The drug Lamotrigine Canon (25mg, 50mg, 100mg) from the manufacturer

Publications in the media

(Lamoiriginum) INN

Synonyms. Lamictal.

Composition and release form. Tablets of 0.025, 0.05 and 0.1 g of lamotrigine.

Indications. Epilepsy (mono- and auxiliary therapy for partial and generalized seizures).

Pharmachologic effect. Lamotrigine is an anticonvulsant that can block the action of excitatory non-irotransmitter amino acids (glutamate and aspartate). Blockade of voltage-dependent sodium channels, prevention of the release of excitatory amino acids and stabilization of presynaptic neuronal membranes provide its anticonvulsant effect. Lamotrigine exerts its action through NMDA receptors of excitatory amino acids. Pharmacokinetics. When taken orally, the drug is absorbed quickly and completely from the gastrointestinal tract into the blood; the bioavailability of lamotrigine is 98%; food intake does not affect bioavailability. The volume of distribution is 1.2 l/kg. Peak plasma concentrations are observed on average 2.5 hours after administration. Binds to plasma proteins by 55%. The drug is almost completely metabolized in the liver with the formation of the main metabolite - N-glucuronide. T1/2 is 29 hours. It is excreted mainly in the urine in the form of the main metabolite and, partially, unchanged. Side effects . Nausea, vomiting; feeling tired, headache, dizziness, irritability, drowsiness, tremor; blurred vision, diplopia; allergic reactions; lymphadenopathy. Contraindications. Severe diseases of the liver, kidneys; hypersensitivity to the drug.

Adverse reactions when interacting with other drugs. The drug is not recommended to be taken simultaneously with drugs that depress the central nervous system and with alcohol due to the dangerous potentiation of effects. Valproic acid, chloramphenicol, cimetidine inhibit the metabolism of lamotrigine and may increase its side effects. Carbamazepine, when taken simultaneously with lamotrigine, causes dizziness, diplopia, and blurred vision. The clearance of lamotrigine increases when it is taken simultaneously with carbamazepine or phenobarbital, or phenytoin, or primidone, which leads to a decrease in its T1/2. Information for the patient. Lamotrigine is prescribed to adults and children 0.05 g 2 times a day 30-40 minutes before meals or, to avoid irritation of the gastric mucosa, after meals. If necessary, the daily dose can be increased. Alcohol and other CNS depressants should not be used during treatment with lamotrigine. Use caution when driving. Lamotrigine should be avoided during pregnancy. The drug is discontinued gradually to avoid a sharp exacerbation of the disease. Missed dose: Take the missed dose as soon as possible; if there is no time left to take the missed dose, do not take it; do not take double doses.

Lamotrigine FT

Skin rash Undesirable skin reactions have been noted; they usually developed within the first 8 weeks of starting lamotrigine treatment. In most cases, the rash is mild and goes away on its own. However, there have also been reports of severe rashes that required discontinuation of lamotrigine and immediate hospitalization. These reactions included potentially life-threatening lesions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug reactions with eosinophilia and systemic symptoms. It has been reported that the rash may also be one of the symptoms of hypersensitivity syndrome, characterized by a variable complex of systemic manifestations (see section "Side effects"). In studies in adults taking lamotrigine at the recommended dosing regimen, the incidence of severe skin rash in patients with epilepsy was approximately 1/500 (i.e., severe rash occurred in 1 in 500 patients). Approximately half of these cases were diagnosed with Stevens-Johnson syndrome (incidence 1/1000). In clinical trials, the incidence of severe lesions in patients with bipolar disorder treated with lamotrigine was approximately 1/1000. Children are at higher risk of developing severe skin rashes than adults. Available information from a number of studies indicates that the incidence of skin rashes requiring hospitalization ranges from 1/300 to 1/100 in children with epilepsy. The initial manifestations of a rash in children during the initial assessment may be mistakenly regarded as a symptom of an infectious disease. It must be remembered that rash and fever that occur in children in the first 8 weeks of starting lamotrigine therapy may be adverse reactions associated with the use of the drug. In general, it appears that the risk of rash is largely associated with: - high starting doses of lamotrigine, exceeding the recommended rate of increasing doses of lamotrigine (see section "Method of administration and dosage regimen"); - concomitant use of valproate (see section “Method of administration and dosage regimen”). If you have previously experienced allergic reactions or rashes in connection with taking other antiepileptic drugs, you should inform your doctor before starting to use Lamotrigine FT. In such situations, caution is required when taking lamotrigine. It was noted that in such patients the incidence of mild rash after treatment with lamotrigine was approximately 3 times higher than in patients who had no history of these events. If a rash appears while using Lamotrigine FT, you should immediately consult your doctor. Lamotrigine should be stopped immediately in all cases unless it is clearly established that the rash is not related to lamotrigine. In the future, it is recommended not to restart lamotrigine treatment if lamotrigine has been discontinued due to the development of a rash in response to the drug; The decision to restart treatment in such patients can only be made when the expected benefits of treatment clearly outweigh the potential risks. If Stevens-Johnson syndrome, toxic epidermal necrolysis, or a drug reaction with eosinophilia and systemic symptoms develops in connection with lamotrigine, reintroduction of lamotrigine in any case is prohibited. It has been reported that the rash may also be a symptom of hypersensitivity syndrome, which is characterized by a variable constellation of systemic symptoms including fever, swollen lymph nodes, facial swelling, blood and liver abnormalities, and aseptic inflammation of the meninges (see section "Side Effects" ). This syndrome can have variable clinical severity and can, in rare cases, lead to disseminated intravascular coagulation and multiple organ failure. It is important to remember that early manifestations of hypersensitivity (eg, fever, lymphadenopathy) may be present even in the absence of rash. If these symptoms and signs are detected in the patient, it is necessary to immediately evaluate his condition and, if an alternative cause for the observed pathological phenomena cannot be established, stop taking lamotrigine. In most cases, after stopping the drug, aseptic meningitis was a reversible phenomenon. However, in a number of cases, aseptic meningitis developed again after an attempt to restart lamotrigine therapy. Resumption of treatment resulted in a rapid return of symptoms, which were often more severe. Treatment with lamotrigine should not be restarted if lamotrigine was previously interrupted due to aseptic meningitis associated with lamotrigine therapy. Clinical deterioration and suicide risk

