Ketamine formulation and route comparisons
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Ketamine formulation and route comparisons Ketamine formulations which maximise first-pass metabolism and delay the amount of time that ketamine maximum concentrations are present (Tmax) "will be better tolerated and safer than formulations which lack these characteristics", according to the results of a structured review reported in the European Journal of Clinical Pharmacology. The review included 41 treatment arms identified from 21 publications where patients or volunteers received either racemic ketamine (n=29) or S-ketamine (n=12). A ketamine solution was administered in 29 treatment arms, either IV (n=11) or by nasal spray (n=6), orally (n=4) or by IM injection (n=4). Other treatment arms received rectal suppositories (n=4) or solid oral dosage forms as sublingual tablets (n=3), controlled-release tablets (n=3) or immediate-release tablets (n=2). Pharmacokinetic analyses revealed that ketamine:norketamine ratios were strongly positively correlated with ketamine absolute bioavailability, change in dissociation ratios, and change in blood pressure, but not with dose, which the authors note is "not unexpected" as ketamine’s pharmacokinetics are dose-linear. In addition, there was a strong negative correlation between ketamine:norketamine ratios and ketamine Tmax, which was strongly positively correlated with change in both dissociation ratios and blood pressure. So the rapid absorption of solution formulations, resulting in earlier Tmax values, led to more increases in dissociation ratios and blood pressure than solid dose formulations. "There are two additional ketamine formulations reported in the literature", a nanoparticle formulation administered by depot injection and a transdermal patch formulation, which may have these favourable pharmacokinetic parameters, but "the associated human pharmacokinetic data have yet to be published". Glue P, et al. Influence of formulation and route of administration on ketamine’s safety and tolerability: systematic review. European Journal of Clinical Pharmacology : 18 Nov 2020. Available from: URL: http://doi.org/10.1007/s00228-020-03047-z 803519473
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Reactions 5 Dec 2020 No. 1833
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