Efopam

• Acute Moderate to Severe Pain:
  Approved for the management of moderate to severe acute pain, including postoperative pain, musculoskeletal pain, and traumatic injuries.
• Adjunct in Multimodal Analgesia:
  Used as part of combination therapy to reduce opioid consumption and improve pain control.
• Off-label Uses:
  Occasionally used in certain chronic neuropathic pain conditions and for preventing postoperative pain sensitization, though evidence is limited.

• Adults:
• Oral: 30 mg every 8 hours (total daily dose up to 90 mg).
• Intravenous or intramuscular: 20 to 30 mg every 4 to 6 hours as needed, not exceeding 120 mg per day.
• Elderly:
  Start with lower doses; monitor for increased sensitivity to side effects.
• Pediatrics:
  Safety and efficacy not established; use only if benefits outweigh risks.
• Renal Impairment:
  Use with caution; no formal dose adjustment guidelines. Monitor for toxicity.
• Hepatic Impairment:
  Use cautiously; consider dose reduction in moderate to severe impairment.
• Administration Route: Oral, IV, or IM as per clinical scenario.
• Duration: Short-term use recommended, aligned with acute pain management needs.

Nefopam Hydrochloride acts centrally as a non-opioid analgesic. It inhibits the reuptake of serotonin, norepinephrine, and dopamine in the central nervous system, enhancing descending inhibitory pain pathways. Additionally, it exhibits mild anticholinergic and NMDA receptor antagonist effects, contributing to its analgesic action without engaging opioid receptors, thereby minimizing opioid-related side effects.

• Absorption: Rapid and efficient; peak plasma levels within 30 to 60 minutes post oral administration.
• Bioavailability: Approximately 30%, reduced by first-pass hepatic metabolism.
• Distribution: Crosses blood-brain barrier; widely distributed in tissues.
• Metabolism: Extensively metabolized in the liver by conjugation and oxidation.
• Elimination: Primarily via urine as metabolites.
• Half-life: Approximately 3 to 8 hours.
• Onset of Action: Within 15 to 30 minutes after administration.

• Pregnancy:
  Limited human data; animal studies show no direct teratogenicity. Use only if potential benefits justify risks.
• Lactation:
  Unknown if excreted in human milk; exercise caution when administered to nursing mothers.

• Primary Class: Analgesic
• Subclass: Non-opioid, centrally acting analgesic

• Hypersensitivity to nefopam or any component of the formulation.
• History of convulsions or epilepsy.
• Concurrent or recent (within 14 days) use of monoamine oxidase inhibitors (MAOIs).
• Severe hepatic or renal impairment.
• Narrow-angle glaucoma.
• Urinary retention.
• Known arrhythmias or ischemic heart disease (use cautiously).

• Seizure Risk: Increased risk; contraindicated in epileptic patients.
• Central Nervous System Effects: May cause dizziness, sedation, confusion; caution in activities requiring alertness.
• Cardiovascular Effects: Monitor for tachycardia and palpitations.
• Anticholinergic Effects: Dry mouth, blurred vision, urinary retention; especially in elderly.
• Serotonin Syndrome: Potential risk when combined with serotonergic drugs.
• Monitoring: Regular clinical assessment recommended during therapy.

• Common: Nausea, vomiting, dizziness, dry mouth, sweating, headache.
• Less Common: Confusion, hallucinations, tachycardia, palpitations, urinary retention, blurred vision.
• Serious (Rare): Seizures, severe hypotension, anaphylaxis, serotonin syndrome.
• Onset: Side effects may occur soon after initiation or dose increase; dose-related.

• Contraindicated: Monoamine oxidase inhibitors (MAOIs).
• Increased Risk: Serotonergic agents (SSRIs, SNRIs, triptans) — risk of serotonin syndrome.
• Additive CNS Depression: Alcohol and other CNS depressants.
• Additive Anticholinergic Effects: Other anticholinergic drugs.
• Seizure Threshold: Drugs lowering seizure threshold increase risk.
• Metabolism: No major CYP450 interactions documented.

• Nefopam remains recommended as an effective non-opioid analgesic in multimodal pain management.
• Warnings emphasizing seizure risk and serotonin syndrome have been reinforced.
• Use in elderly and patients with neurological conditions is advised with caution.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light; keep in original tightly closed container.
• Do not freeze.
• Keep out of reach of children.
• Injectable forms: Follow manufacturer’s instructions; usually no refrigeration required.