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Opioid Mechanism of Action
19, Jun, 2025

What is an Opioid?

Opioids are a class of drugs that act on the nervous system to relieve pain. They include natural, semi-synthetic, and synthetic substances derived from or modeled after the opium poppy. While highly effective, opioids carry a risk of tolerance, dependence, and addiction.

🧪 Types of Opioids

Type Examples Source
Natural opioids Morphine, Codeine Extracted from opium
Semi-synthetic Oxycodone, Hydrocodone, Heroin Modified from natural opioids
Synthetic Fentanyl, Methadone, Tramadol Fully synthetic
Endogenous Endorphins, Enkephalins Produced naturally in the body

🧠 How Do Opioids Work?

Opioids bind to specific receptors in the brain, spinal cord, and other organs, mainly the μ (Mu) receptors, to block pain signals and alter pain perception.

🔑 Key Receptors

  • μ (Mu): Main receptor for pain relief, euphoria, respiratory depression.
  • κ (Kappa): Less euphoria, spinal pain relief.
  • δ (Delta): Mood regulation and pain modulation.

⚙️ Mechanism Summary

  1. Opioid binds to μ-receptor.
  2. Inhibits calcium influx & opens potassium channels.
  3. Prevents neurotransmitter (like substance P, glutamate) release.
  4. Reduces pain signal to the brain.
  5. Brain perceives less pain.

💊 Therapeutic Effects

  • Severe pain relief (cancer, trauma, surgery)
  • Cough suppression (e.g., codeine)
  • Treatment of diarrhea (e.g., loperamide)
  • Palliative care and anesthesia

⚠️ Side Effects

  • Drowsiness, sedation
  • Constipation
  • Nausea and vomiting
  • Respiratory depression
  • Itching, pinpoint pupils (miosis)
Risks: Long-term use can lead to tolerance, physical dependence, addiction (opioid use disorder), and overdose.

🧬 Endogenous Opioids

Your body produces natural opioids such as endorphins during stress, exercise, and emotional activities. They bind to the same receptors to regulate pain, mood, and stress.

🔄 Tolerance and Withdrawal

  • Tolerance: Higher dose needed over time to get same effect.
  • Withdrawal symptoms: Anxiety, sweating, cramps, nausea, goosebumps.

🧠 Visual Summary

[ Opioid Drug ]
↓
[ Binds to μ-Receptor ]
↓
[ Blocks Calcium Influx ]
↓
[ Prevents Neurotransmitter Release ]
↓
[ Reduces Pain Signal Transmission ]
↓
[ Brain Perceives Less Pain ]
Note: Opioid overdose can be reversed using naloxone, which blocks opioid receptors.

✅ Safe Use Guidelines

  • Use the lowest effective dose for the shortest period.
  • Combine with non-opioid painkillers if possible.
  • Avoid alcohol and sedatives.
  • Monitor for signs of misuse or side effects.
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