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Pharmacology for Nurses

36.6 Androgens, Antiandrogens, and Anabolic Steroids

Pharmacology for Nurses36.6 Androgens, Antiandrogens, and Anabolic Steroids

Learning Outcomes

By the end of this section, you should be able to:

  • 36.6.1 Identify the characteristics of androgen, antiandrogen, and anabolic steroid drugs used to treat reproductive disorders.
  • 36.6.2 Explain the indications, actions, adverse reactions, and interactions of androgen, antiandrogen, and anabolic steroid drugs used to treat reproductive disorders.
  • 36.6.3 Describe nursing implications of androgen, antiandrogen, and anabolic steroid drugs used to treat reproductive disorders.
  • 36.6.4 Explain the client education related to androgen, antiandrogen, and anabolic steroid drugs used to treat reproductive disorders.

Androgens, antiandrogens, and anabolic steroids drugs are natural and synthetic forms of testicular hormones. They are used to treat hypogonadism, delayed male puberty, and some types of female breast cancer. They can also be used off-label for stimulation of appetite and to increase muscle mass in malignancy and acquired immunodeficiency syndrome (AIDS) (Ganesan et al., 2023).

Androgens

Androgens are sex hormones. Testosterone is the primary androgen and is produced in the testes. The other androgens are produced in the adrenal glands. Testosterone is responsible for the growth and development of male sex organs and the secondary sex characteristics such as voice deepening, hair distribution, and redistribution of muscle and fat. It also contributes to bone growth, red blood cell production, decreased excretion of calcium in the urine, and the retention of sodium, potassium, and phosphorous.

Hypogonadism is the condition where the testes are undeveloped and fail to produce androgen, sperm, or both. Males with hypogonadism do not experience puberty. Delayed puberty is when the sex characteristics do not develop at the expected time in puberty. Clients experiencing either condition may need exogenous hormone therapy to develop sex organs and secondary sex characteristics.

The prototype androgen is testosterone. It comes in oral, parenteral, topical, implantable, and buccal forms. Dosage and frequency vary depending on the form of the drug and the individual need of the client. Table 36.20 lists common androgens and typical routes and dosing for adult clients.

Drug Routes and Dosage Ranges
Testosterone
(Depo-testosterone, Androderm)
Male hypogonadism/delayed puberty:
Depo-testosterone: 50–400 mg intramuscularly every 2–4 weeks.
Androderm: 4 mg/day transdermal patch (adjusted per serum testosterone concentration).
Fluoxymesterone
(Halotestin)
Male hypogonadism/delayed puberty: 5–20 mg daily orally.
Breast cancer treatment in postmenopausal females: 10–40 mg/day orally.
Methyltestosterone
(Methitest)
Hypogonadism, delayed puberty in males: 10–50 mg daily orally.
Breast cancer treatment in postmenopausal females: 50–200 mg/day orally.
Table 36.20 Drug Emphasis Table: Androgens (source: https://dailymed.nlm.nih.gov/dailymed/)

Adverse Effects and Contraindications

The adverse effects of testosterone for males include gynecomastia, prolonged penile erections, and decreased ejaculatory volume. For females taking testosterone for advanced breast cancer, side effects are generally related to masculinization—voice deepening, clitoral enlargement, and hirsutism. Menstrual irregularities and amenorrhea may develop in premenopausal clients.

Androgens are contraindicated in hypersensitivity to the drug, male breast and prostate cancer, and serious cardiac, hepatic, or renal disease. Additionally, testosterone must be used cautiously in prepubescent clients because of the possibility of early bone maturation and early closure of the epiphyseal growth plates. This condition can lead to stunted growth. When young clients are on testosterone therapy, they need radiographs every 6 months to monitor bone maturation.

Clients with preexisting gynecomastia may have a worsening of the condition. Older clients may have an increased risk of benign prostatic hyperplasia (BPH) and prostate cancer. Clients with BPH may develop urethral obstruction. Testosterone is contraindicated for pregnant clients because it can cause masculinization of the female fetus, and the risks of the drug outweigh the potential benefits for pregnant clients. See Urinary and Bladder Disorder Drugs for more about BPH and its treatment.

Table 36.21 is a drug prototype table for androgens featuring testosterone. It lists drug class, mechanism of action, adult dosage, indications, therapeutic effects, drug and food interactions, adverse effects, and contraindications.

