Pharm Chapter 31

Front 1

three major therapeutic uses of opioids

Back 1

analgesics, antitussives, and antidiarrheals

Front 2

prototype of a strong analgesic, full agonist

Back 2

morphine

Front 3

mixed agonist-antagonist MOA

Back 3

activates one opioid receptor subtype while blocking another

Front 4

three opioids that undergo extensive first-pass metabolism

Back 4

morphine, hydromorphone, oxymorphone

Front 5

crossing the placental barrier can result in?

Back 5

fetal respiratory depression, physical dependence

Front 6

metabolism of opioids

Back 6

hepatic

Front 7

metabolites

Back 7

inactive glucuronide conjugates

Front 8

elimination of opioids

Back 8

renal

Front 9

metabolite with analgesic activity equivalent to morphine

Back 9

morphine-6-glucuronide

Front 10

metabolite that is neuroexcitatory

Back 10

morphine-3-gluruonide

Front 11

cytochrone CYP2D6 metabolizes which?

Back 11

codeine, oxycodone, hydrocodone

Front 12

codeine is demethylated by CYP2D6 to form what active metabolite?

Back 12

morphine

Front 13

what causes increased peak serum levels of hydromorphone and oxymorphone?

Back 13

alcohol

Front 14

what is meperidine metabolized to and why is this significant?

Back 14

normeperidine, may cause seizures at high plasma levels

Front 15

what is remifentanil and how is it metabolized?

Back 15

congener of fentanyl; plasma and tissue esterases (has a very short half life)

Front 16

location of action for opioid receptors functioning as pain modulators

Back 16

primary afferents and spinal cord pain transmission neurons and neurons in the midbrain and medulla

Front 17

location of opioid receptors that may be involved in altering reactivity to pain

Back 17

neurons in the basal ganglia, hypothalamus, limbic structures, and cerebral cortex

Front 18

three major opioid receptor subtypes

Back 18

u, delta, K

Front 19

major role of the u-receptor activation

Back 19

respiratory depressant actions of opioids

Front 20

major role of the K-receptor activation

Back 20

with u-receptors=slows GI transit
alone= sedative actions

Front 21

major role of the d-receptor activation

Back 21

development of tolerance

Front 22

how are opioid receptors activated?

Back 22

endogenous peptides under physiologic conditions

Front 23

Examples of these peptides?

Back 23

B-endorphin, enkephalins, dynorphins

Front 24

peptides and receptors with most affinity

Back 24

u receptors-endorphins
K receptors-dynorphins
d receptors- enkephalins

Front 25

other places where opioid receptors are found

Back 25

adrenal medulla and neural plexus of the gut

Front 26

MOA of opioid analgesics

Back 26

inhibit synaptic activity through direct activation of opioid receptors and partly through release of the endogenous opioid peptides

Front 27

how do they work at postsynaptic level

Back 27

activation of receptors can open potassium ion channels and cause membrane hyperpolarization (inhibitory)

Front 28

how do they work at the presynaptic level

Back 28

receptor activation can cause voltage-gated calcium ion channels to inhibit neurotransmitter release

Front 29

presynaptic actions result in the inhibition of release of what neurotransmitters

Back 29

acetylcholine, norepinephrine, serotonin, glutamate, and substance P

Front 30

examples of strong agonists with highest analgesic efficacy

Back 30

morphine, methadone, meperidine, fentanyl, levorphanol, heroin

Front 31

examples of drugs with mixed agonist-antagonist actions

Back 31

buprenoprphine

Front 32

partial agonists with mild to moderate analgesic efficacy

Back 32

codeine, hydrocodone, oxycodone

Front 33

opioid actions in the medulla

Back 33

inhibition of respiratory center, with decreased response to CO2 challenge

Front 34

consequence of increased pCO2

Back 34

cerebrovascular dilation, resulting in increased blood flow and increased intracranial pressure

Front 35

opioid analgesics contraindicated in what population?

Back 35

those with head injuries

Front 36

cause of nausea and vomiting with opioids

Back 36

activation of the chemoreceptor trigger zone

Front 37

effect on smooth muscle

Back 37

contraction of biliary tract smooth muscle, resulting in biliary colic or spasm, increased ureteral and bladder sphincter tone, and a reduction in uterine tone (prolonging labor)

Front 38

cause of flushing and pruritus associated with opioid analgesics

Back 38

histamine release

Front 39

effects of opioid analgesics on hormone release

Back 39

release of ADH and prolactin, inhibit release of LH

Front 40

agents that block opioid tolerance

Back 40

antagonists of glutamate N-methyl-D-aspartate receptors (ketamine), and d-receptor antagonists

Front 41

abstinence syndrome symptoms

Back 41

rhinorrhea, chills, goosebumps, muscle aches, diarrhea, yawning, anxiety, and hostility

Front 42

useful oral antitussive drugs

Back 42

codeine and dextromethorphan

Front 43

two oral antidiarrheal opioids

Back 43

diphenoxylate and loperamide

Front 44

acute pulmonary edema opioid

Back 44

morphine (parenteral) due to hemodynamic actions

Front 45

major component of anesthesia for cardiac surgery

Back 45

high dose IV opioids (morphine, fentanyl)

Front 46

methadone use for opioid dependence

Back 46

longer acting opioid; permits a slow tapering of opioid effect that diminishes the intensity of abstinence symptoms; blocks europhic reelings of short acting opioids

Front 47

alternative withdrawal medicine other than methadone

Back 47

buprenorphine

Front 48

overdose triad of opioids

Back 48

pupillary constriction, comatose state, respiratory depression

Front 49

how is overdose diagnosed?

Back 49

injection of naloxone (antagonist) resulting in prompt signs of recovery

Front 50

most important drug interactions involving opioid analgesics

Back 50

additive CNS depression with ethanol, sedative-hypnotics, anesthetics, antipsychotic drugs, tricyclic antidepressants, antihistamines

Front 51

result of concomitant use of certain opioids with MAOIs

Back 51

increases incidence of hyper-pyrexic coma

Front 52

properties of buprenorphine

Back 52

agonist-antagonist; u-receptor partial agonist with weak antagonist effects at K and d recptors; long duration; resistant to naloxone reversal

Front 53

properties of butorphanol

Back 53

partial agonist or antagonist at u-receptor

Front 54

effects of agonist-antagonist drugs

Back 54

sedation at analgesic doses

Front 55

pure opioid receptor antagonists

Back 55

naloxone, nalmefene, naltrexone

Front 56

receptor affinity of pure antagonists

Back 56

mainly u-receptors (more strongly than others)

Front 57

duration of actions of pure antagonists

Back 57

naloxone (1-2 hr)