NR 566 Week 6 Study Guide
Chapter 22: Drugs Affecting the Reproductive System
• Know the pharmacodynamics, pharmacotherapeutics, clinical use, drug interactions, and ADRs for:
Erectile dysfunction (ED) drugs, Estrogen
...
NR 566 Week 6 Study Guide
Chapter 22: Drugs Affecting the Reproductive System
• Know the pharmacodynamics, pharmacotherapeutics, clinical use, drug interactions, and ADRs for:
Erectile dysfunction (ED) drugs, Estrogens and Progesterone, and Antiandrogen drugs
• Androgen drugs
o Testosterone is the primary male androgen
o Responsible for:
▪ Growth, maturation, and maintenance of male sex organs and secondary sexual
characteristics
▪ Skeletal growth spurt in adolescence and termination of linear growth by fusion of the
epiphyseal growth plate
▪ Activation of sebaceous glands (acne during puberty)
▪ Enhances production of erythropoietic stimulating factor, increased RBCs production
▪ Libido
o Androgen Drugs: testosterone propionate (in oil, DepoTesterone), testosterone enanthate (in oil,
Delatestryl), testosterone cypionate (in oil, Depo-Testosterone), methyltestosterone (Android,
Methitest, Testred, Virilon), testosterone gel (AndroGel 1%, AndroGel 1.62%, Axiron, Testium),
fluoxymesterone, TD testosterone (Testoderm, Androderm), and buccal testosterone (Striant)
▪ Used to treat Indicated for the symptomatic Tx of
• 1) deficiency states in males associated with hypogonadism and
• 2) in both sexes for d/os such as CA and HIB, Tx libido, endometriosis, and
postmenopausal symptoms in women, have been used illicitly to enhance athletic
performance and increase muscle mass
o Contraindicated: male breast CA, prostate CA, and Pregnancy (Category X), and lactation
• Antiandrogens: several different categories
o Androgen hormone inhibitors (5-alpha-reductase inhibitors)
▪ Drugs: Finasteride (Propecia, Proscar) and dutasteride (Avodart)
▪ MOA: Block conversation of testosterone to dihydrotesterone
▪ Used to Tx BPH
▪ PSA levels and digital prostate examination are required monitoring for men on these agents
▪ Finasteride (Propecia, Proscar):
• Extensive hepatic metabolism
• BPH: 5mg/day, 6 to 12 months of therapy until therapeutic response
o Regression of prostate size increased urinary flow, and improve BPH
symptoms
• Approved for Male pattern baldness: 1 mg/day, three months until results
• Stopping the drugs reverses the effect within 12 months
• ADRs: decreased libido, impotence (can occur at both doses)
▪ Dutasteride (Avodart)
• Inhibits both type 1 and 2 (5-alpha-reductase)
• Peak clinical effect 6 to 12 months of therapy
• Extensively metabolized in the liver (CYP3A4 and CYP3A5)
• Used to Tx BPH
• Absorbed through the skin, women who are pregnant or may become pregnant should
not handle dutasteride capsules r/t risk of fetal anomaly to a male fetus
• ADR: decreased libido and impotence
o Gonadotropin-releasing hormone analogue: luteinizing hormone-releasing hormone
antagonist
▪ Leuprolide acetate (Lupron)
▪ Create a reversible chemical orchiectomy state in males and an oophorectomy state in
females
▪ Used to Tx: advanced prostatic CA and for management of endometriosis and uterine
leiomyomata (fibroids)
▪ 1 mg SC daily or IM every 3 months (depot formulation)
▪ Increased suppression when used with flutamide (direct antiandrogen)
▪ Peds: Tx central precocious puberty
▪ Women: reducing uterine fibroids, endometriosis, and PCOS (pain relief, regain fertility)
o Direct antiandrogens
▪ Flutamide (Eulexin), bicalutamide (Casodex), and nilutamide (Nilandron)
▪ Inhibit androgen uptake or nuclear binding of androgen at target tissues
▪ Uses as part of combo therapy Tx of prostatic carcinoma
▪ Flutamide: competitive antagonist at the androgen receptor site
• Truly a nonsteroidal agent
• ADRs: gynecomastia and reversible liver toxicity
• Renal doses: less than 29 mL/min
• BLACK BOX WARNING: hepatic failure, hepatic encephalopathy, and death
o Usually within the first 3 months of therapy
o Baseline and monthly LFTs for the first 4 months of therapy and periodically
o D/c if any symptoms of hepatic injury or jaundice develop
o Spironolactone (Aldactone): aldosterone antagonist and inhibitor of 5-alpha-reductase
▪ used as a K sparing diuretic
▪ Off label use for Tx of female hirsutism and acne due to antiandrogenic properties
• 50 to 200 mg/day
▪ Competitive inhibitor of the dihydrotestosterone, aldosterone, and interferes with the
androgen receptors in the prostate
• Also reduces 17-alpha-hydroxylase activity: lowers plasma levels of testosterone and
androstenedione
▪ Metabolized by the liver
▪ Short term use for primary hyperaldosteronism in patients preoperatively
▪ Long term: for those who are not good candidates for Sx with idiopathic hyperaldosteronism
▪ PMS/PMDD symptoms may be relieved by spironolactone (25 mg QID beginning on day 14
of the menstrual cycle)
▪ ADRs: dose-related and reversible when the drug is d/c GI upset, drowsiness, gynecomastia,
impotence, cutaneous eruptions, and urticaria
▪ BLACK Box Warning: r/t animal chronic toxicity studies demonstrated tumorigenicity
▪ Contraindications: pregnancy
• Drug Interactions
o Finasteride: Nevirapine: Combo induces hepatic metabolism of finasteride: monitor f
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