Lamotrigine in the treatment of chronic pain syndromes

Lamotrigine (Lamictal, Lamitor, Lamolep, Sezar)

Epilepsy

Adults and children over 12 years old

For monotherapy, the initial dose of Lamictal is 25 mg 1 time / day for the first 2 weeks, followed by an increase in dose to 50 mg 1 time / day over the next 2 weeks. The dose should then be increased by 50-100 mg every 1-2 weeks until the optimal therapeutic effect is achieved. The standard maintenance dose to maintain the optimal therapeutic effect is 100-200 mg/day in 1-2 doses. Some patients require Lamictal at a dose of 500 mg/day to achieve a therapeutic effect.

As part of combination therapy when using Lamictal together with valproic acid drugs in combination with other antiepileptic drugs (AEDs) or without them, the initial dose of Lamictal is 25 mg every other day for the first 2 weeks; subsequently – 25 mg 1 time/day for the next 2 weeks. Then the dose should be increased by a maximum of 25-50 mg/day every 1-2 weeks until the optimal therapeutic effect is achieved. The standard maintenance dose to maintain the optimal therapeutic effect is 100-200 mg/day in 1-2 doses.

As part of combination therapy with concomitant therapy with AEDs or other drugs that induce glucuronidation of lamotrigine (phenytoin, carbamazepine, phenobarbital and primidone), in combination or without other AEDs (except for valproic acid drugs), the initial dose of Lamictal is 50 mg 1 time / day for the first 2 weeks, then over the next 2 weeks - 100 mg / day in 2 doses. Then the dose is increased by 100 mg every 1-2 weeks until the optimal therapeutic effect is achieved. The standard maintenance dose is 200-400 mg/day in 2 divided doses. Some patients may require a dose of 700 mg/day to achieve a therapeutic effect.

As part of combination therapy with oxcarbazepine in combination with or without any other inducers or inhibitors of lamotrigine glucuronidation, the initial dose of Lamictal is 25 mg 1 time / day for the first 2 weeks, then 50 mg / day in 1 dose for the next 2 weeks. Then the dose is increased by a maximum of 50-100 mg every 1-2 weeks until the optimal therapeutic effect is achieved. The standard maintenance dose is 100-200 mg per day in 1 or 2 doses.

Due to the risk of developing a rash, the initial dose of the drug and the recommended dose escalation regimen should not be exceeded.

Table 1. Recommended dosage regimen for the treatment of epilepsy in adults and children over 12 years of age.

Children aged 2 to 12 years

It should be noted that accurate initial therapy with Lamictal in 5 mg tablets according to the proposed dosage regimen is impossible if the child’s body weight is less than 17 kg. Children ages 2 to 6 years are likely to require the highest maintenance doses.

The initial dose of Lamictal for monotherapy of typical absence seizures is 0.3 mg/kg body weight/day in 1 or 2 divided doses during the first 2 weeks, followed by a dose increase to 0.6 mg/kg/day in 1 or 2 divided doses over the next 2 weeks. The dose should then be increased by a maximum of 0.6 mg/kg every 1-2 weeks until the optimal therapeutic effect is achieved. The usual maintenance dose for optimal therapeutic effect is 1 to 10 mg/kg/day in 1 or 2 divided doses, although some patients with typical absence seizures require higher doses to achieve therapeutic effect.

As part of combination therapy when using Lamictal with valproic acid drugs in combination with other AEDs or without them, the initial dose of Lamictal is 0.15 mg/kg body weight 1 time/day for the first 2 weeks, then 0.3 mg/kg 1 time/day over the next 2 weeks. The dose should then be increased by 0.3 mg/kg every 1-2 weeks until the optimal therapeutic effect is achieved. The standard maintenance dose is 1-5 mg/kg/day in 1-2 doses. The maximum daily dose is 200 mg.

As part of combination therapy with concomitant therapy with AEDs or other drugs that induce glucuronidation of lamotrigine (phenytoin, carbamazepine, phenobarbital and primidone), in combination with or without other AEDs (except for valproic acid drugs), the initial dose of Lamictal is 0.6 mg/kg/day in 2 divided doses during the first 2 weeks, then - 1.2 mg/kg/day in 2 divided doses over the next 2 weeks. Then the dose should be increased by a maximum of 1.2 mg/kg/day every 1-2 weeks until the optimal therapeutic effect is achieved. The standard maintenance dose at which the maximum therapeutic effect is achieved is 5-15 mg/kg/day in 2 divided doses. The maximum daily dose is 400 mg.

