General purpose anticonvulsants. Anticonvulsants and antiepileptic drugs

The activation of a nerve impulse simultaneously by a group of certain neurons is similar to the signal given by motor-type neurons in the cerebral cortex. In the event of a lesion of this type, the nerve endings do not appear in tics or convulsions, but cause bouts of pain.

The purpose of the use of anticonvulsants is to eliminate pain or muscle spasms without provoking oppression of the central nervous system. Depending on the complexity of the disease, these drugs can be used from several years to lifelong use in severe chronic or genetic forms of the disease.

Attacks of convulsive activity are associated with an increase in the degree of excitation of nerve endings in the brain, usually localized in certain areas of its structure and diagnosed upon the onset of a condition characteristic of the onset of a convulsive syndrome.

The cause of seizures can be a deficiency in the body of essential chemical elements, such as magnesium or potassium, pinching of a muscle nerve in the canal, or a sharp prolonged exposure to cold. Deficiency of potassium, calcium or magnesium provokes failures in the transmission of signals to the muscles from the brain, as evidenced by the occurrence of spasms.

In the initial stage, the manifestation of the development of a neurological type of disease consists in local pain sensations emanating from the area of ​​the affected nerve cells and manifested by bouts of pain of varying strength and nature of manifestation. With the course of the disease due to the development of inflammatory processes or muscle spasms in the area of ​​pinched nerve endings, the strength of the attacks increases.

In the case of an early appeal to a specialist, a complex of drugs is used for therapy, eliminating the causes and signs of damage to the nerve endings. Self-diagnosis and treatment does not allow choosing from a wide range of anticonvulsants the most suitable for stopping pain symptoms and eliminating the cause of discomfort.

When observed by a specialist, he evaluates the work of the prescribed drug by its effectiveness and diagnoses the absence of pathological changes after taking it according to the results of blood tests.

Fundamentals of anticonvulsant therapy

The composition of complex treatment for convulsive manifestations includes groups of drugs of various principles of action, including:

• non-steroidal medications with anti-inflammatory action, reducing temperature and eliminating pain, and a feeling of discomfort after inflammation has been eliminated;
• tablets for neuralgia of the antiviral type are used to prevent the onset of disorders or reduce the degree of pain in case of occurrence;
• drugs of the analgesic group, which have an analgesic effect, are used to eliminate pain in a strictly dosed amount to eliminate the occurrence of side effects;
• means for eliminating muscle spasms with manifestations of a paroxysmal nature, belonging to the group of muscle relaxants;
• external agents in the form of ointments and gels for treating affected areas or injections for stopping the manifestation of muscle spasms;
• drugs that normalize the functioning of the nervous system and sedatives;
• anticonvulsant type drugs, the action of which is based on the elimination of pain symptoms by reducing the activity of nerve cells, these drugs are most effective when the source of pain is concentrated in the brain or spinal cord, and less so for the treatment of peripheral nerve disorders.

Some of the prescribed drugs have the effect of inhibiting the development or preventing the occurrence of allergic-type reactions.

The main groups of anticonvulsants

Anticonvulsants are divided into several groups, a list of which is offered below.

Iminostilbenes

Iminostilbenes are characterized by an anticonvulsant effect, after their use, pain symptoms are eliminated and mood is improved. The drugs in this group include:

• Carbamazepine;
• Finlepsin;
• Tegretol;
• Amizepine;
• Zeptol.

Sodium valproate and derivatives

Valproates, used as anticonvulsants and as iminostilbenes, help to improve the emotional background of the patient.

In addition, when using these drugs, tranquilizing, sedative and muscle relaxant effects are noted. The drugs in this group include:

Barbiturates

Barbiturates are characterized by a sedative effect, help lower blood pressure and have a hypnotic effect. Among these drugs, the most commonly used are:

Benzodiazepines

Anticonvulsants based on benzodiazepine have a pronounced effect, they are used in the event of the appearance of convulsive conditions in epilepsy and prolonged attacks of neuralgic disorders.

These drugs are characterized by sedative and muscle relaxant effects, with their use, normalization of sleep is noted.

Among these drugs:

Succiminides

Anticonvulsants of this group are used to eliminate spasms of the muscles of individual organs with neuralgia. When using drugs in this group, sleep disturbances or nausea are possible.

Among the most used means are known:

Anticonvulsants used for leg cramps:

Hitting the nine convulsive "gates"

The main anticonvulsants that are most often used for epilepsy, convulsive seizures and neuralgia of various origins:

1. Finlepsin is used in cases of neurological diseases with lesions of the trigeminal and glossopharyngeal nerves. It has analgesic properties, anticonvulsant, antidepressant effects. The principle of action of the drug is based on calming the membrane of nerves with a high degree of excitation by blocking sodium channels. The drug is characterized by complete absorption by the intestinal walls for a sufficiently long time. Among the contraindications to the use of the drug are poor tolerance to Carbamazepine and increased eye pressure.
2. Carbamazepine is used as an anticonvulsant in the treatment of trigeminal neuralgia and has an antidepressant effect. The start of the drug should be gradual as the dose of the previous drug is reduced. Preparations containing Phenobarbital reduce the effectiveness of Carbamazepine, which must be taken into account when prescribing complex treatment.
3. Clonazepam is characterized by an anticonvulsant effect and is used to treat neuralgia with alternating myoclonic attacks. It has pronounced sedative and hypnotic effects. Possible side effects when using the drug are a violation of the functions of the musculoskeletal system, loss of concentration and mood disorders. The remedy eliminates the feeling of anxiety, has a hypnotic effect, a sedative and relaxing effect on the patient's body.
4. Phenytoin is used in cases of convulsive statuses with an action based on slowing down nerve endings and fixing membranes at the cellular level.
5. Voltaren is used as an anticonvulsant for neurological disorders in the spine.
6. Ketonal is used to reduce pain symptoms on the body that have different localization areas. When prescribing a drug for therapy, it is necessary to take into account the possible intolerance of the components and, as a result, the risk of developing cross-type allergies.
7. Sodium valproate is used in cases of seizures associated with the therapy of mild forms, the epileptic nature of muscle contraction. The drug reduces the production of electrical impulses sent by the nervous system from the cerebral cortex, normalizes the state of the patient's psyche. Possible side effects of the drug are violations of the digestive system, changes in blood clotting.
8. Benzobamil, used for focal seizures, is characterized by low toxicity and high efficiency in providing a sedative effect. Side effects of using the remedy are a state of weakness, a reduced emotional background, which is reflected in the degree of activity of the patient.
9. Phenobarbital is prescribed for children, has a sedative effect, is characterized by a hypnotic effect. May be used in combination with other agents, such as vasodilators for nervous system disorders.

Practical experience of consumers

What is the situation with anticonvulsant therapy in practice? This can be judged by the reviews of patients and doctors.

I take Carbamazepine as a replacement for Finlepsin, since the foreign analogue is more expensive, and the domestic drug is excellent for therapy with my illness.

Since I tried both drugs, I can say that both drugs are highly effective, but a significant difference in cost is a significant disadvantage of a foreign remedy.

After several years of taking Finlepsin, on the advice of a doctor, I changed it to Retard, since the specialist believes that this drug is more suitable for me. I had no complaints while taking Finlepsin, however, in addition to a similar action, Retard has a sedative effect.

In addition, the drug is characterized by great ease of use, since, compared with analogues, it must be taken not three times a day, but once.

The drug Voltaren helps with pain syndromes of moderate severity. It is good to use it as an addition to the main treatment.

Time to collect stones

A distinctive feature of anticonvulsants is the impossibility of a quick end of their intake. With a noticeable effect from the action of the drug, the term for canceling its use is up to six months, during which there is a gradual decrease in the rate of taking the drug.

According to the popular opinion of doctors, the most effective drug for the treatment of seizure activity is Carbamazepine.

Less effective are drugs such as Lorazepam, Phenytoin, Relanium, Seduxen, Clonazepam, Dormicum and valporic acid, arranged in order of decreasing therapeutic effect.

It remains to be added that it is impossible to obtain anticonvulsants without prescriptions, which is good, since it is very dangerous to take them irresponsibly.

This section was created to take care of those who need a qualified specialist, without disturbing the usual rhythm of their own lives.

Hello, I am a disabled person with epilepsy, I take the anticonvulsant drugs carbamazepine when I took this drug, I felt better, and how carbamazepine disappeared in pharmacies and finlepsin appeared again, I had to take it again and I began to get sick again, the attacks became more frequent, I began to feel weak, my head does not work return the drug carbamazepine to the pharmacy as expected. this drug is not strictly registered, please return the carbamazepine.

Convulsions of various origins in children occur six times more often than in adults. They can be the result of dehydration of the body, imbalance of fluid and minerals, a critical deficiency of potassium and magnesium, hypothermia, poisoning, intoxication, epilepsy, pinched nerve in the canal, and so on. Seizures require immediate intervention, especially if they occur in babies of the first two years of life, because if the spasms are not eliminated in time, this is fraught with serious damage to the baby's central nervous system, cerebral edema. Anticonvulsants come to the rescue.

