Anticonvulsants are medications that can prevent seizures of varying severity and origin, without affecting other functions of the body. This broad pharmacological group is also called anticonvulsants. It is divided into several subgroups of the second and third levels, as well as new and old generation drugs. The attending physician must decide which medicine is suitable in each individual case.
- psychomotor and grand mal seizures, status epilepticus - Difenin;
- psychomotor and grand mal seizures during stroke - Carbamazepine;
- psychomotor seizures, myoclonic epilepsy - Clonazepam;
- severe psychomotor partial seizures, clonic-tonic convulsions - Lamotrigine;
- myoclonic epilepsy – sodium valproate;
- focal seizures, status epilepticus in children - Benzobamil.
- grand mal seizures;
- status epilepticus;
- violations heart rate with organic lesions of the central nervous system;
- overdose of cardiac glycosides;
- trigeminal neuralgia.
- epilepsy;
- seizures;
- tonic-clonic seizures;
- mixed forms of seizures;
- alcohol withdrawal;
- acute manic states.
- all forms of epilepsy in adults and children;
- epileptic seizures - complex and simple;
- secondary caused simple seizures;
- primary and secondary tonic-clonic seizures;
- myoclonic and clonic convulsions;
- Lennox-Gastaut syndrome;
- paroxysmal fear syndrome.
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Classification
Anticonvulsants are divided into several generally accepted classifications, each of which is actively used in medicine. The first classification divides anticonvulsants according to their mechanism of action, the second - according to chemical structure active substance.
No anticonvulsant drug is available in pharmacies without a prescription.
By mechanism of action
Anticonvulsants work by two main mechanisms: stimulation of dopaminergic transmission and inhibition of cholinergic transmission. The funds representing these groups are presented in the table:
Anticholinergics that do not have central action, and those that are effective locally are, as a rule, not used in the treatment of convulsions.
By chemical structure
The classification of drugs with anticonvulsant action according to their chemical structure is more extensive. It includes five main groups that combine drugs based on the structure of the active substance:
The table shows the main groups of anticonvulsants by chemical structure. Medicines based on valproic acid, iminostilbenes, and oxazolidinones can also be used. When treating convulsions and neuralgia, it is important not only to achieve a therapeutic effect, but also to reduce the likelihood of side effects. For this purpose, a classification of anticonvulsants has been developed for each type of epileptic seizure. The classification presents new generation drugs.
Drugs of choice
Drugs of choice are drugs that are widely used for certain diseases and in most cases studied are most effective. The main convulsive pathologies and the list of drugs of choice for them:
If the drugs of choice do not have an effect or are poorly tolerated, the option of replacing the drug with an analogue in action from the second line of drugs for a specific pathology is considered.
Difenin
A drug based on phenytoin represents the first line of treatment for status epilepticus and grand mal seizures. Sold in the form of tablets, 10 pieces in a blister, 99.5 mg of active ingredient per tablet.
Pharmacological properties
Inhibits convulsive activity, stabilizes the threshold of excitability. Actively distributed in tissues, secreted by saliva and gastric juice, penetrates the placenta. Metabolized in the liver.
Indications
Difenin is indicated for the following pathologies:
It is used as a prophylactic agent to prevent epilepsy in neurosurgery.
Contraindications
The use of Diphenin in case of heart failure, atrioventricular block, sinus bradycardia. Not prescribed for liver or kidney failure, porphyria.
Use with caution for children with rickets, the elderly and diabetics, and chronic alcoholism. Combination with Delavirdine is contraindicated.
Adverse reactions
When treated with phenytoin-based drugs, side effects such as nausea, vomiting, nervousness, and dizziness are observed. A laboratory blood test may reveal leukopenia, granulocytopenia, thrombocytopenia, and pancytopenia.
Such unwanted reactions, such as thickening of the lips and facial contours, osteoporosis, skin rashes, dermatitis, systemic lupus erythematosus. The allergic reaction is accompanied by anaphylaxis.
Carbamazepine
Drugs based on it are indicated for psychomotor and grand mal seizures. Carbamazepine is dispensed in tablets with a concentration of the active substance of 0.2 g.
Pharmacological properties
Drugs used for leg cramps and generalized seizures work by blocking sodium channels and reducing synaptic transmission of nerve impulses.
Carbamazepine stabilizes nerve fiber membranes and prevents the occurrence of neuronal discharges. You should choose a drug for your feet after additional consultations with a cardiologist and phlebologist.
Indications for use
Carbamazepine is indicated for the following pathologies:
Can be used for neuralgia of the glossopharyngeal and trigeminal nerves in the composition complex therapy.
Contraindications
Carbamazepine is not prescribed to patients with atrioventricular block, bone marrow suppression and hepatic porphyria, including cutaneous porphyria tarda. Combination with MAO inhibitors is prohibited.
Adverse reactions
The most common undesirable reactions from the central nervous system are: dizziness, headache, drowsiness, migraine, weakness. Taking Carbamazepine may be accompanied by undesirable effects from gastrointestinal tract: nausea, vomiting.
Allergic manifestations are characterized by urticaria, skin rashes, vasculitis, lymphadenopathy. If there are disturbances in other organs as a result of allergies, the drug should be discontinued.
Clonazepam
Representative of the group of benzodiazepine derivatives. Available in the form of tablets with a concentration active substance- clonazepam - 2 mg. Contains lactose.
Pharmacological properties
It affects many structures of the central nervous system, the limbic system and the hypothalamus, structures associated with the regulation of emotional functions. Strengthens the inhibitory effect of GABAergic neurons in the cerebral cortex.
Reduces the activity of noradrenergic, cholinergic, serotonergic neurons. Acts as an anticonvulsant, sedative, anti-anxiety and hypnotic.
Indications
The use of Clonazepam is indicated in the following cases:
Can be used to eliminate fears and phobias, in particular the fear of open spaces. Not used to treat phobias in minor patients.
Contraindications
The use of Clonazepam is contraindicated if respiratory function or respiratory failure, with disorders of consciousness and sleep apnea.
Prescription is prohibited for patients with acute-angle glaucoma, myasthenia, during breastfeeding. Severe liver and/or kidney dysfunction is a contraindication.
Adverse reactions
The most common adverse reactions are observed from the central nervous system: fatigue, muscle weakness, impaired coordination of movements, dizziness. Symptoms are temporary and disappear on their own or when the dosage is reduced.
With long-term treatment, the phenomenon of slow speech and weakened coordination, visual disturbances in the form of double vision develops. Allergic reactions are possible.
Lamotrigine
One of the most popular drugs against seizures and epilepsy. Available in tablet form. One tablet contains 25, 50, 100 or 200 mg of lamotrigine.
The drug also contains lactose monohydrate.
Pharmacological properties
An anticonvulsant drug whose mechanism of action is associated with blocking voltage-gated sodium channels of the presynaptic membrane. The drug acts so that glutamate, an amino acid that plays a decisive role in the formation of an epileptic seizure, does not enter the synaptic cleft.
Indications and contraindications
For adults and children over 12 years of age, Lamotrigine is prescribed as the main and complementary therapy epilepsy, including partial and generalized seizures. Effective against tonic-clonic seizures and seizures associated with Lennox-Gastaut syndrome.
Lamotrigine is used in children over 2 years of age for the same indications.
It is contraindicated increased sensitivity To active substance or other components of the drug.
Convulsions of various origins It occurs six times more often in children than in adults. They can be the result of dehydration, imbalance of fluids and minerals, 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 children in 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 and cerebral edema. Anticonvulsants come to the rescue.
