Mastodon

Nefopam (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

Centrally acting 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 elimination half-life (T1/2) averages 5 hours.

After a 20 mg intravenous dose, the T1/2 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 the urine account for 6%, 3%, and 36% of the intravenously administered dose, respectively.

Indications

Symptomatic treatment of acute pain syndrome, including postoperative pain.

ICD codes

ICD-10 code Indication
R52.0 Acute pain
R52.2 Other chronic pain
ICD-11 code Indication
MG30.Z Chronic pain syndrome, unspecified
MG31.Z Acute pain, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Solution

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

Intramuscularly – 20 mg 3-4 times/day.

Intravenously 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.

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.

Adverse Reactions

From the central nervous system, 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; the use of Nefopam in elderly patients is not recommended due to its anticholinergic effect.

Use in Pregnancy and Lactation

Due to the lack of animal studies 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 persons.

Special Precautions

When using Nefopam, there is a risk of drug dependence.

Nefopam does not belong to narcotic analgesics and opioid antagonists. Thus, discontinuation of treatment with narcotic analgesics in dependent patients 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.

It should not be prescribed for the treatment of chronic pain syndromes.

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

Effect on the 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 consequence, reduced alertness.

Drug Interactions

Concomitant use with narcotic drugs (analgesics, antitussives, and drugs for substitution therapy of dependence), 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 central nervous system depression and lead to reduced alertness.

Ethanol and ethanol-containing preparations 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.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

B-PHARM, LLC (Russia)

Manufactured By

Kursk Biopharmaceutical Plant – Firm "Biok", FKP (Russia)

Dosage Form

Bottle Rx Icon Nefopam Infusion and intramuscular injection solution 10 mg/1 ml: amp. 2 ml 5 pcs.

Dosage Form, Packaging, and Composition

Solution for infusion and intramuscular injection transparent, colorless.

1 ml
Nefopam hydrochloride 10 mg

Excipients : sodium phosphate dibasic dodecahydrate – 1.72 mg, sodium phosphate monobasic dihydrate – 16.1075 mg, water for injections – up to 1 ml.

2 ml – ampoules (5) – cardboard packs.

Marketing Authorization Holder

R-Pharm JSC (Russia)

Dosage Form

Bottle Rx Icon Nefopam Infusion and intramuscular solution 10 mg/ml: 2 ml vial 5 pcs.

Dosage Form, Packaging, and Composition

Solution for infusion and intramuscular injection transparent, colorless.

1 vial
Nefopam hydrochloride 20 mg

Excipients : sodium phosphate dibasic dodecahydrate – 3.44 mg, sodium phosphate monobasic dihydrate – 32.215 mg, water for injections – up to 2 ml.

2 ml – vials (5) – cardboard packs.

Marketing Authorization Holder

Ecofarmplus, JSC (Russia)

Dosage Form

Bottle Rx Icon Nefopam Infusion and intramuscular injection solution 10 mg/1 ml: amp. 2 ml 5 pcs.

Dosage Form, Packaging, and Composition

Solution for infusion and intramuscular injection transparent, colorless, odorless.

1 ml
Nefopam hydrochloride (calculated as dry substance) 10 mg

Excipients : sodium phosphate monobasic dihydrate – 16.1075 mg, sodium phosphate dibasic dodecahydrate – 1.72 mg, water for injections – up to 1 ml.

2 ml – ampoules of neutral glass (5) – contour cell packaging made of polyvinyl chloride film (1) – cardboard packs.

Marketing Authorization Holder

Endocrine Technologies, LLC (Russia)

Manufactured By

Moscow Endocrine Plant FSUE (Russia)

Dosage Form

Bottle Rx Icon Nefopam Infusion and intramuscular solution 10 mg/1 ml: 2 ml amp. 5 pcs. and 2 ml syringe-tubes 1, 2, or 5 pcs.

Dosage Form, Packaging, and Composition

Solution for infusion and intramuscular injection in the form of a colorless, transparent liquid.

1 ml
Nefopam hydrochloride 10 mg

Excipients : sodium phosphate dibasic dodecahydrate – 1.72 mg, sodium phosphate monobasic dihydrate – 16.11 mg, water for injections – up to 1 ml.

2 ml – ampoules of colorless glass (5) – contour cell packaging (1) – cardboard packs.
2 ml – polyethylene syringe-tubes (1) – cardboard packs.
2 ml – polyethylene syringe-tubes (2) – cardboard packs.
2 ml – polyethylene syringe-tubes (5) – cardboard packs.

Marketing Authorization Holder

Endocrine Technologies, LLC (Russia)

Manufactured By

Moscow Endocrine Plant FSUE (Russia)

Dosage Form

Bottle Rx Icon Nefopam Film-coated tablets, 30 mg: 20 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; the core in cross-section is from almost white to light brown.

1 tab.
Nefopam hydrochloride 30 mg

Excipients : microcrystalline cellulose – 79.1 mg, povidone type K-30 – 2.7 mg, calcium hydrogen phosphate dihydrate – 7.8 mg, copovidone – 1.3 mg, pregelatinized starch – 6.5 mg, colloidal silicon dioxide – 1.3 mg, magnesium stearate – 1.3 mg.

Film coating composition ready-made white film coating – 4 mg, incl.: hypromellose (E464) – 2.96 mg, titanium dioxide (E171) – 1.04 mg.

10 pcs. – contour cell packaging (2) – cardboard packs.

Table of Contents

→ TABLE OF CONTENTS