Pharmacokinetics of testosterone and estradiol gel preparations in healthy young men

Psychoneuroendocrinology

Volumn 38, Issue 2, 2013, Pages 171-178

  Eisenegger, Christoph ^a   von Eckardstein, Arnold ^b   Fehr, Ernst ^c   von Eckardstein, Sigrid ^d  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b UNIVERSITY HOSPITAL ZURICH   (Switzerland)

^c UNIVERSITY OF ZURICH   (Switzerland)

^d Kantonsspital Luzern ^*  (Switzerland)

Author keywords

Behavioral endocrinology; Estradiol; Gel; Pharmacokinetics; Testosterone

Indexed keywords

ESTRADIOL; HYDROCORTISONE; LUTEINIZING HORMONE; PLACEBO; SEX HORMONE BINDING GLOBULIN; TESTOSTERONE;

ADULT; ARTICLE; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG MEGADOSE; ESTRADIOL BLOOD LEVEL; GEL; HUMAN; HUMAN EXPERIMENT; HYDROCORTISONE BLOOD LEVEL; LUTEINIZING HORMONE BLOOD LEVEL; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; TESTOSTERONE BLOOD LEVEL; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, CUTANEOUS; DOUBLE-BLIND METHOD; ESTRADIOL; GELS; HEALTHY VOLUNTEERS; HUMANS; HYDROCORTISONE; LUTEINIZING HORMONE; MALE; SERUM; SEX HORMONE-BINDING GLOBULIN; TESTOSTERONE; YOUNG ADULT;

EID: 84872858651     PISSN: 03064530     EISSN: 18733360     Source Type: Journal    
DOI: 10.1016/j.psyneuen.2012.05.018     Document Type: Article

References (42)

