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Drug development in anaesthesia: the remifentanil
1Metabolic, Cardiovascular and Oncology, Therapeutic Development Group, Glaxo Wellcome, Greenford, UK.
Minerva Anestesiologica
|August 31, 2000
Summary
Remifentanil, a new anesthetic drug, offers rapid action and predictable recovery due to its unique esterase metabolism. This allows for precise control during anesthesia, benefiting both short and long procedures.
Area of Science:
- Anesthesiology
- Pharmacology
- Drug Development
Background:
- Anesthetic drug development faces unique challenges, requiring drugs to meet clinical goals without unacceptable toxicity.
- The trend towards short-acting anesthetic agents necessitates innovative drug design.
Purpose of the Study:
- To describe the development of remifentanil, a novel mu-opioid receptor agonist.
- To highlight how drug design can improve anesthetic practice, focusing on rapid and predictable offset of action.
Main Methods:
- Design of a 4-anilidopiperidine molecule with an alkyl ester group for targeted metabolism.
- Evaluation of remifentanil's pharmacokinetic and pharmacodynamic properties, including its susceptibility to non-specific esterase metabolism.
Main Results:
- Remifentanil retains desired mu-opioid receptor pharmacology while being rapidly metabolized by blood and tissue esterases.
- The drug exhibits rapid onset and offset of action, allowing for high-dose titration and stable anesthesia.
- Lack of accumulation ensures prompt recovery even after prolonged infusions.
Conclusions:
- Remifentanil's unique metabolism provides precise control over the anesthetic process.
- Its characteristics are valuable for both short and long surgical procedures.
- Potential future applications in intensive care settings are suggested.