As part of combination therapy with oxcarbazepine without any other inducers or inhibitors of lamotrigine glucuronidation, the initial dose of Lamictal is 0.3 mg/kg body weight 1 or 2 times a day for the first 2 weeks, then 0.6 mg/kg/day 1 or 2 times a day. 2 doses over the next 2 weeks. Then the dose is increased by a maximum of 0.6 mg/kg every 1-2 weeks until the optimal therapeutic effect is achieved. The standard maintenance dose is 1-10 mg/kg/day in 1 or 2 divided doses. The maximum dose is 200 mg/day.

To ensure that the therapeutic dose is maintained, it is necessary to monitor the child's body weight and adjust the drug dose as it changes.

Due to the risk of developing a rash, the initial dose of the drug and the recommended dose escalation regimen should not be exceeded.

Table 2. Recommended dosage regimen for the treatment of children with epilepsy aged 2 to 12 years (total daily dose in mg/kg body weight).

There is insufficient information on the use of Lamictal in children under 2 years of age .

When discontinuing concomitant antiepileptic drugs to switch to Lamictal monotherapy or when prescribing other drugs or AEDs while taking Lamictal, it is necessary to take into account that this may affect the pharmacokinetics of lamotrigine.

Bipolar disorders

Adult patients over 18 years of age

Due to the risk of developing a rash, the initial dose of the drug and the subsequent dose escalation regimen should not be exceeded.

It is necessary to follow a transitional dosing regimen, which includes increasing the dose of lamotrigine over 6 weeks to a maintenance stabilizing dose (Table 3), after which, if indicated, other psychotropic and/or antiepileptic drugs can be discontinued (Table 4).

Table 3. Recommended dosage escalation schedule to achieve a maintenance daily stabilization dose for adults (over 18 years of age) with bipolar disorders.

The maintenance stabilizing dose varies depending on the clinical effect.

As part of combination therapy with the combined use of Lamictal and other AEDs that inhibit liver enzymes (for example, with valproic acid preparations), Lamictal is prescribed at a dose of 25 mg every other day for the first 2 weeks, then 25 mg 1 time / day for the next 2 weeks, at week 5 the dose should be increased to 50 mg/day in 1-2 doses. The stabilizing dose at week 6 is 100 mg/day in 1-2 doses; however, it may be increased to a maximum daily dose of 200 mg depending on clinical response.

As part of combination therapy with the combined use of Lamictal and other AEDs that induce liver enzymes (for example, carbamazepine, phenobarbital), in patients not receiving valproic acid drugs, during the first 2 weeks Lamictal is prescribed at a dose of 50 mg 1 time / day, for 3 Week 4 - 100 mg/day in 2 divided doses, week 5 - 200 mg/day in 2 divided doses. At week 6, the dose can be increased to 300 mg/day, however, the stabilizing dose to achieve the optimal therapeutic effect is 400 mg/day in 2 doses, and is prescribed starting from week 7.

When using Lamictal monotherapy or as part of combination therapy when using Lamictal together with lithium drugs, bupropion, olanzapine, oxcarbazepine, without the use of inducers or inhibitors of lamotrigine glucuronidation during the first 2 weeks, Lamictal is prescribed at a dose of 25 mg 1 time / day, for 3-4 weeks - 50 mg/day in 1-2 doses, at week 5 - 100 mg/day in 1-2 doses. The stabilizing dose at week 6 is 200 mg/day in 1-2 doses. However, clinical trials used doses ranging from 100 to 400 mg.

After reaching the daily maintenance stabilizing dose, other psychotropic drugs may be discontinued.

Table 4. Maintenance stabilizing total daily dose for the treatment of bipolar disorders after discontinuation of concomitant psychotropic or antiepileptic drugs.

If necessary, the dose can be increased to 400 mg/day.

After discontinuation of additional therapy with inhibitors of lamotrigine glucuronidation (for example, valproic acid), the stabilizing initial dose of lamotrigine is doubled and maintained at this level.

After discontinuation of additional therapy with inducers of lamotrigine glucuronidation (including phenytoin, carbamazepine, phenobarbital, primidone), the dose of lamotrigine is gradually reduced over 3 weeks depending on the initial maintenance dose.

After discontinuation of concomitant psychotropic or antiepileptic drugs that do not have significant pharmacokinetic interactions with lamotrigine (for example, lithium, bupropion, olanzapine, oxcarbazepine), the stabilizing dose of Lamictal achieved during the escalation regimen should be maintained.

There is no clinical experience with adjustment of daily doses of lamotrigine in patients with bipolar disorders after the addition of other drugs. However, based on drug interaction studies, the following recommendations can be made (Table 5).

Table 5. Adjustment of daily doses of lamotrigine in patients with bipolar disorder after adding other drugs to therapy.

During clinical trials of Lamictal for bipolar disorders, abrupt discontinuation of lamotrigine did not cause an increase in the frequency, severity, or nature of adverse reactions compared to placebo. Thus, Lamictal can be discontinued immediately, without gradually reducing the dose.

