CHAPTER 34
Women’s Health Drugs
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Female Reproductive Functions

Female sex steroid hormones



Estrogens
Progestins
Pituitary gonadotropin hormones


Follicle stimulating hormone (FSH)
Luteinizing hormone (LH)
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Female Reproductive
Functions (cont’d)

Female sex steroid hormones and pituitary
gonadotropin hormones promote:


Development of primary and secondary sex
characteristics
Start of menses and regulation of menstrual cycle
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Estrogens

Three major endogenous estrogens





Estradiol (principal and most active)
Estrone
Estriol
Synthesized from cholesterol in ovarian
follicles
Basic chemical structure of a steroid
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Exogenous Estrogenic Drugs–
Synthetic

Steroidal


Conjugated estrogens, estradiol transdermal,
many others
Nonsteroidal


Diethylstilbestrol
No longer available in the United States
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Estrogens
Responsible for :
 Development and maintenance of the female
reproductive system
 Development of female secondary sex
characteristics
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Estrogens: Indications

Treatment or prevention of disorders that
result from estrogen deficiency

Atrophic vaginitis
 Hypogonadism
 Oral contraception (given with a progestin)
 Dysmenorrhea
 “Hot flashes” of menopause
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Estrogens: Indications (cont’d)

Treatment or prevention of disorders that
result from estrogen deficiency (cont’d)

Uterine bleeding
 Palliative treatment of advanced breast and
prostate cancer
 Osteoporosis treatment and prophylaxis
 Many other indications
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Estrogens: Contraindications




Any estrogen-dependent cancer
Undiagnosed abnormal vaginal bleeding
Pregnancy
Active thromboembolic disorder or history
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Estrogens: Adverse Effects





Thrombolytic events—most serious
Nausea—most common
Hypertension, thrombophlebitis, edema
Vomiting, diarrhea, constipation, abdominal
pain
May cause photosensitivity, chloasma
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Estrogens:
Adverse Effects (cont’d)



Amenorrhea, breakthrough uterine bleeding
Tender breasts, fluid retention, headaches
Others
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Estrogens and HRT


Currently there is controversy about whether
or not hormone replacement therapy (HRT) is
safe
Ongoing studies
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Progestins

Synthetic derivatives of progesterone





hydroxyprogesterone (Hylutin)
medroxyprogesterone (Provera)
megestrol (Megace)
etonogestrel implant (Implanon)
Many others
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Progestins: Indications

Treatment of functional uterine bleeding
caused by:


Hormonal imbalance, fibroids, or uterine cancer
Treatment of primary and secondary
amenorrhea
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Progestins: Indications (cont’d)



Palliative treatment of some cancers and
endometriosis
Prevention of threatened miscarriage
Alleviation of PMS symptoms
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Progestins: Indications (cont’d)

megestrol (Megace)



Adjunct therapy for treatment of breast and
endometrial cancers
Management of anorexia, cachexia, or
unexplained weight loss in AIDS patients
To stimulate appetite and promote weight gain in
cancer patients
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Progestins: Adverse Effects






Liver dysfunction—cholestatic jaundice
Thrombophlebitis, thromboembolic disorders,
such as PE
Nausea, vomiting
Amenorrhea, breakthrough uterine bleeding,
spotting
Edema, weight gain or loss
Others
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Contraceptive Drugs


Medications used to prevent pregnancy
Oral medications

Monophasic, biphasic, and triphasic forms
• Triphasic form most closely duplicates the normal
hormonal levels of the female cycle


Newer extended cycle products
Most contain estrogen-progestin combinations
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Contraceptive Drugs (cont’d)

Other contraceptive forms available



Long-acting injectable form of
medroxyprogesterone (Depo-Provera)
Transdermal contraceptive patch
Intravaginal contraceptive ring
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Contraceptive Drugs:
Mechanism of Action

Prevent ovulation by inhibiting the release of
gonadotropins and increasing uterine mucous
viscosity, resulting in:


Decreased sperm movement and fertilization of
the ovum
Possible inhibition of implantation of a fertilized
egg (zygote)
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Contraceptive Drugs:
Other Drug Effects



Improve menstrual cycle regularity
Decrease blood loss during menstruation
Decrease incidence of functional ovarian
cysts and ectopic pregnancies
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Contraceptive Drugs: Indications


Primarily used to prevent pregnancy
Other uses:



Treatment of endometriosis and hypermenorrhea
Production of cyclic withdrawal bleeding
Postcoital emergency contraception
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Contraceptive Drugs:
Adverse Effects

Drawbacks to the use of these drugs include:

Hypertension
 Thromboembolism, possible PE, MI, stroke
 Alterations in lipid and carbohydrate metabolism
 Increases in serum hormone concentrations

