Critical Care >Analgesia, Sedation, and Neuromuscular Blockade

John M. Oropello, Stephen M. Pastores, Vladimir Kvetan+

Table 16–2bOpioid analgesics (adapted from Joffe et al6).

Opioid Elimination Half-Life Metabolic Pathway Active Metabolites Notes

Histamine release may be important

Morphine 1.5-2 h Liver: glucuronidation Morphine 6- and 3-glucuronide from a cardiovascular and pulmonary
perspective. Caution in renal failure.

Accumulation with hepatic

Hydromorphone 2-3 h Liver: glucuronidation None
dysfunction.

Significant increase in context-

Fentanyl 3-4 h Liver: N-dealkylation CYP3A4/5 None sensitive half-time with infusions >12
h.

Remifentanil 10-20 min Plasma esterase hydrolysis None Abrupt discontinuation of analgesia.

Oxycodone 3-4 h Liver: CYP2D6 Noroxycodone and oxymorphone

NMDA receptor-antagonist,
unpredictable pharmacokinetics (risk
Methadone 8-59 h Liver: N-methylation CYP3A4, 2D6 none
for accumulation). Multiple drug–drug
interactions. Can prolong QTc.

NMDA, N-methyl-D-aspartate.

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