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TYPE OF OPIOID DRUGS

NAME OF DRUGS STRONG AGONISTS 1. Morphine 2. Methadone 3. Pethidine 4. Fentanyl USE Analgesia Anaesthesia Severe pain o Acute (cancer pain) o Chronic (post-op, obstetric labour, post-MI) Methadone stable chronic pain (long T) with equal efficacious as morphine Penthidine acute episodes of moderate to severe pain (faster onset, shorter duration of action) Fentanyl for pt who x swallow morphine (transdermal patch) + fast onset after iv Less efficacious than strong agonists 10% converted to morphine (analgesia) Moderate pain Analgesic (sub-lingual tablets) Stop heroin addiction Analgesic ( receptors) Less side effect MODE OF ACTION/MECHANISM receptor agonist most strong agonist o Activate receptors o Release endogenous opioid peptides (can bind other opioid receptor subtypes) Activation of opioid receptors at SC, Cx, BS o Inhibit nerves convey pain o Activate nerves inhibit pain Remove/reduce perception of pain, retain consciousness ADVERSE EFFECTS Euphoria Dysphoria o Restlessness, malaise Respiratory depression o Inhibit BS respiratory mechanism Miosis (opioid overdose) Sedation Nausea & vomiting o Trigger BS chemoreceptor trigger zone Constipation Pruritis

MODERATE AGONISTS Codeine

Lower affinity opioid receptors -

PARTIAL AGONIST Buprenorphine MIXED AGONISTANTAGONIST Nalbuphine OPIOID ANTAGONIST Naloxone OTHER OPIOIDS

Partial agonist (full receptor occupancy, produce smaller response than full agonists) receptor antagonist BUT receptor agonist

Tx of opioid overdose

High affinity for receptor Lower affinity for and receptor

Diarrhea antidiarrheal drugs Cough antitussive drugs