Opioid Basics Flashcards
Mild to moderate agonists
- Phenanthrenes –> Codeine; codeine + APAP, Hydrocodone
- Phenylpiperidines –> Diphenoxylate, Loperamide
Strong Agonists (All C-II)
- Phenanthrenes –> Morphine, oxycodone, oxymorphone, hydromorphone
- Phenylheptylamines/diphenylheptanes –> methadone
- Phenylpiperidines –> Meperidine, fentanyl
“Weak” Mu-agonist/SNRI
- Tramadol*
- Tapentadol (more potent cousin)
Mixed Agonist/Antagonist
- Nalbuphine
- Butophanol (C-IV)
- Pentazocine (C-IV)
- Buprenorphine** (C-III)
This drug is metabolized by 2D6 to become morphine and has increasing toxicity in ultra-rapid metabolizers
-Codeine
What are the ADR’s of codeine to be aware of?
- BBW in peds d/t unpredictability
- Non-immune hypersensitivity: N/V, pruritus, hives
(same reactions seen with morphine)
Codeine + APAP = ?
Hydrocodone + APAP = ?
- Tylenol
- Vicodin
What enzyme is hydrocodone metabolized by? What is it metabolized to?
Hydrocodone –> 2D6 –> Hydromorphone
-Hydromorphone is more potent
What drug is first-line for severe pain and used in pediatrics due to its predictable response?
Morphine
Which drugs are first-line for severe pain?
Morphine
Oxycodone
Hydromorphone
Which drugs are first-line for mild-moderate pain?
- tramadol
- hydrocodone
This drug is the active metabolite of oxycodone
Oxymorphone (not used much)
This drug is a substrate of 3A4 and has a black-box warning regarding use with 3A4 inhibitors
Oxycodone (OxyContin)
This drug has a short half-life and may cause less pruritus and nausea than morphine
Hydromorphone
Which Strong Agonists are available in IV formulations?
- Morphine
- Oxymorphone
- Hydromorphone
- Methadone
- Meperidine
Which strong agonist has a long half-life, needs careful titration, has no active metabolites, and ADRs include QT prolongation and an increased risk of respiratory depression?
Methadone
What are the phenanthrenes?
Morphine
Oxycodone
Oxymorphone
Hydromorphone
What opioid falls in the phenylheptylamines family?
Methadone
When two meds fall in the phenylpiperidines family?
Meperidine
Fentanyl
This strong agonist is a potent 5-HT stimulator. It is ONLY for short-term acute pain, there is death associated with MAOI, and IM injectino can lead to muscle fibrosis. What am I?
Meperidine
I am second line for severe pain and should not be used in opioid naive patients. I am contraindicated with clarithromycin. If combined with a sertonin drug, there is risk of Serotonin Syndrome. I am a transdermal patch. What am ?
Fentanyl
What are the two u-AG/SNRIs?
Tramdadol
Tapentadol
This drug is first line for mild-mod pain. It is metabolized by 2D6 into active metabolite. CI includes history of seizures, stroke, head trauma, ETOH withdrawal, and clarithromycin. This sohuld be avoided in peds. What is it?
Tramadol
What are the CI of tramadol?
Hx of seizures, stroke, head trauma, ETOH withdrawal
Clarithromycin
This opioid is similar to tramdadol but stronger. Comparable to Oxycodone 10-15mg. ADR is seizures.
Tapentadol
What four opioids are mixed AG/AAG?
Nalbuphine
Butorphanol
Pentazocine
Buprenorphine
What 3 opioids have incomplete reversal with Naloxone, leading to an increased risk of harm?
Nalbuphine
Butorphanol
Pentazocine
This opioid binds with high affinity and slowly dissociates from u receptors. It acts as an AAG. It’s a substrate of 3A4 and is CI with clarithromycin. It has a lower abuse potential and has fewer withdrawal symptoms.
Buprenorphine
What drug should you give to reverse an opioid overdose?
Naloxone
