Lamictal tabs 100mg #30

Instruction for Lamictal

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Composition

One tablet contains 25, 50 or 100 mg of lamotrigine, the active ingredient.
Additional ingredients: sodium starch glycolate (type A), lactose monohydrate, microcrystalline cellulose, povidone, magnesium stearate, iron oxide yellow (E172).
One soluble (chewable) tablet includes 5, 25 or 100 mg of lamotrigine, the active ingredient.
Additional ingredients: low-substituted hydroxypropylcellulose, magnesium stearate, calcium carbonate, aluminum-magnesium silicate, sodium saccharin, povidone K30, sodium starch glycolate (type A), blackberry flavor 500.009 / AP 0551.

Form of issue

The drug Lamictal is available in the form of tablets or soluble (chewable) tablets, 30 pieces in one package.

pharmachologic effect

Anticonvulsant.

Pharmacodynamics and pharmacokinetics

The mechanism of action of Lamictal is the blocking of potential-dependent sodium channels, the stabilization of neuronal membranes, and the suppression of glutamic acid production, which plays a primary role in the formation of seizures of an epileptic nature.
Absorption of lamotrigine from the intestine passes completely and quickly enough. Plasma Cmax is observed after approximately 2.5 hours after oral administration. Tmax increases slightly with eating, although the absorption level does not change.
An internal dose of up to 450 mg is characterized by a linear pharmacokinetics.
The recorded connection with plasma proteins is about 55%, with a volume of distribution equal to 0.92-1.22 l / kg.
Metabolic transformations of lamotrigine take place with the participation of the enzyme glucuronyltransferase. The pharmacokinetics of other antiepileptic drugs does not depend on lamotrigine.
The clearance of lamotrigine in adults is 39 ± 14 ml / min on average.
Metabolism continues to glucuronides, excreted from the body with urine. Less than 10% of the drug in unchanged form is also excreted in urine, approximately 2% with feces. T1 / 2 and clearance of the drug do not depend on the oral dose taken.
The lamotrigine's clearance, in relation to body weight, is higher in childhood, especially in patients under 5 years of age. Also in children, in comparison with adults, T1 / 2 is usually shorter.
There are data that confirm the absence of significant differences in the clearance of creatinine in elderly and young patients.
The average coefficient of clearance of lamotrigine, when taken by patients with chronic renal failure (CRF) and patients on hemodialysis is 0.42 ml / min / kg (with CRF), 0.33 ml / min / kg (with admission between hemodialysis passes ) and 1.57 ml / min / kg (with hemodialysis). Proportionately, the average T1 / 2 is observed at 42.9 / 57.4 / 13 hours.
During 4 hours of hemodialysis, approximately 20% lamotrigine is excreted. In this regard, with kidney pathologies, the initial dosage of lamotrigine is calculated according to the standard regimen for the use of antiepileptic drugs. With pathologies of kidney function of a serious nature, it is recommended to lower the maintenance dosages.
The average clearance rate of lamotrigine, when administered to patients with mild, moderate and severe hepatic impairment (Child-Pugh stages A, B and C) is 0.31 / 0.24 / 0.1 mL / min / kg, respectively.
The initial, increasing and maintenance dosages should be reduced by approximately 50% with a moderate degree of liver failure (stage B) and approximately 75% with a severe degree of liver failure (stage C). In the future, the initial and increasing doses of the drug must be adjusted according to the observed clinical effect.

Indications for use

Patients over 12 years of age

Epilepsy (generalized and partial seizures, including the manifestation of tonic-clonic seizures, as well as seizures developing with Lennox-Gastaut disease), both in monotherapy and combined treatment.

Patients from 2 to 12 years of age

Epilepsy (generalized and partial seizures, including the development of tonic-clonic seizures, as well as bouts of developing with Lennox-Gastaut disease), as part of a comprehensive treatment (further cancellation of other antiepileptic drugs (PEP) and continuation of therapy with one Lamictal, but only after full control of epilepsy is achieved against the background of complex treatment being conducted).
Treatment of typical absences (monotherapy).

Patients over 18 years of age

In order to prevent mood disorders (mania, depression, hypomania, and mixed episodes).

Contraindications

The only absolute contraindication to taking Lamictal is hypersensitivity to the components of tablets.
Caution is recommended to prescribe the drug in case of kidney failure.

