Remifentanil (Ultiva) was designed as a “soft drug.” Softdrugs are designed to undergo metabolism quickly and thushave ultrashort durations of action. In place of the ethylaromatic ring seen on the other piperidine opioids, remifentanilhas an ester group. This ester group is metabolizedby esterases in the blood and tissue to a weaklyactive metabolite (1:300–1:1,000 the potency of remifentanil). The n-octanol/water partition coefficient ofremifentanil is 17.9. The pKa of remifentanil is 7.07, thus itis predominately unionized at physiological pH. Both ofthese properties account for its rapid distribution across theblood-brain barrier (<1 minute). The ester hydrolysis leadsto a quick recovery (5–10 minutes) independent of durationof drug administration, renal, or liver function. The favorablepharmacodynamics of remifentanil have led to its usefor induction and maintenance of surgical anesthesia.
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