13. Opioids
Terms
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- Methadone
- Mu agonist, good oral bioavailability, long half-life, used for replacement therapy in heroin users
- Pentazocine
- Weak partial mu agonist, can precipitate withdrawal in an opioid dependent person
- Oxycodone
- Metabolized into oxymorphone
- Dextromethorphan
- Antitussive, NMDA antagonist
- Codeine
- Metabolized into morphine
- Naltrexone
- Opioid antagonist that can be given orally
- Meperidine
- Mu opioid agonist similar to morphine, but better bioavailability, active metabolite may induce tremors or seizures, not used for long term analgesia
- Morphine
- Mu opioid receptor agonist, causes pinpoint pupils on overdose, causes itching and constipation
- Methylnaltrexone
- Opioid antagonist that acts peripherally, does not enter CNS
- Heroin
- Metabolized into morphine, with more rapid entry into CNS than morphine
- Fentanyl
- Potent mu agonist, used as anesthetic adjunct and post-surgical anesthesia, fewer cardio effects
- Buprenorphine
- Partial mu agonist, high first pass metabolism
- Diphenoxylate
- Opioid agonist, strong constipating effect, available only with atropine
- Naloxone
- Opioid antagonist, short half life, poor oral bioavailability, used to reverse opioid overdose
- Propoxyphene
- Less selective mu agonist than morphine, has major metabolite that can contribute to toxicity