OPIODS

Question 1

What acts as a partial agonist? Why is that benificial?

Answer 1

Cuz ull get the analgesic effect, but w/ out alot if SE

Question 2

Which one should be careful eith overdosing? Why

Answer 2

Buprenorphine lana its soo tightly bound to its receptor and so hard to dispace!

Question 3

Which one is safe in renal impairment?

Answer 3

buprenorphine

Question 4

Why can some ppl come and say oh codein wasnt that benefital? But some can say it was goals?

Answer 4

It depends on how much CYP 2D6 enzyme is expressed in their body, some have too much of it, some dont have alot

Question 5

WHO analgesic ladder?

Answer 5

1) simple analgesia» paracetamol, NSAIDS
2) weak opiod» codeine
3) strong opiod» Morphine, fentanyl

Question 6

Least lipophillic opiod

Answer 6

Morphine

Question 7

CYP 2D6 is inhibited by ?

Answer 7

Flouxetine

Question 8

When giving IV, Why should u not give nalxone as a bolus? but as a slow infusion

Answer 8

Bc if u give it as a bolus, it will competitivly antagonize R, & knock Morphine out of the way, u will then stop the bolus and the patient will leave the hospital with that morohine still circulating in their blood for longer than naloxone, and they rebind w/ the receptors> RESP DEPRRSSION.
BUT if u give short slow infusion, it was competitively antagonize that Morphine & reverse its effects very slowly, so the patient at least has time to metabolize that circulating morphine whilst that naloxone is still bound» u wont get crash

Question 9

What is codeine?

Answer 9

Moderate agonist

Question 10

Half life of fentanyl

Answer 10

6mins

Question 11

Which one is good to give if polypharmacy? Elderly? Why?

Answer 11

Burpenorphine, less syncopal effects and fall effects

If u have patients whose taking loads of meds and r more likely to fall as SE, u don‘t wanna give them an opiod thats gunna make them fall more

Question 12

Which drug doesn’t give u alot of SE? Why?

Answer 12

burprenorphine, once bound, only acts as a PARTIAL AGONIST, so u get the anelgesic effects but w/out the side effects

Question 13

Duration of action of naloxone?

Answer 13

1/2-1 hr

Question 14

Which one is less tho renally excreted than morphine?

Answer 14

Fentanyl

Question 15

Codeine is converted to morphine via?

Answer 15

CYP 2D6

Mohim lalls

Question 16

Which one is good for opiod addiction?

Answer 16

Buprenorphine

Question 17

What is used for terminal illness?

Answer 17

Diamorphone» epidurally

Question 18

Which one has low oral bioavailability? What does that mean

Answer 18

Naloxone, bc it has 1st pass effect in liver, only 2% is available in the circulation

Question 19

Which one has a RAPID onset of action?

Answer 19

Naloxone

Question 20

What is our main antagonist

Answer 20

Naloxone

Question 21

Explain naloxone’s affinity to recepters in comparison to buprenorphine & morphine?

Answer 21

Has a greater affinity to Mu than morphine

But less that buprenorphine

Question 22

Compared to morphine, is fentanyl more efficacious?potent?

Answer 22

Yes, has a high affinity for Mu R» more efficacious

No, less potent that Morphine

Question 23

What do we give to treat opioid addiction? Why?

Answer 23

Buprenorphine

We can swap someone w/ their current opoiod that we think theyre abusing onto bup. So their pain is still well controlled, but we DONT have the risk of resp. depression. SO THEN we can titrate down that dose,

But its important to know that they may still get w/ drawl SE, bc theyre not getting that high response.

Question 24

When giving it IV, Why cant we give naloxone as a bolus and must be given as a slow infusion?

Answer 24

It has a short half life, so if u give it as a bolus it will competitively antagonize those receptors & knock all morphine out if the way, u will then stop the bolus and they will get angry, cuz u reversed they high, they will walk out the hospital but that morphine is still circulating in their system for longer than naloxone & it will rebind to the recepters and u will get respiratory depression again & the patient will collapse.

Where as slow infusion, u will competitively antagonize that morphine & reverse the effects slowly & in a safe way, so that the patient has time to metabolize and eliminate that morphine, whilst the naloxone is still bound.

Question 25

Which one should u be aware of giving it alongside another opioid? Why?

Answer 25

Buprenorphine, it easily displaces them

Question 26

What can be given as a patch and lasts within a week, and slowly reduces its dose?

Answer 26

Buprenorohine

Has a ling half life

Question 27

Name a competitive antagonist?

Answer 27

Naloxone

Question 28

Which drug when given w/ another opioid, it displaces it?

Answer 28

Buprenorphine

Question 29

Which one has an elimination via bilialry system

Answer 29

Buprenorohine» Biliary

Question 30

Why is oral not the best route for naloxone?

Answer 30

Bc it has a very low oral bioavailability, even tho it 90% absorption in the gut, it doesnt matter lana most of it goes through 1st pass metabolism in the liver and only 3% is available in the circulation

Question 31

What is our main competitive antagonist?

Answer 31

Naloxone

Question 32

What disease should u be cautious in when giving morphine? Why?

Answer 32

Athamatics»

Cuz morohine causes Mast degranulation, massive histimine release> asthma attack

Question 33

What is contraindicated it children below 12? Why?

Answer 33

Codeine, bc of the resp. Depression, children have massive tonsils and adenoids

Question 34

Does it have a better or lower affinity to Mu R than morphine?

Answer 34

Greater affinity than Mor

But less than Bupr

Question 35

How do u measure morphine in someone?

Answer 35

Measure it in urine

Question 36

Whynis morphine given mainly IV?

Answer 36

Cuz first pass metabolism in GI > slow> so we give it IV

Question 37

What do we give for diharrea why?

Answer 37

Morohine? Inhibits myenteric olexus & cause SM contraction

Question 38

Do we give naloxone for opioid addiciton? Why?

Answer 38

No,