Suicidal ideation and suicidal behavior have been reported in patients taking antiepileptic drugs for several indications.
A summary analysis of clinical studies of the use of antiepileptic drugs also showed a slight increase in the risk of suicidal thoughts and suicidal behavior. The mechanism of formation of this risk is unknown; Based on the available information, we cannot exclude the possibility of an increased risk when taking lamotrigine. Therefore, it is necessary to be alert for signs of suicidal thinking and behavior and decide on the appropriate treatment. If signs of suicidal thoughts or behavior appear, you should immediately seek qualified help. People with bipolar disorder may experience worsening depressive symptoms and/or suicidality whether or not they are taking medications for bipolar disorder, including lamotrigine. At the beginning of the course of treatment or during periods of changing the dose, you must be alert for the occurrence of suicidal thoughts or behavior, and if necessary, seek qualified medical help. The risk of suicidal thoughts or suicide attempts may be higher in: - persons with a history of suicidal thoughts or suicidal behavior; — young adult patients; - persons with strongly expressed suicidal ideation before the start of treatment. Hormonal contraceptives
Effect of hormonal contraceptives on the effectiveness of lamotrigine Use of the ethinyl estradiol/levonorgestrel combination (30 mcg/150 mcg) increases the elimination rate of lamotrigine by approximately 2-fold, resulting in decreased lamotrigine levels (see Drug Interactions and Other Interactions section) ).
Decreased lamotrigine levels may be accompanied by loss of seizure control. In most cases, once dosing is titrated, higher maintenance doses of lamotrigine (up to a doubling of the initial maintenance dose) will be required to achieve maximum therapeutic response. When you stop taking a hormonal contraceptive (for example, in women whose contraceptive regimen includes a week-long break in taking the contraceptive), the clearance of lamotrigine may decrease by 2 times. The resulting increased concentrations of lamotrigine may lead to the development of dose-dependent adverse reactions. It is necessary to take this information into account and be alert to the development of any changes, if necessary, seek medical help. Women who have not yet taken any inducer of lamotrigine glucuronidation and who are taking a hormonal contraceptive regimen that includes a week-long break from hormonal therapy (1 week of inactive treatment) will experience gradual, transient increases in lamotrigine levels during that week-long break (see section "Method of administration and dosage regimen"). This variability in lamotrigine levels may result in adverse reactions. Therefore, you should consult with your healthcare provider about prescribing a contraceptive regimen that does not require a one-week break as a first-line regimen (for example, continuous hormonal contraceptives or the use of non-hormonal methods). Interactions between other oral contraceptives and lamotrigine, and between hormone replacement therapy drugs and lamotrigine, have not been studied. However, it is possible that these drugs may affect the pharmacokinetic parameters of lamotrigine in a similar manner as described above. The effect of lamotrigine on the effectiveness of hormonal contraceptives
When lamotrigine is prescribed together with a hormonal contraceptive (ethinyl estradiol/levonorgestrel combination), there is a slight increase in the rate of elimination of levonorgestrel and changes in the concentrations of follicle-stimulating and luteinizing hormones in the blood serum (see section "Interaction with other drugs and other types of interactions" ).
The effect of these changes on ovulatory activity of the ovaries is not known. However, we cannot exclude the possibility that such changes will lead to a decrease in the effectiveness of contraceptives taking hormonal drugs during lamotrigine therapy. Therefore, patients should be warned to promptly report changes in menstrual patterns, including sudden, unexpected bleeding. Dihydrofolate reductase
Lamotrigine has a weak inhibitory effect on dihydrofolate reductase.
Therefore, there is a possibility of changes in folate metabolism during long-term therapy with lamotrigine (see section "Fertility, Pregnancy and Lactation"). However, during chronic use in humans, lamotrigine did not induce significant changes in hemoglobin concentration, MCV (mean erythrocyte volume), serum or red blood cell folate concentrations up to 1 year, or changes in red blood cell folate concentrations up to 5 years. Renal failure
In studies with single-dose lamotrigine in patients with end-stage renal disease, no significant changes in lamotrigine plasma concentrations were observed.
However, accumulation of a lamotrigine metabolite is expected; therefore, caution should be exercised when administering lamotrigine therapy to patients with renal failure (see section "Method of administration and dosage regimen"). Liver dysfunction.
The dose size for each stage (initial treatment, in the process of increasing the dose and maintenance dose) should be selected by the doctor.
In cases of impaired hepatic function of various Child-Pugh classes (A, B and C), the rate of lamotrigine excretion through the liver is reduced, so doses at each stage should be lower than for normal liver function (see section "Method of administration and dosage regimen") . Patients taking other drugs containing lamotrigine
Without consulting a doctor, Lamotrigine FT should not be taken while already taking any other drug containing lamotrigine.
Child development
