Valecard-health

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT VАLECARD-ZDOROVYE (VALECARD-ZDOROVYE)

Composition:

Active substances: phenobarbital; ethyl ether of alpha-bromoisovaleric acid;

1 ml (20 drops) of the preparation contains phenobarbital 18.4 mg; ethyl ether of alpha-bromoisovaleric acid 18.4 mg;

Excipients: peppermint oil, hop oil, ethanol 96%, purified water.

Pharmaceutical form. Oral solution, drops.

Main physicochemical properties: colorless liquid with a fragrant odor and bitter taste. Opalescence may occur.

Pharmacotherapeutic group. Hypnotics and sedatives. Barbiturates in combination with drugs from other groups. ATC code N05C B02.

Pharmacological properties.

Pharmacodynamics. A combination medicinal product containing phenobarbital and ethylbromovalerianate (ethyl ether of alpha-bromovalerianic acid). Depending on the dose, both substances exert sedative and hypnotic effects, and at high doses – narcotic effects. Like other derivatives of barbituric acid, phenobarbital inhibits the inhibitory system of the reticular formation. Ethylbromovalerianate has both spasmolytic and sedative properties. Peppermint oil exerts a reflex vasodilatory and spasmolytic effect. At the concentration present in the medicinal product, ethylbromovalerianate acts as a synergist of phenobarbital (rapid onset of efficacy).

Pharmacokinetics. Phenobarbital is rapidly absorbed (directly in the stomach). Approximately 35% of it is bound to plasma proteins; the unbound portion is filtered by the kidneys. Reabsorption occurs at a low pH level. Reverse diffusion does not occur due to the alkalinity of urine. Approximately 30% of phenobarbital is excreted unchanged in urine, and only a small portion is oxidized in the liver. With prolonged use, accumulation of the active substance in plasma occurs, as well as induction of liver enzymes. As a result of this induction, the oxidation process of phenobarbital and other medicinal products is accelerated.

Bromine in ethylbromovalerianate is very slowly excreted from the body. If the drug is used for a prolonged period, accumulation of bromine in the central nervous system (CNS) occurs, leading to chronic bromine intoxication.

Clinical characteristics.

Indications.

• Functional disorders of the cardiovascular system;
• Neuroses accompanied by increased irritability and feelings of fear;
• Psychosomatically induced anxiety;
• States of excitation with pronounced vegetative manifestations;
• Sleep onset disorders.

Contraindications. Hypersensitivity to any component of the medicinal product. Diabetes mellitus, depression, myasthenia, acute hepatic porphyria, severe impairment of liver and kidney function. Medicinal products containing phenobarbital are contraindicated in alcoholism, drug and narcotic dependence (including in the medical history), respiratory diseases with dyspnea, obstructive syndrome, marked arterial hypotension, depressive disorders with a tendency toward suicidal behavior, and acute myocardial infarction.

Interaction with other medicinal products and other forms of interaction. When used concomitantly with other medicinal products that depress the CNS, mutual enhancement of effects (sedative-hypnotic effect) is possible, which may be accompanied by respiratory depression. Medicinal products containing valproic acid enhance the effect of barbiturates. Alcohol enhances the effect of the drug and may increase its toxicity. The drug increases the toxicity of methotrexate.

Phenobarbital induces liver enzymes and thus may accelerate the metabolism of certain drugs metabolized by these enzymes (e.g., coumarin derivatives, antibiotics, and sulfonamides). Unfavorable interaction of the medicinal product (due to phenobarbital content) with lamotrigine, thyroid hormones, doxycycline, chloramphenicol, antifungal agents (azole group), griseofulvin, glucocorticoids, and oral contraceptives due to the possibility of reduced efficacy of these agents.

Phenobarbital enhances the effect of analgesics, anesthetics, anesthetic agents, neuroleptics, and tranquilizers, while reducing the effect of paracetamol, indirect anticoagulants, metronidazole, tricyclic antidepressants, salicylates, and digoxin. There may be an effect on blood concentrations of phenytoin, as well as carbamazepine and clonazepam. Monoamine oxidase inhibitors (MAO) prolong the effect of phenobarbital. Rifampicin may reduce the effect of phenobarbital. When used concomitantly with gold-containing preparations, the risk of kidney damage increases. With prolonged concurrent use of nonsteroidal anti-inflammatory drugs, there is a risk of gastric ulceration and bleeding. Concurrent use of preparations containing phenobarbital together with zidovudine enhances the toxicity of both drugs.

Special precautions for use

The product contains 55% v/v ethanol.

Life-threatening skin reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome), have been reported with the use of phenobarbital.

Patients should be warned about the signs and symptoms, and skin reactions should be closely monitored. The risk of developing Stevens-Johnson syndrome and Lyell's syndrome is highest during the first weeks of treatment.