Anticonvulsants for children are prescribed in combination with other medicines (anti-inflammatory, analgesics, antiviral, sedatives) after identifying the cause of seizures.

To do this, the doctor will carefully study the full picture of the disease, take into account at what time of day the seizures most often occur with the child, how often they occur, what provokes them. Treatment usually takes place in a hospital under the constant supervision of doctors.

Therapy with anticonvulsant drugs will also require a lot of additional research - ECG, MRI, etc.

How do they act?

Anticonvulsants act on the central nervous system, suppressing it, due to this, it is possible to stop convulsive spasms. However, some representatives of anticonvulsants have an additional effect - they depress the respiratory center, and this can be very dangerous for children, especially small ones. Barbiturates, magnesium sulfate are considered such depressant drugs against convulsions.

Benzodiazepines, droperidol with fentanyl, and lidocaine are considered drugs that have little effect on the child's breathing.

With the help of relatively sparing benzodiazepines ("Sibazon", "Seduxen"), convulsions of any origin can be dealt with. They prevent the spread of nerve impulses in the brain and spinal cord.

Droperidol with fentanyl is quite commonly used to treat children.

Lidocaine, with rapid intravenous administration, stops any convulsions by acting at the cellular level - ions begin to penetrate the cell membrane more easily.

Among the barbiturates, the most famous are Phenobarbital, Hexenal. "Phenobarbital" acts for a long time, but the effect of taking it is not achieved immediately, and when stopping seizures, it is time that sometimes plays a decisive role. Moreover, with age, the effect of the drug is achieved faster. In babies up to a year, it occurs only 5 hours after ingestion, and in children older than two years, Phenobarbital is absorbed from the gastrointestinal tract twice as fast.

They try not to prescribe "Geksenal" to children, since it has a very strong effect on the respiratory system, suppressing it like anesthetics.

Magnesium sulfate in pediatrics is also used infrequently, mainly in the elimination of seizures associated with cerebral edema, magnesium imbalance.

The most important factor in the treatment of seizures in children is the determination of the optimal dose of the drug. It is calculated strictly individually, experts try to start treatment with small doses, gradually increasing them as needed.

The most difficult question to answer is how long the course of treatment with anticonvulsants lasts. There is no single standard, since the child needs to take them either until complete recovery, or all his life if convulsions are associated with severe hereditary pathologies.

Classification

According to the method of exposure and the active substance, all anticonvulsants are divided into several groups:

• Iminostilbenes. Anticonvulsant drugs with excellent analgesic and antidepressant effects. Improve mood, eliminate muscle spasms.
• Valproates. Anticonvulsants, which have the ability to relax muscles, while providing a sedative effect. They also improve mood and normalize the psychological state of the patient.
• Barbiturates. They perfectly stop convulsions, at the same time lower blood pressure and have a rather pronounced hypnotic effect.
• Succiminides. These are anticonvulsant drugs that are indispensable in cases where it is tedious to eliminate spasms in individual organs, with neuralgia.
• Benzodiazepines. With the help of these medicines, long-term convulsive seizures are suppressed, drugs are prescribed for epilepsy.

Children's anti-seizure drugs must meet several important criteria. They should not have an overwhelming effect on the psyche, should not be addictive and addictive, while the medicines must be hypoallergenic.

Parents have neither the moral nor the legal right to choose such serious drugs for children on their own. All anticonvulsants in Russian pharmacies are sold only upon presentation of a prescription, which is issued by a doctor after establishing the causes of convulsive conditions.

List of anticonvulsant medicines for children

"Carbamazepine". This antiepileptic drug from the category of iminostibens has a lot of advantages. It reduces pain in those who suffer from neuralgia. Reduces the frequency of seizures in epilepsy, after several days of taking the drug, there is a decrease in anxiety, a decrease in aggressiveness in adolescents and children. The drug is absorbed slowly enough, but it acts completely and for a long time. The tool is available in tablets. "Carbamazepine" is prescribed to children from 3 years.

"Zeptol". An antiepileptic drug such as iminostilbenes improves mood by suppressing the production of norepinephrine and dopamine, and relieves pain. The drug is prescribed for epilepsy, trigeminal neuralgia. The drug is produced in the form of tablets. Children can be given medicine from the age of three.

"Valparin". Anticonvulsant drug of the vaoproate group. The drug does not depress breathing, does not affect blood pressure, has a moderate sedative effect. "Valparin" is prescribed in the treatment of epilepsy, with convulsions associated with organic brain lesions, with febrile convulsions (convulsions at high temperature in children from birth to 6 years).

"Apilepsin". This anticonvulsant drug is prescribed not only for the treatment of epilepsy, but also for children's tics, as well as for febrile convulsions in babies. The drug is available in the form of drops for oral administration, tablets, dry matter for intravenous injections and droppers, as well as in the form of syrup. Children under 3 years of age can take the medicine in syrup. Starting from 3 years, other forms of the drug are allowed.

"Convulex". The anticonvulsant drug of the vaoproate group has a mild sedative effect and the ability to relax muscles. The drug allows you to cope with a wide range of seizures of various origins from epileptic to febrile. In addition, Konvuleks is prescribed for children who have bipolar disorders. The release forms are different - from dry matter for the subsequent preparation of injections to capsules and tablets. The so-called "children's" forms of medicine - drops for oral administration and syrup. Capsules and tablets are contraindicated in children under 3 years of age. They can only be given liquid forms of Convulex.

"Phenobarbital". This anticonvulsant belongs to the category of barbiturates. It depresses some areas of the cerebral cortex, including the respiratory center. Has a hypnotic effect. The drug will be prescribed to a child in the treatment of epilepsy, severe sleep disorders, with spastic paralysis, with a number of seizures not associated with manifestations of epilepsy. Available in tablets. Can be assigned to children from birth.

"Clonazepam". The brightest representative of the group of benzodiazepines. Approved for use in children of any age with epilepsy, nodding convulsions, atonic seizures. Available in tablets and in solution for intravenous administration.

"Sibazon" - a tranquilizer with an anticonvulsant effect. May lower blood pressure. It is used for muscle cramps of various origins. Available in tablets and solution for intravenous injection. It is used to relieve epileptic seizures and febrile convulsions in children from the age of one.

In addition, Antilepsin, Ictoril, Rivotril, Pufemid, Ronton, Etimal and Sereysky Mix are effective against children's seizures.

What can't be done?

If your child has seizures, don't try to figure out the cause yourself. Call an ambulance, and while you are waiting for the doctors, carefully observe the baby - what kind of convulsions does he have, how great is the pain syndrome, pay attention to the duration of convulsive spasms. All this information will be useful later for specialists to establish the correct diagnosis.

Do not give your child any anticonvulsant drugs. Also, do not give the baby water and food, because their particles can get into the respiratory tract and cause suffocation.

Do not try to get the child's tongue. This is a common misconception. The baby will not swallow the tongue, but it is possible to suffocate from the fact that fragments of teeth, injured when trying to open the jaw, get into his airways.

Do not hold a child in a state of convulsions in one fixed position. This can cause serious joint injuries, sprains, and muscle ruptures.

The well-known pediatrician Komarovsky tells in detail about convulsions:

Advice to parents from a doctor of the Union of Pediatricians of Russia:

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Anticonvulsants - List of drugs and medicines

Description of the pharmacological action

Potentiates GABA-ergic transmission in the CNS: inhibits GABA reuptake, increases (by 60-70%) the concentration and time of its stay in the synaptic cleft of neuronal and glial cells.