Drug Class
Androgen

Mechanism of Action
Binds to and activates androgen receptors
Drug Dosage
Male hypogonadism/delayed puberty:
Depo-testosterone: 50–400 mg intramuscularly every 2–4 weeks.
Androderm: 4 mg/day transdermal patch (adjusted per serum testosterone concentration).
Indications
Replacement therapy in conditions associated with symptoms of deficiency or absence of endogenous testosterone

Therapeutic Effects
Development of male sex characteristics
Drug Interactions
Oral anticoagulants
May decrease blood glucose levels in clients with diabetes, so hyperglycemic drug doses may need to be decreased

Food Interactions
No significant interactions
Adverse Effects
Hypercalcemia in immobilized clients
Gynecomastia
Excessive frequency and duration of penile erections
Hirsutism
Male pattern baldness
Seborrhea
Acne
Nausea
Cholestatic jaundice
Alterations in liver function tests
Venous thromboembolism
Increased or decreased libido
Headache
Anxiety
Depression
Contraindications
Known hypersensitivity to the drug
Male breast cancer
Prostate cancer
Pregnancy
Serious cardiac, hepatic, or renal disease

Caution:
Benign prostatic hyperplasia
Table 36.21 Drug Prototype Table: Testosterone (source: https://dailymed.nlm.nih.gov/dailymed/)

Antiandrogens

Antiandrogens are medications that compete with testosterone for androgen-receptor binding sites; in other words, they work against androgens and testosterone. Antiandrogens either prevent these hormones from binding to proteins in the target cells or decrease the amount of a hormone produced. Antiandrogens are used to treat advanced prostate cancer. Bicalutamide is the primary medication used. It should be taken in combination with a gonadotropin-releasing hormone analog to treat metastatic prostate cancer.

Antiandrogens are frequently used in combination with gonadotropin-releasing hormone analogs to treat advanced prostate cancer (Freedland & Abrahamsson, 2021). These two groups of medications have different mechanisms of action, but both decrease testosterone to nonexistent levels comparable to surgical castration.

Adverse Effects and Contraindications

Contraindications for the use of antiandrogens are allergy to the drug or its components and liver dysfunction or elevated liver enzymes. The adverse effects of antiandrogens include gynecomastia, breast pain, hot flashes, decreased libido, impotence, diarrhea, anemia, and abnormal liver function. Liver failure can occur.

Table 36.22 is a drug prototype table for antiandrogens featuring bicalutamide. It lists drug class, mechanism of action, adult dosage, indications, therapeutic effects, drug and food interactions, adverse effects, and contraindications.

Drug Class
Antiandrogen

Mechanism of Action
Inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue
Drug Dosage
50 mg orally daily (along with a luteinizing hormone–releasing hormone [LHRH] analog).
Indications
Treatment of stage D2 metastatic carcinoma of the prostate

Therapeutic Effects
Stops the growth and spread of cancer cells
Drug Interactions
Coumadin

Food Interactions
No significant interactions
Adverse Effects
Pain (general)
Back pain
Asthenia
Pelvic pain
Infection
Abdominal pain
Chest pain
Headache
Flu syndrome
Hot flashes
Nausea
Leg cramps
Hypercholesteremia
Elevated liver enzymes
Gynecomastia
Contraindications
Known hypersensitivity to the drug or its components
Use in female clients
Pregnancy
Table 36.22 Drug Prototype Table: Bicalutamide (source: https://dailymed.nlm.nih.gov/dailymed/)

Anabolic Steroids

Anabolic steroids are analogues of testosterone developed for use in tissue building in conditions such as illness or surgery that have caused significant wasting of tissue, weight loss, and depletion of red blood cells. Oxandrolone is the primary anabolic steroid. It is indicated for weight gain and cancer treatment. The dosage for oxandrolone is 2.5 mg–20 mg, two to four times daily, administered orally.

Both androgens and anabolic steroids stimulate protein synthesis in skeletal muscle and thus increase the buildup of cellular tissue. They also stimulate increased production of red blood cells. For those reasons, androgens and anabolic steroids are used in clients who are debilitated by chronic illnesses (e.g., cancer, HIV, anemias), trauma, long-term steroid use, or surgery in order to increase muscle mass, gain weight, repair tissue, and increase red blood cell count (Ganesan et al., 2023).

Adverse Effects and Contraindications

In general, anabolic steroids can cause electrolyte imbalances, liver damage, insomnia, weight gain, acne, depression, anxiety, aggression, increased cholesterol and low-density lipoprotein levels, hypertension, and changes in the structure of the left ventricle of the heart (DailyMed, Oxandrolone tablet, 2022).

The adverse effects in prepubertal clients include phallic enlargement, hirsutism, and increased skin pigmentation. In postpubertal clients, side effects can include decreased testicular function and testicular atrophy, gynecomastia, priapism, baldness, and changes in libido. Prostate problems, especially in older clients, may also be a side effect of these drugs. Female clients may experience hirsutism, voice deepening, clitoral enlargement, baldness, reduced breast volume, and menstrual irregularities (DailyMed, Oxandrolone tablet, 2022).

These medications are contraindicated in allergy to the drug, pregnancy and lactation, liver or coronary heart disease, nephrosis, hypercalcemia, and breast or prostate cancer in males (DailyMed, Oxandrolone tablet, 2022).

