Pharmacokinetics and Pharmacodynamics of Remifentanil

Minto, Charles F.; Schnider, Thomas W.; Shafer, Steven L.

doi:10.1097/00000542-199701000-00005

Cited by 583 publications

(297 citation statements)

References 12 publications

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“…Owing to the rapid breakdown of remifentanil in the blood and tissues, this half-life does not vary with the duration of infusion (Minto et al, 1997a, b). EEG measurements have yielded a context-sensitive half-life of 3-5 min (estimated at 3.7 min from the population model, for volunteers in this study) (Minto et al, 1997b), in agreement with our fMRI estimate from the insular cortex t 1/2W ¼ 3.07 min (1.09, 5.05 min: 95% confidence intervals), and from reported pain intensity t 1/2W ¼ 2.80 min (1.12, 4.48 min: 95% confidence intervals). Half-life measurements based on concentration data give 3.270.9 min (Kapila et al, 1995) and based on a pharmacodynamic measure of ventilation give 5.471.8 min (Kapila et al, 1995).…”

Section: Discussionmentioning

confidence: 86%

Using fMRI to Quantify the Time Dependence of Remifentanil Analgesia in the Human Brain

Wise

Williams

Tracey

2003

Neuropsychopharmacol

108

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To understand and exploit centrally acting drugs requires reliable measures of their time course of action in the human brain. Functional magnetic resonance imaging (fMRI) is able to measure noninvasively, drug-induced changes in task-related brain activity. Here, we have characterized, in a specific region of the brain, the time of onset of action and the half-life of action of a clinically relevant dose of a potent opioid analgesic agent, remifentanil. These times were established from the temporal variation of the amplitude of the blood oxygen level-dependent response in the insular cortex contralateral to a painfully hot thermal stimulus, in volunteers receiving a remifentanil infusion. The insular cortex has repeatedly been reported as activated by noxious thermal stimulation. The times of onset and offset of drug action were each characterized by a half-life for changes in fMRI signal from within the insula. These characteristic times agreed with the observed drug-induced analgesia and previous pharmacokinetic-pharmacodynamic measurements for remifentanil. We have successfully measured, for the first time using fMRI, temporal pharmacological parameters for a CNS-active drug based on its effect on task-related activity in a specific brain region. Comparison of the time course of regional brain activity with pain perception could reveal those regions engaged in drug-induced analgesia.

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Section: Discussionmentioning

confidence: 86%

Using fMRI to Quantify the Time Dependence of Remifentanil Analgesia in the Human Brain

Wise

Williams

Tracey

2003

Neuropsychopharmacol

108

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“…14 Anesthesia was induced with propofol 1.5 mgÁkg -1 and remifentanil (targeting a Ce of 1 ngÁmL -1 ). The Ce of remifentanil (using Minto's pharmacokinetic model) 15,16 was maintained with a commercial target-controlled infusion (TCI) system (Orchestra Ò Base Primea; Fresenius Vial, Brezins, France). After confirmation of adequate muscle relaxation with the administration of rocuronium 0.6 mgÁkg -1 iv, an endotracheal tube (ETT) with an internal diameter of 6.5 mm (female) or 7.5 mm (male) was inserted into the trachea.…”

Section: Methodsmentioning

confidence: 99%

Efficacy of a single dose of dexmedetomidine for cough suppression during anesthetic emergence: a randomized controlled trial

Lee

Choi

Kang

et al. 2014

Can J Anesth/J Can Anesth

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Purpose Maintenance of a remifentanil infusion during anesthetic emergence has been reported to decrease the incidence of coughing and thereby help to ensure a smooth emergence. It may, however, cause respiratory depression and possibly delay emergence. The purpose of this study was to investigate the effect of a single dose of dexmedetomidine combined with a low-dose remifentanil infusion on cough suppression during emergence from general anesthesia. Methods American Society of Anesthesiologists physical status I-II adults undergoing elective thyroidectomy under sevoflurane anesthesia were recruited and randomly allocated to receive either dexmedetomidine 0.5 lgÁkg -1 iv (Group D, n = 70) or saline (Group S, n = 71), each combined with a low-dose remifentanil infusion ten minutes before the end of surgery. Coughing was assessed using a four-point scale. The respiratory rate (RR), heart rate (HR), and mean arterial pressure were also recorded. Results The incidence of coughing was lower in Group D than in Group S (64% vs 91%, respectively; mean difference 27%; 95% confidence interval [CI] 13 to 41; P \ 0.001). The median cough grade at extubation was also lower in Group D. Mean arterial pressure and HR were elevated in Group S during tracheal extubation but were similar to baseline values in Group D. There was no difference in RR between the two groups throughout the study. A small delay in extubation was observed in Group D (3 minutes longer than Group S; 95% CI 2 to 4; P \ 0.001). Conclusion Compared with an infusion of low-dose remifentanil alone, the addition of a single dose (0.5 lgÁkg -1 ) of dexmedetomidine during emergence from sevofluraneremifentanil anesthesia was effective in attenuating coughing and hemodynamic changes and did not exacerbate respiratory depression after thyroid surgery. This trial was registered at Clinicaltrial.gov, identifier: NCT01774305. RésuméObjectif Il a été rapporté que le maintien d'une perfusion de remifentanil pendant l'émergence anesthésique diminuait This study was presented as a scientific poster at the

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“…A target-controlled infusion of remifentanil (concentration 20 mg.ml ¹1 ) was started at an initial target plasma concentration (C T ) of 1.6 ng.ml ¹1 and anaesthesia was induced with a target-controlled infusion of 1% propofol. A Graseby 3400 intravenous infusion pump linked to a microprocessor programmed with pooled pharmacokinetic data for remifentanil [4] and a Diprifusor Graseby 3500 were used to provide the target-controlled infusions for remifentanil and propofol, respectively. A laryngeal mask was inserted, and ventilation was assisted manually as required until spontaneous respiration resumed.…”

Section: Methodsmentioning

confidence: 99%

Target‐controlled remifentanil in combination with propofol for spontaneously breathing day‐case patients

1999

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SummaryRemifentanil is a new potent opioid with a very short duration of action irrespective of duration of infusion. It may have a role in day-case anaesthesia as part of a balanced total intravenous anaesthetic technique with propofol. We examined the respiratory depressant effects of remifentanil in 20 patients undergoing day-case anaesthesia. The target plasma concentration of remifentanil was varied while maintaining a constant target-controlled infusion of 4.5 mg.ml ¹1 propofol. In only 12 patients was satisfactory spontaneous respiration maintained. In these patients the median remifentanil target concentration was 1.6 ng.ml ¹1 and was achieved with a median infusion rate of 0.05 mg.kg ¹1 .min ¹1 . The range of target concentrations associated with satisfactory spontaneous respiration was wide and varied over a 4.7-fold range from 0.6 to 2.8 ng.ml ¹1 .

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Pharmacokinetics and Pharmacodynamics of Remifentanil

Abstract: Based on the EEG model, age and LBM are significant demographic factors that must be considered when determining a dosage regimen for remifentanil. This remains true even when interindividual pharmacokinetic and pharmacodynamic variability are incorporated in the analysis.

Cited by 583 publications

References 12 publications

Using fMRI to Quantify the Time Dependence of Remifentanil Analgesia in the Human Brain

Using fMRI to Quantify the Time Dependence of Remifentanil Analgesia in the Human Brain

Efficacy of a single dose of dexmedetomidine for cough suppression during anesthetic emergence: a randomized controlled trial

Target‐controlled remifentanil in combination with propofol for spontaneously breathing day‐case patients

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