Tazepam (Tablets) Instructions for Use

Marketing Authorization Holder

Tarchomin Pharmaceutical Works Polfa, S.A. (Poland)

ATC Code

N05BA04 (Oxazepam)

Active Substance

Oxazepam (Rec.INN registered by WHO)

Dosage Form

Tazepam

Film-coated tablets, 10 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; the cross-section of the tablet is white or almost white.

Excipients: potato starch – 5.5 mg, gelatin – 2.4 mg, polysorbate 80 – 0.1 mg, sodium carboxymethyl starch (type A) – 0.5 mg, talc – 1.7 mg, magnesium stearate – 1 mg, lactose monohydrate – 53.8 mg.

Film coating composition: hypromellose – 0.17 mg, macrogol 6000 – 0.03 mg.

25 pcs. – blisters (2) – cardboard packs with first-opening control (stickers).

Clinical-Pharmacological Group

Anxiolytic (tranquilizer)

Pharmacotherapeutic Group

Anxiolytic agent (tranquilizer)

Pharmacological Action

Anxiolytic agent (tranquilizer) from the group of benzodiazepine derivatives. It has anxiolytic and sedative effects. Possesses anticonvulsant and central muscle relaxant activity. The mechanism of action is associated with the enhancement of GABA-ergic processes in the brain. It primarily affects the activating reticular formation of the brain, reducing the perception of impulses from sensory receptors to the limbic system and diminishing emotional coloring.

Pharmacokinetics

After oral administration, it is absorbed slowly and completely. Plasma protein binding is 97%. C_max is achieved within 1-4 hours and is 450 ng/ml after a 30 mg dose. It penetrates the blood-brain barrier, placental barrier, and into breast milk. It is metabolized in the liver to form glucuronides, which have no pharmacological activity. T_1/2 is 5-15 hours. It is excreted by the kidneys and in feces. C_ss is noted after 1-3 days of treatment. Accumulation upon repeated administration is minimal (belongs to benzodiazepines with short and medium T_1/2), elimination after discontinuation of treatment is rapid.

Indications

Neuroses, sleep disorders, psychovegetative disorders. Autonomic disorders in women associated with menstrual cycle disorders or the climacteric period, as well as with severe premenstrual syndrome. Reactive depressions (as part of combination therapy).

ICD codes

Dosage Regimen

Determine the dosage individually based on clinical indication and patient response.

Initiate therapy at a low dose and titrate upward to achieve the desired therapeutic effect.

The typical daily dosage ranges from 10 mg to 120 mg, divided into three or four separate administrations.

For mild to moderate anxiety disorders, administer 10-15 mg three to four times daily.

For severe anxiety states or alcohol withdrawal, a higher dosage of 15-30 mg three to four times daily may be required.

For sleep induction, a single dose of 15-25 mg may be administered at bedtime.

Use the lowest effective dose for the shortest duration necessary to minimize the risk of dependence and adverse effects.

In elderly or debilitated patients, initiate treatment at 10 mg once or twice daily; increase cautiously if needed.

Avoid abrupt discontinuation after prolonged use due to the risk of withdrawal syndrome.

Upon treatment completion, gradually reduce the dosage over a period of several days or weeks under medical supervision.

The total duration of therapy should be as brief as possible; regularly reassess the need for continued treatment.

Adverse Reactions

From the nervous system at the beginning of treatment (especially in elderly patients): drowsiness, dizziness, fatigue, impaired concentration, ataxia, unsteady gait and poor coordination of movements, lethargy, blunted emotions, slowed mental and motor reactions; rarely – headache, euphoria, depression, tremor, depressed mood, stupor, memory impairment, dystonic extrapyramidal reactions (uncontrolled movements, including eyes), weakness, muscle weakness during the day, dysarthria (slurred speech), confusion; extremely rarely – paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendency, muscle spasm, hallucinations, acute agitation, irritability, anxiety, insomnia).

From the hematopoietic system: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia.

From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, anorexia, constipation, diarrhea, impaired liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.

From the urinary system: urinary incontinence, urinary retention, impaired renal function.

From the reproductive system: increased or decreased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Effect on the fetus: teratogenicity, CNS depression, respiratory depression and suppression of the sucking reflex in newborns whose mothers used the drug.

Other: habituation, drug dependence, decreased blood pressure; rarely – respiratory center depression, visual impairment (diplopia), bulimia, weight loss, tachycardia, anterograde amnesia.

With a sharp dose reduction or discontinuation of use: withdrawal syndrome (irritability, headache, anxiety, agitation, excitement, feeling of fear, nervousness, sleep disturbance, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely – acute psychosis).

Contraindications

Coma, shock, acute alcohol intoxication with weakened vital functions, acute intoxication with drugs that have a depressant effect on the central nervous system (narcotic, hypnotic and psychotropic drugs), myasthenia gravis, closed-angle glaucoma (acute attack or predisposition), severe COPD (progression of the degree of respiratory failure), acute respiratory failure, severe depression (suicidal tendencies may be noted), pregnancy (especially the first trimester), lactation (breastfeeding), children under 6 years of age, hypersensitivity to oxazepam.

Use in Pregnancy and Lactation

Oxazepam has a toxic effect on the fetus and increases the risk of congenital malformations when used in the first trimester of pregnancy. Taking therapeutic doses later in pregnancy may cause CNS depression in the newborn. Continuous use during pregnancy can lead to physical dependence with the development of withdrawal syndrome in the newborn. Children, especially at a young age, are very sensitive to the CNS depressant effect of benzodiazepines. Use immediately before or during childbirth may cause respiratory depression, decreased muscle tone, hypotension, hypothermia, and sluggish sucking syndrome in the newborn. Contraindicated during lactation.

Use in Hepatic Impairment

Use with caution in hepatic insufficiency.

Use in Renal Impairment

Use with caution in renal insufficiency.

Pediatric Use

Contraindicated in children under 6 years of age.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Any change in dose should be carried out under medical supervision.

Use with caution in cases of tendency to arterial hypotension, increased risk of drug dependence formation, in elderly patients, with hepatic and/or renal insufficiency, cerebral and spinal ataxias, hyperkinesis, tendency to abuse psychotropic drugs, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, nocturnal apnea (established or suspected).

Oxazepam should not be used for a long time (for several months) due to the possibility of drug dependence development. During prolonged treatment, monitoring of liver function and peripheral blood status is necessary.

Effect on the ability to drive vehicles and mechanisms

During the treatment period, one should not drive vehicles or engage in other potentially hazardous activities that require increased attention; alcohol should not be consumed.

Drug Interactions

With simultaneous use with oral contraceptives, the effectiveness of oxazepam decreases.

With simultaneous use, the bioavailability of zidovudine is moderately increased and the frequency of headache development increases.

With simultaneous use with phenytoin, there is a risk of decreased plasma concentration of oxazepam.

With simultaneous use with ethanol, the depressant effect on the central nervous system is enhanced.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.