Lamictal

The antiepileptic, anticonvulsant drug Lamictal is released to the modern pharmaceutical market by the Polish company Glaxo Smith Kline Pharmaceuticals S.A.

"Hercules' disease", "divine disease", "falling sickness" - epilepsy has been called many names over the centuries, but it has remained a problem. It interferes with a person's life, closing the doors to some professions, reducing the quality of life. However, today pharmaceutical companies with their products allow, if not to cure the patient, then significantly improve his condition, and prophylactic use of an anticonvulsant drug, for example, Lamictal, is quite effective in preventing an impending attack. Be more attentive to your health. And if you have a history of the disease in question, do not give up, modern medicine is ready to help. It is only worth remembering that such medications should be prescribed only by an experienced qualified specialist.

Indications Lamictal

Due to the pharmacodynamic features of the active ingredient lamotrigine, the indications for the use of the drug Lamictal are determined:

1. As a monotherapy drug for epilepsy (for minor seizures).
2. Stopping partial and generalized seizures.
3. As a medicine for the complex treatment of epilepsy (in more severe pathological manifestations of the disease).
4. Bipolar disorders.
5. Prevention of disturbances in the patient's emotional state.
6. Treatment of typical absences (short generalized epileptic seizures with sudden, rapid onset and end).
7. Depression in bipolar mental disorders.

[ 1 ], [ 2 ]

Release form

The anticonvulsant drug Lamictal is released to the market of medical drugs in the form of round or rectangular tablets. Tablets are the main form of release of the drug in question.

The tablets of this medicine may be white or yellowish-brown. The shape and color determine the different dosage of the main active substance lamotrigine. The tablet unit of the medicine may contain 5, 25, 50 or 100 mg of the mentioned active chemical compound.

Each tablet has its own fruit aroma and taste (for example, blackcurrant).
Additional chemical compounds that make up Lamictal: hydroxypropyl cellulose, povidone K30, calcium carbonate, sodium glycolate, magnesium stearate, sodium saccharin and fruit flavoring.

[ 3 ]

Pharmacodynamics

Lamictal was created by the manufacturer as an oral antiepileptic, anticonvulsant drug, hence the pharmacodynamics of the drug in question.

The active chemical compound of the drug is lamotrigine (INN - lamotriginum). It is this that determines the direction of the pharmacological properties of the tablets.

The active substance of the drug in question has a depressing effect on potential-dependent sodium channels, blocking their work. Lamotrigine effectively balances the functional instability of neuronal membranes. Reduces the rate of release of glutamic acid, which is dominant in the process of provoking epileptic seizures.

[ 4 ], [ 5 ], [ 6 ]

Pharmacokinetics

But for effective treatment, not only the pharmacodynamics of the drug is important, the attending physician also needs to know the parameters of the drug in terms of the absorption rate and the quality of its elimination from the patient's body. Therefore, before taking any medication, the pharmacokinetics of Lamictal are also assessed by a specialist.

In this case, Lamictal has a high rate of complete absorption by the gastrointestinal mucosa.

The maximum amount of the active active component of the drug in the blood plasma is observed already two and a half hours after oral administration. The bioavailability of Lamictal is estimated at 55%. Lamotrigine in the patient's body is almost completely transformed into its metabolites, the main one of which is N-glucuronide.

The volumes distributed by the body are quite individual, but on average fall within the range of 0.92 to 1.22 l/kg.

On average, the half-life (T _1/2 ) of an adult patient lasts up to 29 hours. Lamictal is excreted from the body in the form of metabolites and in small amounts unchanged (less than ten percent), mainly through the kidneys together with urine and only about 2% with feces. Food intake prolongs T _1/2. This indicator has no effect on the level of adsorption.

In adults, creatinine clearance is approximately 25 to 53 ml/min. Creatinine clearance and half-life are directly related to the dose administered to the body. There are no differences in these values between young and elderly people.

In small patients, creatinine clearance is tied to dosage and body weight. The highest value is found in children under five years of age. The half-life in small patients is somewhat shorter than in adults.

Creatinine clearance differs from the average statistical value in people suffering from chronic renal dysfunction and in those patients who are on hemodialysis. The average values, respectively, show 0.42 ml/min per kilogram of weight and 0.33 ml/min per kilogram of weight (in the interval between extrarenal blood purification) or 1.57 ml/min per kilogram of weight (directly during the hemodialysis procedure).

_{Accordingly, the time T 1/2} changes, which approximately corresponds to:

• For patients with chronic renal failure – 42 hours 55 minutes.
• For patients between hemodialysis sessions – 57 hours 25 minutes.
• For patients during extrarenal blood purification procedure – 13 hours.

Based on this knowledge, the specialist prescribes the schedule and dosage of Lamictal.

Creatinine clearance changes in people with liver dysfunction, depending on the severity of the pathology.

• Mild impairment – on average about 0.31 ml/min per kilogram of weight.
• The average degree of pathology is about 0.24 ml/min per kilogram of weight.
• Severe degree of pathological changes – only about 0.1 ml/min per kilogram of weight.

