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xPharm Exam 1 > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

Strong Agonists (6)

A
  • Morphine
  • Hydromorphone
  • Methadone
  • Meperidine
  • Fentanyl
  • Levophanol

(MMM FHL)

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2
Q

Mild/Moderate Agonists (5)

A
  • Codeine
  • Oxycodone
  • Hydrocodone
  • Diphenoxylate/Loperamide
  • Tramadol

(HD COT)

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3
Q

Mixed or Partial Agonists (4)

A
  • Pentazocine
  • Nalbuphine
  • Butorphanol
  • Buprenorphine

(BBNP)

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4
Q

Antagonists

A

-Naloxone

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5
Q

Morphine:
2 important things
4 Advantages
4 Disadvantages

A
  • Opioid Gold Standard
  • 2 metabolites: M-3-G and M-6-G (more active)

Advantages:

  • no ceiling effect for analgesia
  • sedation >30 min during procedures
  • multiple dosage forms
  • least expensive

Disadvantages:

  • histamine release (wheezing, hypotension)
  • poor oral bioavailability
  • respiratory depression
  • pruritis
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6
Q

Hydromorphone:

4 important things

A
  • Most common opioid in suppository form
  • Available as injection, oral solids and liquids, powder and suppository
  • Extensive 1st pass effect
  • Extended release tablets for extended pain control
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7
Q

Methadone:

3 important things

A
  • Gold standard for opioid withdrawal
  • More potent than morphine
  • May cause cardiac effects (QT prolongation & Torsades de Pointe)
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8
Q

Meperidine:

3 important things

A
  • Short DOA (less than 3 hours)
  • Painful IM administration
  • Toxic metabolite (normerperidine) causes CNS excitation with tremors, twitching, seizure
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9
Q

Fentanyl:

5 important things

A
  • 100x more potent than morphine (shorter DOA)
  • Rigid chest phenomenon
  • Alfentanyl: immediate onset, histamine release
  • Sufentanyl, Remifentanyl: 1-3 min onset
  • Available as IV, patch, lozenge
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10
Q

Levorphanol:

3 important things

A
  • Longer DOA and t1/2 than morphine
  • Dextromethorphan: D Isomer of levorphanol (NMDA agonist, doesn’t act on opioid receptors)
  • Antitussive (the DM in drugs)
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11
Q

Codeine:

5 important things

A
  • Do NOT give IV (hypotension)
  • Prodrug (metabolized by CYP2D6 to morphine)
  • Most constipating opioid
  • Antitussive
  • Onset 30-60 minutes, duration 4-6 hours
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12
Q

Oxycodone:

2 important things

A
  • Less hallucinations than morphine

- Combined with acetaminophen (percocet) or aspiran (percodan)

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13
Q

Hydrocodone:

2 important things

A
  • Antitussive
  • Combined with acetaminophen (Vicodin)
  • Onset 10-20 minutes, duration 3-6 hours
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14
Q

Diphenoxylate/Loperamide:

3 important things

A
  • Single dose: no morphine effect
  • High dose: euphoria, suppression of morphine abstinence
  • Only use: diarrhea
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15
Q

Tramadol:

3 important things

A
  • Analgesic activity through Mu receptor
  • Prodrug
  • Increases serotonin activity (causes serotonin syndrome)
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16
Q

Pentazocine:

3 important things

A
  • Mixed: kappa receptor agonist (Mu receptor antagonist)
  • Less biliary sphincter activity
  • Large doses are dysphoric and psychomimetic
17
Q

Nalbuphine:

5 important things

A
  • Mixed antagonist and agonist
  • Structurally related to naloxone and oxymorphone
  • Ceiling effect
  • Abstinence syndrome (use <7 days): headache, hallucination, irritability
  • No increase in cardiac work, BP, pulmonary or arterial pressure
18
Q

Butorphanol:

4 important things

A
  • Nasal spray for migraine
  • For acute pain
  • Caution in heart disease and elderly
  • Ceiling effect for respiratory depression
19
Q

Buprenorphine:

4 important things

A
  • Maintenance agent for opioid dependents
  • Prototype of partial agonists
  • 25-50x more potent and longer DOA than morphine
  • Can be paired with naloxone to avoid respiratory depression
20
Q

Naloxone:

6 important things

A
  • Must be given IV (1st pass effect)
  • For opioid induced pruritis
  • Acts on all opioid receptor sites
  • Overshoot phenomenon: arrythmias
  • Does not relieve pain
  • DOA is only 20-60 minutes so additional doses often needed
21
Q

What do opioids do?

6 things

A
  • Activate descending CNS tracts
  • Sedation
  • Analgesia (no amnesia)
  • Moderate anxiolysis
  • Euphoria
  • Cough suppression
22
Q

4 factors influencing the selection of opioids

A
  • Pain intensity
  • Pharmacokinetic considerations
  • Previous adverse effects
  • Presence of coexisting disease
23
Q

9 adverse effects of opioids

A
  • Respiratory depression
  • Miosis
  • Truncal rigidity
  • Nausea
  • Vomiting
  • Constipation
  • Sedation
  • Biliary constriction
  • Histamine release
24
Q

Overdose of opioids

3 things

A
  • Coma
  • Pinpoint pupils
  • Respiratory depression
25
Q

3 advantages to patient controlled analgesia

A
  • Less delay between patient’s request for relief
  • Better pain control using less opioid
  • Minimizes peaks and valleys in plasma
26
Q

Tolerance in opioids

4 things

A
  • A physiologic dependence
  • Occurs with large doses and short intervals or 2-3 weeks at regular doses
  • The longer the half life, the longer it takes to develop tolerance
  • Can lead to withdrawal or abstinence syndrome
27
Q

Psychological dependence

3 things

A
  • Pronounced craving for drug
  • Can persist for months after withdrawal is over
  • Promoted by euphoria and sedation
28
Q

Tapentadol

4 things

A
  • Moderate to severe acute pain
  • MOA: binds mu and inhibits NE reuptake
  • Less GI than opioids
  • More expensive

xPharm Exam 1 (7 decks)

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