pharm- opioid analgesics

Question 1

what is the critical role of opioids

Answer 1

balanced anesthesia and perioperative pain management

Question 2

what is synergism?

Answer 2

combining opioids with other sedatives

Question 3

what is done to minimize the risk of adverse effects of opioids?

Answer 3

dose adjustments

Question 4

what are considered semisynthetic opioids

Answer 4

simple modifications of the morphine molecule

Question 5

what are more complex, mixed agonist- antagonists opioids

Answer 5

nalbuphine and even complete antagonists such as naloxone

Question 6

what was the first completely synthetic opioid ?

Answer 6

meperidine

Question 7

the mechanism of action of opioids cause an activation of ________, causing inhibitory effects, these inhibitory effects cause _____________, then causing a reduction of ___________

Answer 7

G protein

hyperpolatization

neuronal excitability

Question 8

opioid receptors are linked to G proteins, activation of Gi leads to decreased _____

Answer 8

cAMP

Question 9

what multiple sites are affected by opioids?

Answer 9

dorsal horn of the spinal cord, brainstem, forebrain

Question 10

absorption of opiates via IM, SC routes is rapid and reaches peak plasma levels within ____

Answer 10

30 min

Question 11

Oral absorption of opiates is rapid and has a significant firsta pass ratio with a los ____/_____ ratio

Answer 11

oral/ parenternal

Question 12

opiates rapidly conjugates with ______ in the _____ and ______

Answer 12

glucuronide

liver and intestine

Question 13

what is the active metabolite of morphine

Answer 13

morphine-6-glucoronide

Question 14

does morphine cross placenta?

Answer 14

yes

Question 15

what is the main CNS effect of opioids

Answer 15

analgesia - interferes with forebrain mechanisms, inhibits conduction

Question 16

what side effects to the CNS can opiates have?

Answer 16

behavioral effects such as dysphoria followed by euphoria, sedation, drowsiness, and mental clouding, antitussive (direct action on medulla to suppress cough reflex)

Question 17

what effect do opiates have on hypothalamus?

Answer 17

decreases body temp., decreases ACTH, FSH, LH, TSH

Question 18

what effect do opiates have on respiration?

Answer 18

respiratory depression

OD death by resp. failure

Question 19

what effect do opiates have on GI tract?

Answer 19

increase tone and decrease peristalsis (constipation)

Question 20

what effect do opiates have on biliary tract?

Answer 20

gall bladder or bile duct spasm due to increased biliary pressure

Question 21

what effect do opiates have on urinary tract?

Answer 21

increased muscle tone and decreased urinary output

Question 22

what effect do opiates have on cardiovascular system and brain?

Answer 22

orthostatic hypotension as a result of CNS actions, histamine release

cerebral vasodilation increasing CSF pressure

Question 23

what effect to opiates have on immune system?

Answer 23

suppression of function of NK cells

Question 24

what is wood thorax?

Answer 24

when rapid administration and large doses of fentanyl make ventilation via a bag and mask impossible because of vocal cord rigidity and closure

Question 25

acute toxic symptoms of opiates include a triad of __?

Answer 25

coma, pinpoint pupils, respiratory depression

Question 26

how do you treat toxicity of opiates?

Answer 26

maintain respiration, opioid antagonists (naloxone)

Question 27

a prodrug: where morphine is the active compound and is metabolized by O-demethylation into morphine by the liver (CYP2D6)

Answer 27

codeine

Question 28

a patient with a lack of CYPD26 would not benefit from what opioid?

Answer 28

codeine

Question 29

a prototype opioid replaced by fentanyl as the most used intraoperative, with a prolonged latency to peak effect

Answer 29

morphine

Question 30

what opioid penetrates the CNS slowly making it less likely to cause respiratory distress?

Answer 30

morphine

Question 31

what opiates active metabolite is M6G?

Answer 31

morphine

Question 32

what is the most important opioid in modern anesthesia practice?

Answer 32

fentanyl

Question 33

what routes can fentanyl be administrated?

Answer 33

intravenous , transdermal, transmucosal, transnasal, and transpulmonary

Question 34

fentanyl has a high first pass avoidance this means?

Answer 34

larger bioavailability

Question 35

what route administration is best for pain in opioid tolerant cancer patients

Answer 35

oral transmucosal (OTFC) + transdermal fentanyl patch

Question 36

what was the first opioid to be administered by continuous infusion?

Answer 36

alfentanil

Question 37

short acting opioid with high diffusible fraction, reaches peak effect effect site concentrations quickly

Answer 37

alfentanil

Question 38

what opioid has an unpredictable hepatic metabolism with significant interindividual variability of hepatic CYP3A4

Answer 38

alfentanil

Question 39

what is the most potent opioid commonly used in anesthesia? 1000 fold less than morphine dose

Answer 39

sufentanil

Question 40

opioid with specific clinical goals: very short acting opioid, losing u-receptor agonist activity upon ester hydrolysis. drug that can be titrated up and down as necessary/ used in total intravenous anesthesia

Answer 40

remifentanil

Question 41

class of drugs that is a partial agonist and competitive antagonist at the U receptor

Answer 41

opioid agonist-antagonist

Question 42

what class of drugs have ceiling effect? what does that mean?

Answer 42

opioid agonist-antagonists analgesics with more limited ventilatory depression (less analgesia)

Question 43

tramadol, buprenorphine, and nalbuphine are

Answer 43

opioid agonist- antagonists read slide on info of those

Question 44

what are pure opioid antagonists

Answer 44

complete competitive antagonists of the opioid receptor, used for opioid overdose

Question 45

injectable u antagonist

Answer 45

naloxone/naltrexone

Question 46

go over guides for rational use of opiod analgesics

Answer 46

:)