Latrigine

Lathridge is an anticonvulsant drug.

Indications of the lathridge

It is used for the treatment of epilepsy in adolescents from 12 years and adults - as monotherapy or as an additional agent (for example, in general or partial attacks, including tonic-clonic type seizures and seizures caused by SLH).

It is also used to treat bipolar disorders in adults - to prevent the development of stages of emotional disorders in such people (usually those are episodes of depression).

[1]

Release form

The release takes place in a tablet form, 10 pieces inside a blister cell. In a separate package - 3 blister plates.

Pharmacodynamics

The drug blocks the activity of potential-dependent Na channels within presynaptic neuronal membranes during the slow inactivation stage. In addition, it slows the release of excess neurotransmitters (mainly from 2-aminopentanedioic acid - an excitatory amino acid, which is an important participant in the formation of epileptic seizures).

[2], [3], [4],

Pharmacokinetics

After oral administration, the drug is completely and very quickly absorbed inside the digestive tract. Peak plasma values of the substance are observed after 2.5 hours. The period of achievement of this indicator may be prolonged with the use of the drug with food (the degree of absorption remains the same).

Hepatic metabolism occurs with the participation of the enzyme glucuronyltransferase, during which an element of N-glucuronide is formed. The half-life is 29 hours.

[5], [6], [7]

Dosing and administration

Take orally, without regard to eating. The tablets are swallowed without chewing.

When appointing a component that does not correspond to the indices of the active ingredient in the dosage table, it is required to reduce the dose to 0.5 tablets or the whole.

Re-start the therapeutic course.

When appointing a repeat course to people who have stopped therapy, it is necessary to clearly identify the need to increase the maintenance dose, because there is a possibility of a rash due to a high initial dosage and non-compliance with the recommended scheme of increasing portions. The greater the interval between the time of consumption of the previous dose, the more carefully it is necessary to follow the regime of increasing the dose to the supporting values. After exceeding the half-life half an interval after the end of the LS application, it is possible to increase the dosage of lamotrigine to the maintenance level, taking into account the data recommended by the scheme of application.

It is forbidden to begin a second course if the therapy was canceled because of the rash as a result of previous treatment with lamotrigine. In such a situation, before making a decision to reuse the drug, it is necessary to correlate the likely benefits of its use and the expected risk.

With epilepsy, adolescents from 12 years and adults.

Monotherapy.

The size of the initial portion of the drug is equal to a one-time intake of 25 mg per day for 14 days. During the next 14 days, 50 mg / day is used, and then the dose can be increased every 1-2 weeks by 50-100 mg, until the optimal result is obtained. The standard maintenance dose is 100-200 mg / day (it is consumed in 1-2 doses). There are also patients who need to take 0.5 grams of drugs per day.

Combined treatment.

Individuals taking valproate (as a monotherapy, or together with other anticonvulsants), it is required to take 25 mg of the drug every other day during the 14 days, and during the next 14 days to take the same dose, but every day. Then, the dosage is increased every 1-2 weeks (no more than 25-50 mg / day) until the optimal medication is obtained. The size of the standard maintenance dose is 100-200 mg / day (consumed 1-2 methods).

People taking other anticonvulsants or other drugs (inducers of liver enzymes) with or without other anticonvulsant drugs (except sodium valproate), the size of the initial dose of Latrigine is a single dose of 50 mg / day for a period of 14 days. Next, use 100 mg per day in 2 doses per day (for 2 weeks). Later, the portion is increased every 1-2 weeks (a maximum of 0.1 g) until the required drug exposure is obtained. In general, the maintenance dose is 0.2-0.4 g / day, which is consumed in 2 doses. Some patients may need to take 700 mg per day.

People using other drugs that induce or depress liver enzymes weakly need to take 25 mg once a day (for 2 weeks) and then 50 mg per day (also during 14 days) once a day. In the future, the dosage is increased at intervals of 1-2 weeks (no more than 0.05-0.1 g / day) until the desired drug effect is obtained. Often, the size of the maintenance dose is 0.1-0.2 g / day (consumed by 1-2 techniques).

