Gidazepam^® (Tablets) Instructions for Use

Marketing Authorization Holder

Valenta Pharm, JSC (Russia)

Manufactured By

Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)

Contact Information

VALENTA PHARM JSC (Russia)

ATC Code

N05BA (Benzodiazepine derivatives)

Active Substance

Hydrazinocarbonylmethylbromphenyldihydrobenzodiazepin (Grouping name)

Dosage Forms

	Gidazepam®	Tablets 20 mg: 30 pcs.
		Tablets 50 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Tablets white or almost white, round, flat-cylindrical, with a bevel.

Excipients: lactose monohydrate – 58 mg, potato starch, calcium stearate, povidone (K17).

10 pcs. – contour cell packs (3) – cardboard packs.

Tablets white or almost white, round, flat-cylindrical, with a bevel.

Excipients: lactose monohydrate – 115.5 mg, potato starch, calcium stearate, povidone (K17).

10 pcs. – contour cell packs (3) – cardboard packs.

Clinical-Pharmacological Group

Anxiolytic (tranquilizer)

Pharmacotherapeutic Group

Psychotropic agents. Anxiolytics. Benzodiazepine derivatives

Pharmacological Action

Mechanism of action

The active substance interacts with the benzodiazepine complex of the GABA receptor.

It enhances the inhibitory effect of GABA in the CNS by increasing the sensitivity of GABA receptors to the mediator.

It stimulates benzodiazepine receptors, reduces the excitability of subcortical structures of the brain, and inhibits polysynaptic spinal reflexes.

Pharmacodynamic effects

Gidazepam^® belongs to the group of benzodiazepine derivatives and has an original spectrum of pharmacological activity, in which the anxiolytic effect is combined with an antidepressant effect with low severity of side effects and low toxicity.

It has the properties of a daytime tranquilizer and a selective anxiolytic.

It differs from other benzodiazepines by having a weakly expressed muscle relaxant effect.

The anxiolytic effect is manifested in a reduction of emotional tension, weakening of anxiety, fear, and restlessness; the sedative effect is manifested in a reduction of psychomotor excitability, daytime activity, decreased concentration of attention, and reduced reaction speed.

It has practically no effect on productive symptoms of psychotic genesis (acute delusional, hallucinatory, affective disorders); a reduction in affective tension and delusional disorders is rarely observed.

In average therapeutic doses, it does not contribute to rapid fatigue during the performance of operational activities.

Pharmacokinetics

Absorption

When taken orally, Gidazepam^® is rapidly absorbed.

After a single dose, the effect of the drug develops within 30-60 minutes.

C_max is reached 4 hours after administration and is dose-dependent.

The bioavailability is 90%.

Distribution

C_max of the drug is noted in the liver, kidneys, and adipose tissue.

Metabolism

It has been established that only the dealkylated metabolite is detected in human plasma; the unchanged drug is not detected even in trace amounts.

Elimination

A feature of the pharmacokinetics of Gidazepam^® is the low elimination rate of its main metabolite after a single dose.

T_1/2 from plasma is 86.7 hours, clearance is 3.03 L/h, the time for determining the drug concentration in the blood is 127.32 hours.

Indications

For adults from 18 years

• Anxiety disorder;
• Alcohol withdrawal syndrome.

ICD codes

Dosage Regimen

Orally.

In the treatment of anxiety disorders, the average daily dose is 60-150 mg (20-50 mg 3 times/day).

The duration of treatment is from 7 days to 1 month with breaks.

The dose selection is carried out starting from the minimum and gradually increasing it to the optimal (the dynamics of complaints and the clinical picture can serve as a guide).

Treatment is carried out under strict medical supervision.

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

The duration of treatment is from several days (7-10 days) to 1 month.

Subsequently, the course of treatment is determined individually depending on the patient’s condition, drug tolerance, and the course of the disease.

Elderly patients do not require dose adjustment.

Patients with impaired renal function the drug is contraindicated in patients with chronic renal failure.

Patients with impaired hepatic function the drug is contraindicated in patients with chronic hepatic failure.

Children the safety and efficacy of Gidazepam^® in children aged 0 to 18 years have not been established.

Data are not available.

Adverse Reactions

The determination of the frequency of adverse reactions is carried out in accordance with the following criteria: very common (≥ 1/10), common (from ≥1/100 to <1/10), uncommon (from ≥1/1000 to <1/100), rare (from ≥1/10000 to <1/1000), very rare (<1/10000), frequency not known (cannot be estimated from the available data).

Blood and lymphatic system disorders very rare – neutropenia (with long-term use, periodic blood count monitoring is recommended), leukopenia, agranulocytosis, anemia, thrombocytopenia.