Side effects

CNS

    anxiety;
    dizziness;
    irritability;
    headache;
    drowsiness;
    fatigue;
    insomnia;
    disturbance of balance;
    nystagmus;
    tremor;
    ataxia;
    tics;
    aggressiveness;
    hallucinations;
    excitation;
    confusion of consciousness;
    motor disorders;
    choreoathetosis;
    extrapyramidal disorders;
    more frequent seizures.

Skin and subcutaneous tissue

    rash on the skin, mostly spotty-papular nature;
    exudative erythema multiforme (including Stevens-Johnson syndrome), as well as epidermal toxic necrolysis (including Lyell's disease) (rarely).
As a rule, a rash on the skin is observed during the first 2 months of the onset of therapy and disappears when treatment is withdrawn.
In some cases, it is possible to develop skin reactions of a severe nature, mainly occurring after the withdrawal of treatment (sometimes residual scars were observed). It is also possible to form states of potentially life-threatening patients (Lyell and Stevens-Johnson syndromes).

Hemopoietic and lymphatic system

    leukopenia;
    agranulocytosis;
    neutropenia;
    anemia;
    pancytopenia;
    thrombocytopenia;
    aplastic anemia.
The association of these hematological abnormalities with DIC syndromes and hypersensitivity has not been proven, and they can develop both because of these syndromes and on their own.

The immune system

    hypersensitivity syndrome (mainly manifested by fever, facial edema, lymphadenopathy, hematologic disorders, DIC syndrome, liver damage, multiple organ failure).
Early manifestations of hypersensitivity (such as lymphadenopathy and fever) can occur even without a previous skin rash. In this case, in the absence of another reason for the development of these manifestations, it is necessary to examine the patient and temporarily cancel the therapy with lamotrigine.
Eruptions on the skin are part of hypersensitivity manifestations with varying degrees of severity, in single cases up to the formation of the DIC syndrome and multiple organ failure.

The organs of sight

    conjunctivitis;
    blurred vision;
    diplopia.

Digestive system

    a feeling of nausea with possible vomiting;
    diarrhea;
    increase in the content of hepatic enzymes;
    decreased liver function;
    Insufficiency of the liver.

Musculoskeletal system

    low back pain;
    arthralgia;
    lupus-like syndrome.
Rapid cancellation of Lamictal can lead to increased frequency of observed seizures (withdrawal syndrome).
It has been proved that, with unsatisfactory lamotrigine efficacy, including with established epileptic status, it is possible to develop multi-organ dysfunction, rhabdomyolysis, disseminated intravascular coagulation, which can cause the patient's death.

Instructions for use Lamictal (Method and dosage)

Instructions for use Lamictal recommends the taking of tablets orally whole, washed down with a small amount of water (without preliminary chewing).
Dissolve (chewable) tablets before use should be filled with water so that it covers the surface of the tablet.
Treatment of epilepsy with Lamictal as a monopreparation

Patients over 12 years of age

Initiation of therapy is carried out in a single daily dose of 25 mg, which is taken 14 days. Over the next 14 days, a single daily dose of Lamictal is increased to 50 mg. Further, every 7-14 days, the dosage should be increased by 50-100 mg, until the best therapeutic efficiency is achieved, which is maintained by a daily dose of 100-200 mg taken once or twice every 24 hours.
Some patients, in order to achieve optimal treatment effectiveness, require the administration of elevated maintenance daily doses of Lamictal - up to 500 mg.

Patients from 3 to 12 years of age

When Lamictal monotherapy is used for patients with typical absences, the initial daily dose of lamotrigine should be 0.3 mg / kg divided into 1 or 2 doses, the first 14 days, with a further increase in double dose (0.6 mg / kg /) with the same multiplicity and duration of admission (14 days). In the future, the dose should be increased by no more than 0.6 mg / kg in 7-14 days, until the patient's response to the treatment is positive and stable.
Such a dosage regimen allows for a relatively accurate dosage of the drug in children weighing 40 kilograms or more. Typically, the usual maintenance daily dose of the drug is a dose of 1 to 10 g / kg, taken once or twice in 24 hours. Some patients may require higher doses. Exceed the initial, as well as subsequent doses of lamotrigine is not recommended because of the risk of rash.
Combined treatment of epilepsy