There is no information on the effect of lamotrigine on growth, puberty and the development of cognitive, emotional, and behavioral areas in children.
Epilepsy
Abruptly stopping antiepileptic drugs, including lamotrigine, can trigger a recurrence of seizures.
The dose of lamotrigine should be reduced gradually over 2 weeks under medical supervision. The exception is when, for safety reasons, abrupt discontinuation of lamotrigine is required, for example, if a rash occurs. There are reports in the literature that severe seizures, including status epilepticus, can lead to muscle tissue destruction, multiple organ dysfunction, and widespread intravascular coagulation. In such situations, death has sometimes occurred. Similar cases have been described in connection with the use of lamotrigine. In the presence of seizures of different types, instead of improving the condition (decreasing the frequency of attacks), an increase in the frequency of attacks may be observed. Treatment with lamotrigine should be carried out under regular medical supervision to assess the balance between the benefits of controlling one type of seizure and the harm associated with any observed worsening of other types of seizures. Lamotrigine may worsen myoclonic seizures. In children, when lamotrigine is used to treat typical absence seizures, the effectiveness of therapy may not be maintained in all patients. Bipolar disorder
In children and adolescents (<18 years of age) with major depressive disorder and other mental disorders, antidepressant treatment is associated with an increased risk of suicidal ideation and behavior.
Brugada syndrome
In rare cases, arrhythmogenic activity of the drug occurred, namely changes in the ST-T interval and the appearance on the ECG of a typical picture of Brugada syndrome.
If you have a history of Brugada syndrome or are prescribing lamotrigine, the possibility of using lamotrigine should be discussed with your doctor. Excipients
The drug Lamotrigine FT contains lactose.
If you have an intolerance to certain sugars (for example, a rare hereditary disorder such as galactose intolerance, lactase deficiency, glucose-galactose malabsorption), you must inform your doctor about this before starting treatment with Lamotrigine FT. Fertility, pregnancy and lactation
If you are pregnant or breastfeeding, if you are currently pregnant, or if you are planning a pregnancy, please consult your doctor before starting to use this medicine.
General risks associated with antiepileptic drugs
Women of childbearing age should seek specialist advice.
If you are planning a pregnancy, contact your doctor to discuss the possibility of using antiepileptic drugs. Abrupt withdrawal of antiepileptic therapy should be avoided as this may lead to sudden seizures, which can have serious consequences for you and the embryo/fetus. In all cases, preference should be given to monotherapy, since the use of a combination of antiepileptic drugs may be associated with a higher risk of congenital malformations than the use of monotherapy (depending on the drugs used in the combination regimen). Risk associated with lamotrigine
Pregnancy Extensive experience with lamotrigine monotherapy during the first trimester of pregnancy (more than 8,700 cases) does not indicate a significant increase in the risk of major congenital malformations, including oral clefts. Animal studies have demonstrated the developmental toxicity of lamotrigine. If the use of lamotrigine during pregnancy is considered necessary, the lowest possible therapeutic dose should be taken. Theoretically, lamotrigine may increase the risk of embryonic/fetal developmental disorders by reducing folic acid levels. It is necessary to consult with your doctor about the advisability of taking folic acid during pregnancy planning and in early pregnancy. Physiological changes that occur during pregnancy may affect lamotrigine levels and/or its therapeutic effect. Decreased plasma levels of lamotrigine have been reported during pregnancy, creating a potential risk of loss of seizure control. After delivery, lamotrigine concentrations may increase rapidly, increasing the risk of dose-related adverse reactions. Therefore, you should be observed by your doctor to carefully monitor the concentration of lamotrigine in the blood serum before, during and after pregnancy, including in the immediate period after childbirth. It may be necessary to adjust the dose of the drug to maintain the concentration of the active substance in the blood serum at the same level as before pregnancy, or adjust the dose depending on the therapeutic effect. It is also necessary to be alert to the occurrence of dose-related adverse reactions. If, while using Lamotrigine FT, you suspect or discover that you are pregnant, consult your doctor about the possibility of continuing treatment with this drug. Lactation Lamotrigine passes into breast milk in varying amounts; Total lamotrigine levels in breastfed infants may be up to approximately 50% of maternal levels. Therefore, in some children, lamotrigine serum concentrations may reach levels at which its pharmacological effects occur. In a limited group of children, no adverse reactions were observed. You should consult your doctor to evaluate the potential benefits of continuing breastfeeding and the potential risk of adverse reactions that your baby may experience. If a decision is made to continue breastfeeding during treatment with Lamotrigine FT, the child should be under medical supervision to monitor the occurrence of adverse reactions. Fertility Animal studies have not shown any impairment of fertility associated with the administration of lamotrigine.

