Lamictal
Lamictal: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. With impaired renal function
- 10. For violations of liver function
- 11. Use in the elderly
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Lamictal
ATX code: N03AX09
Active ingredient: Lamotrigine (Lamotrigine)
Producer: GlaxoSmithKline Trading (Russia)
Description and photo update: 2019-12-08
Prices in pharmacies: from 480 rubles.
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Lamictal is an anticonvulsant.
Release form and composition
Dosage forms:
- Tablets: from yellow-brown to pale yellow, square shape with rounded corners, the inscription "GSEC7", "GSEE1" or "GSEE5" is embossed on the flat side, a convex square engraved with "25", "50" or “100”, respectively (10 pcs. In blisters, in a cardboard box 3 blisters);
- Soluble or chewable tablets: white or almost white in color with slight inclusions, with the smell of black currant; elongated biconvex tablets are engraved with “GS CL2” on one side, “5” on the other, square with rounded corners - on one side there is a convex square engraved with “25” or “100”, on the other - “GS CL5” "Or" GS CL7 "respectively (10 pcs. In blisters, in a box of 3 blisters).
The active ingredient of Lamiktal is lamotrigine:
- 1 tablet: 25 mg, 50 mg or 100 mg
- 1 tablet, soluble or chewable: 5 mg, 25 mg or 100 mg.
Auxiliary components:
- Tablets: microcrystalline cellulose, lactose monohydrate, sodium carboxymethyl starch, magnesium stearate, povidone, yellow iron oxide (E172);
- Soluble or chewable tablets: low-substituted hydroxypropyl cellulose, calcium carbonate, aluminum-magnesium silicate, povidone K30, sodium starch glycolate type A, sodium saccharin, magnesium stearate, black currant flavor 500.009 / AP 0551.
Pharmacological properties
Pharmacodynamics
Lamotrigine blocks voltage-gated sodium channels. In neuronal culture, the substance contributes to the voltage-dependent blockade of continuously repetitive impulses and minimizes the pathological release of glutamic acid (this amino acid plays a significant role in the development of epileptic seizures), and also inhibits the depolarization caused by glutamate.
Pharmacokinetics
Lamotrigine is absorbed at a high rate and almost completely from the intestine, almost not participating in the first-pass first-pass metabolic processes. After taking Lamiktal inside, its maximum plasma content is recorded after about 2.5 hours. After a meal, the maximum concentration is reached a little more slowly, but this does not affect the degree of absorption.
A single dose of the drug, not exceeding 450 mg, confirms the linear nature of the pharmacokinetics of lamotrigine. There are significant individual fluctuations in the maximum concentration of this compound in the equilibrium state, however, fluctuations in each individual patient remain quite rare.
The binding of lamotrigine to blood plasma proteins is approximately 55%. The release of a compound chemically bound to these proteins is unlikely to provoke a severe toxic effect. The volume of distribution is 0.92-1.22 l / kg.
The metabolism of lamotrigine is carried out by the enzyme uridine diphosphate glucuronyl transferase. Depending on the dose of the drug, there is a slight increase in the own metabolism of the active component. However, there is no information confirming the effect of lamotrigine on the pharmacokinetics of other antiepileptic drugs and the likelihood of interaction between this compound and other drugs, in the metabolic processes of which the cytochrome P 450 system is involved.
In adults without health problems, the average equilibrium clearance of lamotrigine is approximately 39 ± 14 ml / min. The active substance of Lamictal is metabolized, forming glucuronides, which are excreted through the kidneys. Less than 10% of lamotrigine is excreted unchanged in the urine, and approximately 2% through the intestines.
The half-life and clearance of Lamiktal are not related to the dose of the drug taken. In healthy adults, the elimination half-life ranges from 24 to 35 hours. Patients with Gilbert's syndrome showed a 32% decrease in drug clearance compared with the test group, but its value did not go beyond the normal values for the human population.
Other drugs taken concurrently with Lamictal have a significant effect on the half-life of lamotrigine. When combined with drugs-inducers of glucuronidation (phenytoin, carbamazepine), the half-life is reduced to about 14 hours, when taken simultaneously with valproate, it increases to an average of 70 hours.
In children, the clearance of lamotrigine, calculated per unit of body weight, is higher than in adult patients (the highest is in children under 5 years of age). In this category of patients, the half-life is usually shorter than in adults. Its average value is approximately 7 hours when combined with drugs that promote glucuronidation (phenytoin, carbamazepine), and increases to 45-50 hours when combining Lamictal with valproate.
