Opioid Analgesics Flashcards
1
Q
Strong Agonists (6)
A
- Morphine
- Hydromorphone
- Methadone
- Meperidine
- Fentanyl
- Levophanol
(MMM FHL)
2
Q
Mild/Moderate Agonists (5)
A
- Codeine
- Oxycodone
- Hydrocodone
- Diphenoxylate/Loperamide
- Tramadol
(HD COT)
3
Q
Mixed or Partial Agonists (4)
A
- Pentazocine
- Nalbuphine
- Butorphanol
- Buprenorphine
(BBNP)
4
Q
Antagonists
A
-Naloxone
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
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
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)
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
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
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)
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
12
Q
Oxycodone:
2 important things
A
- Less hallucinations than morphine
- Combined with acetaminophen (percocet) or aspiran (percodan)
13
Q
Hydrocodone:
2 important things
A
- Antitussive
- Combined with acetaminophen (Vicodin)
- Onset 10-20 minutes, duration 3-6 hours
14
Q
Diphenoxylate/Loperamide:
3 important things
A
- Single dose: no morphine effect
- High dose: euphoria, suppression of morphine abstinence
- Only use: diarrhea
15
Q
Tramadol:
3 important things
A
- Analgesic activity through Mu receptor
- Prodrug
- Increases serotonin activity (causes serotonin syndrome)
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
3 advantages to patient controlled analgesia
- Less delay between patient's request for relief
- Better pain control using less opioid
- Minimizes peaks and valleys in plasma
26
Tolerance in opioids
| 4 things
- 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
Psychological dependence
| 3 things
- Pronounced craving for drug
- Can persist for months after withdrawal is over
- Promoted by euphoria and sedation
28
Tapentadol
| 4 things
- Moderate to severe acute pain
- MOA: binds mu and inhibits NE reuptake
- Less GI than opioids
- More expensive
