Lamictal pills 100 mg 30 pcs
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Active ingredients
Lamotrigine
Release form
Pills
Composition
Active ingredient: Lamotrigine (Lamotrigine) Active ingredient concentration (mg): 100
Pharmacological effect
Antiepileptic drug. Lamotrigine is a blocker of potential-dependent sodium channels. In the culture of neurons, it causes a potential-dependent blockade of continuously repeated impulses and suppresses the pathological release of glutamic acid (an amino acid that plays a key role in the development of epileptic seizures), and also inhibits glutamate-induced depolarization. Lamictal's effectiveness in preventing mood disorders in patients with bipolar disorders was demonstrated in two fundamental clinical studies. As a result of a combined analysis of the obtained results, it was found that the duration of remission, defined as the time until the first episode of depression occurred and before the first mania / hypomania / mixed episode after stabilization, was longer in the lamotrigine group compared to placebo. The duration of remission is more pronounced for depression.
Pharmacokinetics
AbsorptionAfter ingestion, lamotrigine is rapidly and completely absorbed from the gastrointestinal tract, practically not undergoing the first-pass metabolism of the system. Cmax in plasma is reached approximately 2.5 hours after taking the drug. The time to achieve Cmax increases slightly after a meal, but the degree of absorption remains unchanged. The pharmacokinetics of lamotrigine is linear when taking a single dose of up to 450 mg (the highest dose studied). Significant interindividual Cmax fluctuations are observed in the equilibrium state, however, with rare fluctuations in each individual person. DistributionLamotrigine is associated with plasma proteins by approximately 55%. It is unlikely that the release of the drug from the connection with the protein could lead to the development of a toxic effect. Vd is 0.92-1.22 l / kg. Metabolism The enzyme uridine diphosphate glucuronyltransferase (UDP-glucuronyltransferase) participates in the metabolism of lamotrigine. Lamotrigine slightly increases its own metabolism, depending on the dose.However, there is no evidence that lamotrigine affects the pharmacokinetics of other antiepileptic drugs and that there is an interaction between lamotrigine and other drugs metabolized by the cytochrome P450 system, on average, 39 ± 14 ml / min. Lamotrigine is metabolized to glucuronides, which are excreted by the kidneys. Less than 10% of the drug is excreted by the kidneys unchanged, about 2% through the intestines. Clearance and T1 / 2 do not depend on the dose. T1 / 2 in healthy adults averages from 24 hours to 35 hours. Patients with Gilbert's syndrome showed a 32% reduction in drug clearance compared with the control group, which, however, did not go beyond the limits of normal values for the general population. T1 / 2 lamotrigine is greatly influenced by co-medications. The average T1 / 2 is reduced to approximately 14 hours while taking it with drugs that stimulate glucuronization, such as carbamazepine and phenytoin, and increases to an average of 70 hours when taken together with valproatom. Pharmacokinetics in special clinical cases of children have lamotrigine clearance when calculating body weight higher than in adults; it is highest in children under 5 years old. In children, T1 / 2 lamotrigine is usually less than in adults. Its average value is approximately 7 hours while taking it with drugs that stimulate glucuronization, such as carbamazepine and phenytoin, and increases to 45-50 hours on average when taken together with valproat. The clinically significant differences in the clearance of lamotrigine in elderly patients compared to young patients were not detected. In case of kidney dysfunction, the initial dose of lamotrigine is calculated in accordance with the standard regimen of antiepileptic drug administration. Dose reduction may be required only with a significant reduction in renal function. Initial, increasing and maintenance doses should be reduced by approximately 50% in patients with moderate hepatic insufficiency (class B on the Child-Pugh scale) and 75% in patients with severe liver failure (class C on the Child-Pugh scale). Increasing the dose and maintenance dose should be adjusted depending on the clinical effect.
Indications
Children from 3 to 12 years old. Epilepsy (partial and generalized seizures, including tonic-clinical seizures, as well as seizures in Lennox-Gastaut syndrome) as part of combination therapy. canceled, and lamotrigine was continued in mototherapy. Monotherapy of typical absences. Adults and children (over 12 years). Epilepsy (partial and generalized seizures, including tonic-clinical seizures, and seizure with Lennox-Gastaut syndrome) in a combination therapy or mototerapii.Bipolyarnoe .Vzroslye affective disorder (18 years and older) Prevention of mood disorders (depression, mania, hypomania, mixed episodes) in patients with bipolar disorder.
