Androgel Testosterona Gel 50g Besins Pacote de 1 x 5 g x 10

AndroGel, embalagem com 10 sachês

Androgel Testosterona Gel 50g Besins Pacote de 1 x 5 g x 10

Androgel is a transdermal hydroalcoholic testosterone gel that contains a 1% or 1.62% concentration of testosterone by weight. It was originally released in 2.5 gram and 5-gram 1% sachets, equating to a total per-application testosterone dose of 25 mg and 50 mg respectively. The newer 1.62% version provides 40.5 mg of testosterone. The AndroGel® prescribing information states that the product has a transdermal bioavailability of approximately 10%. This means that each 2.5 or 5 gram dose will deliver approximately 2.5 mg or 5 mg of hormone systemically. With this mode of administration, testosterone levels begin to elevate approximately 30 minutes after the gel is applied to the body, and substantial elevations in serum androgen levels are achieved within 4 hours. Testosterone levels will remain elevated for approximately 24 hours after administration, so that that the drug is applied once per day. Regular dosing will provide a steady hormone balance over each 24-hour period.

História:

AndroGel® was developed in the United States by Unimed Pharmaceuticals, a division of Solvay. It was approved by the FDA for sale as a prescription drug in February of 2000. It is indicated for use in adult males with conditions associated with a deficiency or absence of endogenous testosterone. This includes cases of primary hypogonadism, which may be caused by cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter’s syndrome, chemotherapy, or alcohol/heavy metal toxicity. It is also prescribed to treat hypogonadotrophic hypogonadism, including patients with luteinizing hormone or luteinizing hormone-releasing hormone (LHRH) deficiency caused by tumors, injury, or radiation. Primary hypogonadism is usually characterized by low testosterone and high gonadotropin (LH/FSH) levels, while hypogonadotrophic hypogonadism is usually associated with low testosterone and low to normal gonadotropin levels. AndroGel® is said to have a clinical success rate of 87%, perhaps owing to the greater patient comfort and compliance this form of testosterone offers in comparison with hormone injections.

Outros géis hidroalcoólicos transdérmicos de testosterona foram lançados nos EUA e no exterior desde a introdução do AndroGel®. Testim® da Auxilium Pharmaceuticals é talvez a marca concorrente mais conhecida, amplamente vendida nos EUA e na Europa. Este produto também vem na forma de um gel de testosterona a 1%, alegando um nível de biodisponibilidade de 10%. Estudos demonstraram que o Testim® fornece até 38% mais testosterona livre para uma determinada dose em comparação com o AndroGel®.⁴²³Observa-se que Testim® usa um gel mais espesso e pegajoso em comparação com AndroGel®, o que pode explicar a maior transferência de hormônio. Em janeiro de 2006, o FDA aprovou o primeiro gel genérico de testosterona nos EUA, fabricado pela Watson Pharmaceuticals. Os géis de testosterona são um dos métodos mais populares de administração de testosterona na medicina clínica atualmente e provavelmente serão encontrados em breve em todos os mercados globais que apoiam uma indústria ativa de terapia de reposição hormonal.

Como fornecido:

Géis hidroalcoólicos transdérmicos de testosterona estão disponíveis em muitos mercados de medicamentos humanos. A composição e a dosagem podem variar de acordo com o país e o fabricante, mas geralmente contêm 1% de testosterona por peso; embalado em tubos volumétricos ou pacotes de dose única contendo 2,5 gramas ou 5 gramas de gel. AndroGel® (EUA) também é produzido em um dispensador de bomba contendo 75 gramas de gel, que oferece 60 aplicações dosadas de 1,25 gramas cada.

Características estruturais:

AndroGel® é um gel hidroalcoólico contendo 1% de testosterona (livre) em peso. Ele foi projetado para fornecer uma administração transdérmica contínua de testosterona por 24 horas após a aplicação na pele. Aproximadamente 10% da dose aplicada é absorvida pela pele durante cada período de 24 horas.

Efeitos colaterais (estrogênicos):

Testosterone is readily aromatized in the body to estradiol (estrogen). The aromatase (estrogen synthetase) enzyme is responsible for this metabolism of testosterone. Elevated estrogen levels can cause side effects such as increased water retention, body fat gain, and gynecomastia. Testosterone is considered a moderately estrogenic steroid. Exceeding therapeutic doses will increase the likelihood of estrogenic side effects. In such cases, an anti-estrogen such as clomiphene citrate or tamoxifen citrate is commonly applied to prevent estrogenic side effects. One may alternately use an aromatase inhibitor like Arimidex® (anastrozole), which more efficiently controls estrogen by preventing its synthesis. Aromatase inhibitors can be quite expensive in comparison to anti-estrogens, however, and may also have negative effects on blood lipids.

