Opioids Flashcards
3 types of endogenous opioid peptides
enkephalins
beta-endorphins
dynorphins
opioids receptors
mu
delta
kappa
non-opioid like (NOP)
mu receptor endogenous ligand
beta-endorphin
enkephalin
delta receptor endogenous ligand
enkephalin
kappa receptor endogenous ligand
dynorphin
CYP2D6
potent - codeine to morphine
potent - tramadol to metabolite
hydrocodone and oxycodone variants
CYP3A4
fentanyl, buprenorphine, and methadone metabolism
CYP3B6
methadone and propofol
women have higher activity
mu receptor effect
analgesia euphoria sedation physical dependence respiratory depression miosis constipation urinary retention bradycardia pruitis skeletal muscle rigidity biliary spasm
kappa receptor effect
analgesia dysphoria sedation low abuse potential mitosis antishivering
delta receptor effects
analgesia physical dependence respiratory depression constipation urinary retention
opioid histamine release
codeine
morphine
meperidine
phenanthrene alkaloids
natural occurring: morphine, codeine, thebaine
semisynthetic: heroin, vicodan, dalaudid, oxycontin, oxymorphone, and antagonists (narcan etc.)
synthetic: levorphanol, butorphanol, nalbuphine, pentazocaine
piperidine derivatives
phenylpiperidines: meperidine, loperamide
anilidopiperidines: fentanyl, sufentanil, alfentanil, remifentanil
diphenylheptanes
methadone
opioid potency ratios are estimates relative to ______
morphine
metabolism - remifentanil
non-specific esterase’s
opioids effect on CTZ versus vomiting center
stimulate CTZ - short term effect
inhibit vomiting center - long term effect
incidence on muscle rigidity with opioids and treatment
dose, speed or administration, use of nitrous oxide, older age, absence of muscle relaxants
treatment: muscle relaxants and airway control
opioids - ocular effects
mitosis - excitatory parasympathetic
fentanyl decrease intraocular pressure
opioids that inhibits shivering
meperidine
treatment for increased biliary pressure
atropine, glycopyrrolate
nitroglycerin
glucagon
narcan
what drug is contraindicated in children after tonsillectomy or adenoidectomy
codeine
also contraindicated in all children under 12 and breastfeeding mothers
demerol metabolism and contraindications
metabolized to normeperidine which is toxic
contraindicated in elderly, renal failure, and with concurrent use of MAO inhibitors
serotonin syndrome
signs: mental status changes, autonomic instability, neuromuscular hyperactivity, hyperthermia
drugs: MAO inhibitors, SSRIs, SNRIs, tricyclic antidepressants, linezolid (antibiotic), meperidine, fentanyl, tramadol, pentazocine, dextromethorphan, reglan, sofrían, herbal products, lithium, tryptophan, and many more…
stop the offending agent, may need paralysis and sedation