Contraindications
Hypersensitivity. With caution should be prescribed for renal failure.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Fertility Studies on the reproductive function of animals in the application of lamotrigine did not reveal any impairment of fertility. Studies on the effect of lamotrigine on human fertility have not been carried out. Pregnancy The risk associated with AEDs in generalWomen who are able to bear children should be consulted with experts. If a woman plans pregnancy, the need for treatment of AEDs should be reviewed. In women who are undergoing treatment for epilepsy, the sudden cessation of anti-epileptic therapy should be avoided, since this can lead to renewed seizures, which can have serious consequences for the woman and the unborn child. In the offspring of mothers who received AED, the risk of congenital malformations increases by 2-3 times compared with the expected incidence of the population as a whole, which is about 3%. The most frequently recorded defects are cleft lip, heart and vascular defects, defects of neural tube repair. Multiple PEP therapy is associated with a higher risk of congenital malformations than monotherapy, in this regard, monotherapy should be used whenever possible. Risk associated with lamotrigina therapy impaired development of the embryo and fetus due to reduced levels of folic acid.Consideration should be given to taking folic acid during pregnancy planning and early pregnancy. Data from post-registration observation from several prospective pregnancy registries made it possible to document the outcomes of pregnancies of about 8,700 women who received Lamictal monotherapy during the first trimester of pregnancy. In general, the data obtained do not confirm a general increase in the risk of congenital malformations. Although out of a limited number of pregnancy registers there are reports of an increased risk of developing malformations of the oral cavity, a completed case-control study did not reveal an increase in the risk of developing malformations of the oral cavity compared with other serious developmental defects arising after the use of lamotrigine. combination therapy is not enough to assess whether the risk of malformations is associated with other drugs used in combination with dzhinom.T.k. and other drugs, Lamictal should be prescribed during pregnancy only if the expected therapeutic benefit exceeds the potential risk. Physiological changes during pregnancy can affect the concentration of lamotrigine and / or its therapeutic effect. There are reports of a decrease in the concentration of lamotrigine in the blood during pregnancy. The purpose of Lamictal should be provided to pregnant women with appropriate management tactics. Breastfeeding periodLamotrigine penetrates to breast milk to varying degrees, the total concentration of lamotrigine in breastfed babies can reach approximately 50% of the concentration of lamotrigine registered in the mother. Thus, in some breastfed babies, serum concentrations of lamotrigine can reach levels at which pharmacological effects occur. It is necessary to correlate the potential benefits of breastfeeding with the potential risk of developing unwanted reactions in a child. If a woman taking the drug Lamictal decides to breastfeed, then the child should be monitored for the occurrence of any adverse reactions.
Dosage and administration
If the calculated dose of Lamictal (for example, when prescribing to children — only for epilepsy; or for patients with impaired liver function) cannot be divided into a whole number of lower dosage pills, then the patient should be assigned such a dose that corresponds to the nearest value of the whole tablet in lower dosage. In case of resuming the use of Lamictal, doctors should evaluate the need to increase the maintenance dose in patients who have stopped taking the drug for any reason, since have high initial doses and exceeding the recommended doses are associated with a risk of severe rash. The more time has passed since the last dose of the drug, the more caution should be increased dose to support. If the time after stopping the administration exceeds 5 half-life, then the dose of lamotrigine should be increased to maintain according to the appropriate regimen. Lamotrigine therapy should not be resumed in patients whose cessation of treatment was associated with a rash, unless the potential benefits of such therapy obviously exceed the possible risks.
Side effects
On the part of the skin and subcutaneous tissue: often - a skin rash, mainly of a maculopapular nature; rarely, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). Skin rash usually appears during the first 8 weeks after the start of lamotrigine and disappears when it is canceled. In rare cases, it can develop severe skin reactions, which in most cases disappear after drug withdrawal (some patients may have scars), as well as potentially life-threatening conditions such as Stevens-Johnson syndrome and Layel syndrome. lymphatic and lymphatic systems: rarely - neutropenia, leukopenia, anemia, thrombocytopenia, pancytopenia, aplastic anemia, agranulocytosis. Hematological disorders may or may not be associated with hypersensitivity syndrome and the syndrome of DVS. manifestations such as fever, lymphadenopathy, swelling of the face, hematological disorders, liver damage, DIC syndrome, multiple organ failure. Early signs of hypersensitivity (for example, fever and lymph denopatiya) may appear even in the absence of skin rash.In such a case, the patient should immediately inspect and stop taking lamotrigine if there is no other obvious reason for the onset of these symptoms. : often - irritability, anxiety, headache, fatigue, drowsiness, insomnia, dizziness, imbalance, tremor, nystagmus, ataxia. Sometimes - aggressiveness. Rarely - tics, hallucinations, confusion, agitation, imbalance, movement disorders, extrapyramidal disorders, choreoathetosis, increased seizure seizures. including nausea, vomiting, and diarrhea; seldom - increase in liver function tests, abnormal liver function, liver failure. From the musculoskeletal system: often - arthralgia, back pain; rarely, lupus-like syndrome.
