AIM: The principal study objective was to investigate the pharmacokinetic characteristics of a new sublingual ketamine wafer and to establish its absolute bioavailability and local tolerability. METHODS: The study was of open label, two way randomized crossover design in eight healthy male volunteers. Each participant received either a single 10 mg intravenous dose as a constant rate 30 min infusion or a 25mg sublingual dose of ketamine wafer in two treatment periods with a 7 day wash out. Pharmacokinetic blood sampling and local tolerability and safety assessments were carried out during 24 h following both dosing occasions. Plasma concentrations were analyzed by non-compartmental methods and local tolerability was assessed using modified Likert scales. RESULTS: The median (90% CI lower, upper limit) absolute bioavailability of sublingual ketamine was 29% (27, 31%). The first quantifiable plasma ketamine concentration was observed within 5 min for all eight participants for both routes of administration and the median (min–max) time of the peak plasma concentration was 0.75 h (0.25–1.0 h) after sublingual administration. The ketamine wafer had very good local tolerability. CONCLUSION: Sublingual administration of the ketamine wafer resulted in rapid absorption. The ketamine wafer has comparable bioavailability with other oral transmucosal formulations of ketamine but with markedly reduced inter-subject variability, warranting further evaluation as an analgesic adjunct.
RCT Entities:
AIM: The principal study objective was to investigate the pharmacokinetic characteristics of a new sublingual ketamine wafer and to establish its absolute bioavailability and local tolerability. METHODS: The study was of open label, two way randomized crossover design in eight healthy male volunteers. Each participant received either a single 10 mg intravenous dose as a constant rate 30 min infusion or a 25mg sublingual dose of ketamine wafer in two treatment periods with a 7 day wash out. Pharmacokinetic blood sampling and local tolerability and safety assessments were carried out during 24 h following both dosing occasions. Plasma concentrations were analyzed by non-compartmental methods and local tolerability was assessed using modified Likert scales. RESULTS: The median (90% CI lower, upper limit) absolute bioavailability of sublingual ketamine was 29% (27, 31%). The first quantifiable plasma ketamine concentration was observed within 5 min for all eight participants for both routes of administration and the median (min–max) time of the peak plasma concentration was 0.75 h (0.25–1.0 h) after sublingual administration. The ketamine wafer had very good local tolerability. CONCLUSION: Sublingual administration of the ketamine wafer resulted in rapid absorption. The ketamine wafer has comparable bioavailability with other oral transmucosal formulations of ketamine but with markedly reduced inter-subject variability, warranting further evaluation as an analgesic adjunct.
Authors: Daniel B Carr; Leonidas C Goudas; William T Denman; Daniel Brookoff; Peter S Staats; Loralie Brennen; Geoff Green; Randi Albin; Douglas Hamilton; Mark C Rogers; Leonard Firestone; Philip T Lavin; Fred Mermelstein Journal: Pain Date: 2004-03 Impact factor: 6.961
Authors: Panos Zanos; Ruin Moaddel; Patrick J Morris; Lace M Riggs; Jaclyn N Highland; Polymnia Georgiou; Edna F R Pereira; Edson X Albuquerque; Craig J Thomas; Carlos A Zarate; Todd D Gould Journal: Pharmacol Rev Date: 2018-07 Impact factor: 25.468
Authors: Jennifer Swainson; Alexander McGirr; Pierre Blier; Elisa Brietzke; Stéphane Richard-Devantoy; Nisha Ravindran; Jean Blier; Serge Beaulieu; Benicio N Frey; Sidney H Kennedy; Roger S McIntyre; Roumen V Milev; Sagar V Parikh; Ayal Schaffer; Valerie H Taylor; Valérie Tourjman; Michael van Ameringen; Lakshmi N Yatham; Arun V Ravindran; Raymond W Lam Journal: Can J Psychiatry Date: 2020-11-11 Impact factor: 4.356
Authors: Jennifer Swainson; Larry J Klassen; Stefan Brennan; Pratap Chokka; Martin A Katzman; Robert L Tanguay; Atul Khullar Journal: CNS Drugs Date: 2022-02-14 Impact factor: 5.749