Psychiatry Psychiatry and psychopharmacotherapy named after. P.B. Gannushkina No. 05 2004

The mechanisms of alcohol dependence formation involve various systems of neurotransmitter regulation of the brain, the most important and significant of which are the dopamine [1, 2], opioid [3], serotonergic [4–6], and GABAergic [7, 8] systems.
In drug treatment practice, anticonvulsants have been used for quite a long time to relieve alcohol withdrawal syndrome (AAS), actualize pathological craving for alcohol, and prevent convulsive paroxysms [9–17]. Until recently, the pathogenetic justification for the use of this group of drugs was data on similar mechanisms of the formation of paroxysmal brain activity and pathological craving syndrome [10]. At present, new data have emerged on the possibility of a therapeutic effect of mood stabilizers (anticonvulsants) on pathological desire through the regulation of the GABAergic system [18–24]. Some authors [25] indicate that mood stabilizers can enhance dopaminergic and adrenergic neurotransmission. This gives grounds to consider anticonvulsants as the drugs of choice in the treatment of pathological craving for alcohol. One of the promising drugs in this group is Lamictal (lamotrigine). The results of clinical studies of Lamictal indicate its high effectiveness in the treatment of a wide range of different types of epileptic seizures, including simple and complex partial, primary or secondary generalized. Many authors point to the significant therapeutic effect of Lamictal on cognitive functions, mood, and behavior. The effectiveness of Lamictal in drug treatment practice has practically not been studied [26]. The undertaken clinical comparative study is devoted to solving these questions. The purpose of the study
was to study the therapeutic effectiveness of Lamictal in the treatment of pathological craving for alcohol in patients with alcohol dependence in comparison with carbamazepine. The effect of Lamictal on pathological craving for alcohol was studied at various stages of the disease: AAS, post-withdrawal state and the formation of remission.

Material and research methods

The total number of patients who took part in the study was 40 people.
All patients were men and underwent an inpatient course of treatment from 2002 to 2003 in the Department of Clinical Psychopharmacology of the National Research Center for Narcology. The age of the patients ranged from 35 to 60 years, the average age was 42.3±7.8 years. The duration of the disease in the presented sample varied from 3 to 35 years, the average duration was 15.5±8.5 years. Patients with a high suicidal risk were excluded from the study; chronic somatic diseases in the acute stage; hypersensitivity to the drug; history of epileptiform seizures of non-alcoholic origin; received treatment within 30 days prior to inclusion in the study with antidepressants, anticonvulsants, antipsychotics, tranquilizers, nootropics. The sample was divided into groups using a block randomization method. The groups did not differ in age and socio-demographic indicators; the main clinical and dynamic characteristics are presented in Table.
1 .

