Drugs Used in the Reproductive System

Subtopic:

Androgens

These are primarily male sex hormones. The main androgen is testosterone, predominantly produced in the testes. Smaller quantities of androgens are also generated by the adrenal glands in both sexes and by the ovaries in females.

Testosterone stands out as the most crucial naturally occurring androgen. In adult males, the body typically produces 8-10mg daily. The secretion of testosterone is regulated by gonadotropins and gonadotropin-releasing hormone (GnRH). Insufficient androgen production can arise from pituitary gland dysfunction or atrophy, testicular injury, or removal. Androgens are vital for promoting the development of male characteristics.

Naturally Occurring Androgens:

  • Testosterone: The primary androgenic hormone, synthesized by the Leydig cells within the testes.

  • Dehydroepiandrosterone (DHEA): Produced by the adrenal cortex.

Common Terminology

  • Anabolic steroids: Synthetic androgens designed to emphasize protein-building (anabolic) effects over the development of male characteristics (androgenic) effects.

  • Androgenic effects: The effects linked to the development of male sexual characteristics and secondary sexual characteristics. These include features like a deepened voice, changes in hair distribution, genital maturation, and acne.

  • Androgens: A class of male sex hormones, with testosterone being the most prominent. They are primarily produced in the testes and adrenal glands.

  • Hirsutism: A pattern of hair distribution resembling male secondary sexual characteristics in women. This includes increased hair growth on the trunk, arms, legs, and face.

  • Hypogonadism: A condition characterized by the underdevelopment of the gonads, specifically the testes in males.

  • Penile Erectile Dysfunction: The inability to achieve or maintain a penile erection due to insufficient blood flow to the corpus cavernosum. This can be associated with aging, neurological disorders, or vascular issues.

Examples of Androgens

Drug NameUsual DosageUsual Indications
danazol (Danocrine)100–600 mg/day PO, varies by use and responsePrevent ovulation in endometriosis treatment; prevention of hereditary angioedema.
fluoxymesterone (Androxy)5–20 mg/day PO for replacement; 10–40 mg/day PO for breast cancersTreat delayed puberty in males and certain breast cancers in postmenopausal women.
testosterone (Androderm, Depo-testosterone)50–400 mg IM every 2–4 weeks, varies by preparation; patch 4–6 mg/day dailyReplacement therapy for hypogonadism (refer to detailed information below).
methyltestosterone (Testred, Virilon)Males: 10–50 mg/day PO; Females: 50–200 mg/day POReplacement therapy for hypogonadism; treat delayed puberty in males; manage specific breast cancers in postmenopausal women.

TESTOSTERONE (Depo-Testosterone, Androderm)

  • Classification:

    • Therapeutic: Hormone

    • Pharmacological: Androgen

    • Pregnancy Category: X (Contraindicated in pregnancy)

    • Schedule III Controlled Substance (in some regions)

  • Dosage:

    • 50–400 mg via intramuscular (IM) injection every 2–4 weeks, dosage varies with the specific formulation. Some long-acting depot forms are available.

    • Dermal patch: 4–6 mg/day, applied and replaced daily.

  • Effects of Testosterone:

    • Anabolic Effects (Growth and Metabolic Functions):

      • Maintains bone density and strength.

      • Regulates the distribution of body fat.

      • Supports the production of red blood cells.

      • Promotes muscle growth, strength, and overall body mass.

      • Facilitates recovery from injuries.

      • Enhances the retention of essential minerals like nitrogen, sodium, potassium, and phosphorus within the body.

      • Reduces calcium excretion in urine.

      • Increases protein anabolism (synthesis) and decreases protein catabolism (breakdown), leading to a net gain in protein.

    • Androgenic Effects (Sexual Characteristics and Functions):

      • Boosts sex drive and libido.

      • May increase aggressive tendencies.

      • Can contribute to acne development.

      • Stimulates beard and body hair growth.

      • Associated with male pattern baldness in predisposed individuals.

      • Essential for the development and maintenance of male reproductive organs.

      • Supports spermatogenesis (sperm production).

      • Can increase the size of the prostate gland.

  • Control of Testosterone Secretion:

    The hypothalamus releases Gonadotropin-Releasing Hormone (GnRH), which signals the anterior pituitary gland to secrete Follicle-Stimulating Hormone (FSH) and Luteinizing Hormone (LH). LH then stimulates Leydig cells in the testes to produce testosterone. A negative feedback loop is in place: elevated levels of testosterone in the bloodstream signal the anterior pituitary gland and hypothalamus to reduce the secretion of LH and GnRH, respectively, thus regulating testosterone production.

