In Brief: Azmiro A Single-Dose Injectable Formulation of Testosterone Cypionate The Medical Letter Inc

Testosterone Cypionate Injection, USP100 mg mL and 200 mg mL

Testosterone is in a class of medications called androgenic hormones. Testosterone is a hormone produced by the body that contributes to the growth, development, and functioning of the male sexual organs and typical male characteristics. Testosterone injection works by supplying synthetic testosterone to replace the testosterone that is normally produced naturally in the body. When used to treat breast cancer, testosterone works by stopping the release of estrogen. A multi-center, prospective randomized trial compared the PKs, efficacy, and safety of the transdermal system to IM testosterone enanthate (TE) injections (25). Treatment was for 24 weeks and 33 subjects were enrolled per group. For the transdermal system group, the starting dose was 5 mg/day (2×2.5 mg/day patches, no longer commercially available).

Both options are supplied in 100 mg/mL (10 mL) and 200 mg/mL (1 and 10 mL) concentrations, prepared in cottonseed oil. The USA FDA recommended starting dose for male hypogonadism is 50 to 400 mg IM every 2 to 4 weeks (41). The Endocrine Society Clinical Practice Guidelines for testosterone therapy suggest an alternative of either 75 to 100 mg IM weekly or 150 to 200 mg IM every 2 weeks (3). The efficacy of the transdermal patch is often limited by lack of adherence or discontinuation due to skin blistering, pruritus, or irritation. This is due to permeation enhancers included in the transdermal system which are necessary to increase absorption.

Regular use can lead to improved strength, faster recovery, and increased lean mass (Snyder et al., 2000). These benefits make it a preferred compound among athletes and bodybuilders. Testosterone levels generally peak during adolescence and early adulthood. As you age, your testosterone level gradually declines — typically about 1% a year after age 30 or 40. For older men, it’s important to determine if a low testosterone level is due to normal aging or if it is due to a disease (hypogonadism).

If you have any questions, consult your doctor or pharmacist. Testosterone is a controlled substance because it can be misused or lead to dependence. Store testosterone in a safe place to protect it from theft. Testosterone should not be used if you have prostate cancer or certain types of breast cancer. Certain testosterone injectable products and testosterone pellets may also be used to help start puberty in boys with delayed puberty. There have been no reports of acute overdosage with the androgens.

Free thyroid hormone levels remain unchanged, however, and there is no clinical evidence of thyroid dysfunction. Androgens may decrease levels of thyroxine­binding globulin, resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. The time-course for the spectrum of effects of testosterone may vary considerably, as testosterone actions are exerted through a cascade of many different pathways. Most of the actions of testosterone take place via the androgen receptor as a transcription factor activated by testosterone. Over the past two decades evidence of rapid responses to androgens, dependent or independent of the androgen receptor, occurring at the cellular and organ level has accumulated.

The patient experiences, to his satisfaction, profound changes in his physical appearance and his mental makeup. The attending physician observes the changes the patient undergoes and rarely fails to be fascinated by the multitude of functions testosterone appears to have in the process of masculinization in the broadest sense (1). Talk with your doctor about other drug options that may work for you. Testosterone cypionate is given by injection into a muscle (usually the buttocks).

Low testosterone levels in males can lead to mood changes, difficulty concentrating, erectile dysfunction (trouble getting or keeping an erection), and low sex drive. It can also cause reduced growth of the penis and testicles, gynecomastia (breast growth), loss of body hair and muscle mass, anemia (low level of red blood cells), and osteoporosis (weakened bones). In addition, androgens have been linked to increased risk of heart disease, including congestive heart failure, heart attack and stroke. Appropriate studies on the relationship of age to the effects of testosterone cypionate injection have not been performed in the geriatric population. However, elderly patients are more likely to have heart or prostate problems (including enlarged prostate), which may require caution in patients receiving this medicine.

The FDA has only approved testosterone for hypogonadism in cases where it is the result of an underlying medical condition rather than aging. Women should inform their care team if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child. Talk with your care team about your birth control options while taking this medication. If you have diabetes, check with your care team before you change your diet or the dose of your diabetic medication. Talk to your medical provider about testosterone tablets, gels, or patches. The upfront cost may be more, but these forms don’t involve additional fees for the injection.

Other testosterone cypionate 250 mg injections such as testosterone enanthate have about the same retail price. However, other formats such as generic testosterone tablets, gels, or transdermal patches may be cheaper. Even if the price is higher, they won’t include extra charges involved with injecting a drug.