Stabilizes voltazhzavisimye sodium tubule cell membranes and blocks the release of neurotransmitters, especially glutamate. As activating amino acid glutamate plays a key role in the occurrence of epileptic seizures.
Rapidly and completely absorbed in the intestine without being substantially primary metabolism in the liver. After 2.5 hours after ingestion reached maximum plasma concentration. Eating slows down the process of absorption, but does not affect its effectiveness. The pharmacokinetics of single dose not exceeding buy primobolan depot, is linear. The concentration in the saturation stage is pronounced individual character. The bioavailability of . Contact proteins is, it is unlikely that the displacement of lamotrigine due to proteins may cause toxic effects. The volume of distribution buy primobolan depot body weight.
Metabolism in the liver due glucuronyl transferase uridine-diphosphate. Among all the metabolites predominate N-glucuronides. The moderate, dose-dependent manner, Lamotrigine induces its own metabolism.
Excretion: average clearance in the saturation stage in healthy adults is 39 ± 14 ml / min. Displayed along with the urine in the form of glucuronide conjugate, less than 10% – unchanged buy primobolan depot. About 2% of active compound and degradation products are displayed, along with stool. The clearance half-life and do not depend on the dosage. t 1/2 = healthy volunteers 24-35 hours.
Provided with breast milk. Concentration in breast milk is 40-60% of the plasma concentration. In some cases, the drug concentration in the serum of infants whose mothers took the drug during lactation reaches therapeutic levels.
Children’s age: Clearance, recalculated per kg of body weight in children is higher than in adults, is highest under 5 years of age. The half-life is usually shorter than that of adults, while admission enziminduktora is 7 hours, and when taking sodium valproate – 45-60 hours.
Advanced age Ground clearance of lamotrigine young and elderly patients with epilepsy minimally different from each other.
Indications Epilepsy Adults and children over 12 years: as monotherapy or in combination with other antiepileptic drugs for the treatment of partial and generalized seizures, including tonic-clonic seizures and seizures with Lennox-Gastaut syndrome.
Children over 2 years: In combination with other antiepileptic drugs for the treatment of partial and generalized seizures, including tonic-clonic seizures and seizures with Lennox-Gastaut syndrome.
patients older than 18 years: prevention and treatment mainly episodes of depression.
: Hypersensitivity to any component of the drug
– Children under 2 years
Renal failure (due to the possible cumulation glucuronide metabolite). It should be used with caution in children lamotrigine as the drug of choice as monotherapy in the treatment of epilepsy.
Pregnancy and lactation:
Pregnancy: Due to the inhibitory effects of lamotrigine on dihydrofolate reductase, likely to develop malformations of the fetus in the case of the treatment of pregnant women, however, available data are insufficient to determine the degree of safety of lamotrigine for pregnant women. Receiving Lamotrigine is contraindicated during pregnancy except in cases where the expected benefit to pregnant exceeds the degree of potential risk to the fetus.
Lactation: The number of observations in the period of lactation is limited. Concentration in breast milk lamotrigine is 40-60% of the plasma concentration. A few observations show that the drug concentration in the serum of infants whose mothers took the drug during lactation reaches therapeutic levels. You should carefully weigh the benefits of breast-feeding while taking the drug and the risk of side effects in infants.
Dosage and administration Monotherapy Epilepsy Adults and children over 12 years: initial dose for 2 weeks 25 mg once daily; in the next 2 weeks – 50 mg once a day. Subsequently, every 1-2 weeks the daily dose can be increased to 50-100 mg until until the optimum effect is reached. Usually maintenance daily dose, distributed on one or two steps, is 100-200 mg. In rare cases, the desired effect is provided by doses of 500 mg / day.
Combination therapy Epilepsy
Adults and children over 12 years: patients taking sodium valproate in combination with other antiepileptic buy primobolan depot drugs or without them, the initial dose of lamotrigine in two weeks is 25 mg every other day; for the next two weeks of daily take one 25 mg once a day. Subsequently, every 1-2 weeks the dose may be increased to 25-50 mg until until it reaches an optimal effect. Regular maintenance daily dose is 100-200 mg in 1-2 reception.
Patients receiving antiepileptic drug being enziminduktorom (phenytoin, carbamazepine, phenobarbital, primidone)) in combination with other antiepileptic drugs, or without them, but not receiving sodium valproate, the initial daily dose of lamotrigine for two weeks is 50 mg once a day ; for the next two weeks at 100 mg per day, 2 Hour. Subsequently, every 1-2 weeks the dose can be increased by no more than 100 mg to obtain an optimal effect. Regular maintenance daily dose is 200-400 mg in 1-2 reception. In rare cases, a 700 mg / day.
In the case of treatment of antiepileptic drugs, a pharmacokinetic interaction with lamotrigine is not known, the dose of lamotrigine should be increased for smaller doses of the scheme described for taking sodium valproate.
