Search PubMed⌕ Search

PubMed · 9506244

Transdermal testosterone.

Abstract

Nightly application of testosterone transdermal (TTD) system to nonscrotal sites in men with hypogonadism results in a 24-hour serum testosterone concentration profile which mimics the circadian pattern observed in healthy young men. The system also normalises dihydrotestosterone/testosterone and estradiol/testosterone ratios and reduces luteinising hormone levels towards the normal range. A multicentre, open-label study demonstrated that nocturnal erectile response and overall sexual function improved during 12 months' treatment with the TTD system (5 mg/day) in men with hypogonadism. Individual variables of sexual desire, arousal, frequency of sexual activity, orgasm and satisfaction also improved. The TTD system is well tolerated, with application site reactions such as pruritus, burn-like blisters and erythema being the most commonly reported events. Prostate-specific antigen levels and prostate volume remain in the normal range during long term treatment.

Explore related subjects

Keep this discovery

Explore connections, maps & timelines

BibTeXRIS

K J McClellan, K L Goa. 1998. Transdermal testosterone.. https://doi.org/10.2165/00003495-199855020-00006

Cite the original work for its findings. Save a collection to share your selection of sources.

KEEP EXPLORING

Related citations

Comparison of the effect of ultrasound and of chemical enhancers on transdermal permeation of caffeine and morphine through hairless mouse skin in vitro.

The effect of ultrasound (US) on permeation of two model drugs, caffeine (CAF) and morphine (MOR), through hairless mouse skin in vitro was compared with that of three chemical enhancers. Low-frequency (40 KHz), low-power (<0.5 W/cm(2)) US was used; the effect of high-frequency US (1.5-3.0 MHz) was also evaluated in the case of CAF. The chemical enhancers, tested in combination with propylene glycol (PG), were benzalkonium chloride (BAC) oleyl alcohol (OA) and alpha-terpineol (TER). The high-frequency US enhancement of CAF transdermal flux was not statistically significant, while low frequency produced a small but significant increase of the enhancement factor. The effect of US on CAF permeation, however, was lower than that produced by chemical enhancers, in particular OA. The effect of low-frequency US on permeation of MOR was significantly greater (about 10-fold) when compared, on the same frequency and intensity basis, with the effect on CAF. The most active chemical enhancer for MOR, OA, had practically the same effect as low-frequency US. Sonicated skin, although showing slight histological changes, recovered its original low permeability characteristics after turning off sonication. Within the tested system, chemical enhancement appears to offer some advantages over low-frequency US.

Administration, Cutaneous↗

The effect of surfactants on the skin penetration of diazepam.

The percutaneous permeation of diazepam was investigated in rat skin after application of a water-propylene glycol (50:50% v/v) using a diffusion cell technique. The effect of various surfactants (sodium lauryl sulfate (SLS), cetyltrimethylammonium bromide (CTAB), benzalkonium chloride or Tween 80) with different concentrations on skin permeability were evaluated. Flux, K(p), lag time and enhancement ratios (ERs) of diazepam were measured over 10 h and compared with control sample (containing no surfactant). Furthermore, diazepam solubility in presence of surfactants was determined. The in vitro permeation experiments with rat skin revealed that the surfactant enhancers varied in their ability to enhance the flux of diazepam. Benzalkonium chloride which possessed the highest lipophilicity (logP=1.9) among cationic surfactants provided the greatest enhancement for diazepam flux (7.98-fold over control). CTAB (logP<1) at a concentration of 1% w/w exhibited no significant increase in flux of diazepam compared to control (1.16-fold over control). The results also showed that the highest ER was obtained in presence of 1% w/w surfactant with the exception of SLS and CTAB. The increase in flux at low enhancer concentrations is normally attributed to the ability of the surfactant molecules to penetrate the skin and increase its permeability. Reduction in the rate of transport of the drug present in enhancer systems beyond 1% w/w is attributed to the ability of the surfactant to form micelles and is normally observed only if interaction between micelle and the drug occurs. The results showed that the nature of enhancer greatly influences cutaneous barrier impairment.

Administration, Cutaneous↗

In vitro study of low-frequency ultrasound-enhanced transdermal transport of fentanyl and caffeine across human and hairless rat skin.

The effect of low-frequency sonophoresis on fentanyl and caffeine permeation through human and hairless rat skin was studied in vitro. Experiments were performed using 20 kHz ultrasound applied at either continuous or discontinuous mode and with an average intensity of 2.5 W/cm(2). The results showed that low-frequency ultrasound enhanced the transdermal transport of both fentanyl and caffeine across human and hairless rat skin. This was explained by both increasing flux during sonication and shortening the lag time. Discontinuous mode was found to be more effective in increasing transdermal penetration of fentanyl while transdermal transport of caffeine was enhanced by both continuous and pulsed mode. Histological and electron microscopy studies showed that human and hairless rat skin was unaffected by ultrasound exposure. Further studies will be necessary to determine the relative contribution of ultrasound parameters in low-frequency ultrasound-induced percutaneous enhancement of drug transport.

Administration, Cutaneous↗