, 150 or 200 mg;
• auxiliary components (50/100/150/200 mg): hyprolosis - 1/2/3/4 mg; microcrystalline cellulose - 14/28/42/56 mg; magnesium stearate - 1.2 / 2.4 / 3.6 / 4.8 mg; low-substituted hyprolosis - 12.5 / 25 / 37.5 / 50 mg; salting HD 90 (microcrystalline cellulose and anhydrous colloidal silicon dioxide) - 31.3 / 62.6 / 93.9 / 125.2 mg; crospovidone - 10/20/30/40 mg;
• film coating (50/100/150/200 mg): Opadry II (color) 85F20249 purple / 85F38040 yellow / 85F27043 golden / 85F30675 blue (macrogol - 20.2 / 20.2 / 20.2 / 20.2%; talc - 14.8 / 14.8 / 14.8 / 14.8%; polyvinyl alcohol - 40/40/40/40%; titanium dioxide - 24.07 / 19.17 / 23.09 / 20%; indigo carmine dye FD&C blue 2 - 0.69 / 0/0/5%; dye iron oxide red - 0.22 / 0 / 0.42 / 0%, dye iron oxide yellow - 0 / 5.83 / 1.39 / 0%, dye iron oxide black - 0.02 / 0 / 0.1 / 0%) - 4.8 / 9.6 / 14.4 / 19.2 mg.

Composition of 1 ml of syrup:

• active substance: lacosamide - 15 mg;
• auxiliary components: sodium carmellose, glycerol, liquid (crystalline) sorbitol, macrogol 4000, sodium chloride, acesulfame potassium, anhydrous citric acid, sodium methyl parahydroxybenzoate, sodium propyl parahydroxybenzoate, masking flavor 501521 T, strawberry flavor 501440 T, purified water.

Composition of 1 ml of infusion solution:

• active substance: lacosamide - 10 mg;
• auxiliary components: 10% diluted hydrochloric acid - up to pH 4; sodium chloride - 7.62 mg; water for injection - up to 1 ml.

Pharmacological properties

Pharmacodynamics

The active substance of Vimpat is lacosamide (R-2-acetamido-N-benzyl-3-methoxypropionamide) - a functionalized amino acid, antiepileptic agent.

The exact mechanism of the drug's antiepileptic action has not been clarified. In in vitro electrophysiological studies, it was found that lacosamide is able to selectively enhance the slow inactivation of voltage-gated sodium channels, as a result of which hyperexcitable neuronal membranes are stabilized.

In animal studies, lacosamide prevented the development of seizures of primary generalized and partial epilepsy, delayed the formation of increased seizure activity.

In preclinical studies, Vimpat has been used in combination with gabapentin, lamotrigine, phenytoin, levetiracetam, topiramate, valproate, or carbamazepine. Lacosamide exhibited a synergistic additive anticonvulsant effect.

The efficacy of Vimpat as an adjunctive therapy (when taken in the recommended daily doses of 200 or 400 mg) has been proven in three placebo-controlled, randomized, multicenter clinical studies with a 12-week maintenance period. The effect of Vimpat in a daily dose of 600 mg was also shown in the course of controlled additional therapeutic studies, however, the severity of the action was comparable to that when taking the drug in a daily dose of 400 mg, while the tolerance was worse due to the development of side effects from the gastrointestinal tract and the central nervous system. In this regard, it is not recommended to take Vimpat at a dose of 600 mg per day. The maximum recommended daily dose is 400 mg. These studies were developed and carried out,to evaluate the efficacy and safety of lacosamide with the simultaneous use of 1 to 3 antiepileptic drugs in patients with uncontrolled partial seizures, including those with secondary generalization. 1308 patients took part in them, in the history of which there is data on the development of partial seizures during an average period of 23 years. According to the results, a 50% decrease in the frequency of seizures in the placebo, lacosamide 200 mg / day and lacosamide 400 mg / day groups was noted in 23, 34 and 40% of patients, respectively. According to the results, a 50% decrease in the frequency of seizures in the placebo, lacosamide 200 mg / day and lacosamide 400 mg / day groups was observed in 23, 34 and 40% of patients, respectively. According to the results, a 50% decrease in the frequency of seizures in the placebo, lacosamide 200 mg / day and lacosamide 400 mg / day groups was noted in 23, 34 and 40% of patients, respectively.

