NEBIDO (test undeacanoate ) in TRT

[Vitor Ennnergy]

What are your thoughts on NEBIDO (undecanoate testosterone 1g - 4cc ) from schering labs , they promise a single trimestral injection to get stable physiologic levels of serum testosterone?
Does someone here have personal experience with this drug?

 

[FerrariF50]

good stuff. you're lucky to get your hands on it imo

 

[FerrariF50]

infrequent 1g testosterone injections have been studied as a means to reduce injection burden and iirc have shown fairly good results

but smaller less frequent injections have been shown to be provide more optimal testosterone replacement therapy (TRT) hormone levels (testosterone values not exceeding the normal range and persistence of normal levels)

 

[FerrariF50]

The Journal of Clinical Endocrinology & Metabolism Vol. 89, No. 11 5429-5434
Copyright © 2004 by The Endocrine Society

Intramuscular Testosterone Undecanoate: Pharmacokinetic Aspects of a Novel Testosterone Formulation during Long-Term Treatment of Men with Hypogonadism

M. Schubert, T. Minnemann, D. Hübler, D. Rouskova, A. Christoph, M. Oettel, M. Ernst, U. Mellinger, W. Krone and F. Jockenhövel

Klinik II und Poliklinik für Innere Medizin der Universität zu Köln (M.S., T.M., A.C., W.K.), 50931 Köln, Germany; Jenapharm GmbH & Co. KG (D.H., D.R., M.O., M.E., U.M.), 07745 Jena, Germany; and Evangelisches Krankenhaus Herne (F.J.), 44623 Herne, Germany

In an open-label, randomized, prospective trial, we investigated pharmacokinetics and several efficacy and safety parameters of a novel, long-acting testosterone (T) undecanoate (TU) formulation in 40 hypogonadal men (serum testosterone concentrations < 5 nmol/liter). For the first 30 wk (comparative study), the patients were randomly assigned to receive either 10 x 250 mg T enanthate (TE) im every 3 wk (n = 20) or 3 x 1000 mg TU im every 6 wk (loading dose) followed by 1 x 1000 mg after an additional 9 wk (n = 20). In a follow-up study, observation continued in those patients who completed the comparative part and opted for TU treatment (8 x 1000 mg TU every 12 wk in former TU patients and 2 x 1000 mg TU every 8 wk plus 6 x 1000 mg every 12 wk in former TE patients) for an additional 20–21 months. Here we report only the pharmacokinetic aspects of the new TU formulation for the first approximately 2.5 yr of treatment. At baseline, serum T concentrations did not significantly differ between the two study groups. In the TE group, mean trough levels of serum T were always less than 10 nmol/liter before the next injection, whereas in the TU group, mean trough levels of serum T were 14.1 ± 4.5 nmol/liter after the first two doses (6-wk intervals) and 16.3 ± 5.7 nmol/liter after the 9-wk interval at wk 30. The mean serum levels of dihydrotestosterone and estradiol also increased in parallel to the serum T pattern and remained within the normal range. In the follow-up study, the former TU patients (n = 20) received eight TU injections at 12-wk intervals, and the TE patients (n = 16) switched to TU and initially received two TU injections at 8-wk intervals (loading) and continued with six TU injections at 12-wk intervals (maintenance). This regimen resulted in stable mean serum trough levels of T (ranging from 14.9 ± 5.2 to 16.5 ± 8.0 nmol/liter) and estradiol (ranging from 98.5 ± 45.2 to 80.4 ± 14.4 pmol/liter). The present study has shown that 1000 mg TU injected into male patients with hypogonadism at 12-wk intervals is well tolerated and leads to T levels within normal ranges, using four instead of 17 or more TE injections per year. An initial loading dose of either 3 x 1000 mg TU every 6 wk at the beginning of hormone substitution or 2 x 1000 mg TU every 8 wk after switching from the short-acting TE to TU were found to be a adequate dosing regimens for starting of treatment with the long-acting TU preparation.

