Mechanism of Action:

Tapentadol works through dual mechanisms:

1. Mu-opioid receptor agonism – provides opioid-type pain relief.

2. Norepinephrine reuptake inhibition (NRI) – enhances pain inhibition by increasing norepinephrine levels.

This dual action makes Tapentadol effective for neuropathic as well as nociceptive pain.

Indications:

• Moderate to severe acute pain (e.g., post-surgical)

• Chronic musculoskeletal pain (e.g., low back pain, osteoarthritis)

• Pain associated with diabetic peripheral neuropathy (extended-release version)

Dosage & Administration:

• Initial dose: Typically 50–100mg every 4 to 6 hours as needed

• Maximum daily dose: Should not exceed 600mg for immediate-release

• Dosing must be tailored individually, especially in opioid-tolerant patients

Side Effects:

Common:

• Nausea, vomiting

• Dizziness, drowsiness

• Constipation

• Headache

Serious:

• Respiratory depression

• Seizures

• Serotonin syndrome (when combined with other serotonergic drugs)

• Risk of dependence, abuse, and addiction

Contraindications:

• Severe respiratory depression

• Acute or severe bronchial asthma

• Paralytic ileus

• Use with monoamine oxidase inhibitors (MAOIs) (within 14 days)

Warnings:

• CNS depression when used with alcohol, benzodiazepines, or other sedatives

• Potential for misuse and addiction

• Use with caution in patients with a history of seizures or head injury

Pregnancy Category: C (risk cannot be ruled out)

Controlled Substance: Schedule II (USA)

Would you like a patient-friendly version or a comparison with other opioids (e.g., Tramadol or Morphine)?