Overdose
It was reported about a single dose, exceeding the maximum therapeutic 10-20 times. Overdose was manifested by the following symptoms: nystagmus, ataxia, impaired consciousness, and coma. Treatment: hospitalization and maintenance therapy is recommended in accordance with the clinical picture or recommendations of the National Toxicological Center.
Interaction with other drugs
UDP-glucuronyltransferase is the main enzyme that metabolizes lamotrigine. There is no evidence of the ability of lamotrigine to cause a clinically significant induction or inhibition of microsomal liver enzymes. In this regard, the interaction between lamotrigine and drugs metabolized by cytochrome P450 isoenzymes is unlikely. Lamotrigine can induce its own metabolism, but this effect is mild and has no clinical significance.
special instructions
Skin rash There are data on the development of skin rashes, which were usually observed during the first 8 weeks after the start of treatment with Lamictal.In most cases, skin rashes are mild and pass on their own, but at the same time there have been serious cases requiring the patient to be hospitalized and Lamictal canceled (for example, Stevens-Johnson syndrome and Lyell's syndrome). Severe skin reactions in adults taking Lamictal in accordance with generally accepted recommendations, develop with a frequency of about 1 in 500 patients with epilepsy. In about half of these cases, Stevens-Johnson syndrome (1 in 1000) was recorded. In patients with bipolar disorders, the incidence of severe skin rashes according to clinical studies is approximately 1 per 1000 patients. In children, the risk of developing severe skin rashes is higher than in adults. According to available data, the frequency of skin eruptions that required hospitalization in children with epilepsy ranged from 1 to 300 to 1 per 100 children. In children, the initial manifestations of the rash can be mistaken for an infection, so you should consider the possibility of children's reactions to the drug, manifested by the development of rash and fever in the first 8 weeks of therapy. In addition, the overall risk of developing rash is largely associated with a high initial dose of Lamictal and an excess of the recommended rate of increase, as well as with combined use Patients with a history of allergic reactions or a rash in response to other antiepileptic drugs, since the incidence of rash (not classified as serious) in patients with this history was 3 times more common with lamotrigine, than in patients with an uncomplicated history. When a rash is detected, all patients (adults and children) should be immediately examined by a doctor. Reception of a lamotrigine has to be immediately stopped except for those cases when it is obvious that development of rash is not connected with administration of drug. It is not recommended to resume taking lamotrigine in cases where its previous purpose was canceled due to the development of a skin reaction, unless the expected therapeutic effect of the drug use does not exceed the risk of side effects. It was reported that the rash may be part of the hypersensitivity syndrome associated with various systemic manifestations , including fever, lymphadenopathy, swelling of the face and abnormalities in the blood and liver.The severity of the syndrome varies over a wide range and in rare cases can lead to the development of DIC and multiple organ failure. It should be noted that early manifestations of hypersensitivity syndrome (ie, fever, lymphadenopathy) can be observed, even if there are no obvious manifestations of a rash. With the development of such symptoms, the patient should be immediately examined by a doctor and, if no other cause of symptoms is identified, lamotrigine should be canceled. Septic meningitis The development of aseptic meningitis is reversible when the drug is discontinued in most cases and resumes in some cases with repeated administration. Reappointment results in the rapid return of symptoms, which are often more severe. Lamotrigine is not prescribed repeatedly to patients in whom discontinuation of treatment was associated with aseptic meningitis. Hormonal contraceptives1. The effect of hormonal contraceptives on lamotrigine pharmacokinetics. It was shown that the combined drug ethinyl estradiol / levonorgestrel (30 µg / 150 µg) approximately 2 times increases the clearance of lamotrigine, which leads to a decrease in its plasma level. In order to achieve its maximum therapeutic effect, it is necessary to increase the maintenance doses of lamotrigine, but not more than 2 times. In women who are no longer taking lamotrigine glucuronidation inducers and taking hormonal contraceptives, whose treatment regimen includes a week of taking an inactive drug (or a week-long break in taking a contraceptive), a transient increase in lamotrigine will be observed during this period of time. The increase in concentration will be more pronounced if the next increase in the dose of lamotrigine is carried out immediately before or during the period of inactive drug use. Health care workers need to master the clinical management skills of women who start or stop taking hormonal contraceptives during lamotrigine treatment, as this may require correction of the dose of lamotrigine . Other oral contraceptives and hormone replacement therapy have not been studied, although they may in a similar manner affect s on the pharmacokinetic parameters lamotridzhina.2.The effect of lamotrigine on the pharmacokinetics of hormonal contraceptives The joint administration of lamotrigine and the combined hormonal contraceptive (ethinyl estradiol / levonorgestrel) leads to a moderate increase in the