Patients over 12 years of age

Patients who have been treated with valproic acid in combination with or without other valproic acid are advised to begin Lamictal treatment with a daily dose of 25 mg taken once a day, the first 14 days, with further administration of the same dose every day, and another 14 days. Subsequently, the daily dose of lamotrigine is increased by 25-50 mg, but not more, every 7-14 days, to the optimal therapeutic dose. The maintenance dose, as a rule, is equal to 100-200 mg, taken 1 or 2 times in 24 hours.
Patients undergoing parallel therapy with PEP or other drugs inducing glucuronidation of lamotrigine, in combination with or without other drugs (excluding valproates) are prescribed Lamictal in the initial daily dosage of 50 mg, the first 14 days. In the next 14 days, the daily dose is raised to 100 mg in 2 divided doses, after which, to determine the optimal therapeutic effectiveness, it is further increased by 100 mg, but not more, every 7-14 days.
Supportive therapy, usually takes place in daily doses of 200-400 mg, divided into two doses. In rare cases, it may be necessary to administer higher daily doses, up to 700 mg.
Patients who take drugs that do not significantly inhibit or induce lamotrigine glucuronin initiation are treated with Lamictal from a single daily dose of 25 mg, the first 14 days, with an increase of 50 mg in the subsequent 14 days. Further increase in dosage is carried out every 7-14 days, by 50-100 mg, but no more, until the optimal treatment regimen is determined. Supportive therapy, usually takes place in a daily dose of 100-200 mg, once or twice a day.

Patients from 3 to 12 years of age

Children who take valproic acid medicines in combination with or without other AEDs are given an initial single daily dose of Lamictal corresponding to 0.15 mg / kg, the first 14 days. Then, the daily dose is raised to 0.3 mg / kg, once every 24 hours for another 14 days. In the future, this dose increases every 7-14 days by 0.3 mg / kg, until the optimal response to treatment is determined. Supportive therapy, as a rule, requires daily doses of 1 to 5 mg / kg, taken once or twice in 24 hours. The maximum daily dosage is 200 mg. This dosing scheme allows for a relatively accurate selection of doses in children weighing 40 kilograms or more.
Children who undergo parallel therapy with PEP or other drugs that induce glucuronidation of lamotrigine in combination with or without other PEP (except valproate) are given Lamictal at an initial daily dosage of 0.6 mg / kg divided into two doses over a period of 14 days. Within the next 14 days, the dose is increased to 1.2 mg / kg, with the same reception frequency.
Further increase in doses, before selecting the optimal dosing regimen, occurs every 7-14 days, but not more than 1.2 mg / kg. Supportive treatment is carried out at a daily dose of 5-15 mg / kg divided by two times. The maximum daily dosage is 400 mg.
Children who take drugs that do not significantly inhibit or induce lamotrigine glucuronin initiation are treated with Lamictal from a single daily dose of 0.3 mg / kg, once or twice every 24 hours, for 14 days.
The next 14 days continue treatment at a daily dose of 0.6 mg / kg, in 1 or 2 doses. Further, the increase in daily doses is every 7-14 days, no more than 0.6 mg / kg, until the best therapeutic effectiveness is achieved. Supportive treatment, as a rule, requires the administration of daily doses from 1 to 10 mg / kg, taken once or twice in 24 hours. The maximum daily dosage is 200 mg.

Patients under 3 years of age

Children under 3 years of age are not prescribed Lamictal in a solid dosage form (tablets). For this age category (from 2 years) there are chewable (soluble) tablets.
In order to maintain the optimal therapy and dosage regimen, the weight of the child should be monitored and, with its modification, dose adjustments should be made.
Exceed the initial, as well as subsequent doses of lamotrigine is not recommended because of the risk of rash.
Patients taking PEP with unexplained pharmacokinetic interaction with lamotrigine should use a dosing regimen designed for valproate. For patients undergoing valproate therapy, no treatment should be prescribed in the case of a calculated dose of lamotrigine equal to 2.5 mg.
Bipolar affective disorder

