Nefopam

Nefopam is a Analgesics belonging to non-opioid or non-narcotic painkiller.

Nefopam is used in the treatment of Acute pain and Chronic pain.

Nefopam is Absorbed from the gastrointestinal tract. Bioavailability: 40% (oral). and enters breast milk. Plasma protein binding: Approx 73%. It is Extensively metabolised in the liver to form desmethylnefopam, nefopam N-oxide, and N-glucuronide and get excreted Mainly via urine (87%, <5% as unchanged drug); faeces (approx 8%).

The Tmax of Nefopam was found to be about approximately 1-2 hours.

Nefopam shows common side effects like Dizziness, drowsiness, headache, paraesthesia, tremor, convulsion, lightheadedness.

Nefopam is available in Tablet and injection

Nefopam is available in India, Germany, Canada, France, USA

Nefopam (nefopam hydrochloride) is a potent, rapidly-acting non-narcotic analgesic. It is totally distinct from other centrally-acting analgesics such as morphine, codeine, pentazocine and propoxyphene. Unlike the narcotic agents, nefopam (nefopam hydrochloride) has been shown not to cause respiratory depression. It is indicated for the relief of acute and chronic pain, including post-operative pain, dental pain, musculo-skeletal pain, acute traumatic pain and cancer pain. Its mechanism of action is unclear.

Nefopam is available in the form of Tablet and injection.

Nefopam is used in the treatment of Acute and Chronic pain.

Nefopam is a potent, centrally-acting, non-opioid analgesic with anticholinergic and sympathomimetic actions. Its exact mechanism is unclear; however, in vitro studies suggest that it inhibits the reuptake of norepinephrine, serotonin and dopamine.

Nefopam is approved for use in the following clinical indications

Acute Pain and Chronic Pain.

• Intramuscular

Acute pain, Postoperative pain

Adult: Usual dose: 20 mg, repeated 6 hourly if needed. Max: 120 mg daily. Patient must lie down during and for 15-20 minutes after administration.

• Intravenous

Acute pain, Postoperative pain

Adult: Usual dose: 20 mg via slow IV bolus infusion over at least 15 minutes, repeated 4 hourly if needed. Max: 120 mg daily. Patient must lie down during and for 15-20 minutes after administration.

• Oral

Moderate acute pain, Moderate chronic pain

Adult: For the relief of pain including postoperative, dental, musculoskeletal, acute traumatic and cancer pain: Initially, 60 mg tid. Usual dose: 30-90 mg tid, adjusted according to patient response.

Child: ≥12 years Same as adult dose.

Elderly: Initially, 30 mg tid.

Nefopam is available in the dosage strength of 30 mg, 20 mg/2ml.

Nefopam is available in the form of Tablet and injection

Take after eating and with a full glass of water to decrease gastric upset.

Nefopam is contraindicated in patients with:

History of convulsive disorders. IM/IV: Urinary retention linked to urinary or prostate disorders, angle-closure glaucoma. Oral: Concomitant use with MAOIs.

• Common Adverse effects:

Dizziness, drowsiness, headache, paraesthesia, tremor, convulsion, lightheadedness.

• Less Common Adverse effects:

Vomiting, blurred vision, drowsiness, sweating, insomnia, headache, confusion, seeing, feeling or hearing things that are not there, rapid heartbeat and worsening of chest pain.

• Rare Adverse effects

Temporary harmless pink discolouration of the urine may occur.

The common side effects of Nefopam include the following :

Dizziness, drowsiness, headache, paresthesia, tremor, convulsion, lightheadedness.

Symptoms: Tachycardia with hyperdynamic circulation; agitation, hallucinations, convulsions, and coma.

Management: Supportive and symptomatic treatment. Perform gastric lavage, or induce vomiting or diuresis. May administer activated charcoal to prevent absorption. May give diazepam for convulsions and hallucinations, and β-adrenergic blockers for CV complications.

• Pharmacodynamic

Nefopam (nefopam hydrochloride) is a potent, rapidly-acting non-narcotic analgesic. It is totally distinct from other centrally-acting analgesics such as morphine, codeine, pentazocine and propoxyphene. Unlike the narcotic agents, nefopam (nefopam hydrochloride) has been shown not to cause respiratory depression. It is indicated for the relief of acute and chronic pain, including post-operative pain, dental pain, musculo-skeletal pain, acute traumatic pain and cancer pain. Its mechanism of action is unclear.

• Pharmacokinetics

Absorption: Absorbed from the gastrointestinal tract. Bioavailability: 40% (oral). Time to peak plasma concentration: Approx 1-3 hours (oral); 0.5-1 hour (IM).

Distribution: Enters breast milk. Plasma protein binding: Approx 73%.

Metabolism: Extensively metabolised in the liver to form desmethylnefopam, nefopam N-oxide, and N-glucuronide.

Excretion: Mainly via urine (87%, <5% as unchanged drug); faeces (approx 8%). Elimination half-life: Approx 4 hours.

• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364710/
• https://reference.medscape.com/drug/colestid-Nefopam -342452
• https://go.drugbank.com/drugs/DB00375
• https://www.sciencedirect.com/topics/medicine-and-dentistry/Nefopam
• https://europepmc.org/article/med/6988203