Radedorm^® 5 (Tablets) Instructions for Use

Marketing Authorization Holder

AWD.pharma GmbH & Co. KG (Germany)

ATC Code

N05CD02 (Nitrazepam)

Active Substance

Nitrazepam (Rec.INN registered by WHO)

Dosage Form

Radedorm® 5

Tablets 5 mg: 20 pcs.

Dosage Form, Packaging, and Composition

10 pcs. – blister packs (2) – cardboard packs.

Clinical-Pharmacological Group

Hypnotic drug

Pharmacotherapeutic Group

Hypnotic agent

Pharmacological Action

A hypnotic drug from the benzodiazepine group. It has a pronounced hypnotic effect, as well as anxiolytic, sedative, anticonvulsant, and central muscle relaxant effects.

The mechanism of action is associated with the enhancement of the inhibitory influence of GABA in the CNS by increasing the sensitivity of GABA receptors to the mediator as a result of the stimulation of benzodiazepine receptors.

It increases the depth and duration of sleep. Sleep usually occurs within 20-40 minutes after administration and lasts for 6-8 hours. It moderately suppresses the REM sleep phase.

Pharmacokinetics

Absorption from the gastrointestinal tract is rapid and complete. Bioavailability ranges from 54% to 98% (depending on the dosage form). Plasma protein binding is about 85-90%.

It penetrates well through histohematic barriers, including the blood-brain barrier and the placental barrier. It is metabolized in the liver by reduction of the nitro group and subsequent acetylation with the formation of inactive acetyl derivatives.

The T_1/2 is 16-48 hours (depends on the age and body weight of the patients). The main metabolites are excreted in the urine (65-71%) and in the feces (14-20%). About 1-5% is excreted unchanged by the kidneys.

Indications

Sleep disorders of various origins, somnambulism, premedication before surgical operations, encephalopathies accompanied by epileptic (myoclonic) seizures; epilepsy in children aged from 4 months to 1-2 years – West syndrome (infantile spasms or lightning nodding salaam seizures).

ICD codes

Dosage Regimen

Administer orally. Determine the dose, regimen, and duration of therapy individually based on the clinical indication, patient age, and condition.

For adult insomnia, initiate treatment with 5 mg once daily, taken 30-60 minutes before bedtime.

For premedication before surgical operations, a single dose of 5-10 mg is typically used.

In elderly or debilitated patients, initiate treatment with a reduced dose of 2.5 mg.

For the treatment of West syndrome (infantile spasms) in children aged 4 months to 2 years, the daily dose is 0.5-1.0 mg/kg body weight.

Adjust the dose cautiously based on tolerability and clinical response. The maximum daily dose for adults should not exceed 10 mg.

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

Avoid abrupt discontinuation after prolonged use. Taper the dose gradually under medical supervision to prevent withdrawal syndrome.

Adverse Reactions

From the nervous system: at the beginning of treatment (especially in elderly patients) – drowsiness, feeling of fatigue, dizziness, decreased ability to concentrate, ataxia, unsteady gait, lethargy, blunted emotions, slowed mental and motor reactions; headache, euphoria, depression, tremor, depressed mood, catalepsy, anterograde amnesia, confusion, dystonic, extrapyramidal reactions (uncontrolled body movements, including eyes), weakness, myasthenia, dysarthria; paradoxical reactions (aggressive outbursts, fear, suicidal tendency, muscle spasm, confusion, hallucinations, acute awakening, irritability, anxiety, insomnia).

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

From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea; impaired liver function, increased activity of “liver” 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 impairment and suppression of the sucking reflex in newborns whose mothers used Nitrazepam.

Other: habituation, drug dependence; decreased blood pressure; respiratory center depression, visual impairment (diplopia), bulimia, weight loss, tachycardia. With a sharp dose reduction or discontinuation – withdrawal syndrome.

Contraindications

Hypersensitivity to benzodiazepines; coma, shock, acute alcohol intoxication with weakening of vital functions, acute intoxication with drugs that have a depressant effect on the CNS (including narcotic analgesics and hypnotics); drug addiction, alcoholism; myasthenia gravis; closed-angle glaucoma (acute attack); temporal lobe epilepsy, severe COPD (progression of the degree of respiratory failure), acute respiratory failure, hypercapnia, severe depression (suicidal tendencies may be noted); pregnancy (especially the first trimester), lactation period (breastfeeding). During treatment, patients are strictly prohibited from consuming ethanol.

With caution hepatic and/or renal failure, respiratory failure, cerebral and spinal ataxias, hyperkinesis, history of drug dependence, tendency to abuse psychoactive drugs, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, nocturnal apnea (established or suspected); children and adolescents under 18 years of age; elderly age.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy (especially in the first trimester) and during lactation (breastfeeding). If it is necessary to use during lactation, breastfeeding should be discontinued.

Use in Hepatic Impairment

Should be used with caution in hepatic insufficiency.

Use in Renal Impairment

Should be used with caution in renal insufficiency.

Pediatric Use

Should be used with caution in children and adolescents under 18 years of age – strictly according to indications, in doses and dosage forms recommended for the respective age. It is necessary to strictly follow the instructions in the nitrazepam drug labels regarding contraindications for the use of specific nitrazepam dosage forms in children of different ages.

Geriatric Use

Should be used with caution in elderly patients.

Special Precautions

In renal/hepatic insufficiency and during long-term treatment, monitoring of the peripheral blood picture and liver enzyme levels is necessary.

The risk of drug dependence formation increases with the use of large doses (20 mg), significant duration of treatment in patients who have previously abused ethanol or drugs. With prolonged use, the development of tolerance is possible.

In case of drug dependence development, abrupt withdrawal of nitrazepam is accompanied by a withdrawal syndrome (headache, myalgia, anxiety, tension, confusion, irritability, agitation, excitement, feeling of fear, nervousness, sleep disturbances, increased sweating, depression, nausea, vomiting, tremor, in severe cases – derealization, depersonalization, hyperacusis, photophobia, paresthesia in the limbs; hallucinations and epileptic seizures, tachycardia, convulsions, hallucinations, rarely – acute psychosis).

Withdrawal of nitrazepam should be carried out gradually.

Effect on the ability to drive vehicles and mechanisms

During the treatment period, patients are prohibited from driving any vehicles and engaging in other activities that require high concentration and speed of psychomotor reactions.

Drug Interactions

The effect of nitrazepam is enhanced and prolonged with simultaneous use with cimetidine, oral estrogen-containing contraceptives (delayed excretion and prolonged T_1/2).

Inhibitors of liver microsomal enzymes prolong the T_1/2 of nitrazepam and increase the risk of toxic effects.

With simultaneous use, Nitrazepam reduces the effectiveness of levodopa in patients with parkinsonism.

Mutual enhancement of action occurs with simultaneous use with drugs affecting the CNS, including lithium preparations, narcotic analgesics, general anesthetics, ethanol, H₁-receptor blockers, sedative drugs, clonidine, barbiturates and other anxiolytic agents (tranquilizers), muscle relaxants.

With simultaneous use, inducers of liver microsomal enzymes reduce the effectiveness of nitrazepam. Narcotic analgesics enhance euphoria, leading to an increase in drug dependence.

With simultaneous use with nitrazepam, the effect of antihypertensive agents is potentiated.

Against the background of simultaneous use with clozapine, an enhancement of respiratory depression is possible.

With simultaneous use with nitrazepam, the toxicity of zidovudine may increase.

With simultaneous use with nitrazepam, valproic acid may enhance the effect of nitrazepam in children with epilepsy.

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.