Opioid Analgesics I-II Flashcards

1
Q

Name 2 methadone family (phenyheptamines) agonists. What receptor do they act on?

A
  1. methadone and relatives
  2. propoxyphene (Darvon)
  • *** all are μ-receptor agonists
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2
Q

Where in the body does opioid tolerance NOT occur?

A
  • in the GI tract
  • eyes (miosis)
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3
Q

Name the endogenous opioid class:

  • short acting; not systemic
  • released at synapses (NTs)
  • derived from pro-enkephalins
  • brain and spinal cord
A

enkephalins

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4
Q

What is the tx for opioid OD?

A
  • naloxone (Narcan)
  • Naltrexone (Revia)
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5
Q

Name the an endogenous opioid class:

  • new family
  • μ-receptor selective
A

endomorphins

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6
Q

What is dependence?

A

the psych need to use the drug to maintain homeostasis and prevent withdrawal effects

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7
Q

When are opiates contraindicated?

A
  • respiratory problems of any kind
  • head injury
  • HTN
  • shock
  • excessive histamine release
  • hypothyroidism
  • hepatic dysfunction
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8
Q

Name the endogenous opioid class:

  • larger
  • NTs and neurohormones
  • derived from POMC
  • hypothalamus and pituitary (stress)
A

endorphins

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9
Q

What is an endorphin?

A
  • an endogenous opioid class
  • larger
  • NTs and neurohormones
  • derived from POMC
  • hypothalamus and pituitary (stress)
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10
Q

How are opioids used as cough suppressants?

A

they inhibit the cough center of medulla

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11
Q

When are opiates indicated?

A
  • relief of moderate to severe pain (malignancy, post-op, obstetrics)
  • cough
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12
Q

What is a dynorphin?

A
  • an endogenous opioid class
  • unk role
  • derived from prodynorphin
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13
Q

Name 3 meperidine and other phenypiperdine agonists. What receptor do they act on?

A
  1. meperidine (Demerol)
  2. loperimide (Imodium)
  3. fentanyl and relatives
  • *** all are μ-receptor agonists
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14
Q

Name the 4 classes of endogenous opioids.

A
  1. enkephalins
  2. endorphins
  3. dynomorphins
  4. endomorphins
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15
Q

What is the effect of opioid binding in the chemorecptor trigger zone (CTZ)?

A

nausea/vomiting (except overdose levels)

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16
Q

What is the life-threatening SE of opioids?

A

respiratory depression

17
Q

Name the endogenous opioid class:

  • unk role
  • derived from prodynorphin
A

dynorphins

18
Q

Name 8 opioid phenanthrene agonists. What receptor do they act upon?

A
  1. Morphine
  2. Heroin
  3. Codeine
  4. Hydromorphone (Dilaudid)
  5. Oxymorphon
  6. Oxycodone (oxycontin, Percocet)
  7. Hydrocodone (Vicodin)
  8. Tramadol (ultram)- also blocks MAO uptake
  • *** μ-receptor agonists
19
Q

What are the 3 receptors that opioids can bind to? How often are they used as drug targets? What kind of receptors are they?

A
  1. μ (most),
  2. δ (no drugs avail)
  3. κ (some)
  • all are GTP receptor types (Gi and Go)
20
Q

Why do opioids cause miosis?

A

they excite the Edinger-Westfall nucleus

21
Q

What is tolerance?

A
  • prior dose doesn’t produce same effects
  • increased dose needed to produce same effects
22
Q

How do opioids cause respiratory depression?

A

they bind to brainstem nuclei –> decrease sensitivity of CO2

23
Q

What 3 other drugs can opioids interact with? What is the effect?

A
  1. Barbs (additive)
  2. Phenothiazines (antipsychotics- can increase SEs)
  3. MAOIs/tricyclic antidepressants (increase SEs, cause excitation, delirium, SZs)
24
Q

What is an endomorphin?

A
  • an endogenous opioid class
  • new family
  • μ-receptor selective
25
Q

What is an enkephalin?

A
  • an endogenous opioid class
  • short acting - not systemic
  • released at synapses (NTs)
  • derived from pro-enkephalins
  • brain and spinal cord
26
Q

Name 2 opioid antagonists. What are they used for?

A
  1. Naloxone (Narcan)
  2. Naltrexone (Revia)
  • *** these reverse opioid OD
27
Q

What is the effect of opioid binding in the GI tract?

A
  • binds at smooth muscle –> constipation, spasm
  • biliary spasm/pain/pressure –> stones
  • bind at ureters/bladder –> increase tone and contraction
28
Q

Name 4 mixed opioid agonists/antagonists and partial agonists. What receptor do they act upon?

A
  1. buprenorphine (*** partial μ-receptor agonist)
  2. pentazocine (k agonist, μ antagonist)
  3. butorphanol (k agonist)
  4. nalbuphine (k agonist, μ antagonist)