Oxadol (Tablets, Solution) Instructions for Use

ATC Code

N02BG06 (Nefopam)

Active Substance

Nefopam (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Non-opioid centrally acting analgesic

Pharmacotherapeutic Group

Non-narcotic analgesic agent

Pharmacological Action

Non-narcotic centrally acting analgesic agent.

In vitro, Nefopam inhibited the reuptake of dopamine, noradrenaline, and serotonin in rat synaptosomes.

In vivo, Nefopam demonstrated antinociceptive activity in animals, possibly by reducing glutamate release at the presynaptic level and activating N-methyl-D-aspartate receptors at the postsynaptic level.

Nefopam showed a positive effect on postoperative shivering in clinical studies.

Nefopam does not have anti-inflammatory or antipyretic effects, does not depress respiration, and does not affect intestinal peristalsis.

Nefopam has a slight m-cholinolytic effect.

During studies, a temporary and moderate increase in heart rate and blood pressure was observed.

Pharmacokinetics

After a single 20 mg intramuscular dose, the maximum serum concentration is observed after 30-60 minutes and averages 25 ng/ml.

The T_1/2 averages 5 hours.

After an intravenous dose of 20 mg, the T_1/2 averages 4 hours.

Plasma protein binding is 71-76%.

Biotransformation is significant; three main metabolites have been identified: desmethylnefopam, Nefopam N-oxide, and Nefopam N-glucuronide.

Desmethylnefopam and Nefopam N-oxide are not glucuronidated in the liver and do not exhibit analgesic activity in animal studies.

It is excreted mainly by the kidneys: 87% of the administered dose is present in the urine, less than 5% of the administered dose is excreted unchanged.

The metabolites found in urine account for 6%, 3%, and 36%, respectively, of the intravenously administered dose.

Indications

Symptomatic treatment of acute pain syndrome, including postoperative pain.

ICD codes

Dosage Regimen

Tablets

The dose is set individually. Depending on the severity of the pain syndrome, take 30-90 mg orally 3 times/day.

The maximum daily dose is 120 mg.

Solution

The dose is set individually. The dose should correspond to the intensity of the pain syndrome and the patient’s response.

IM – 20 mg 3-4 times/day.

IV administered as an infusion. The recommended single dose is 20 mg. If necessary, the administration can be repeated every 4 hours.

During the administration of Nefopam and for 15-20 minutes after the injection, the patient should be in a lying position.

The maximum daily dose is 120 mg.

Adverse Reactions

From the CNS, psyche very common – drowsiness; common – dizziness; rare – convulsions, irritability, agitation, hallucinations, drug dependence; frequency unknown – confusion, coma.

From the digestive system very common – nausea, vomiting; common – dry mouth.

Allergic reactions rare – hypersensitivity, urticaria, angioedema, anaphylactic shock.

Other very common – increased sweating; common – tachycardia, urinary retention; rare – malaise.

Contraindications

Hypersensitivity to Nefopam; children under 15 years of age (due to lack of clinical data); convulsions or history of convulsions, epilepsy; risk of urinary retention caused by diseases of the urethra and/or prostate gland; risk of acute glaucoma; pregnancy, breastfeeding period.

Caution should be exercised in hepatic insufficiency; in renal insufficiency (due to the risk of accumulation and, consequently, an increased risk of adverse events); in patients with cardiovascular pathology, as the drug may cause tachycardia; in elderly patients, the use of Nefopam is not recommended due to its anticholinergic effect.

Use in Pregnancy and Lactation

Due to the lack of studies in animals and clinical data in humans, the risk of using the drug has not been established, therefore Nefopam is contraindicated during pregnancy and breastfeeding.

Use in Hepatic Impairment

Use with caution in patients with impaired liver function.

Use in Renal Impairment

Use with caution in patients with impaired renal function.

Pediatric Use

Contraindicated in children under 15 years of age.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

There is a risk of drug dependence when using Nefopam.

Nefopam does not belong to narcotic analgesics or opioid antagonists. Thus, discontinuation of treatment with narcotic analgesics in patients dependent on them who are already receiving Nefopam therapy increases the risk of withdrawal syndrome.

The benefit/risk ratio during treatment with the drug should be constantly re-evaluated.

Should not be prescribed for the treatment of chronic pain syndromes.

Should not be used concomitantly with alcohol, ethanol-containing and sedative drugs.

Effect on ability to drive vehicles and operate machinery

During treatment, it is not recommended to drive vehicles or engage in other activities requiring increased concentration and speed of psychomotor reactions due to the possible occurrence of drowsiness and, as a result, reduced alertness.

Drug Interactions

Concomitant use with narcotic drugs (analgesics, antitussives, and drugs for substitution therapy of addiction), neuroleptics, barbiturates, benzodiazepines, non-benzodiazepine anxiolytics (such as meprobamate), hypnotics, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), sedative H₁-histamine receptor blockers, centrally acting antihypertensive drugs, baclofen, thalidomide and other sedative agents is not recommended, as this may enhance CNS depression and lead to reduced alertness.

Ethanol and ethanol-containing drugs enhance the sedative effect of Nefopam.

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.