Anticonvulsants for children are prescribed in combination with other medications (anti-inflammatory, analgesics, antivirals, sedatives) after identifying the cause of seizures.
To do this, the doctor will carefully study the full picture of the disease, take into account what time of day the child most often experiences seizures, how often they occur, and what provokes them. Treatment usually takes place in a hospital setting under the constant supervision of doctors.
Therapy with anticonvulsants will also require a lot of additional research- ECG, MRI, etc.
How do they work?
Anticonvulsants act on the central nervous system, suppressing it, thereby stopping convulsive spasms. However, some representatives anticonvulsants have an additional effect - they depress the respiratory center, and this can be very dangerous for children, especially small ones. Such respiratory depressants against seizures include barbiturates and magnesium sulfate.
Medicines that have a slight effect on the child’s breathing are benzodiazepines, droperidol with fentanyl, and lidocaine.
With the help of relatively gentle benzodiazepines (Sibazon, Seduxen), you can cope with seizures of any origin. They prevent the propagation of nerve impulses in the brain and spinal cord.
Droperidol with fentanyl is quite often used to treat children.
Lidocaine for fast intravenous administration stops any seizures by acting at the cellular level - ions begin to penetrate the cell membrane more easily.
Among the barbiturates, the most famous are Phenobarbital and Hexenal.“Phenobarbital” acts for a long time, but the effect of taking it is not achieved immediately, and when stopping seizures, time sometimes plays a decisive role. Moreover, with age, the effect of the drug is achieved faster. In children under one year old, it occurs only 5 hours after administration, and in children over two years old, Phenobarbital is absorbed from the gastrointestinal tract twice as fast.
They try not to prescribe Hexenal to children, since it has a very strong effect on the respiratory system, suppressing it like anesthesia.
Magnesium sulfate is also used infrequently in pediatrics, mainly to eliminate seizures associated with cerebral edema and magnesium imbalance.
Most important factor When treating seizures in children, it is necessary to determine the optimal dose of the drug. It is calculated strictly individually; specialists 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 for the rest of his life if the seizures are associated with severe hereditary pathologies.
Classification
According to the method of action and active substance, all anticonvulsants are divided into several groups:
- Iminostilbenes. Anticonvulsant medications with excellent analgesic and antidepressant effects. Improves mood, eliminates muscle spasms.
- Valproate. Anticonvulsants, which have the ability to relax muscles while providing a sedative effect. They also improve mood and normalize psychological condition patient.
- Barbiturates. They perfectly stop seizures, lower blood pressure and have a fairly pronounced hypnotic effect.
- Succiminids. These are anticonvulsant medications, which are indispensable in cases where it is necessary to eliminate spasms in individual organs, with neuralgia.
- Benzodiazepines. With the help of these medications, prolonged convulsive seizures are suppressed; the drugs are prescribed for epilepsy.
Pediatric anti-seizure medications must meet several important criteria. They should not have a suppressive effect on the psyche, should not cause addiction or dependence, and the medications must be hypoallergenic.
Parents have neither the moral nor the legal right to choose such serious drugs for their children on their own. All anticonvulsants in Russian pharmacies are sold only upon presentation of a prescription, which is prescribed by a doctor after establishing the causes of convulsive conditions.
List of anticonvulsant medications for children
"Carbamazepine". This antiepileptic drug from the category of iminosbenes has many advantages. It reduces pain in those who suffer from neuralgia. Reduces the frequency of attacks in epilepsy; after several days of taking the drug, there is a decrease in anxiety, a decrease in aggressiveness in adolescents and children. The medicine is absorbed quite slowly, but it acts completely and for a long time. The product is available in tablets. Carbamazepine is prescribed to children from 3 years of age.
"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 and trigeminal neuralgia. The drug is available in tablet form. Children can be given the medicine from the age of three.
"Valparine". Anticonvulsant medicine of the vaoproate group. The drug does not depress breathing, does not affect blood pressure, and has a moderate sedative effect. "Valparin" is prescribed for the treatment of epilepsy, for seizures associated with organic brain lesions, for febrile seizures (convulsions due to 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 childhood tics, as well as for febrile seizures in children. The medicine is available in the form of drops for oral administration, tablets, dry substance for intravenous injections and droppers, as well as in the form of syrup. Children under 3 years of age can take the medication 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, Konvulex is prescribed to children who have bipolar disorders. Release forms are different - from dry substances for subsequent preparation of injections to capsules and tablets. The so-called “children's” forms of the medicine are oral drops and syrup. Capsules and tablets are contraindicated in children under 3 years of age. They can only be given liquid forms"Convulexa".
"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 for the treatment of epilepsy, severe sleep disorders, spastic paralysis, and a number of seizures not associated with manifestations of epilepsy. Available in tablets. Can be prescribed to children from birth.
"Clonazepam". The brightest representative of the group of benzodiazepines. Approved for use in children of any age with epilepsy, nodule spasms, and atonic seizures. Available in tablets and solution for intravenous administration.
"Sibazon"- a tranquilizer with an anticonvulsant effect. May lower blood pressure. Used for muscle cramps of various origins. Available in tablets and solution for intravenous injections. It is used to relieve epileptic seizures and febrile convulsions in children from one year of age.
In addition, Antilepsin, Iktoril, Rivotril, Pufemid, Ronton, Etimal and Sereysky’s Mixture are effective against childhood seizures.
What not to do?
If your child has seizures, do not try to figure out the cause on your own. Call " Ambulance“And while you are waiting for the doctors, carefully observe the baby - what type of convulsions he is experiencing, how severe the pain syndrome is, pay attention to the duration of the convulsive spasms. All this information will be useful later for specialists to establish the correct diagnosis.
You should not give your child any anticonvulsants on your own. Also, do not give your baby water or food, because their particles may get into the Airways and cause suffocation.
Do not try to get the child's tongue. This is a common misconception. The baby won’t swallow his tongue, but he can suffocate if fragments of teeth injured when trying to open his jaw get into his respiratory tract.
Do not hold a child in a state of convulsions in one fixed position. This can cause serious joint injuries, sprains, and muscle tears.
The famous pediatrician Komarovsky talks in detail about seizures:
Advice for parents from a doctor at the Russian Union of Pediatricians:
ANTICONVULSATIVE (ANTIEPILEPTIC) MEDICINES
According to the modern classification, anticonvulsant drugs are divided into anticonvulsant barbiturates (benzobamyl, benzonal, hexamidine, phenobarbital), hydantoin derivatives (difenin), oxazolidinedione derivatives (trimethine), succinimides (pufemide, suxilep), iminostilbenes (carbamazepine), benzodiazepine derivatives (clonazepam), valproates (acediprole), various anticonvulsants (methindione, mydocalm, chloracon)
ACEDIPROL (Acediprolum)
Synonyms: Sodium valproate, Apilepsin, Depakin, Konvulex, Konvulsovin, Diplexil, Epikin, Orfilept, Valprin, Depaken, Deprakin, Epilim, Everiden, Leptilan, Orfiril, Propimal, Valpakin, Valporin, Valpron, etc.
Pharmachologic effect. It is a broad-spectrum antiepileptic drug.
Acediprol has not only an anticonvulsant (antiepileptic) effect. It improves the mental state and mood of patients. Acediprole has been shown to have a tranquilizing (relieving anxiety) component, and unlike other tranquilizers, while reducing the state of fear, it does not have a somnolent (causing increased drowsiness), sedative (calming effect on the central nervous system) and muscle relaxant (muscle relaxant) effect.
Indications for use. Used in adults and children for different types of epilepsy: various forms ah generalized seizures - small (absences), large (convulsive) and polymorphic; with focal seizures (motor, psychomotor, etc.). The drug is most effective for absence seizures (short-term loss of consciousness with complete loss of memory) and pseudo-absences (short-term loss of consciousness without memory loss).
Method of administration and dose. Take acediprole orally during or immediately after meals. Start by taking small doses, gradually increasing them over 1-2 weeks. until a therapeutic effect is achieved; then an individual maintenance dose is selected.
The daily dose for adults is 0.3-0.6 g (1-2 tablets) at the beginning of treatment, then it is gradually increased to 0.9-1.5 g. Single dose- 0.3-0.45 g. The highest daily dose is 2.4 g.
The dose for children is selected individually depending on age, severity of the disease, and therapeutic effect. Typically, the daily dose for children is 20-50 mg per 1 kg of body weight, the highest daily dose is 60 mg/kg. Treatment is started with 15 mg/kg, then the dose is increased weekly by 5-10 mg/kg until the desired effect is achieved. The daily dose is divided into 2-3 doses. It is convenient for children to prescribe the drug in the form of a liquid dosage form - acediprole syrup.
Acediprole can be used alone or in combination with other antiepileptic drugs.
For minor forms of epilepsy, they are usually limited to the use of only acediprole.
Side effect. Possible side effects: nausea, vomiting, diarrhea (diarrhea), stomach pain, anorexia (lack of appetite), drowsiness, allergic skin reactions. As a rule, these phenomena are temporary.
With long-term use of large doses of acediprole, temporary hair loss is possible.
Rare, but the most serious reactions to acediprole are dysfunction of the liver, pancreas and deterioration of blood clotting.
Contraindications. The drug is contraindicated in cases of liver and pancreas dysfunction, hemorrhagic diathesis (increased bleeding). The drug should not be prescribed in the first 3 months. pregnancy (at a later date, it is prescribed in reduced doses only if other antiepileptic drugs are ineffective). The literature provides data on cases of teratogenic (damaging to the fetus) effect when using acediprole during pregnancy. It should also be taken into account that in breastfeeding women the drug is excreted in milk.
Release form. Tablets of 0.3 g in packs of 50 and 100 pieces; 5% syrup in glass bottles of 120 ml with a dosing spoon attached.
Storage conditions. List B. In a cool, dark place.
BENZOBAMIL (Benzobamylum)
Synonyms: Benzamyl, Benzoylbarbamyl.
Pharmachologic effect. It has anticonvulsant, sedative (calming), hypnotic and hypotensive (lowering blood pressure) properties. Less toxic than benzonal and phenobarbital.
Indications for use. Epilepsy, mainly with subcortical localization of the focus of excitation, “diencephalic” form of epilepsy, status epilepticus in children.
Method of administration and dose. Inside after meals. Doses for adults are 0.05-0.2 g (up to 0.3 g) 2-3 times a day, for children, depending on age, from 0.05 to 0.1 g 3 times a day. Benzobamil can be used in combination with dehydration (dehydration), anti-inflammatory and desensitizing (preventing or inhibiting allergic reactions) therapy. In case of addiction (weakening or lack of effect with prolonged repeated use), benzobamyl can be temporarily combined with equivalent doses of phenobarbital and benzonal, followed by replacing them again with benzobamyl.
The equivalent ratio of benzobamyl and phenobarbital is 2-2.5:1.
Side effect. Large doses of the drug can cause drowsiness, lethargy, decreased blood pressure, ataxia (impaired coordination of movements), nystagmus (involuntary rhythmic movements of the eyeballs), difficulty speaking.
Contraindications. Damage to the kidneys and liver with impairment of their functions, decompensation of cardiac activity.
Release form. Tablets of 0.1 g in a package of 100 pieces.
Storage conditions. List B. In a tightly sealed container.
BENZONAL (Benzonalum)
Synonyms: Benzobarbital.
Pharmachologic effect. Has a pronounced anticonvulsant effect; unlike phenobarbital, it does not have a hypnotic effect.
Indications for use. Convulsive forms of epilepsy, including Kozhevnikov epilepsy, focal and Jacksonian seizures.
Method of administration and dose. Inside. Single dose for adults - 0.1-0.2 g, daily - 0.8 g, for children, depending on age - single dose 0.025-0.1 g, daily - 0.1-0.4 g. The most effective and tolerable dose of the drug. Can be used in combination with other anticonvulsants.
Side effect. Drowsiness, ataxia (impaired coordination of movements), nystagmus (involuntary rhythmic movements of the eyeballs), dysarthria (speech disorder).
Release form. Tablets of 0.05 and 0.1 g in a package of 50 pieces.
Storage conditions.
GEXAMIDINE (Gexamidinum)
Synonyms: Primidone, Mizolin, Primaclon, Sertan, Deoxyphenobarbitone, Lepimidine, Lespiral, Liscantin, Mizodin, Milepsin, Prilepsin, Primolin, Prizolin, Sedilen, etc.
Pharmachologic effect. It has a pronounced anticonvulsant effect, its pharmacological activity is close to phenobarbital, but does not have a pronounced hypnotic effect.
Indications for use. Epilepsy of various genesis (origin), mainly grand mal seizures. When treating patients with polymorphic (various) epileptic symptoms, it is used in combination with other anticonvulsants.
Method of administration and dose. Orally 0.125 g in 1-2 doses, then the daily dose is increased to 0.5-1.5 g. Higher doses for adults: single - 0.75 g, daily - 2 g.
Side effect. Itching, skin rashes, mild drowsiness, dizziness, headache, ataxia (impaired coordination of movements), nausea; with long-term treatment, anemia (decrease in the number of red blood cells in the blood), leukopenia (decrease in the level of leukocytes in the blood), lymphocytosis (increase in the number of lymphocytes in the blood).
Contraindications. Diseases of the liver, kidneys and hematopoietic system.
Release form. Tablets of 0.125 and 0.25 g in a package of 50 pieces.
Storage conditions. List B. In a cool, dry place.
DIFENIN (Dipheninum)
Synonyms: Phenytoin, Diphentoin, Epanutin, Hydantoinal, Sodanton, Alepsin, Digidantoin, Dilantin sodium, Difedan, Eptoin, Hydantal, Fengidon, Solantoin, Solantil, Zentropil, etc.
Pharmachologic effect. Has a pronounced anticonvulsant effect; There is almost no hypnotic effect.
Indications for use. Epilepsy, mainly grand mal seizures. Diphenine is effective in some forms of cardiac arrhythmias, especially in arrhythmias caused by an overdose of cardiac glycosides.
Method of administration and dose. Orally after meals, "/2 tablets 2-3 times a day. If necessary, the daily dose is increased to 3-4 tablets. The highest daily dose for adults is 8 tablets.
Side effect. Tremor (shaking of hands), ataxia (impaired coordination of movements), dysarthria (speech disorder), nystagmus (involuntary movements of the eyeballs), eye pain, increased irritability, skin rashes, sometimes fever, gastrointestinal disorders, leukocytosis (increased number of white blood cells in the blood), megaloblastic anemia
Contraindications. Liver and kidney diseases, cardiac decompensation, pregnancy, cachexia (extreme exhaustion).
Release form. Tablets of 0.117 g in a package of 10 pieces.
Storage conditions. List B. In a place protected from light.
CARBAMAZEPINE (Carbamazepinum)
Synonyms: Stazepin, Tegretol, Finlepsin, Amizepine, Carbagretil, Carbazep, Mazetol, Simonil, Neurotol, Tegretal, Temporal, Zeptol, etc.
Pharmachologic effect. Carbamazepine has a pronounced anticonvulsant (antiepileptic) and moderate degree antidepressant and mood-improving (mood-improving) effects.
Indications for use. Carbamazepine is used for psychomotor epilepsy, grand mal seizures, mixed forms (mainly with a combination of grand mal seizures with psychomotor manifestations), local forms (post-traumatic and post-encephalitic origin). It is not effective enough for minor seizures.
Method of administration and dose. Prescribed orally (during meals) for adults, starting with 0.1 g ("/2 tablets) 2-3 times a day, gradually increasing the dose to 0.8-1.2 g (4-6 tablets) per day.
The average daily dose for children is 20 mg per 1 kg of body weight, i.e. on average, under the age of 1 year - from 0.1 to 0.2 g per day; from 1 year to 5 years - 0.2-0.4 g; from 5 to 10 years -0.4-0.6 g; from 10 to 15 years -0.6-1 g per day.
Carbamazepine can be prescribed in combination with other antiepileptic drugs.
As with the use of other antiepileptic drugs, the transition to carbamazepine treatment should be gradual, with a reduction in the dose of the previous drug. Treatment with carbamazepine should also be stopped gradually.
There is evidence of the effectiveness of the drug in a number of cases in patients with various hyperkinesis (violent automatic movements due to involuntary muscle contractions). The initial dose of 0.1 g was gradually (after 4-5 days) increased to 0.4-1.2 g per day. After 3-4 weeks. the dose was reduced to 0.1-0.2 g per day, then the same doses were prescribed daily or every other day for 1-2 weeks.
Carbamazepine has an analgesic (pain-relieving) effect in trigeminal neuralgia (inflammation of the facial nerve).
Carbamazepine is prescribed for trigeminal neuralgia, starting with 0.1 g 2 times a day, then the dose is increased by 0.1 g per day, if necessary to 0.6-0.8 g (in 3-4 doses). The effect usually occurs 1-3 days after the start of treatment. After the pain disappears, the dose is gradually reduced (to 0.1-0.2 g per day). The drug is prescribed for a long time; If the drug is discontinued prematurely, the pain may recur. Currently, carbamazepine is considered as one of the most effective drugs for this disease.
Side effect. The drug is usually well tolerated. In some cases, loss of appetite, nausea, and rarely - vomiting, headache, drowsiness, ataxia (impaired coordination of movements), impaired accommodation (impaired visual perception) are possible. A decrease or disappearance of side effects occurs when the drug is temporarily stopped or the dose is reduced. There is also evidence of allergic reactions, leukopenia (decrease in the level of leukocytes in the blood), thrombocytopenia (decrease in the number of platelets in the blood), agranulocytosis (sharp decrease in granulocytes in the blood), hepatitis (inflammation of liver tissue), skin reactions, exfoliative dermatitis (inflammation of the skin) . If these reactions occur, stop taking the drug.
The possibility of the occurrence of mental disorders in patients with epilepsy treated with carbamazepine should be taken into account.
During treatment with carbamazepine, it is necessary to systematically monitor the blood picture. It is not recommended to prescribe the drug in the first 3 months. pregnancy. Carbamazepine should not be prescribed simultaneously with irreversible monoamine oxidase inhibitors (nialamide, etc., furazolidone) due to the possibility of increased side effects. Phenobarbital and hexamidine weaken the antiepileptic activity of carbamazepine.
Contraindications. The drug is contraindicated for cardiac conduction disorders and liver damage.
Release form. Tablets of 0.2 g in packs of 30 and 100 pieces.
Storage conditions. List B. In a place protected from light.
CLONAZEPAM (Clonazepamum)
Synonyms: Antelepsin, Klonopin, Ictoril, Ictorivil, Ravatril, Ravotril, Rivatril, Rivotril, etc.
Pharmachologic effect. Clonazepam has a sedative, muscle-relaxing, anxiolytic (anti-anxiety) and anticonvulsant effect. The anticonvulsant effect of clonazepam is stronger than that of other drugs in this group, and therefore it is used mainly for the treatment of convulsive conditions. In patients with epilepsy taking clonazepam, seizures occur less frequently and their intensity decreases.
Indications for use. Clonazepam is used in children and adults for minor and major forms of epilepsy with myoclonic seizures (twitching of individual muscle bundles), psychomotor crises, and increased muscle tone. It is also used as a hypnotic, especially in patients with organic brain damage.
Method of administration and dose. Treatment with clonazepam begins with small doses, gradually increasing them until an optimal effect is obtained. The dosage is individual depending on the patient’s condition and his response to the drug. The drug is prescribed at a dose of 1.5 mg per day, divided into 3 doses. Gradually increase the dose by 0.5-1 mg every 3rd day until the optimal effect is obtained. Usually prescribed 4-8 mg per day. It is not recommended to exceed the dose of 20 mg per day.
For children, clonazepam is prescribed in the following doses: newborns and children under 1 year old - 0.1-1 mg per day, from 1 year to 5 years - 1.5-3 mg per day, from 6 to 16 years old - 3-6 mg per day. day. The daily dose is divided into 3 doses.
Side effect. When taking the drug, there may be disturbances in coordination of movements, irritability, depressive states(state of depression), increased fatigue, nausea. To reduce side effects, it is necessary to individually select the optimal dose, starting with smaller doses and gradually increasing them.
Contraindications. Acute diseases liver and kidneys, myasthenia gravis (muscle weakness), pregnancy. Do not take simultaneously with MAO inhibitors and phenothiazine derivatives. The drug should not be taken the day before or during work by transport drivers and persons whose work requires quick mental and physical reactions. During treatment with the drug, you must refrain from drinking alcohol.
The drug penetrates the placental barrier and into breast milk. It should not be prescribed to pregnant women or during breastfeeding.
Release form. Tablets of 0.001 g (1 mg) in packs of 30 or 50 pieces.
Storage conditions. List B. In a place protected from light.
METHINDIONE (Methindionum)
Synonyms: Indomethacin, Inteban.
Pharmachologic effect. An anticonvulsant that does not depress the central nervous system, reduces affective (emotional) stress and improves mood.
Indications for use. Epilepsy, especially in the temporal form and epilepsy of traumatic origin (origin).
Method of administration and dose. Orally (after meals) for adults, 0.25 g per dose. For epilepsy with frequent seizures, 6 times a day at intervals of 1 "/2-2 hours (daily dose 1.5 g). For rare seizures, the same single dose 4-5 times a day (1-1. 25 g per day).For seizures at night or in the morning, an additional 0.05-0.1 g of phenobarbital or 0.1-0.2 g of benzonal is prescribed. psychopathological disorders in patients with epilepsy, 0.25 g 4 times a day. If necessary, treatment with methindione is combined with phenobarbital, seduxene, and eunoctine.
Side effect. Dizziness, nausea, tremor (shaking) of fingers.
Contraindications. Severe anxiety, tension.
Release form. Tablets of 0.25 g in a package of 100 pieces.
Storage conditions.
MYDOCALM
Synonyms: Tolperison hydrochloride, Mideton, Menopatol, Myodom, Pipetopropanone.
Pharmachologic effect. Suppresses polysynaptic spinal reflexes and reduces increased tone skeletal muscles.
Indications for use. Diseases accompanied by increased muscle tone, including paralysis ( complete absence voluntary movements), paresis (decreased strength and/or range of motion), paraplegia (bilateral paralysis of the upper or lower limbs), extrapyramidal disorders (impaired coordination of movements with a decrease in their volume and tremors).
