Powder Testosterone Undecanoate

Description

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.

Testosterone undecanoate Indication

Testosterone undecanoate is indicated for testosterone replacement therapy in adult males for conditions associated with a deficiency or absence of endogenous testosterone. These conditions include:

Congenital or acquired primary hypogonadism: testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter's syndrome, chemotherapy, or toxic damage from alcohol or heavy metals. These men usually have low serum testosterone concentrations and gonadotropins (follicle-stimulating hormone FSH, luteinizing hormone LH) above the normal range.

Congenital or acquired hypogonadotropic hypogonadism: gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency or pituitary-hypothalamic injury from tumors, trauma, or radiation. These men have low testosterone serum concentrations but have gonadotropins in the normal or low range.

Testosterone undecanoate is not used to treat age-related hypogonadism.

Mechanism of action

Testosterone is a critical male sex hormone that is responsible for the normal growth and development of the male sex organs and the maintenance of secondary sex characteristics, such as the growth and maturation of male sex organs, the development of male hair distribution, vocal cord thickening, and alterations in body musculature and fat distribution. Male hypogonadism, resulting from insufficient testosterone secretion, has two main etiologies: primary hypogonadism is caused by defects in the gonads, whereas secondary hypogonadism is the failure of the hypothalamus (or pituitary) to produce sufficient gonadotropins (FSH and LH).

In the circulation, testosterone undecanoate is cleaved by endogenous non-specific esterases to release testosterone, the active component of the compound. The undecanoate side chain is pharmacologically inactive. Testosterone can be further converted by 5α reductase to its more biologically active form, dihydrotestosterone (DHT). The actions of testosterone and DHT are mediated via androgen receptor, which is widely expressed in many tissues, including the bone, muscle, prostate, and adipose tissue. Testosterone binds to androgen receptors with high affinity and regulates target gene transcription involved in the normal growth and development of the male sex organs and the maintenance of secondary sex characteristics.Testosterone can cause improved sexual function, increased lean body mass, bone density, erythropoiesis, prostate size, and changes in lipid profiles.

Testosterone Undecanoate Works?

There was an idea to produce an anabolic androgenic oral steroid that could be used for men with low testosterone and the product seemed to achieve what it was supposed to. Nonetheless, this product didn't got too popular, because topicals (such as androgel) and especially injectable testosterones are considered much more helpful.

The product is not going through the liver unlike other oral steroids – but this stuff is going through the lymphatic system. This is what avoids the steroid from being eliminated by the liver and enter the blood stream. This is the difference between Testosterone Undecanoate and other oral steroids that are methylated or 17AA.

As soon as it enters the blood stream – the product is working the exact same way as any other testosterone. Some benefits of boosting the testosterone levels include: better sleep and boosted libido. This stuff is a great mood and confidence improver for men but most importantly – it helps you to lose fat and to gain muscles.

What is Testosterone Undecanoate Used For?

Testosterone is the primary male hormone and is responsible for many man like features such as losing fat, muscle and strength gaining, facial hair growth and others.

In medical settings, the product is given to those people who are suffering from low testosterone production but for bodybuilders, it is offering as a performance enhancing drug. But the product is not very widely used because it is considered weak.

Anyway, the product is going to have a positive effect on workouts, on libido and on recovery, but that's only when this stuff is used in higher doses. The good news is that this product can be used for treating low testosterone or as a performance enhancer product without damaging your liver.

Testosterone Undecanoate is most often used by bodybuilders who do not want to inject the product for whatever the reason or use the topical product because of whatever the reason (most often they include site injection pain, allergies to topicals or others).

Although this form of testosterone is used as a PED (performance enhancer drug) – it is not recommended to use any testosterone undecanoate products alone because the stuff is too weak to see any results. The product is going to do a great job when combined so better to stack it.

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