Acapella

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

Composition:

Active substance: 1-(hydrazinocarbonyl)-methyl-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one;

1 tablet contains 1-(hydrazinocarbonyl)-methyl-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one 0.02 g (20 mg);

Excipients: lactose monohydrate; potato starch; povidone; calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: tablets from white to almost white, round-shaped, with flat surface and beveled edges, with a score line.

Pharmacotherapeutic group. Psycholeptics. Anxiolytics. Benzodiazepine derivatives. ATC code N05BA.

Pharmacological Properties

Pharmacodynamics

The active ingredient of the medicinal product, 1-(hydrazinocarbonyl)-methyl-7-brom-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one, belongs to the group of benzodiazepine derivatives. It has an original spectrum of pharmacological activity, combining anxiolytic and activating effects with antidepressant action, while exhibiting minimal side effects and low toxicity. It acts as a daytime tranquilizer and a selective anxiolytic. It differs from other benzodiazepines by a pronounced activating effect and weakly expressed myorelaxant action. At moderate therapeutic doses, it does not cause drowsiness and does not accelerate fatigue during operant activity.

In patients with alcoholism during therapeutic remission, mild calming and anxiolytic effects were observed within the first days of treatment, with significant reduction in psychomotor agitation, anxiety, and irritability. The drug exerts its greatest effect on manifestations of withdrawal syndrome and during remission in patients with alcoholism.

Pharmacokinetics

After oral administration, the active ingredient of the medicinal product is rapidly absorbed. Following single doses, the effect of the drug appears within 30–60 minutes, reaching maximum within 1–4 hours, followed by gradual attenuation. The highest distribution occurs in the liver, kidneys, and adipose tissue. Biological availability is sufficiently high. It has been shown that only the dealkylated metabolite is detected in blood plasma; the unchanged drug is not detectable, even in trace amounts.

A distinctive feature of the pharmacokinetics of the active ingredient is the low elimination rate of its main metabolite after single administration. The elimination half-life from plasma is 146 hours, clearance is 3.03 L/h, and the mean residence time in the body is 127.32 hours.

The pharmacokinetic characteristics of the active ingredient allow its use as a tranquilizer with a reduced risk of adverse effects.

Clinical Characteristics

Indications

Use as a daytime tranquilizer in neurotic and psychopathic asthenias, in conditions accompanied by anxiety and fear (particularly prior to surgical interventions and painful diagnostic procedures), increased irritability, sleep disturbances, as well as emotional lability. Use for the management of alcohol withdrawal syndrome and for maintenance therapy during remission in chronic alcoholism, logoneuroses, and migraine.

Contraindications

Hypersensitivity to any component of the medicinal product. Severe pronounced myasthenia gravis, significant liver function impairment (cirrhosis, Botkin's disease), and kidney dysfunction.

Interaction with Other Medicinal Products and Other Forms of Interaction

The medicinal product is compatible with other psychotropic, hypnotic, and anticonvulsant agents. Akapella® potentiates the effect of phenamine and 5-hydroxytryptophan, and enhances the effects of alcohol, hypnotic drugs, neuroleptics, and narcotic analgesics.

Special precautions for use

The use of the medicinal product Acapella® should be restricted in individuals with open-angle glaucoma, chronic renal and hepatic insufficiency, and alcoholic liver disease.

The medicinal product contains lactose; therefore, it should not be administered to patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding. The medicinal product should not be used during pregnancy or breastfeeding.

Ability to influence reaction rate when driving or operating machinery. During treatment, patients should refrain from activities requiring heightened attention and rapid reaction.

Administration and Dosage

The medicinal product is taken orally.

Take without chewing, 20–50 mg up to 3 times daily. If necessary, the dose may be gradually increased to a total daily dose of 200 mg to achieve the therapeutic effect. A daily dose of 100 mg is considered optimal. Administration of higher daily doses (150–200 mg) may be accompanied by increased daytime drowsiness and a sensation of muscle weakness.

As a daytime tranquilizer, Acapella® is recommended for the treatment of asthenic, depressive, phobic, and hypochondriac disorders at doses of 60–120 mg daily.

The average daily dose of the drug for the treatment of neurotic, neurosis-like, psychopathic, and psychopath-like conditions is 60–200 mg; for migraine — 40–60 mg.

For the management of alcohol withdrawal, the initial dose is 50 mg, the average daily dose is 150 mg. The maximum daily dose in alcohol withdrawal is 500 mg.

The duration of treatment ranges from several days to 1–4 months and is determined individually by the physician depending on the patient's condition and disease course.

The drug may be used in outpatient practice.

Children. Use of the medicinal product in children is contraindicated.

Overdose

Adverse effects typical of other benzodiazepine tranquilizers may occur, such as drowsiness, lethargy, dizziness, nausea, mild ataxia, and allergic reactions. In such cases, the dose should be reduced or administration of Acapella® discontinued.

Treatment: symptomatic therapy.

Adverse Reactions

When using the medicinal product Akapella® in high doses or in patients with increased individual sensitivity, reactions typical of other benzodiazepine derivative tranquilizers may occur.

Central nervous system: headache, drowsiness, lethargy, reduced reaction speed, decreased attention and work capacity, general weakness, dizziness.

Gastrointestinal tract: nausea.

Cardiovascular system: arterial hypotension.

Musculoskeletal system: muscle weakness.

Skin: rash, pruritus, skin hyperemia, urticaria.

Immune system: allergic reactions, including angioneurotic edema.

Other: ataxia (a case of ataxia temporally associated with the use of the medicinal product has been reported).

If adverse reactions occur, the dose should be reduced or the medicinal product discontinued.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after registration of the medicinal product is of great importance. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the automated pharmacovigilance information system at: https://aisf.dec.gov.ua.

Shelf life. 2 years.

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

Storage conditions. Store at temperatures not exceeding 25 °C. Keep out of reach and sight of children.

Packaging. 10 tablets in a blister; 1 or 2 blisters per carton.

Prescription status. Prescription only.

Manufacturer: JSC "Farmak".

Manufacturer's address and place of business. 74, Kyrylivska Street, Kyiv, 04080, Ukraine.