Hydazepam ic®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT GIDAZEPAM® IS (GIDAZEPAM® IS)

Composition:

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

Each tablet contains 1-(hydrazinocarbonyl)-methyl-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one 20 mg (0.02 g) or 50 mg (0.05 g);

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

Pharmaceutical form. Tablets.

Main physicochemical properties: tablets of white or white with cream shade color, flat cylindrical shape, with a bevel; the company trademark is imprinted on one surface of the tablet.

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 selective anxiolytic. It differs from other benzodiazepines by the presence of a pronounced activating effect and weakly expressed myorelaxant action. At moderate therapeutic doses, it does not produce sedative effects and does not accelerate fatigue during operant activity.

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

Pharmacokinetics

After oral administration, the active ingredient of the medicinal product is rapidly absorbed. Following single doses, the drug's effect 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, while 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 86.7 hours, clearance is 3.03 L/h, and the mean residence time is 127.32 hours.

The pharmacokinetic characteristics of the active ingredient allow the medicinal product to be used as a tranquilizer with a reduced risk of adverse effects.

Clinical characteristics.

Indications.

Used as a daytime tranquilizer in neurotic and psychopathic asthenias, in conditions accompanied by anxiety and fear (including prior to surgical interventions and painful diagnostic examinations), increased irritability, sleep disturbances, as well as emotional lability. Also used for managing alcohol withdrawal syndrome and for maintenance therapy during remission in chronic alcoholism, logoneuroses, and migraine.

Contraindications.

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

Interaction with other medicinal products and other forms of interactions.

The medicinal product is compatible with other psychotropic, hypnotic, and anticonvulsant drugs. Potentiates the effect of phenamine and 5-oxytryptophan, enhances the effect of alcohol, hypnotic agents, neuroleptics, and narcotic analgesics.

Special precautions for use.

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

The product contains lactose and therefore should not be administered to patients with rare hereditary disorders of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding.

This product should not be used during pregnancy or breastfeeding.

Ability to influence the speed of reactions when driving or operating machinery.

During treatment, patients should avoid activities requiring heightened attention and quick reactions.

Dosage and Administration.

The drug is intended for oral use.

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

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

The average daily dose for treating patients with neurotic, neurosis-like, psychopathic, and psychopathy-like conditions is 60–200 mg; for migraine – 40–60 mg.

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

The duration of treatment course 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.

The use of the drug 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 the drug discontinued.

Treatment: symptomatic therapy.

Adverse reactions.

When the medicinal product is used in large doses or in patients with increased individual sensitivity, reactions typical for other benzodiazepine derivative tranquilizers may occur.

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: rashes, itching, skin hyperemia, urticaria.

Immune system: allergic reactions, including angioedema.

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

If adverse reactions occur, the dose should be reduced or the medication should be 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. Medical and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all cases of suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at https://aisf.dec.gov.ua.

Shelf life. 5 years.

Storage conditions.

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

Keep out of reach of children.

Packaging.

10 tablets in a blister; 1, 2 or 3 blisters per pack (for the 20 mg dosage).

10 tablets in a blister; 1 or 2 blisters per pack (for the 50 mg dosage).

Prescription category. Prescription only.

Manufacturer.

Limited Liability Company "INTERSHEM".

Manufacturer's location and address of its business activity.

Ukraine, 65025, Odesa, 21st km, Starokyivska Road, 40-A.