Table 1.
Oxycodone [21, 22, 53–58] | Morphine [59–61] | Fentanyl [59, 61–63] | Sufentanil [64–67] | Pethidine [61, 68–70] | Hydromorphone [71, 72] | |
---|---|---|---|---|---|---|
Absorption | ||||||
T max | 6–25 min | 19 min | 4 min | 6 min | 1.2 min | 20 min |
Distribution | ||||||
Plasma protein binding | 45% | 35–36% | 84% | ~ 90% | ~ 58% | 8–19% |
VD | 2–3 l/kg | 1–4.7 l/kg | 4 l/kg | 1.7–5.2 l/kg | 3–5 l/kg | 302.9 l |
Metabolism | ||||||
Major metabolites | Noroxycodone, oxymorphone | Morphine-3-glucuronide | Norfentanyl | Norfentanyl | Norpethidine | Hydromorphone-3-glucuronide |
Excretion | ||||||
Cl | 1.10 l/min | 0.9–1.2 l/kg/h | 0.8–1.0 ml/min/kg | 57.6 l/h | 20.5 l/h | 1.96 l/min |
T1/2 | 2–3.5 h | 1.5–4.5 h | 3.7 h | 2.7 h | 2–5 h | 2.3 h |
Opioid receptor action | ||||||
μ | +++ | +++ | +++ | +++ | +++ | +++ |
κ | ++ | + | + | + | + | Nil |
δ | ++ | + | Nil | + | + | + |
Cl, clearance; Tmax, time to maximum plasma concentration; T1/2, half-life; VD, volume of distribution; μ, mu-opioid receptor; κ, kappa-opioid receptor; δ, delta-opioid receptor