Those who use anticonvulsants with an unexplained interaction with Latrigine are required to use the same regimen used during the combination of lamotrigine and valproate.

For adults with bipolar disorder.

The following transition mode should be observed when using. This includes a scheme for increasing the dosage until the stabilizing dose is reached (for 6 weeks), and then stopping the use of other psychotropic or anticonvulsant drugs (in the presence of drug necessity).

It is also necessary to consider the need for additional treatment that will prevent the development of manic episodes, because there is no accurate data on the effective use of drugs to treat manic syndrome.

Scheme of increasing the dosage to a stabilizing maintenance dose (per day) in adults with bipolar disorders:

• an additional course with the use of drugs-inhibitors of liver enzymes (among those valproate): 1-14 days - taking a day through 25 mg of LS; 15-28 days - daily intake of 25 mg per day; 29-35 days - 50 mg / day in 1-2 additions; 36-42 days - the stabilization dose is 0.1 g / day (in 1-2 doses). A day is allowed to take no more than 0.2 g;
• an additional course with the use of inducers of liver enzymes to people who do not take inhibitors (carbamazepine, primidon, phenytoin, phenobarbital or other inductor): 1-14 days - 1-time intake per day 50 mg; 15-28 days - taking 0.1 g per day (in 2 applications); 29-35 days - consumption of 0.2 g per day (2 methods); 36-42 days - the stabilization dose is 0.3 g / day (2 methods). It is allowed to increase to 0.4 g / day at week 7;
• monotherapy with lamotrigine or additional use in persons using other medicines that do not have clinically significant inhibition / induction for liver enzymes: 1-14 days - 1-fold intake of 25 mg per day; 15-28 days - 50 mg per day (1-2 methods); 29-35 days - intake in 1-2 administration of 100 mg per day; 36-42 days - a stabilizing dose - take 1-2 consumption of 200 mg per day (in the range of 100-400 mg).

After receiving the required maintenance stabilizing dose, the use of other psychotropic drugs can be stopped by the following schemes:

• with the further abolishment of the means that slow down the enzymes of the liver (valproate): during the first week, double the stabilization dose (but not exceed the limit of 0.1 g / week) - for example, from 0.1 g / day to 0.2 g / day; during the 8-21 days it is required to maintain a dosage of 0.2 g / day (divide by 2 uses);
• with a further discontinuation of taking inductor-enzymes of liver enzymes (taking into account the initial portion): there are 3 schemes:

1. the first 7 days - 0.4 g; the second 7 days - 0.3 g; from the 15th day - 0.2 g;
2. the first 7 days - 0.3 g; the second 7 days 225 mg; from the 15th day - 150 mg;
3. the first 7 days - 0.2 g; the second 7 days - 150 mg; from the 15th day - 0.1 g;

• with further cancellation of other drugs that do not have clinically significant induction / inhibition of liver enzymes: maintenance of the dosage, which was determined with an increase (200 mg / day), which is divided into 2 uses (within 100-400 mg).

People who use anticonvulsants, whose interaction with Latrigine has not been studied, it is necessary to comply with the regime in which the existing dosage of lamotrigine remains, and correct it, based on the clinical picture.

Correction of doses of lamotrigine to people with bipolar disorders with additional use of other drugs.

Schemes with additional intake of inhibitors of liver enzymes (valproate), taking into account the initial portion of lamotrigine:

1. stabilizing portion lamotrizhdina - 0.2 g / day; the first 7 days - 0.1 g; from the 8th day onwards, maintaining a dosage of 0.1 g / day;
2. stabilization - 0.3 g / day; the first 7 days - 150 mg; from the 8th day onwards - maintenance of admission 150 mg / day;
3. stabilization - 0,4 g / day; the first 7 days - 0.2 g; from the 8th day onwards and maintenance of a dose of 0.2 g / day.

Schemes with additional reception of inducers of liver enzymes to persons not using valproate, taking into account the initial portion:

1. stabilization - 0.2 g / day; 1-7 days - 200 mg; 8-14 days - 300 mg; from the 15th day - 400 mg;
2. stabilization - 150 mg / day; 1-7 days - 150 mg; 8-14 days - 225 mg; from the 15th day - 300 mg;
3. stabilization - 100 mg / day; 1-7 days - 100 mg; 8-14 days - 150 mg; from the 15th day - 200 mg.