If symptoms of Stevens-Johnson syndrome or Lyell's syndrome occur (e.g., progressive skin rash, often with blisters, and mucosal lesions), treatment must be discontinued.

The best outcomes in treating Stevens-Johnson syndrome or Lyell's syndrome have been observed with early diagnosis and immediate discontinuation of any suspected causative drug.

If a patient has developed Stevens-Johnson syndrome or Lyell's syndrome while taking this medicinal product, the drug must never be administered to that patient again.

If chest pain persists after taking the product, medical advice must be sought to rule out acute coronary syndrome. Use with caution in patients with hyperkinesia, hyperthyroidism, adrenal insufficiency, decompensated heart failure, acute or persistent pain, severe arterial hypotension, and acute intoxication with medicinal products.

Prolonged use of the product is not recommended due to the risk of drug dependence, bromide accumulation in the body, and bromism.

Use during pregnancy or breastfeeding. The product is contraindicated during pregnancy and breastfeeding.

Ability to influence reaction speed when driving or operating machinery. The medicinal product reduces reaction speed. Patients should refrain from potentially hazardous activities requiring heightened attention and increased speed of mental and motor reactions.

Method of Administration and Dosage

For adult use only.

Take orally during meals, diluting a single dose in a small amount of liquid.

Recommended dosage: 15–20 drops three times daily. In patients with insomnia, the dose may be increased to 30 drops.

The duration of treatment is determined individually by a physician, depending on the clinical response and tolerability of the drug.

Children. There is no experience with the use of this drug in children.

Overdose.

Symptoms.

Acute (mild to moderate) barbiturate poisoning:

dizziness, fatigue, and even deep sleep from which the patient cannot be awakened.

Hypersensitivity reactions may occur: angioedema, urticaria, itching, rash.

Acute severe poisoning:

deep coma accompanied by tissue hypoxia; shallow breathing, initially rapid and later slowed; increased heart rate, depression of cardiovascular function (including cardiac arrhythmias, slowed pulse, decreased arterial pressure, bradycardia, vascular collapse); nystagmus, headache, diminished or absent reflexes; nausea, weakness, decreased body temperature, reduced diuresis.

Without emergency treatment, death may occur due to sudden depression of cardiovascular function, respiratory paralysis, or pulmonary edema.

With prolonged use of organic bromine compounds, bromine poisoning may develop, characterized by the following symptoms: confusion, ataxia, apathy, depressive mood, conjunctivitis, cold-like symptoms, acne, or purpura.

Treatment.

Cases of acute poisoning should be treated similarly to poisoning with other hypnotics and barbiturates, depending on the severity of symptoms. The patient should be transferred to an intensive care unit. Respiratory and circulatory functions must be stabilized and normalized. If necessary, perform artificial ventilation; treat shock with transfusion of blood plasma or plasma substitutes. If a significant amount of time has passed since ingestion, gastric lavage should be performed (introduce 10 g of activated charcoal powder into the stomach and slowly inject 2 tablespoons of sodium sulfate solution). To accelerate the elimination of barbiturates from the body, forced alkaline diuresis, hemodialysis, and/or hemoperfusion may be performed.

Treatment of bromine poisoning: elimination of bromide ions from the body can be accelerated by administering a large volume of sodium chloride solution along with saluretic agents.

In case of hypersensitivity reactions, administer desensitizing medications.

Side effects

Central nervous system: asthenia, weakness, ataxia, impaired motor coordination, nystagmus, hallucinations, paradoxical excitation, insomnia (in elderly patients), decreased concentration, fatigue, slowed reaction time, headache, cognitive disturbances. In individual cases, drowsiness and mild dizziness, confusion may occur.

Musculoskeletal system: with prolonged use of products containing phenobarbital, there is a risk of impaired osteogenesis and development of rickets. Cases of decreased bone mineral density, osteopenia, osteoporosis, and fractures have been reported in patients receiving long-term phenobarbital therapy. The mechanism by which phenobarbital affects bone tissue metabolism has not been established.

Gastrointestinal system: nausea, vomiting, constipation, feeling of heaviness in the epigastric area, with prolonged use – impaired liver function.

Blood system: agranulocytosis, thrombocytopenia, anemia (including megaloblastic).

Cardiovascular system: decreased arterial pressure, bradycardia.

Very rare: allergic reactions, including facial swelling, dyspnea, angioneurotic edema, rash, pruritus.

Serious skin adverse reactions reported with phenobarbital use: Stevens-Johnson syndrome, Lyell's syndrome, urticaria, rhinitis, conjunctivitis, lacrimation, acne, purpura.

Shelf life. 3 years from the date of manufacture in "in bulk" packaging.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 20 mL or 50 mL in a vial stoppered with a dropper plug and cap, in a box.

Dispensing category. Without prescription – 20 mL vials. By prescription – 50 mL vials.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's location and address of business activity.

22 Shevchenko Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.