Piracetam, Cinnarizine

Pharmacological properties

combined drug that improves blood circulation and brain metabolism.

Piracetam is a nootropic drug. It positively affects the processes of metabolism and blood circulation in the brain, increases its energy potential, stimulates redox processes, increases glucose utilization, improves microcirculation in ischemic areas of the brain. Piracetam improves the integrative activity of the brain, helps to consolidate memory, improves learning processes.

Cinnarizine is a blocker of calcium ions and histamine H₁receptors. It has vasodilating activity mainly against cerebral and coronary vessels, due to both the direct effect of the drug on the smooth muscles of blood vessels and its antagonism to certain endogenous vasoconstrictors (norepinephrine, angiotensin). Also potentiates the vasodilating effect of CO₂ on the vessels of the brain. Systemic blood pressure, contractility and myocardial conduction are not significantly affected. Increases red blood cell elasticity and decreases blood viscosity. As a result of antihistamine H₁-activity shows a weak sedative effect, reduces the excitability of the vestibular apparatus, reduces the tone of the sympathetic system, increases the resistance of tissues to hypoxia.

Both components mutually potentiate the antihypoxic effect of each other. The toxicity of the combination does not exceed the toxicity of the individual components.

Pharmacokinetics The combined drug is rapidly and completely absorbed in the digestive tract. The therapeutic effect is manifested in 1-6 hours.

C_max piracetam in plasma is observed after 2-6 hours.

Piracetam is distributed rapidly to all important organs.

Piracetam does not bind to plasma proteins and is not metabolized in the body, it penetrates well into tissues, the BBB and the placenta. Piracetam is excreted unchanged in the urine after approximately 30 hours.

After 1–4 h, the maximum level of cinnarizine is determined not only in the blood, but also in the liver, kidneys, heart, lungs, spleen and brain. It binds to 91% with plasma proteins. Cinnarizine is actively metabolized in the liver. About 30% of the metabolites are excreted in the urine, the rest through the intestines. T_½ - about 4 hours

Indications

Circulatory disorders. supportive treatment for symptoms of cerebrovascular origin, which include memory impairment and thinking functions, decreased concentration, mood disorders (irritability).

Migraine Prevention

Imbalance. Supportive care for symptoms of labyrinthine disorders, including dizziness, tinnitus, nystagmus, nausea, and vomiting.

Motion sickness. Prevention of motion sickness.

Application

Capsules eurizam should be used orally after meals, without chewing, with water.

Circulatory disorders: 1 capsule 3 times a day.

Imbalance: 1 capsule 3 times a day.

Diseases of movement: 1 capsule half an hour before a walk, repeated every 6 hours.

The course of treatment is 1-3 months. Do not use for longer than 3 months. It is possible to conduct 2-3 courses per year.

Children. Do not use in children.

Contraindications

Hypersensitivity to piracetam, cinnarizine or any of the auxiliary components of the drug; individual sensitivity to pyrolidone derivatives.

The terminal stage of renal failure, acute cerebrovascular accident (hemorrhagic stroke), Huntingtons chorea, parkinsonism, increased intraocular pressure, psychomotor agitation.

Side effects

From the nervous system: hyperkinesia, ataxia, headache, insomnia, vestibular disorders, increased frequency of epilepsy attacks, imbalance, tremors, hypersomnia, lethargy, dyskinesia, parkinsonism, fatigue.prolonged use in elderly patients can lead to the development of extrapyramidal phenomena.

From the immune system: hypersensitivity, including anaphylaxis.

From the digestive system: dry mouth, dyspepsia, abdominal pain, pain in the upper abdomen, discomfort in the stomach, diarrhea, cholestatic jaundice, increased salivation, nausea, vomiting.

From the vestibular system: vertigo.

On the part of the skin: angioedema, dermatitis, itching, rash, urticaria, photosensitivity, hyperhidrosis (hypersensitivity), lichen-like keratosis, subacute cutaneous lupus erythematosus and lichen planus.

Mental disorders: increased irritability, nervousness, drowsiness, depression, anxiety, embarrassment, confusion, hallucinations.

From the musculoskeletal system: muscle stiffness.

On the part of the blood system and lymphatic system: hemorrhagic disorders.