There is currently insufficient information on the possibility of discontinuing concomitant antiepileptic drugs and the use of lacosamide as monotherapy.

The pharmacokinetic characteristics and safety of a single saturating dose of infusional lacosamide were determined in a multicenter open-label study of the safety and tolerability of a rapid initiation of lacosamide therapy using a single intravenous saturating dose of 200 mg, followed by oral administration of Vimpat 2 times a day at a similar dosage as an adjunctive therapy in patients with partial seizures at the age of 16-60 years.

Pharmacokinetics

Suction:

• solution for infusion: the maximum concentration (C _max) is reached at the end of the infusion. After intravenous (IV) administration of Vimpat at a dose of 50–300 mg, the plasma concentration of lacosamide increases in proportion to the dose;
• syrup and film-coated tablets: after taking Vimpat inside, lacosamide is rapidly and completely absorbed. Bioavailability is about 100%. The concentration in plasma after taking the drug rapidly increases, the maximum level reaches within 0.5-4 hours. Food does not affect the degree of absorption and its speed.

The volume of distribution of lacosamide is about 0.6 l / kg, the connection with plasma proteins is less than 15%.

At least 95% of the received dose of Vimpat is excreted through the kidneys: unchanged ~ 40%, in the form of O-desmethylmetabolite - less than 30%. The polar fraction (presumably serine derivatives) found in urine is about 20%, in blood plasma - no more than 2%. The amount of other metabolites in urine is 0.5–2%.

According to in vitro data, the formation of O-desmethylmetabolite occurs mainly with the participation of cytochrome isoenzymes CYP2C19, 2C9 and 3A4. There are no significant differences in the elimination of lacosamide in patients who are extensive metabolizers (with a functional cytochrome CYP2C19 isoenzyme) and slow metabolizers (with a lack of a functional cytochrome CYP2C19 isoenzyme). In addition, studies on the interaction of lacosamide with omeprazole, which is an inhibitor of the isoenzyme CYP2C19, found that there were no clinically significant changes in the plasma concentration of lacosamide, which indicates the low significance of this pathway.

O-desmethylmetabolite has no pharmacological activity, its plasma concentration is about 15% of the level of lacosamide.

Lacosamide is excreted from the body by renal excretion and biotransformation. After intravenous administration and oral administration of lacosamide labeled with a radioactive isotope, approximately 95% of radioactivity was noted in urine, in feces - less than 0.5%. The half-life (T _½) of lacosamide in unchanged form is 13 hours. The pharmacokinetics of the drug is proportional to the dose, constant over time and characterized by low individual variability.

When using Vimpat 2 times a day, stationary concentrations of the drug in the blood are reached within 3 days. With cumulation, there is an increase in plasma concentration by about 2 times.

The steady-state concentration of a substance in the blood after a single loading dose of 200 mg is comparable to that when Vimpat is taken orally 2 times a day, 100 mg.

Special patient groups:

• race: no clinically significant differences were found in the pharmacokinetics of lacosamide in the Caucasian, Negroid and Asian races;
• gender: in clinical studies it was found that there are no significant differences in the plasma concentration of lacosamide in women and men;
• advanced age: studies with 4 patients over 75 years old showed an increase in the area under the concentration-time curve (AUC) by 50% in women and 30% in men compared with younger patients. This is partly due to the reduced body weight (in women - 23%, in men - 26% of normal body weight). According to research data, in elderly patients, in addition, renal clearance is somewhat reduced;
• impaired renal function: with mild to moderate renal failure, AUC increases to about 30%, with severe and terminal stage requiring hemodialysis - up to 60% compared with patients without impaired renal function. Moreover, C _maxdoes not change. Lacosamide is removed from plasma by hemodialysis. A four-hour hemodialysis session reduces the AUC by an average of 50%, therefore, an additional dose of Vimpat is recommended after the procedure. With mild to moderate renal failure, the release of O-desmethylmetabolite decreased several times. In patients with end-stage renal disease in the absence of hemodialysis, the levels of this metabolite were increased and increased continuously during 24-hour follow-up. It is not fully established whether the reduced release of O-desmethylmetabolite can cause an increase in the number of side effects in patients with end-stage renal failure, but it has been confirmed that this metabolite does not have pharmacological activity;
• impaired liver function: with moderate hepatic failure, an increase in the plasma concentration of lacosamide is observed (an increase in AUC by about 2 times). One of the reasons for increased exposure in patients participating in the studies is a concomitant decrease in renal function. The decrease in non-renal clearance in patients who participated in the studies was estimated as an increase in the AUC of lacosamide by 20%. The pharmacokinetic parameters of lacosamide in severe hepatic failure have not been studied.