All anabolic steroids are DEA Schedule III drugs; however, anabolic steroids and testosterone have been misused by many athletes, both professional and amateur, for the purposes of bodybuilding and enhancing physical performance in sports (Chegeni et al., 2021; Ganesan et al., 2023; Schneider et al., 2020). These drugs are not approved to be used for bodybuilding or enhancing physical performance and, thus, are not prescribed by health care professionals for those purposes, nor are they permitted by athletic competition boards.

Table 36.23 is a drug prototype table for anabolic steroids featuring oxandrolone. It lists drug class, mechanism of action, adult dosage, indications, therapeutic effects, drug and food interactions, adverse effects, and contraindications.

Drug Class
Anabolic steroid

Mechanism of Action
Inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue
Drug Dosage
2.5–20 mg orally given in 2–4 divided doses.
Indications
Adjunctive therapy to offset the protein catabolism associated with prolonged administration of corticosteroids

Therapeutic Effects
Relief of the bone pain frequently accompanying osteoporosis
Weight gain and muscle building
Drug Interactions
Coumadin
Oral hypoglycemic medications
Adrenal steroids or adrenocorticotropic hormone (ACTH)

Food Interactions
No significant interactions
Adverse Effects
Cholestatic jaundice
Habituation
Excitation
Insomnia
Depression
Changes in libido
Edema
Retention of serum electrolytes (sodium chloride, potassium, phosphate, calcium)
Decreased glucose tolerance
Increased creatinine excretion
Increased serum creatinine phosphokinase (CPK)
Inhibition of gonadotropin secretion
Hepatic necrosis and death (rare)
In Prepubertal Males:
Phallic enlargement and increased frequency or persistence of erections
In Postpubertal Males:
Inhibition of testicular function
Testicular atrophy
Oligospermia
Impotence
Chronic priapism
Epididymitis
Bladder irritability
Gynecomastia
In Females:
Clitoral enlargement
Menstrual irregularities
Deepening of the voice
Hirsutism and male pattern baldness
Masculinization of the fetus
Contraindications
Known hypersensitivity to the drug or its components
Use in female clients
Pregnancy
Known or suspected prostate or male breast cancer
Female breast cancer with hypercalcemia
Nephrosis
Hypercalcemia

Caution:
Clients with moderate to severe chronic obstructive pulmonary disease (COPD) and who are unresponsive to bronchodilators should be monitored closely for COPD exacerbation and fluid retention
Table 36.23 Drug Prototype Table: Oxandrolone (source: https://dailymed.nlm.nih.gov/dailymed/)

Nursing Implications

The nurse should do the following for clients who are taking androgens, antiandrogens, anabolic steroids, or GnRH analogues:

  • Determine the reason for use of androgens, antiandrogens, anabolic steroids, or GnRH analogues.
  • Assess understanding of indication for specific drug therapy and ability to comprehend instructions.
  • Perform gender- and age-appropriate physical assessment, including height, weight, and blood pressure.
  • Assess past medical history and family history for cardiovascular disease (heart attack, stroke, hypertension), pregnancy/lactation status, breast or prostate cancer, gynecomastia, and BPH.
  • Obtain medication list including OTC and herbal remedies.
  • Assess smoking history and use of alcohol.
  • Obtain pertinent diagnostic testing such as long bone radiographs and laboratory studies for liver and renal function, complete blood count, serum chemistries, and lipids, and monitor as necessary.
  • Assess ability to administer drug at home and follow medication regimen.
  • Monitor for any misuse of drug therapy.
  • Provide client teaching regarding the drug and when to call the health care provider. See below for client teaching guidelines.

Client Teaching Guidelines

The client taking an androgen, antiandrogen, anabolic steroid, or GnRH analogue should:

  • Understand the medication’s purpose, side effects, contraindications, and precautions.
  • Understand the medication dosage and route and be able to self-administer correctly (oral, patch, injections).
  • Monitor any signs and symptoms of adverse effects and report those that require immediate attention.
  • Monitor and record pertinent observations such as weight, height, and blood pressure as instructed.
  • Monitor and report emotional and/or behavioral changes to health care provider.
  • Know how to manage the side effects of various hormonal medications.
  • Understand drug, food, and/or herbal interactions that could be harmful. See drug prototype tables for specific drugs.
  • Verbalize the importance of follow-up appointments to manage the medication regimen and to observe for adverse effects.

The client taking an androgen, antiandrogen, anabolic steroid, or GnRH analogue should not:

  • Alter the dosage or abruptly discontinue these medications.
  • Smoke or consume alcohol.

FDA Black Box Warning

Oxandrolone

Oxandrolone can cause serious liver problems, including hepatitis and tumors, and serum lipid changes that could cause coronary heart disease.

Oxandrolone may accelerate bone maturation without producing compensatory gain in linear growth, a condition called premature closure of epiphyses in children. This adverse effect results in compromised adult height.

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