Scheme with additional administration of drugs that do not have a significant inducing or inhibitory effect on liver enzymes: maintenance of the dosage that was obtained after applying the regimen increase mode - 200 mg / day (within 100-400 mg).

Women who use hormonal type contraceptives.

The beginning of lamotrigine therapy in women already using hormonal contraception.

While oral contraceptives increase the level of lamotrigine clearance, it is not necessary to change the mode of increasing the portion of medicines when combined only with contraception. Dose increase in this mode occurs only when Latrigine is added to the inhibitor or inducer of liver enzymes (also when added without valproate or inducer of liver enzymes).

The beginning of the use of hormonal contraception in women who already use lamotrigine in maintenance portions and do not use inducers of liver enzymes.

Often, an increase in the maintenance dose of lamotrigine is required in half. It is recommended that from the beginning of the use of hormonal contraception, the dose of Latrigine increased by 50-100 mg / day after every 7 days (taking into account the patient's reaction to therapy). In the process of increasing the dose, this limit can not be exceeded (this occurs only if there is a similar need in accordance with the clinical response of the patient).

The abolition of therapy with the use of hormonal contraception in women who already use lamotrigine in supporting portions, but do not use inducers of liver enzymes.

Often, a reduction of up to 50% of the maintenance portion of lamotrigine is required. To reduce the daily dosage of drugs, it is necessary to gradually - every week for 50-100 mg (maximum 25% of the total weekly portion) for 3 weeks. An exception can be cases where there is a non-standard individual clinical response.

With liver failure.

The initial dose, the increase in dosage and the size of the maintenance dose should be reduced by approximately 50% in people with moderate stage of the disease (Level B on the Child-Pugh scale) or 75% in people with severe pathology (level C). Increase in dosage and maintenance dose can be adjusted taking into account the medicinal effect.

[12], [13], [14]

Use of the lathridge during pregnancy

The results of the tests show that there is no noticeable increase in the risk of many congenital anomalies in the 1 st trimester, but some tests have revealed that the probability of an anomaly such as an isolated gap in the oral cavity increases. Control tests did not demonstrate an increased risk of an isolated gap in the oral cavity compared to other negative effects of lamotrigine use.

Information on the combined use of lamotrigine is too small to unequivocally conclude that the drug affects the likelihood of developmental abnormalities associated with other drugs. Latrijin can be appointed pregnant only in a situation where the likelihood of helping a woman from using it will be higher than the risk of complications in the fetus.

Changes in the physiological nature of pregnancy can affect the lamotrigine or its medicinal effects. There is evidence of a decrease in the substance in pregnant women. In this regard, pregnant women who are treated with lamotrigine should be under regular doctor control.

There is evidence that the drug can pass into the mother's milk in various concentrations, reaching the infant to values corresponding to 50% of the maternal parameters. Because of this, in some infants who are breastfed, the serum level of drugs can reach the values at which the drug effect can develop.

Therefore, it is necessary to take into account the risk of negative reactions in the infant, and to correlate it with the need for breastfeeding during the treatment period.

Contraindications

The main contraindications: hypersensitivity to the elements of the drug and children's age to 12 years (for therapy with epilepsy). You can not also appoint under the age of 18 to eliminate bipolar disorders, because there is no information about the use of drugs to this group of patients.