These effects are caused by the estrogen
component
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Contraceptive Drugs:
Adverse Effects (cont’d)

May also cause:

Edema, dizziness, headache, depression, nausea,
vomiting, diarrhea, increased appetite, increased
weight, breast changes, many others
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Contraceptive Drugs:
Interactions

Drugs that decrease effectiveness of oral
contraceptive drugs

Antibiotics, barbiturates, isoniazid, rifampin
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Contraceptive Drugs:
Interactions (cont’d)

Drugs that may have reduced effectiveness if
given with oral contraceptive drugs

Anticonvulsants, beta-blockers, hypoglycemic
drugs, oral anticoagulants, theophylline, TCAs,
vitamins, hypnotics
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Osteoporosis




Low bone mass
Increased risk of fractures
Primarily affects women
20% with this condition are men
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Osteoporosis: Risk Factors





Caucasian/Asian
descent
Slender body build
Early estrogen
deficiency
Smoking
Alcohol consumption



Low-calcium diet
Sedentary lifestyle
Family history
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Drug Therapy for Osteoporosis

Calcium supplements and vitamin D may be
recommended for women at high risk for
osteoporosis
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Drug Therapy for
Osteoporosis (cont’d)

Bisphosphonates


Selective estrogen receptor modifier (SERM)


alendronate (Fosamax), ibandronate (Boniva),
risedronate (Actonel), zoledronic acid (Reclast)
raloxifene (Evista)
Hormone


calcitonin
teriparatide (Forteo)
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Drug Therapy for
Osteoporosis (cont’d)

Bisphosphonates


Work by inhibiting osteoclast-mediated bone
resorption, thus preventing bone loss
SERMs

Stimulate estrogen receptors on bone and
increase bone density
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Drug Therapy for
Osteoporosis (cont’d)

calcitonin (Calcimar)


Directly inhibits osteoclastic bone resorption
teriparatide (Forteo)



Only drug that stimulates bone formation
Derivative of parathyroid hormone
Action similar to natural parathyroid hormone
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Drug Therapy for Osteoporosis:
Indications

Bisphosphonates


Both prevention and treatment of osteoporosis
Bisphosphonates also used for glucocorticoidinduced osteoporosis and Paget’s disease
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Drug Therapy for Osteoporosis:
Indications (cont’d)

calcitonin (Calcimar)


raloxifene (Evista)


Treatment of osteoporosis
• Nasal spray (Miacalcin) most commonly used
Prevention of postmenopausal osteoporosis
teriparatide (Forteo)

Treatment for those with highest risk of fracture
(prior history of fractures)
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Drug Therapy for Osteoporosis:
Adverse Effects

SERMs




Hot flashes, leg cramps
Increased risk of venous thromboembolism
Contraindicated if patient is near age of menopause
because of possible hot flashes
Leukopenia
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Drug Therapy for Osteoporosis
Adverse Effects (cont’d)

Bisphosphonates



Headache, GI upset, joint pain
Risk of esophageal burns if medication lodges in
esophagus before reaching the stomach
Risk of osteonecrosis of the jaw
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Fertility Drugs

Various medical techniques used to treat
infertility

Includes in vitro fertilization and medication
therapy (ovulation stimulation)
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Fertility Drugs (cont’d)

clomiphene (Clomid, others)


Nonsteroidal ovulation stimulant
Blocks estrogen receptors in the uterus and
brain, resulting in a false signal of low estrogen
levels
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Fertility Drugs (cont’d)

clomiphene (Clomid, others) (cont’d)


Increases production of Gn-RH, FSH, and LH
As a result, maturation of ovarian follicles is
stimulated, leading to ovulation and increased
chance of conception
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Fertility Drugs (cont’d)

mentropins (Pergonal)



Standardized mixture of FSH and LH
Stimulates development of ovarian follicles,
leading to ovulation
May also be given to men to stimulate
spermatogenesis
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Fertility Drugs (cont’d)

chorionic gonadotropin alfa (Ovidrel)



Recombinant form of human chorionic
gonadotropin
Causes rupture and ovulation of mature ovarian
follicles, and maintenance of corpus luteum
Used to stimulate ovulation
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Fertility Drugs: Indications


Used primarily to induce ovulation in
anovulatory patients
Also may be used to promote
spermatogenesis in infertile men
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Fertility Drugs: Adverse Effects




Tachycardia, phlebitis, DVT
Dizziness, headache, flushing, depression,
anxiety, nervousness, fatigue
Nausea, bloating, constipation, others
Ovarian hyperstimulation, multiple
pregnancies, blurred vision, breast pain,
others
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Uterine-Active Medications


Medications used to alter uterine contractions
Used to:



Promote labor
Prevent the start or progression of labor
Postpartum use: reduce the risk of postpartum
hemorrhage
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Uterine Stimulants

