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BR 3rd Ed > Ch 11 - Pain Medicine: Opioid Pharmacology > Flashcards

Ch 11 - Pain Medicine: Opioid Pharmacology Flashcards

1
Q

What are the presynaptic actions of opioids?

A

Lower influx of Ca to reduce NT release in sensory C fibers

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2
Q

What are the postsynaptic actions of opioids?

A

Inc the transport of K in the cell to facilitate hyperpolarization in 2nd
order neurons

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3
Q

Opiates activate the chemoreceptor trigger zone in the medulla, which leads to ____.

A

GI SE of nausea and vomiting

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4
Q

Opioid receptor type Mu1 causes

A

Analgesia

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5
Q

Opioid receptor type Mu2 causes

A 
Respiratory depression Sedation
Vomiting
Euphoria
Anorexia
Physical dependence
Pruritus
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6
Q

Opioid receptor type Delta causes

A

Analgesia

Spinal analgesia

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7
Q

Opioid receptor type Kappa causes

A 
Analgesia
Sedation
Psychomimetic effects
Dyspnea
Respiratory depression
Euphoria
Dysphoria
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8
Q

Lipid-soluble drugs exert most of their effect at ___.

A

Localized areas where they are administered

ex) fentanyl

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9
Q

What are the endogenous opioids?

A

Leu-Enkephalin
Beta-Endorphin
Dynorphin A&B

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10
Q

What are the opioid agonists?

A 
Morphine
Diamorphine (heroin)
Fentanyl
Meperidine
Methadone
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11
Q

What are the opioid antagonists?

A

Naloxone

Naltrexone

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12
Q

What are the partial opioid agonists?

A

Buprenorphine

Pentazocine

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13
Q

MOA of oxycodone

A

Mu agonist

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14
Q

Metobalites of Oxycodone

A

Oxymorphone

Noroxycodone

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15
Q

MOA of Oxymorphone

A

Opioid agonist

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16
Q

Metabolites of Oxymorphone

A

6-Hydroxy-oxymorphone

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17
Q

MOA of Hydromorphone

A

Mu agonist

18
Q

Metabolites of Hydromorphone

A

Hydromorphone-3-Glucuronide

19
Q

MOA of Tramadol

A

Weak Mu agonist

Weak NE/5HT reuptake inhibitor

20
Q

Contraindication for Tramadol

A

CI with MAOI or SSRI d/t serotonin syndrome

21
Q

MOA of Morphine

A

Mu agnoist

22
Q

Metabolites for Morphine

A

Morphine-3-glucuronide
Morphine-6-glucuronide
Hydromorphone

23
Q

Contraindication for Morphine

A

Do not use in renal failure

24
Q

MOA of Meperidine

A

Weak mu

agonist

25
Q

Metabolites of Meperidine

A

Normeperidine

26
Q

Contraindication for Meperidine

A

Do not
administer with
MAOI

27
Q

MOA of Hydrocodone

A

Mu and kappa

agonist

28
Q

Metabolites of Hydrocodone

A

Dihydrocodeine

Hydromorphone

29
Q

MOA of Methadone

A 
Mu and delta
agonist
NE and 5HT
reuptake
inhibitor
NMDA
antagonist
30
Q

Metabolites of Methadone

A

2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP) (inactive)

31
Q

Contraindication for Methadone

A

May cause QT

prolongation

32
Q

MOA of Fentanyl

A

Mu agonist

33
Q

Metabolites of Fentanyl

A

Norfentanyl

34
Q

MOA of Buprenorphine (Subutex or Suboxone)

A 
Partial mu and kappa agonist, delta antagonist Suboxone
contains naloxone (receptor antagonist)
35
Q

MOA of Pentazocine (Talwin)

A

Kappa agonist, mu antagonist

36
Q

MOA of Butorphanol (Stadol)

A

Kappa agonist, mu antagonist

37
Q

MOA of Nalbuphine (Nubain)

A

Kappa agonist, mu antagonist

38
Q

How can opioids cause respiratory sedation?

A

Acts on brainstem to reduce sensitivity of the respiratory centers to PCO2

39
Q

How can opioids suppress coughing?

A

Inhibitory effect on the brainstem nuclei in the cough reflex pathway
(common use for codeine)

40
Q

How do opioids cause constipation?

A

Maintained contraction of the smooth muscles in the gut (and therefore decreased
motility)

41
Q

How do opioids cause sexual dysfunction?

A

Correlated to hypogonadism and
associated with lower testosterone levels
(erectile dysfunction, decreased libido)

BR 3rd Ed (92 decks)

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