Opioids

Question 1

2 opioids used for diarrhea

Answer 1

1) loperamide
2) diphenyoxylate

lack analgesic effects at usual doses

Question 2

coanalgesic for neuropathic pain

Answer 2

imipramine

Question 3

meperidine AE

Answer 3

large doses given in short intervals - seizures, mydriasis

meperidine = short t 1/2 BUT its metabolite = normeperidine has a t 1/2 of 15-20 hours

Question 4

fentanyl is metabolized by

Answer 4

CYP3A4

Question 5

which opioids are metabolized by CYP2D6

Answer 5

codeine (used CYP2D6 to convert to morphine)
oxycodone
hydrocodone

Question 6

combination of which two opioid types can cause withdrawal sxs

Answer 6

pure agonist + weak partial agonist - risk of diminishing analgesia OR inducing withdrawal

Question 7

what is meperidine contraindicated with

Answer 7

MAOI, serotinergic agents

- meperidine can block reuptake of serotonin

Question 8

what is tramadol contraindicated with

Answer 8

MAOI
epileptic patients: inc risk of seizures in pt with seizure disorders and those taking medications that lower seizure threshold

Question 9

what are opioids contraindicated with

Answer 9

1) sedatives

2) anti psychotics

Question 10

what clinical conditions are opioids contraindicated with

Answer 10

impaired: pulmonary, renal, liver, adrenal function

pregnancy

head injuries

Question 11

opioids for severe pain

Answer 11

1) morphine
2) heroine
3) oxycodone hydrocodone

Question 12

methadone AE

Answer 12

QT prolong - torsades

death

Question 13

tramadol contraindications

Answer 13

serotinergic drugs –> serotonin syndrome

Question 14

tramadol use

Answer 14

neuropathic pain

Question 15

tramadol MOA

Answer 15

weak mu agonist AND NE/serotonin reuptake inhib

Question 16

methadone MOA

Answer 16

strong mu agonist, NMDA antagonist, serotonin/NE reuptake inhibitor

Question 17

pentazocine

Answer 17

mixed agonist and antagonist opioid

kappa agonist, mu antagonist/partial agonist

Question 18

butorphanol

Answer 18

mixed agonist and antagonist opioid

kappa agonist, mu antagonist/partial agonist

Question 19

nalbuphine

Answer 19

mixed agonist and antagonist opioid

kappa agonist, mu antagonist/partial agonist

Question 20

buprenorphine

Answer 20

mixed agonist and antagonist opioid

partial mu agonist, kappa antagonist

Question 21

ceiling effect in which drugs

Answer 21

1) pentazocine
2) butorphanol
3) nalbuphine
4) buprenorphine

Question 22

mixed agonist and antagonist opioids AE

Answer 22

all cause psychomimetic effects except: buprenorphine

Question 23

mixed agonist and antagonist opioids use

Answer 23

to reduce addiction potential of opioids

• potent in opioid naive pt
• can precipitate withdrawal in pt who are already physically dependent

Question 24

buprenorphine use

Answer 24

management of opioid addiction
psychomimetic effect is uncommon
partial mu agonist and kappa antagonist

Question 25

naloxone

Answer 25

used in tx of opioid OD | opioid antagonist at mu, delta, kappa receptors

Question 26

naltrexone

Answer 26

used for opioid addiction -- dec alcohol craving | opioid antagonist at mu, delta, kappa receptors

Question 27

antitussives (2)

Answer 27

dextrometorphan | codeine

Question 28

which receptors to antimotility opioids work at

Answer 28

mu and delta receptors on enteric nerves, epithelial cells, and muscle

Question 29

topical and blocks VG sodium channels

Answer 29

lidocaine

Question 30

loperamide and diphenoxylate act on which receptors

Answer 30

mu and delta on enteric nerves, epithelial cells, muscle

Question 31

which drug decreases craving for alcohol in chronic alcoholics?

Answer 31

naltrexone

Question 32

which drug is preferred for managing opioid withdrawal?

Answer 32

methadone

Question 33

what makes methadone a good drug for managing opioid withdrawal

Answer 33

long t 1/2 = abstinence syndrome is prolonged BUT less severe less profound sedation euphoria

Question 34

methadone vs morphine

Answer 34

equal in potency | less euphoria, longer duration

Question 35

fentanyl MOA

Answer 35

mu agonist rapid onset/short duration 100x more potent than morphine

Question 36

meperidine MOA

Answer 36

mu receptor agonist | not recommended b/c of metabolite toxicity

Question 37

heroin MOA

Answer 37

hydrolyzes to 6-MAM --> then to morphine

Question 38

heroin vs morphine

Answer 38

heroin and its metabolite (6-MAM) more liposoluble than morphine = enter brain more readily

Question 39

morphine MOA

Answer 39

strong agonist of mu, delta, kappa high affinity at mu low affinity at delta and kappa

Question 40

which drugs are hydrolyzed by tissue esterases

Answer 40

heroin | remifentanil

Question 41

opioid metabolism

Answer 41

convert to glucuoronides = excretd by kidneys

Question 42

morphine conjugated

Answer 42

morphine-3-glucoronide = neuroexcitatory | also conjugates to M6G = more potent than morphine

Question 43

ingestion of toxic doses of mu agonists presents with

Answer 43

pinpoint pupils - d/t PS excitation

Question 44

where are mu receptors located

Answer 44

peripheral terminals of sensory neurons

Question 45

opioids MOA

Answer 45

close VG Ca2+ channels of PRESYNAPTIC NT and open K+ on POSTSYNAPTIC neurons

Question 46

receptors associated with supraspinal analgesia

Answer 46

mu, kappa, delta

Question 47

receptors associated with spinal analgesia

Answer 47

mu, kappa, delta

Question 48

receptors associated with respiratory depression

Answer 48

mu

Question 49

receptors associated with dec GI motility

Answer 49

mu, delta

Question 50

receptors associate with psychotomimesis

Answer 50

kappa

Question 51

receptors associated with sedation

Answer 51

mu, kappa

Question 52

G protein associated with opioid receptors

Answer 52

G(i)