Opioids Flashcards
High efficacy agonist- prototype against which all others are compared
Morphine
High efficacy agonist- much less potent than morphine but faster acting.
Meperidine (demerol)
High efficacy agonist- Used to treat Heroin addicts. Has a long T1/2 and good bioavailability.
Methadone (Dolophine)
High efficacy agonist- prodrug that is rapidly converted to morphine. Metabolites are the active agents. Not legal in US (schedule 1 drug)
Heroin
High efficacy agonist- more lipophilic than morphine and 75-100X more potent. Short acting and can be given via many routes (lollipop, transdermal patch, orally, buccally, sublingual and nasal spray.
Fentanyl
Medium efficacy agonist- good anti-tussive
Codeine
Medium efficacy agonist- highest efficacy in this category.
Oxycodone (Percocet, percodan, Combunox) OxyContin (slow release preparation)
Mixed agonist/antagonist/other- Only give this orally due to severe injection site necrosis and sepsis when given IV.
Pentazocine (schedule IV)
Mixed agonist/antagonist/other- risk of seizures, avoid taking with MAOI’s (serotonin syndrome)
Tramadol (Ultram, UltramER)
Mixed agonist/antagonist/other- analgesic effects due to mu partial agonism, also kappa antagonist. SL route preferred. Widely used to treat opioid dependence.
Buprenorphine
Antagonist- competitive antagonist at ALL opioid receptors (but not at non-opioid receptors like DM). IV only. Use for treatment of opioid overdose. Short duration of 1 hr.
Naloxone (Narcan)
Non-analgesic opioids- Anti-tussive that is not active at opioid receptors but is at DM receptors.
Dextromethorphan
Non-analgesic opioids- Anti-diarrheal, little BBB penetration. Active ingredient in Imodium-AD
Loperamide
Derived from opium
Opiate
Compound with similar pharmacology to morphine
Opioid
Pain relieving
Analgesic
Sleep inducing
Narcotic
Endogenous opioid ligand released from pituitary as a hormone and also present as a neurotransmitter
Beta endorphins