Author(s): Beers R, Camporesi E
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Abstract The anilidopiperidine opioid remifentanil has pharmacodynamic properties similar to all opioids; however, its pharmacokinetic characteristics are unique. Favourable pharmacokinetic properties, minimally altered by extremes of age or renal or hepatic dysfunction, enable easy titration and rapid dissipation of clinical effect of this agent, even after prolonged infusion. Remifentanil is metabolised by esterases that are widespread throughout the plasma, red blood cells, and interstitial tissues, whereas other anilidopiperidine opioids (e.g. fentanyl, alfentanil and sufentanil) depend upon hepatic biotransformation and renal excretion for elimination. Consequently, remifentanil is cleared considerably more rapidly than other anilidopiperidine opioids. In addition, its pKa (the pH at which the drug is 50\% ionised) is less than physiological pH; thus, remifentanil circulates primarily in the non-ionised moiety, which quickly penetrates the lipid blood-brain barrier and rapidly equilibrates across the plasma/effect site interface. By virtue of these distinctive pharmacokinetic properties, the context-sensitive half-time (i.e. the time required for the drug's plasma concentration to decrease by 50\% after cessation of an infusion) of remifentanil remains consistently short (3.2 minutes), even following an infusion of long duration (> or =8 hours). Remifentanil, a clinically versatile opioid, is useful for intravenous analgesia and sedation in spontaneously breathing patients undergoing painful procedures. Profound analgesia may be achieved with minimal effect on cognitive function. Remifentanil may also provide sedation and analgesia during placement of regional anaesthetic blocks, and in conjunction with topical anaesthesia and airway nerve blocks, it may be useful for blunting reflex responses and facilitating 'awake' fibreoptic intubation. Compared with fentanyl and alfentanil in a day-surgery setting, remifentanil supplementation of general anaesthesia may improve intraoperative haemodynamic control. Both emergence time and the incidence of respiratory depression during post-anaesthetic recovery may be reduced. However, outcomes such as home discharge time, post-emergence adverse effect profile, and patient and provider satisfaction are not significantly improved, and the incidence of intraoperative hypotension and bradycardia is greater. In addition, drug acquisition costs for remifentanil are higher and clinicians may need extra time to familiarise themselves with the drug's unique pharmacokinetics.Ironically, the quick dissipation of opioid analgesic effect following remifentanil discontinuation may be a significant clinical disadvantage. Unless little or no postoperative pain is anticipated, the clinician may wish to treat prospectively using local or regional anaesthesia, non-opioid analgesics, or longer-acting opioid analgesics.
This article was published in CNS Drugs
and referenced in Journal of Microbial & Biochemical Technology