  • Indications:

    1. Hypogonadism and impotence in males resulting from testicular, pituitary, or hypothalamic deficiencies.

    2. Confirmed testosterone deficiency.

    3. Palliative treatment for breast cancer in postmenopausal women when surgery is not an option.

    4. Management of delayed puberty in adolescent males.

    5. Historically used for prevention of postpartum breast engorgement (less common now).

    6. Illicit use by athletes for muscle enhancement and performance improvement (anabolic steroids).

    7. To block follicle-stimulating hormone and luteinizing hormone release in women, preventing ovulation in the treatment of endometriosis.

    8. Prevention of hereditary angioedema.

  • Contraindications:

    • Known allergy to androgens or any component of the formulation to avoid hypersensitivity reactions.

    • Pregnancy and lactation due to potential risks to the fetus or neonate. Androgens may pass into breast milk.

    • Presence or history of prostate or breast cancer, as testosterone can exacerbate these conditions.

    • Pre-existing liver dysfunction or cardiovascular disease, which can be worsened by androgen therapy.

    • Black Box Warning (Topical Testosterone): Risk of virilization in children through secondary exposure.

    • Black Box Warning (Danazol): Risks of thromboembolic events, fetal abnormalities, hepatitis, and intracranial hypertension.

    • Use with caution in patients with diabetes mellitus, benign prostatic hyperplasia (BPH), and sleep apnea.

  • Side Effects and Adverse Effects of Testosterone:

    • In Men:

      • Gynecomastia (breast enlargement).

      • Testicular atrophy.

      • Suppression of testicular function.

      • Impotence or erectile dysfunction.

      • Penile enlargement (priapism – prolonged, painful erection).

      • Nausea and vomiting.

      • Jaundice.

      • Headache.

      • Anxiety.

      • Male pattern baldness.

      • Acne.

      • Depression.

      • Fatigue.

      • Abdominal cramps.

      • Confusion.

      • Deepening of voice.

      • Edema (fluid retention).

      • Drug-induced hepatitis.

      • Gingivitis.

      • Hirsutism (increased body hair).

    • In Women (receiving androgens for breast carcinoma):

      • Amenorrhea (absence of menstruation).

      • Virilization: Development of male secondary sexual characteristics, including changes in body and facial hair, deepened voice, acne, menstrual irregularities, and clitoral enlargement.

  • Drug Interactions:

    1. May enhance the effects of anticoagulants (like warfarin), oral hypoglycemic agents, and insulin, potentially increasing the risk of bleeding or hypoglycemia.

    2. Concurrent use with corticosteroids may elevate the risk of edema.

  • Nursing Interventions/Involvement:

    • For buccal tablets, instruct the patient on proper placement in the mouth and advise against swallowing, chewing, smoking, or drinking until dissolved.

    • For injections, administer deep intramuscularly into the gluteal muscle.

    • Administer oral testosterone with or just before meals to minimize gastrointestinal upset.

    • For transdermal systems (e.g., Testoderm), apply to clean, dry scrotal skin, shaving hair for optimal contact.

    • Monitor fluid intake and output.

    • Monitor weight twice weekly.

    • Assess for and report edema.

    • Monitor for secondary sexual characteristics in men.

    • Monitor for menstrual irregularities and voice deepening in women.

    • Periodically monitor hemoglobin and hematocrit levels.

    • Monitor urine and serum calcium levels.

  • Patient/Family Teaching:

    1. Instruct patients to report signs of priapism, urinary difficulties, hypercalcemia, edema, unexplained weight gain, swelling in extremities, hepatitis symptoms, or unusual bleeding.

    2. Explain the dangers of using testosterone to enhance athletic performance.

    3. Advise women to notify their doctor if pregnancy is suspected or confirmed.

    4. Patients with diabetes mellitus should closely monitor blood glucose levels as medication adjustments may be needed.

    5. Emphasize the importance of regular follow-up appointments, laboratory tests, and physical examinations.

    6. For female patients, advise reporting any signs of male-pattern hair growth, voice deepening, or menstrual irregularities.

ANABOLIC STEROIDS

These are synthetic androgens designed to be less readily converted to the potent androgen dihydrotestosterone (DHT). This results in reduced androgenic effects but enhanced anabolic (protein-building) effects.

Commonly misused anabolic steroids by athletes include nandrolone, stanozolol, and methenolone. These are controlled substances, making their non-medical use illegal.

Clinical Uses/Indications of Anabolic Steroids:

  • Osteoporosis management.

  • Appetite stimulation and improvement of well-being in certain conditions.

  • Counteracting osteoporosis induced by chronic glucocorticosteroid therapy.

  • Promoting linear growth in prepubertal boys (height increase).

  • Used in managing some renal diseases.

