Opioid analgesica

Question 1

morphine analogues:

Answer 1

structure similar to morphine

Question 1

synthetics:

Answer 1

unrelated structure to morphine

Question 2

morphine-like alkaloids:

Answer 2

morphine
diamorphine
codeine

Question 3

heroin vs morphine

Answer 3

both strong analgesic
more lipid soluble
shorter duration

Question 4

codeine vs morphine

Answer 4

less analgesia
NSAID
antitussive

Question 5

codeine as an antitussive replaced with…

Answer 5

dextropmethorphran

Question 6

synthetic opiates:

Answer 6

benzamorphanes
phenylpiperidine
thebaine

Question 7

pethidine vs morphine

Answer 7

restlessness
antiuscarinic
shorter duration of action

Question 8

fentanyl vs morphine

Answer 8

80-100 x more potent than morphine
rapid onset
short duration
anesthesia

Question 9

the activity of tramadol:

Answer 9

weak mu agonist
serotonin and norepinephrine reabsorption inhibitor
moderate to severe pain

Question 10

both tramadol and codeine are….

Answer 10

partial agonist

Question 11

explanation of tramadol psychotropic effects:

Answer 11

it is an serotonin and norepinephrine reabsorption inhibitor

Question 12

methadone receptor selectivity

Answer 12

mu

Question 13

methadone vs morphine

Answer 13

slow acting
longer duration of action
less problems with withdrawal
given orally

Question 14

methadone applications:

Answer 14

wean off heroin and morphine addiction

Question 15

pharmacokinetics of Heroin vs methadone

Answer 15

methadone plasma concentration doesn’t induce euphoria or withdrawal

Question 16

loperamide receptor selectivity

Answer 16

mu

Question 17

loperamide effects:

Answer 17

decreases GIT motility
suppresses gastocolic reflex

Question 18

why does loperamide have reduced circulation?

Answer 18

P-glycoprotein efflux

Question 19

loperamide permeability:

Answer 19

poor blood-brain barrier permeability and so no analgesic activity/ euphoria

Question 20

loperamide uses:

Answer 20

anti-diarrhea

Question 21

full agonists:

Answer 21

morphine
heroin

Question 22

agonist-antagonists

Answer 22

cyclazocine
pentazocine

Question 23

antagonists

Answer 23

naloxone
naltrexone

Question 24

partial agonists:

Answer 24

partial effiacy, regarldess of max concntration codeine

Question 25

agonist and antagonist

Answer 25

different towards different receptors different depending on the concentration

Question 26

antagonists

Answer 26

competitive or non-competitive

Question 27

pentazocine selectivity:

Answer 27

agonist at K receptors weak antagonist at mu and delta

Question 28

pentazocine at low doses

Answer 28

similar to morphine

Question 29

pentazocine at high doses:

Answer 29

dysphoria respiratory depression decreases GIT activity hallucinations nightmares