Module 9: Opiates & Opioids Flashcards
opium poppy
Papaver Somniferum
Miosis
Pinpoint pupils (constricted)
Follows 1st-pass metabolism when taken orally
Low oral bioavailability (more potent when taken other ways)
Slow to cross blood-brain barrier
Metabolite of codeine and heroin
Duration of action: 4-5 hours
Morphine
Endogenous Opioid Peptide that bind to mu opioid receptors.
Endorphins
Endogenous Opioid Peptide that bind to delta opioid receptors primarily.
Enkephalins
Endogenous Opioid Peptide that bind to kappa opioid receptors primarily.
Dynorphins
3 types of Opioid receptors
Mu, Kappa, Delta
Peak of Opioid Abstinence Syndrome
36-72 hours
Duration of Opioid Abstinence Syndrome
7-10 days
Beginning of Opioid Abstinence Syndrome
6-8 hours
Category of Opioids including morphine, codeine, hydromorphone, etc.
Phenanthrenes
Category of Opioids including Fentanyl, sufentanil, furanryl fentanyl, etc.
Phenylpiperidines
Opioid Classifications (mode of action)
Agonist, Antagonist, Mixed Agonist/Antagonist
Agonist
Highest oral bioavailability
10-15% metabolized to morphine
Duration of analgesia: 3-4 hours
Codeine
Agonist
2-3 times more potent than morphine (penetrates BBB)
poor oral biovavailbility
rapid metabolism to 6MAM (half life = 2-6 min) then to morphine
Heroin
Agonist Derivative of Codeine
metabolized to hydromorphone and dihydrocodeine
Duration of analgesia: 3-5 hours
Hydrocodone
Agonist
metabolite of hydrocodone and morphine (minor)
More potent than morphine
Duration of analgesia: 4-5 hours
Hydromorphone
Agonist
Derived from thebaine
15% metabolized to oxymorphone
Duration of analgesia: 3-4 hours
Oxycodone
Agonist
Metabolite of Oxycodone
Duration of analgesia: 3-4 hours
Oxymorphone
Agonist
Most potent and fast-acting opioid
50-200x more potent than Morphine
Transdermal patches can give delayed concentrations for 12-24 hrs
Duration of analgesia: 1-15. hours
Fentanyl
Agonist
Long elimination half life
Metabolizes to EDDP and EDMP
Duration of analgesia: 4-6 hours
Methadone
Atypical opioid agonist
Metabolite (o-dm-) is 2x more potent (contributes to toxicity)
Duration of analgesia: 4-6 hours
Tramadol