Testosterone, undecanoate

456.711

456.70

227-712-6

H16A5VCT9C

C1249

2937290024

43.4

9.15

White crystalline powder

1.0±0.1 g/cm3

45-47.5 °C

550.7±50.0 °C at 760 mmHg

230.3±30.2 °C

1.522

H2O: Insoluble

Controlled Substance, -20ºC Freezer

3

R36/37/38:Irritating to eyes, respiratory system and skin . R43:May cause sensitization by skin contact. R42/43:May cause sensitization by inhalation and skin contact .

S7-S26-S36/37/39-S45-S37/39-S24-S36/37-S22

EN0330050

Xn,Xi

P201, P202, P260, P261, P263, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P312, P304+P340, P308+P313, P312, P322, P330, P363, P405, P501

H302

|Danger|H302 (93.18%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P263, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P312, P304+P340, P308+P313, P312, P322, P330, P363, P405, and P501|Aggregated GHS information provided by 44 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

There is evidence that in adolescent users, testosterone at supra-therapeutic levels may contribute to aggressive behaviour and increased rates of suicide. However, testosterone does not appear to negatively affect cognition in adult men receiving testosterone replacement therapy and may in fact benefit cognitive function. Administration of exogenous testosterone affects normal physiological hormonal regulation, and ultimately depresses the release of follicle-stimulating hormone and luteinizing hormone resulting in reduced sperm production. This should be considered before initiating testosterone in males who wish to start or grow a family. Increased levels of testosterone can also cause increased sebum production, therefore acne may be observed in patients taking exogenous testosterone. Since testosterone is converted to estrogen in the body by aromatization, males taking testosterone replacement may experience gynecomastia and/or breast pain.

Circulating testosterone is highly protein bound with about 40% bound to sex hormone-binding globulin (SHBG), and a large percentage of the remaining hormone loosely bound to albumin and other plasma proteins. Only about 2% of testosterone is unbound.

Testosterone undecanoate is indicated for replacement therapy in adult males with conditions that are linked with an absence or deficiency in endogenous testosterone production.|FDA Label

Testosterone plays a key role in male sexual differentiation and is involved in regulation of hematopoiesis, body composition, and bone metabolism. As a result, testosterone replacement therapy in males with hypogonadism can result in improved sexual function, increased lean body mass, bone density, erythropoiesis, prostate size, and changes in lipid profiles.

Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power. (See all compounds classified as Androgens.)

The absorption of testosterone undecanoate varies based on the formulation. The intramuscular formulation of testosterone esters is suspended in oil and is absorbed from the lipid phase. Testosterone is released when tissue esterases cleave the undecanoic acid side chain. The oral formulation of testosterone undecanoate is also formulated as a prodrug, is best absorbed with food and ideal absorption occurs when taken with a meal containing at least 30 g of fat.|The majority (~90%) of an intramuscularly administered dose of testosterone is conjugated and eliminated in the urine. Approximately 6% of the dose is eliminated primarily unconjugated in the feces.

The side chain of testosterone undecanoate is cleaved by non specific esterases when it enters circulation and the undecanoic acid side chain is metabolized by the beta-oxidation pathway. The resulting Testosterone molecule is then metabolized to dihydrotestosterone (DHT) by the enzyme 5-alpha reductase. DHT is reduced by 3-alpha-hydroxysteroid dehydrogenase (major) and 3-beta-hydroxysteroid dehydrogenase prior to being glucuronidated and cleared by the kidneys. It should be noted that testosterone is metabolized to several other 17-keto steroids in the body.

Based on one source, Testosterone undecanoate in castor oil (for intramuscular injection) has a half life of 33.9 days, allowing it to maintain serum levels in the normal range for over 6 weeks. It should be noted that the half life of testosterone reported in the literature is inconsistent.

Testosterone is produced by Leydig cells and exerts it's effects by binding to androgen receptors throughout the body. Testosterone affects the voice, genitalia, mood, and influences muscle growth and protein expression. Accordingly, males with low levels of testosterone often experience decreased libido, fatigue, mood changes and dysphoria. Exogenous sources of testosterone are designed to mimic the effects of endogenous testosterone.

Andriol

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients