Valproic acid: instructions for use, analogues and reviews

Valproic acid (sodium valproate) refers to a relatively new group of anticonvulsants, which differ from the previously used antiepileptic agents both in terms of chemical structure and the principle of action.

Description of the substance

This chemical was synthesized in 1882 as an analogue of valerian acid by Dr. V. Barton. It consists of 2 groups of cut. For many decades, the valproic acid was used only in the laboratory as an inert solvent of various organic compounds. Its antisuspicious properties were discovered by a fluke.

Valproic acid is clear and liquid at room temperature. In this case, it is capable of interacting with a base, for example sodium or magnesium hydroxide, to form a salt of valproate, which is a solid substance. This substance, in fact, is 2-propylvaleric acid and its sodium salt. Unlike other antiepileptic drugs, it is a nitrogen-free compound. The mechanism of action of this acid and its salts is associated with a specific effect on the metabolism of gamma-aminobutyric acid, which is an inhibitor of the enzyme transferase.

Preparations, which contain valproic acid, lower the exciting and convulsive reaction of the motor zones of the brain. This is due to the fact that this substance increases the content of gamma-aminobutyric acid in the structures of the nervous system. Valproic acid, whose reviews indicate its effectiveness in the treatment of anticonvulsants, belongs to the group of fatty acid derivatives.

Characteristics of valproic acid, its analogs

Valproic acid, the instruction to which describes its complex effects on humans, is issued under different names. The most famous drugs, which include this substance, are "Depakin", "Konvuleks", "Convulsofin", "Orphilin", "Deprakin", "Epilim", "Everiden", "Enkorat", "Apilepsin", "Valparin XP, Dipromal. In the finished dosage forms, it can be in the form of an acid or a sodium salt thereof, called sodium valproate. The activity of the drug does not decrease from this. Valproic acid, analogues of which are listed above, is taken orally right after eating. All preparations containing it are rapidly absorbed. After 2 hours, this acid appears in the blood plasma. It penetrates well through tissue barriers. Residual traces of this substance are determined in the cerebrospinal fluid and in many other internal environments of the body. It is found in amniotic fluid (amniotic fluid) in pregnant women.

Operating principle

How does valproic acid work? The instruction to this drug does not give an exact answer to the question of what is the mechanism of its therapeutic influence. This is due to the fact that the experts have not yet fully studied its effect on the change in the properties of sodium channels. In this case, valproic acid is included in the list of medicines that are vital and important for people.

Action per person

Valproic acid is used not only for epilepsy. The instruction for the use of this medication indicates that it has not only an anticonvulsant effect. It improves the mood, as well as the mental state of a person. Experts say that this acid has a tranquilizing component. Unlike other drugs of this kind, it reduces the state of fear, without having a miolexant or sedative effect. This is due to its effect on postsynaptic membranes. At the same time, the processes of nerve impulse transmission are suppressed.

In small forms, epilepsy is most often limited to the intake of a single valproic acid or its analogues. In more severe cases, this drug is combined with other antiepileptic drugs.

Valproic acid in epilepsy

This drug is used for various forms of epilepsy. In this case, its reception is based on the established by the doctor scheme. Valproic acid, the instruction for its use indicates its effectiveness in various forms of this disease, is used in individual cases in different doses. It is also often prescribed for focal seizures.

Application of the drug

Valproic acid, the instruction to which requires the appointment of the medicine by the attending physician and strict adherence to the therapy regimen, is applied in such cases:

• prevention of various complications in epilepsy;

• convulsive conditions that occur in certain diseases of the central nervous system;

• presence of a nervous tic;

• Manic-depressive psychosis, which is not amenable to treatment with preparations containing lithium;

• convulsive conditions that occur in childhood.

The intake of valproic acid and preparations containing it must be carried out exclusively under the supervision of the attending physician. Only after carrying out all necessary researches and an estimation of a condition of the patient the expert can choose safe and effective dosage of the given medicine.

Form of issue

Valproic acid, the form of which can be different, is packaged by different manufacturers in the following form:

• Tablets coated with a shell soluble in the intestine. They contain 150, 200, 300, 500 mg of valproic acid (sodium valproate).

• Capsules of 150, 300 mg.

• Medicine (syrup) containing 50 or 300 ml of drug substance in 1 ml.

Compatibility with other drugs

Valproic acid can enhance the action of other anticonvulsants and antieleptics, antipsychotics, antipsychotics, antidepressants, and alcohol. When taking this medicine, alcohol can not be consumed. Valproic acid, analogues of this drug, salicylic acid and anticoagulants have a retarding effect on platelet aggregation. When ingested, this drug is rapidly absorbed into the bloodstream. In this case, the use of valproic acid simultaneously with any food reduces its effectiveness somewhat.