Diagnosis of axial dependence syndromes was carried out according to ICD-10. The majority of patients (32 people) were diagnosed with the middle stage of alcohol dependence. This was confirmed by the following clinical manifestations: fully formed primary pathological craving for alcohol, loss of quantitative control, maximum tolerance to alcohol, developed AAS, sharpening of premorbid personality characteristics. In most patients, the rate of progression of the disease was classified as average, and the form of use was classified as pseudo-binge. 3 patients were diagnosed with transitional stage II–III. This was evidenced by the changing type of drunkenness: an intermittent form of alcohol abuse was observed. 5 patients had clinical signs of the final stage of chronic alcoholism. The diagnostic criteria were a decrease in tolerance to alcohol, the appearance of binge drinking, signs of alcohol degradation and encephalopathy, and significant somatic and social consequences of alcoholism. All patients had chronic somatic diseases caused by long-term alcohol intoxication (without exacerbation), mainly toxic damage to the liver and heart. Negative social consequences were characterized by disruption of family relationships and a decrease in professional skills. The structure of AAS included somatovegetative and psychopathological disorders. All patients had hyperhidrosis, thirst, tremor, dyspeptic disorders, fluctuations in blood pressure, tachycardia, weakness, fatigue, sleep disorders, depressed mood, anxiety, irritability, and dysphoria. The severity of AAS was classified as moderate in 28 patients and severe in 12 patients. 12 patients had preliminary disorders in the form of severe internal anxiety, prolonged insomnia with nightmares and anxiety dreams before admission, anorexia, hypnagogic hallucinations, erratic agitation in the emergency department, severe general tremor, fragmentary overvalued unsystematized ideas of persecution with a pronounced affective substrate in the form of fear and dysphoria . Convulsive seizures within 3 days before admission were observed in 5 patients. After relief of acute disorders in the post-withdrawal state, the most common were various depressive disorders: low mood, anxiety, irritability, dysphoria, asthenic manifestations. The main research methods were clinical-psychopathological and statistical. When assessing the spectrum of therapeutic effectiveness of the drugs, we used scales specially developed in the Department of Clinical Psychopharmacology for assessing psychopathological and somatovegetative manifestations in AAS, the post-withdrawal state, and a scale of general clinical impression. The clinical study of the drugs was carried out using a specially developed protocol that best meets the international requirements of GCP (good clinical practice). Statistical processing of the results was carried out using the Microsoft Excel 2000 computer program. In connection with the assigned tasks, intragroup and intergroup comparisons were carried out. We checked the reliability of changes in pathological craving for alcohol, the severity of affective and behavioral disorders under the influence of Lamictal in comparison with carbamazepine. The severity of each symptom was assessed on a 4-point scale: 0 – absence of symptom; 1 – weak expression; 2 – moderate severity; 3 – strong expression. The results were recorded according to the following scheme: mean value±confidence interval. The reliability criterion was considered to be achievement of a level of p<0.05 or less. Quantitative indicators were compared using Student's t test.

Study design

The study was carried out in two stages. At the first stage, the relief of affective disorders in the structure of AAS was carried out. The treatment was comprehensive, detoxification measures, restorative and symptomatic therapy were carried out. Anticonvulsants were prescribed from the first day of hospitalization as monotherapy. It is important to note that in severe cases of AAS, with significantly pronounced psychopathological and somatovegetative symptoms, tranquilizers (phenazepam in a dose of up to 4–6 mg/day or Relanium at a dose of up to 10–15 mg/day). In addition, in preliminary conditions, infusion detoxification therapy lasted 2–3 days longer than usual. At the second stage, treatment was carried out for affective, ideational, and behavioral disorders in a post-abstinence state, which are part of the structure of pathological craving for alcohol. Anticonvulsants were prescribed as the only pathogenetic drug. The daily therapeutic dose was 400–600 mg for carbamazepine and 200 mg for lamictal. Carbamazepine was prescribed 1 tablet 2–3 times a day, Lamictal - 1 tablet 2 times a day. The overall duration of the clinical trial was 4 weeks. Patients were examined on the day of admission (day 0), and subsequently on days 3, 7, 14, and 30 of treatment. The therapeutic effect of the drug was considered good if a 70% reduction in symptoms was achieved according to scales for assessing somatovegetative and psychopathological manifestations on the 3rd day, according to the General Clinical Impression scale on the 7th day of the study; complete reduction of symptoms according to the scale for assessing psychopathological manifestations on the 30th day of the study.

Research results

First of all, attention was paid to the ability of Lamictal to stop the pathological craving for alcohol.
As can be seen from table.
2 , its reduction in the main group was observed already by the 3rd day of treatment, while in the control group – only by the 7th.

The drug had the most pronounced effect on disorders such as low mood, anxiety and sleep disorders. These disorders in the main group were relieved by the 3rd day of treatment (p<0.05), while in the control group, a reduction in anxiety, the ideational component of PVN, and an improvement in mood were noted by the 7th day, and sleep disturbances were relieved only by the 14th day. the next day of treatment. The drug had a less pronounced effect on dysphoria, irritability and internal tension, which were reduced by days 7–14 of treatment. When comparing these indicators with the control group, there were no statistical differences, and dysphoria under the influence of carbamazepine was relieved faster (by the 3rd day of treatment in the control group compared to the 7th day in the main group). Lamictal also had a good effect on somatovegetative and neurological manifestations. A noticeable reduction in neurological disorders (tremor, ataxia) was observed by the 3rd day of treatment, while in the control group - by the 7th day of treatment ( table 3

Separately, it is necessary to note the high anticonvulsant effect of Lamictal, which in the study sample was superior to carbamazepine. Thus, in patients with epileptiform seizures in AAS after taking Lamictal, seizures did not recur during treatment (3 patients), and in patients taking carbamazepine, repeated seizures were observed on the 2nd day of therapy (2 patients).

