A377 Pharmacokinetics and Pharmacokinetic/-Dynamic (Pk/Pd) Relationship of Org 9488, the 3-Desacetyl Metabolite of Org 9487

Schiere, Sjouke; Proost, Hans; Wierda, J. M. K. H.

doi:10.1097/00000542-199709001-00377

Cited by 7 publications

(2 citation statements)

References 3 publications

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“…The drug is partially converted into a 3-OH metabolite, Org 9488, which is a more potent neuromuscular blocking agent than rapacuronium (ED 90 0.5 mg kg" 1 ) and has a longer duration of action (54 min for 75% recovery of single twitch). 9 Determination of Org 9488 concentrations in maternal and fetal plasma is therefore important.…”

Section: British Journal Of Anaesthesiamentioning

confidence: 99%

Rapacuronium for modified rapid sequence induction in elective Caesarean section: neuromuscular blocking effects and safety compared with succinylcholine, and placental transfer

Abouleish¹,

Abboud

Bikhazi

et al. 1999

British Journal of Anaesthesia

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We have compared rapacuronium 2.5 mg kg-1 (n = 20) with succinylcholine 1.5 mg kg-1 (n = 22) in a multicentre, blinded, randomized study in full-term parturients undergoing elective Caesarean section under general anaesthesia. Thiopental 5 mg kg-1 was given i.v. followed by the neuromuscular blocking agent. Sixty seconds later intubation was performed. Intubating conditions, evaluated as excellent, good or poor, were good to excellent in 95% and 91% in the intent-to-treat patients after rapacuronium and succinylcholine, respectively (ns). Mean onset times at the adductor pollicis muscle for rapacuronium and succinylcholine were 80.4 (SEM 14.4) s and 63.9 (5.6) s (ns) while maximum block was 96 (1.9)% and 99 (0.4)%, respectively (ns). Rate of recovery was significantly longer after rapacuronium; times for return of T1 to 25% were 16.9 (1.5) min and 9.6 (1.1) min for rapacuronium and succinylcholine, respectively (P = 0.0004). Maternal side effects included more tachycardia and skin erythema with rapacuronium; no maternal mortality or morbidity, including bronchospasm, occurred in either group. There were no neonatal adverse effects in either group based on: Apgar scores at 1 and 5 min; times to sustained respiration; neuroadaptive capacity scores at 15 min, 2 h and 24 h; and umbilical venous and arterial blood-gas values and acid-base status. At delivery (17.7 (3.2) min), mean maternal plasma concentrations of rapacuronium were 9041.4 (1259.1) ng ml-1 and 506.4 (24.9) ng ml-1 for Org 9488 (the main metabolite). Corresponding values for umbilical venous plasma were 808.0 (92.1) ng ml-1 and 59.1 (6.5) ng ml-1, and for umbilical arterial plasma, 361.4 (56.4) ng ml-1 and 29.7 (4.6) ng ml-1, respectively. Umbilical venous to maternal venous ratios for rapacuronium and Org 9488 were 8.8% (1.3)% and 10.2 (1.7)%, respectively.

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Section: British Journal Of Anaesthesiamentioning

confidence: 99%

Rapacuronium for modified rapid sequence induction in elective Caesarean section: neuromuscular blocking effects and safety compared with succinylcholine, and placental transfer

Abouleish¹,

Abboud

Bikhazi

et al. 1999

British Journal of Anaesthesia

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“…Little is known about the potency of this metabolite, although it was reported to be more potent and to have a longer duration than rapacuronium. 10 Except for a more rapid equilibration between plasma and effect compartments, the kinetic characteristics of rapacuronium are similar to those of other steroidal NMBAs. Its dynamic characteristics, therefore, cannot be explained adequately using traditional kinetic variables.…”

mentioning

confidence: 83%

Clinical Pharmacology of Rapacuronium Bromide, a New Short‐Acting Neuromuscular Blocking Agent

1999

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Rapacuronium is a new steroidal, nondepolarizing, neuromuscular blocking agent. It appears to be the least potent of all available nondepolarizing muscle relaxants. Its onset of action resembles that of succinylcholine, and its recovery times are shorter than those of other nondepolarizing agents. The clinical duration of rapacuronium can be shortened significantly with early (2 min) administration of neostigmine, which may be beneficial in patients with difficult airway or failed intubation. Rapacuronium appears to be free of significant cardiovascular complications.

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Muscle Relaxants in Clinical Anaesthesia: An Update

Vilardi

Sanfilippo

Verdi

1999

Anaesthesia, Pain, Intensive Care and Emergency Medicine — A.P.I.C.E.

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A377 Pharmacokinetics and Pharmacokinetic/-Dynamic (Pk/Pd) Relationship of Org 9488, the 3-Desacetyl Metabolite of Org 9487

Cited by 7 publications

References 3 publications

Rapacuronium for modified rapid sequence induction in elective Caesarean section: neuromuscular blocking effects and safety compared with succinylcholine, and placental transfer

Rapacuronium for modified rapid sequence induction in elective Caesarean section: neuromuscular blocking effects and safety compared with succinylcholine, and placental transfer

Clinical Pharmacology of Rapacuronium Bromide, a New Short‐Acting Neuromuscular Blocking Agent

Muscle Relaxants in Clinical Anaesthesia: An Update

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