Interaction with other medicines
Sodium valproate competitively blocks liver enzymes and inhibits the metabolism of lamotrigine, increasing almost twice its average t 1/2, extending it to 70 hours.
Antiepileptics Inductors of hepatic enzymes (phenytoin, carbamazepine, phenobarbital, primidone), paracetamol stimulate the metabolism of lamotrigine and shorten its TA 2 times, ie, to 14 hours (phenytoin, carbamazepine). Patients taking carbamazepine, lamotrigine administration may cause increased side reactions of the central nervous system: dizziness, ataxia, diplopia, blurred vision and nausea.Reducing the dose of carbamazepine usually leads to the disappearance of complaints.
No effect on the plasma concentrations of other antiepileptic drugs on ethinyl estradiol and levonorgestrel concentration after taking oral contraceptives.
Lamotrigine does not reduce the clearance of drugs, especially those that are excreted through CYP2D6. Clozapine, phenelzine, risperidone, trazodone sertalin and apparently did not affect the clearance of lamotrigine.
Data on the effect of lamotrigine on the pharmacokinetics of other antiepileptic drugs and drug interactions between him and drugs, depending on CYP450. no.
Compatible with sedative, anxiolytic and antiepileptic agents.
Evidence of inducing and inhibitory effects of lamotrigine on the enzymes of oxidation in the liver in clinically relevant amounts are not available. The ability of the drug to induce its own metabolism is low and probably has no clinical significance.
Do not assign Lamolep simultaneously with other containing lamotrigine, drugs.
If Lamolep provides good control of epilepsy, receiving other antiepileptic drugs can be stopped.
The objective criterion for the effectiveness of treatment is the ability to reduce the frequency of spikes in the EEG at 78-98%.
In the first 8 weeks of treatment may develop skin reactions. Skin rashes, usually are mild severity, disappear spontaneously, however, possible severe forms requiring hospitalization and discontinuation of lamotrigine eg, Stevens-Johnson syndrome and toxic epidermal necrolysis. High initial doses and accelerating the pace of increasing the dose prescribed lamotrigine, as well as the simultaneous reception of valproate contribute to the appearance of skin rash. To avoid the appearance of a skin rash should be strictly observe the specified dosage and rate of their increase.
Children are more likely to develop severe forms of skin reactions (incidence requiring hospitalization of children is 1: 300/1: 100).
Early symptoms of an allergic rash easily confused with an infectious rash, so if high fever and rash occur in the first 8 weeks of treatment, we must assume the development of drug reaction.
It is important to remember that early manifestations of hypersensitivity (eg, fever, lymphadenopathy) may occur without a rash. When a rash of each patient, regardless of age, should be buy primobolan depot immediately and thoroughly evaluated and lamotrigine stop treatment if symptoms develop can not be explained by another cause.
The appearance of the rash may be accompanied by a variety of systemic manifestations of hypersensitivity (fever, lymphadenopathy, facial edema, reactions on the part of the liver and hematopoietic system). The severity of hypersensitivity reactions may be different, and sometimes can be disseminated intravascular coagulopathy (CAAC) and the functional failure of multiple organs. It should be borne in mind that the early signs of hypersensitivity (eg, fever, lymphadenopathy) are not always accompanied by skin rash.
Abnormal liver function, generally, are part of the hypersensitivity syndrome, however, is not always accompanied by other symptoms of hypersensitivity.
Prolonged treatment lamotrigine can alter the metabolism of folic acid, as Lamotrigine is a weak inhibitor of dihydrofolate reductase. In this long, 12-month treatment lamotrigine does not significantly affect the level of hemoglobin, mean erythrocyte volume, folic acid concentrations in plasma and erythrocytes, after 5 years of treatment – the concentration of folic acid.
If lactose intolerance should be aware that Lamolepa 25 mg tablet contains 16.35 mg of lactose monohydrate, 50 mg tablet – 32.5 mg and 100 mg tablet – 65 mg.
Despite the fact that when taking oral contraceptives lamotrigine does not affect kontsetratsii ethinyl estradiol and levonorgestrel, changes during the menstrual cycle lamotrigine therapy taking oral contraceptives, requires close attention of the attending physician.
When treating patients with renal failure on hemodialysis, should be in the form of, on average, during a 4-hour hemodialysis of the body is derived 20% of lamotrigine.
Epilepsy: A sudden withdrawal of lamotrigine treatment provoke epileptic seizures, up to status epilepticus. Therefore, except in special cases (eg. The appearance of skin rash), requiring immediate treatment discontinuation, withdrawal of the drug should be carried out gradually, with a smooth, within 2 weeks, dose reduction.
Severe seizures and status epilepticus buy primobolan depot may lead to rhabdomyolysis, multiple organ dysfunction and disseminated intravascular coagulopathy, sometimes fatal. Similar cases have occurred in connection with the use of lamotrigine.