Method of administration and dose. Orally 0.05 g 3 times a day with a gradual increase in dose to 0.3-0.45 g per day; intramuscularly, 1 ml of 10% solution 2 times a day; intravenously (slowly) 1 ml in 10 ml of saline 1 time per day.
Side effect. Sometimes a feeling of slight intoxication, headache, increased irritability, sleep disturbance.
Contraindications. Not identified.
Release form. Dragee 0.05 g in a package of 30 pieces; ampoules of 1 ml of 10% solution in a package of 5 pieces.
Storage conditions. List B. In a cool, dry place.
PUPHEMID (Puphemidum)
Pharmachologic effect. Anticonvulsant action.
Indications for use. For various forms of epilepsy such as petit mal (minor seizures), as well as for temporal lobe epilepsy.
Method of administration and dose. Orally before meals for adults, starting with 0.25 g 3 times a day, gradually increasing the dose if necessary to 1.5 g per day; children under 7 years old - 0.125 g, over 7 years old - 0.25 g 3 times a day.
Side effect. Nausea, insomnia. For nausea, it is recommended to prescribe the drug 1-1/2 hours after meals, for insomnia 3-4 hours before bedtime.
Contraindications. Acute liver and kidney diseases, hematopoietic dysfunction, pronounced atherosclerosis, hyperkinesis (violent automatic movements due to involuntary muscle contractions).
Release form. Tablets of 0.25 g in a package of 50 pieces.
Storage conditions. List B. In dark glass jars.
SUXILEP
Synonyms: Ethosuximide, Azamide, Pycnolepsin, Ronton, Zarontin, Etomal, Etimal, Pemalin, Petinimid, Sucimal, etc.
Pharmachologic effect. Anticonvulsant action.
Indications for use. Minor forms of epilepsy, myoclonic seizures (convulsive twitching of individual muscle groups).
Method of administration and dose. Orally (taken with meals) 0.25-0.5 g per day with a gradual increase in dose to 0.75-1.0 g per day (in 3-4 divided doses).
Side effect. Dyspeptic disorders (digestive disorders); in some cases, headache, dizziness, skin rashes, leukopenia (decrease in the level of leukocytes in the blood) and agranulocytosis ( a sharp decline number of granulocytes in the blood).
Contraindications. Pregnancy, breastfeeding.
Release form. Capsules of 0.25 g in a package of 100 pieces.
Storage conditions. List B. In a cool, dry place.
TRIMETHIN (Trimethinum)
Synonyms: Trimethadione, Ptimal, Tridion, Trimedal, Absenthol, Edion, Epidion, Petidion, Trepal, Troxidon.
Pharmachologic effect. Has an anticonvulsant effect.
Indications for use. Epilepsy, mainly petit mal (minor seizures).
Method of administration and dose. Orally during or after meals, 0.25 g 2-3 times a day, for children, depending on age - from 0.05 to 0.2 g 2-3 times a day.
Side effect. Photophobia, skin rashes, neutropenia (decreased number of neutrophils in the blood), agranulocytosis (sharp decrease in granulocytes in the blood), anemia (decreased hemoglobin in the blood), eosinophilia (increased number of eosinophils in the blood), monocytosis (increased number of monocytes in the blood).
Contraindications. Liver and kidney dysfunctions, diseases optic nerve and hematopoietic organs.
Release form. Powder.
Storage conditions. List B. In a cool, dry place.
PHENOBARBITAL (Phenobarbitalum)
Synonyms: Adonal, Efenal, Barbenil, Barbifen, Dormiral, Epanal, Episedal, Fenemal, Gardenal, Hypnotal, Mefabarbital, Neurobarb, Nirvonal, Omnibarb, Phenobarbitone, Sedonal, Sevenal, Somonal, Zadonal, etc.
Pharmachologic effect. Usually considered as a hypnotic. However, currently highest value has as an antiepileptic drug.
In small doses it has a calming effect.
Indications for use. Treatment of epilepsy; used for generalized tonic-clonic seizures (grand mal), as well as for focal attacks in adults and children. Due to its anticonvulsant effect, it is prescribed for chorea (a disease of the nervous system accompanied by motor agitation and uncoordinated movements), spastic paralysis, and various convulsive reactions. As a sedative in small doses in combination with other drugs (antispasmodics, vasodilators) it is used for neurovegetative disorders. As a sleeping pill.
Method of administration and dose. For the treatment of epilepsy, adults are prescribed starting with a dose of 0.05 g 2 times a day and gradually increasing the dose until seizures stop, but not more than 0.5 g per day. For children, the drug is prescribed in smaller doses according to age (not exceeding the highest single and daily doses). Treatment is carried out for a long time. It is necessary to stop taking phenobarbital for epilepsy gradually, since sudden withdrawal of the drug can cause the development of a seizure and even status epilepticus.
Phenobarbital is often prescribed in combination with other medications to treat epilepsy. Usually these combinations are selected individually depending on the form and course of epilepsy and general condition sick.
As a sedative and antispasmodic, phenobarbital is prescribed in a dose of 0.01-0.03-0.05 g 2-3 times a day.
Higher doses for adults orally: single dose - 0.2 g; daily - 0.5 g.
The simultaneous use of phenobarbital with other sedative-acting drugs (calming) leads to an increase in the sedative-hypnotic effect and may be accompanied by respiratory depression.
Side effect. Suppression of the central nervous system, decreased blood pressure, allergic reactions ( skin rash etc.), changes in the blood formula.
Contraindications. The drug is contraindicated in cases of severe damage to the liver and kidneys with impairment of their functions, alcoholism, drug addiction, myasthenia gravis ( muscle weakness). It should not be prescribed in the first 3 months. pregnancy (to avoid teratogenic effects /damaging effects on the fetus/) and women who are breastfeeding.
Extract form. Powder; tablets of 0.005 g for children and 0.05 and 0.1 g for adults.
Storage conditions. List B. In a place protected from light.
GLUFERAL (Gluferalum)
A combined drug containing phenobarbital, bromizal, sodium caffeine benzoate, calcium gluconate.
Indications for use.
Method of administration and dose. For adults, after meals, depending on the condition, 2-4 tablets per dose. The maximum daily dose is 10 tablets. Children, depending on age, are prescribed from 1/2 to 1 tablet per dose. The maximum daily dose for children under 10 years of age is 5 tablets.
Side effects and Contraindications.
Release form. Tablets containing: phenobarbital - 0.025 g, bromizal - 0.07 g, sodium caffeine benzoate - 0.005 g, calcium gluconate - 0.2 g, 100 pieces in an orange glass jar.
Storage conditions. List B. In a place protected from light.
PAGLUFERAL-1,2,3 (Pagluferalum-1,2,3)
A combined drug containing phenobarbital, bromizal, sodium caffeine benzoate, papaverine hydrochloride, calcium gluconate.
The pharmacological action is due to the properties of its constituent components.
Indications for use. Mainly for epilepsy with major tonic-clonic seizures.
Method of administration and dose. Different ratios of ingredients in different options Paglufersht tablets make it possible to individually select doses. Start taking 1-2 tablets 1-2 times a day.
Side effects and Contraindications. The same as for phenobarbital.
Release form. Pagluferal tablets 1, 2 and 3, containing, respectively: phenobarbital - 0.025; 0.035 or 0.05 g, brominated - 0.1; 0.1 or 0.15 g, sodium caffeine benzoate -0.0075; 0.0075 or 0.01 g, papaverine hydrochloride -0.015; 0.015 or 0.02 g, calcium gluconate - 0.25 g, in orange glass jars of 40 pieces.
Storage conditions. List B. In a place protected from light.