Search for a drug

Drugs with pharmacological action "Anticonvulsant"

• Actinerval (tablets)
• Alprox (tablets)
• Apo-Carbamazepine (oral tablets)
• Apo-Lorazepam (oral tablets)
• Benzobarbital (Substance-powder)
• Benzonal (Substance-powder)
• Benzonal (oral tablets)
• Berlidorm 5 (Pills oral)
• Bromidem (oral tablets)
• Valium Roche (oral tablets)
• Valparin XP (oral tablets)
• Gabitril (oral tablets)
• Gapentek (Capsule)
• Hexamidine (Substance)
• Hexamidine (Substance)
• Hexamidine (oral tablets)
• Geminevrin (Capsule)
• Gopantam (oral tablets)
• Diazepam Nycomed (Solution for intravenous and intramuscular administration)
• Diazepam Nycomed (Pills, oral)
• Diazepex (oral tablets)
• Diapam (oral tablets)
• Difenin (Substance-powder)
• Difenin (oral tablets)
• Dormicum (Solution for intravenous and intramuscular administration)
• Dormicum (oral tablets)
• Zagretol (oral tablets)
• Carbamazepine Nycomed (oral tablets)
• Carbapine (oral tablets)
• Karbasan retard (Pills, oral)
• Keppra (Concentrate for solution for infusion)
• Keppra (oral tablets)
• Keppra (oral solution)
• Clonazepam (oral tablets)
• Clonotril (oral tablets)
• Xanax (oral tablets)
• Lameptil (effervescent tablets)
• Lamictal (oral tablets)
• Lamictal (chewable tablets)
• Lamitor (oral tablets)
• Lamitor DT (Effervescent Tablets)
• Lamolep (oral tablets)
• Lamotrigine (Substance powder)
• Lamotrix (oral tablets)
• Lepsitin (Capsule)
• Magnesium sulfate (Powder for oral suspension)
• Magnesium sulfate (Substance-powder)
• Magnesium sulfate (Solution for infusion)
• Magnesium sulfate (Solution for injection)
• Magnesium sulfate-Darnitsa (Solution for injection)
• Mazepin (oral tablets)
• Maliazin (Dragee)

• Misolin (Pills oral)
• Napoton (Dragee)
• Neurox (Solution for intravenous and intramuscular administration)
• Neurotropin (Solution for injection)
• Neurol (oral tablets)
• Nitrazadone (oral tablets)
• Nitrazepam (oral tablets)
• Nitrazepam (Substance-powder)
• Nitram (oral tablets)
• Nitrosan (oral tablets)
• Nobritem (Capsule)
• Pantogam Active (Capsule)
• Primidon (Substance-powder)
• Radenarcon (Solution for injection)
• Relanium (Solution for intravenous and intramuscular administration)
• Relium (Solution for intravenous and intramuscular administration)
• Relium (oral tablets)
• Rivotril (Solution for intravenous administration)
• Rivotril (oral tablets)
• Rohypnol (oral tablets)
• Rohypnol (Solution for injection)
• Seduxen (Solution for injection)
• Seduxen (oral tablets)
• Sibazon (Solution for intravenous and intramuscular administration)
• Sibazon (Substance-powder)
• Sibazon (tablets)
• Stazepine (tablets)
• Storylat (tablets)
• Suxilep (Capsule)
• Tazepam (oral tablets)
• Tebantine (Capsule)
• Tegretol (Syrup)
• Tegretol (oral tablets)
• Tranxen (Capsule)
• Fezipam (oral tablets)
• Phenazepam (Solution for intravenous and intramuscular administration)
• Phenazepam (Substance-powder)
• Phenazepam (oral tablets)
• Phenorelaxan (Solution for intravenous and intramuscular administration)
• Phenorelaxan (oral tablets)
• Phenotropil (Substance-powder)
• Phenotropil (Pills, oral)
• Flormidal (Solution for injection)
• Flormidal (oral tablets)
• Chloracon (oral tablets)
• Chloracon (Substance-powder)
• Celandine grass (Vegetable raw material)
• Egipentine (Capsule)
• Egipentine (oral tablets)
• Elenium (Pills, oral)
• Eunoctin (oral tablets)

Attention! The information provided in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. Descriptions of drugs are provided for informational purposes only and are not intended for prescribing treatment without the participation of a doctor. There are contraindications. Patients need specialist advice!

If you are interested in any other Anticonvulsants and drugs, their descriptions and instructions for use, synonyms and analogues, information on the composition and form of release, indications for use and side effects, methods of application, dosages and contraindications, notes on the treatment of children with medicine, newborns and pregnant women, price and reviews of medicines, or if you have any other questions and suggestions - write to us, we will definitely try to help you.

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Anticonvulsants

The action of anticonvulsants

The action of anticonvulsants is aimed at eliminating muscle spasms and epileptic seizures. Some of these drugs are taken in combination for best results. They not only relieve convulsions, but also facilitate the general condition of the body. The first attempts at such treatment were made at the end of the 9th and beginning of the 20th century. Then, potassium bromide was used to combat seizures. Since 1912 they began to use Phenobarbital. Since 1938, the list has been replenished with Phenytoin. Currently, modern medicine uses more than thirty drugs. Today, more than 70% of people suffer from mild epilepsy and are successfully treated with anticonvulsants. However, the treatment of severe forms of the disease remains one of the most urgent problems for scientists. Any prescribed medicine must have anti-allergic properties in the absence of effects on the central nervous system. It is also necessary to exclude addiction, a feeling of apathy and weakness.

The main task of each remedy is to eliminate spasms without suppressing the central nervous system of psychophysical disorders. Any drug is prescribed only by a doctor after a comprehensive examination and a part of the brain. Taking anticonvulsant drugs can last for several years, and in some cases throughout life. This happens in the case of severe heredity or a chronic form of the disease. In some situations, in addition to drug therapy, surgery is done on the affected area of ​​the brain.

Groups of anticonvulsants

Modern medicine classifies anticonvulsants according to the following scheme:

• barbiturates;
• hydantoin preparations;
• oxazolidiones;
• drugs based on succinamide;
• iminostilbenes;
• benzodiazepine tablets;
• valproic acid products

Anticonvulsant drugs list

The main anticonvulsants are:

1. Phenytoin. It is used for convulsive seizures with status epilepticus. Its action is aimed at inhibiting nerve receptors and stabilizing membranes at the level of the cell body. The drug has a number of side effects: nausea, trembling, vomiting, involuntary rotation of the eyes, dizziness.
2. Carbamazeline is used for major convulsive psychomotor seizures. It stops severe attacks in the active stage of the disease. During the reception, the patient's mood improves. But there are a number of side effects: impaired blood circulation, drowsiness, dizziness. Contraindications are pregnancy and allergies.
3. Phenobarbital is used in epileptic seizures in conjunction with other drugs. The medicine calms and normalizes the nervous system. Pego should be taken for a long time. Cancellation occurs very carefully and gradually, as the elements of the drug accumulate in the body. Among the side effects of blood pressure disorders, difficulty breathing. Do not use during lactation and in the first trimester of pregnancy. It is also forbidden to use with kidney failure, with muscle weakness and alcohol dependence.
4. Clonazepam is used for myoclonic epilepsy and psychomotor seizures. The drug eliminates involuntary convulsions and reduces their intensity. Under the influence of tablets, the muscles relax and the nervous system calms down. Among the side effects are a disorder of the musculoskeletal system, fatigue, irritability, and a protracted depressive state. Contraindication to use is hard physical work that requires increased concentration, pregnancy, kidney failure and liver disease. During treatment, it is imperative to refrain from drinking alcohol.
5. The action of the drug Lamotrigine is aimed at eliminating severe seizures, mild seizures and clonic and tonic convulsions. It stabilizes the activity of brain neurons, which leads to a reduction in seizures and eventually they completely disappear. A side effect can be in the form of a skin rash, nausea, dizziness, diarrhea, tremor. It is not recommended during the treatment period to engage in physical work that requires increased concentration.
6. Sodium volproate is indicated for the treatment of severe psychomotor seizures, mild seizures, and myoclonic epilepsy. The drug reduces the production of electrical impulses of the brain, eliminates anxiety and stabilizes the mental state of the patient. Side effects are expressed by disorders of the gastrointestinal tract, circulatory disorders and blood clotting. You can not take the medicine during pregnancy and lactation, with diseases of the pancreas, as well as hepatitis in various forms.
7. Primidone is used for psychomotor seizures and myoclonic epilepsy. The action of the drug inhibits the activity of neurons in the damaged area of ​​the brain and eliminates involuntary spasms. Due to the fact that the drug causes increased arousal, it is not prescribed to children and the elderly. Side effects include: nausea, allergies, anemia, headaches, apathy and addiction. Contraindicated use during pregnancy and lactation, as well as liver disease and renal failure.
8. Beklamid stops generalized and partial seizures. It blocks electrical impulses in the head, reduces excitability and eliminates convulsions. Side effects include dizziness, gastrointestinal irritation, weakness, and allergies. Use is contraindicated in case of hypersensitivity to the components of the drug.
9. Benzobamil is prescribed for children with epilepsy, as well as for focal seizures. This is the least toxic drug that has a sedative effect on the central nervous system. Side effects include weakness, nausea, lethargy, and involuntary eye movements. Treatment with the drug is contraindicated in heart, kidney failure and liver disease.

Non-prescription anticonvulsants

Anticonvulsants are prescribed only by a doctor for the treatment of serious diseases, so they can only be purchased with a prescription. Of course, you can try to buy them without a prescription, but this can seriously harm your health. If you order some medicines in an online pharmacy, then often you will not be asked for a prescription.

Anticonvulsants for the legs

If there is no epilepsy and inflammation of the nerves in the history of the disease, then the following drugs are prescribed for the treatment of convulsions:

1. Valparin suppresses convulsive activity in epileptic seizures. It does not have a pronounced sedative and hypnotic effect.
2. Xanax is a psychotropic drug that eliminates feelings of anxiety, fear and emotional tension. It has a moderate sedative effect.
3. Difenin has a muscle relaxant and anticonvulsant effect. It increases the pain threshold for neuralgia and reduces the duration of convulsive attacks.
4. Antinerval relieves convulsions, depression and anxiety. It is also used to prevent depressive disorders.
5. Keppra is an anti-epileptic drug designed to suppress neuronal firing and relieve seizures.

