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Year 2 Pharmacology > Opioid analgesics > Flashcards

Opioid analgesics Flashcards

1
Q

definition: opium

A

exudate from poppy seeds containing 20 biologically active components including morphine and codeine

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2
Q

definition: opiate

A

drug extracted from exudate of the poppy

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3
Q

definition: opioid

A

natural or synthetic drug that binds to opioid receptors producing agonist effects

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4
Q

what are the endogenous opioids?

A

endorphins, enkaphalins, dynorphins

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5
Q

what are the endogenous opioid receptors?

A

mu 1

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6
Q

where are the mu 1 receptors located? what is their function?

A

outside spinal cord

central interpretation of pain - supraspinal analgesia

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7
Q

where are the mu 2 receptors located? what is their function?

A

throughout CNS - brainstem and spinal cord

supraspinal and spinal analgesia 
respiratory depression 
constipation 
physical dependence 
euphoria
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8
Q

what are the metabolites of morphine?

A

morphine-6-glucoronide (M6G) and M3G

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9
Q

how is morphine metabolized?

A

glucoronidation

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10
Q

heroin and codeine are metabolized to what compound?

A

morphine

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11
Q

what GPCRs are associated with opioid binding?

A

Gi / Go

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12
Q

what is the mechanism of opioid binding to Gi / Go receptors?

A

inhibition of adenylyl cyclase - decreased cAMP
loss of intracellular calcium and decreased release of NTs
increase postsynaptic opening of potassium - hyperpolarization

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13
Q

what is the mechanism of analgesia for opioids in the ascending pain pathways?

A

inhibition of afferent pain transmission
peripheral effects
dorsal horn - presynaptic blocking of pain mediating NTs and postsynaptic activation of secondary afferent neurons via increased potassium

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14
Q

opioids have what effect on NTs in the spinal cord? what is the result?

A

opioids activate GABA neurons in spinal cord

reduced activation of secondary afferent neurons

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15
Q

what is the mechanism of analgesia for opioids in the DESCENDING pain pathways?

A

blockage of inhibitory GABAergic interneurons

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16
Q

what are the sites of action for opioids in the descending pain pathways?

A

periaqueductal gray - midbrain
rostral ventral medulla - brainstem
locus coeruleus - pons

17
Q

what occurs as a result of increased pCO2 following opioid-induced respiratory depression? what is the clinical significance?

A

reflexive cerebral dilation

contraindication in head trauma

18
Q

what is the mechanism for opioid-induced cough suppression?

A

via brainstem chemoreceptor trigger zone (area postrema)

19
Q

what are the CV effects of opioids?

A

hypotension and bradycardia

20
Q

which drug class should be avoided in combination with opioid use? which opioid specifically should be avoided? why?

A

MAOI

meperidine

hyperpyrexic reaction including hypertension

21
Q

what are the opioid antagonists? what is their clinical use?

A

naloxone, naltrexone

opioid overdose

22
Q

what are the cough suppressant opioid agents?

A

codeine, dextromethorphan

23
Q

what is the role of diphenoxylate?

A

antidiarrheal

24
Q

what is the role of loperimide?

A

antidiarrheal

25
Q

morphine is an agonist at which receptors?

A

mu, kappa, delta

26
Q

hydromorphone is how many times more potent than morphine?

A

7-10x

27
Q

which opioid antagonist is the primary overdose agent that can reverse CNS and respiratory depression within 30 seconds?

A

naloxone (IV)

28
Q

which opioid antagonist is the primary maintenance drug in the treatment of addiction?

A

naltrexone

29
Q

how do opioids affect the reward pathway?

A

modify action of DA in nucleus accumbens and central/ventral tegmental areas

30
Q

what is the leading cause of opiate dependence and abuse?

A

euphoria

31
Q

what agent is the primary pharmacologic intervention used to treat opioid addiction? what is the strategy?

A

methadone

tapering effect

Year 2 Pharmacology (70 decks)

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