SEREYSKI MIXTURE (Mixtio Sereyski)
Complex powder containing phenobarbital, bromizal, sodium caffeine benzoate, papaverine hydrochloride, calcium gluconate.
The pharmacological action is due to the properties of its constituent components.
Indications for use. Mainly for epilepsy with major tonic-clonic seizures.
Method of administration and dose. 1 powder 2-3 times a day (for mild forms of the disease, take a powder with a lower weight content of components, for more severe forms, take a powder with a higher weight content of components /see Release form./).
Side effects and contraindications. The same as for phenobarbital.
Release form. Powder containing: phenobarbital - 0.05-0.07-0.1-0.15 g, bromisal - 0.2-0.3 g, sodium caffeine benzoate - 0.015-0.02 g, papaverine hydrochloride - 0.03 -0.04 g, calcium gluconate -0.5-1.0 g.
Storage conditions. List B. In a dry place, protected from light.
FALILEPSIN (Fali-Lepsin)
A combination drug containing phenobarbital and pseudonorephedrine.
The pharmacological action is due to the properties of its constituent components. The inclusion of pseudonorephedrine, which has a moderate stimulating effect on the central nervous system, somewhat reduces the inhibitory effect (drowsiness, decreased performance) of phenobarbital.
Indications for use. Various forms of epilepsy.
Method of administration and dose. Adults and children over 12 years of age, starting with 1/2 tablet (50 mg) per day, gradually increasing the dose to 0.3-0.45 g (in 3 divided doses).
Release form. Tablets of 0.1 g, in a package of 100 pieces.
Storage conditions. List B. In a place protected from light.
CHLORACONUM (Chloraconum)
Synonyms: Beclamid, Gibicon, Nidran, Posedran, Benzchlorpropamide.
Pharmachologic effect. Has a pronounced anticonvulsant effect.
Indications for use. Epilepsy, mainly with grand mal seizures; psychomotor agitation of an epileptic nature; with frequent seizures (in combination with other anticonvulsants); prescribed to patients with epilepsy during pregnancy and those who have had liver disease.
Method of administration and dose. Orally 0.5 g 3-4 times a day, if necessary, up to 4 g per day; children - 0.25-0.5 g 2-4 times a day (depending on age).
Side effect. Irritant effect on the gastric mucosa in patients who have undergone gastrointestinal diseases. With long-term treatment, it is necessary to monitor the function of the liver, kidneys, and blood count.
Release form. Tablets of 0.25 g in packs of 50 pieces.
Storage conditions. List B. In a cool, dry place.
Purpose anticonvulsants clear from their name. The purpose of these drugs is to reduce or completely eliminate muscle cramps and epileptic attacks. Many drugs are taken in combination to improve the effect.
This method of treatment was first used at the border of the nineteenth and twentieth centuries. At first they used for this potassium bromide, began to be used a little later and, starting in 1938, gained popularity Phenytoin.
Modern doctors use more than three dozen anticonvulsants. No matter how scary it may sound, the fact remains that in our time about seventy percent of the planet's population have light form epilepsy.
But if in some cases the problem is successfully solved anticonvulsants, then complex forms of such an ancient disease as epilepsy are not so easy to cure.
IN in this case main task The drug is intended to eliminate spasms without disrupting the functioning of the central nervous system.
It is designed to have:
- antiallergic properties;
- completely eliminate addiction;
- avoid depression and despondency.
Groups of anticonvulsants
In modern medical practice anticonvulsants or anticonvulsants divided by different groups depending on the main active ingredient.
These today are:
- Barbiturates;
- Hydantoin;
- Oxazolidionone group;
- Succinamide;
- Iminostilbenes;
- Benzodiazepine;
- Valproic acid;
Anticonvulsants
The main drugs of this type:
- Phenytoin. Indicated if the patient’s seizures are of a pronounced epileptic nature. The drug inhibits the action of nerve receptors and stabilizes membranes at the cellular level.
Has side effects, including:
- vomiting, nausea;
- dizziness;
- spontaneous eye movement.
- Carbamazepine. Used for prolonged attacks. IN active stage diseases, the drug is able to stop attacks. Improves the patient's mood and well-being.
Main side effects will turn out to be:
- dizziness and drowsiness.
Contraindicated pregnant women.
- Possible use in combination with other drugs. This medicine perfectly calms the central nervous system. As a rule, it is prescribed for a long time. It should also be withdrawn gradually.
Side effects:
- changes in blood pressure;
- breathing problems.
Contraindicated for:
- initial stage of pregnancy;
- renal failure;
- alcohol addiction;
- and muscle weakness.
- Used in the treatment of myoclonic epilepsy. Fights involuntary cramps. Under the influence of the medicine, the nerves calm down and the muscles relax.
Also among the associated effects: 
- increased irritability and apathetic state;
- discomfort of the musculoskeletal system.
During use the following is contraindicated:
- Lamotrigine. Successfully fights both mild seizures and severe epileptic seizures. The action of the drug leads to the stabilization of brain neurons, which, in turn, leads to an increase in the time between attacks. If successful, the seizures disappear completely.
Side effects may appear as:
- diarrhea;
- nausea;
- skin rash.
- Sodium valproate. Prescribed for the treatment of severe seizures and myoclonic epilepsy. The drug stops the production of electrical impulses in the brain, securing a stable somatic state of the patient. Side effects usually include stomach and intestinal disorders.
It is prohibited to take:
- pregnant women;
- for hepatitis and pancreatic disease.
- Used for psychomotor seizures, as well as in the treatment of myoclonic epilepsy. Slows down the activity of neurons in the damaged area and reduces spasms. The medicine can intensify arousal, therefore it is contraindicated in children and elderly people of the older generation.
Related actions include: 
- headache;
- development of anemia;
- apathy;
- nausea;
- allergic reactions and addiction.
Contraindications:
- pregnancy;
- liver and kidney diseases.
- Beclamid. Eliminates partial and generalized seizures. The drug reduces excitability and eliminates spasms.
Possible side effects:
- dizziness;
- bowel irritation;
- allergy.
- Benzabamil. It is usually prescribed to children with epilepsy, as it is the least toxic of its kind. Has a mild effect on the central nervous system.
Side effects are:
- lethargy;
- nausea;
- weakness;
- involuntary eye movement.
Contraindicated for:
- heart disease;
- kidney and liver diseases.
List of drugs without prescriptions
Unfortunately or fortunately, the composition of these drugs is such that they forbidden dispensed without a doctor's prescription on the territory of the Russian Federation.
If a pharmacist offers you to buy any anticonvulsant, saying that a prescription is not needed, know that this is illegal and he does it only at his own peril and risk!
The easiest way to get drugs today over the counter— order via the Internet. Formally, the courier, of course, will be obliged to ask you for a recipe, but most likely this will not happen.
List of drugs for children
Substances that can significantly reduce the excitability of the central nervous system are used as anticonvulsants for children. Unfortunately, many drugs of this type have a depressant effect on breathing and can be dangerous for the baby.
According to the level of danger, drugs are divided into two groups:
- The first includes: benzodiazepines, lidocaine, droperidol with fentanyl and sodium hydroxybutyrate. These drugs have little effect on breathing.
- The second group includes: chloral hydrate, barbiturates, magnesium sulfate. Substances more dangerous to breathe. They have a strong depressant effect.
The main drugs used in the treatment of seizures in children:
- Benzodiazepines. The most commonly used drug from this series is sibazon, also known as seduxen or diazepam. An injection into a vein can stop seizures within five minutes. In large quantities, respiratory depression is still possible. In such cases, it is necessary to inject physostigmine intramuscularly; it can eliminate the nervous system and facilitate breathing.