Based on this, depending on the severity of the disorder, the administered dosage should be adjusted: reduced by up to 50% for mild and moderate disorders and up to 75% for severe disorders.

[ 7 ], [ 8 ]

Dosing and administration

Any medication, including Lamictal, is prescribed and prescribed only by a qualified experienced specialist. Pharmacologists of the manufacturing company offer only the recommended method of administration and dosage, and a more specific schedule of administration and dosage adjustment remains with the attending specialist.

The tablet should not be chewed before swallowing, but should be washed down with a sufficient amount of water.

The drug in question can be used as a single drug in the treatment of epilepsy. The following schedule of administration is recommended for adolescent patients (over 12 years old) and adults:

1. Initial 14 days – 0.025 g once a day, every day.
2. The next 14 days – 0.05 g once a day, every day.
3. Further gradual titration of the dosage until the required clinical efficacy is achieved.

On average, the maintenance dose of Lamictal administered reaches doses from 100 to 200 mg. Some patients achieve the necessary result with a dosage of 500 mg.

If we are talking about a protocol of complex treatment (for example, with the drug sodium valproate), then it is necessary to reduce the amount of lamotrigine taken. Such a schedule of administration may look like this:

1. Initial 14 days – 0.025 g once, every other day.
2. The next 14 days – 0.025 g once daily.
3. Subsequently, the previous dosage is increased daily by 0.025–0.05 g, bringing the administered volumes to the point of obtaining a medicinal effect and regression of pathological symptoms.

On average, the maintenance daily dosage is 100 to 200 mg, divided into two daily doses.

If the treatment protocol includes not two, but more, medications, at least one of which stimulates the work of liver enzymes, it is recommended:

1. The starting dose of Lamictal is 0.05 g per day. The duration of such treatment is two weeks.
2. The next two weeks – 0.1 g, taken daily, but divided into two doses.
3. To maintain the achieved effect, the daily amount of the drug in question is mainly prescribed within the range of 0.2 to 0.4 g.

In antiepileptic therapy for young patients, whose age falls within the age range from two to twelve years, against the background of the introduction of sodium valproate, the schedule of administration and dosage of the antiepileptic drug in question is recommended as follows:

1. The initial daily dose, during the first 14 days, is 0.15 mg per kilogram of the small patient’s weight.
2. Over the next 14 days, this indicator increases and amounts to 0.3 mg per kilogram of the patient’s weight.
3. Subsequently, every subsequent day, the basic dosage is increased by 0.3 mg per kilogram of weight, ultimately bringing it to a value of 1–1.5 mg per kilogram of weight, divided into two daily doses.

In this case, it is necessary to ensure that the calculated amount of the drug does not exceed 0.2 g per day.

If the treatment protocol includes not two, but more, medications, at least one of which stimulates the work of liver enzymes, for children from 2 to 12 years old it is recommended:

1. The initial daily dose, during the first 14 days, is 0.6 mg per kilogram of the small patient’s weight.
2. Over the next 14 days, this indicator increases and amounts to 1.2 mg per kilogram of the patient’s weight.
3. Further gradual titration of the dosage until the required stable clinical efficacy is achieved.

When a patient is diagnosed with bipolar disorder while taking anticonvulsants, the following schedule of administration of Lamictal is recommended:

1. Initial 14 days – 0.025 g once, every other day.
2. The next 14 days – 0.025 g once daily.
3. The maintenance daily dosage is 0.1 g.

In this case, it is necessary to ensure that the maximum amount of lamotrigine administered does not exceed 0.2 g daily.

Particular caution should be exercised in the following clinical cases:

1. If the patient suffers from serious disorders in the excretory system (kidneys, ureters, etc.).
2. If the patient has a history of liver failure, the amount of Lamictal administered is reduced by half. If this pathology is considered severe, the dose can be reduced by 75%.
3. To avoid withdrawal symptoms, do not suddenly stop taking the antiepileptic drug. A gradual reduction in dosage usually takes a couple of weeks. The exception is a threat to the patient's life.
4. The drug in question should not be introduced into the treatment protocol if a drug containing lamotrigine has already been prescribed.

When taking Lamictal, you should not drive vehicles and/or operate complex machinery that requires increased attention.

[ 12 ], [ 13 ]

Use Lamictal during pregnancy

When a woman is in an "interesting position" or in the postpartum period breastfeeds a newborn baby, she tries to take any medications as rarely and in smaller quantities as possible. This is due to her fear of harming the fetus or the already born baby. The use of the antiepileptic, anticonvulsant drug Lamictal during pregnancy has not been determined. This is due to the fact that there is no data and no results of such clinical studies.

Theoretically, doctors can assume a high possibility of Lamictal influencing the development of the fetus, causing congenital anomalies. This conclusion is based on the ability of lamotrigine to inhibit the synthesis of the enzyme dihydrofolate reductase.

There is no data on the ability of Lamictal to penetrate into breast milk.

Therefore, if the question of treating a pregnant woman with the medication in question arises, this issue is resolved individually based on the degree of medical necessity. During lactation, in order not to risk the baby's health, it is better to stop breastfeeding and transfer the newborn to adapted formulas.

