Respiratory Effects of Biased Ligand Oliceridine in Older Volunteers: A Pharmacokinetic–Pharmacodynamic Comparison with Morphine
Authors' conclusion
Oliceridine and morphine differ in their respiratory pharmacodynamics with a more rapid onset and offset of respiratory depression for oliceridine and a smaller magnitude of respiratory depression over time.
Study context
- Population
- Healthy male and female volunteers aged 55 to 89 yrcrossover, four occasions
- Participants
- 18 participants
- Comparison
- IV oliceridine 0.5 or 2 mg vs morphine 2 or 8 mg
- Primary endpoint
- V̇E55 (population pharmacokinetic-pharmacodynamic analysis)
Methodological detailsfour-arm, double-blind, crossover, population pharmacokinetic-pharmacodynamic analysis
- Four-arm
- Double-blind
- Crossover
- Population pharmacokinetic-pharmacodynamic analysis
Primary result
As reported in the abstract
Effect-site concentration causing 50% depression of V̇E55, oliceridine (median ± SE of estimate)
29.9 ± 3.5 ng/ml
Effect-site concentration causing 50% depression of V̇E55, morphine (median ± SE of estimate)
21.5 ± 4.6 ng/ml
Blood effect-site equilibration half-life, oliceridine
44.3 ± 6.1 min
Blood effect-site equilibration half-life, morphine
214 ± 27 min
Further findings
Oliceridine clearance in poor CYP2D6 metabolizers (subgroup)
- Three poor CYP2D6 metabolizers: significant difference in oliceridine clearance by about 50%, higher plasma concentrations after low- and high-dose oliceridine vs other participants
Original publication
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