The clearance of lamotrigine in elderly patients is practically the same as in younger patients.
In case of renal dysfunction, the initial dose of the drug is determined in accordance with the standard regimen for the use of antiepileptic drugs. A dose adjustment downward may be required only with a significant deterioration in renal function.
In patients with moderate hepatic impairment (class B according to the Child-Pugh scale), the initial, increasing and maintenance doses should be reduced by about 50%, and in patients with severe hepatic insufficiency (class C according to the Child-Pugh scale) - by 75%. Dose increase and maintenance dose should be adjusted in accordance with the clinical effect.
Basic clinical trials have proven the effectiveness of lamotrigine in the prevention of mood disorders in patients with bipolar disorder. The combined analysis of the results obtained confirmed that the duration of remission, which was defined as the period before the onset of the first episode of a depressive state and before the first episode of hypomania / mania / mixed episode of hypomania and mania after stabilization, was greater in the group of patients receiving lamotrigine compared with the placebo group. The duration of remission is increased in the case of depression.
Indications for use
The use of Lamiktal is indicated in the treatment of epilepsy:
- Patients over 12 years of age: monotherapy and as part of the combined treatment of partial and generalized seizures, including tonic-clonic seizures, seizures in Lennox-Gastaut syndrome;
- Children 3-12 years old: combination therapy of partial and generalized seizures, including tonic-clonic seizures, seizures in Lennox-Gastaut syndrome (after achieving clinical control of the patient's epilepsy, the patient can be transferred to monotherapy with lamotrigine); monotherapy for typical absences.
In addition, for patients over 18 years of age with bipolar affective disorders, the drug is prescribed to prevent mood disorders (hypomania, mania, depression, mixed episodes).
Contraindications
- Treatment of bipolar disorder in patients under 18 years of age;
- Hypersensitivity to drug components.
According to the instructions, Lamictal should be administered with caution in case of renal failure.
The appointment of lamotrigine during pregnancy and breastfeeding is possible only if the expected benefit to the mother outweighs the potential risk to the fetus and baby. Since the physiological changes that develop during pregnancy can affect the effect of lamotrigine and / or reduce the level of its concentration, it is necessary to provide the appropriate therapy for the patient's condition.
Instructions for the use of Lamiktal: method and dosage
Lamictal tablets are taken orally, swallowing whole, without breaking or chewing. If the doses calculated taking into account body weight correspond to incomplete tablets, it is necessary to take a smaller number of whole tablets.
The dissolving or chewable tablets can be dissolved in a small amount of water (sufficient to cover the tablet) before taking, or chewed or swallowed whole with water.
The dosage regimen and the period of use are prescribed by the doctor based on clinical indications.
Recommended dosage for patients over 12 years old:
- Monotherapy: initial dose - 25 mg 1 time per day for 2 weeks, then 50 mg 1 time per day for 2 weeks. Further, in order to achieve an optimal clinical effect, the dose should be increased by 50-100 mg every 1-2 weeks, sometimes up to 500 mg per day. Maintenance dose - 100-200 mg per day, taken 1-2 times;
- Combination therapy with valproic acid and other antiepileptic drugs or without them: the initial dose is 25 mg per day, taken every other day for 2 weeks, then 25 mg 1 time per day for 2 weeks. To achieve the optimal clinical effect, the dose is increased by 25-50 mg with an interval of 1-2 weeks. Maintenance dose of Lamiktal - 100-200 mg per day for 1 or 2 doses;
- Combination therapy (without valproic acid) with phenytoin, carbamazepine, phenobarbital, primidone (antiepileptic drugs that induce liver enzymes) and other antiepileptic drugs or without them: initial dose - 50 mg once a day for 2 weeks, then 50 mg 2 times a day for 2 weeks. The dose is increased at intervals of 1-2 weeks by no more than 100 mg until the desired therapeutic effect is achieved, in some cases up to 700 mg per day. The maintenance dose is 100-200 mg 2 times a day.
