chapter 22 drugs affecting the reproductive system
chapter 31 contraception
chapter 44 sexually transmitted infections and vaginitis
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Chamberlain College Of Nursing
NR 566 (NR566)
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NR 566 Week 6 Chapters 22, 31, 44(download to score A+)
Chapter 22: Drugs Affecting the Reproductive System
Chapter 31: Contraception
Chapter 44: Sexually Transmitted Infections and Vaginitis
Chapter 22: Drugs Affecting the Reproductive System
Androgens
• Testosterone primary male androgen
• many tissues , it’s activity depends on reduction to dihydrotesterone, which binds to cytosol-
receptor proteins. Androgen-receptor complex then transported to nucleus of the cell, where it
initiates transcription events and cellular changes
• Dihydrotestosterone (DHT) is the essential androgen in the prostate
• Responsible for
o normal growth, maturation, and maintenance of male sex organs and secondary sexual
characteristics
o skeletal growth spurt in adolescence and for termination of linear growth by fusion of
episphyseal growth plate
o activation of sebaceous glands some cases of acne during puberty
o enhancing production of erythropoietic stimulating factor increased RBC production
o playing a role in libido
• Synthetic androgens meant to supplement or replace endogenous hormones & used to treat
disorders in male and female reproductive tract
Uses
• primary indication primary hypogonadal males or hypogonadotropic hypogonadism, and
male climacteric
• both sexes for disorders such as cancer & HIV
• treat libido, endometriosis, & postmenopausal symptoms in women
• have been used to enhance athletic performance and increase muscle mass
• oral administration rapid
• buccal administration lengthens ½ life
• IM administration can last 2-4 weeks varying rates of administration leads to significant
fluctuation in testosterone levels
• transdermal by gel or patch once daily application to intact nonscrotal skin (Androderm,
Androgel, Axiron, Testim) well absorbed through skin and results in rises in serum
testosterone levels within 2-4 hours. Testoderm rapid return to baseline within two hours of
removal
Effects
• contraindications: male breast cancer, prostate cancer, pregnancy (X), lactation
• transdermal not for use in women
• increased risk for prostatic hypertrophy and prostatic carcinoma
• drug interactions anticoagulatns, diabetic agents, corticosteroids
Side effects (When used in high doses)
• hepatitis, hepatic neoplasms, cholestatic hepatitis, jaundice, gynecomastia, reduced sperm
levels, acne, baldness, paradoxical decrease in libido, depression, headache, scrotal pain,
priaprism, n/v
Monitoring
• goal is to have normal serum testosterone levels
• check at baseline, 3 -6months after initiating, then annually while on treatment
• Male patients prostate-specific antigen (PSA) and digital prostate evaluation prior to
initiation of therapy and throughout the duration of treatment due to the increased risk of
prostate hypertrophy and cancer associated with androgens
,Antiandrogens
, • androgen hormone inhibitors (5-alpha-reductase inhibitors)
o block conversion of testosterone to dihydrotesterone (DHT)
• key agents:
o finasteride (proscar, propecia)
▪ BPH 5mg per day
▪ male pattern baldness 1mg (3months usually required to see results)
▪ 100% selective for 5-alpha reductase type 2 (isoenzyme primarily in prostate,
seminal vesicles, epididymis, hair follicles
▪ absorbs well orally
▪ reduction in DHT begins within 8 hours and lasts about 24
▪ undergoes extensive hepatic metabolism, (excreted in urine 39% & feces 57%)
▪ side effects: decreased libido, impotence
o dutasteride (Avodart)
▪ inhibits both type 1 & 2 forms of the isoenzyme
▪ doesn’t bind to human androgen receptor
▪ absorbed well orally, reaches peak within 2-3 hours, peak clinical affect after 6-
12 months of therapy
▪ metabolized in liver, utilizing CYP450 3A4/5 substrate
▪ excreted mainly in feces
▪ used to treat BPH
▪ absorped through skin, pregnant women shouldn’t handle
▪ adverse side effects decreased libido and impotence
o Leuprolide acetate (Lupron)
▪ luteinizing hormone-releasing hormone agonist create a reversible chemical
orchiectomy state in males and an oophorectomy state in women
▪ effective in treating advanced prostatic cancer & management of endometriosis
and uterine leiomyomata (fibroids)
▪ 1mg SC daily, or IM every 3 months in depot formulation
▪ greater suppression when used with flutamide
▪ used to treat precocious puberty in pediatric patients
o Flutamide (Eulexin, Euflex)
▪ inhibit androgen uptake or nuclear binding of androgen at target tissues
▪ behaves like a competitive antagonist at the androgen receptor site (truly a
nonsteroidal agent)
▪ part of combo therapy for prostatic carcinoma
▪ adverse effects in men: gynecomastia and reversible liver toxicity
▪ rapidly absorbed orally
▪ black box warning hepatic failure, hepatic encephalopathy, death)
▪ baseline and monthly LFTs necessary for 1st 4 months, then periodically
o Sprinolactone (Aldactone)
▪ competitive inhibitor of DHT, aldosterone, and interferes with androgen
receptors in prostate
▪ also reduced 17-alpha-hydroxylase activity lowering plasma testosterone and
androstenedione levels
▪ used as a potassium sparing diuretic
▪ used for primary hyperaldosteronism preoperatively short term
▪ off-label use for treatment of female hirtutism and acne 50-200mg/day
▪ relief of symptoms from PMS/PMDD
▪ absorbed orally, reaching peak in 2 hours
▪ metabolized by liver, excreted through portal system
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