In no case should you take these medicines on your own, since the cause of seizures can be hypothermia, trauma, flat feet, or a lack of certain vitamins.

Anticonvulsants for children

Anticonvulsant therapy for children provides an individual approach to each small patient. The frequency of attacks, at what time they occur, the overall clinical picture is taken into account. An important point in the treatment is the correct selection of medication and dose. Proper treatment helps in many cases to completely get rid of seizures. At first, small doses of the drug are prescribed, which gradually increase. It is necessary to keep accurate records of seizures and monitor their dynamics. Convulsive seizures in infants and toddlers are always an indication for emergency treatment. Delay can lead to swelling of the brain and damage to vital functions in the body. Initially, a 20% glucose solution is administered intravenously. If convulsions continue, then very carefully, controlling the work of the heart muscle, a 25% solution of magnesium sulfate is administered. If the effect does not occur, then pyridoxine hydrochloride is prescribed. The main drug is Phenobarbital. It calms the baby and has a dehydrating effect. The drug is prescribed according to age doses and depending on the nature and frequency of attacks. If after two or three days there is no improvement, then sodium bromide, Caffeine or Benzonal are added. In some cases, treatment is combined with the appointment of Difenin. It does not have cumulative properties, it can give side effects in the form of decreased appetite, nausea, irritation on the oral mucosa, stomatitis. Children with frequent seizures are sometimes prescribed Hexamidin in combination with Phenobarmital and Definin. In inhibited babies, such treatment significantly improves the condition. Contraindications are diseases of the kidneys, liver and blood-forming organs. At an early age, treatment with a mixture of Sereysky or its modifications is often prescribed. The main components of the drug are caffeine, papaverine, luminal.

Probably everyone at least once in his life experienced what a cramp is. These are involuntary brain symptoms that can lead to impaired consciousness, emotional disturbances, or strong fibers in the arms or legs.

If you have seizures quite often, then this is the reason why you urgently need to see a doctor. They can signal serious diseases not only in the nervous system, but also in other organs. After the examination, the doctor will definitely prescribe the appropriate treatment, which will include anticonvulsants, in order to reduce the frequency of seizures.

Causes of convulsive conditions

Convulsions can appear in a person at different periods of life, the most common causes of such conditions include:

In order to get rid of such problems, it is necessary to accurately determine their cause, because in each case, anticonvulsants are prescribed individually.

Varieties of seizures

It is possible to give the following classification of convulsive conditions:

1. Generalized convulsions. They most often capture the entire body, as, for example, during epileptic seizures.

• clonic. There is a change in muscle tension, twitching is observed.
• tonic. Spasm of muscle fibers.
• Tonic-clonic. Mixed convulsions, which are characterized by both alternating involuntary twitching and spasm.

2. Local. Seen in certain muscles, such as calf cramps.

Generalized seizures are more serious because they affect the entire body. They may be accompanied by loss of consciousness.

Any convulsive conditions have a cause that must be identified in order to prescribe adequate treatment.

Epilepsy, its causes and symptoms

This is a disease of the nervous system, it is characterized by sudden, during which convulsions cover the entire body of the patient. If a person is diagnosed correctly, then it is possible, using new generation anticonvulsants, to achieve good results.

The main causes of epilepsy include:

• Damage to brain neurons.
• pathology during pregnancy.
• Birth trauma.
• hereditary factor.
• Violation of blood circulation in the brain structures.
• Oxygen starvation of the brain.
• Viral infections.

Many doctors still cannot speak with high accuracy about the causes of this disease in each individual person.

The most common and striking symptom of this disease are convulsive seizures. They happen periodically and always start suddenly. During an attack, the patient does not react at all to external stimuli, after it ends, the person usually feels weak, but the attack itself does not remember.

The seizure may not cover the entire body, then the patient simply loses consciousness, or spasms of the facial muscles and illogical, same-type movements are observed.

Epilepsy can be diagnosed only after a thorough examination. If timely and correct treatment is prescribed, then in most cases it is possible to avoid attacks, and the quality of life of a person improves significantly.

Epilepsy treatment

Most patients diagnosed with epilepsy are on the path to recovery if the treatment is correct, and the patient and his family members take an active part in this process.

During treatment, it is very important not only to prescribe anticonvulsants (for epilepsy), but to solve a number of problems:

1. Find out the causes of seizures.
2. If possible, exclude the influence of those factors that can become provocateurs of seizures.
3. Make a correct diagnosis of the type of epilepsy.
4. Prescribe adequate medical treatment. It can also be inpatient care.
5. Much attention should be paid to rest, social problems, employment of patients.

Among the main principles of treatment of epilepsy are:

• Selection of a medicine that will correspond to the type of seizure. Anticonvulsants are prescribed (such drugs help to eliminate or alleviate seizures).
• It is desirable to use monotherapy, that is, to use one drug for convulsive conditions.
• Use of physiotherapy treatment.

Anticonvulsants

The following classification can be given, which is used for drugs for seizures.

1. Benzodiazepines. This group includes: "Diazepam", "Clonazepam", "Dormicum" and others. These drugs are used to relieve an attack and to prevent it.
2. Valproates. Anticonvulsant drugs of this group interfere with the conduction of a nerve impulse, so there are fewer seizures. These include: "Acediprol", "Apilepsin" and many others.
3. "Lamotrigine". It is usually used in the complex therapy of epilepsy until the patient's condition is normalized.
4. Hydantoin derivatives. This includes "Difenin", it reduces the excitability of nerve cells. It has an anticonvulsant effect.
5. Succinoids. In their action, they are similar to the drug of the previous group.
6. Derivatives of oxazolidinedione. This is "Trimetin", which is ineffective for complex and extensive convulsions, and can be useful for local ones.
7. Iminostilbenes. This includes "Finlepsin", it does not allow the reproduction of repeated action potentials, which are precisely the basis of convulsive activity.
8. Anticonvulsants of the barbiturate group belong to the older generation of drugs. Compared to modern drugs, they are already ineffective, so they are used less and less. In addition, with prolonged use, they are addictive.

Any anticonvulsant drugs for epilepsy should be prescribed by a doctor. Only then can effective treatment be guaranteed. It is worth considering that if they are abruptly canceled, the condition may worsen, so the doctor selects the dosage for the entire course of treatment.

Treatment of convulsive conditions in children

Seizures in children are much more common than in adults. This can be caused by many things, ranging from brain disorders to the usual high fever during a viral infection.

The predisposition of young children to frequent convulsions can be explained by the immaturity of brain structures. At the first symptoms of an attack, it is necessary to take all necessary measures to stop it, otherwise irreversible changes in the central nervous system are possible.

According to the degree of danger, anticonvulsant drugs for children can be divided into two groups:

1. Drugs that practically do not depress breathing. These include benzodiazepines: Droperidol, Lidocaine.
2. Respiratory depressants. These are barbiturates, "Magnesium sulfate".

If you have diagnosed a seizure in your child, then you should not wait for its recurrence, but you must urgently consult a doctor. With single convulsions during a high temperature, the next time you should not wait for the thermometer to rise above 38 degrees, bring it down earlier and do not provoke an attack.

If such conditions are observed in a child often, then he will be prescribed treatment. Any anticonvulsant is used strictly in the dosage prescribed by the doctor. In young children, Phenobarbital is most often used in treatment.

It not only prevents the appearance of convulsions, but also calms the nervous system and has a slight hypnotic effect.

Doctors often prescribe one anticonvulsant for children in the treatment of such conditions - this is a mixture of Sereysky and its varieties. It consists of: luminal, caffeine and papaverine. In combination, they relieve spasms well and improve the nutrition of nerve cells.

Muscle spasm in the legs

If an epileptic seizure, which is accompanied by convulsions, is a relatively infrequent phenomenon, since the percentage of such patients is relatively small, then almost every person probably experienced a sharp spasm in the legs. It appears at a time when the muscle stops contracting. Most often, this phenomenon can be observed in the calf muscle. This spasm usually lasts for several minutes. After its completion, pain may disappear without a trace, and in some cases, pain in the muscle can be felt for several more days.

Often such attacks occur at night, some remember the sensations when in the water while swimming in the sea. In this case, it is desirable that someone be nearby and provide assistance.

If this happens to you quite often, then you should not dismiss this problem, but you should consult a doctor.

Causes of leg cramps

If we talk about the reasons that can provoke the development of a sharp muscle spasm in the leg, then the following can be noted:

1. Idiopathic Occurs for an unknown reason, most often at night, especially in the elderly. Athletes are aware of such problems. According to scientists, this occurs when the muscle is already in a contracted state, and the nervous system sends another impulse to contract to it. If you periodically train your muscles and perform stretching exercises, you can reduce the number of such attacks or eliminate them altogether.
2. Another group of seizures can signal a number of problems in the body:

• Dehydration.
• Pregnancy.
• Flat feet.
• Overweight.
• Lack of calcium and magnesium.
• Nervous tension.
• Diseases of the thyroid gland.
• Imbalance of potassium and sodium in the blood.
• Narrowing of the leg arteries, which is often seen in smokers.
• Alcohol abuse.
• Hypothermia of the legs.
• Lack of vitamins of group B, lack of vitamins D, E.