Other: asthenia, hypertension, hyperthermia, thrombophlebitis, increased sexual activity, weight gain.

special instructions

Evrysam may cause irritation in the epigastric region; taking the drug after a meal will reduce the irritation of the gastric mucosa.

Since Eurisam can cause drowsiness, especially at the beginning of treatment, you should refrain from the simultaneous use of alcohol and the use of drugs that inhibit the activity of the central nervous system (central nervous system depressants).

Avoid the use of Euryzam in porphyria.

Due to the fact that piracetam reduces platelet aggregation, it is necessary to prescribe the drug with caution to patients with hemostatic disorders, conditions that may be accompanied by hemorrhages (gastrointestinal ulcer), during major surgeries (including dental interventions), and patients with severe symptoms bleeding or a patient with a history of hemorrhagic stroke; patients who use anticoagulants, platelet antiplatelet agents, including low doses of acetylsalicylic acid.

The drug is excreted by the kidneys, so it is necessary to pay special attention to patients with renal failure. With long-term therapy for elderly patients, regular monitoring of renal function indicators is recommended; if necessary, the dose should be adjusted depending on the results of creatinine clearance studies.

Use the drug with caution in patients with liver failure.

The drug contains lactose. Therefore, patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use this medication.

Do not use the drug after the expiration date indicated on the package.

Use during pregnancy or lactation. Do not use the drug during pregnancy or lactation. If treatment with the drug is necessary, breast-feeding should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Caution should be exercised when driving vehicles or working with other mechanisms, given the possibility of adverse reactions from the central nervous system.

Interactions

Piracetam

Thyroid hormones. When combined with thyroid hormones (T3 + T4), increased irritability, disorientation and sleep disturbances are possible.

Acenocoumarol. Clinical studies have shown that in patients with severe recurrent thrombosis, the use of piracetam in high doses (9.6 g / day) did not affect the dose of acenocoumarol to achieve a prothrombin time (INR) of 2.5–3.5, but with its simultaneous a significant decrease in platelet aggregation, fibrinogen level, von Willebrand factors (VIII: C; VIII: vW: Ag; VIII: vW: Rco), blood viscosity and blood plasma was noted.

Pharmacokinetic interactions. The probability of changing the pharmacodynamics of piracetam under the influence of other drugs is low, since 90% of the drug is excreted unchanged in the urine.

In vitro, piracetam does not inhibit the cytochrome P450 isoform of CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11 at a concentration of 142, 426, 1422 μg / ml.

At a concentration of 1422 μg / ml, slight inhibition of CYP 2A6 (21%) and 3A4 / 5 (11%) was noted. However, level K_і of these two CYP isomers is sufficient when exceeding 1422 μg / ml. Therefore, metabolic interactions with drugs that undergo biotransformation by these enzymes are unlikely.

Antiepileptic drugs. The use of piracetam in a dose of 20 mg / day daily for 4 weeks or more did not change the curve of the concentration level and C_max antiepileptic drugs in blood plasma (carbamazepine, phenytoin, phenobarbital, sodium valproate) in patients with epilepsy.

Alcohol. The combined intake with alcohol did not affect the level of concentration of piracetam in the blood plasma and the concentration of alcohol in the blood plasma did not change when taking 1.6 g of piracetam.

Cinnarizine. Alcohol / CNS depressants / tricyclic antidepressants: concomitant use may enhance the sedative effect of any of these drugs or cinnarizine.

Diagnostic procedures. Due to the antihistamine action, cinnarizine can mask positive reactions to skin reactivity factors during a skin test, so the use of Evrysam should be discontinued 4 days before it.

Overdose

Symptoms: increased manifestations of side effects of the drug. in isolated cases of acute overdose, dyspeptic symptoms (diarrhea with blood, abdominal pain), a change in consciousness from drowsiness to stupor and coma, vomiting, extrapyramidal symptoms, arterial hypotension were observed. in children with an overdose, excitation reactions predominate - insomnia, anxiety, euphoria, irritability, tremor, nightmares, hallucinations, convulsions.

Treatment: gastric lavage, the use of activated carbon. There is no specific antidote. During the first hour after oral administration, gastric lavage is necessary. If warranted, activated carbon may be prescribed. Conduct symptomatic therapy. Perhaps the use of hemodialysis.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° c.