NEFOBOL

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NEFOBOL (NEFOBOL)

Composition:

Active substance: nefopam;

One coated tablet contains 30 mg of nefopam hydrochloride;

Excipients: calcium hydrogen phosphate dihydrate (Di-Tab); microcrystalline cellulose (Avicel pH 101); partially pregelatinized corn starch (starch 1500); colloidal anhydrous silicon dioxide (Aerosil 200 Pharma); magnesium stearate; Opadry (Y-1-7000).

Pharmaceutical form. Coated tablets.

Main physicochemical properties: white, round tablets, smooth on both sides.

Pharmacotherapeutic group.
Analgesics and antipyretics. ATC code: N02BG06.

Pharmacological Properties.

Pharmacodynamics.

Nefopam hydrochloride is a potent and fast-acting analgesic. It is completely different from other centrally-acting analgesics such as morphine, codeine, pentazocine, and propoxyphene.

Unlike narcotic agents, nefopam hydrochloride does not depress respiration. Preclinical studies have not confirmed dependence on nefopam hydrochloride.

Pharmacokinetics.

Nefopam hydrochloride is absorbed from the gastrointestinal tract. Peak plasma concentrations are reached approximately within 1–3 hours after oral administration.

Approximately 73% is bound to plasma proteins. The elimination half-life is about 4 hours. Nefopam hydrochloride is extensively metabolized and primarily excreted via urine. Less than 5% of the dose is excreted unchanged in urine. Approximately 8% of the dose is excreted in feces.

Clinical characteristics.

Indications.

For relief of acute and chronic pain, including postoperative pain, dental pain, musculoskeletal pain, acute pain due to injuries, and pain associated with oncological diseases.

Contraindications.

Hypersensitivity to nefopam or to any of the excipients.

Seizures or history of seizures.

Concomitant use of monoamine oxidase inhibitors (MAOIs).

Interaction with other medicinal products and other forms of interaction.

Caution is advised when administering nefopam concomitantly with tricyclic antidepressants.

It should be noted that nefopam may interfere with screening tests for benzodiazepines and opioids. These screening tests for benzodiazepines and opioids may yield false-positive results in patients taking Neobol.

Special precautions for use.

The side effects of Neofobol may be additive to the effects of other agents with anticholinergic or sympathomimetic activity.

The drug should not be used for the treatment of myocardial infarction, as there is no clinical experience regarding this indication.

Hepatic and renal impairment may interfere with the metabolism and elimination of nefopam.

Nefopam should be used with caution in patients with closed-angle glaucoma.

Cases of dependence and abuse with nefopam have been reported.

The drug should be used with caution in patients with urinary retention or at risk of urinary retention. Rarely, transient harmless pink discoloration of urine may occur.

Use during pregnancy or breastfeeding.

There are no data on the use of the drug in pregnant women. There are also no preclinical data indicating that the drug is safe. Neofobol should be avoided during pregnancy.

Neofobol should not be used during breastfeeding.

Ability to affect reaction speed when driving vehicles or operating machinery.

The risk of drowsiness during treatment with the drug should be considered, as it may affect the ability to drive vehicles or operate machinery.

Dosage and Administration

For oral use.

Adults

The dosage may range from 1 to 3 tablets three times daily depending on the severity of pain and individual patient response. The recommended initial dose is 2 tablets three times daily.

Special patient groups

Elderly patients: A dosage reduction may be required due to slowed metabolism. It is strongly recommended that the initial dose should not exceed 1 tablet three times daily, as elderly individuals are more sensitive, particularly to central nervous system side effects. Cases of hallucinations and confusion have been reported in this age group.

Patients with end-stage renal failure: During treatment with nefopam in patients with end-stage renal failure, increased peak plasma concentrations may occur. To avoid this, a reduction in the daily dose is recommended not only for elderly patients but also for patients with end-stage renal failure.

Children: The safety and efficacy of nefopam hydrochloride in children under 12 years of age have not been established; therefore, the use of this medicinal product in this age group is not recommended.

Overdose

The clinical picture of toxicity following overdose of nefopam hydrochloride involves the nervous system (convulsions, hallucinations, and agitation) and the cardiovascular system (coma, tachycardia with hyperdynamic circulation). Standard supportive measures should be taken, and the ingested drug should be promptly removed by gastric lavage or by inducing emesis. Oral administration of activated charcoal may help prevent absorption.

Seizures and hallucinations should be managed (e.g., by intravenous or rectal administration of diazepam). Beta-adrenergic blockers may help control cardiovascular complications.

Adverse Reactions.

Nausea, nervousness, dry mouth, mild dizziness, urinary retention, arterial hypotension, syncope, palpitations, gastrointestinal disorders (including abdominal pain and diarrhea), dizziness, anesthesia, seizures, tremor, confusion, hallucinations, angioedema, and allergic reactions may occur.

Less frequently reported are anaphylactic reactions, coma, vomiting, blurred vision, somnolence, sweating, insomnia, headache, and tachycardia.

Reporting of adverse reactions.

Reporting of suspected adverse reactions after drug registration is important. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Information System for Pharmacovigilance at the following link: https://aisf.dec.gov.ua.

Shelf life. 5 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C, in a place inaccessible to children.

Packaging. 10 tablets per blister; 3 blisters per cardboard box.

Prescription status.

Prescription only.

Manufacturer.

DjPAX Pharmaceuticals Private Limited / GPAX Pharmaceuticals Private Limited

Manufacturer's address and location of its business operations.

Plot No. 646/1&2, Agrawal Industrial Estate, Somnath Temple Road, Dabhel, Daman – 396 210, India / Plot No. 646/1&2, Agrawal Industrial Estate Somnath Temple Road, Dabhel, Daman – 396 210, India.

Marketing Authorization Holder.

Mili Healthcare Limited / Mili Healthcare Limited.

Address of the Marketing Authorization Holder.

Second Floor Office Suite, 4 Chartfield House, Castle Street, Taunton, Somerset, England TA1 4AS, Great Britain / Second Floor Office Suite, 4 Chartfield House, Castle Street, Taunton, Somerset, England TA1 4AS, Great Britain.