Lamictal pills 25 mg 30 pcs
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Active ingredients
Lamotrigine
Release form
Pills
Composition
Active ingredient: Lamotrigine Concentration of the active substance (mg): 25 mg
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
Absorption After ingestion, lamotrigine is rapidly and completely absorbed from the gastrointestinal tract, practically without being subjected to a first-pass first-pass metabolism. 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 situations 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 glucuronidation, such as carbamazepine and phenytoin, and increases to 45-50 hours on average when taken together with valproat. 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
Dermatophyte infections of the skin caused by Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum canis, and Epidermophyton floccosum: ringworm, smooth skin, inguinal athlete, athlete’s hand and foot infections, Skin candidi, Surgical loosening, Seborrheic dermatitis, hand and foot athlete's swelling, Sphorrhea dermatitis, Sphorrhoea, Scytherophytosis of the hands and feet, Skin candidiasis, Ophthalmic fungal infections
Contraindications
Lamictal is not used in persons with excessive sensitivity to the components of its formula.
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, and therefore, monotherapy should be used whenever possible. Risk associated with lamotrigina therapy Lamotrigine has a slight inhibitory effect on dihydrofolic acid reductase and therefore, in theory, may lead to an increased risk 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
Taking Lamictal pills: pills do not need to be chewed before swallowing. Lamictal soluble pills require a small amount of water sufficient to cover their surface. You can also drink them with moderate amounts of liquid.In cases of dose adjustment in patients under 12 years of age or with impaired excretory function, when the prescribed dosage does not coincide with the amount of the active ingredient of the whole tablet, the minimum effective fraction of the drug is taken. Monotherapy of epilepsy with Lamictal in adults and adolescents is carried out as follows: in the first two weeks of administration, 25 mg once a day, the next two weeks of the course — 50 mg of Lamictal with the same dose rate, then the dose is titrated until the maximum clinically significant effect is achieved. Maintenance therapy is carried out in a dose of 100-200 mg of the drug per day, and in some patients it can reach 0.5 g. Simultaneous administration of sodium valproate and Lamictal in epileptic syndrome requires some reduction in the dosage of the latter. In the first two weeks, 25 mg of the drug is prescribed every other day, then daily in the same daily dose for another two weeks. Then the daily dosage of Lamictal increases by 25–50 mg before symptoms regress. The stabilizing dose is 100–200 mg per day. This amount of the drug is divided into two doses. Multicomponent therapy for epiphriscups, which, in addition to Lamictal, include means activating hepatic enzymes, provides for a daily dose of 50 mg of Lamictal in the first two weeks. In the next half a month, the daily amount of the drug is doubled. A month after starting therapy, the daily dose of Lamictal reaches 100 mg in two doses. To maintain the therapeutic effect, use 200-400 mg of the drug per day. The initial dose of Lamictal in children 2–12 years of age with the treatment with sodium valproate and other anticonvulsants is 0.15 mg / kg per day. This amount of the drug is taken for two weeks. The next two weeks, children are prescribed at 0.3 mg / kg per day. The dose of Lamictal is increased by 0.3 mg / kg daily until regression of the disease is achieved. In this case, maintenance dosages reach 1–1.5 mg / kg / day when taken twice. In this group of patients, the maximum daily dose does not exceed 200 mg. Joint administration of Lamictal and other anticonvulsants, including those activating hepatic enzymes, in children 2–12 years of age suggests an initial dose of 0.6 mg / kg / day for 2 weeks. 1.2 mg / kg / day take another two weeks.Then the dose is titrated to achieve a lasting effect. Combined therapy of bipolar disorders of Lamictal and hepatic enzyme-inhibiting anticonvulsants in adults and adolescents begins with 25 mg of Lamictal at intervals of two days a day. The next two weeks of the course, patients take the same amount of the drug daily. The stabilizing dose of Lamictal in this case is 100 mg. It should not exceed the maximum - 200 mg / day. Simultaneous administration of Lamictal with drugs that activate hepatic enzymes provides for a twofold increase in dosage compared with multi-component therapy with inhibitors of hepatic proteases. In the case of the unknown nature of the interaction of Lamictal with other prescribed anticonvulsants, the treatment regimen is similar to that of monotherapy. Belonging to the older age group does not require additional dose adjustment.
