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OU PharmCare Fall 2017 > Test 2 Narcotic Analgesics > Flashcards

Test 2 Narcotic Analgesics Flashcards

1
Q

Endogenous Opioid peptide families

A
  • Prepro-opiomelanocortin
  • Preproenkephalin
  • Preprodynorphin
  • Prepronociceptin
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2
Q

Endogenous Opioid peptides

A
  • Leu-enkephalin
  • Dynorpin A
  • Met-enkephalin
  • Beta-endorphin
  • Nociceptin
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3
Q

Opioid Receptor Subtypes

A
  • MOP (µ)
  • KOP (κ)
  • DOP (δ)
  • NOP = Nociceptin/Orphanin FQ peptide receptor
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4
Q

What is the most dangerous effect of opiates?

A

respiratory depression

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5
Q

Opioid Overdose Triad

A
  • coma
  • respiratory depression
  • miosis (dose dependent, no tolerance, marker of opioid use)
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6
Q

Common Opioid Adverse Effects

A
  • N/V
  • euphoria
  • constipation
  • sedation
  • orthostatic hypotension
  • bradycardia
  • fainting
  • sensitivity reactions
  • biliary spasm
  • urinary retention
  • hyperalgesia
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7
Q

define endogenous opioids

A

molecules found in the brain that produce their actions through one of the four opioid receptor subtypes

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8
Q

What are the types of MOA of opioid analgesics?

A
  • indirectly inhibiting tonic release of GABA
  • directly inhibiting release of neurotransmitters
  • bind to mu receptors
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9
Q

MOA: indirectly inhibiting tonic release of GABA

A
  • inhibits descending analgesic pathway
  • GABA is a brake that is always on the descending analgesic pathway
  • removing the brake = mu opioids allow the descending analgesic pathway to work; also activates the release of NE and 5HT
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10
Q

MOA: directly inhibiting release of neurotransmitters

A
  • ex. Substance P, glutamate, CGRP which activate ascending pain pathways at the level of the spinal cord
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11
Q

MOA: bind to mu receptors

A
  • this alters the perception of pain
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12
Q

limitations to naloxone

A
  • short acting

- less potent than fentanyl and carfentanil

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13
Q

Analgesic Tolerance

A

Decrease in amount of pain relief over time with a given dose

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14
Q

Physical Dependence

A

presence of withdrawal symptoms when drug is stopped or antagonist added

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15
Q

symptoms of withdrawals

A
  • diarrhea
  • dilated pupils
  • anxiety
  • hyperventilation
  • N/V
  • fevers / chills
  • increased BP, HR
  • muscle aches
  • appetite loss
  • watery eyes
  • runny nose
  • restlessness / hostility
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16
Q

Psychological Dependence / Addiction

A

Characterized by drug-seeking behavior in addition to withdrawal syndrome

17
Q

Which drug(s) have these drug-specific adverse effects: ↓ seizure threshold

A
  • meperidine metabolite: normeperidine

- morphine metabolite: M3G

18
Q

Which drug(s) have these drug-specific adverse effects: precipitate opioid withdrawal in opioid-dependent patient

A
  • buprenorphine
  • pentazocine
  • butorphanol
  • nalbuphine
  • naloxone
  • naltrexone
19
Q

Which drug(s) have these drug-specific adverse effects: prolonged Q-T intervals

A

methadone

20
Q

Which drug(s) have these drug-specific adverse effects: tendency to produce dysphoria

A
  • pentazocine
  • butorphanol
  • nalbuphine
21
Q

Which drug(s) have these drug-specific adverse effects: diuresis

A
  • butorphanol

- nalbuphine

22
Q

How different metabolizer phenotypes alter efficacy and adverse effect potential of tramadol.

A
  • poor / intermediate metabolizers: will not be converted to active compounds
23
Q

How different metabolizer phenotypes alter efficacy and adverse effect potential of codeine.

A
  • Pro-drug: 5-10% bio-transformed by CYP2D6 to morphine and M6G; 80% to C6G
  • poor / intermediate metabolizers: will not be converted to active compounds
  • ultra rapid metabolizers: pro-drug will be metabolized quickly to produce toxicity
24
Q

genetic variability of metabolizers

A
  • Poor metabolizers: limited or inactive enzyme
  • Intermediate metabolizers: partially deficient
  • Extensive metabolizers: considered normal
  • Ultra rapid metabolizers: excess activity
25
Q

morphine metabolism

A
  • by UGT
  • 90% to M3G (non-opioid)
  • 10% to M6G (active opioid; more potent than morphine

OU PharmCare Fall 2017 (22 decks)

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