AndroGel® (testosterone gel) 1%

AndroGel® (testosterone gel) 1%

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AndroGel® (testosterone gel) 1%

AndroGel (testosterone gel) 1% is a clear, colorless hydroalcoholic gel containing testosterone.

The active pharmacologic ingredient in AndroGel 1% is testosterone, an androgen. Testosterone USP is a white to practically white crystalline powder chemically described as 17-beta hydroxyandrost-4-en-3-one.

Pharmacologically inactive ingredients in AndroGel 1% are carbomer 980, ethanol 67.0%, isopropyl myristate, purified water, and sodium hydroxide. These ingredients are not pharmacologically active.

Indications and usage

AndroGel 1% is indicated for replacement therapy in males for conditions associated with a deficiency or absence of endogenous testosterone:

  • Primary hypogonadism (congenital or acquired).
  • Hypogonadotropic hypogonadism (congenital or acquired).

Limitations of use:

  • Safety and efficacy of AndroGel 1% in men with “age-related hypogonadism” have not been established.
  • Safety and efficacy of AndroGel 1% in males less than 18 years old have not been established.
  • Topical testosterone products may have different doses, strengths or application instructions that may result in different systemic exposure

Mechanism of Action

Endogenous androgens, including testosterone and dihydrotestosterone (DHT), are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include the growth and maturation of prostate, seminal vesicles, penis and scrotum; the development of male hair distribution, such as facial, pubic, chest and axillary hair; laryngeal enlargement, vocal chord thickening, alterations in body musculature and fat distribution. Testosterone and DHT are necessary for the normal development of secondary sex characteristics.

Male hypogonadism, a clinical syndrome resulting from insufficient secretion of testosterone, has two main etiologies. Primary hypogonadism is caused by defects of the gonads, such as Klinefelter’s syndrome or Leydig cell aplasia, whereas secondary hypogonadism is the failure of the hypothalamus (or pituitary) to produce sufficient gonadotropins (FSH, LH).

Dosage and administration

  • Dosage and Administration for AndroGel 1% differs from AndroGel 1.62 %. For dosage and administration of AndroGel 1.62% refer to its full prescribing information.
  • Prior to initiating AndroGel 1%., confirm the diagnosis of hypogonadism by ensuring that serum testosterone has been measured in the morning on at least two separate days and that these concentrations are below the normal range
  • Starting dose of AndroGel 1% is 50 mg of testosterone (two 25 mg packets or one 50 mg packet), applied once daily in the morning.
  • Apply to clean, dry, intact skin of shoulders and upper arms and/or abdomen. Do NOT apply AndroGel 1% to any other parts of the body including the genitals, chest, armpits (axillae), knees, or back.
  • Dose adjustment: AndroGel 1% can be dose adjusted using 50 mg, 75 mg, or 100 mg of testosterone on the basis of total serum testosterone concentration. The dose should be titrated based on the serum testosterone concentration. Additionally, serum testosterone concentration should be assessed periodically.
  • Patients should wash hands immediately with soap and water after applying AndroGel 1% and cover the application site(s) with clothing after the gel has dried. Wash the application site thoroughly with soap and water prior to any situation where skin-to-skin contact of the application site with another person is anticipated.

Contraindications

  • Men with carcinoma of the breast or known or suspected prostate cancer.
  • Women who are pregnant. Testosterone may cause fetal harm.

Warnings and precautions

  • Monitor patients with benign prostatic hyperplasia (BPH) for worsening of signs and symptoms of BPH.
  • Avoid unintentional exposure of women or children to AndroGel 1%. Secondary exposure to testosterone can produce signs of virilization. AndroGel 1% should be discontinued until the cause of virilization is identified.
  • Venous thromboembolism (VTE), including deep vein thrombosis (DVT) and pulmonary embolism (PE) have been reported in patients using testosterone products. Evaluate patients with signs or symptoms consistent with DVT or PE.
  • Some postmarketing studies have shown an increased risk of myocardial infarction and stroke associated with use of testosterone replacement therapy.
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  • Exogenous administration of androgens may lead to azoospermia.
  • Edema, with or without congestive heart failure (CHF), may be a complication in patients with preexisting cardiac, renal, or hepatic disease.
  • Sleep apnea may occur in those with risk factors.
  • Monitor serum testosterone, prostate specific antigen (PSA), hemoglobin, hematocrit, liver function tests, and lipid concentrations periodically.
  • AndroGel 1% is flammable until dry

Adverse reactions

Most common adverse reactions (incidence ≥ 5%) are acne, application site reaction, abnormal lab tests, and prostatic disorders.

Drug interactions

Insulin: Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease insulin requirements.

Oral Anticoagulants: Changes in anticoagulant activity may be seen with androgens, therefore more frequent monitoring of international normalized ratio (INR) and prothrombin time are recommended in patients taking anticoagulants, especially at the initiation and termination of androgen therapy.

Corticosteroids: The concurrent use of testosterone with adrenocorticotropic hormone (ACTH) or corticosteroids may result in increased fluid retention and requires careful monitoring particularly in patients with cardiac, renal or hepatic disease.

Use in specific populations

Pregnancy: AndroGel 1% is contraindicated in pregnant women. Testosterone is teratogenic and may cause fetal harm when administered to a pregnant woman based on data from animal studies and its mechanism of action. Exposure of a female fetus to androgens may result in varying degrees of virilization.

Lactation: AndroGel 1% is not indicated for use in women.

Infertility: Testis disorder, testicular atrophy, and oligospermia have been identified during use of AndroGel 1% .

During treatment with large doses of exogenous androgens, including AndroGel 1%, spermatogenesis may be suppressed through feedback inhibition of the hypothalamic-pituitarytesticular axis. Reduced fertility is observed in some men taking testosterone replacement therapy. Testicular atrophy, subfertility, and infertility have also been reported in men who abuse anabolic androgenic steroids. With either type of use, the impact on fertility may be irreversible.

Pediatric Use: The safety and efficacy of AndroGel 1% in pediatric patients less than 18 years old has not been established. Improper use may result in acceleration of bone age and premature closure of epiphyses.

Geriatric Use: There have not been sufficient numbers of geriatric patients involved in controlled clinical studies utilizing AndroGel 1% to determine whether efficacy in those over 65 years of age differs from younger subjects. Additionally, there is insufficient long-term safety data in geriatric patients to assess the potential risks of cardiovascular disease and prostate cancer. Geriatric patients treated with androgens may also be at risk for worsening of signs and symptoms of BPH.

Drug abuse and dependence

Controlled Substance: AndroGel 1% contains testosterone, a Schedule III controlled substance in the Controlled Substances Act.

Abuse: Drug abuse is intentional non-therapeutic use of a drug, even once, for its rewarding psychological and physiological effects. Abuse and misuse of testosterone are seen in male and female adults and adolescents. Testosterone, often in combination with other anabolic androgenic steroids (AAS), and not obtained by prescription through a pharmacy, may be abused by athletes and bodybuilders. There have been reports of misuse by men taking higher doses of legally obtained testosterone than prescribed and continuing testosterone despite adverse events or against medical advice

Overdosage

There is one report of acute overdosage with use of an approved injectable testosterone product: this subject had serum testosterone concentrations of up to 11,400 ng/dL with a cerebrovascular accident.

Treatment of overdosage would consist of discontinuation of AndroGel 1%, washing the application site with soap and water, and appropriate symptomatic and supportive care.

Storage

Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].

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