[8], [9],

Side effects of the lathridge

The use of drugs in the elimination of epilepsy can lead to such side effects:

• lesions of the subcutaneous layers along with the skin: often there are eruptions (usually maculopapular type), occasionally - Stevens-Johnson syndrome, and singly - TEN, against which the scars can form. The risk of rash is usually due to the intake of large portions of lamotrigine at the initial stage, ignoring the standard dosage regimen, and in addition to taking it along with valproate. In addition, there is an opinion that the rash is an element of the syndrome of intolerance, accompanied by various common manifestations. Occasionally, cutaneous lesions (TEN or Stevens-Johnson syndrome) resulted in death;
• disorders of the lymph and hematopoietic system: lymphadenopathy or hematological disorders (such as anemia (sometimes aplastic type), leuko-, thrombocyto- or neutropenia, as well as agranulocytosis) are noted. Deviations of the hematological nature can sometimes be caused by the hypersensitivity syndrome;
• immune disorders: the intolerance syndrome is manifested, expressed in the form of lymphadenopathy, fever, hematological disorders, facial swelling, skin rashes (varying degrees of severity), liver function problems, internal combustion engines, and multi-organ failure. Early signs of increased sensitivity (among such lymphadenopathy or fever) can develop even in the absence of skin rashes. If the patient has such signs, he should be examined immediately and, if no other symptoms are found, stop taking drugs;
• mental disorders: often there are feelings of irritability and aggressiveness. Isolated hallucinations, tick and sensation of confusion are noted;
• reactions of organs of the National Assembly: headaches are often noted. A little less often - nystagmus, dizziness, tremor, a feeling of drowsiness or insomnia. Occasionally, ataxia develops. There is a single feeling of anxious excitement in the aseptic form of meningitis, motor disorders and loss of balance, extrapyramidal symptoms, exacerbation of trembling paralysis, increased epileptic seizures and choreoathetosis;
• lesions of visual organs: often visual blurred and diplopia. Occasionally, conjunctivitis develops;
• disorders in the work of the digestive tract: often there is vomiting, diarrhea or nausea;
• disorders of the hepatobiliary system: single note liver failure, problems in the liver and an increase in the activity of liver transaminases. Problems with liver functioning are often a reaction of intolerance, although cases that did not have visible symptoms of hypersensitivity were also recorded;
• lesions of organs of ODA with connective tissues: lice-like manifestations appear singly;
• systemic disorders: often shows increased fatigue.

Side effects of taking tablets in bipolar disorder:

• lesions in the area of subcutaneous tissue along with the skin: most often there are rashes. Occasionally, Stevens-Johnson syndrome develops;
• reactions in the NA: most often there are headaches. Often there is a feeling of drowsiness or anxiety, as well as dizziness;
• manifestations in the field of connective tissue and ODA: arthralgia often develops;
• systemic signs: often there are painful sensations (in particular in the back area).

[10], [11]

Overdose

There is information about cases of acute poisoning (taking portions that exceeded the maximum medicinal values by 10-20 times). At the same time there was a disorder of consciousness, nystagmus with ataxia and a coma.

When the drug is intoxicated by the patient, it is necessary to be hospitalized to perform adequate maintenance treatment.

Interactions with other drugs

Medicines containing valproic acid inhibit the metabolism of lamotrigine, increasing the half-life of the substance to 70 hours.

Primidone with carbamazepine and phenytoin with paracetamol and phenobarbital increase the metabolic rate of the drug, halving the half-life of lamotrigine. Combined use with carbamazepine increases the development of some negative effects (ataxia, visual fuzziness, dizziness and diplopia with nausea), which disappear after a decrease in the portion of carbamazepine.

As a result of combined intake of 100 mg / day of lamotrigine and anhydrous lithium gluconate (twice a day, 2 g), no changes in the pharmacokinetic parameters of lithium are observed during the 6-day period.

The repeated use of bupropion does not significantly affect the pharmacokinetic characteristics of lamotrigine, slightly increasing the level of its decay product, glucuronide lamotrigine.

[15], [16], [17], [18]

Storage conditions

Lathirgin is kept in a place that is not accessible to young children. The maximum storage temperature is 25 ° C.

Special instructions

Reviews

Lathridge receives mostly positive feedback from patients. With a slow increase in the dose, no side effects are observed. Along with this, many indicate that the drug has a fairly stable antidepressant effect, as well as a weak anti-manic. In addition, the drug reduces the feeling of irritability.

Of the shortcomings - there are patients who had to refuse to take drugs because of the appearance of rashes.

Shelf life

Lathridine is allowed to be used for 2 years from the date of release of the drug.