Opioids Flashcards
(17 cards)
Morphine
- Mu agonist. Activated by metabolism.
- Stimulation causes a decrease in release of cAMP. Disinhibition of efferents from PAG results in increased modulation of medullary 5HT and NE outputs.
- Supraspinal and spinal analgesia, sedation, inhibition of respiration, slowed GI transit, modulation of hormone release, miosis, euphoria.
Fentanyl
-Mu agonist, 100x as potent as morphine.
Methadone
- Mu agonist.
- Used in treatment of opioid abuse and chronic pain.
Meperidine
- Mu agonist. Forms toxic metabolite that can accumulate with frequent use.
- Lesser duration of analgesia.
Heroin
- Mu agonist. Activated by metabolism.
- Much more lipophilic than morphine (means more abuse potential).
Codeine
- Mu agonist.
- Not so great at alleviating pain. Much better antitussive.
Oxycodone
- Mu agonist.
- Moderate to severe pain.
Hydrocodone
- Opioid agonist.
- Moderate to severe pain, antitussive.
Hydromorphone
-Opioid agonist. 2-3 X as potent as morphine.
3 endogenous opioids:
- B-endorphin (Mu)
- Dynorphin (Kappa)
- Enkephalin (Delta)
Nalbuphine
- Mu antagonist and kappa agonist.
- Stimulation results in supraspinal and spinal analgesia, psychotomimemtic effects, slowed GI transit.
- Can precipitate withdrawal in opioid-dependent patients since you’re not getting the full morphine effect.
Buprenorphine
- Partial Mu agonist.
- A component of Suboxone (used to treat opioid dependency).
Naloxone
- Mu antagonist, used to treat opioid overdose.
- Component of Suboxone.
Naltrexone
-Mu antagonist, used to treat both opioid addiction and alcoholism.
Dextromethorphan
Only an antitussive.
Tramadol
- Weak Mu agonist. Also blocks NE and 5HT uptake.
- Used to treat mild to moderate pain.
Suboxone
- Buprenorphine + Naloxone.
- Used to treat opioid dependency.