Side effects

This drug sometimes causes side effects in the form of nausea, vomiting, decreased appetite, severity and soreness in the stomach, diarrhea. Coverage or antispasmodics are used to eliminate these conditions. Valproic acid can cause general depression and fatigue, so it is rarely prescribed to people engaged in intense physical and mental work. Taking this medication sometimes leads to nervous system disorders that manifest themselves as tremor of limbs, bifurcation of images and a visual disturbance, drowsiness, headache, dizziness, psychomotor agitation, depressive state and apathy.

In some cases, the administration of this drug leads to the following consequences: decrease and increase in body weight, the appearance of allergic reactions, temporary hair loss, menstrual irregularities, changes in the hemogram. Rare but very serious side effects of taking this remedy are violations of the functioning of the liver or pancreas, a decrease in blood coagulability. Hepatotoxic effect is most likely when taking this drug simultaneously with clonazepam, phenobarbital.

When using valproic acid, it must be remembered that in diabetic patients it is able to distort the result of urine analysis, increasing the content of ketone bodies in it. To prevent various complications during treatment, the content of bilirubin, liver enzymes, and platelet counts are regularly determined.

Contraindications

Valproic acid, whose products are sold in a pharmacy without a prescription, also has serious contraindications. These include:

• impaired functioning of the pancreas and liver;

• porphyria;

• diathesis hemorrhagic;

• individual intolerance;

• First trimester of pregnancy;

• the period of feeding (the drug passes into the mother's milk).

In the second and third trimester of pregnancy, this drug is prescribed in smaller doses and only for serious indications, as it penetrates the placenta and can affect the unborn child.

When taking valproic acid, you must carefully monitor the functioning of the liver, monitor blood clotting and platelet aggregation. During the treatment with this drug, women who have sex life should use the most reliable methods of contraception to prevent pregnancy.

Schemes of application

Preparations containing this acid are taken in different schemes. Optimum doses are selected individually. The choice of the regimen is influenced by the patient's condition, weight and age. Most often at the beginning of the course, adults and children weighing more than 25 kg are prescribed 10-15 mg / kg per day. In the future, every week the dose of the drug is increased by 5-10 mg / kg, bringing it to a maximum of 30 mg / kg. The daily dose for children is 20-50 mg / kg. When switching to treatment with valproic acid, the use of other anticonvulsant drugs is gradually reduced. The maximum dose of valproic acid should not be higher than 50 mg / kg per day.

There are various forms of release of this medication. Intravenous administration involves taking 400-800 mg of sodium valproate per day. Throughout the course of therapy it is necessary to determine the level of this drug in the blood. According to the analysis, corrections can be made to the treatment regimen.

Approximate schemes of application:

• Children under 3 years: in the first week they drink 150 mg 1 p. A day, the second - 150 mg of 2 p. Per day, and in the third - 150 mg 3 r. in a day.

• Children 3 to 10 years: in the first week, take 450 mg, the second - 600 mg, the third - 900 mg per day. According to another scheme, 300, 450, 600, 900 mg per day, respectively, at 1, 2, 3 and 4 weeks.

• After 10 years: in the first week they drink 600 mg, the second - 900, the third - 1200 mg per day. According to another scheme, 300, 600, 900, 1200 mg per day are taken at 1, 2, 3 and 4 weeks, respectively.

For patients who have previously taken other anticonvulsants, valproic acid is prescribed in reduced doses. At the same time, the number of other funds is decreasing. The maintenance dose for adults is 900-1200 mg. Valproic acid, tablets and capsules that are prescribed only after 10 years, is taken in 2-4 admission. For children, a syrup or mixture with this drug is most often prescribed.

"Depakin" (valproic acid)

On sale there are different drugs with this acid, but one of the most popular is "Depakin". In pharmacies there are several types of this drug: "Chrono", "300 Enteric", "Chrono-sphere granules" and others. All of them differ somewhat in the content of the active substance and in the form of the release. "Depakin" is prescribed as an anticonvulsant and mood-stabilizing drug. He proved himself well in the treatment of epilepsy, bipolar disorders, tonic-clonic seizures, myoclonus, depression, migraine headaches. It is also used for the therapy of neuropathic pain. Recently, this drug has been studied as a medicine for some types of cancer and HIV infection.

Valproic acid prolonged action

Among drugs valproic acid "Depakin" and its analogues are in high demand. This is due to the fact that it has a prolonged effect. Use of this drug leads to a decrease in the frequency of the appearance of convulsive seizures. It also reduces their severity and facilitates flow. "Depakin" reduces the likelihood of developing more severe complications.

The processes of valproic acid metabolization are carried out by liver cells. When taking the usual substance, the elimination half-life is about 6-8 hours. Modern drugs allow you to maintain a therapeutic concentration of the active substance in the body up to 16 hours. The rate of excretion of valproic acid depends to a large extent on the functioning of the liver. Valproic acid, reviews of which are more positive, affects each patient in its own way. This is due to the fact that each organism is unique and can perceive this substance with some deviations from the norm.