Disease relevance of REMIFENTANIL

• BACKGROUND: Clinical studies suggest that intraoperative administration of the clinical remifentanil formulation Ultiva (GlaxoWellcome GmbH & Co, Bad Oldesloe, Germany) increases postoperative pain and postoperative analgesic requirements, but mechanisms remain unclear [1].

High impact information on REMIFENTANIL

• Considering that both components of Ultiva (remifentanil hydrochloride and glycine) could be involved in NMDA receptor activation, experiments were performed first with remifentanil hydrochloride, second with glycine, and third with the two components within Ultiva [2].
• In the current study, the authors investigated the effects of remifentanil hydrochloride, with and without its vehicle, glycine, on the activation of NMDA receptors and the modulation of NMDA-induced current on neurons inside the lamina II from the dorsal horn of rat spinal cord [2].
• The authors hypothesized that Ultiva directly stimulates human NMDA receptors [1].
• In these studies, GI 87084B (0.3-20 nmol/kg/min i.v.) produced dose-dependent decreases in heart rate, arterial blood pressure, +dP/dt and cardiac output [3].
• Insurmountable antagonism of GI 87084B by naloxone was observed in the rat vas deferens [4].

Biological context of REMIFENTANIL

• 1. The agonist dissociation constant (KA) for GI 87084B (220 +/- 90 nM) was determined by receptor alkylation with beta-chlornaltrexamine in the guinea pig ileum [4].
• Remifentanil hydrochloride was given IV via PCA over 1 min with a lockout time of 1 min [5].

Associations of REMIFENTANIL with other chemical compounds

• Remifentanil (Ultiva) is a novel, ultra-short-acting opioid which has recently been approved for use as an analgesic during induction and maintenance of general anesthesia [6].
• In the present study, the influence of transcranial electrical stimulation (TCES) on the analgesic effect of remifentanil hydrochloride (HCl) in rats was determined [7].
• Although remifentanil hydrochloride, fentanyl citrate (I50 values; 1.45mM and 6.1 mM, respectively) inhibited the activity of the enzyme belonging to the healthy person, they did not alter enzyme activity on two of the three persons with G6PD deficiency [8].

References