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
-Tapentadol (more potent cousin)
This drug is metabolized by 2D6 to become morphine and has increasing toxicity in ultra-rapid metabolizers
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 = ?
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?
Which drugs are first-line for severe pain?
Which drugs are first-line for mild-moderate pain?
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
This drug has a short half-life and may cause less pruritus and nausea than morphine
Which Strong Agonists are available in IV formulations?
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?
What are the phenanthrenes?
What opioid falls in the phenylheptylamines family?
When two meds fall in the phenylpiperidines family?
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?
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 ?
What are the two u-AG/SNRIs?
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?
What are the CI of tramadol?
Hx of seizures, stroke, head trauma, ETOH withdrawal
This opioid is similar to tramdadol but stronger. Comparable to Oxycodone 10-15mg. ADR is seizures.
What four opioids are mixed AG/AAG?
What 3 opioids have incomplete reversal with Naloxone, leading to an increased risk of harm?
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.
What drug should you give to reverse an opioid overdose?