Indications for use

According to the instructions, Vimpat is prescribed for adults and children from 16 years of age for the treatment of partial seizures with / without secondary generalization (simultaneously with other drugs).

Infusion administration is indicated in cases where oral administration of the drug is not possible.

Contraindications

Absolute:

• phenylketonuria (for syrup, since it contains aspartame);
• deficiency of sucrase-isomaltase, hereditary fructose intolerance, glucose-galactose malabsorption (for syrup, since it contains fructose);
• AV block II – III degree;
• age up to 16 years (there are no data on the effectiveness / safety of the drug in this group of patients);
• lactation period (there are no data on the effectiveness / safety of the drug in this group of patients);
• individual intolerance to the components of Vimpat.

Relative (diseases / conditions in which Vimpat is prescribed with caution):

• severe renal failure (with creatinine clearance ≤ 30 ml / min);
• conduction disturbances;
• heart failure;
• a history of myocardial infarction;
• combined use with drugs that can lead to an extension of the PR interval;
• old age with an increased likelihood of heart disease;
• pregnancy (there are no clinical data to assess the efficacy / safety of Vimpat; use is possible only in cases where the expected benefit is higher than the possible risk; in cases of planning pregnancy, the appropriateness of therapy should be assessed).

Instructions for use of Vimpat: method and dosage

Vimpat syrup and tablets are taken orally, regardless of the meal time.

Vimpat solution is intended for intravenous administration. The drug is administered for 15-60 minutes.

The daily dose is divided into 2 parts - in the morning and evening.

The recommended starting dose is 50 mg 2 times a day. After 7 days, the dose is increased to 100 mg 2 times a day.

Given the tolerance / efficacy, in the future, the maintenance dose can be increased (depending on the dosage form):

• tablets: up to 150 mg 2 times a day in the third week of administration;
• syrup, infusion solution: 50 mg 2 times a day, weekly.

The maximum daily dose from the fourth week is 400 mg.

When canceling, the dose is reduced gradually - by 200 mg every 7 days.

Vimpat solution can be administered with or without additional dilution.

There is an experience of using a solution lasting up to 5 days, the patient should be transferred to oral administration of the drug as soon as possible.

Dosage forms of Vimpat can be changed without repeated dose titration. In this case, the daily dose and frequency of use should not be adjusted.

The maximum dose for severe renal failure (with creatinine clearance ≤ 30 ml / min) is 300 mg per day. Patients on hemodialysis are advised to use an additional dose of 50% of the standard dose immediately after the end of the procedure. The therapy is carried out with caution, since the clinical experience of using Vimpat in such patients is small and the accumulation of a metabolite is possible, which does not have a known pharmacological activity. Dose titration should be done with caution in all patients with impaired renal function.

In mild / moderate impairment of hepatic function, the dose is not adjusted, but in such patients, dose titration is performed with caution, taking into account the possible concomitant functional impairment of the kidneys.

Before the introduction of Vimpat, you need to visually make sure that the solution in the vial has not changed its properties - it does not contain foreign impurities, colorless and transparent.

Compatible solvents: 5% dextrose solution, 0.9% sodium chloride solution, Ringer's lactate solution.

After dissolution, the prepared solution can be used for 24 hours if stored in PVC / glass vials at temperatures up to 25 ° C.

Side effects

The most common adverse reactions are headache, dizziness, diplopia and nausea. They are usually mild to moderate in nature. The severity of some disorders depends on the dose and decreases after its decrease. The frequency and severity of adverse reactions of the nervous and digestive systems in most cases decreases over time. Dizziness is the most common unwanted disorder leading to discontinuation of Vimpat.

Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):

• cardiovascular system: infrequently - bradycardia, AV block, atrial fibrillation and atrial flutter;
• digestive system: very often - nausea; often - vomiting, flatulence, constipation, dry mouth, dyspeptic disorders;
• musculoskeletal system: often - muscle spasms;
• immune system: infrequently - hypersensitivity reactions;
• central nervous system: very often - dizziness, headache; often - impaired coordination of movements, balance, attention and memory, hypesthesia, drowsiness, nystagmus, tremor, dysarthria, cognitive impairment;
• blood and lymphatic system: with an unknown frequency - agranulocytosis;
• organ of sight and hearing: very often - diplopia; often - blurred vision, vertigo, tinnitus;
• psyche: often - confusion, depression, insomnia; infrequently - euphoria, aggression, agitation, hallucinations, mental disorders, suicidal attempts / thoughts;
• skin and subcutaneous fat: often - itching, rash; infrequently - urticaria, angioedema;
• liver and biliary tract: infrequently - changes in liver function tests;
• general disorders and disorders at the injection site: often - irritability, gait disturbance, fatigue, asthenia, skin irritation at the injection site, pain or discomfort; infrequently - redness of the skin at the injection site;
• intoxication, injury and complications of manipulation: often - an increased risk of injury / fall, skin damage (associated with impaired coordination of movements and the appearance of dizziness).

Overdose

Clinical data on drug overdose are limited. After taking Vimpat in a daily dose of 1200 mg, symptoms of the gastrointestinal tract and the central nervous system (nausea, dizziness) were mainly observed, which disappeared after the dose was reduced.

In the program of clinical trials, the largest declared overdose of lacosamide was 12,000 mg, the drug was taken simultaneously with other antiepileptic drugs in toxic doses. The patient fell into a coma, but later recovered completely without serious consequences.

There is no antidote to lacosamide. Overdose treatment is symptomatic. If necessary, hemodialysis can be performed.

special instructions

Dizziness may occur when using Vimpat, which can lead to injury or falls. In this regard, patients should be careful during therapy.

The possibility of suicidal thoughts / behavior should be taken into account.

Due to the existing probability of prolongation of the PR interval, it is recommended to periodically monitor the ECG.

Sodium propyl parahydroxybenzoate and sodium methyl parahydroxybenzoate, which are part of Vimpat syrup, can cause allergic reactions, including delayed-type reactions.

For 200 mg of lacosamide in syrup, there are:

• 3700 mg of sorbitol, which corresponds to 9.7 kcal;
• 25.2 mg sodium to consider when following a sodium restricted diet.

Influence on the ability to drive vehicles and complex mechanisms

Since therapy may be accompanied by the appearance of dizziness or blurred vision, it is recommended to refuse to drive vehicles while using Vimpat.

Application during pregnancy and lactation

An undesirable effect of the drug on fertility or reproduction in rats of both sexes was not observed when lacosamide was used at doses that create a plasma AUC concentration of about 2 times higher than in humans when used at the maximum recommended dose.

According to the results of studies of all antiepileptic drugs, it was found that the incidence of congenital malformations in children whose mothers received therapy for epilepsy is 2–3 times higher than in the general population (where this indicator is 3%). In patients undergoing treatment, an increase in the incidence of congenital malformations in children was noted against the background of polytherapy, however, the degree of influence of the disease and / or treatment on increasing this risk is still unknown. In addition, effective antiepileptic therapy should not be stopped during pregnancy, since the worsening of the course of the disease also has a negative effect on the fetus and the expectant mother.

There are no clinical data on the use of lacosamide during pregnancy in humans. Teratogenic effects have not been reported in animal studies. However, embryotoxicity was observed in rats and rabbits when using Vimpat in doses toxic to the mother's body. The potential risk to humans has not been identified. In this regard, Vimpat is allowed to be used during pregnancy only in cases where the benefits of therapy for the mother are definitely higher than the possible risks to the fetus. Women planning a pregnancy should carefully evaluate the appropriateness of using lacosamide.

Physicians are advised to register the data of pregnant patients in the European and International Registry of Antiepileptic Drugs and Pregnancy (EURAP) in order to monitor the effects of Vimpat during the period of gestation.

Whether lacosamide is excreted in mother's milk is unknown. In animal studies, excretion has been noted. In this regard, breastfeeding should be discontinued if treatment is required during lactation.