As you can see, there are many reasons why leg cramps can bother you and make your life difficult.

First aid and treatment of leg cramps

When a person reduces his leg or arm, the primary task is to remove this attack as soon as possible. What can be recommended to do so that the spasm stops?

• Stand on the leg that has cramped, only holding on to the chair. Although this action is painful, it is considered quite effective.
• You can put your foot under hot water, if possible.
• Sharply press on the middle of the muscle.
• Do self-massage, starting from the ankle to the thigh.
• Grasp with both hands and pull up and towards you.
• Try to pinch yourself for a spasmodic place several times.
• Advice from athletes is to prick a muscle with a pin.

After you manage to relieve painful muscle spasm, it is advisable not to delay a visit to the doctor, especially if you are often visited by convulsions. Treatment should be prescribed by a doctor, taking into account the established causes of this condition.

There are several ways to deal with this problem:

• Medical treatment.
• Using folk remedies.
• Special gymnastics.

If we talk about drug treatment, then the best anticonvulsants for the legs are Orthocalcium + Magnesium and Ortho Taurine Ergo.

The first medicine saturates the body with magnesium, as well as other minerals and vitamins, without which normal muscle function is impossible. Sometimes after the first application, the effect is noticeable, but most often it is necessary to undergo a monthly course of treatment with this drug.

"Ortho Taurine Ergo" is even more effective, it is prescribed even for epileptic seizures. He, like all anticonvulsants (anticonvulsant drugs), relieves an attack. Its action is enhanced by the presence of vitamins E, B, zinc and lipoic acid.

Doctors often prescribe new generation anticonvulsant drugs for the legs because they not only help relieve spasm quickly, but also reduce mental and physical fatigue.

An even greater effect will be achieved if these two drugs: Orthocalcium + Magnesium and Ortho Taurine Ergo are taken together. Spasms will disturb less and less, and the treatment will go faster.

Gymnastics can positively influence the speed of treatment and ego efficiency. Some exercises (best performed in the morning) will help your muscles bounce back faster:

1. Standing near a chair, place your feet crosswise and lean on the outside. After a few seconds, take a starting position.
2. Sitting on a chair, bend your fingers with all your might, and then straighten them.
3. From a standing position, rise on your toes so that your heels are off the floor, and then drop sharply.
4. Before going to bed, you can perform rotational movements with your feet, as well as flexion and extension of your toes.

The abilities of traditional medicine should also not be discounted. Healers offer the following tips for leg cramps:

1. Rub lemon juice into the skin every morning and evening. It is not worth wiping, it is necessary for it to be absorbed by itself.
2. Laurel oil helps a lot. You can prepare it in the following way: 50 grams of a leaf should be poured with 250 ml of vegetable oil and left for two weeks in a dark place. After filtering, it is necessary to smear them with places where cramps most often reduce.
3. Mix celandine juice and petroleum jelly in a ratio of 1: 2, rub hands or feet with this mixture, where spasms occur.

Any disease requires an integrated approach. Seizures are no exception. Treatment will be more effective if drugs, folk remedies and exercise are used together.

Prevention of convulsive conditions

If the cause of seizures is epilepsy, then this requires serious treatment. Only regular intake of medications and the implementation of all the recommendations of doctors will help to avoid periodic convulsive seizures.

With frequent muscle spasms in the arms or legs, the following recommendations can be advised:

1. Build a diet so that it contains a sufficient amount of all the necessary minerals and vitamins.
2. In winter, you can replenish the supply of elements by taking synthetic vitamins and biological supplements.
3. You need to drink about 2 liters of water per day.
4. You need to limit your sugar intake.
5. Do not get carried away with caffeine, it can wash out calcium from bones.
6. If you play sports, then you need to properly distribute the load.
7. Do not go into too cold water when relaxing at sea.
8. When sitting in a chair, never put your legs under you, especially both at the same time.

If, nevertheless, prevention did not help you, and convulsions occur, then you should consult a doctor. Do not buy anticonvulsants without prescriptions, otherwise you can only harm yourself even more.

Anticonvulsants are medicines used to treat seizures as the main manifestation of epilepsy. The term “antiepileptic” drugs is considered more correct, since they are used to combat epileptic seizures, which are not always accompanied by the development of seizures.

Anticonvulsants, today, are represented by a fairly large group of drugs, but the search and development of new drugs continues. This is due to the variety of clinical manifestations. After all, there are many varieties of seizures with different mechanisms of development. The search for innovative means is also determined by the resistance (resistance) of epileptic seizures to some existing drugs, the presence of side effects that complicate the patient's life, and some other aspects. From this article you will learn for yourself information about the main antiepileptic drugs and the features of their use.

Some basics of epilepsy pharmacotherapy

A feature of the use of drugs is their good tolerability. The most common side effects include:

• dizziness and drowsiness;
• dry mouth, impaired appetite and stool;
• blurred vision;
• erectile dysfunction.

Gabapentin is not used in children under 12 years of age, Pregabalin is prohibited under 17 years of age. Drugs are not recommended for pregnant women.

Phenytoin and Phenobarbital

These are "veterans" among therapeutic drugs for epilepsy. To date, they are not first-line drugs, they are resorted to only in case of resistance to treatment with other drugs.

Phenytoin (Difenin, Digidan) can be used for all types of seizures, with the exception of absences. The advantage of the drug is its low price. The effective dose is 5 mg/kg/day. The drug can not be used for problems with the liver and kidneys, heart rhythm disturbances in the form of various blockades, porphyria, heart failure. When using Phenytoin, side effects may occur in the form of dizziness, fever, agitation, nausea and vomiting, trembling, excessive hair growth, swollen lymph nodes, increased blood glucose, difficulty breathing, allergic rashes.

Phenobarbital (Luminal) has been used as an anticonvulsant since 1911. It is used for the same types of seizures as Phenytoin, at a dose of 0.2-0.6 g / day. The drug "faded" into the background due to the large number of side effects. Among them, the most common are: the development of insomnia, the appearance of involuntary movements, cognitive impairment, rashes, lowering blood pressure, impotence, toxic effects on the liver, aggressiveness and depression. The drug is prohibited for alcoholism, drug addiction, severe liver and kidney diseases, diabetes mellitus, severe anemia, obstructive bronchial diseases, during pregnancy.

Levetiracetam

One of the new drugs for the treatment of epilepsy. The original drug is called Keppra, generics - Levetinol, Komviron, Levetiracetam, Epiterra. Used to treat both partial and generalized seizures. The daily dose is, on average, 1000 mg.

Main side effects:

• drowsiness;
• asthenia;
• dizziness;
• abdominal pain, loss of appetite and stool;
• rashes;
• double vision;
• increased cough (if there are problems with the respiratory system).

There are only two contraindications: individual intolerance, pregnancy and lactation (because the effect of the drug has not been studied in such conditions).

The list of existing drugs for epilepsy can be continued further, since the ideal drug does not yet exist (there are too many nuances in the treatment of epileptic seizures). Attempts to create a "gold standard" for the treatment of this disease are ongoing.

Summing up the above, I would like to clarify that any drug from anticonvulsants is not harmless. It must be remembered that treatment should be carried out only by a doctor, there can be no question of any independent choice or change of the drug!

The modern arsenal of medicines is quite large, but insufficient for the treatment of all forms of epilepsy. Bromides (potassium bromide) were the first anticonvulsants introduced into the pharmacotherapy of epilepsy as early as 1857 by Charles Lockock. In 1938, phenytoin (difenin), a derivative of hydantoin, was synthesized structurally close to barbiturates. Since then, numerous antiepileptic drugs have been developed, but phenytoin remains the drug of choice for epilepsy with grand mal seizures. The history of the emergence of valproates as anticonvulsants dates back to 1962, when R. Eymard accidentally discovered anticonvulsant properties in these compounds. However, as a chemical compound, valproic acid was synthesized 80 years earlier - in 1882 it will melt. This compound has been used for many years in laboratory biochemical and pharmacological research work as a lipophilic agent for dissolving water insoluble compounds. To the surprise of researchers, valproic acid itself (W. Gosher) also had anticonvulsant properties. Currently, valproates remain one of the groups of anticonvulsants that are in great demand (the target for valproates is primary generalized seizures - convulsive absences and idiopathic form of epilepsy) and are used as basic drugs for monotherapy in patients with epilepsy. In recent years, new, fairly safe drugs, such as lamotrigine, topiramate, have been obtained and found their use, which are often used alongside drugs synthesized earlier, very often as a combination therapy.

