Nicotine transdermal absorption

Gorsline, J. Okerholm, R.A. Rolf, C.N. Moos, C.D. Hwang, S.S. Comparison of plasma nicotine concentrations after application of nicoderm (nicotine transdermal system) to different skin sites. J. Clin. Pharmacol. 1992,32, 576-581. Wester, R.C. Maibach, H.I. Bucks, D.A.W. In vivo percutaneous absorption of paraquat from hand, leg and forearm of humans. J. Toxicol. Environ. Health 1984, 14, 759-762. Taskovich, L. Shaw, J.E. Regional differences in the morphology of human skin correlation with variations in drug permeability. J. Invest. Dermatol. 1978, 70, 111. Roberts, M.S. Eavretto, W.A. Meyer, A. Reckmann, M. Wongseelashote, T. Topical bioavailability of methyl sahcy-late. Aust. N.Z. J. Med. 1982, 12, 303-305. 

Fant RV, Henningfleld JE, Shiffman S, Strahs KR, Reitberg DP (2000) A pharmacokinetic crossover study to compare the absorption characteristics of three transdermal nicotine patches. Pharmacol Biochem Behav 67(3) 479 82... 

There are several approaches to help patients stop smoking. One approach is replacement therapy with nicotine in the form of gum, transdermal patch, nasal spray, or inhaler. All these forms have low abuse potential and are effective in patients motivated to stop smoking. Their action derives from slow absorption of nicotine that occupies 4 2 receptors in the central nervous system and reduces the desire to smoke and the pleasurable feelings of smoking. 

Vanakoski, J. Seppala, T. Sievi, E. Lunell, E. Exposure of high ambient temperature increases absorption and plasma concentrations of transdermal nicotine. Clin. Pharmacol. Ther. 1996, 60, 308-315. 

Ashton P, Walters KA, Brain KR, Hadgraft J. Surfactant effects in percutaneous absorption. Part 1. Effects on the transdermal flux of methyl nicotinate. Int J Pharm 1992 87(10) 261—264. 

Nicotine bioavailability also varies with the delivery system. The reported bioavailability from the nasal spray and transdermal patch is 53% and 82%, respectively (93,184). In nicotine polacrilex gum, nicotine is bound to an ion exchange resin and is released only by chewing. Nicotine bioavailability, therefore, is dependent on the vigor, rapidity, and duration of chewing. Of the 10 mg in each cartridge of a nicotine inhaler, only 4 mg is actually delivered from the device to the oral mucosa and is available for absorption. 

One of the earlier studies demonstrating the role of blood flow on percutaneous absorption in humans used comparison dermal concentrations after topical application in vitro and in vivo (Schaefer and Stuttgen, 1978). Perfusion caused by cutaneous microcirculation also affected responses after the topical penetration of the vasodilator methyl nicotinate in humans (Guy et al., 1983). Altered transdermal drug absorption of the vasoactive nonsteroidal antiinflammatory drug (NSAID) methyl salicylate (MeSA) has also been attributed to changes in in vivo cutaneous perfusion. Exercise, heat exposure, or both increased MeSA absorption more than three times the control levels in six volunteers (Danon etal., 1986). A later case study reported that skin necrosis and other toxic symptoms occurred when a heating pad was used with a topical MeSA and menthol formulation meant to treat arthritic pain (Heng, 1987). 

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