Minaxolone, clinical effects and pharmacokinetics. Subanaesthetic infusion regimen

Minaxolone, infused at a constant rate of 0.01 mg/kg/min produced drowsiness followed by a sleep-like state from which subjects could be easily awakened. After the infusion was stopped, initial recovery was rapid, and completed within 45 minutes. The ability to produce this state rapidly and reversibly would have great value in outpatient surgery, short operative procedures and for basal sedation during procedures performed under regional anaesthesia. In common with many intravenous induction agents, involuntary skeletal muscle movement and twitching during the latter part of the infusion regimen was observed in some subjects. The rapid recovery was consistent with the pharmacokinetic characteristics of Minaxolone, i.e. high total body clearance (near or even exceeding that of indocyanine green) and rapid redistribution. However, renal clearance of unchanged Minaxolone was negligible.