When using Lamictal, skin hyperemia and pinpoint rash were observed in 2 cases. These disorders were leveled out by reducing the dose of the drug or prescribing symptomatic therapy after 2–3 days. In the control group, 5 people were diagnosed with diplopia, unsteady gait, and accommodation disturbances. The Clinical Global Impression Scale confirmed the high therapeutic efficacy of Lamictal ( see figure

Discussion

In its therapeutic spectrum, Lamictal is superior to the standard drug of this group, carbamazepine: it has a more pronounced normothymic and anti-anxiety effect and effect on insomnia disorders. It should be emphasized that the drug has a significant effect on neurological disorders in the structure of AAS (general tremor, ataxia, etc.). Lamictal is better tolerated by patients and causes virtually no side effects with long-term use compared to carbamazepine. The results of the study showed that Lamictal has a more pronounced redynamic effect compared to carbamazepine - increased physical activity, performance and mood stabilization without increasing anxiety and restlessness. This clinical study of the drug is practically the first experience of using Lamictal in the treatment of alcohol dependence, in particular, the possibility of stopping the pathological craving for alcohol through the use of drugs with normothimic activity. The results of the study confirm the prospects of using mood stabilizers (using the example of Lamictal) in the treatment of pathological desire and depressive disorders in its structure.

References

Voronkova, K.V., Petrukhin, A.S., Pylaeva, O.A. and others. Rational antiepileptic pharmacotherapy. - M.: Binom, 2007. - 275 p.
Mashkovsky, M. D. Medicines. — 15th ed. - M.: Novaya Volna, 2005. - P. 40-41.
Petrukhin, A.S., Mukhin, K.Yu., Kalinina, L.V. and others. Lamictal: poly- and monotherapy for epilepsy. Psychiatry and psychopharmacotherapy, 2004. - pp. 20-25.
Hussain, A., Dar, M., Wani, R. et al. Role of lamotrigine augmentation in treatment-resistant obsessive compulsive disorder: a retrospective case review from South Asia. Indian J Psychol Med journal, 2015. - Vol. 37(2). — P. 154-158.
Ghaemi, N., Shirzadi, A., Filkowski, M. Publication bias and the pharmaceutical industry: the case of lamotrigine in bipolar disorder. Medscape journal of medicine, 2008. - Vol. 10(9). - P. 211.

Using the drug for a hangover

Inside a person, ethanol is first absorbed into the walls of the stomach and intestines. Then it is supplied along with blood to all organs. The liver metabolizes alcohol and breaks it down into its components. Acetaldehyde is one of the decomposition substances, poison. It is more toxic and dangerous than ethanol itself.

This poison causes a hangover:

dizziness;
nausea and involuntary eruption of stomach contents;
sleep disturbance;
pain in the head area;
general weakness and poor health.

People undergoing course treatment should not drink alcohol. If you have a hangover, you should not take medicine either. Ethanol leaves the body for a long time, which depends on the amount drunk and the patient’s condition. Therefore, it is necessary to begin therapy taking into account recent alcohol consumption only after consultation with a doctor.

Use of the drug for alcoholism

Alcohol displaces fluid from the body and penetrates the plasma membrane. There is a persistent desire to drink alcohol - it becomes an indispensable link in the construction of cells.

With constant drinking of strong drinks the following are observed:

Violations in the behavior of the drinker - unreasonable aggression, anxiety, depression.
Confused speech - words are confused, “tongue is twisted”, sentences are incoherent.
Short-term amnesia - a person does not remember events while intoxicated.
Alcohol coma can be fatal.

Dependence on alcohol is recognized as a disease, which is given the name alcoholism. Dependent patients often have a serious liver problem, including cirrhosis - this is a contraindication for use.

People with epileptic seizures should not drink strong drinks. Ethanol provokes an attack in 99% of cases.

Before starting the course, a person needs to recover from alcoholism and put his internal organs in order.

Lamotrigine is an anticonvulsant drug used to treat various forms of epilepsy and mood disorders associated with bipolar disorder.

Synonyms Russian

Lamictal, lapeptil, convulsan, lamitor, lamolep, lamothrix, seisar, triginet.

English synonyms

Lamotrigin, Lamictal.

Research method

Gas chromatography-mass spectrometry (GC-MS).

Units

µg/ml (micrograms per milliliter).

What biomaterial can be used for research?

Venous blood.

How to properly prepare for research?

Do not eat for 2-3 hours before the test; you can drink clean still water.
Children under 1 year of age should not eat for 30-40 minutes before the test.
Do not smoke for 30 minutes before the test.

