This is a brief summary of medicines that target the opioid receptors.
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ADDITIONAL TAGS
Opioids
Drug
Mechanism of action
Indication
Notes
Heroin
Strong μ agonist
Manage pain, suppress cough, antimotility for diarrhea
Contraindication: phenothiazine, MAO inhibitors, and tricyclic antidepressants (depressant effects); alcohol and benzodiazepine (respiratory effects); hepatic metabolism
Often abused IV; not legal in US;
Morphine
Strong μ agonist
Prototypical opioid; various routes of admin
Fentanyl
Strong μ agonist
Rapid onset and offset with small doses; CV stability; 100x more potent than morphine
Methadone
Strong μ agonist
Also used for opioid/heroin withdrawal; racemic mixture of NMDA antagonist and mu agonist
Meperidine
Strong μ agonist
No biliary SE, doesn't constrict sphincter of Oddi; seizures
Codeine
Moderate μ agonist
Less potent morphine
Hydrocodone
Moderate μ agonist
Most prescribed opiate; often combined with NSAIDs/acetaminophen
Oxycodone
Moderate μ agonist
Similar to hydrocodone
Tramadol
Weak μ agonist
Synthetic codeine; lower addiction risk; can cause seizures and serotonin syndrome
Buprenorphine
μ agonist; κ antagonist
Analgesic; deterrent, detoxification
High affinity, low efficacy at mu receptor → partial agonist
Nalbuphine
κ agonist; μ antagonist
Treats opioid-induced pruritus
Originally hoped to be less addictive, less side effects than other opioids → no
Naloxone
μ antagonist (short acting)
Treat opioid addiction, overdose, and toxicity; reverses mu agonist effects; increases respiratory rate within 1-2 min
Better for opioid overdose; half-life is 1 hour
Naltrexone
μ antagonist (long acting)
Treats alcoholism; lasts 24 hours after moderate dose
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