Nervous system disorders common – weakness, drowsiness, ataxia; uncommon – confusion, depression, dysarthria, incoherent speech, decreased activity, headache, dizziness, tremor, memory impairment, insomnia, hallucinations, anxiety, decreased ability and concentration of attention; rare – euphoria, depressed mood, catalepsy, extrapyramidal reactions (uncontrolled body movements, including eyes), hyporeflexia; changes on the electroencephalogram are possible; very rare – paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendency, muscle spasm, irritability, acute agitation).

Eye disorders uncommon – blurred vision, diplopia, nystagmus.

Cardiac disorders uncommon – palpitations, bradycardia.

Vascular disorders uncommon – fainting, cardiovascular collapse.

Gastrointestinal disorders uncommon – constipation, nausea, vomiting, dryness of the oral mucosa or hypersalivation, heartburn, hiccups, gastralgia, decreased appetite.

Hepatobiliary disorders very rare – jaundice (with long-term use, periodic liver function monitoring is recommended), impaired liver function, increased activity of hepatic transaminases and ALP.

Skin and subcutaneous tissue disorders rare – urticaria, skin rash, itching.

Musculoskeletal and connective tissue disorders uncommon – muscle weakness.

Renal and urinary disorders uncommon – urinary incontinence, urinary retention, impaired renal function.

Reproductive system and breast disorders uncommon – menstrual cycle disorders, decreased potency and libido.

Contraindications

• Hypersensitivity to hydrazinocarbonylmethylbromphenyldihydrobenzodiazepine (gidazepam) or to any of the excipients included in the drug;
• Myasthenia gravis;
• Chronic renal failure;
• Chronic hepatic failure;
• Acute attack of glaucoma;
• Angle-closure glaucoma.

With caution

Open-angle glaucoma; elderly and debilitated patients.

Use in Pregnancy and Lactation

Pregnancy

The use of the drug during pregnancy is contraindicated. If pregnancy occurs, the drug should be discontinued.

Breastfeeding

The use of the drug during breastfeeding is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be discontinued for the duration of treatment.

Fertility

Data on the effect of the drug on fertility are not available.

Use in Hepatic Impairment

The drug is contraindicated in patients with chronic hepatic failure.

Use in Renal Impairment

The drug is contraindicated in patients with chronic renal failure.

Pediatric Use

The safety and efficacy of Gidazepam^® in children aged 0 to 18 years have not been established. Data are not available.

Geriatric Use

Dose adjustment is not required.

Special Precautions

When using any benzodiazepines, a paradoxical reaction may develop in individual cases. If patients develop paradoxical reactions such as increased aggressiveness, acute states of agitation, anxiety, feeling of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, shallow sleep, the use of the drug should be discontinued.

It is necessary to take into account the personality type before prescribing the drug to exclude passive-dependent personality traits.

Long-term uncontrolled use of the drug (more than 4 weeks) should be avoided, as drug dependence and tachyphylaxis may develop.

To prevent the “withdrawal” syndrome (convulsions, tremor, abdominal and muscle cramps, vomiting, sweating), it is necessary to gradually discontinue the drug.

Psychotic disorders are possible in patients with severe depression.

Caution is required when prescribing the drug to patients with chronic lung disease, as respiratory failure may worsen.

During treatment, alcohol consumption should be avoided.

Excipients

Gidazepam^® contains lactose. Patients with rare hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take Gidazepam^®.

Effect on ability to drive vehicles and operate machinery

Gidazepam^® has a pronounced effect on the ability to drive vehicles and operate machinery.

Patients should be warned about the possibility of adverse reactions that affect these abilities (see the “Adverse Reactions” section).

During the treatment period, it is necessary to refrain from driving vehicles and operating machinery.

Overdose

Symptoms drowsiness, confusion, paradoxical agitation, decreased reflexes, areflexia, stupor, reduced reaction to painful stimuli, deep sleep, dysarthria, ataxia, visual impairment (nystagmus), tremor, bradycardia, shortness of breath or difficulty breathing, apnea, pronounced weakness, decreased blood pressure, collapse, depression of cardiac and respiratory activity, coma.

Treatment gastric lavage, intake of activated charcoal, monitoring of vital body functions, maintenance of respiratory and cardiovascular activity.

Symptomatic therapy.

Hemodialysis is not very effective.

As a specific antagonist, flumazenil can be used – intravenously (in a 5% glucose (dextrose) solution or 0.9% sodium chloride solution) at an initial dose of 0.2 mg (if necessary, up to a dose of 1 mg).

Drug Interactions

The drug enhances the depressant effect on the CNS of:

• Ethanol;
• Sedative and antipsychotic drugs (neuroleptics);
• Antidepressants;
• Narcotic analgesics;
• Drugs for general anesthesia;
• Muscle relaxants.

Inhibitors of liver microsomal enzymes and anticonvulsants enhance the effect of Gidazepam^®.

Storage Conditions

The drug should be stored out of the reach of children, in a light-protected place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 4 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.