Treatment of Pain

Question 1

key selective agonists of mu receptors (5 drugs)

Answer 1

morphine
fentanyl
methadone
meperidine
buprenorphine

Question 2

key selective agonists of delta receptors (endogenous)

Answer 2

enkephalins

Question 3

key selective agonists of kappa receptors (3 drugs)

Answer 3

butorphanol
pentazocine
nalbuphine

Question 4

endogenous agonists of mu receptors

Answer 4

endomorphic 1 and 2
enkephalins
beta endorphin

Question 5

endogenous agonists of kappa receptors

Answer 5

dynorphins

Question 6

key antagonists of mu receptors (2 drugs)

Answer 6

naloxone (Narcan) makes you breathe again, puts you into withdrawal
naltrexone (Regia) PO, t-rex eats things

Question 7

key antagonist of delta receptors

Answer 7

naltrindole

Question 8

strong opioids (MMMFHOHH)

Answer 8

morphine
meperidine
methadone
fentanyl
heroin
oxycodone
hydromorphone
hydrocodone

Question 9

moderate to low opioids

Answer 9

codeine

propoxyphene

Question 10

mixed agonist/antagonists

Answer 10

pentazocine
butorphanol
nalbuphine

Question 11

kappa agonist, mu delta antagonists

Answer 11

pentazocine

butorphanol

Question 12

kappa agonist, mu antagonist

Answer 12

nalbuphine

Question 13

partial mu agonist
kappa antagonist
used in tx of pregnant addicts
-why is this drug commonly abused by physicians?

Answer 13

buprenorphine

-does not cause miosis

Question 14

three opioid receptor antagonists

Answer 14

naloxone
naltrexone
nalmefene

Question 15

opium contains three alkaloids, what are they?

Answer 15

morphine
codeine
papaverine

Question 16

Opioid tolerance does not develop to three effects

Answer 16

miosis
constipation
respiratory depression

Question 17

What are the sxs of opiate withdrawal aka rebound phenomenon?

Answer 17

hyperalgesia
hyperventilation
mydriasis, diarrhea, dysphoria

Question 18

contraindications to opioid use

Answer 18

hepatic insufficiency
respiratory insufficiency
head injury

Question 19

hydrogenated ketone of morphine
7x more potent than oral morphine
less active metabolites than morphine

Answer 19

hydromorphone

Question 20

as potent as morphine
causes constipation and biliary spasms
long half life
used in opiate withdrawal
odd overdose propensity in Appalachia

Answer 20

methadone

Question 21

recreational
metabolized to 6-monoacetylmorphine then morphine
higher BBB penetrance than morphine
-name the drug
-what metabolite is found in urine?

Answer 21

heroin

6-monoacetylmorphine

Question 22

orally equipotent to morphine

extended release formula problem for abuse

Answer 22

hydrocodone

Question 23

semi synthetic analog of morphine

delayed release formula, bad for abuse

Answer 23

oxycodone, oxycontin

Question 24

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

Answer 24

meperidine, normeperidine

Question 25

meperidine analog | available as a lozenge

Answer 25

fentanyl

Question 26

meperidine analog 6000x a potent as morphine less respiratory depression, chest wall rigidity

Answer 26

sufentanil

Question 27

``` low potency analgesic metabolized by CYP2D6 -name the drug and highlight its effects on: -slow metabolizers -fast metabolizers ```

Answer 27

codeine - no analgesia - OD due to rapid conversion to morphine

Question 28

kappa agonist, mu antagonist may block morphine analgesia may precipitate withdrawal in patients on opioids co-ad with which antihistamine to avoid excessive euphoria?

Answer 28

pentazocine (Talwin with Naloxone) | tripelennamine

Question 29

partial mu agonist, kappa antagonist im/iv given sublingual for opioid dependence

Answer 29

buprenorphine

Question 30

``` chemically unrelated to opiates weak opioid agonist inhibits NE and 5-HT reuptake partially inhibited by naloxone used for chronic pain ```

Answer 30

tramadol

Question 31

suppresses cough no analgesia less constipation than codeine not antagonized by naloxone

Answer 31

dextromethorphan (Delsym, Tussin)

Question 32

antidiarrheals | mediated by mu receptors in myenteric nerve plexus

Answer 32

diphenoxylate (Lomotil) | loperamide (Imodium)

Question 33

alpha 2 adrenergic agonist mimics effects of NE at pre and post synaptic neurons in dorsal horn used in neuropathy and cancer pain

Answer 33

clonidine

Question 34

antidepressants (3) NE and 5HT reuptake inhibitors may also alter perception of pain used for neuropathy

Answer 34

TCA-amitriptyline | SNRI- venlafaxine, duloxetine

Question 35

``` anti epileptics (2) reduce activation of N and P/Q Ca channels used in neuropathy, post herpetic neuralgia, and diabetic neuropathy ```

Answer 35

gabapentin and pregabalin

Question 36

anti epileptic | stabilizes inactive voltage gated na channels

Answer 36

carbamazepine

Question 37

blocks NMDA and glutamate signaling

Answer 37

Ketamine