Specific opioid agents Flashcards

1
Q

Agonists with high oral bioavailability

A

Levorphanol
Codeine
Methadone

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2
Q

Agonists with low/no oral bioavailability

A

Fentanyl

Morphine

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3
Q

Morphine

A

Mu agonist (kappa and delta at higher)

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4
Q

Hydromorphone

A

Mu agonist (kappa and delta at higher)

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5
Q

Oxymorphone

A

Mu agonist (kappa and delta at higher)

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6
Q

Heroin

A

Full mu agonist

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7
Q

Codeine

A

Mu agonist

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8
Q

Oxycodone

A

Mu agonist

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9
Q

Hydrocodone

A

Mu agonist

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10
Q

Meperdine

A

Mu agonist

DOESNT CROSS PLACENTA!

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11
Q

Fentanyl

A

Mu agonist
VERY POTENT
Fast onset, SHORT duration

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12
Q

Sufentanil

A

Mu agonist
VERY potent
FAST onset, SHORT duration

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13
Q

Remifentanyl

A

Mu agonist
VERY potent
FAST onset, SHORT duration

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14
Q

Levorphanol

A
Mu agonist (synthetic)
Also antagonizes NMDA receptors
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15
Q

Methadone

A

WEAK mu agonist (used for addiction to reduce cravings and withdrawal symptoms)

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16
Q

Naloxone

A

Mu, Kappa, and Delta ANTAGONIST

SHORT acting

17
Q

Naltrexone

A

Mu, Kappa, and Delta ANTAGONIST

LONG acting

18
Q

Nalmefene

A

SELECTIVE mu antagonist

19
Q

Pentazocine

A

Partial mu agonist, K agonist

Low doses good
High doses bad, start getting dysphoria/psychomimetic activity from k agonism

20
Q

Which antagonists are injectable only?

A

All of them!

21
Q

Which antagonists are available orally?

A

None of them!

22
Q

Nalbuphine

A

Full K agonist, mu antagonist

More effective in women

23
Q

Butorphanol

A

Partial mu agonist, full K agonist

24
Q

Buprenorphine

A

Partial mu agonist, full K antagonist

In suboxone!

25
Q

Tramadol

A

Weak mu agonist + SERT/NET inhibition

26
Q

Tapentadol

A

Weak mu agonist + NET inhibition

27
Q

Spiradoline

A

Full K antagonist

BAD

28
Q

CR845

A

Didn’t say what it does?
Doesn’t cross BBB!
Outstanding analgesia!

29
Q

Dextramorphan

A

D-isomer of codeine
No analgesia; does not bind opioid receptor
Used for cough

30
Q

Diphenoxylate

A

Weak mu agonist
Used as antidiarrheal
Schedule V - high doses can cause CNS effects (euphoria, abuse liability)

31
Q

Loperamide

A

Weak mu agonist, crosses BBB but is pumped out by P-GP transporter

32
Q

Which mixed action drugs are available orally?

A

Pentazokine
CR845
Buprenorphine

33
Q

Which mixed action drugs are not available orally?

A

Nalbuphine

Spiradoline

34
Q

Which mixed action drug is a nasal spray?

A

Butorphanol