- Feitanil and droperidol. These drugs effectively act on the hippocampus (the area that triggers seizures), but due to the presence of morphine, babies under one year of age may have problems with breathing. The problem is eliminated with the help of nalorphine.
- Lidocaine. Almost instantly suppresses seizures of any origin in children when administered into a vein. During treatment, a saturating dose is usually administered first, after which they move on to droppers.
- Hexenal. It is a strong anticonvulsant, but has a depressant effect on the respiratory tract, and therefore its use in children is somewhat limited.
- Used for treatment and prevention. It is prescribed mainly for mild attacks, since the effect develops quite slowly from four to six hours. Main value drug in duration of action. In young children, the effect can last up to two days. Parallel administration of phenobarbital and sibazon gives excellent results.
List of drugs for epilepsy
Not all anticonvulsants are necessarily used to treat epilepsy. To combat this disease in Russia, about thirty medications.
Here are just a few of them: 
- Carbamazepine;
- Valproate;
- Ethosuximide;
- Topiramate;
- Oxcarbazepine;
- Phenytoin;
- Lamotrigine;
- Levetiracetam.
At the end of the article I would like to warn you. Anticonvulsants are quite serious drugs with special properties and consequences for the human body. Their thoughtless use can lead to very sad consequences. Such remedies can only be used after consulting with your doctor.
Don't study self-medication is not the case. Be healthy!
18.09.2016The modern arsenal of drugs is quite large, but insufficient to treat all forms of epilepsy. Bromides (potassium bromide) were the first anticonvulsants, introduced into the pharmacotherapy of epilepsy back in 1857 by Charles Locock. In 1938, phenytoin (diphenin), a derivative of hydantoin, which was structurally close to the barbiturates, was synthesized. Numerous antiepileptic drugs have subsequently been developed, but phenytoin remains the treatment 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. At the same time, how chemical compound valproic acid was synthesized 80 years earlier - in 1882. 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 the researchers, valproic acid itself had anticonvulsant properties (W. Gosher). Currently, valproates remain one of the groups of anticonvulsant drugs that are in great demand (the target for valproates is primary generalized seizures - convulsive absences and idiopathic forms of epilepsy) and are used as basic drugs for monotherapy in patients with epilepsy. IN last years New, fairly safe drugs, such as lamotrigine and topiramate, have been obtained and found their use, which are used next to drugs synthesized earlier, very often as combination therapy.
Antiepileptic drugs - These are drugs of various origins used to prevent or reduce (in intensity and frequency) their corresponding equivalents (loss or impairment of consciousness, behavioral and autonomic disorders, etc.), which are observed during recurrent attacks of various forms of epilepsy.
Epilepsy is a consequence of the occurrence in the cerebral cortex or subcortical brain centers (substantia nigra, tonsils, etc.) of foci of excitation, which is transmitted to the nervous and muscular systems, which leads to the development of epileptic convulsive seizures or an epileptic state. The cause of epilepsy is not clear, so the main medications are aimed at eliminating the seizure or preventing it.
Home clinical sign epilepsy is a sudden attack 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, and the release of bloody saliva due to biting the tongue. Such convulsions are classified as major attacks (grand mal). During minor seizures (petit mal), consciousness is lost for a very long time. a short time, sometimes even the sick person herself does not have time to notice this. Very frequent attacks 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 source of excitation. During a convulsive attack, medications are administered to the patient, and after its completion, individual anti-relapse pharmacotherapy is selected.
Classification of antiepileptic drugs
According to chemical structure:
I. barbiturates and their derivatives: phenobarbital (bafetal) benzobarbital (benzonal).
II. Hydantoin derivatives phenytoin (diphenin).
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 (Encorat, Encorat-chrono, convulex)
5.2) sodium valproate (Depakine, Depakine-Enterik)
5.3) combined (valproic acid and sodium valproate) depakine-chrono.
VI. Various anticonvulsant and antispastic drugs: lamotrigine (Lamictal), topiramate (Topamax), gabapeptin (Neuralgin).
By mechanism of action
1. Sodium channel inhibitors: phenytoin; carbamazepine; valproic acid; sodium valproate; topiramate; lamotrigine.
2. Drugs that suppress calcium channels (T and L types): trimethine; sodium valproate; Gabapentin.
3. Agents that activate the GABAergic system:
3.1) postsynaptic action benzodiazepines; barbiturates; gabapentin;
3.2) presynaptic action sodium valproate; tiagabine;
4. Drugs 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 for partial seizures (psychomotor seizures): carbamazepine; sodium valproate; lamotrigine; gabapentin; phenobarbital; clonazepam; difenin.
2. Means used for generalized seizures:
2.1) grand mal seizures ( grand mat): sodium valproate; carbamazepine; phenobarbital; diphenin; lamotrigine;
2.2) minor seizures of epilepsy - absence (petit mat): sodium valproate; lamotrigine; clonazepam.
3. Means used for status epilepticus: diazepam; lorazepam; clonazepam; anesthetics (sodium hydroxybutyrate, 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 (valproic acid derivatives, diazepam) (Fig. 3.13);
Muscle relaxant (phenytoin, clonazepam, diazepam) (Fig. 3.14);
Cerebroprotective;
Analgesic (Fig. 3.15).
Algorithm of the mechanism of action antiepileptic drugs can be reduced to two main points:
1) inhibition of pathological hyperactivity of nerve cells in the epileptogenic fire;
2) inhibition of the spread of hyperactivity from the epileptogenic focus to other neurons, prevents the generalization of excitation and the occurrence of attacks.
In a generalized form, it is customary to distinguish 3 main mechanisms antiepilepticactions drugs, in particular:
1) facilitation of GABA and glycine-dependent (inhibitory) transmission;
2) suppression of excitatory (glutamate- and aspartatergic) transmission;
3) change in ionic 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 attacks in alcohol withdrawal syndrome. Affective and schizoaffective psychoses (as a means of prevention). Diabetes insipidus central origin, polyuria and polydipsia of neurohormonal nature.
Status epilepticus, somnambulism, various forms of muscle hypertonicity, sleep disorders, psychomotor agitation. Convulsive syndrome during 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 attacks of seizures; when editing. How sedative to reduce anxiety, tension, fear. Hyperbilirubinemia. Behavioral disorders associated with epilepsy. Febrile convulsions in children, childhood tics. West syndrome.
Side effects of antiepileptic drugs their group affiliation is determined by their mechanism of action. Thus, drugs that increase GABAergic inhibition more often than others cause behavioral disorders in patients. Skin reactions in the form of a rash are more typical for drugs that affect sodium channels of cell membranes. Besides, adverse reactions can be determined by the pharmacological variability of the body - 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 when using any of the antiepileptic drugs; lupus-like syndrome is more common when using phenytoin and carbamazepine. These reactions are not dose dependent and can occur at any stage of therapy.
Dose-dependent side effects of anticonvulsants can be divided into 3 large groups:
1) from the central nervous system (phenobarbital, phenytoin, carbamazepine, benzodiazepines, topiramate)
2) hematological (valproate, carbamazepine, phenytoin, phenobarbital)
3) leading to reproductive health disorders (valproates).
Dose-dependent side effects from the central nervous system are important clinical significance. Phenytoin and carbamazepine can cause dysfunction of the brainstem and cerebellum, 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 exceeding 20 mcg/ml can lead to severe brainstem dysfunction and stupor. Already after the patient begins to emerge from stupor, a second wave of this complication is possible, due to the formation of a large number of toxic 10,11-epoxide metabolites. Cognitive side effects may occur with topiramate therapy, mainly during the titration period when the drug dose is rapidly increased.