 

[FerrariF50]

Journal of Andrology, Vol 19, Issue 6 761-768, Copyright © 1998 by The American Society of Andrology

JOURNAL ARTICLE

A pharmacokinetic study of injectable testosterone undecanoate in hypogonadal men

G. Y. Zhang, Y. Q. Gu, X. H. Wang, Y. G. Cui and W. J. Bremner
National Research Institute for Family Planning (World Health Organization Collaborating Center for Research in Human Reproduction), Beijing, People's Republic of China.

Testosterone undecanoate (TU) provides testosterone (T) replacement for hypogonadal men when administered orally but requires multiple doses per day and produces widely variable serum T levels. We investigated the pharmacokinetics of a newly available TU preparation administered by intramuscular injection to hypogonadal men. Eight patients with Klinefelter's syndrome received either 500 mg or 1,000 mg of TU by intramuscular injection; 3 months later, the other dose was given to each man (except to one, who did not receive the 1,000-mg dose). Serum levels of reproductive hormones were measured at regular intervals before and after the injections. Mean serum T levels increased significantly at the end of the first week, from less than 10 nmol/L to 47.8+/-10.1 and 54.2+/-4.8 nmol/ L for the lower and higher doses, respectively. Thereafter, serum T levels decreased progressively and reached the lower-normal limit for adult men by day 50 to 60. Pharmacokinetic analysis showed a terminal elimination half-life of 18.3+/-2.3 and 23.7+/-2.7 days and showed a mean residence time of 21.7+/-1.1 and 23.0+/-0.8 days for the lower and higher doses, respectively. The area under the serum T concentration-time curve and the T-distribution value related to serum T concentration were significantly higher following the 1,000-mg dose than following the 500-mg dose. The 500-mg dose, when given as the second injection, yielded optimal pharmacokinetics (defined as mean peak T values not exceeding the normal range and persistence of normal levels for at least 7 weeks), suggesting that repeated injections of 500 mg at 6-8-week intervals may provide optimal T replacement. The mean serum levels of estradiol were normalized following the injections, and prolactin levels were normal throughout the study. Significant decrease of serum luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels was observed, with the decrease in LH levels being more pronounced. There were no significant differences in serum LH and FSH levels between the two doses. Sex hormone-binding globulin (SHBG) levels before any T therapy were near the upper limit of normal for adult men and were reduced by approximately 50% just prior to the second dose of TU. The decreased SHBG levels produced by the first TU injection could have led to lower peak total T levels and to a more rapid clearance of T following the second TU injection. We conclude that single-dose injections of TU to hypogonadal men can maintain serum T concentration within the normal range for at least 7 weeks without immediately apparent side effects. It is likely that this form of T would require injections only at 6-8-week or longer intervals, not at the 2-week intervals necessary with currently used T esters (enanthate and cypionate). This injectable TU preparation may provide improved substitution therapy for male hypogonadism and, in addition, may be developed as an androgen component of male contraceptives.

 

[Perfection Awaits]

I wish i could use it. It's the best thing for testosterone replacement therapy (TRT) out there. You're lucky if you're getting it.

 

[DADAWG]

i find it really hard to believe that you can use this stuff and get as stable a blood test level as weekly injects with eth/cyp. drug manafacturere claims ans studies " that they paid for " ar usually not entirely accurate ,just my opinion.

 

[Warmachine]

i find it really hard to believe that you can use this stuff and get as stable a blood test level as weekly injects with eth/cyp. .

but you would be more stable injecting this once a week as opposed to eth/cyp.
i inject eth/cyp 2x a week otherwise my emotions and anxiety start going crazy.

 

[DADAWG]

but you would be more stable injecting this once a week as opposed to eth/cyp.
i inject eth/cyp 2x a week otherwise my emotions and anxiety start going crazy.

very likely you could divide the dose and injecty more often and get good results. you probablly would need prop at first while the undeconate slowly built up imo.

 

[DocJ]

Yes, undecanoate or decanoate more frequently would be ideal.