General information about the study

Lamotrigine is an antiepileptic drug with a broad spectrum of action in various forms of epilepsy, which can have a beneficial effect on mood in bipolar disorders. The drug is used as mono- or additional therapy for partial and generalized convulsive seizures, seizures in Lennox-Gastaut syndrome, for typical absence seizures, as well as for the prevention of mood disorders (depression, mania, hypomania) in patients with bipolar disorder. In addition, the use of lamotrigine is being considered for migraine, trigeminal neuralgia and treatment-refractory depression.

Its pharmacological action is associated with blocking voltage-gated sodium channels, stabilizing the membrane of nerve cells and suppressing the release of glutamic acid.

The bioavailability of lamotrigine is very high and amounts to 98%. After oral administration, the drug is quickly and fairly completely absorbed from the gastrointestinal tract; food intake slows down the absorption process, but does not reduce its effectiveness. The maximum concentration in the blood is observed 2.5 hours after administration. Binding to blood proteins is no more than 55%. The therapeutic concentration in the blood is 2.5-15 mcg/ml. Lamotrigine is metabolized in the liver by conjugation with glucuronic acid using the enzyme glucuronyltransferase and without the participation of the cytochrome P450 system. The half-life of lamotrigine is 24-35 hours and depends on concomitant medications. The drug is excreted from the body primarily by the kidneys in the form of glucuronides or unchanged (10%), and about 2% through the intestines.

While taking lamotrigine, headaches, fatigue, drowsiness or insomnia, nausea, vomiting, a decrease in the number of leukocytes and platelets in the blood, skin rashes and allergic reactions may occur; in rare cases, the development of Stevens-Johnson syndrome and Lyell's syndrome may occur. In some cases, abrupt cessation of the drug may provoke epileptic seizures, therefore, when discontinuing lamotrigine, the dose must be reduced gradually.

The concentration of the drug in the blood should be monitored and adjusted in case of liver and kidney failure, while taking it with other drugs. It is also important to consider fluctuations in lamotrigine blood levels during pregnancy and postpartum (FDA Fetal Category C). During pregnancy, a decrease in the concentration of lamotrigine in the blood is observed due to an increase in body weight and increased excretion under the influence of estrogens. This circumstance can lead to a worsening of the disease. On the other hand, after childbirth, due to the reverse development of the above processes, conditions are physiologically created for the appearance of signs of intoxication. Therefore, when planning pregnancy in women taking lamotrigine, it is advisable to determine the level of the drug in the blood and monitor it during pregnancy and after childbirth.

What is the research used for?

Monitoring drug concentrations in the blood;
assessment of drug interactions;
overdose diagnosis;
identification of violations of the drug administration regimen.

When is the study scheduled?

If symptoms persist or the disease worsens while taking lamotrigine;
with the simultaneous administration of other anticonvulsants that affect the concentration of lamotrigine in the blood;
if the patient has liver and kidney dysfunction;
before and during pregnancy, as well as after childbirth;
if adverse events occur, possibly related to taking lamotrigine, and a drug overdose is suspected.

What do the results mean?

Reference values: 4 - 10 µg/ml.

What can influence the result?

The concentration of lamotrigine in the blood increases: when taking valproic acid;
with impaired liver and kidney function.

Medicines that can reduce the concentration of lamotrigine in the blood: phenytoin, carbamazepine, phenobarbital, primidone, oral contraceptives, estrogens.

Compatibility of Lamotrigine and alcohol

? Doctors do not recommend mixing Lamotrigine with alcohol. Alcohol is a colorless liquid, often with a strong, unpleasant odor. In chemistry it is called ethanol, or ethyl monohydric alcohol.

The substance will disintegrate in the body:

volatile aldehydes;
furfural;
acetic acid;
carbon dioxide;
cholesterol;
fatty acid;
water.

All decomposition products are toxic to humans. Doctors do not recommend taking the medicine together with alcoholic beverages. At best, such a mixture will not give any positive effect. But it is also possible that the side effects of the drug may increase.

Lamotrigine and beer

Lamotrigine and beer are incompatible. The effect of the anticonvulsant drug is inhibited due to the lack of influence on the sodium channels of the nervous tissue upon penetration of toxic ethanol.

The release of glutamate, which causes epileptic seizures, increases. Therefore, tonic-clonic seizures occur more often.

Treatment is contraindicated when drinking beer. Ethanol crosses the blood-brain barrier into the central nervous system, causing neuronal damage. The number and quality of seizures increases, the patient’s well-being worsens.

The risk of liver damage increases with the development of hepatitis. The function of the organ decreases, intoxication of the body, hyperbilirubinemia occurs.

