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Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men.

Publication ,  Journal Article
Swerdloff, RS; Wang, C; Cunningham, G; Dobs, A; Iranmanesh, A; Matsumoto, AM; Snyder, PJ; Weber, T; Longstreth, J; Berman, N
Published in: J Clin Endocrinol Metab
December 2000

Transdermal delivery of testosterone (T) represents an effective alternative to injectable androgens. Transdermal T patches normalize serum T levels and reverse the symptoms of androgen deficiency in hypogonadal men. However, the acceptance of the closed system T patches has been limited by skin irritation and/or lack of adherence. T gels have been proposed as delivery modes that minimize these problems. In this study we examined the pharmacokinetic profiles after 1, 30, 90, and 180 days of daily application of 2 doses of T gel (50 and 100 mg T in 5 and 10 g gel, delivering 5 and 10 mg T/day, respectively) and a permeation-enhanced T patch (2 patches delivering 5 mg T/day) in 227 hypogonadal men. This new 1% hydroalcoholic T gel formulation when applied to the upper arms, shoulders, and abdomen dried within a few minutes, and about 9-14% of the T applied was bioavailable. After 90 days of T gel treatment, the dose was titrated up (50 mg to 75 mg) or down (100 mg to 75 mg) if the preapplication serum T levels were outside the normal adult male range. Serum T rose rapidly into the normal adult male range on day 1 with the first T gel or patch application. Our previous study showed that steady state T levels were achieved 48-72 h after first application of the gel. The pharmacokinetic parameters for serum total and free T were very similar on days 30, 90, and 180 in all treatment groups. After repeated daily application of the T formulations for 180 days, the average serum T level over the 24-h sampling period (C(avg)) was highest in the 100 mg T gel group (1.4- and 1.9-fold higher than the C(avg) in the 50 mg T gel and T patch groups, respectively). Mean serum steady state T levels remained stable over the 180 days of T gel application. Upward dose adjustment from T gel 50 to 75 mg/day did not significantly increase the C(avg), whereas downward dose adjustment from 100 to 75 mg/day reduced serum T levels to the normal range for most patients. Serum free T levels paralleled those of serum total T, and the percent free T was not changed with transdermal T preparations. The serum dihydrotestosterone C(avg) rose 1.3-fold above baseline after T patch application, but was more significantly increased by 3.6- and 4.6-fold with T gel 50 and 100 mg/day, respectively, resulting in a small, but significant, increase in the serum dihydrotestosterone/T ratios in the two T gel groups. Serum estradiol rose, and serum LH and FSH levels were suppressed proportionately with serum T in all study groups; serum sex hormone-binding globulin showed small decreases that were significant only in the 100 mg T gel group. We conclude that transdermal T gel application can efficiently and rapidly increase serum T and free T levels in hypogonadal men to within the normal range. Transdermal T gel provided flexibility in dosing with little skin irritation and a low discontinuation rate.

Duke Scholars

Published In

J Clin Endocrinol Metab

DOI

ISSN

0021-972X

Publication Date

December 2000

Volume

85

Issue

12

Start / End Page

4500 / 4510

Location

United States

Related Subject Headings

  • Testosterone
  • Sex Hormone-Binding Globulin
  • Patient Compliance
  • Middle Aged
  • Male
  • Luteinizing Hormone
  • Hypogonadism
  • Humans
  • Gels
  • Estradiol
 

Citation

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Swerdloff, R. S., Wang, C., Cunningham, G., Dobs, A., Iranmanesh, A., Matsumoto, A. M., … Berman, N. (2000). Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men. J Clin Endocrinol Metab, 85(12), 4500–4510. https://doi.org/10.1210/jcem.85.12.7045
Swerdloff, R. S., C. Wang, G. Cunningham, A. Dobs, A. Iranmanesh, A. M. Matsumoto, P. J. Snyder, T. Weber, J. Longstreth, and N. Berman. “Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men.J Clin Endocrinol Metab 85, no. 12 (December 2000): 4500–4510. https://doi.org/10.1210/jcem.85.12.7045.
Swerdloff RS, Wang C, Cunningham G, Dobs A, Iranmanesh A, Matsumoto AM, et al. Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men. J Clin Endocrinol Metab. 2000 Dec;85(12):4500–10.
Swerdloff, R. S., et al. “Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men.J Clin Endocrinol Metab, vol. 85, no. 12, Dec. 2000, pp. 4500–10. Pubmed, doi:10.1210/jcem.85.12.7045.
Swerdloff RS, Wang C, Cunningham G, Dobs A, Iranmanesh A, Matsumoto AM, Snyder PJ, Weber T, Longstreth J, Berman N. Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men. J Clin Endocrinol Metab. 2000 Dec;85(12):4500–4510.
Journal cover image

Published In

J Clin Endocrinol Metab

DOI

ISSN

0021-972X

Publication Date

December 2000

Volume

85

Issue

12

Start / End Page

4500 / 4510

Location

United States

Related Subject Headings

  • Testosterone
  • Sex Hormone-Binding Globulin
  • Patient Compliance
  • Middle Aged
  • Male
  • Luteinizing Hormone
  • Hypogonadism
  • Humans
  • Gels
  • Estradiol