Opioid

Question 1

What are the 3 opioid receptors?

Answer 1

Mu/kappa/delta

Question 2

What protein is mu receptor coupled with and where do you find these receptors?

Answer 2

Gi coupled

Pre and post synaptic

Question 3

How does stimulating mu receptor decrease pain?

Answer 3

Stimulate presynaptic mu—>decrease Ca influx—>decrease substance P (pain transmitter)
Stimulate postsynaptic mu—>increase K efflux—>membrane hyperpolarization

Question 4

What are the Gi coupled presynaptic and post synaptic receptors besisdes mu?

Answer 4

Presynaptic—>MAD2

Postsynaptic—>M2

Question 5

What is the analgesia effect?

Answer 5

Increase pain tolerance and decrease perception and reaction to pain

Question 6

What is the mechanism of morphine and what are its effect? what drug is used for overdose?

Answer 6

Mu agonist
Analgesia/sedation
Respiratory depression—>decrease response to increase CO2
Naloxone—>mu blocker

Question 7

Morphine cause vasodilation or vasoconstriction? and what should we be cautious about giving morphine to head trauma pt?

Answer 7

Morphine—>histamine release—>vasodilation

Vasodilation might cause increase intracranial pressure

Question 8

What are the side effects of opioid?

Answer 8

Miosis 
Decrease peristalsis--->constipation
Urinary retention
Gallbladder spasm
Increase biliary pressure

Question 9

Does opioid suppress or induce coughing/vomiting?

Answer 9

Suppress coughing (antitussive)
Induce vomiting

Question 10

How is morphine metabolized and what is the effect of the metabolite?

Answer 10

Glucuronidation

Morphine-6-glucuronide—>high active

Question 11

Opioid is contraindicated in pul dysfunction but what pul condition can opioid be benefit?

Answer 11

Pul edema

Question 12

Which opioid cause mydrasis/tachycardia?

Answer 12

Meperidine—>anti M as well

Metabolized into normeperidine and act as a SSRI

Question 13

Which opioid is used as a cough suppressant? CYP450 inhibitor increase or decrease the effect of codeine?

Answer 13

Codeine

Decrease—>codeine is a prodrug and is needed to be metabolized into morphine

Question 14

What are the full and mixed agonist of mu receptor?

Answer 14

Full agonist–>meperidine/methadone/codeine

Mixed agonist—>buprenophine/nalbuphine/pentazocine

Question 15

What receptors do these mixed agonist work on?

Answer 15

Mixed agonist—>stimulate kappa receptor/block mu receptor

Question 16

What would happen if you take buprenophine/nalbuphine/pentazocine and a full mu agonist like heroine at the same time?

Answer 16

Cause heroine withdraw:

Heroine is a full mu agonist—>buprenophine/nalbuphine/pentazocine block mu—>cause heroine withdraw

Question 17

Nalbuphine and pentazocine should not be given with?

Answer 17

A full mu agonist—>cause withdraw

Question 18

What drug is used for opioid induced constipation?

Answer 18

Methylnaltrexone

Question 19

Why is suboxone used for opiate addict?

Answer 19

Suboxone—>combo of buprenorphine + naloxone—>if taken IV—->get withdraw instead of a high

Question 20

What are the withdraw signs of opioid?

Answer 20

Yawning/sweating/anxiety

Question 21

What drugs are used to manage opioid withdrawal?

Answer 21

Methadone and clonidine (alpha 2 agonist to offside some of the sympathetic symptoms of opioid withdraw)

Question 22

What is another drug besides codeine that can be used as antitussive?

Answer 22

Dextromethorphan

Question 23

What are the mechanisms of cocaine and amphetamine? what are their withdraw symptoms?

Answer 23

Cocaine—>block reuptake of DA/NE/5HT
Amphetamine—>increase release and block reuptake NE
Withdraw—>depression like

Question 24

What are the withdraw symptoms of benzo/barb/alcohol?

Answer 24

Stimulant like—>anxiety and agitation

Question 25

What is the mechanism of weed?

Answer 25

Bind to CB1 and CB2 cannabinoid receptors

Question 26

PCP works similarly like ___?

Answer 26

Ketamine–>they are both NMDA receptor blocker