Barboval®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT BARBOVAL® (BARBOVAL)

Composition:

Active substances: ethyl ether of α-bromoisovaleric acid, solution of menthol in menthyl ether of isovaleric acid, phenobarbital;

1 capsule contains: ethyl ether of α-bromoisovaleric acid – 10 mg, solution of menthol in menthyl ether of isovaleric acid – 46 mg, phenobarbital – 9.8 mg;

Excipients: castor oil, lactose monohydrate (200), microcrystalline cellulose 102, crospovidone, calcium stearate, colloidal anhydrous silicon dioxide.

Pharmaceutical form. Hard capsules.

Main physicochemical properties: hard gelatin capsules size № 0, blue cap, white body with or without butterfly image. The capsule contents – a homogeneous powder of white or almost white color.

Pharmacotherapeutic group. Hypnotics and sedatives. Combined barbiturate preparations. ATC code N05CB02.

Pharmacological properties.

Pharmacodynamics.

Barbival® is a combined medicinal product, whose therapeutic effect is determined by the pharmacological properties of its constituent components.

Ethyl ether of α-bromoisovaleric acid exerts a reflex, sedative, and spasmolytic effect, which is due to reduced reflex excitability in the central parts of the nervous system and enhanced inhibitory processes in neurons of the cerebral cortex and subcortical structures of the brain, as well as decreased activity of central vasomotor centers and direct local spasmolytic action on smooth muscle.

Phenobarbital suppresses the activating influence of the reticular formation centers in the midbrain and medulla oblongata on the cerebral cortex, thereby reducing excitatory impulses to the cerebral cortex and subcortical structures. Reduction of activating influences results, depending on the dose, in sedative, tranquilizing, and hypnotic effects. Barbival® reduces excitatory influences on vasomotor centers and on coronary and peripheral vessels, thereby lowering overall arterial pressure and relieving or preventing vascular spasms, especially in the heart.

Menthol in menthyl isovalerate exerts a calming effect on the central nervous system, slows gastric and intestinal peristalsis, reduces meteorism, and also produces a moderate reflex vasodilatory and spasmolytic effect.

Pharmacokinetics.

Not studied.

Clinical characteristics.

Indications.

Neuroses accompanied by increased excitability, insomnia; hysteria; as part of complex treatment of mild angina attacks, initial stage of arterial hypertension; functional tachycardia; in gastric and intestinal spasms, flatulence.

Contraindications.

Hypersensitivity to any component of the drug, hepatic and renal insufficiency, hepatic porphyria, pronounced arterial hypotension, acute myocardial infarction, severe cardiac failure, diabetes mellitus, depression, myasthenia, alcoholism, narcotic and drug dependence, respiratory diseases with dyspnea, obstructive syndrome.

Interaction with other medicinal products and other types of interactions.

Concomitant use with neuroleptics and tranquilizers potentiates, while with central nervous system stimulants – reduces the effect of each component of the drug. Barboval®, containing barbituric acid derivatives, enhances the effect of local anesthetics, analgesics, and sedatives. Alcohol enhances the effects of the drug and may increase its toxicity. The drug's effect is enhanced when used concomitantly with valproic acid preparations. The presence of phenobarbital in Barboval® may induce liver enzymes, making its concomitant use undesirable with drugs metabolized in the liver (including coumarin derivatives – indirect anticoagulants, griseofulvin, glucocorticoids, oral contraceptives, cardiac glycosides, antimicrobial, antiviral, antifungal, antiepileptic, anticonvulsant, psychotropic, oral hypoglycemic, hormonal, immunosuppressive, cytostatic, antiarrhythmic, antihypertensive drugs), since their efficacy will be reduced due to increased metabolism.

Monoamine oxidase inhibitors (MAO inhibitors) prolong the effect of phenobarbital. Rifampicin may reduce the effect of phenobarbital.

Concomitant use of phenobarbital with gold preparations increases the risk of kidney damage.

With prolonged concomitant use of phenobarbital and nonsteroidal anti-inflammatory drugs, there is a risk of gastric ulceration and bleeding.