Lamotrigine is not indicated for bipolar disorder in children and adolescents under 18 years of age . The safety and effectiveness of lamotrigine for bipolar disorder have not been evaluated in patients in this age group.

When prescribing Lamictal to women already taking hormonal contraceptives, special lamotrigine dose escalation regimens have not been developed (despite the fact that hormonal contraceptives increase the clearance of lamotrigine). Dosage escalation regimens should follow recommended guidelines depending on whether lamotrigine is administered with valproic acid (an inhibitor of lamotrigine glucuronidation) or an inducer of lamotrigine glucuronidation; or lamotrigine is prescribed in the absence of valproic acid or inducers of lamotrigine glucuronidation (Table 1 for epilepsy and Table 3 for bipolar disorder).

When prescribing hormonal contraceptives to patients already taking maintenance doses of Lamictal and not taking inducers of lamotrigine glucuronidation, in most cases an increase in the dose of lamotrigine is required, but not more than 2 times. When prescribing hormonal contraceptives, it is recommended to increase the dose of lamotrigine by 50 - 100 mg/day every week, depending on the clinical picture. It is not recommended to exceed these figures unless the patient's clinical condition requires a further increase in the dose of lamotrigine.

When stopping hormonal contraceptives in patients already taking maintenance doses of Lamictal and not taking inducers of lamotrigine glucuronidation, in most cases a lamotrigine dose reduction is required by half. It is recommended to gradually reduce the daily dose of lamotrigia by 50-100 mg every week (reduction of no more than 25% of the daily dose per week) for more than 3 weeks, depending on the clinical picture.

Although lamotrigine plasma concentrations were decreased atazanavir/ritonavir was co-administered Lamotrigine dose increases should be based on recommendations based on whether lamotrigine is added to therapy with valproic acid (an inhibitor of lamotrigine glucuronidation) or therapy with a glucuronidation inducer of lamotrigine, or whether lamotrigine is used in the absence of valproic acid or the glucuronidation inducer lamotrigine.

In patients already taking maintenance doses of lamotrigine and not taking inducers of lamotrigine glucuronidation, the lamotrigine dose may need to be increased when atazanavir/ritonavir is prescribed, and the lamotrigine dose may need to be reduced when atazanavir/ritonavir is discontinued.

dosage adjustment is required in elderly patients (over 65 years of age) (since the pharmacokinetics in this age group do not differ from those in adults).

For moderate (Child-Pugh class B) and severe (Child-Pugh class C) liver dysfunction, the initial, escalating and maintenance doses should be reduced by approximately 50% and 75%, respectively. Incremental and maintenance doses should be adjusted based on clinical response.

For end-stage renal failure, the initial dose of lamotrigine is calculated in accordance with the standard antiepileptic drug regimen. For patients with a significant decrease in renal function, a reduction in the maintenance dose may be recommended.

Lamictal chewable/dissolvable tablets can be chewed, dissolved in a small volume of water (enough to cover the entire tablet), or swallowed whole with a small amount of water.

If the calculated dose of lamotrigine (for example, when prescribed to children or patients with impaired liver function) cannot be divided into a whole number of lower-strength tablets, then the patient should be prescribed a dose that corresponds to the nearest whole tablet at a lower dosage.

When restarting lamotrigine, the physician should evaluate the need to increase the maintenance dose in patients who have discontinued the drug for any reason, as high initial doses and higher than recommended doses are associated with a risk of severe rash. The more time has passed since the last dose of the drug, the more caution you should increase the dose to maintenance. If the time after discontinuation exceeds 5 half-lives, the dose of lamotrigine should be increased to a maintenance dose according to an appropriate dosage regimen.

Lamotrigine therapy should not be restarted in patients whose lamotrigine treatment was discontinued because of rash, unless the potential benefit of such therapy clearly outweighs the potential risk.

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:

1. Violations in the behavior of the drinker - unreasonable aggression, anxiety, depression.
2. Confused speech - words are confused, “tongue is twisted”, sentences are incoherent.
3. Short-term amnesia - a person does not remember events while intoxicated.
4. 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.

Interaction

Combination with hormonal contraceptives (containing levonorgestrel and ethinyl estradiol to a decrease in the effectiveness of the drug and AUC .

Valproates block liver enzymes, slow down the metabolism of the drug, and the drug is excreted from the body almost twice as long.

Medicines that induce liver enzymes , on the contrary, have the ability to accelerate the metabolism of Lamotrigine up to two times. These drugs include: Phenytoin, Phenobarbital, Carbamazepine, Primidone, Paracetamol . Also, when these drugs were taken in combination, ataxia , nausea , dizziness , and diplopia .

The drug does not have the ability to displace other drugs for epilepsy blood plasma proteins .