Patients over 18 years of age

For patients who are already taking valproate, the onset of Lamictal therapy is indicated in a daily dose of 25 mg taken every other day, the first 14 days. After that, in the next 14 days, they switch to taking the same dose every day. At the fifth week of therapy, the daily dose is increased to 50 mg, in 1 or 2 doses. As a rule, in the future, as a supportive take a daily dose of 100 mg, broken down into 1 or 2 admission. The maximum allowable daily dosage is 200 mg.
Patients taking medications in parallel - stimulants lamotrigine glucuronin (Primidone, Carbamazepine, Phenytoin, Phenobarbital) and not taking valproate, are prescribed Lamictal therapy with an initial single daily dose of 50 mg, for 14 days. In the next 14 days, an increase in the daily dose to 100 mg, divided into two doses, should be noted.
The fifth week of therapy takes place at a daily dose of 200 mg, and the sixth in 300 mg, in two divided doses. As a rule, the maintenance daily dosage, appointed from the seventh week of treatment, is taken twice a day and equal to 400 mg.
When Lamictal is prescribed in monotherapy or patients who do not take lamotrigine glucuronide inhibitors or inducers, the initial single daily dose is 25 mg, for 14 days, with the transition to the next 14 days, to receive a daily dose of 50 mg taken once or twice in 24 hours. On the fifth week, an increase in the daily dose to 100 mg is recommended.
The subsequent optimal therapy, usually carried out at a daily dose of 200 mg, with the same frequency of drug intake. It is possible to use lamotrigine in the dose range from 100 mg to 400 mg.
Subsequently, with the selection of a maintenance daily dose, other psychotropic drugs can be canceled and corrected dose of Lamictal.
With the abolition of valproates, the maintenance dose of Lamictal is doubled.
With the elimination of glucuronation inducers, the dose of Lamictal gradually (over 3 weeks) decreases, usually twice.
With the elimination of antiepileptic or psychotropic drugs that do not inhibit or induce glucuronation, the maintenance dose of Lamictal is maintained at the level of optimal efficiency.
Clinical experience of adjustment of doses of Lamictal in the treatment of bipolar affective disorders, after joining to the therapy of other drugs, is absent, nevertheless, one can assume relatively correct correction schemes based on the studied drug interactions.
When adding lamotrigine (valproic acid) glucuronide inhibitors to therapy, the sustained daily dose of Lamictal should be reduced by half.
When glucuronation inducers are added, the dose of Lamictal gradually (for 3 weeks) increases, usually two times.
With the addition of antiepileptic or psychotropic drugs that do not inhibit or induce glucuronation, the maintenance dose of Lamictal is maintained at the level of optimal efficiency.
Patients taking PEP with unexplained pharmacokinetic interaction with lamotrigine should use a dosing regimen designed for valproate.
If it is necessary to cancel Lamictal therapy, with bipolar affective disorders, it is possible to cancel the drug without gradually lowering the dosages.
Exceed the initial, as well as subsequent doses of lamotrigine is not recommended because of the risk of rash.
Changes in dosing regimens Lamictal, for the treatment of elderly patients (after 65 years), is not required.
In liver pathologies, the initial and subsequent doses of lamotrigine should be reduced by approximately 50% in patients with moderate (stage B) degree of impairment and by 75% in patients with severe (stage C) degree of impairment.
In kidney pathologies, especially with a significant decrease in their function, a reduction in maintenance doses of the drug may be necessary.

Overdose

There is evidence of a single application of doses of Lamictal, which exceeded the maximum allowable by 10-20 times, with symptoms of overdose being: ataxia, nystagmus, impaired consciousness, coma is also possible.
If an overdose is detected, it is necessary to hospitalize the patient and prescribe supportive treatment according to the general condition picture or the recommendations of the toxicology service.

Interaction

The simultaneous administration of valproic acid suppresses the glucuronidation of lamotrigine, which leads to a decrease in the rate of its metabolism and an increase in its half-life almost twice.
Some PEP (carbamazepine, phenytoin, primidone, phenobarbital), which are inducers of microsomal liver enzymes, affect the acceleration of metabolism and the glucuronidation of lamotrigine.
Parallel administration of carbamazepine may lead to dizziness, diplopia, ataxia, blurred vision and nausea. These symptoms disappear with decreasing doses of carbamazepine.
The combined use of Lamictal and Topiramate increases the plasma concentration of the latter by 15%.
Multiple oral administration of Bupropion does not significantly affect the pharmacokinetics of lamotrigine, but leads to a slight increase in its AUC.
A single dose of olanzapine 15 mg lowers Cmax and lamotrigine AUC, by approximately 20% and 24%, respectively.
The simultaneous administration of Lamictal and Risperidone may cause drowsiness.
The minimal effect on the release of 2-N-glucuronide (lamotrigine metabolite) is: Amitriptyline, Bupropion, Clonazepam, Lorazepam, Fluoxetine, Haloperidol.
The use of combined oral contraceptives, which contain 150 μg of levonorgestrel and 30 μg of ethinylestradiol, can lead to approximately a twofold increase in lamotrigine clearance, which in turn leads to a decrease in its Cmax and AUC by 39% and 52%, respectively.
During 7 days free from the use of the active drug, an increase in the plasma content of lamotrigine was detected, its plasma content by the end of the free week was twice as high. There was also a slight increase in the clearance of levonorgestrel, which causes a decrease in its Cmax and AUC by 12% and 19%, respectively. In connection with this, there was a slight increase in hormonal activity, although it did not lead to confirmed ovulation.
Taking Rifampicin lowers T1 / 2 and increases the clearance of lamotrigine. In this regard, patients taking Rifampicin should begin taking Lamictal according to the scheme of joint administration with drugs inductors of glucuronidation.
With the appointment of lopinavir / ritonavir, the plasma content of lamotrigine was reduced by approximately 50%. In this regard, patients taking lopinavir / ritonavir should begin taking Lamictal according to the scheme of joint administration with drugs induction glucuronation.
The use of atazanavir / ritonavir (300 mg / 100 mg) lowers Cmax and lamotrigine AUC (100 mg) by 6% and 32%, respectively.

