Measured Context-sensitive Half-times of Remifentanil and Alfentanil

Kapila, Atul; Glass, Peter S. A.; Jacobs, Joachim; Muir, Keith T.; Hermann, David; Shiraishi, Masa; Howell, Scott; Smith, Richard L.

doi:10.1097/00000542-199511000-00009

Cited by 370 publications

(109 citation statements)

References 8 publications

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“…The context-sensitive half-time of remifentanil is constant and independent of duration of drug administration when administered for up to 6 hours [3], but does this situation change when remifentanil is given for days rather than hours? One study looked at the pharmacodynamic offset of remifentanil at various time points over 3 days in ICU patients and found that the offset time was constant over this period [5].…”

Section: Discussionmentioning

confidence: 99%

“…Remifentanil is metabolised by non-specific plasma esterases and is therefore independent of organ function [2]. Remifentanil is rapidly metabolised and has a context-sensitive half-time of about 2 to 3 min that is independent of duration of infusion [3]. These features of remifentanil make it an ideal agent for use in critically ill patients.…”

Section: Introductionmentioning

confidence: 99%

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Section: Discussionmentioning

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Section: Introductionmentioning

confidence: 99%

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et al. 2005

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“…The reason for the short duration of effect is the redistribution of thiopental from highly perfused tissues, particularly the CNS, to other tissues [258]. Clinical studies with anesthetic drugs revealed that the elimination half-life often failed to predict the loss of anesthetic effect (recovery from anesthesia) [259,260]. For example, the half-life of loss of anesthetic effect was 5 and 50 min for remifentanil and alfentanil, respectively, while the corresponding elimination half-lives were 20 and 110 min [259].…”

Section: Pharmacokinetic Half-life Vs Pharmacologic Halflifementioning

confidence: 99%

“…Clinical studies with anesthetic drugs revealed that the elimination half-life often failed to predict the loss of anesthetic effect (recovery from anesthesia) [259,260]. For example, the half-life of loss of anesthetic effect was 5 and 50 min for remifentanil and alfentanil, respectively, while the corresponding elimination half-lives were 20 and 110 min [259]. Sufentanil, with an elimination half-life of 577 min, had a shorter half-life of anesthetic recovery compared to alfentanil, whose half-life of loss anesthesia was 50 min.…”

Section: Pharmacokinetic Half-life Vs Pharmacologic Halflifementioning

confidence: 99%

Tissue Distribution and Pharmacodynamics: A Complicated Relationship

Lin¹

2006

CDM

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With few exceptions, drugs exert their effects not within the plasma compartment, but in the defined target tissues. The process of drug distribution to the active site constitutes the "link-bridge" of the pharmacokinetic/pharmacodynamic (PK/PD) relationship. In spite of the importance of drug distribution as a key factor in determining pharmacologic response, research on drug distribution has historically received much less attention than that of absorption, metabolism, and excretion. The negligence of research on drug distribution is due mainly to the inaccessibility of the target tissues for obvious ethical reasons. In addition, lack of reliable experimental tools to assess the distribution process is also a major contributing factor. Because of this negligence, drug distribution has been referred to as "the forgotten relative in clinical pharmacokinetics." Although recent advances in molecular biology have led to the identification of many drug transporters, many of the processes of drug distribution are still not fully understood. The primary aim of this article is to provide new insight into the mechanisms of drug distribution, with an attempt to describe the relationship between the drug distribution and pharmacologic response. In addition, the factors that affect the processes of drug distribution will also be reviewed. Also, validity of some key assumptions that are used to relate the processes of tissue distribution with pharmacologic activity will be discussed.

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“…All opioids depress the central nervous, respiratory and cardiovascular system (particularly meperidine), and they increase the intrabiliary pressure, decrease gastric motility and cause nausea/vomiting and constipation. Though sufentanil, alfentanil and remifentanil are superior to fentanyl, fentanyl is a good choice with the less cost [8,9]. …”

Section: Opioidsmentioning

confidence: 99%

Pharmacology of Sedation Agents and Reversal Agents

Fassoulaki

Theodoraki

Melemeni³

2010

Digestion

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Sedation for gastrointestinal endoscopies is obtained by opioids, benzodiazepines, propofol, ketamine and/or droperidol. The pharmacokinetic profile of some sedatives/anesthetics renders them advantageous over others. Opioids, mainly pethidine and fentanyl, are the most popular. Though newer opioids provide a faster recovery, fentanyl is safe and advantageous due to its lower cost. Remifentanil, due to its pharmacokinetic profile (elimination half-life: 9 min), is advantageous for ambulatory patients, though it is not known whether the high cost compensates the benefits. Midazolam is the benzodiazepine of choice as it has a shorter duration of action and a better pharmacokinetic profile than diazepam. Propofol, an intravenous anesthetic, has become very popular for gastrointestinal endoscopies in sedative doses. The opioid and benzodiazepine antagonists, naloxone and flumazenil, are indicated only in particular circumstances, like deep sedation with threatening respiratory depression. Ketamine and droperidol are not popular agents for sedation in the modern endoscopic practice.

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Measured Context-sensitive Half-times of Remifentanil and Alfentanil

Cited by 370 publications

References 8 publications

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Tissue Distribution and Pharmacodynamics: A Complicated Relationship

Pharmacology of Sedation Agents and Reversal Agents

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