Recommended dosage for children 2 to 12 years old:
- In combination with valproate and other antiepileptic drugs or without them: the initial dose is at the rate of 0.15 mg per 1 kg of the child's weight 1 time per day for 2 weeks, then 0.3 mg per 1 kg 1 time per day for 2 weeks. Further, the dose is increased by 0.3 mg per 1 kg of body weight every 1-2 weeks until the onset of the optimal clinical effect. The maintenance daily dose is 1-5 mg per 1 kg of the child's weight in 1-2 doses, but not more than 200 mg per day;
- In combination with antiepileptic drugs that induce liver enzymes (carbamazepine, primidone, phenytoin, phenobarbital), in combination with other antiepileptic drugs or without them (except for valproate): initial daily dose - 0.6 mg per 1 kg of child's weight in 2 divided doses, duration - 2 weeks, then - 1.2 mg per 1 kg of the child's weight in 2 divided doses, duration - 2 weeks. The dose is increased by 1.2 mg per 1 kg of the child's weight every 1-2 weeks until the optimal therapeutic effect is achieved. The maintenance daily dose is 5-15 mg per 1 kg of the child's weight in 2 divided doses, but not more than 400 mg per day.
Correction of the dosage regimen should be carried out in accordance with the change in the child's weight. The maintenance dose for children 2-6 years old may correspond to the upper limit of the recommended doses.
Side effects
- Nervous system: often - fatigue, irritability, headache, anxiety, drowsiness, dizziness, insomnia, imbalance, nystagmus, ataxia, tremor; sometimes - aggressiveness; rarely - hallucinations, tics, confusion, agitation, choreoathetosis, motor and / or extrapyramidal disorders, increased frequency of seizures;
- Dermatological reactions: often - skin rash (usually maculopapular, transient, appears during the first two months of therapy); rarely - toxic epidermal necrolysis (Lyell's syndrome), exudative erythema multiforme (including Stevens-Johnson syndrome);
- Digestive system: often - dysfunction of the gastrointestinal tract (nausea, vomiting, diarrhea); rarely - a functional disorder of the liver, an increase in liver function tests, liver failure;
- Hematopoietic and lymphatic systems: rarely - anemia, neutropenia, pancytopenia, leukopenia, aplastic anemia, thrombocytopenia, agranulocytosis;
- Musculoskeletal system: often - back pain, arthralgia; rarely - lupus-like syndrome;
- Immune system: rarely - hypersensitivity syndrome (fever, facial edema, lymphadenopathy, hematological disorders, thrombohemorrhagic syndrome, liver damage, multiple organ failure);
- Organ of vision: often - blurred vision, diplopia, conjunctivitis;
- Others: with a sharp withdrawal of Lamiktal - increased frequency of seizures against the background of the development of withdrawal syndrome; may be noted (with insufficient clinical effect, including with status epilepticus) - multiple organ dysfunction, rhabdomyolysis, disseminated intravascular coagulation up to death.
Overdose
Fatal cases have been reported with doses of Lamictal 10–20 times the maximum recommended. Overdose symptoms were manifested in the form of ataxia, impaired consciousness, nystagmus, epileptic seizures and coma. Also, an overdose may be accompanied by an expansion of the QRS interval, that is, an increase in the time of intraventricular conduction.
As a treatment, hospitalization in a hospital and carrying out maintenance therapy measures is recommended in accordance with the protocols of the national toxicological center and the clinical picture of the patient's condition.
special instructions
In the absence of an obvious cause of the appearance of fever and lymphadenopathy (against the background of the absence of a skin rash), the drug should be discontinued, the patient needs an immediate thorough examination.
Skin rash is one of the symptoms of hypersensitivity syndrome, in rare cases, its severity can lead to the development of multiple organ failure and thrombohemorrhagic syndrome.
Rashes on the skin in most cases are mild, go away on their own and are not a dose-dependent effect (except for Lyell's and Stevens-Johnson's syndrome).
Cancellation of the drug should be made by gradually reducing the dose over two weeks, except in cases requiring urgent discontinuation of therapy, including the appearance of a skin rash.
Due to the risk of developing a skin rash, including serious cases requiring hospitalization, it is impossible to exceed the recommended dosage regimen or violate the therapy regimen.
Being a weak inhibitor of dihydrofolate reductase, with prolonged use Lamictal can affect the metabolism of folate. However, with therapy lasting up to 1 year, serious changes in the level of the average volume of corpuscles in the blood, hemoglobin, folate concentration in serum or erythrocytes (with a duration of admission up to 5 years) do not occur.
Due to the risk of accumulation of glucuronide (a metabolite of lamotrigine), the drug should be administered with caution in patients with renal insufficiency.
The drug should not be taken without consulting a doctor while concomitant therapy with other antiepileptic drugs containing lamotrigine.