Side effects
From the side of the central nervous system: ataxia (from ≥0. 1 to less than 1%); cases of cognitive impairment with a progressive onset (giving a complete picture of dementia syndrome), reversible within a few weeks or months after discontinuation of the drug (≤ 0. 01%). Confusion or convulsions: in several cases of treatment with valproatom, stupor or lethargy is described, sometimes resulting in transient coma (encephalopathy); these cases were isolated or associated with a paradoxical increase in the frequency of convulsions during therapy, their frequency decreased when the treatment process was suspended or the dose was reduced. Most often, such cases are described with complex treatment (especially with phenobarbital) or after a sharp increase in the dose of valproate. Isolated cases of reversible parkinsonism. Headache, mild postural tremor and drowsiness. On the part of the digestive system: some patients at the beginning of treatment often develop gastrointestinal disorders (nausea, vomiting, gastralgia, diarrhea), but they usually disappear without discontinuation of drug therapy within a few days. Cases of pancreatitis, sometimes fatal (less than 0. 01%), requiring early cessation of treatment. Liver dysfunction (from ≥0. 01 to less than 0. 1%). From the hemopoietic system: frequently occurring dose-dependent thrombocytopenia; oppression of bone marrow hematopoiesis (from ≥ 0. 01% to less than 0. 1%), including anemia, leukopenia or pancytopenia. From the urinary system: enuresis (less than 0. 01%); isolated cases of reversible Fanconi syndrome (genesis is not clear).Allergic reactions: skin rash, urticaria, vasculitis; in some cases (less than 0. 01%) toxic epidermal necrolysis, Stevens-Johnson syndrome, and erythema multiforme were described. On the part of laboratory parameters: isolated and moderate hyperaemonemia often occurs without changes in the analysis of liver functions, especially with polytherapy (discontinuation of the drug is not required in this case); however, hyperammonemia associated with neurological symptoms is also described (this condition requires further examination); possible increase in liver transaminase activity; individual cases of a decrease in fibrinogen level or an increase in bleeding time are described, usually without associated clinical manifestations and especially when used in high doses (sodium valproate has an inhibitory effect on the second stage of platelet aggregation); hyponatremia (less than 0. 01%). Other: teratogenic risk, hair loss; rare reports of hearing loss (from ≥ 0. 01 to less than 0. 1%) both reversible and irreversible; very rare cases of mild peripheral edema (less than 0. 01%), weight gain, since this is a risk factor for polycystic ovarian syndrome, careful monitoring of such patients is recommended. There are also reports of gynecomastia, amenorrhea, a violation of the regularity of the menstrual cycle.
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
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. The effect of other drugs on lamotrigine glucuronization. Powerful inhibitors of lamotrigine glucuronization. Powerful inductors of lamotrigine glucuronization.little effect on gglyukuronizatsii lamotridzhinavalproevaya acid karbamazepinfenitoinprimidonfenobarbitalrifampitsinlopinavir / ritonaviratazanavir / ritonavirkombinirovanny medication ethinyl estradiol / levonorgestrel preparations litiyabupropionolanzapinokskarbazepinfelbamatgabapentinlevetiratsetampregabalintopiramatzonizamidaripiprazolVliyanie other oral contraceptives and hormone replacement therapy has not been studied, though they may have a similar effect on the pharmacokinetic parameters lamotridzhina.Vzaimode PEPValproic acid, which inhibits lamotrigine glucuronization, reduces its metabolic rate and extends its average T1 / 2 almost 2 times. and its metabolism. It was reported on the development of adverse events on the part of the central nervous system, including dizziness, ataxia, diplopia, blurred vision and nausea in patients who began taking carbamazepine during lamotrigine therapy. These symptoms usually subsided after lowering the dose of carbamazepine. A similar effect was observed when lamotrigine and oxcarbazepine were taken by healthy volunteers, the result of the dose reduction was not studied. When lamotrigine 200 mg and oxcarbazepine 200 mg are administered simultaneously, neither oxcarbazepine nor lamotrigine disrupt each other’s metabolism. times / day and lamotrigine 100 mg 2 times / day did not lead to clinically significant changes in the pharmacokinetics of lamotrigine. When combined with lamotrigine and gabapentin, the visible clearance of lamotrigine did not change. In Possible drug interactions of levetiracetam and lamotrigine were investigated in assessing the serum concentrations of both drugs in placebo-controlled clinical trials. These data show that lamotrigine and levetiracetam do not affect each other's pharmacokinetics. There was no effect of pregabalin at a dose of 200 mg 3 times / day on equilibrium concentrations of lamotrigine, i.e. pregabalin and lamotrigine do not interact pharmacokinetically with each other. The use of topiramate did not lead to a change in the concentration of lamotrigine in the plasma.However, taking lamotrigine increased the concentration of topiramate by 15%. Taking zonisamide (at a dose of 200-400 mg / day) during the clinical program together with lamotrigine (at a dose of 150-500 mg / day) did not lead to a change in pharmacokinetic parameters of lamotrigine. Studies showed that lamotrigine does not affect plasma concentrations of other