Antiepileptic drugs - these are drugs of various origins used to prevent or reduce (in intensity and frequency) by the court, their equivalents (loss or impairment of consciousness, behavioral and autonomic disorders, etc.), which are observed during recurrent seizures of various forms of epilepsy.

Epilepsy is a consequence of the occurrence in the cerebral cortex or subcortical brain centers (substance nigra, tonsils, etc.) of foci of excitation that is transmitted to the nervous and muscular systems, which leads to the development of epileptic seizures or an epileptic state. The cause of epilepsy is not clear, so the main drugs are aimed at eliminating the seizure or preventing it.

The main clinical sign of epilepsy is a sudden onset of clonic or tetanic seizures with loss of consciousness. Clonic convulsions are characterized by periodic contraction and relaxation of muscles, and tonic or tetanic convulsions are characterized by simultaneous contraction of the flexor and extensor muscles, which is accompanied by a tense posture with the head thrown back, the release of bloody saliva due to biting the tongue. Such convulsions are classified as major attacks (grand mal). During small seizures (petit mal) consciousness is lost for a very short time, sometimes even the sick person herself does not have time to notice it. Very frequent seizures sometimes turn into an epileptic state. As a rule, this pathology is confirmed by characteristic epileptic waves-peaks (discharges) on the electroencephalogram (EEG), which makes it possible to accurately determine the localization of the focus of excitation. During a convulsive seizure, drugs are administered to the patient, and after it ends, an individual anti-relapse pharmacotherapy is selected.

Classification of antiepileptic drugs

By chemical structure:

I. barbiturates and their derivatives: phenobarbital (bafetal) benzobarbital (benzonal).

II. Hydantoin derivatives phenytoin (difenin).

III. Carboxamide derivatives: carbamazepine (tegretol, finlepsin).

IV. Benzodiazepine derivatives: phenazepam; clonazepam; Diazepam (Sibazon, Relium) Nitrazepam (Radedorm) Midazolam (Fulsed).

V. Fatty acid derivatives:

5.1) valproic acid (Enkorat, Enkorat-chrono, convulex)

5.2) sodium valproate (depakin, depakin-Enteric)

5.3) combined (valproic acid and sodium valproate) depakine-chrono.

VI. Various anticonvulsants and antispastic drugs: lamotrigine (lamiktal), topiramate (topamax), gabapeptin (Neuralgin).

According to the mechanism of action

1. Means that suppress sodium channels: phenytoin; carbamazepine; valproic acid; sodium valproate; topiramate; lamotrigine.

2. Means that suppress calcium channels (T and L type): trimetin; sodium valproate; gabapentin.

3. Means that activate the GABAergic system:

3.1) postsynaptic action benzodiazepines; barbiturates; gabapentin;

3.2) presynaptic action sodium valproate; tiagabine;

4. Means that suppress the glutamatergic system.

4.1) postsynaptic action barbiturates; topiramate;

4.2) presynaptic action of lamotrigine.

According to clinical indications, antiepileptic drugs can be divided into the following groups:

1. Means used in partial seizures (psychomotor seizures): carbamazepine; sodium valproate; lamotrigine; gabapentin; phenobarbital; clonazepam; diphenin.

2. Means used in generalized seizures:

2.1) grand mal seizures ( grandmat): sodium valproate; carbamazepine; phenobarbital; diphenin; lamotrigine;

2.2) small seizures of epilepsy - absence (petite mat): sodium valproate; lamotrigine; clonazepam.

3. Means used in status epilepticus: diazepam; lorazepam; clonazepam; drugs for anesthesia (sodium oxybutyrate, sodium thiopental).

Types of action of antiepileptic drugs on the body (pharmacological effects):

Anticonvulsant;

Sedative (phenobarbital, magnesium sulfate)

Sleeping pills (phenobarbital, benzobarbital, diazepam) (Fig. 3.12);

Tranquilizing (derivatives of valproic acid, diazepam) (Fig. 3.13);

Muscle relaxant (phenytoin, clonazepam, diazepam) (Fig. 3.14);

Cerebroprotective;

Analgesic (Fig. 3.15).

Action mechanism algorithm antiepileptic drugs can be summarized in two main points:

1) inhibition of pathological hyperactivity of nerve cells in the epileptogenic bonfire;

2) inhibition of the spread of hyperactivity from the epileptogenic focus to other neurons, prevents generalization of excitation and the occurrence of seizures.

In a generalized form, it is customary to distinguish 3 main mechanisms antiepilepticactions drugs, in particular:

1) facilitation of GABA and glycine-depleted (inhibitory) transmission;

2) suppression of excitatory (glutamate and aspartatergic) transmission;

3) change in ion currents (primarily blockade of sodium channels).

Indications: epilepsy: large, focal, mixed (including large and focal) epileptic seizures. In addition, the pain syndrome is predominantly of neurogenic origin, incl. essential trigeminal neuralgia, trigeminal neuralgia in multiple sclerosis, essential glossopharyngeal neuralgia. Diabetic neuropathy with pain syndrome. Prevention of seizures in alcohol withdrawal syndrome. Affective and schizoaffective psychoses (as a means of prevention). Diabetes insipidus of central origin, polyuria and polydipsia of a neurohormonal nature.

Status epilepticus, somnambulism, various forms of muscle hypertonicity, sleep disturbances, psychomotor agitation. Convulsive syndrome when editing, eclampsia, poisoning with convulsive poisons.

Rice. 3.12. Mechanism of hypnotic action

Figure 3.13. Mechanism of tranquilizing action

Rice. 3.14. Mechanism of muscle relaxant action

Rice. 3.15. Mechanism of analgesic action

For emergency treatment of acute seizures; when editing. As a sedative to reduce anxiety, tension, fear. Hyperbilirubinemia. Behavioral disorders associated with epilepsy. Febrile convulsions in children, children's tick. West syndrome.

Side effects of antiepileptic drugs their group affiliation is determined by the mechanism of action. Thus, drugs that increase GABAergic inhibition more often than others cause disturbances in behavioral reactions in patients. Skin reactions in the form of a rash are more characteristic of drugs that affect the sodium channels of cell membranes. In addition, adverse reactions can be determined by the pharmacological variability of the organism - idiosyncrasy. Idiosyncratic side effects include liver failure, which can develop when using phenytoin, carbamazepine, valproic acid salts; pancreatitis can occur when taking valproate; agranulocytosis - as a result of treatment with phenytoin, phenobarbital, carbamazepine, valproate; aplastic anemia sometimes complicates treatment with phenytoin, phenobarbital, carbamazepine; Stevens-Johnson syndrome may occur during treatment with phenytoin, phenobarbital, carbamazepine, lamotrigine; allergic dermatitis and serum sickness occur with the use of any of the antiepileptic drugs; lupus-like syndrome is more common when using phenytoin, carbamazepine. These reactions are dose-independent and may occur at any stage of therapy.

Dose-dependent side effects of anticonvulsants can be divided into 3 large groups:

1) from the side of the central nervous system (phenobarbital, phenytoin, carbamazepine, benzodiazepines, topiramate)

2) hematological (valproates, carbamazepine, phenytoin, phenobarbital)

3) leading to impaired reproductive health (valproates).

Dose-dependent side effects from the central nervous system are of great clinical importance. Phenytoin and carbamazepine can cause brainstem and cerebellar dysfunction, with ataxia, dysarthria, nystagmus, and sometimes diplopia. Tremor may be a dose-dependent stigmatizing consequence of valproate use. Paradoxical psychomotor agitation is possible in children taking benzodiazepines and barbiturates. Serum benzodiazepine concentrations greater than 20 µg/mL can lead to marked brainstem dysfunction and stupor. Already after the start of the patient's recovery from stupor, a second wave of this complication is possible, due to the formation of a large amount of toxic 10,11-epoxy metabolites. Cognitive side effects can be observed during topiramate therapy, mainly during the titration period, with a rapid increase in the dose of the drug.

Complications from the hematopoietic organs when using anticonvulsants can be clinically manifested by leukopenia, neutropenia, thrombocytopenia, as well as complex - aplastic anemia, agranulocytosis and megaloblastic anemia. Megaloblastic anemia may occur with long-term use of phenytoin. Treatment with phenytoin, carbamazepine may be complicated by agranulocytosis. Thrombocytopenia is characteristic of phenytoin, carbamazepine, and especially valproic acid, which has an inhibitory effect on platelet aggregation and depletes fibrinogen stores, which can lead to increased bleeding. Valproates cause hyperandrogenism in girls, dangerous during puberty.

Some adverse reactions to anticonvulsant zysobs are associated with their inducing effect on liver enzymes. This effect is most pronounced in phenobarbital, carbamazepine, and phenytoin. Enzyme inducers may increase the elimination of concomitant medications, especially anticonvulsants (such as lamotrigine), corticosteroids, anticoagulants, and some antibiotics. Serious problems can arise if the metabolism of endogenous substances, for example, cholecalciferol (vitamin D3), is increased, which leads to the development of rickets in children; metabolic disorders of steroid and thyroid hormones; an increase in the level of α1-acid glycoprotein, sex hormone-binding globulin, γ-glutamyl transferase and alkaline phosphatase, the ability to exacerbate porphyria.