Complications from the hematopoietic organs when using anticonvulsants can clinically manifest as leukopenia, neutropenia, thrombocytopenia, as well as complex ones - aplastic anemia, agranulocytosis and megaloblastic anemia. Megaloblastic anemia may occur with long-term use of phenytoin. Treatment with phenytoin and 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, which is dangerous during puberty.
Some adverse reactions to anticonvulsant zysobs are associated with their inductive effect on liver enzymes. This effect is most pronounced in phenobarbital, carbamazepine and phenytoin. Enzyme inducers may increase the elimination of drugs that are prescribed concomitantly, especially anticonvulsants (such as lamotrigine), corticosteroids, anticoagulants, and some antibiotics. Serious problems can arise if the metabolism of endogenous substances, for example, colecalciferol (vitamin D3), is increased, which leads to the development of rickets in children; metabolic disorders of steroid and thyroid hormones; increased levels of α1-acid glycoprotein, sex hormone binding globulin, γ-glutamyltransferase and alkaline phosphatase, the ability to cause exacerbation of porphyria.
Contraindications to the prescription of antiepileptic drugs: dysfunction of the liver and pancreas, hemorrhagic diathesis, sharp and chronic hepatitis AV blockade, myelodepression, history of intermittent porphyria, simultaneous use of MAO inhibitors and lithium preparations; myasthenia gravis; acute poisoning drugs that have a depressant effect on the central nervous system, and alcohol; drug dependence, drug addiction; chronic alcoholism; acute pulmonary failure, respiratory depression. Adams-Stokes syndrome, heart failure, cachexia; diseases of the hematopoietic system; pregnancy, lactation.
Sodium valproate - sodium salt valproic (dipropyloctic) acid.
Pharmacokinetics. After taking before meals, it is quickly and almost completely (70-100%) absorbed in the stomach and small intestine. In case of pre-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% bound to proteins, and 10% of it is in ionized form. It accumulates mainly in the structures of the central nervous system, where there is a large amount of GABA transaminase (cerebellum, etc.). Penetrates poorly into other body fluids and tissues: into 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 is 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, has not been fully studied, and does not fully explain the variety of clinical effects, since this drug has a wide spectrum of action and is indicated for almost all types of attacks. 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;
V) indirect impact on the synthesis and breakdown of GABA.
Gamma-aminobutyric transaminase (GABA-T) ensures the conversion of GABA to succinate (succinate, succinic) semialdehyde in the GABA cycle, which 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, human vigilance, while barbiturates significantly suppress it. In patients prone to depressive reactions, sodium valproate improves mood, improves mental state, and reduces fears without causing a hypnogenic effect.
In addition, valproate exhibits a moderate n-cholinolytic effect, as evidenced by the prevention of tonic convulsions caused by nicotine by valproate.
Indications: epilepsy, especially in children.
Rice. 3.16. Neurotransmitter profiles of sodium valproate action.
Note: “+” - activation; "-" - Inhibition, Sir - serotonin, N-xp - n-cholinergic receptor, DA - dopamine, NA - noradrension, GABA - γ-chobutyric acid, GABA-T GABA-transamine PDK - glutamate decarboxylase, BD-site - benzodiazepine site, Glu - glutamate
Contraindications: pregnancy, breastfeeding, liver disease, pancreas disease, hemorrhagic diathesis, hypersensitivity to the drug, alcohol consumption; Drivers and other persons whose work requires increased attention should not take the drug.
Side effects: decreased appetite, nausea, abdominal pain, vomiting, diarrhea, sometimes dysfunction of the liver, pancreas (usually 2-12 weeks after starting the drug does not require stopping treatment, but requires careful monitoring of the patient’s condition); hair loss (0.5%); weight gain; acute hepatoencephalopathy (exclusively children under 2 years of age in polytherapy) hemorrhagic-necrotizing pancreatitis (extremely rare).
Interaction. Sodium valproate in combination with diphenin and phenobarbital displaces both drugs from protein binding and significantly increases the content of their free fractions in the blood. In some cases, the drug combined with another antiepileptic drug can lead to agitation of the body.
Difenin (phenytoin) According to its 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 just one epileptic focus in the cerebral cortex or subcortical structures, but a decrease in the irradiation of epileptic discharges to other brain centers and through 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. This effect is likely due to 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.
Diphenine effectively suppresses the spread of epileptic impulses without changing normal function nerve cells. The drug significantly weakens, and in the case of long-term use, can completely prevent the development of major seizures in patients with focal or patchy 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 stomach and duodenum, severe violations liver and kidney functions, cardiac decompensation, diseases of the hematopoietic system.
Side effect triad of symptoms (nystagmus, diplopia, ataxia), gingival hyperplasia.
Carbamazepine, unlike diphenine, which suppresses the spread of epileptic discharges in the brain, acts predominantly on nerve cells of the spinal and medulla oblongata. Its anticonvulsant activity is almost 3 times less than diphenine. Carbamazepine normalizes metabolism, activates choline and adrenergic mediator systems, and has a high antidepressant effect. It significantly suppresses the activity of Na +, K + -ATPase and reduces the elevated level of cAMP, which is considered as the main mechanism of its antiepileptic effect. After taking it, patients' motivation for treatment increases, their mood and interest in their surroundings increase, depression, fear, and hypochondria decrease.
Indications: all forms of epilepsy, especially the “temporal” form with aura, myoclonic and tonic-clonic spasms of the facial muscles.
Contraindications: pregnancy, bronchial asthma, blood diseases, liver and kidney dysfunctions.
Side effect. Of course, adverse reactions appear in the first week after the start of treatment, more often in older people 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 carbamazepine is combined with diphenine, the level of the latter in the blood plasma may increase due to a delay in its metabolism. Diphenine and phenobarbital reduce the level of carbamazepine in the blood plasma by accelerating its biotransformation.
IN Lately 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 stimulants ( glutamic acid) or accumulation of inhibitory mediators (GABA, glycine) in the central nervous system. Tiagabine(gabitril) is, in contrast to the irreversible blocker of GABA, its functional blocker.
Lamotrigine blocks prolonged 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 voltage-gated sodium channels of neurons and prolongation of the cell's refractory period. Lamotrigine inhibits the release of excitatory glutamic acid, indicating a possible neuroprotective effect of this drug. Lamotrigine is well absorbed when taken orally (both with and without food). Bioavailability is close to 100 %. Serum concentration is achieved 2-3 hours after taking the drug. Lamotrigine is metabolized in the liver, mainly by conjugation with glucuronic acid. Its main metabolite, 2-N-conjugate of glucuronic acid, is excreted in the urine.
Indications: forms of epileptic seizures resistant to other drugs, primarily partial, primary and secondary generalization, absence seizures, atonic, Lennox-Gastaut syndrome.
Side effect allergic reactions in the form skin rashes, angioedema, diplopia, blurred vision, dizziness, drowsiness, headache, when combined with valproate - squamous dermatitis.
Interaction diphenine, phenobarbital and carbamazepine reduce the concentration of lamotrigine. Valproate increases (up to 2 or more times) the concentration of lamotrigine, taking into account the potentiating effect of the interaction of lamotrigine and valproate, it is recommended to prescribe a dose of lamotrigine no 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 concentration in blood plasma is achieved 2-4 hours after administration. Approximately 15% of the drug is bound 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 membrane sodium channels and potentiates GABA activity at non-benzodiazepine GABA receptor sites. Blocks the corresponding types of glutamate receptors of the postsynaptic membrane.
Indications: epilepsy (grand 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, thinking disorders.