When prescribing a daily dose of 1-2 mg, it is allowed to take it every other day, 2 mg for the first 2 weeks. Do not take the drug in a dose less than 1 mg.
In pediatric practice, children with a primary diagnosis should not be given drug monotherapy as the initial treatment. Only after the anticonvulsant effect is achieved with the help of combination therapy, it is possible to cancel the simultaneously used antiepileptic drugs and continue treatment with Lamictal in the form of monotherapy.
It is necessary to take into account the possibility of a violation of the pharmacokinetics of lamotrigine when changing therapy associated with the addition or withdrawal of concomitant antiepileptic drugs.
During the period of application of Lamiktal, patients need to refrain from potentially hazardous activities, the implementation of which requires a high speed of psychomotor reactions and concentration of attention.
With impaired renal function
In patients with end-stage renal failure, the initial dose of Lamiktal is calculated according to the standard antiepileptic drug regimen. For patients with significant renal dysfunction, a reduction in the maintenance dose is recommended.
For violations of liver function
For moderate liver dysfunctions (class B according to the Child-Pugh scale) and severe (class C according to the Child-Pugh scale), it is recommended to reduce the initial, increasing and maintenance doses by about 50 and 75%, respectively. The increasing and maintenance doses are adjusted depending on the therapeutic effect.
Use in the elderly
Since the pharmacokinetics of Lamictal in elderly patients is similar to that in adult patients, there is no need for dose adjustment.
Drug interactions
Phenytoin, phenobarbital, carbamazepine, primidone (antiepileptic drugs), paracetamol accelerate metabolism and halve the decay time of half of all atoms (T 1/2) of lamotrigine.
Valproate inhibits the metabolism of lamotrigine and prolongs its T 1/2 to 45-55 hours in children and up to 70 hours in adults, since it is competitively metabolized by hepatic enzymes.
Prescribing Lamictal to carbamazepine therapy can cause nausea, dizziness, diplopia, ataxia, blurred vision (it is recommended to reduce the dose of carbamazepine to eliminate unwanted effects).
Joining the intake of anhydrous lithium gluconate (2 g 2 times a day for 6 days) does not violate the pharmacokinetics of lithium at a dose of lamotrigine 100 mg per day.
After taking a single dose of bupropion with its repeated use, there is no significant change in the pharmacokinetics of lamotrigine, except for a slight increase in AUC for lamotrigine glucuronide.
Analogs
Analogs of Lamictal are: Vimpat, Gabapentin, Keppra, Lyrica, Neurontin, Topiramate, Levetiracetam, Egipentin, Tebantin, Konvulsan, Lamitor, Lameptil, Lamotrix, Lamotrigine, Lamotrigine Canon, Lamolep, Seizar, Triginet.
Terms and conditions of storage
Store at temperatures up to 30 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lamiktal
Reviews of Lamictal vary from positive to sharply negative, so it is impossible to give an unambiguous answer to the question of the effectiveness and safety of the drug. This is due to the fact that diseases for which lamotrigine is prescribed require the selection of an individual treatment regimen, both in terms of the drugs themselves and their dosages.
Patients who have tolerated Lamictal therapy well say that it helps quite well when used according to indications. The most common side effect is a skin rash, which in most cases goes away on its own.
The price of Lamictal in pharmacies
The approximate price for Lamictal in a package containing 30 tablets is 516-630 rubles (dosage 25 mg), 900-1235 rubles (dosage 50 mg) and 1684-1959 rubles (dosage 100 mg). Soluble or chewable tablets Lamictal with a dosage of 25 mg can be purchased for about 503-539 rubles, and with a dosage of 100 mg - for 1751-1904 rubles (the package contains 30 pieces).
Lamictal: prices in online pharmacies
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Drug name Price Pharmacy |
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Lamictal 25 mg tablets 30 pcs. 480 RUB Buy |
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Lamictal 5 mg tablets, soluble / chewable 30 pcs. RUB 525 Buy |
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Lamictal tablets 25mg 30 pcs. RUB 678 Buy |
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Lamictal 50 mg tablets 30 pcs. 891 RUB Buy |
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Lamictal tablets 50mg 30 pcs. 1166 RUB Buy |
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Lamictal 100 mg tablets 30 pcs. 1698 RUB Buy |
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Lamictal tablets 100mg 30 pcs. 1900 RUB Buy |
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!