Contraindications to the appointment of antiepileptic drugs: impaired liver and pancreas function, hemorrhagic diathesis, acute and chronic hepatitis AV blockade, myelodepression, history of intermittent porphyria, simultaneous use of MAO inhibitors and lithium preparations; myasthenia gravis; acute poisoning with drugs that have a depressing effect on the central nervous system, and alcohol; drug addiction, drug addiction; chronic alcoholism; acute pulmonary insufficiency, respiratory depression. Adams-Stokes syndrome, heart failure, cachexia; diseases of the hematopoietic system; pregnancy, lactation.

sodium valproate- sodium salt of valproic (dipropylacetic) acid.

Pharmacokinetics. After taking before meals, it is quickly and almost completely (70-100%) absorbed in the stomach and small intestine. In case of preliminary dissolution, bioavailability increases by 10-15%. But you should not dissolve the tablet in mineral water, as valproic acid may form, and the solution will become cloudy, although its activity does not decrease. After 1-3 hours, the maximum concentration in the blood plasma is reached, where sodium valproate is 90% protein-bound, and 10% of it is in an ionized form. It accumulates mainly in the structures of the central nervous system, where there is a large amount of GABA transaminase (cerebellum, etc.). It penetrates poorly to other body fluids and tissues: in the CSF - 12%; saliva - 0.4-4.5 %; nursing milk - 5-10%.

The main part of sodium valproate is metabolized in the liver to inactive derivatives, which are excreted through the kidneys and intestines. T1 / 2 about 10 hours. Only about 3% leaves the body in the form of propionic acid, which can lead to false positive results for ketonuria, as well as for urine glucose.

Pharmacodynamics. The mechanism is quite complex, not fully understood, does not fully explain the whole variety of clinical effects, since this drug has a wide spectrum of action and is indicated for almost all types of seizures. The main mechanism of action of valproates is the ability to increase the content of GABA (Fig. 3.16) in the central nervous system, which is due to:

a) inhibitory effect on the breakdown of GABA, due to the suppression of GABA transaminases;

b) increased release of GABA into the synaptic cleft;

c) an indirect effect on the synthesis and breakdown of GABA.

Gamma-aminobutyric transaminase (GABA-T) provides the conversion of GABA to succinate (succinate, succinic) semialdehyde in the GABA cycle, is closely related to the Krebs cycle. Due to the inhibition of this enzyme, a large amount of the inhibitory mediator GABA accumulates, which leads to a decrease in the activity of overly excited nerve cells in the epileptic focus. Sodium valproate does not reduce, but also increases a person's vigilance, while barbiturates significantly suppress it. In patients prone to depressive reactions, sodium valproate improves mood, improves mental state, reduces fears without causing a hypnogenic effect.

In addition, valproate exhibits a moderately pronounced n-anticholinergic effect, as evidenced by the prevention of nicotine-induced tonic convulsions by valproate.

Indications: epilepsy, especially in children.

Rice. 3.16. Neurotransmitter action profiles of sodium valproate.

Note: "+" - activation; "-" - Inhibition, Sir - serotonin, N-xp - n-cholinergic receptor, DA - dopamine, NA - noradrenshn, GABA - γ-shobutyric acid, GABA-T GABA transaminsh MPC - glutamate decarboxylase, BD-site - benzodiazepine site, Glu - glutamate

Contraindications: pregnancy, lactation, liver disease, pancreas, hemorrhagic diathesis, hypersensitivity to the drug, alcohol consumption; drivers and other persons whose work requires increased attention should not be taken.

Side effects: loss of appetite, nausea, abdominal pain, vomiting, diarrhea, sometimes impaired liver function, pancreas (more often 2-12 weeks after the start of the drug does not require discontinuation of treatment, but requires careful monitoring of the patient's condition); hair loss (0.5%); weight gain; acute hepatoencephalopathy (only children under 2 years of age in terms of polytherapy) hemorrhagic-necrotic pancreatitis (extremely rare).

Interaction. Sodium valproate in combination with diphenine and phenobarbital displaces both drugs from their association with proteins and significantly increases the content of their free fractions in the blood. In some cases, the drug against the background of another antiepileptic drug can lead to excitation of the body.

Difenin (phenytoin) according to the chemical structure, it is a derivative of hydantoin (a mixture of 5,5-diphenylhydantoin and sodium bicarbonate). The main mechanism of action of difenin is the suppression of not one epileptic focus in the cerebral cortex or in subcortical structures, but a decrease in the irradiation of epileptic discharges to other brain centers and through the efferent nerves to the muscular system. Along with this, the drug reduces the excitability of nerve cells and increases the threshold for secondary trace discharges, which determine the maintenance of epileptic activity in the focus. Probably, this effect is due to the inhibition of NADH-dehydrogenase activity in the mitochondria of nerve cells, a significant decrease in oxygen consumption in them, and, consequently, insufficient energy supply for epileptic discharges. Equally important is the reduced penetration of calcium into nerve cells and its ionization in cells that produce mediators and hormones that can provoke the development of epileptic discharges.

Difenin effectively suppresses the spread of epileptic impulses without changing the normal function of nerve cells. The drug significantly weakens, and in the case of long-term use, it can completely prevent the development of major seizures in patients with focal or focal epilepsy.

Indications: epilepsy of various forms (generalized tonic-clonic, simple and complex partial psychomotor seizures); prevention by court after injuries and neurosurgical operations on the brain.

Contraindications: peptic ulcer of the stomach and duodenum, severe violations of the liver, kidneys, decompensation of cardiac activity, diseases of the hematopoietic system.

Side effect triad of symptoms (nystagmus, diplopia, ataxia), gingival hyperplasia.

Carbamazepine, unlike difenin, which suppresses the spread of epileptic discharges in the brain, it acts mainly on the nerve cells of the spinal cord and medulla oblongata. Its anticonvulsant activity is almost 3 times less than difenin. Carbamazepine normalizes metabolism, activates the choline and adrenergic mediator systems, and has a high antidepressant effect. It significantly inhibits the activity of Na +, K + -ATPase, reduces the elevated level of cAMP, which is considered as the main mechanism of its antiepileptic effect. After taking it, patients have increased motivation for treatment, increased mood, interest in the environment, decreased depression, fear, hypochondria.

Indications: all forms of epilepsy, especially the "temporal" form with aura, myoclonic and tonic-clonic spasms of the muscles of the face.

Contraindications: pregnancy, bronchial asthma, blood diseases, disorders of the liver, kidneys.

Side effect. Of course, adverse reactions appear in the first week after the start of treatment, more often in the elderly in the form of nausea, anorexia, vomiting, dizziness, ataxia, and allergic reactions. Sometimes there is also an increase in seizures, especially in children. Rarely - jaundice, changes in the blood picture (thrombocytopenia, agranulocytosis, aplastic anemia, etc.), peripheral neuritis.

Interaction. When combining carbamazepine with diphenine, the level of the latter in the blood plasma may increase due to a delay in its metabolism. Difenin and phenobarbital reduce the level of carbamazepine in blood plasma by accelerating its biotransformation.

Recently, a group of new generation drugs has appeared, in particular, lamotrigine, tiagabine, etc. They have a different mechanism of action, but the final effect is to reduce the level of excitatory (glutamic acid) or accumulation of inhibitory mediators (GABA, glycine) in the CNS. Tiagabin(gabitril) is, in contrast to the irreversible GABA blocker, its functional blocker.

Lamotrigine blocks long-term high-frequency discharge of neurons in the same way as depakine and carbamazepine. It is assumed that this effect is mediated by a suppressive effect on the voltage-gated sodium channels of neurons and a prolongation of the refractory period of the cell. Lamotrigine inhibits the release of excitatory glutamic acid, indicating a possible neuroprotective effect of this drug. Lamotrigine is well absorbed when taken orally (both when taken with and without food). Bioavailability close to 100 %. Serum concentration is reached 2-3 hours after taking the drug. Lamotrigine is metabolized in the liver, mainly by conjugation with glucuronic acid. Its main metabolite, 2-N-glucuronic acid conjugate, is excreted in the urine.

Indications: forms of epileptic seizures resistant to other drugs, primarily partial, primary and secondary generalizations, absences, atonic, Lennox-Gastaut syndrome.

Side effect allergic reactions in the form of skin rashes, angioedema, diplopia, blurred vision, dizziness, drowsiness, headache, when combined with valproates - squamous dermatitis.

Interaction diphenin, phenobarbital and carbamazepine reduce the concentration of lamotrigine. Valproate increases (up to 2 or more times) the concentration of lamotrigine, given the potentiating effect of the interaction of lamotrigine and valproate, it is recommended to prescribe a dose of lamotrigine not higher than 250 mg / day to prevent the development of side effects.