Lamotrigine Canon tablets 100 mg bl N10x3 Canonpharma

Interactions with PEP. Valproic acid inhibits the glucuronidation of lamotrigine, reducing its rate of metabolism and prolonging its half-life. almost 2 times. Some AEDs (eg, phenytoin, carbamazepine, phenobarbital and primidone) that induce liver microsomal enzymes accelerate lamotrigine glucuronidation and metabolism. Dizziness, ataxia, diplopia, blurred vision and nausea have been reported in patients taking carbamazepine in combination with lamotrigine (these symptoms usually disappear when the dose of carbamazepine is reduced). A similar effect was observed with lamotrigine and oxcarbazepine; the effect of dose reduction was not studied. When lamotrigine 200 mg is taken concomitantly with oxcarbazepine 1200 mg, neither oxcarbazepine nor lamotrigine interferes with each other's metabolism. The combined use of felbamate at a dose of 1200 mg 2 times a day and lamotrigine 100 mg 2 times a day did not lead to clinically significant changes in the pharmacokinetics of lamotrigine. There was no pharmacological interaction between lamotrigine and gabapentin. Potential drug interactions between levitiracetam and lamotrigine were investigated by assessing serum concentrations of both drugs in placebo-controlled clinical trials. These data indicate that lamotrigine and levetiracitam do not affect each other's pharmacokinetics. There was no effect of pregabalin at a dose of 200 mg 3 times a day on the steady-state concentrations of lamotrigine, i.e. Pregabalin and lamotrigine do not interact pharmacokinetically with each other. With simultaneous use of lamotrigine and topiramate, the plasma concentration of the latter increases by 15%. Taking zonisamide (at a dose of 200 - 400 mg per day) during a clinical program together with lamotrigine (at a dose of 150 - 500 mg per day) did not lead to changes in the pharmacokinetic parameters of lamotrigine. Studies have shown that lamotrigine does not affect plasma concentrations of other antiepileptic drugs. Lamotrigine does not displace other antiepileptic drugs from binding to plasma proteins. Interactions when used in combination with other psychotropic drugs. Lamotrigine at a dose of 100 mg/day does not interfere with the pharmacokinetics of anhydrous lithium gluconate (2 g 2 times a day for 6 days) when administered together. Repeated oral administration of bupropion does not have a statistically significant effect on the pharmacokinetics of a single dose of lamotrigine and causes a slight increase in the area under the concentration-time curve (AUC) of lamotrigine glucuronide. Olanzapine at a dose of 15 mg reduced the AUC and Cmax of lamotrigine by an average of 24% and 20%, respectively, which was not clinically significant. Lamotrigine at a dose of 200 mg does not change the kinetics of olanzapine. Repeated doses of lamotrigine 400 mg per day did not have a clinically significant effect on the pharmacokinetics of risperidone after a single dose of 2 mg in healthy volunteers. At the same time, drowsiness was observed in 12 of 14 patients when taking lamotrigine and risperidone in combination; in 1 in 20 patients when taking risperidone alone; none of the patients received lamotrigine alone. In a study of 18 adult patients with bipolar disorder receiving lamotrigine (100-400 mg/day), increasing the dose of aripiprazole from 10 mg/day to 30 mg/day over 7 days showed a 10% decrease in lamotrigine AUC and Cmax without clinically significant consequences. Inhibition of lamotrigine by amitriptyline, bupropion, clonazepam, fluoxetine, haloperidol, or lorazepam has minimal effect on the formation of lamotrigine's primary metabolite 2-N-glucuronide. A study of the metabolism of bufuralol by liver microsomal enzymes isolated from humans allows us to conclude that lamotrigine does not reduce the clearance of drugs metabolized primarily by CYP2D6 isoenzymes. Results from in vitro studies also suggest that clozapine, phenelzine, risperidone, sertraline or trazodone are unlikely to affect the clearance of lamotrigine. Interactions with hormonal contraceptives. The effect of hormonal contraceptives on the pharmacokinetics of lamotrigine. Taking combined oral contraceptives containing 30 mcg ethinyl estradiol and 150 mcg levonorgestrel causes an approximately two-fold increase in the clearance of lamotrigine (after oral administration), resulting in a decrease in lamotrigine AUC and Cmax by an average of 52% and 39%, respectively. During the week without taking the active drug, an increase in lamotrigine plasma concentrations is observed, with lamotrigine concentrations measured at the end of this week before the next dose being administered on average 2 times higher than during the period of active therapy. Effect of lamotrigine on the pharmacokinetics of hormonal contraceptives. During the period of equilibrium concentrations, lamotrigine at a dose of 300 mg does not affect the pharmacokinetics of ethinyl estradiol. There was a slight increase in the clearance of levonorgestrel, which led to a decrease in AUC and Cmax of levonorgestrel by 19% and 12%, respectively. Measurements of serum FSH, LH, and estradiol during this study revealed a slight decrease in ovarian hormonal suppression in some women, although measurements of plasma progesterone concentrations in none of the 16 women revealed hormonal evidence of ovulation. The effect of a moderate increase in levonorgestrel clearance and changes in plasma concentrations of FSH and LH on the ovulatory activity of the ovaries has not been established. The effects of lamotrigine doses other than 300 mg/day have not been studied, and studies involving other hormonal agents have not been conducted.