Exam 4 Opioid

Question 1

opiates vs opioids

Answer 1

opiates- alkaloids found in opium poppies
opioids- semi-synthetic or synthetic drugs that resemble opiates
***Opium makes morphine and heroin!

Question 2

what is used for opiod emergencies?

Answer 2

naloxone (Narcan) - a pure opiod antagonist

Question 3

two naturally occuring opiates?

Answer 3

morphine and codeine

Question 4

what is unique about pentazocine action on receptors?

Answer 4

mu receptor antagonist but kappa receptor agonist

Question 5

what is unique about naloxone on receptors?

Answer 5

antagonist to both mu and kappa receptors

Question 6

opiod actions on CNS, respiratory, cardio, GI, eye and others?

Answer 6

CNS- analgesic, mental clouding, nausea (chemoreceptor trigger zone), and antitussive action (cough suppression)

respiratory depression -fatal

cardio- vasodilation due to histamine release and CO2 retention

GI- stimulant, increase muscle tune, makes ya poop (OIC) bc so many MU RECEPTORS in GI

eye- constriction

histamine release which is NOT a true allergy

Question 7

3 endogenous opioid receptor families?

Answer 7

enkephalin, endorphin and dynorphin

Question 8

morphine overdose triad effects?

Answer 8

1) comatose (narcosis)
2) cyanotic depressed respiration (CO2 retention)
3) pinpoint pupils (miosis)

Question 9

first past effect on morphine?

Answer 9

significant amount of morphine fails to reach circulation due to first past effect, need a LARGE oral dose or normal parental dose

Question 10

CYP2D6 metabolizes what?

Answer 10

codeine, hydrocodone, oxycodone, tramadol

Question 11

CYP3A4 metabolizes what?

Answer 11

meperidine, fentanyl, buprenorphineq

*poor oral availability

Question 12

morphine is metabolized where? conjugated with what? makes what irritant?

Answer 12

liver
conjugated with glucuronic acid
morphine 3 glucuonide is a cerebral irritant

Question 13

black box warning for codeine for children? good to use for what in adult?

Answer 13

they may hyper express CYP2D6, otherwise it’s a great antitussice (cough) although not a good pain med like morphine

Question 14

what is vicodin?

Answer 14

hydrocodone

Question 15

hydrocodone

Answer 15

analgesic effect b/w morphine and codeine (M>H>C); all schedule 2

Question 16

heroin is schedule?

Answer 16

schedule 1, the most lipid soluble

Question 17

meperidine (Demerol)

- two derivatives?

Answer 17

diphenoxylate which CAN pass BBB and loperamide which canNOT pass BBB
- it is a cerebral irritant

Question 18

codeine is a ____ drug?

Answer 18

pro-drug

Question 19

fentanyl

Answer 19

not FDA recomended for acute or postop pain

• more potent than morphine but short acting
• terrrorist attacks

Question 20

methadone (dolophine)

Answer 20

not much use for dentists bc of slow onset, but good to treat addiction bc you don’t get withdrawal when you wean off
- significant role in overdose fatality and fatal cardiac arrhythmias

Question 21

Tramadol (Ultram)

• schedule?
• active metabolite?
• assos. w/ what syndrome?

Answer 21

a schedule 4 pro-drug

• metabolized into schedule 2 tapentadol (Nucyntar) metabolite by CYP450/CY2D6
• serotonin syndrome

Question 22

two parital opiod antagonists?

Answer 22

1) pentazocine

2) buprenorphrine - used in maintenance therapy (Ex: Suboxone contains naloxone)

Question 23

two mu receptor activation pathways?

inhibits the release of ____

Answer 23

1) close Ca+ channel, LESS transmitter released in pre-synaptic
2) open K+ channels, hypERpolarizes postsynaptic nerve making it harder to activate
* *inhibites glutamate release - primary pain fiber in dorsal horn of spinal cord**

Question 24

do not combine opioid pain medications with what other drug class?

Answer 24

benzodiazepine