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 Testoster...
chapter 22 drugs affecting the reproductive system
• know the pharmacodynamics
and adrs for erectile dysfunction ed
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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 for effectiveness
of finasteride
o Leuprolide: Pituitary, gonadotropic, and gonadal function lab test: misleading results: consider if lab
test reports show unexpected values
o Flutamide: Warfarin: Increased INR and risk of bleeding: monitor INR closely
o 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 different therapy
Estrogens:
Drugs: estrogen (conjugated A/Synthetics)(Cenestin), esterified estrogen/methyltestosterone (Covaryx,
Covaryx HS, EEMT, EEMT HS), estrogen (conjugated B/Synthetic)(Enjuvia), estrogen (esterified)(Menest),
estrogen (conjugated/equine)(Premarin), estrogen (conjugated/equine) and Medroxyprogesterone (Premphase,
Prempro)
Endogenous hormone with multiple actions
Primary role: maturation and function of the female reproductive system
Nonreproductive effects: bone, CV system, CNS, and GI tract
Contraindication: estrogen-only products in women with an intact uterus
o Combo estrogen and progesterone products in these patients
Pharmacodynamics
Estrogen occurs naturally in several forms
Primary sources of estrogen in the normally cycling adult women is the ovarian follicle (70 to 500 mcg of
estradiol daily)
This estradiol is converted to estrone: circulates in about equal amounts to the estradiol and too small
amounts of estriol
After menopause: endogenous estrogen is generated from conversion by peripheral tissues of
androstenedione, secreted by the adrenal cortex, to estrone
Effects of estrogen on the reproductive system
o Maturation of reproductive organs
o Development of secondary sex characteristics
o Regulation of the menstrual cycle
o Endometrial regeneration post menstruation
Other physical effects:
o Closure of long bones after the pubertal growth spurt
o Maintenance of bone density by decreasing the rate of bone resorption through antagonizing the
effects of parathyroid hormone (PTH)
o Maintenance of the normal structure of skin and blood vessels through its actions on the endothelial
cells in the arterial wall, including the induction of NO to facilitate vasodilation and O2 uptake by
cells
o Reduction of the motility of the bowel through its modulation of SNS control over smooth muscle
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