clearance of levonorgestrel and changes in the concentration of FSH and LH. The effect of these changes on the ovulatory activity of the ovaries is unknown. However, we cannot exclude the possibility that in some patients taking lamotrigine and hormonal contraceptives, these changes may cause a decrease in the effectiveness of contraceptives. Patients should be informed of the need to immediately inform the doctor about changes in the nature of the menstrual cycle, i.e. about sudden bleeding. Dihydrofolate reductase Lamotrigine is a weak inhibitor of dihydrofolate reductase, and therefore the drug during prolonged therapy can affect folate metabolism. However, it was shown that even with long-term use lamotrigine did not cause serious changes in hemoglobin content, average red blood cell volume, folate concentration in serum (when taken for up to 1 year) or red blood cells (when taken for up to 5 years). The effect of lamotrigine on the cationic carrier organic substratesLamotrigine is an inhibitor of tubular secretion by influencing the cationic carrier of proteins. This may lead to an increase in plasma concentrations of certain drugs, which are mainly excreted through the kidneys. Co-administration of lamotrigine and substrates with a narrow therapeutic range, such as dofetilide, is not recommended. Renal failure The single administration of lamotrigine in patients with severe renal insufficiency did not reveal significant changes in the concentration of lamotrigine. However, accumulation of the glucuronide metabolite is very likely, so care must be taken when treating patients with renal insufficiency. Patients taking other drugs containing lamotrigine If a patient is receiving any other drug containing lamotrigine, he should not take Lamictal without consulting a doctor. Epilepsy like other AEDs, it can trigger seizures.If abrupt discontinuation of therapy is not a safety requirement (for example, when a rash appears), the dose of lamotrigine should be reduced gradually over 2 weeks. There are reports in the literature that severe convulsive seizures, including status epilepticus, can lead to the development of rhabdomyolysis, multiorgan disorders and disseminated inside the vascular coagulation, sometimes with fatal outcome. Similar cases have been observed in the treatment of patients with lamotrigine. Suicidal risk The symptoms of depression and / or bipolar disorder may be observed in patients with epilepsy. Patients with epilepsy and concomitant bipolar disorder are at high risk of suicide. 25-50% of patients with bipolar disorder had at least one suicidal attempt; in such patients, there may be a worsening of suicidal thoughts and suicidal behavior (suicidality) in patients receiving drugs for the treatment of bipolar disorder, including lamotrigine, as well as without treatment. Suicidal thoughts and suicidal behavior were observed in patients taking PEP for several reasons, including epilepsy bipolar disorder. A meta-analysis of randomized, placebo-controlled AED studies (including lamotrigine) showed a slight increase in suicidal risk. The mechanism of this action is unknown, and the available data do not exclude the possibility of an increased risk of suicide when using lamotrigine. Therefore, patients should be carefully monitored for suicidal thoughts and behaviors. Patients and caregivers should be informed about the need for medical advice when such symptoms occur. Bipolar affective disorder Children and adolescents under 18 years old. Treatment with antidepressants is associated with an increased risk of suicidal thoughts and behavior in children and adolescents with major depression and other mental disorders. Clinical deterioration Patients with bipolar affective disorder Patients with bipolar disorder receiving lamotrigine must be monitored carefully. orient symptoms of clinical deterioration (including the emergence of new symptoms) and suicidality, especially at the beginning of the course of treatment and at the time of dose change.Patients who have a history of suicidal thoughts or suicidal behavior, young patients and patients who have experienced a significant degree of suicidal thoughts before starting therapy are at high risk of suicidal thoughts or suicidal behavior, such patients should be under strict observation during treatment. Patients (and caregivers) should be warned to monitor any deterioration in the patient’s condition ( including the emergence of new symptoms) and / or the appearance of suicidal thoughts / behavior or thoughts about hurting yourself and should seek medical help immediately if these symptoms are present. At the same time, the situation should be assessed and appropriate changes should be made to the therapy regimen, including the possibility of drug withdrawal patients who have clinical deterioration (including the emergence of new symptoms) and / or the emergence of suicidal thoughts / behavior, especially if these symptoms are severe, with a sudden onset and not previously observed. Data on the ability to drive vehicles and control mechanisms Two studies conducted with healthy volunteers showed that the effect of lamotrigine on accurate visual-motor coordination, eye movements and the subjective sedative effect did not differ from the placebo effect. There are reports of side effects of lamotrigine of a neurological nature, such as dizziness and diplopia. Therefore, before you get behind the wheel of a car or control the mechanisms, patients should assess the effect of lamotrigine on their condition. the effect of all antiepileptic drugs has individual variability, then patients should consult with their doctor about the possibility of driving a car.