Hydazepam ic®

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

Composition:

Active substance: gidazepam;

1 sublingual tablet contains 20 mg (0.02 g) or 50 mg (0.05 g) of gidazepam;

Excipients: lactose monohydrate, mannitol (E 421), potato starch, povidone, sodium citrate, potassium acesulfame, crospovidone, talc, magnesium stearate, melon flavor.

Pharmaceutical form. Sublingual tablets.

Main physicochemical properties: tablets of white or white with creamish shade, flat cylindrical shape, with bevelled edges; the trade mark of the manufacturer is imprinted on one side of the tablet, a line on the other side.

Pharmacotherapeutic group.

Psycholeptics. Anxiolytics. Benzodiazepine derivatives. ATC code N05BA.

Pharmacological Properties

Pharmacodynamics

Hydazepam 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 its 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 within the first days of treatment, significantly reducing psychomotor agitation, anxiety, and irritability. The drug exerts the greatest effect on symptoms of withdrawal syndrome during remission in patients with alcoholism.

Pharmacokinetics

After sublingual administration, hydazepam is rapidly absorbed. Following sublingual administration of single doses, the effect of the drug appears within 5–15 minutes, reaching its maximum within 1–4 hours, followed by gradual decline. Hydazepam is predominantly distributed in the liver, kidneys, and adipose tissue. Its bioavailability is sufficiently high. It has been shown that only the dealkylated metabolite is detected in plasma; the unchanged drug is not detectable, even in trace amounts.

A distinctive feature of hydazepam pharmacokinetics is the slow elimination rate of its main metabolite after single-dose 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 hydazepam allow its use 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, fear (including prior to surgical interventions and painful diagnostic examinations), increased irritability, sleep disturbances, as well as emotional lability. Also used to control alcohol withdrawal syndrome and for supportive therapy during remission in chronic alcoholism, logoneuroses, and migraine.

Contraindications.

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

Interaction with other medicinal products and other types of interactions.

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

Special precautions for use.

Hydroxyzine should be used with caution in patients with open-angle glaucoma, chronic renal or hepatic insufficiency, and alcoholic liver disease.

The drug contains lactose and therefore should not be administered to patients with rare hereditary conditions such as galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding.

The drug should not be used during pregnancy or breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

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

Method of Administration and Dosage

The drug should be administered sublingually.

Take 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, 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 of the drug in the treatment of patients with 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, and 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 can be used in outpatient practice.

Children

The use of the drug in children is contraindicated.

Overdose

Possible occurrence of adverse effects typical for other benzodiazepine tranquilizers, such as drowsiness, lethargy, dizziness, nausea, mild ataxia, and allergic reactions. In such cases, the dose should be reduced or hydazepam discontinued.

Treatment: symptomatic therapy.

Side effects.

When using hidazepam in high doses or in patients with increased individual sensitivity, adverse effects typical for other benzodiazepine-derived tranquilizers may occur.

Nervous system side effects: headache, drowsiness, lethargy, reduced reaction speed, decreased attention and work capacity, general weakness, dizziness.

Gastrointestinal tract side effects: nausea.

Cardiovascular system side effects: arterial hypotension.

Musculoskeletal system side effects: muscle weakness.

Skin side effects: rashes, itching, skin hyperemia, urticaria.

Immune system side effects: allergic reactions, including angioneurotic edema.

Other: ataxia (a case of ataxia has been reported, temporally associated with hidazepam administration).

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

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 per blister; 1 blister (for 50 mg dosage) or 2 blisters (for 20 mg dosage) per carton.

Prescription status. Prescription only.

Manufacturer.

Limited liability company "INTERKHIM".

Manufacturer's address and location of business activity.

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