Examples of Anabolic Steroids:

  • NANDROLONE:

    • A naturally occurring steroid, also synthesized under trade names like Deca-Durabolin and Durabolin.

    • Has been associated with illegal performance enhancement in professional sports.

  • STANOZOLOL:

    • A synthetic steroid, brand name Winstrol.

    • Notably available in oral form.

    • Illegally used by athletes for rapid strength gains.

  • OXANDROLONE:

    • Synthetic steroid, brand name Anavar.

    • Approved for use in osteoporosis treatment.

    • Misused by bodybuilders for muscle growth.

Contraindications of Anabolic Steroids:

  • Male patients with breast cancer or known/suspected prostate carcinoma.

  • Breast cancer in women with hypercalcemia.

  • Pregnancy (due to potential masculinization of a female fetus).

  • Nephrosis or the nephrotic phase of nephritis.

Side Effects of Anabolic Steroids:

  • Severe acne, oily skin and hair, and hair loss (virilization).

  • Liver diseases and complications (heart attack, stroke).

  • Mood alterations, irritability, increased aggression, depression, suicidal tendencies.

  • Changes in cholesterol and blood lipid profiles.

  • Hypertension.

  • Gynecomastia (breast enlargement in men).

  • Testicular shrinkage.

  • Azoospermia (absence of sperm in semen).

  • Menstrual irregularities in women.

  • Infertility.

  • Excessive facial or body hair and deepening voice in women.

  • Stunted growth in teenagers.

  • Risk of viral or bacterial infections from non-sterile injections.

  • Edema.

  • Prostate cancer risk.

  • Injury from skin contact with topical testosterone gels or solutions.

Drug Interactions of Anabolic Steroids:

  • Anticoagulants: Anabolic steroids can enhance sensitivity to oral anticoagulants, potentially requiring a reduction in anticoagulant dosage to maintain therapeutic prothrombin time. Close monitoring is essential when starting or stopping anabolic steroid therapy in patients on oral anticoagulants.

Patient Information Regarding Anabolic Steroids:

  • Instruct patients to report any of the following: hoarseness, acne, menstrual changes, increased facial hair, nausea and vomiting, skin color changes, or ankle swelling.

ANTI-ANDROGENS

Also known as androgen antagonists or testosterone blockers, these drugs prevent androgens from exerting their biological effects. They function by blocking androgen receptors and/or inhibiting androgen production.

Examples of Anti-Androgens:

  • Danazol

  • Finasteride

  • Spironolactone

  • Flutamide

  • Cyproterone

  • Ketoconazole

  • Bicalutamide

  • Nilutamide

Finasteride

  • Available Preparations: Tablets, 5mg and 1mg

  • Available Brands: Finest, Proscar, Propecia (1mg for hair loss)

Finasteride is a synthetic androgen hormone inhibitor that prevents the conversion of testosterone to dihydrotestosterone (DHT). DHT plays a key role in prostate gland development. By reducing DHT levels, finasteride lessens its effect on the prostate, leading to a decrease in prostate size and associated symptoms of benign prostatic hyperplasia (BPH).

  • Indications:

    • Benign Prostatic Hyperplasia (BPH).

    • Androgenetic alopecia (male pattern baldness) in men only (lower dose formulation).

  • Mechanism of Action:

    Finasteride inhibits the enzyme 5-alpha-reductase. This enzyme is responsible for converting testosterone into DHT in the prostate, liver, and skin. DHT contributes to both prostatic hyperplasia and hair loss.

  • Dose:

    • BPH: 5mg once daily.

    • Alopecia: 1mg daily, for at least 3 months or longer for noticeable effects.

  • Side Effects:

    • Decreased libido (sexual desire).

    • Reduced ejaculate volume.

    • Erectile dysfunction/impotence.

    • Breast tenderness and enlargement (gynecomastia).

    • Testicular pain.

  • Contraindications/Precautions:

    • Known hypersensitivity to finasteride.

    • Use with caution in patients with hepatic impairment as it is metabolized in the liver.

  • Nursing Implications:

    • Assess for symptoms of prostatic hyperplasia (e.g., incomplete bladder emptying, interrupted urinary stream).

    • Digital rectal examination should be performed before and periodically during BPH therapy.

    • Monitor prostate-specific antigen (PSA) levels, as finasteride can lower PSA levels, which is a marker used in prostate cancer screening.

    • Administer the drug without regard to meals.

  • Patient/Family Teaching:

    1. Finasteride poses a risk to a male fetus. Advise males to avoid sexual contact with pregnant women or use condoms to prevent exposure.

    2. Inform the doctor immediately if a sexual partner is or may become pregnant, as medication discontinuation or condom use may be necessary to avoid fetal risk.