Opioids Flashcards
Codeine
Mu agonist
Converted to Morphine by demethylation (CYP2D6)
Fentanyl
Mu agonist Patch- Severe chronic pain Oral, IV, Epidural (labor pain), Intrathecal/subarachnoid Rapid onset Very potent Can be used for surgical sedation 3rd line drug
Hydrocodone
Mu receptor agonist
Metabolized to Hydromorphone by CYP2D6
Acts with other drugs like Acetaminophen, doesn’t have much effect on its own
Heroin
Mu agonist
Converted to Morphine
Has a very rapid effect!
Hydromorphone
Mu receptor agonist
Faster onset
5X more potent than morphine
Meperidine
Mu agonist More lipid soluble than morphine Faster onset Less potent Serotonin reuptake inhibitor Can cause Serotonin Syndrome
Morphine
Benchmark opioid drug
Mu receptor agonist
Low lipid solubility- slow action on the brain
Lasts for 4 hours
Not affected by liver disease, but greatly affected by renal insufficiency (prolonged and severe effect)
Chronic pain- intrathecal spinal
Acute pain- intrathecal or epidural
Methadone
Mu agonist
Oral
Long half life (15-60 hrs)
Used for opioid drug addiction (license needed)
Used for pain management (no license needed)
Decreased euphoria
Oxycodone
Mu receptor agonist
Metabolized to Oxymorphone by CYP2D6
Can act alone
Oxymorphone
Mu receptor agonist
Major metabolite of Oxycodone
Buprenorphine
Partial Mu agonist Kappa agonist High Mu affinity Treats drug abuse and addiction 7-day patch
Nalbuphine
Kappa agonist
Mu partial agonist/antagonist
Pentazocine
Kappa agonist
Mu partial agonist/antagonist
Tramadol
Partial Mu agonist
Metabolized by CYP2D6 (makes active metabolite) and CYP3A4
Tapentadol
Partial Mu agonist
Metabolized by CYP2C9, CYP2C19, and CYP2D6