1. Adolphs R. What does the amygdala contribute to social cognition?. Ann. N. Y. Acad. Sci. 2010, 1191:42-61.
2. Biegon A., Kim S.W., Alexoff D.L., Jayne M., Carter P., Hubbard B., King P., Logan J., Muench L., Pareto D., Schlyer D., Shea C., Telang F., Wang G.J., Xu Y., Fowler J.S. Unique distribution of aromatase in the human brain: in vivo studies with PET and [N-methyl-(11)C]vorozole. Synapse 2010, 64:801-807.
3. Biegon A., Won Kim S., Logan J., Hooker J.M., Muench L., Fowler J.S. Nicotine blocks brain estrogen synthase (aromatase): in vivo positron emission tomography studies in female baboons. Biol. Psychiatry 2010, 67:774-777.
4. Bos P.A., Terburg D., van Honk J. Testosterone decreases trust in socially naive humans. Proc. Natl. Acad. Sci. U. S. A. 2010, 107:9991-9995.
5. Bos P.A., Panksepp J., Bluthe R.M., van Honk J. Acute effects of steroid hormones and neuropeptides on human social-emotional behavior: a review of single administration studies. Front. Neuroendocrinol. 2012, 33:17-35.
6. Chik Z., Johnston A., Tucker A.T., Chew S.L., Michaels L., Alam C.A. Pharmacokinetics of a new testosterone transdermal delivery system, TDS-testosterone in healthy males. Br. J. Clin. Pharmacol. 2006, 61:275-279.
7. Cornil C.A., Charlier T.D. Rapid behavioural effects of oestrogens and fast regulation of their local synthesis by brain aromatase. J. Neuroendocrinol. 2010, 22:664-673.
8. de Ronde W., ten Kulve J., Woerdeman J., Kaufman J.M., de Jong F.H. Effects of oestradiol on gonadotrophin levels in normal and castrated men. Clin. Endocrinol. (Oxf.) 2009, 71:874-879.
9. Eisenegger C., Naef M., Snozzi R., Heinrichs M., Fehr E. Prejudice and truth about the effect of testosterone on human bargaining behaviour. Nature 2010, 463:356.
10. Eisenegger C., Haushofer J., Fehr E. The role of testosterone in social interaction. Trends Cogn. Sci. 2011, 15:263-271.
11. Finkelstein J.S., Whitcomb R.W., O'Dea L.S., Longcope C., Schoenfeld D.A., Crowley W.F. Sex steroid control of gonadotropin secretion in the human male. I. Effects of testosterone administration in normal and gonadotropin-releasing hormone-deficient men. J. Clin. Endocrinol. Metab. 1991, 73:609-620.
12. Granger D.A., Shirtcliff E.A., Booth A., Kivlighan K.T., Schwartz E.B. The " trouble" with salivary testosterone. Psychoneuroendocrinology 2004, 29:1229-1240.
13. Hall K.A., Keks N.A., O'Connor D.W. Transdermal estrogen patches for aggressive behavior in male patients with dementia: a randomized, controlled trial. Int. Psychogeriatr. 2005, 17:165-178.
14. Hermans E.J., Putman P., Baas J.M., Gecks N.M., Kenemans J.L., van Honk J. Exogenous testosterone attenuates the integrated central stress response in healthy young women. Psychoneuroendocrinology 2007, 32:1052-1061.
15. Herrmann B.L., Janssen O.E., Hahn S., Broecker-Preuss M., Mann K. Effects of estrogen replacement therapy on bone and glucose metabolism in a male with congenital aromatase deficiency. Horm. Metab. Res. 2005, 37:178-183.
16. Jones M.E., Boon W.C., McInnes K., Maffei L., Carani C., Simpson E.R. Recognizing rare disorders: aromatase deficiency. Nat. Clin. Pract. Endocrinol. Metab. 2007, 3:414-421.
17. Kaya D., Cevrioglu S., Onrat E., Fenkci I.V., Yilmazer M. Single dose nasal 17beta-estradiol administration reduces sympathovagal balance to the heart in postmenopausal women. J. Obstet. Gynaecol. Res. 2003, 29:406-411.
18. Kornmann B., Nieschlag E., Zitzmann M., Gromoll J., Simoni M., von Eckardstein S. Body fat content and testosterone pharmacokinetics determine gonadotropin suppression after intramuscular injections of testosterone preparations in normal men. J. Androl. 2009, 30:602-613.
19. Kyomen H.H., Satlin A., Hennen J., Wei J.Y. Estrogen therapy and aggressive behavior in elderly patients with moderate-to-severe dementia: results from a short-term, randomized, double-blind trial. Am. J. Geriatr. Psychiatry 1999, 7:339-348.
20. Marbury T., Hamill E., Bachand R., Sebree T., Smith T. Evaluation of the pharmacokinetic profiles of the new testosterone topical gel formulation, Testim, compared to AndroGel. Biopharm. Drug Dispos. 2003, 24:115-120.
21. Nieschlag E. Testosterone Action, Deficiency, Substitution 2006, Cambridge University Press, Cambridge.
22. Nieschlag E. Clinical trials in male hormonal contraception. Contraception 2010, 82:457-470.