Contraindications

There is practically no medicine that would not have contraindications for use. Lamictal has such a list. It is small, since the drug in question is quite easily perceived and processed by the human body.

1. Increased individual intolerance of the patient's body to one or more components of the drug in question.
2. Also, the medication itself and its dosage should be prescribed with great caution to patients with renal and/or hepatic insufficiency.

[ 9 ], [ 10 ], [ 11 ]

Side effects Lamictal

Incorrect dosage prescription, deviation from the schedule of administration or incorrectly maintained dose, individual sensitivity to a specific chemical compound and side effects of Lamictal may appear.

According to statistical processing of monitoring results, patients most often encounter the following pathological symptoms:

1. Exanthematous wounds of allergic etiology may appear on the skin, up to the development of Stevens-Johnson syndrome or Lyell's epidermal necrolysis.
2. Development of lymphadenopathy (enlargement of the lymph nodes).
3. Manifestation of a delayed-type hypersensitivity reaction (DTH).
4. Intravascular sludge (smoothing of characteristics) of blood cellular structures.
5. A decrease in the number of cellular structures of hematopoietic sprouts in the blood.
6. Deterioration of vision.
7. Increased excitability of receptors of the central nervous system, up to and including loss of consciousness.
8. Development of multiple organ failure syndrome.
9. If you suddenly stop taking Lamictal, withdrawal symptoms may occur, leading to seizures.
10. Problems with defecation may occur.
11. The enzymatic activity of the liver decreases.
12. Rhabdomyolysis is the destruction of muscle tissue cells and the manifestation of a number of other pathologies.

Overdose

If a person does not strictly adhere to the schedule and dosage of taking the drug Lamictal prescribed in the therapy protocol, as well as due to individual sensitivity to a specific chemical compound, the amount of the chemical substance entering the body may be exceeded. An overdose of the leading active chemical component lamotrigine can manifest itself in the following pathological symptoms:

1. Dizziness.
2. Nausea.
3. Visual impairment.
4. Lack of coordination of movements.
5. Loss of consciousness.
6. Cranialgia is a headache caused by problems in the cervical spine.

The relief of such pathological symptoms occurs through detoxification of the patient's body: gastric lavage, administration of adsorbent substances (for example, activated carbon).

[ 14 ], [ 15 ], [ 16 ], [ 17 ]

Interactions with other drugs

If the patient's health condition does not cause concern and the treatment affects the problem of epileptic seizures only, then Lamictal can be taken alone, then the patient only needs to monitor his condition and, in the event of side effects, seek advice from his attending physician.

But such a situation, as a rule, occurs quite rarely, much more often sick people take several drugs at the same time, belonging to different pharmacocolonic groups. Therefore, in order to get the expected result and not harm the patient's body, the specialist prescribing the treatment must clearly understand what clinical picture can be obtained in the end with the joint work of two or more pharmacological drugs. Here, knowledge of the interaction with other drugs of Lamictal is mandatory.

But there is not yet sufficiently extensive knowledge and research results on this issue.

It is only known that when the anticonvulsant drug in question is administered together with a drug such as sodium valproate, the metabolite of the latter, obtained through the work of liver enzymes, reduces the patient’s body’s ability to absorb the constituent chemical compounds of Lamictal.

The combined action of an antiepileptic drug and carbamazepine can provoke rapid development of side pathological symptoms.
As clinical observations have shown, taking hormonal contraceptives can activate the process of lamotrigine metabolism and its elimination from the body by two times.

A similar result was achieved with the tandem administration of Lamictal and paracetamol, as well as drugs of its own (antiepileptic) pharmacological group.

[ 18 ], [ 19 ], [ 20 ]

Storage conditions

In order for the treatment to bring the maximum therapeutic effect, in addition to following all the recommendations of the doctor treating the disease, you should read the instructions and learn the storage conditions of Lamictal. If it is stored incorrectly, the active ingredient lamotrigine may lose or significantly reduce its pharmacodynamic characteristics. Therefore, before starting therapeutic treatment, you should carefully read the instructions attached to any pharmacological product.

If all recommendations are followed, one can be sure that the level of pharmacodynamic activity of the anticonvulsant drug will remain high throughout the entire permitted shelf life.

The requirements for storage are in many ways consistent with the set of recommendations that apply to the storage of most medicines:

1. The room where the drug in question is supposed to be stored should not be exposed to direct sunlight.
2. The humidity in the room should be moderate.
3. The storage temperature should not be higher than +30 degrees.
4. Lamictal should be kept in places that are inaccessible to teenagers and small children.

Shelf life

Any product released by a corporation - manufacturer entering the pharmacy market is necessarily provided with date indicators on the packaging material indicating when this anticonvulsant was produced. Another number is the final date, after which the medicine provided with this instruction should not be used as an effective antiepileptic drug.

In this case, the shelf life of the antiepileptic, anticonvulsant drug Lamictal is three years (or 36 months).

[ 21 ], [ 22 ]