Vasoactive properties of lignocaine administered by iontophoresis in human skin.
The vasoactivity of lignocaine has an important influence on its clinical efficacy and systemic vascular absorption. The aim of this study was to evaluate its vasoactive properties when administered by the non-invasive technique of iontophoresis. We used laser Doppler imaging to measure the forearm skin blood flow responses of seven healthy young males to iontophoretic delivery of two preparations of 20 g/l of lignocaine hydrochloride, one containing the preservatives methylparaben and propylparaben and one without. The subjects were blind to the order of drug administration, and we assessed analgesia at the sites using a pinprick test. Delivery of both preparations of (positively charged) lignocaine under the anode caused demonstrable analgesia, but no change in skin blood flow. An increase in perfusion was measured, however, when the preservative-containing preparation was administered under the cathode. There was little or no response to the solution without preservatives, although the difference in response between the two preparations was not statistically significant (P =0.063). Although there were no vasoactive effects of lignocaine at the relatively low dose used in the present study, our results suggest that the preservatives methylparaben and propylparaben are the most likely cause of the vasodilatation that we observed under the cathode, and may therefore have a significant influence on the vasoactivity of this preparation when administered by injection. Both are negatively charged in solution and have been reported to possess vasodilator properties. It might be worth considering the use of alternative, non-vasoactive preservatives in local anaesthetic preparations, or avoiding the use of additives altogether, when this is feasible.
Newton
David J
DJ
Peripheral Vascular Diseases Research Unit, University Department of Medicine, Ninewells Hospital and Medical School, Dundee DD1 9SY, Scotland, UK. d.j.newton@dundee.ac.uk
Amyes
Alexandra K B
AK
Khan
Faisel
F
McLeod
Graeme A
GA
Bannister
Jonathan
J
Belch
Jill J F
JJ
D000279:Administration, Cutaneous; D000328:Adult; D000698:Analgesia; D000779:Anesthetics, Local / Q000494:pharmacology*; D006801:Humans; D007478:Iontophoresis; D017078:Laser-Doppler Flowmetry; D008012:Lidocaine / Q000494:pharmacology*; D008297:Male; D010147:Pain Measurement; D010226:Parabens / Q000494:pharmacology; D011310:Preservatives, Pharmaceutical / Q000494:pharmacology; D012039:Regional Blood Flow / Q000187:drug effects; D016037:Single-Blind Method; D012867:Skin / Q000098:blood supply*; D014664:Vasodilation / Q000187:drug effects*
D000779:Anesthetics, Local; D010226:Parabens; D011310:Preservatives, Pharmaceutical; D008012:Lidocaine; C015358:methylparaben; C006068:propylparaben