Pediatric use

Vimpat is contraindicated for use in children under 16 years of age.

With impaired renal function

With mild to moderate renal impairment (creatinine clearance> 30 ml / min), there is no need to adjust the dose of the drug. In severe renal failure (creatinine clearance <30 ml / min), the daily dose of Vimpat should not exceed 300 mg.

Lacosamide is excreted from plasma by hemodialysis. During a 4-hour procedure, the AUC is reduced by about 50%. In this regard, patients on hemodialysis immediately after the procedure are recommended to take an additional dose, up to 50% of the usual single dose.

Patients with severe renal impairment should be treated with caution, since clinical experience is limited and a metabolite with no known pharmacological activity may accumulate.

All patients with impaired renal function are advised to titrate the Vimpat dose with caution.

For violations of liver function

With mild and moderate impairment of liver function, there is no need to adjust the dosage regimen of Vimpat. However, the dose should be titrated with caution, since impaired hepatic function is often accompanied by impaired renal function.

The pharmacokinetic characteristics of lacosamide in patients with severe hepatic impairment have not been studied.

Use in the elderly

A dose reduction of Vimpat is not required in elderly patients. However, due to the limited experience of using lacosamide in the elderly, care should be taken to take into account the likelihood of an age-related decrease in renal clearance and, as a consequence, the possibility of an increase in the plasma concentration of the drug.

Drug interactions

With the combined use of Vimpat with certain drugs / substances, the following effects may develop:

• anticonvulsants that induce enzymes (carbamazepine, phenytoin, phenobarbital in various doses): a significant decrease in the total systemic exposure of lacosamide;
• rifampicin, St. John's wort: a moderate decrease in the systemic concentration of lacosamide (caution is required when prescribing / canceling the combination);
• levetiracetam, carbamazepine, valproic acid, phenytoin, topiramate, lamotrigine, gabapentin: synergism or additive anticonvulsant action;
• drugs that cause prolongation of the PR interval, including carbamazepine, lamotrigine, pregabalin; class I antiarrhythmic drugs: the combination requires caution.

Analogs

Vimpat analogs are: Algerica, Benzonal, Valparin, Valproic acid, Gabagamma, Gabapentin, Hexamidine, Depakin, Zenitetam, Zeptol, Inovelon, Carbamazepine, Katena, Keppra, Clonazepam, Konvulex, Tegaretaluqtal, Rilepopil, Finlepsin, Enkorat, Epitropil, etc.

Terms and conditions of storage

Store at temperatures up to 25 ° C (infusion solution) or 30 ° C (tablets, syrup). Keep out of the reach of children.

Shelf life:

• syrup - 2 years;
• tablets, infusion solution - 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Vimpat

According to reviews, Vimpat is an effective antiepileptic agent that is well tolerated, does not cause drowsiness, and rarely has side effects.

There are reports in which patients write that this drug was prescribed by a doctor to their children under 16 years old, although this age is a contraindication in the instructions. The treatment was accompanied by adverse reactions, including tearfulness and fear.

The disadvantages of Vimpat include the relatively high cost and absence in many pharmacies.

Price for Vimpat in pharmacies

Average prices for Vimpat in the form of film-coated tablets are: 50 mg each - 638 rubles. for 14 pcs., 100 mg - 1218 rubles. for 14 pcs., 150 mg - 6689 rubles. for 56 pcs., 200 mg - 8774 rubles. for 56 pcs. The cost of syrup and solution for infusion is currently unknown.

Vimpat: prices in online pharmacies

Drug name Price Pharmacy

Vimpat 50 mg film-coated tablets 14 pcs. 434 r Buy

Vimpat tablets p.p. 50mg 14 Pcs. 547 r Buy

Vimpat 100 mg film-coated tablets 14 pcs. RUB 955 Buy

Vimpat tab. p.p. 100mg n14 1044 RUB Buy

Vimpat solution for inf. 10mg / ml 20ml 2142 RUB Buy

Vimpat 10 mg / ml solution for infusion 20 ml 1 pc. 2142 RUB Buy

Vimpat 150 mg film-coated tablets 56 pcs. 5469 RUB Buy

Vimpat 200 mg film-coated tablets 56 pcs. RUB 7,590 Buy

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!