Opioid analgesica Flashcards

1
Q

morphine analogues:

A

structure similar to morphine

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1
Q

synthetics:

A

unrelated structure to morphine

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2
Q

morphine-like alkaloids:

A

morphine
diamorphine
codeine

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3
Q

heroin vs morphine

A

both strong analgesic
more lipid soluble
shorter duration

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4
Q

codeine vs morphine

A

less analgesia
NSAID
antitussive

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5
Q

codeine as an antitussive replaced with…

A

dextropmethorphran

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6
Q

synthetic opiates:

A

benzamorphanes
phenylpiperidine
thebaine

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7
Q

pethidine vs morphine

A

restlessness
antiuscarinic
shorter duration of action

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8
Q

fentanyl vs morphine

A

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

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9
Q

the activity of tramadol:

A

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

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10
Q

both tramadol and codeine are….

A

partial agonist

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11
Q

explanation of tramadol psychotropic effects:

A

it is an serotonin and norepinephrine reabsorption inhibitor

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12
Q

methadone receptor selectivity

A

mu

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13
Q

methadone vs morphine

A

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

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14
Q

methadone applications:

A

wean off heroin and morphine addiction

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15
Q

pharmacokinetics of Heroin vs methadone

A

methadone plasma concentration doesn’t induce euphoria or withdrawal

16
Q

loperamide receptor selectivity

A

mu

17
Q

loperamide effects:

A

decreases GIT motility
suppresses gastocolic reflex

18
Q

why does loperamide have reduced circulation?

A

P-glycoprotein efflux

19
Q

loperamide permeability:

A

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

20
Q

loperamide uses:

A

anti-diarrhea

21
Q

full agonists:

A

morphine
heroin

22
Q

agonist-antagonists

A

cyclazocine
pentazocine

23
Q

antagonists

A

naloxone
naltrexone

24
Q

partial agonists:

A

partial effiacy, regarldess of max concntration
codeine

25
Q

agonist and antagonist

A

different towards different receptors
different depending on the concentration

26
Q

antagonists

A

competitive or non-competitive

27
Q

pentazocine selectivity:

A

agonist at K receptors
weak antagonist at mu and delta

28
Q

pentazocine at low doses

A

similar to morphine

29
Q

pentazocine at high doses:

A

dysphoria
respiratory depression
decreases GIT activity
hallucinations
nightmares