Efeitos colaterais (androgênicos):

Testosterone is the primary male androgen, responsible for maintaining secondary male sexual characteristics. Exceeding normal therapeutic doses is likely to produce androgenic side effects including oily skin, acne, and body/facial hair growth. Men with a genetic predisposition for hair loss (androgenetic alopecia) may notice accelerated male pattern balding. Women are warned of the potential virilizing effects of anabolic/androgenic steroids, especially with a strong androgen such as testosterone. These may include deepening of the voice, menstrual irregularities, changes in skin texture, facial hair growth, and clitoral enlargement.

In androgen-responsive target tissues such as the skin, scalp, and prostate, the high relative androgenicity of testosterone is dependant on its reduction to dihydrotestosterone (DHT). The 5-alpha reductase enzyme is responsible for this metabolism of testosterone. The concurrent use of a 5-alpha reductase inhibitor such as finasteride or dutasteride will interfere with site-specific potentiation of testosterone action, lowering the tendency of testosterone drugs to produce androgenic side effects. It is important to remember that anabolic and androgenic effects are both mediated via the cytosolic androgen receptor. Complete separation of testosterone’s anabolic and androgenic properties is not possible, even with total 5-alpha reductase inhibition.

Efeitos colaterais (hepatotoxicidade):

Testosterone does not have hepatotoxic effects; liver toxicity is unlikely. One study examined the potential for hepatotoxicity with high doses of testosterone by administering 400 mg of the hormone per day (2,800 mg per week) to a group of male subjects. The steroid was taken orally so that higher peak concentrations would be reached in hepatic tissues compared to intramuscular injections. The hormone was given daily for 20 days, and produced no significant changes in liver enzyme values including serum albumin, bilirubin, alanine-amino-transferase, and alkaline phosphatases.⁴²⁴

Efeitos colaterais (cardiovasculares):

Anabolic/androgenic steroids can have deleterious effects on serum cholesterol. This includes a tendency to reduce HDL (good) cholesterol values and increase LDL (bad) cholesterol values, which may shift the HDL to LDL balance in a direction that favors greater risk of arteriosclerosis. The relative impact of an anabolic/androgenic steroid on serum lipids is dependant on the dose, route of administration (oral vs. injectable), type of steroid (aromatizable or non-aromatizable), and level of resistance to hepatic metabolism. Anabolic/androgenic steroids may also adversely effect blood pressure and triglycerides, reduce endothelial relaxation, and support left ventricular hypertrophy, all potentially increasing the risk of cardiovascular disease and myocardial infarction. Therapeutic doses of testosterone used to correct insufficient androgen production in otherwise healthy aging men are unlikely to increase atherogenic risk, and may actually reduce the risk of cardiovascular mortality.⁴²⁵

Para ajudar a reduzir o esforço cardiovascular, é aconselhável manter um programa ativo de exercícios cardiovasculares e minimizar a ingestão de gorduras saturadas, colesterol e carboidratos simples em todos os momentos durante a administração ativa de AAS. Também é recomendada a suplementação com óleos de peixe (4 gramas por dia) e uma fórmula natural de colesterol/antioxidante, como Lipid Stabil ou um produto com ingredientes comparáveis.

Efeitos colaterais (supressão de testosterona):

All anabolic/androgenic steroids when taken in doses sufficient to promote muscle gain are expected to suppress endogenous testosterone production. Testosterone is the primary male androgen, and offers strong negative feedback on endogenous testosterone production.Testosterone-based drugs will, likewise, have a strong effect on the hypothalamic regulation of natural steroid hormones. Without the intervention of testosterone-stimulating substances, testosterone levels should return to normal within 1-4 months of drug secession. Note that prolonged hypogonadotrophic hypogonadism can develop secondary to steroid abuse, necessitating medical intervention.

Administração (Geral):

Testosterone hydroalcoholic gel is applied daily (preferably in the morning) to intact, clean, dry skin of the shoulders, upper arms, and/or abdomen. Patients should be careful about transferring testosterone to their female partner(s). The prescribing information for AndroGel® suggests that patients wash their hands immediately with soap and water after application, and also recommends covering the application site(s) with clothing after the gel has dried. Studies with AndroGel® have demonstrated that female partners of male patients noticed as much as a doubling of serum testosterone levels following 15 minutes of rigorous skin-on-skin contact. This contact was initiated between 2 and 12 hours after drug administration. Testosterone transfer was completely avoided when the male subjects wore a shirt.

Administração (Homens):

To treat androgen insufficiency, the prescribing guidelines for AndroGel® recommend initiating therapy with a 5g daily dose (delivering 5 mg of testosterone systemically). Serum testosterone levels are measured after 14 days, at which point the physician may adjust upwards to 7.5g or 10g if necessary. For physique- or performance-enhancing purposes, higher doses would be necessary to achieve supraphysiological levels of testosterone. The most common dose here is 20 grams per day, which delivers approximately 20 mg of testosterone. This level is sufficient for most users to notice significant gains in muscle size and strength. Lower doses are also regularly used by some athletes, but typically when accompanied by other anabolic/androgenic steroids. Testosterone is ultimately very versatile, and can be combined with many other anabolic/androgenic steroids to tailor the desired effect.