TESTOSTERONE UNDECANOATE: A NEW ORALLY ACTIVE ANDROGEN

1975 ◽  
Vol 80 (1) ◽  
pp. 179-187 ◽  
Author(s):  
C. Hirschhäuser ◽  
C. R. N. Hopkinson ◽  
G. Sturm ◽  
A. Coert
Keyword(s):  
Gas Chromatography ◽  
Oral Administration ◽  
Replacement Therapy ◽  
Elevated Plasma ◽  
Testosterone Undecanoate ◽  
Androgen Replacement Therapy ◽  
Normal Men ◽  
Orally Active ◽  
Elevate Plasma ◽  
Androgen Levels

ABSTRACT Oral testosterone undecanoate (TU) in arachis oil has been evaluated with a view to its possible use as a means of androgen replacement therapy. A single 100 mg dose was found to elevate plasma androgen levels and urinary 17-ketosteroid excretion in 6 normal men. Ninety mg/day and 60 mg/day doses taken by a hypogonadal man resulted in sustained levels of androgen which appeared physiological when measured by radioimmunoassay without chromatography. However, upon separation of the steroids by chromatography it was found that much of the androgen present was in fact dihydrotestosterone not testosterone. Both TU and dihydrotestosterone undecanoate were detected in plasma by gas chromatography and it is suggested that the ester is absorbed as such from the intestine and the unesterified steroid subsequently released by hydrolysis. The convenience of oral administration, the resulting prolonged elevated plasma androgen levels and the probable lack of deleterious effects on the liver may render oral TU of value where androgen replacement therapy is indicated.

scholarly journals Importance of measuring testosterone in enzyme-inhibited plasma for oral testosterone undecanoate androgen replacement therapy clinical trials

2015 ◽  
Vol 1 (4) ◽  
Author(s):  
Sylvain Lachance ◽  
Om Dhingra ◽  
James Bernstein ◽  
Stéphanie Gagnon ◽  
Caroline Savard ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Replacement Therapy ◽  
Testosterone Undecanoate ◽  
Androgen Replacement Therapy

THE PHARMACOLOGY AND METABOLISM OF TESTOSTERONE UNDECANOATE (TU), A NEW ORALLY ACTIVE ANDROGEN

1975 ◽  
Vol 79 (4) ◽  
pp. 789-800 ◽  
Author(s):  
A. Coert ◽  
J. Geelen ◽  
J. de Visser ◽  
J. van der Vies
Keyword(s):  
Portal Vein ◽  
Oral Administration ◽  
Lymphatic System ◽  
Intestinal Wall ◽  
Testosterone Undecanoate ◽  
Androgenic Activity ◽  
Orally Active ◽  
Harmful Effects

ABSTRACT Testosterone undecanoate (TU), either dissolved in arachis oil or as micro-crystal suspension, displays androgenic activity on oral administration to rats in the Hershberger test. The solution in arachis oil is more active than the crystal suspension. When [3H]TU is administered orally to rats, most of it is metabolized in the intestinal wall. The majority of the metabolites probably lose their undecanoate group and are absorbed via the portal vein. The non-metabolized [3H]TU and at least two metabolites are absorbed exclusively via the lymphatic system. One of these metabolites has been identified as 5α-dihydrotestosterone undecanoate (5α-DHTU). TU has no harmful effects on the liver of the rabbits on oral administration.

PLASMA ANDROGEN LEVELS IN MEN AFTER ORAL ADMINISTRATION OF TESTOSTERONE OR TESTOSTERONE UNDECANOATE

1975 ◽  
Vol 79 (2) ◽  
pp. 366-374 ◽  
Author(s):  
E. Nieschlag ◽  
J. Mauss ◽  
A. Coert ◽  
P. Kićović
Keyword(s):  
Oral Administration ◽  
Thin Layer ◽  
Free Testosterone ◽  
Peripheral Circulation ◽  
Plasma Testosterone ◽  
Testosterone Undecanoate ◽  
Striking Increase ◽  
Layer Chromatography ◽  
Effective Medication ◽  
Androgen Levels

ABSTRACT Plasma testosterone and androstenedione levels in men were measured after oral administration of free testosterone and testosterone undecanoate. Both androgens were determined by simultaneous, specific radioimmunoassays after separation and isolation by thin layer chromatography. While free unesterified testosterone had no effect on plasma androgen levels, a striking increase of both testosterone and androstenedione levels was noted after administration of testosterone undecanoate, which is otherwise only achieved by parenteral testosterone application. This effect of testosterone undecanoate is probably due to absorption via the lymph rather than via the portal vessels so that peripheral circulation is reached before metabolism in the liver. Testosterone undecanoate promises to be an effective medication for oral androgen replacement.

Effects of Hormone Replacement Therapy on Plasma and Tissue Fibrinolytic Activity in a Rat Model of Surgically Induced Menopause

2014 ◽  
Vol 37 (2) ◽  
pp. 85 ◽  
Author(s):  
Ata Topcuoglu ◽  
Mustafa Albayrak ◽  
Hayriye Erman ◽  
Huriye Balci ◽  
Mesut Karakus ◽  
...  
Keyword(s):  
Hormone Replacement Therapy ◽  
Oral Administration ◽  
Replacement Therapy ◽  
Plasminogen Activator ◽  
Brain Tissue ◽  
Fibrinolytic Activity ◽  
Hormone Replacement ◽  
17Β Estradiol ◽  
Surgically Induced ◽  
Pai 1

Purpose: The purpose of this study was to analyze the effects of estrogen deficiency and hormone replacement therapy (HRT) on fibrinolytic activity in a rat mode of surgically-induced menopause. Methods: Twelve-week-old, sexually mature female Sprague-Dawley rats, each weighing 200–250 g, were randomly divided into four groups: (1) sham-operated group, (2) ovariectomy group, (3) ovariectomy group followed by oral administration of daily 17β-estradiol (0.02 mg/kg/day) (E2) + norethisterone acetate (0.01 mg/kg/day), and (4) ovariectomy group followed by oral administration of daily 17β-estradiol (0.01 mg/kg/day) + drospirenone (0.02 mg/kg/day). Tissue plasminogen activator (tPA) antigen, plasminogen activator inhibitor-1 (PAI-1) antigen, and PAI-1/tPA levels were measured as markers of fibrinolysis in plasma and liver and brain tissue. Results: Compared with sham-operated rats, ovariectomized rats showed higher levels of fibrinolytic activity; however, the increased fibrinolytic activity in plasma and liver tissue was significantly reduced by HRT regimens. No change was observed in the levels of fibrinolytic activity in brain tissue. Conclusions: HRT showed beneficial effects by decreasing fibrinolytic activity related to surgically-induced menopause. Short-term HRT treatment was associated with a shift in the procoagulant-anticoagulant balance toward a procoagulant state.

scholarly journals Effect of Late Androgen Replacement Therapy on Erectile Function Through Structural Changes in Castrated Rats

2021 ◽  
Vol 9 (4) ◽  
pp. 100348
Author(s):  
Tomoya Kataoka ◽  
Yuji Hotta ◽  
Yuka Yamamoto ◽  
Ayako Fukamoto ◽  
Madoka Takeuchi ◽  
...  
Keyword(s):  
Replacement Therapy ◽  
Erectile Function ◽  
Structural Changes ◽  
Androgen Replacement Therapy

Saliva and serum testosterone following oral testosterone undecanoate administration in normal and hypogonadal men

1983 ◽  
Vol 102 (3) ◽  
pp. 456-462 ◽  
Author(s):  
Th. Schürmeyer ◽  
E. J. Wickings ◽  
C. W. Freischem ◽  
E. Nieschlag
Keyword(s):  
Interindividual Variability ◽  
Serum Testosterone ◽  
Serum Samples ◽  
Additional Increase ◽  
Testosterone Undecanoate ◽  
Absorption Pattern ◽  
High Interindividual Variability ◽  
Normal Men ◽  
Hydrolysis Of ◽  
Testosterone Ester

Abstract. Since saliva testosterone reflects the testosterone fraction available to target tissues the therapeutic effectiveness of orally administered testosterone undecanoate was assessed by measuring testosterone in serum and saliva. Matched saliva and serum samples were obtained from 12 normal men and 8 hypogonadal men before and at hourly intervals after the oral administration of 120 mg testosterone undecanoate. The test was repeated in 3 men after they had taken 40 mg testosterone undecanoate twice daily for 4 to 5 weeks. Following testosterone undecanoate administration serum and saliva testosterone always showed parallel increases. However, the absorption curves showed a high interindividual variability in the time when maximum concentrations were reached, as well as in the maximum levels themselves. The increases in serum and saliva testosterone were similar in normal and hypogonadal men. In normal men basal levels were reached 4 h after the maximum had occurred, while in hypogonadal men testosterone levels were not different from basal levels 2 h after the maximum. The study shows that testosterone undecanoate is well absorbed from the gut and releases significantly elevated amounts of testosterone which is available to target tissues. As the absorption pattern was always parallel in both fluids, hydrolysis of the circulating testosterone ester by the tissue ifself seems to effect no additional increase of testosterone in the tissue.

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