Treatment of Pain Flashcards
key selective agonists of mu receptors (5 drugs)
morphine fentanyl methadone meperidine buprenorphine
key selective agonists of delta receptors (endogenous)
enkephalins
key selective agonists of kappa receptors (3 drugs)
butorphanol
pentazocine
nalbuphine
endogenous agonists of mu receptors
endomorphic 1 and 2
enkephalins
beta endorphin
endogenous agonists of kappa receptors
dynorphins
key antagonists of mu receptors (2 drugs)
naloxone (Narcan) makes you breathe again, puts you into withdrawal
naltrexone (Regia) PO, t-rex eats things
key antagonist of delta receptors
naltrindole
strong opioids (MMMFHOHH)
morphine meperidine methadone fentanyl heroin oxycodone hydromorphone hydrocodone
moderate to low opioids
codeine
propoxyphene
mixed agonist/antagonists
pentazocine
butorphanol
nalbuphine
kappa agonist, mu delta antagonists
pentazocine
butorphanol
kappa agonist, mu antagonist
nalbuphine
partial mu agonist
kappa antagonist
used in tx of pregnant addicts
-why is this drug commonly abused by physicians?
buprenorphine
-does not cause miosis
three opioid receptor antagonists
naloxone
naltrexone
nalmefene
opium contains three alkaloids, what are they?
morphine
codeine
papaverine
Opioid tolerance does not develop to three effects
miosis
constipation
respiratory depression
What are the sxs of opiate withdrawal aka rebound phenomenon?
hyperalgesia
hyperventilation
mydriasis, diarrhea, dysphoria
contraindications to opioid use
hepatic insufficiency
respiratory insufficiency
head injury
hydrogenated ketone of morphine
7x more potent than oral morphine
less active metabolites than morphine
hydromorphone
as potent as morphine causes constipation and biliary spasms long half life used in opiate withdrawal odd overdose propensity in Appalachia
methadone
recreational metabolized to 6-monoacetylmorphine then morphine higher BBB penetrance than morphine -name the drug -what metabolite is found in urine?
heroin
6-monoacetylmorphine
orally equipotent to morphine
extended release formula problem for abuse
hydrocodone
semi synthetic analog of morphine
delayed release formula, bad for abuse
oxycodone, oxycontin
synthetic derivative of morphine
excitement caused at toxic doses due to its metabolite, which is not blocked by naloxone
similar side effects to morphine, but less constipation and urinary retention
MAO inhibitors can cause a severe reaction: excitation, delirium, hyperpyrexia, convulsions, and respiratory depression
-name the drug and it’s hyperactive metabolite
meperidine, normeperidine
meperidine analog
available as a lozenge
fentanyl
meperidine analog
6000x a potent as morphine
less respiratory depression, chest wall rigidity
sufentanil
low potency analgesic metabolized by CYP2D6 -name the drug and highlight its effects on: -slow metabolizers -fast metabolizers
codeine
- no analgesia
- OD due to rapid conversion to morphine
kappa agonist, mu antagonist
may block morphine analgesia
may precipitate withdrawal in patients on opioids
co-ad with which antihistamine to avoid excessive euphoria?
pentazocine (Talwin with Naloxone)
tripelennamine
partial mu agonist, kappa antagonist
im/iv
given sublingual for opioid dependence
buprenorphine
chemically unrelated to opiates weak opioid agonist inhibits NE and 5-HT reuptake partially inhibited by naloxone used for chronic pain
tramadol
suppresses cough
no analgesia
less constipation than codeine
not antagonized by naloxone
dextromethorphan (Delsym, Tussin)
antidiarrheals
mediated by mu receptors in myenteric nerve plexus
diphenoxylate (Lomotil)
loperamide (Imodium)
alpha 2 adrenergic agonist
mimics effects of NE at pre and post synaptic neurons in dorsal horn
used in neuropathy and cancer pain
clonidine
antidepressants (3)
NE and 5HT reuptake inhibitors
may also alter perception of pain
used for neuropathy
TCA-amitriptyline
SNRI- venlafaxine, duloxetine
anti epileptics (2) reduce activation of N and P/Q Ca channels used in neuropathy, post herpetic neuralgia, and diabetic neuropathy
gabapentin and pregabalin
anti epileptic
stabilizes inactive voltage gated na channels
carbamazepine
blocks NMDA and glutamate signaling
Ketamine
