Opiates Flashcards
what plant is opium derived from?
poppy flower
Name 3 opiates that are strictly mu receptor agonists
codeine, oxycodone, hydrocodone
name 3 opiates that can activate both mu and kappa receptors
nalbuphine, butorphanol, buprenorphine
Name the phenanthrenes
natural: codeine, morphine, semisynthetic: hydrocodone, hydromorphone, oxycodone, oxymorphone
name the phenylpiperidines
meperidine, fentanyl
name the phenylheptylamines
methadone (+propoxyphene)
are opiates narcotics?
no - don’t refer to opiates as narcotics
if a phenanthrene isn’t effective for a pt, name 2 drugs you could switch to
meperidine, fentanyl
if fentanyl isn’t effective for the pt, name a drug you could switch to
methadone
True or false: opiates are used as backup therapy, first line depends on the type of pain
TRUE - opiates are backup therapy
according to WHO, mild pain can be treated with
non-opiate analgesics with or without adjuvant medications
according to WHO, mild to moderate pain can be treated with
weak opiate + non-opiate analgesic with or without adjuvant meds
according to WHO, moderate to severe pain can be treated with
strong opiates with our without non-opioid analgesic medication with or without adjuvant medications
NRS
numeric rating scale - should be included on scripts
what is the name of the faces scale for pain?
Wong baker faces rating scale
what are examples of nociceptive pain?
tissue injury, joints, MSK, burns, incisions
what are examples of neuropathic pain?
carpal tunnel, DM, CA, shingles
does neuropathic pain respond well to opiates?
no
where do opiates work in the brain?
site of action is the PAG and it blocks GABA. From the PAG it moves to the medulla which mediates NE and serotonin. MOR blocks Ca2+ and opens K+ channels causing hyperpolarization. Also acts at post-synaptic and K1 receptors
MOA of opiates
inhibition of painful stimuli in the substantia gelatinosa of the spinal cord, brainstem, reticular activating system, thalamus, and th elimbic system
effects of opiates
sedation, euphoria, mental clouding, respiratory depression, miosis, decreased peristaltic motility, depression of the cough reflex and orthostatic HOTN
ADR of opiates
increased esophageal reflux, N/v in the CTZ, peripheral vasodilation, increased histamine, prolongs labor, decreased urinary void reflex
which mu receptor is best known?
mu1
where are mu receptors found?
primarily supraspinal than spinal - all over: PAG, superficial dorsal horn, amygdala
what type of pain do mu receptors relieve
somatic pain more than visceral pain
ADR of mu receptor agonists
respiratory depression, euphoria, dependence, decreased GI motility, miosis
where are kappa receptors mostly located?
spinal more than suprespinal
what type of pain is relieved by kappa receptor agonists?
visceral pain
ADR of kappa receptor agonists?
sedation, miosis, dysphoria
primary location of delta receptors
spinal more than supraspinal
ADR of delta agonists
tachycardia, tachypnea, dysphoria, hallucinations, mydriasis, hypertonia
what is the “relative” of oxycodone with a longer T1/2?
oxycontin
what are opiates used for?
pain relief
are opiates susceptible to first pass effect?
yes
how are opiates metabolised?
CYP450/2D6 (genetic variability in metabolism)