Acute Pain & OFA pt3 Flashcards
(44 cards)
What drug is fentanyl structurally similar to?
Meperidine
Fentanyl has ____ potency, ____ onset of action and _____ duration of action.
High potency
Rapid onset
Short duration
What is the priniciple metabolite of fentanyl?
Norfentanyl
Detectable in urine up to 72 hours after single dose.
Why is elimination of fentanyl slightly prolonged despite very short duration of action?
Lungs serve as large inactive reservoir (up to 75% of initial dose undergoes first pass pulmonary uptake).
Why is fentanyl more potent and rapid than morphine?
Greater lipid solubility
What is responsible for fentanyl’s short duration of action?
Rapid redistribution to fat and muscle
What is the protein binding of fentanyl?
84%
What is hydromorphone and how is it formed?
Hydrogenated ketone of morphine formed by N-demethylation of hydrocodone
Hydromorphone is ______ times as potent as morphine when administered orally.
3 - 5 times
Hydromorphone is ______ times as potent as morphine when administered parenterally.
8.5 times
What is hydromorphone’s primary metabolite?
Hydromorphone-3-glucuronide
What should be known about Hydromorphone-3-glucuronide?
- Lacks analgesic effects
- May potentiate neurotoxic effects (allodynia, myoclonus, seizures).
When is Hydromorphone-3-glucuronide’s neurotoxic side effects a significant concern?
Patients with renal insufficiency
What is the typical dose of parenteral Hydromorphone?
0.2 - 2 mg
What is the typical oral dose of hydromorphone?
2 - 8 mg
What is the duration of action of hydromorphone?
3 - 4 hours
What is hydrocodone derived from?
Codeine
How does the potency of hydrocodone and codeine compare?
Hydrocodone is 6 - 8 x more potent than codeine
What are the two most abused opioids?
1st = Oxycodone
2ⁿᵈ = Hydrocodone
What are the two metabolites of hydrocodone metabolism?
- Hydromorphone (via CYP2D6)
- Norhydrocodone (inactive) via CYP3A4
What is the morphine equivalent of hydrocodone?
1 mg morphine = 3 mg hydrocodone
What is typical hydrocodone dosing?
2.5 - 10mg w/ 300 - 750mg acetaminophen q4-6hours
consider max dose of acetaminophen
What receptors does buprenorphine have affinity to? (3)
μ - partial agonist (strong)
κ - antagonist (strong)
δ - agonist (weak)
What benefits does buprenorphine provide? (4)
- ↓ respiratory depression
- ↓ immune suppression
- ↓ constipation
- No accumulation in renal patients