antiepileptic drugs. Results of in vitro studies have shown that lamotrigine does not force other antiepileptic drugs out of association with plasma proteins. When used with other psychotropic drugs Lamotrigine at a dose of 100 mg / day does not cause a violation of the pharmacokinetics of anhydrous lithium gluconate (2 g 2 times / day for 6 days) when administered together. Repeated administration of bupropion orally does not have a statistically significant effect on the pharmacokinetics of a single dose Lamotrigine and causes a slight increase in AUC of lamotrigine glucuronide. Olanzapine in a dose of 15 mg reduces the AUC and Cmax of lamotrigine on average by 24% and 20%, respectively, which is clinically insignificant. Lamotrigine at a dose of 200 mg does not alter the pharmacokinetics of olanzapine. Repeated intake of lamotrigine at a dose of 400 mg / day did not have a clinically significant effect on the pharmacokinetics of risperidone after a single dose of 2 mg by healthy volunteers. At the same time, drowsiness was noted: in 12 of 14 patients with combined intake of lamotrigine and risperidone; in 1 out of 20 patients with risperidone alone; none of the patients taking lamotrigine. Inhibition of the action of lamotrigine by amitriptyline, bupropion, clonazepam, fluoxetine, haloperidol or lorazepam has a minimal effect on the formation of the 2-N-glucuronide primary metabolite. Investigation of the metabolism of buroralol by microsomaltoraltomaltomaltomaltomaltomaltomalolumine 2-N-glucuronide metabolism. Investigation of the metabolism of buroralol by microsomaltomaltomaltomaltomaltomalolumine 2-N-glucuronide metabolism. the conclusion that lamotrigine does not reduce the clearance of drugs that are metabolized predominantly by CYP2D6 isoenzymes. In vitro studies also suggest that clozapine, phenelzine, risperidone, sertraline, or trazodone are unlikely to affect lamotrigine clearance. Interaction with hormonal contraceptives1. The effect of hormonal contraceptives on lamotrigine pharmacokinetics. Taking combined oral contraceptives containing 30 mcg of ethinyl estradiol and 150 mcg of levonorgestrel causes a twofold increase in lamotrigine clearance (after ingestion), which leads to a decrease in AUC and Cmax of lamotrigine by an average of 52% and 39%, respectively.During the week free from taking the active drug, an increase in the plasma concentration of lamotrigine is observed, while the concentration of lamotrigine, measured at the end of this week before the next dose, is on average 2 times higher than during the period of active therapy.2. The effect of lamotrigine on the pharmacokinetics of hormonal contraceptives. During equilibrium concentrations of lamotrigine at a dose of 300 mg, it does not affect the pharmacokinetics of ethinyl estradiol, a component of the combined oral contraceptive. There is a slight increase in clearance of the second component of the oral contraceptive, levonorgestrel, which leads to a decrease in the AUC and Cmax of levonorgestrel by 19% and 12%, respectively. Measurement of serum levels of FSH, LH and estradiol during this study revealed a slight decrease in the suppression of the hormonal activity of the ovaries in some women, although the measurement of the plasma level of progesterone did not reveal any hormonal evidence of ovulation in 16 women. The effect of a moderate increase in the clearance of levonorgestrel and changes in plasma concentrations of FSH and LH on the ovulation activity of the ovaries has not been established. The effect of other doses of lamotrigine (except 300 mg / day) has not been studied and studies with the inclusion of other hormonal drugs have not been conducted. Interaction with other drugsRifampicin increases the clearance of lamotrigine and reduces its T1 / 2 due to the induction of liver microsomal enzymes responsible for glucuronization. In patients taking rifampicin as concomitant therapy, the regimen of lamotrigine should follow the regimen recommended for co-administration of lamotrigine and drugs that induce glucuronization. When using lopinavir / ritonavir, a decrease in plasma concentration of lamotrigine was observed, possibly due to the induction of glucuronization. In patients taking concomitant treatment with lopinavir / ritonavir, a lamotrigine dosing regimen with concomitant glucuronization inducers should be recommended. In a study of healthy volunteers, atazanavir / ritonavir (300 mg / 100 mg) resulted in a decrease in lamotrigine AUC and Cmax (100 mg in a single dose) ) by about 32% and 6%, respectively. The results of in vitro studies have shown that it is lamotrigine that is an inhibitor of cationic carriers of organic substrates in potentially clinically significant concentrations.These data show that lamotrigine is a more potent inhibitor (half of the inhibitory concentration (IC50) varies from 53.8 nmol / l to 186 nmol / l, respectively) than cimetidine. Interaction, including laboratory indicators Lamotrigine, is reported to affect the performance of some rapid methods urinalysis to identify prohibited drugs that can lead to false-positive results, especially in the detection of phencyclidine (dissociative anesthetic). To confirm a positive result, a more specific alternative chemical method should be used.
special instructions
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, and therefore, monotherapy should be used whenever possible. Risk associated with lamotrigina therapy Lamotrigine has a slight inhibitory effect on dihydrofolic acid reductase and therefore, in theory, may lead to an increased risk 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.