When the drug is combined with Rifampicin, the clearance of is stimulated and elimination from the body is accelerated.

Lamotrigine: instructions for use, analogues, price, reviews, where to buy

Nervous disorders, mood swings, epileptic attacks or convulsions are common in adults and children. Such symptoms cannot be ignored and urgently need to be treated.

There are a huge number of drugs that normalize the functioning of the nervous system and suppress attacks.

One of these is Lamotrigine , the properties of which will be discussed below.

Analogs

If you are intolerant or unavailable in pharmacies, Lamotrigine can be replaced with other generics of similar action:

1. Based on lamotrigine: Gerolamic tablets, Lamal tablets, Lametol tablets, Lamictal, Lamotridex, Lamotrin, Triginet, Epilactal, Epiral.

2. Based on pregabalin: Algerica in capsules, Gabalin, Galara, Zonic, Linbag, Lugabalin, Neogabin, Pagamax, Pafia, Pregabalin.

3. Based on lacosamide: Vimpat.
4. Based on gabapentin: Gabagamma, Gabantin, Grimodin.

In summary, it should be noted that Lamotrigine is a strong antiepileptic drug that is prescribed to children for epilepsy, and to adults for convulsions, seizures and depression.

This antidepressant has a minimum of contraindications and exhibits virtually no side effects when taken in combination or as monotherapy. The tablets are not sold without a prescription, so they are not suitable for self-medication.

Compound

The generic is available in the form of tablets of 25 mg, 50 mg and 100 mg of the active ingredient.

The composition includes the following substances:

• Lamotrigine is a substance belonging to the group of antiepileptic drugs, presented in powder form, practically insoluble in water;
• lactose is used to correct the taste of tablets, and also has a gliding effect for better passage of the tablet through the digestive tract;
• microcrystalline cellulose is used to accelerate the absorption of the drug;
• starch, magnesium stearate, silicon dioxide are additional ingredients necessary for complete absorption, metabolite and excretion.

Due to this composition, Lamotrigine tablets have a wide spectrum of action:

• have a calming effect on the central nervous system;
• suppresses the pathological release of amino acids that provoke epileptic attacks;
• inhibits depolarization.

You can buy Lamotrigine in Moscow at a pharmacy or online store if you have a prescription from a doctor.

Average cost:

• tablets 25 mg No. 30 – 280 rubles;
• tablets 50 mg No. 30 – 350 rubles;
• tablets 100 mg No. 30 – 450 rubles.

When ordering from an online store, the cost may be slightly lower.

It is recommended to use official websites so as not to purchase a fake, which will not help and will cause additional harm to the body.

Patient reviews

Maria Konstantinovna, 40 years old Moscow:

A dosage of 200 mg per day helped me. when the dose was lowered there was no effect, when the dose was increased, nausea and vomiting occurred, and the head and stomach often hurt.

Olga, 18 years old, Krasnodar:

She stopped taking the medications on her own and ended up in the hospital with fits and seizures. Although I felt great while taking it, I didn’t even experience any adverse reactions from the stomach or heart, etc.

Oleg, 36 years old, Tyumen:

The drug is excellent, I take a dosage of 50 mg per day, without increasing it. I'm happy with everything, I feel good.

The only thing is that when taken in the morning, severe drowsiness begins, so I take the drug in the evenings. I sleep well, there is less aggression, there is practically no depression. The pills also relieve cramps.

Publications in the media

Lamotrigine

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 for adults and children 0.05 g 2 times a day 30-40 minutes before meals or after meals to avoid irritation of the gastric mucosa. 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.

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Side effects

Lamotrigine Canon can cause a number of adverse reactions in case of improper use, non-compliance with the dosage or intolerance to the drug:

1. On the part of the nervous system, sleep disturbances may occur - insomnia or, conversely, excessive drowsiness. In rare cases, dizziness and migraine may occur.

   
   In complex therapy, when exposed to other medications, hallucinations may occur, accompanied by aggressive, inappropriate behavior.

2. The hematopoietic organs may disturb the chemical composition of the blood and manifest anemia, thrombocytopenia, neutropenia, leukopenia.
3. Skin rashes of various types may occur from the subcutaneous tissue. As a rule, they appear within 2 months from the start of therapy. In rare cases, Stevens-Johnson syndrome and Lyell's syndrome have been observed. To avoid the development of an allergic reaction and rash, it is recommended to increase the dosage gradually.

4. On the part of the visual organs, swelling of the eyes, blurred vision (decreased sharpness), redness, drying of the cornea, and conjunctivitis may occur.
5. From the gastrointestinal tract - heartburn, nausea, flatulence, diarrhea.

If the above-described negative reactions occur, you should consult a doctor to adjust the dosage, discontinue or replace the drug.

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.