Topiramate well absorbed after oral administration (both with and without food). The maximum plasma concentration is reached 2-4 hours after ingestion. Approximately 15% of the drug binds to plasma proteins. Only a small amount of topiramate is metabolized in the liver, while approximately 80 % The drug is excreted unchanged in the urine.

Pharmacodynamics Topiramate blocks voltage-dependent sodium channels of the membrane, potentiates GABA activity at non-benzodiazepine sites of GABA receptors. It blocks the corresponding types of glutamate receptors in the postsynaptic membrane.

Indications: epilepsy (great tonic-clonic seizures, astatic (falls) in Lennox-Gastaut syndrome as an additional drug in cases resistant to other drugs).

Side effect ataxia, decreased concentration, confusion, dizziness, fatigue, drowsiness, paresthesia, thought disorders.

Anticonvulsants are drugs that can prevent or stop seizures of various origins. Currently, the term anticonvulsants is usually used in relation to drugs used to prevent various manifestations (antiepileptics).

Anticonvulsants include hexamidine (see), difenin (see), (see), (see), (see), (see), benzonal (see).

Anticonvulsants (with the exception of phenobarbital) selectively suppress convulsive reactions without having a general inhibitory effect on the central nervous system and without causing a hypnotic effect.

Depending on the clinical manifestations of epilepsy, different anticonvulsants are prescribed. To prevent major seizures, phenobarbital, benzonal, hexamidine, difenin, chloracone are used. Trimethine is effective in preventing minor seizures. Often, for the treatment of epilepsy, the combined use of several anticonvulsants (simultaneously or sequentially) is rational.

Treatment with anticonvulsants is long-term, for many months. Therefore, various side effects associated with taking anticonvulsants are not uncommon (see articles on individual anticonvulsants). Treatment with difenin, hexamidine, chloracone, trimetine is contraindicated in violation of the functions of the liver, kidneys and hematopoietic organs. Trimetin is also contraindicated in diseases of the optic nerve. Anticonvulsants are used to prevent status epilepticus; for its relief, hexenal, magnesium sulfate (parenteral) or sodium barbital in enemas are used.

Anticonvulsants (synonymous with anticonvulsants) are medicinal substances that can prevent the development of seizures of various etiologies. Strictly speaking, the term anticonvulsants should only refer to substances used to treat various forms of epilepsy, so it is more correct to refer to this group of drugs as “antiepileptic drugs”.

The prevention of convulsions or the elimination of an already developed seizure can also be achieved with the help of other neurotropic substances of the sedative type (narcotics, barbiturates, chloral hydrate), however, in anticonvulsants, the effect is achieved without concomitant signs of CNS depression, i.e., the effect of anticonvulsants is selective. Chemically, modern anticonvulsants are represented by barbiturates, derivatives of hydantoin, dioxohexahydropyrimidine, β-chloropropionamide, oxazolidin-2,4-dione, succinimide, phenylacetylurea. The classification of modern anticonvulsants is based on their chemical structure (Table 1).

Anticonvulsants have the ability to prevent convulsions in animal experiments caused by electrical stimulation or the introduction of chemicals (most often corazol). The selectivity of this effect in individual representatives of anticonvulsants is expressed differently. Some substances are characterized by approximately the same activity in relation to experimental convulsions of one or another origin, for example, phenobarbital (see), hexamidine (see), chloracone (see), phenacone (see), phenacemide. And in clinical practice, these drugs have proven themselves as broad-spectrum anticonvulsants, effective in various, including mixed forms of epilepsy. Other drugs are distinguished by a marked selectivity of effect. So, in relation to electric shock, difenin (see), corazole convulsions - trimetin (see), epimide is most effective. Similarly, these anticonvulsants also find predominantly narrowly targeted use in the clinic: difenin - mainly for large seizures, and trimetin and epimide, which is close to it in action - only for small ones. Thus, the activity according to experimental tests with electroshock and corazol allows to some extent to predict the area of ​​clinical application of the new drug. An important feature is also a sedative effect, clearly expressed in phenobarbital, weakly manifested in chloracone, trimetine and completely absent in difenin. As a rule, if the patient has signs of a sedative effect (apathy, drowsiness), this indicates an overdose of the drug.

The mechanism of action of anticonvulsants is not entirely clear. It can be assumed that an increase in the threshold of excitability of the nervous tissue, which occurs under the influence of certain substances (phenobarbital), plays a role in the implementation of the anticonvulsant effect. However, it is known that difenin does not increase the mentioned threshold. It is possible that the mechanism of action of diphenine is associated with a change in the balance of electrolytes at the level of the nerve cell membrane, which entails a difficulty in the spread of convulsive electrical discharges through the substance of the brain. The antiepileptic effect of trimetine is associated with its inhibitory effect on the subcortical structures of the brain.

The use of anticonvulsants in epilepsy is in most cases only one of the components of the whole complex of therapeutic measures. Anticonvulsants are usually prescribed orally (with status epilepticus, they resort to intravenous or rectal administration).

Treatment is long and in each case requires individual selection of the drug and dose. Most often, combined treatment is carried out. Combinations of different anticonvulsants are used, for example, diphenin and trimetin (in a mixed form with large and small seizures), hexamidine and chloracone (in a dysphoric form with a tendency to affective outbursts, aggression). In other cases, they resort to a combination of anticonvulsants with drugs that have a beneficial, but non-specific effect on the course of the disease, such as diacarb (see), affecting the acid-base and water balance, borax, magnesium sulfate (see), Mercu-Zal ( cm.). Anticonvulsants are well absorbed from the gastrointestinal tract and undergo oxidation in the liver, gradually losing lipoidophilicity and acquiring hydrophilic properties. Oxidation products of anticonvulsants (for substances containing a phenyl group, these are p-hydroxyphenyl derivatives), as a rule, do not have an anticonvulsant effect. The final metabolites of anticonvulsants are excreted from the body by the kidneys in the form of water-soluble paired compounds with sulfuric or glucuronic acid.

For the treatment of large seizures of epilepsy, phenobarbital is used (often in combination with caffeine to relieve sedation), benzonal (see), diphenine and triantoin, hexamidine, chloracone. Difenin is most effective in patients with major seizures, mentally intact or with minor mental defects. It is also used to treat psychomotor seizures. Triantoin, which is close to it in structure, is indicated in the same cases as difenin, but, unlike the latter, has a moderate sedative effect. When prescribing hexamidine, especially to patients who have previously received phenobarbital, one should take into account the lack of a sedative-hypnotic effect inherent in barbiturates. This allows you to increase the daily dose, but at bedtime, the addition of phenobarbital is often required. Hexamidin is indicated mainly for convulsive forms of epilepsy, and the greatest therapeutic effect is achieved in cases with frequent seizures. Mental activity and mood of patients improve, activity increases. In most cases, hexamidine is used in combination with other anticonvulsants.

Chloracone is most effective in various types of atypical convulsive seizures, and phenacon turned out to be one of the few remedies that help with severe mental paroxysms, manifested by a twilight state with aggression, fears and mood disorders. In such cases, but with great limitations due to the extremely high toxicity, phenacemide (fenuron) is also used. For small seizures, few of the anticonvulsants are effective, mainly trimetin and epimide. Both substances are used predominantly in children.

When choosing one or another drug, it is necessary to be guided not only by the selectivity of its action in a given form of epilepsy, but also by knowledge of the equivalent doses of this drug in relation to effective doses of other anticonvulsants. For the most common anticonvulsants, the corresponding ratios are described by E. S. Remezova (table 2).

A correct understanding of equieffective doses of anticonvulsants helps to avoid severe exacerbations of the disease that occur when the dose of one substance is canceled or reduced to replace it with another.

For the treatment of status epilepticus, most anticonvulsants are not suitable due to poor water solubility and the impossibility of parenteral administration. In this case, it is recommended to use hexenal (see). As an additional means, a combination of chloral hydrate (15-20 ml of a 6% solution) with sodium barbital (0.5-0.7 g in 30-40 ml of distilled water) is used; solutions are prepared before use and administered rectally after a cleansing enema. Magnesium sulfate (10 ml of a 25% solution) is sometimes prescribed intravenously along with sodium bromide (10-15 ml of a 10% solution).

Anticonvulsants are widely used for the treatment of epilepsy in pediatric practice, with doses being prescribed depending on the age of the child (Table 3).

Side effects during treatment with anticonvulsants are relatively common, due to the long-term use of these substances. Dizziness, headaches, lethargy, drowsiness, nausea - as a rule, signs of an overdose of the drug disappear with a decrease in the dose. More serious side effects are skin rashes, disorders of the parenchymal organs, damage to the hematopoietic function (leukopenia, agranulocytosis, fatal aplastic anemia). The most dangerous in this respect are trimetine and phenacemide. Some anticonvulsants are characterized by such peculiar side effects as photophobia (trimetin), hyperplastic gingivitis (hydantoin derivatives).