Transcript Reproductive System Drugs

Rachel Picone, MS, APRN, WHNP-BC
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Identify indications, mechanism of action
(MOA), adverse effects (AE) for androgens,
estrogens and progestins
Identify MOA, AE for medications used in
erectile dysfunction
Identify indications, MOA, AE for selected
medications used during pregnancy, labor
and birth
Not responsible for GnRH analogs on the test!
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Male sex hormones testosterone and
androsterone
Induce masculinization by acting on target
receptors in tissues
Synthetic androgens are indicated in the
treatment of:
◦ Hypogonadism (congenital or acquired)
◦ FTM transgendered persons desiring to transition
hormonally
◦ Palliative treatment of advanced breast cancer in
women
◦ Severe fibrocystic breast disease
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Edema
Acne
Sexual changes
Decreased sperm production
Gynecomastia
Hirsutism
Liver dysfunction
Premature fusion of epiphyseal plates (stunting)
Mood changes
Increased LDL, decreased HDL
Insulin resistance
Illegal anabolic steroid use: psychosis, violence
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Danocrine (danazol) 100-400mg PO BID
Android, Testred (methyltestosterone) PO,
buccal
Estratest (methylytestosterone w/ estrogen)
PO
Oxandrin (oxandrolone) PO 2.5-20 mg/day
divided doses
Depo-Testosterone (testosterone) IM,
implant, buccal*
Androderm, AndroGel (testosterone)
transdermal patch, gel*
*used in transgender therapy
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Indicated in treatment of erectile dysfunction
MOA: smooth muscle relaxation, vasodilation
Viagra (sildenafil) 50 mg po 1h before sex
Levitra (vardenafil) 10 mg po before sex or
2.5mg po daily
Cialis (tadalafil) 10 mg po 1h before sex
Max frequency for all: once daily!
Adverse Effects:
◦ Headache, flushing, hearing and vision changes,
dizziness, tinnitus, nasal congestion, back pain
◦ Cardiovascular events (less than 2%): angina,
syncope, tachycardia, hypotension
Caution in:
 Concurrent use of nitrates, alpha-blockers
 Patients with cardiovascular disease
 Erection > 4hrs is a medical emergency!
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Female sex hormone responsible for
feminization
Important in menstrual cycle and pregnancy
Important component in combined hormonal
contraceptives
Used in menopausal therapy (including
surgically or radiation-induced menopause)
MTF transgendered persons desiring to
transition hormonally
Hypogonadism
Landmark 2002 study
 Postmenopausal estrogen therapy increases risk
of heart attack, breast cancer, stroke and clot
 Estrogen should not be used to prevent
cardiovascular disease
 Women with an intact uterus should not take
systemic estrogen-only therapy due to risk of
uterine cancer
 Women should take the smallest effective dose
for the shortest possible time and annually
review the decision with a provider
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Nausea
Acne
Increased triglycerides
Liver abnormalities
Changes in vaginal bleeding
Increased headaches
Visual changes
Mood changes
Breast tenderness
Increased risk of gallbladder disease
Increased risk of clot/VTE, stroke, MI
Endometrial hyperplasia, cancer
See contraceptive presentation!
For relief of vasomotor sx and vaginal atrophy
associated w/ menopause:
 Premarin (conjugated estrogen) PO
 Prempro, Premphase (conjugated estrogen w/
medroxyprogesterone)
 CombiPatch (estradiol/norethindrone)
transdermal
 Estrace* (micronized estrogen) tablet or
intravaginal cream
 Femring, Estring (estradiol) vaginal rings
 Estrasorb, EstroGel (estradiol) topical gel
 Vagifem (estradiol) intravaginal tablet
 Climara, Vivelle (estradiol) transdermal patches
*used in transgender care
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Used to treat abnormal uterine bleeding
Important component in combined hormonal
contraception, or may be used alone for
contraception
Some use in postmenopausal therapy
Breast and uterine cancer treatment
Adjuvant therapy in cancer and AIDS as an
appetite stimulant
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Menstrual irregularities
Weight gain
Edema
Nausea
Breast tenderness, nipple discharge
Headache
Mood changes
Clot/VTE
Decreased bone density with prolonged use
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See contraceptive presentation!
