For the Use of Registered Medical Practitioner Only

1. GENERIC NAME AND BRAND NAME:
Nefopam Hydrochloride tablets 30mg
NEFOSAR^TM

2. QUALITATIVE & QUANTITATIVE COMPOSITION:
Each film coated tablet contains:
Nefopam Hydrochloride…… 30 mg
Excipients…………………. q.s.
Colours: Titanium dioxide I.P., Red oxide of iron, & Yellow oxide of Iron

3. DOSAGE FORM & STRENGTH:
Refer section 1 & 2

4. CLINICAL PARTICULARS:

4.1 THERAPEUTIC INDICATIONS:
Indicated for the relief of acute and chronic pain, including post-operative pain, dental pain, musculo-skeletal pain, acute traumatic pain and cancer pain

4.2 POSOLOGY & AND METHOD OF ADMINISTRATION:
The usual oral dose range is 30 to 90 mg three times daily; the recommended initial dose is 60 mg (or 30 mg in elderly patients) three times daily

4.3 CONTRAINDICATIONS:
Nefopam is contraindicated in patients with a history of convulsive disorders and should not be given to patients taking monoamine oxidase (MAO) inhibitors. Nefopam should not be used in the treatment of myocardial infarction. This advice is based on the lack of clinical experience for this indication.

4.4 SPECIAL WARNINGS AND PRECAUTIONS FOR USE:
Hepatic and renal insufficiency may interfere with the metabolism and excretion of Nefopam. Nefopam should be used with caution in patients with glaucoma and with or at risk of urinary retention. Caution should be exercised when Nefopam is administered concurrently with tricyclic antidepressants. The side effects of Nefopam may be additive to those of other agents with anticholinergic or sympathomimetic activity. Nefopam may cause adverse sympathomimetic effects including tachycardia and aggravation or precipitation of angina. Caution should be exercised in patients with a history of ischaemic heart disease.

4.5 DRUG INTERACTIONS:
The side effects of Nefopam may be additive to those of other agents with anticholinergic or sympathomimetic activity. Nefopam should be used with caution in patients on tricyclic anti-depressants and is contraindicated in patients on MAO inhibitors

4.6 USE IN SPECIAL POPULATIONS (SUCH AS PREGNANT WOMEN, LACTATING WOMEN, PAEDIATRIC PATIENTS, GERIATRIC, PATIENTS ETC.):
Nefopam is not recommended for pregnant women or those likely to become pregnant unless the expected benefit to the mother outweighs any potential risk to the foetus. Nefopam is excreted in human milk. A decision should be made whether to discontinue nursing or discontinue the medication, taking into account the potential for adverse effects for the foetus and the importance of treatment to the mother.

4.7 EFFECTS ON ABILITY TO USE AND DRIVE MACHINES:
Not applicable

4.8 UNDESIRABLE EFFECTS:
More common reactions Nausea, nervousness, dry mouth, light-headedness and urinary retention may occur. Less common reactions Vomiting, blurred vision, drowsiness, sweating, insomnia, headache, confusional state, anaphylactic reactions, coma, hallucinations, tachycardia and aggravation of angina have been reported. Rarely a temporary harmless pink discolouration of the urine has occurred.

4.9 OVERDOSE:
Symptoms and Signs
Nefopam toxicity is manifested by neurological symptoms (coma, convulsions, hallucinations, agitation) and cardiovascular response (tachycardia with hyperdynamic circulation).

Treatment
Supportive treatment is suggested including gastric lavage, forced emesis and diuresis. Oral administration of activated charcoal may help prevent absorption. Convulsions and hallucinations may be controlled (e.g. with diazepam IV or PR). Beta-adrenergic blockers may be of use in controlling the cardiovascular complications

5. PHARMACOLOGIC PROPERTIES:

5.1 MECHANISM OF ACTION:
The clinical studies have shown that nefopam to inhibit the re-uptake of various catecholamines (including noradrenaline, serotonin and dopamine). It is possible that the mechanism of action of nefopam is at least in part by altering the levels of these neuromodulators in the brain and at the spinal level.

5.2 PHARMACODYNAMIC PROPERTIES:
Nefopam is a centrally acting analgesic with a rapid onset of action. The main site of action appears to be in the central nervous system both at the brain and spinal levels. In vitro experiments have shown nefopam to inhibit the re-uptake of various catecholamines (including noradrenaline, serotonin and dopamine). It is possible that the mechanism of action of nefopam is at least in part by altering the levels of these neuromodulators in the brain and at the spinal level.

5.3 PHARMACOKINETIC PROPERTIES:
Nefopam is absorbed from the gastrointestinal tract. Peak plasma concentrations occur 1 to 3 hours after a dose by mouth and up to 1 hour after intramuscular injection. About 73% is bound to plasma proteins. Nefopam is distributed into breast milk. It has an elimination half-life of about 4 hours. It is extensively metabolised and excreted mainly in urine, in which less than 5% of a dose is excreted unchanged. About 8% of a dose is excreted via the faeces.

6. NONCLINICAL PROPERTIES:

6.1 ANIMAL TOXICOLOGY OR PHARMACOLOGY:
Not applicable

7. DESCRIPTION:
NEFOSAR is supplied for oral administration, as a film coated tablet of nefopam hydrochloride. Each film coated tablet of NEFOSAR contains nefopam hydrochloride 30 mg.

8. PHARMACEUTICAL PARTICULARS:

8.1 INCOMPATIBILITIES:
Not applicable

SHELF-LIFE:
Refer Pack

PACKAGING INFORMATION:
Refer Pack

STORAGE CONDITIONS & HANDLING INSTRUCTIONS:
Refer Pack

9. PATIENT COUNSELLING INFORMATION:
Advise the patient to read the Nefopam patient Information leaflet
Inform patients that even at recommended doses of nefopam dry mouth, light-headedness and urinary retention may occur.
Inform patients that even at recommended doses of nefopam Vomiting, blurred vision, drowsiness, sweating, insomnia, headache, confusional state, anaphylactic reactions, hallucinations, coma, tachycardia and aggravation of angina may occur
Advise patients about rare temporary discolouration of urine that may occur with Nefopam

10. DETAILS OF MANUFACTURER:
Refer Pack for manufacturer details.

MARKETED BY:
Abbott India Limited
Angel Space, Lifestyle Bldg. No. D-4,
Gala No. 7 to 10 & 17 to 20 Ground Floor,
107 to 110 & 117 to 120 First Floor,
Pimplas Village, Dist. Thane,
Bhiwandi – 421 302, India

11. DETAILS OF PERMISSION OR LICENCE NUMBER:
Refer Pack for Permission/License details

12. DATE OF REVISION:
Version: 3.0, dated 25th Sep 2023

References:
1) Acuten prescribing information
2) PRAC recommendations dated 9th Feb 2017
3) Acupan prescribing information dated 10th July 2018