Also called oxytocics




Oxytocin (hormonal drug)
Prostaglandins
Ergot derivatives
Progesterone antagonist
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Uterine Stimulants (cont’d)

Oxytocin (Pitocin)—synthetic form


Used to induce labor at or near full-term gestation,
and to enhance labor when contractions are weak
and ineffective
Other uses

Prevent or control postpartum uterine bleeding
 Complete an incomplete abortion (after miscarriage)
 Promote milk ejection during lactation
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Uterine Stimulants (cont’d)

Prostaglandins




Natural hormones
Cause potent contraction of myometrium, smooth
muscle fibers of the uterus
Used to induce labor by softening the cervix and
enhancing uterine muscle tone
dinoprostone (Prostin E2) and misoprostol
(Cytotec)
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Uterine Stimulants (cont’d)

Ergot alkaloids



Increase force and frequency of uterine
contractions
Used after delivery of the infant and placenta to
prevent postpartum uterine atony and hemorrhage
methylergonovine (Methergine)
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Uterine Stimulants (cont’d)

Progesterone antagonist



mifepristone (Mifeprex)
Stimulates uterine contractions to induce abortion
Given with a prostaglandin drug for elective
abortions
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Uterine Stimulants:
Adverse Effects





Hypotension or hypertension, chest pain
Headache, dizziness, fainting
Nausea, vomiting, diarrhea
Vaginal pain, cramping
Leg cramps, joint swelling, chills, fever,
weakness, blurred vision
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Uterine Relaxants:
Tocolytics


Used to stop labor that begins before term to
prevent premature birth
Generally used after the 20th week of
gestation
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Uterine Relaxants:
Tocolytics (cont’d)


Uterine contractions that occur between the
20th and 37th weeks of gestation are
considered premature labor
Nonpharmacologic measures

Bed rest, sedation, hydration
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Uterine Relaxants

terbutaline (Brethine)





Beta-adrenergic drug
Stimulation of beta2-adrenergic receptors on the
uterine smooth muscle
Results in relaxation of the uterus, thus stopping
premature contractions
“Off-label” use
Magnesium sulfate IV also used to stop labor
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Uterine Relaxants:
Adverse Effects





Palpitations, tachycardia, hypertension,
others
Tremors, anxiety, insomnia, headache,
dizziness, others
Nausea, vomiting, anorexia, bloating,
diarrhea, constipation
Hyperglycemia, hypokalemia
Dyspnea, hyperventilation, others
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Herbal Products: Soy



Relief of menopausal symptoms,
osteoporosis prevention
Estrasorb, applied as a lotion
Adverse Effects




Nausea
Diarrhea
Abdominal pain
Estrasorb remains on skin for 8 hours
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Nursing Implications




Assess baseline vital signs, weight, blood
glucose levels, renal and liver function
studies
Assess whether the patient smokes
Assess history and medication history
Assess contraindications, including potential
pregnancy
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Nursing Implications (cont’d)


Before giving any uterine stimulants, assess
the mother’s vital signs and fetal heart rate
Uterine relaxants are used when premature
labor occurs between the 20th and 37th
weeks of gestation
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Nursing Implications (cont’d)

For bisphosphonates, ensure that patients
have no esophageal abnormalities and can
remain upright or in a sitting position for
30 minutes after the dose
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Nursing Implications (cont’d)

Estrogens and progestins




Take the smallest dose needed
Give IM doses deep in large muscle masses, and
rotate sites
Give oral doses with meals to reduce GI problems
Teach patients about correct self-administration
and what to do if a dose is missed
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Nursing Implications (cont’d)

Estrogens and progestins (cont’d)



Increased susceptibility to sunburn may occur—
advise patients to wear sunscreen or avoid
sunlight
Instruct patients to report weight gain
Advise patients to complete annual follow-up
exams, including PAP smear and breast exam
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Nursing Implications (cont’d)


Follow specific administration guidelines
carefully for IV administration of uterine
relaxants or stimulants
Monitor patient’s vital signs and fetal
condition during therapy
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Nursing Implications (cont’d)


Instruct patients taking fertility drugs to take
the medication as ordered
Advise patients to keep a journal while on
fertility drugs
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Nursing Implications (cont’d)

Bisphosphonates


Instruct patients to take medication upon rising in
the morning, with a full glass of water, and
30 minutes before eating
Emphasize that patients should sit upright for at
least 30 minutes after taking the medication
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Nursing Implications (cont’d)

SERMs

Instruct patients that the medication will need to
be discontinued 72 hours before and during any
prolonged immobility (such as surgery or a long
trip)
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Nursing Implications (cont’d)


Monitor for therapeutic responses
Monitor for adverse effects
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