NR 566: Drugs Affecting the
Reproductive System Study
Guide
• Know the pharmacodynamics, pharmacotherapeutics, clinical use, drug
interactions, and ADRs for: Erectile dysfunction (ED) drugs, Estrogens and
Progesterone, and Antiandrogen drugs
• Androgen drugs
• Testosterone is the primary male androgen
• 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
• 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
, • Contraindicated: male breast CA, prostate CA, and Pregnancy (Category
X), and lactation
• Antiandrogens: several different categories
• 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
• 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
• 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)
• 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
• Usually within the first 3 months of therapy
• Baseline and monthly LFTs for the first 4 months of
therapy and periodically
• D/c if any symptoms of hepatic injury or jaundice
develop
• 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
• Finasteride: Nevirapine: Combo induces hepatic metabolism of
finasteride: monitor for effectiveness of finasteride
• Leuprolide: Pituitary, gonadotropic, and gonadal function lab test:
misleading results: consider if lab test reports show unexpected values
• Flutamide: Warfarin: Increased INR and risk of bleeding: monitor INR closely
• Spironolactone:
• renal impairment and agents that affect renal function:
alternation in renal function and electrolytes: monitor K in
young patients with reduced renal function and patients
greater than 65 y/o
• Digitals: may increase or decrease digitalis half-life: Monitor
closely for s/s of dig toxicity and electrolyte and digitalis
levels. Consider alternative Tx.
• Potassium: additive effect increases risk of hyperkalemia: recommend
alternative
• Eplerenone (aldosterone receptor antagonist used
for CHF): severe hyperkalemia: Combination is
contraindicated, do not use together, choose
Reproductive System Study
Guide
• Know the pharmacodynamics, pharmacotherapeutics, clinical use, drug
interactions, and ADRs for: Erectile dysfunction (ED) drugs, Estrogens and
Progesterone, and Antiandrogen drugs
• Androgen drugs
• Testosterone is the primary male androgen
• 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
• 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
, • Contraindicated: male breast CA, prostate CA, and Pregnancy (Category
X), and lactation
• Antiandrogens: several different categories
• 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
• 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
• 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)
• 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
• Usually within the first 3 months of therapy
• Baseline and monthly LFTs for the first 4 months of
therapy and periodically
• D/c if any symptoms of hepatic injury or jaundice
develop
• 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
• Finasteride: Nevirapine: Combo induces hepatic metabolism of
finasteride: monitor for effectiveness of finasteride
• Leuprolide: Pituitary, gonadotropic, and gonadal function lab test:
misleading results: consider if lab test reports show unexpected values
• Flutamide: Warfarin: Increased INR and risk of bleeding: monitor INR closely
• Spironolactone:
• renal impairment and agents that affect renal function:
alternation in renal function and electrolytes: monitor K in
young patients with reduced renal function and patients
greater than 65 y/o
• Digitals: may increase or decrease digitalis half-life: Monitor
closely for s/s of dig toxicity and electrolyte and digitalis
levels. Consider alternative Tx.
• Potassium: additive effect increases risk of hyperkalemia: recommend
alternative
• Eplerenone (aldosterone receptor antagonist used
for CHF): severe hyperkalemia: Combination is
contraindicated, do not use together, choose