Concomitant use of phenobarbital with zidovudine increases the toxicity of both drugs.

The drug increases the toxicity of methotrexate. Consumption of alcoholic beverages should be avoided during treatment with this drug.

Special precautions.

The presence of phenobarbital in the medicinal product may lead to the development of Stevens-Johnson syndrome and Lyell's syndrome, which are most likely to occur during the first weeks of treatment. Prolonged use is not recommended due to the risk of drug dependence, possible accumulation of bromine in the body, and bromine poisoning. If chest pain does not subside after taking the drug, medical advice must be sought to rule out acute coronary syndrome. The drug should be prescribed with caution in cases of decompensated heart failure, arterial hypotension, hyperkinesia, hyperthyroidism, adrenal insufficiency, acute and persistent pain, and acute intoxication with medicinal products.

Castor oil contained in the medicinal product may cause stomach upset and diarrhea.

The drug contains lactose; therefore, it should not be used in patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding.

The drug should not be used in women during pregnancy or breastfeeding.

Ability to influence reaction speed when driving or operating machinery.

The medicinal product may cause drowsiness and dizziness; therefore, during treatment, patients should avoid working with hazardous machinery and driving vehicles.

Dosage and Administration

Barboval should be taken orally. The usual dose for adults is 1–2 capsules 2–3 times daily for 10–15 days. It is best to take the medication 20–30 minutes before meals. After a break of 10–15 days, the treatment course may be repeated. The maximum daily dose is 6 capsules.

Children

There is no experience with the use of this drug in pediatric practice; therefore, it is not recommended for use in children.

Overdose

Prolonged or frequent administration may lead to drug accumulation, resulting in clinical manifestations of overdose:

• Central nervous system depression, which can be counteracted by using CNS stimulants (e.g., caffeine, cordiamine);
• Nystagmus, ataxia, decreased arterial blood pressure, and blood count abnormalities.

Symptoms of chronic bromine poisoning include: depression, apathy, rhinitis, conjunctivitis, hemorrhagic diathesis, and impaired motor coordination. Symptomatic therapy is prescribed to manage these manifestations.

Prolonged continuous use of the drug may lead to habituation, drug dependence, and withdrawal syndrome. Abrupt discontinuation may cause a rebound effect. Long-term use may occasionally result in increased psychodynamic activity instead of the expected sedation.

Symptoms of overdose: respiratory depression, up to respiratory arrest; CNS depression, progressing to coma; cardiovascular depression, including arrhythmias and decreased arterial pressure, up to collapse; nausea, weakness, hypothermia, and reduced diuresis.

Treatment: symptomatic.

Side effects.

The drug is usually well tolerated.

Possible side effects include:

Gastrointestinal system: constipation, feeling of heaviness in the epigastric region, liver function disturbances with prolonged use, nausea, vomiting;

Nervous system: weakness, ataxia, impaired motor coordination, nystagmus, hallucinations, paradoxical excitement, decreased concentration, fatigue, slowed reaction time, headache, cognitive disturbances, confusion, drowsiness, mild dizziness;

Hematopoietic system: anemia, thrombocytopenia, agranulocytosis;

Cardiovascular system: arterial hypotension, bradycardia;

Immune system: hypersensitivity reactions, including angioedema, allergic reactions such as skin rash, itching, urticaria;

Skin and mucous membranes: Stevens-Johnson syndrome, toxic epidermal necrolysis;

Musculoskeletal system: with prolonged use of drugs containing phenobarbital, there is a risk of impaired osteogenesis;

Other: difficulty breathing.

Prolonged use of drugs containing bromine may lead to bromism, characterized by the following symptoms: central nervous system depression, depressive mood, confusion, ataxia, apathy, conjunctivitis, rhinitis, lacrimation, acne or purpura.

Shelf life. 4 years.

Do not use the drug after the expiry date stated on the packaging.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

10 capsules per blister. 1 or 3 blisters per carton.

Prescription status. Over-the-counter.

Manufacturer.

JSC "Farmak".

Manufacturer's address and place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.