Opiate Agonists

Question 1

Mu 3+ agonists only

Answer 1

hydromorphone, oxymorphone, methodone, meperidine, fentanyl, remifentanil

Question 2

Mu 2+ agonist

Answer 2

oxycodone

Question 3

Mu partial agonist only

Answer 3

codeine and hydrocodone

Question 4

Mu partial agonist, kappa agonist

Answer 4

butorphanol and pentazocine

Question 5

buprenorphine specificity

Answer 5

mu partial agonist, kappa antagonist, delta antagonist

Question 6

morphine specificity

Answer 6

Mu 3+, kappa +

Question 7

opiate moa

Answer 7

presynaptic block of Ca2+ influx in response to an action potential; post-synaptic increase in K+ conductance causing hyperpolarization

Question 8

opiate adverse effects

Answer 8

behavioral problems, sedation, nausea, urticaria and pruritus, respiratory depression, immunouppression, increased intracranial pressure, hypotension, urinary retention

Question 9

opiate overdose

Answer 9

coma, pinpoint pupils, respiratory depression

Question 10

NMDA agonist (drugs)

Answer 10

ketamine and dextromethorphan

Question 11

NMDA agonist moa

Answer 11

blockage of NMDA receptors prevents central sensitization; often used prior to surgery

Question 12

katamine adverse effects

Answer 12

hallucinations, amnesia, CV pressor, increased intracranial pressure

Question 13

dextromethorphan adverse effects

Answer 13

dizziness, confusion, fatigue, hallucinations if abused

Question 14

meperidine effects in addition to opiate agonism

Answer 14

inhibts 5-HT and NE reuptake and has central and peripheral anticholinergic actions

Question 15

meperidine adverse effects

Answer 15

serotonin syndrome, blurring of vision, constipation, tachycardia, xerostomia, glaucoma, agitation, delirium, memory deficits

Question 16

administring buprenorphine to an opiate dependent patient

Answer 16

may precipitate withdrawal due to the high binding of buprenorphine to opiate receptors

Question 17

meperidine metabolism

Answer 17

some is metabolized to a toxic metabolite; can be harmful in some patients

Question 18

codeine metabolism

Answer 18

converted to morphine by CYP2D6

Question 19

tramadol moa

Answer 19

weak 5-HT and NE reuptake inhibitor in the spinal cord and weak Mu agonist metabolite

Question 20

tramadol adverse effects

Answer 20

hypoglycemia; serotonin and norepinephrine effects, accumulates in renal failure

Question 21

naloxone and naltrexone moa

Answer 21

antagonists at mu delta and kappa receptors; precipitate withdrawal;
naloxone - overdose treatment
naltrexone: maintenance programs for addicts; also decreases alcohol craving in alcoholics by decreasing baseline endorphin release

Question 22

gabapentine and pregabalin moa

Answer 22

binding to the alpha2delta subunit of the Ca2+ channel blocks up-regulation of the channel leading to inhibition of neuronal excitability, particularly in dense, synaptic connection of the neocortex, amygdala, and hippocampus

Question 23

gabapentine and pregabalin adverse effects

Answer 23

dizziness and drowsiness

Question 24

lamotrigine and carbamazepine moa

Answer 24

block Na+ channel function

Question 25

lamotrigine adverse effects

Answer 25

diplopia, Stevens-Johnson syndrome, hematologic effects

Question 26

carbamazepine adverse effects

Answer 26

dizziness, drowsiness, agranulocytosis (rare)

Question 27

TCA moa

Answer 27

NE and 5-HT reuptake inhibition

Question 28

TCA metabolism

Answer 28

hepatic-2D6 interactions

Question 29

TCA adverse effects

Answer 29

dizziness, lethargy, and hypersomnia

Question 30

TCAs (specific drugs)

Answer 30

amitriptyline, nortriptyline, imipramine, desipramine

Question 31

opiate withdrawal symptoms

Answer 31

agitation, diaphroesis, increased lacrimation, piloerection, dilated pupils, HR and BP are usually wnl (may be slight tachycardia)

Question 32

Tx of opiate withdrawal in outpatients

Answer 32

clonidine

Question 33

Tx of opiate withdrawal in inpatients

Answer 33

methodone

Question 34

optiate symptoms that are refractory to tolerance

Answer 34

miosis, constipation, and convulsions

Question 35

nalbuphine specificity

Answer 35

mu antagonist, kappa agonist 2+