Storage conditions

In a place inaccessible to children, at an ambient temperature of up to 30 ° C.
Shelf life - 36 months.

special instructions

Often reported on the development of rashes on the skin, usually noted during the first 2 months after the start of Lamictal therapy. Mostly, these rashes were slightly expressed and passed without any treatment, but occasionally there were severe cases that required the withdrawal of treatment and hospitalization of the patient (for example, Lyell and Stevens-Johnson syndromes).
The mild form of the rash, as a rule, is dose-independent and is a symptom of hypersensitivity, whereas the Lyell and Stevens-Johnson syndromes depend on the dose of the drug in 100% of cases. Therefore, to exceed the initial, as well as subsequent doses of lamotrigine is not recommended because of the risk of rash.
Lamictal has weak inhibitory properties with respect to dihydrofolate reductase, and therefore, with prolonged use, it can have an effect on folate metabolism. Nevertheless, even when taking lamotrigine for a long period, there were no serious abnormalities in hemoglobin concentration, average number of blood elements, serum folate content (12 months of therapy) or erythrocytes (5 years of therapy).
At extremely severe stage of kidney failure, glucuronide (lamotrigine metabolite) accumulation is possible, therefore, the appointment of Lamictal, in this case, should be done with extreme caution.
Patients taking another drug, which includes lamotrigine, should not start taking Lamictal without first consulting their physician.
In the case when the estimated daily dosage of Lamictal is 1-2 mg, it is allowed to be taken every other day at a dose of 2 mg, during the first 14 days. When the calculated dose of the drug does not exceed 1 mg, it is better not to take Lamictal.
Do not recommend the appointment of Lamictal as a mono drug in pediatric practice, in the case of initial treatment of patients with a primarily diagnosed disease. The use of Lamictal in monotherapy is best performed after achieving a stable anticonvulsant effect, achieved with the combined treatment of lamotrigine and other PEP, which is subsequently canceled.
It is possible that patients from 2 to 6 years of age will require the appointment of the highest recommended maintenance doses.
It should be remembered that patients taking PEP, including Lamictal, are in the zone of suicidal risk, therefore, it is necessary to constantly monitor their psychological state.

Children

It is possible to use Lamictal in children from 2 years, according to some indications related to epilepsy, in dosages according to the age and weight of the patient.
Lamictal is not prescribed for children (under 18 years) with bipolar disorders.

In pregnancy and lactation

According to studies, monotherapy Lamictal, conducted in pregnant women in the first trimester, did not reveal a general increase in the risk of congenital pathology, although some sources confirm an increase in the incidence of anomalies in the oral cavity. In this regard, the appointment of lamotrigine during pregnancy is possible only if the benefit of therapy is higher than the risk for the fetus.
Lamotrigine is found to varying degrees in the mother's milk, the total concentration of the drug in infants sometimes reaches the level of 50% of its content in the mother's body, which may entail the pharmacological effects of the drug. Thus, the benefits of breastfeeding and the possible risk of side effects in the baby should be carefully compared.

Reviews about Lamictal

Reviews about Lamictal are very diverse and do not bear an unambiguous positive or negative answer about the effectiveness and safety of its application. The thing is that the diseases in which lamotrigine is used require individual selection of both the drugs themselves and their dosages.
Those people who approached this drug, speak of Lamictal as a fairly effective drug. Among the side effects, the rash on the skin covers most often, which in most cases disappears on its own.