23. Orwoll E., Lambert L.C., Marshall L.M., Phipps K., Blank J., Barrett-Connor E., Cauley J., Ensrud K., Cummings S. Testosterone and estradiol among older men. J. Clin. Endocrinol. Metab. 2006, 91:1336-1344.
24. Postma A., Meyer G., Tuiten A., van Honk J., Kessels R.P.C., Thijssen J. Effects of testosterone administration on selective aspects of object-location memory in healthy young women. Psychoneuroendocrinology 2000, 25:563-575.
25. Riad-Fahmy D., Read G.F., Walker R.F., Griffiths K. Steroids in saliva for assessing endocrine function. Endocr. Rev. 1982, 3:367-395.
26. Riad-Fahmy D., Read G.F., Walker R.F., Walker S.M., Griffiths K. Determination of ovarian steroid hormone levels in saliva. An overview. J. Reprod. Med. 1987, 32:254-272.
27. Rochira V., Faustini-Fustini M., Balestrieri A., Carani C. Estrogen replacement therapy in a man with congenital aromatase deficiency: effects of different doses of transdermal estradiol on bone mineral density and hormonal parameters. J. Clin. Endocrinol. Metab. 2000, 85:1841-1845.
28. Schleifer L.A., Justice A.J., de Wit H. Lack of effects of acute estradiol on mood in postmenopausal women. Pharmacol. Biochem. Behav. 2002, 71:71-77.
29. Swerdloff R.S., Wang C., Cunningham G., Dobs A., Iranmanesh A., Matsumoto A.M., Snyder P.J., Weber T., Longstreth J., Berman N. Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men. J. Clin. Endocrinol. Metab. 2000, 85:4500-4510.
30. Trainor B.C., Kyomen H.H., Marler C.A. Estrogenic encounters: how interactions between aromatase and the environment modulate aggression. Front. Neuroendocrinol. 2006, 27:170-179.
31. Tuiten A., Van Honk J., Koppeschaar H., Bernaards C., Thijssen J., Verbaten R. Time course of effects of testosterone administration on sexual arousal in women. Arch. Gen. Psychiatry 2000, 57:149-153.
32. van Honk J., Tuiten A., Hermans E., Putman P., Koppeschaar H., Thijssen J., Verbaten R., van Doornen L. A single administration of testosterone induces cardiac accelerative responses to angry faces in healthy young women. Behav. Neurosci. 2001, 115:238-242.
33. van Honk J., Schutter D.J., Bos P.A., Kruijt A.W., Lentjes E.G., Baron-Cohen S. Testosterone administration impairs cognitive empathy in women depending on second-to-fourth digit ratio. Proc. Natl. Acad. Sci. U. S. A. 2011, 108:3448-3452.
34. van Rooij K., Bloemers J., de Leede L., Goldstein I., Lentjes E., Koppeschaar H., Olivier B., Tuiten A. Pharmacokinetics of three doses of sublingual testosterone in healthy premenopausal women. Psychoneuroendocrinology 2012, 37:773-781.
35. van Wingen G., Mattern C., Verkes R.J., Buitelaar J., Fernandez G. Testosterone reduces amygdala-orbitofrontal cortex coupling. Psychoneuroendocrinology 2010, 35:105-113.
36. Vermeulen A., Verdonck L., Kaufman J.M. A critical evaluation of simple methods for the estimation of free testosterone in serum. J. Clin. Endocrinol. Metab. 1999, 84:3666-3672.
37. Viau V. Functional cross-talk between the hypothalamic-pituitary-gonadal and -adrenal axes. J. Neuroendocrinol. 2002, 14:506-513.
38. Wang C., Iranmanesh A., Berman N., McDonald V., Steiner B., Ziel F., Faulkner S.M., Dudley R.E., Veldhuis J.D., Swerdloff R.S. Comparative pharmacokinetics of three doses of percutaneous dihydrotestosterone gel in healthy elderly men - a clinical research center study. J. Clin. Endocrinol. Metab. 1998, 83:2749-2757.
39. Wang C., Berman N., Longrstreth J.A., Chuapoco B., Hull L., Steiner B., Faulkner S., Dudley R.E., Swerdloff R.S. Pharmacokinetics of transdermal testosterone gel in hypogonadal men: application of gel at one site versus four sites: a general clinical research center study. J. Clin. Endocrinol. Metab. 2000, 85:964-969.
40. Wang C., Cunningham G., Dobs A., Iranmanesh A., Matsumoto A.M., Snyder P.J., Weber T., Berman N., Hull L., Swerdloff R.S. Long-term testosterone gel (AndroGel) treatment maintains beneficial effects on sexual function and mood, lean and fat mass, and bone mineral density in hypogonadal men. J. Clin. Endocrinol. Metab. 2004, 89:2085-2098.
41. Wang C. Challenges in the diagnosis of the right patient for testosterone replacement therapy. Eur. Urol. Suppl. 2007, 6:862-867.
42. Zak P.J., Kurzban R., Ahmadi S., Swerdloff R.S., Park J., Efremidze L., Redwine K., Morgan K., Matzner W. Testosterone administration decreases generosity in the ultimatum game. PLoS ONE 2009, 4:e8330.