Depo-Provera IM or SC
Megace (megestrel) oral suspension
Category A
Adequate and well-controlled studies have failed to demonstrate
a risk to the fetus in the first trimester of pregnancy (and there is
no evidence of risk in later trimesters).
Category B
Animal reproduction studies have failed to demonstrate a risk to
the fetus and there are no adequate and well-controlled studies in
pregnant women.
Category C
Animal reproduction studies have shown an adverse effect on the
fetus and there are no adequate and well-controlled studies in
humans, but potential benefits may warrant use of the drug in
pregnant women despite potential risks.
Category D
There is positive evidence of human fetal risk based on adverse
reaction data from investigational or marketing experience or
studies in humans, but potential benefits may warrant use of the
drug in pregnant women despite potential risks.
Category X
Studies in animals or humans have demonstrated fetal
abnormalities and/or there is positive evidence of human fetal
risk based on adverse reaction data from investigational or
marketing experience, and the risks involved in use of the drug in
pregnant women clearly outweigh potential benefits.
FDA Pregnancy Risk Categories. http://chemm.nlm.nih.gov/pregnancycategories.htm
Pitocin (oxytocin) IV or IM
 Used to induce labor
 Stimulates uterine contractions
 In uterine atony or subinvolution, helpts
uterus to contract and stop hemorrhage
 Risks include uterine rupture, placental
abruption, fetal hypoxia and trauma, fetal
death, amniotic fluid embolism, cervical
laceration
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Prostin E2, Cervidil, Prepidil (dinoprostone,
prostaglandin E2)
Cytotec (misoprostol, prostaglandin E1
analog) : off label use, FDA-approved as a
stomach ulcer treatment
Used for cervical ripening in the induction of
labor
Used to stimulate uterine contractions in
elective or therapeutic abortions
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“the abortion pill”
Antiprogesterone used with misoprostol in
medication abortions before 9 weeks
Blocks the action of progesterone, which
supports placenta and maintains pregnancy
FDA-approved up to 49 days gestation (7 wks)
for medication abortion with misoprostolrequires 3 visits
High-quality clinical studies show that use up to
63 days (9 wks) with misoprostol taken at home
is more efficacious with fewer side effectsrequires only 2 visits
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Methergine®, oral or injectable, IV
Ergot alkaloid used in prevention and
treatment of postpartum and postabortion
hemorrhage
MOA: uterine stimulant
Not recommended prior to delivery of
placenta, may cause retained placenta
SE: nausea, vomiting, dizziness, headache,
dyspnea, cardiac symptoms
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Tocolytic
Classified as a bronchodilator, used off-label
in preterm labor
MOA: sympathomimetic action inhibits
uterine contractions via smooth muscle
relaxation
Used in preterm labor with varying success
May be used to buy more time for maternal
betamethasone injections to enhance fetal
lung maturity
SE: tremors, tachycardia, headache, nausea
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Treatment of preeclampsia or eclampsia for
prevention or control of seizures
MOA: CNS depressant, blocks neuromuscular
transmission, vasodilator, lowers BP
AE: CNS depression, flaccid paralysis,
circulatory collapse, severe hypotension,
respiratory paralysis
Contraindicated in heart block!
Antidote: calcium gluconate IV
Centers for Disease Control
U.S. Medical Eligibility for Contraceptive Use
(CDC US MEC)
http://www.cdc.gov/reproductivehealth/Uninte
ndedPregnancy/USMEC.htm
 Drugs and Lactation Database (LactMed)
http://toxnet.nlm.nih.gov/cgibin/sis/htmlgen?LACT
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American College of Obstetrics and Gynecologists
(ACOG). (2005). Medical management of abortion.
National Guideline Clearinghouse. Accessed at
www.guidelines.gov
Woodrow, R., Colbert, B., & Smith, D. (2011).
Essentials of pharmacology for health occupations.
Clifton Park, NY: Delmar Cengage Learning.
U.S. Department of Health and Human Services.
(2008). FDA pregnancy risk categories. Accessed at
http://chemm.nlm.nih.gov/pregnancycategories.ht
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