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7262 MS Block 1 > Emmitte Pharmacology > Flashcards

Emmitte Pharmacology Flashcards

1
Q

Which has better CNS penetration, heroin or morphine?

A

heroin

prodrug, and is more lipophilic

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2
Q

3 C3 methyl ethers:

A

codeine
oxycodone
hydrocodone

all have “co” in name

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3
Q

oxymorphone achieves effects how?

A

mu agonist

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4
Q

nalbupine achieves effects how?

A

kappa agonist

mu antagonist

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5
Q

butorphanol achieves effects how?

A

kappa agonist

mu antagonist

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6
Q

buprenorphine achieves effects how?

A

partial mu agonist

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7
Q

what is the pharmacophore of morphine and derivatives?

A

4-phenylpoiperadine

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8
Q

Opioid receptors are highly selective for __ isomers?

levo or dextro

A

levo

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9
Q

What isomers are used as antitussives?

levo or dextro

A

dextro

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10
Q

How many carbons in R1 group of oxymorphone?

A

1

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11
Q

How many carbons in R1 of naloxone and naltrexone?

A

3-4

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12
Q

How many carbons in R1 group of nalbuphine?

A

5

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13
Q

Naloxone and naltrexone achieve effect how?

A

antagonism of mu receptors

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14
Q

nalbuphine achieves effect how?

A

kappa agonist

mu antagonist

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15
Q

What effect does a hydroxyl at C3 have?

A

slows CNS penetration, increased affinity, decreases antitussive activity

oxymorphone has OH, hhydromorphone does not

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16
Q

An OH at which carbon is associated with histamine release?

A

C6

morphine

17
Q

Is oral bioavailability enhanced or decreased by methyl ether?

A

enhanced

O-demethylation must occur for analgesic activity

18
Q

Is morphine-6-glucuronide active?

A

yes

active metabolite that contributes to analgesic activity

19
Q

What must occur to methyl ether for analgesic activity?

A

O-demethylation

20
Q

CYP450s do not play a significant role in the metabolism of what two opioids?

A

hydromorphone
oxymorphone

DDIs less of a concern

21
Q

C3 methoxys (codeine, hydrocodone, oxycodone) require O-demethylation by what CYP for high affinity binding to mu receptor?

A

2D6

rxn is normally sluggish

22
Q

Replacement of the N-methyl group with __ or __ yields mu receptor antagonists

A

allyl, cyclopropylmethyl

23
Q

What is methylnaltrexone used to treat?

A

constipation in pts on chronic opioids

24
Q

Which mu antagonist is a quaternary amine used for constipation?

A

methylnaltrexone

25
Q

Is buprenorphine a mu antagonist?

A

no

partial mu agonist with 25-50 fold the analgesic potency of morphine

26
Q

Despite the cyclopropylmethyl group, __ is not a mu antagonist - instead a partial mu agonist with 25-50 fold the analgesic potency or morphine

A

buprenorphine

27
Q

2 major side effects of kappa agonists?

A

sedation

dysphoria

28
Q

Kappa agonists produce __ respiratory depression, constipation, euphoria, and potential for addiction than mu agonsits

A

less

29
Q

2 flexible (non-morphine) opioids:

A

meperidine

fentanyl

30
Q

Does fentanyl have a long or short duration of action?

A

short

redistributes rapidly to other tissues; useful for anesthetic adjuvant use

31
Q

Fentanyl contains the __ group, which engenders a very high affinity for mu receptors and increased lipophilicity, which translates into rapid CNS penetration and fast onset

A

N-phenyethyl

32
Q

which flexible (non-morphine derivative) opioid can cause serotonin syndrome?

A

meperidine

CI with MAOIs

33
Q

What flexible opioid metabolite can cause neurological side effects?

A

normeperidine

34
Q

Compounds that interact with CYP__ can effect the exposure of fentanyl and its efficacy/side effects

A

3A4

35
Q

Which enantiomer of methadone has analgesic activity, R or S?

A

R

36
Q

Two metabolites of methadone are mechanism-based inhibitors of which CYP?

A

2C19

37
Q

2 monoamine reuptake inhibitor opioids?

A

tramadol

tapentanol

38
Q

Each tramadol enantiomer as well as the ___ metabolite of the dextrorotatory enantiomer contributes to pharmacological activity

A

O-demethylated

39
Q

Tramadol carries a risk of __ syndrome in pts taking SSRIs, MAOIs, TCAs

A

serotonin

7262 MS Block 1 (11 decks)

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