Transcript Estrogens Progestins

Pharmacology in Nursing
Women’s Health Drugs
Female Reproductive Functions
• Female sex steroid hormones
– Estrogens
– Progestins
• Pituitary gonadotropin hormones
– Follicle stimulating hormone (FSH)
– Luteinizing hormone (LH)
• Development of primary and secondary sex
characteristics
• Menstrual Cycle
Estrogens
• Three major endogenous estrogens
– Estradiol (principal & most active)
– Estrone
– Estriol
• Synthesized from cholesterol in
ovarian follicles
• Basic chemical structure of a steroid
Exogenous Estrogenic Drugs–
Synthetic
• Steroidal
– Conjugated estrogens, estradiol
transdermal, many others
• Nonsteroidal
– Chlorotrianisene, diethylstilbestrol
diphosphate, others
– These drugs no longer available in the
United States
Estrogens Required For
• The development and maintenance of
the female reproductive system
• The development of female secondary
sex characteristics
Estrogens: Indications
• Treatment of or prevention of
disorders that result from estrogen
deficiency
– Atrophic vaginitis
– Hypogonadism
– Oral contraception (given with a
progestin)
– Dysmenorrhea
– “Hot flashes” of menopause
Estrogens: Indications (cont’d)
• Treatment of 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
Estrogens: Indications (cont’d)
• Continuous-combined hormone
replacement therapy (CCHRT)
– Fixed estrogen/progestin combination
products
– Reduce complications, such as
endometrial hyperplasia, that occur from
using estrogen alone
Estrogens:
Contraindications
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Allergy to the medication
Any estrogen dependent cancer
Undiagnosed abnormal vaginal bleeding
Pregnancy
Active thromboembolic disorder or
history
Estrogens:
Adverse Effects
• Thrombolytic events—most serious
• Nausea—most common
• Hypertension, thrombophlebitis, edema
• Vomiting, diarrhea, constipation, abdominal pain
• May cause photosensitivity, chloasma
• Amenorrhea, breakthrough uterine bleeding
• Tender breasts, fluid retention, headaches
Progestins
• Synthetic derivatives of progesterone
– medroxyprogesterone (Provera)
– hydroxyprogesterone
– megestrol (Megace)
– Many others
Progestins: Indications
• Treatment of functional uterine
bleeding caused by:
– Hormonal imbalance, fibroids, or uterine
cancer
• Treatment of primary and secondary
amenorrhea
Progestins: Indications (cont’d)
• Palliative treatment of some cancers
and endometriosis
• Prevention of threatened miscarriage
• Alleviation of symptoms of PMS
Progestins: Indications (cont’d)
• megestrol
– Adjunct therapy for treatment of breast and endometrial cancers
– Also used for management of anorexia, cachexia, or unexplained
weight loss in AIDS patients
– Used to stimulate appetite and promote weight gain in patients
with cancer
• Used with estrogen replacement therapy
after menopause
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
Contraceptive Drugs
• Medications used to prevent
pregnancy
• Oral medications
– Monophasic, biphasic, and
triphasic forms
– Most contain estrogen-progestin
combinations
Contraceptive Drugs (cont’d)
• Other contraceptive forms available
– Long-acting injectable form of
medroxyprogesterone (Depo-Provera)
– Transdermal contraceptive patch
– Intravaginal contraceptive ring
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)
Contraceptive Drugs:
Other Drug Effects
• Improve menstrual cycle regularity
• Decrease blood loss during
menstruation
• Decreased incidence of functional
ovarian cysts and ectopic pregnancies
Contraceptive Drugs:
Indications
• Primarily used to prevent pregnancy
• Other uses
– Treatment of endometriosis and
hypermenorrhea
– To produce cyclic withdrawal bleeding
– Postcoital emergency contraception
Contraceptive Drugs:
Adverse Effects
• Drawbacks to the use of these drugs
include (effects due to estrogen component):
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Hypertension
Thromboembolism, possible PE, MI, stroke
Alterations in lipid and carbohydrate metabolism
Increases in serum hormone concentrations
• Edema, dizziness, headache, depression,
nausea, vomiting, diarrhea, increased appetite,
increased weight, breast changes, many others
Contraceptive Drugs:
Interactions
• Drugs that decrease effectiveness of
oral contraceptive drugs
– Antibiotics, barbiturates, isoniazid,
rifampin, griseofulvin
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, vitamins, hypnotics
Osteoporosis
• Low bone mass
• Increased risk of fractures
• Primarily affects women
• 20% of those with this condition are
men
Osteoporosis
Osteoporosis: Risk Factors
– Caucasian/Asian descent
– Slender body build
– Early estrogen deficiency
– Smoking
– Alcohol consumption
– Low-calcium diet
– Sedentary lifestyle
– Family history
Drug Therapy for
Osteoporosis
• Calcium supplements and vitamin D
may be recommended for women at
high risk for osteoporosis
Drug Therapy for
Osteoporosis (cont’d)
– Bisphosphonates
• alendronate (Fosamax), ibandronate (Boniva), risedronate
(Actonel)
– Selective estrogen receptor modifier
(SERM)
• raloxifene (Evista)
– Hormone
• calcitonin
• teriparatide (Forteo)
Drug Therapy for
Osteoporosis (cont’d)
Biphosphonates
• Work by inhibiting osteoclast-mediated
bone resorption, thus preventing bone
loss
SERMs
• Stimulate estrogen receptors on bone
and increasing bone density
Drug Therapy for
Osteoporosis (cont’d)
calcitonin
– Directly inhibits osteoclastic bone
resorption
teriparatide
– Only drug that stimulates bone formation
– Derivative of parathyroid hormone
– Action similar to natural parathyroid
hormone
Drug Therapy
for Osteoporosis:
Indications
• Bisphosphonates and calcitonin
– Both prevention and treatment of
osteoporosis
– Biphosphanates also used for
glucocorticoid-induced osteoporosis and
Paget’s disease
Drug Therapy
for Osteoporosis:
Indications (cont’d)
• raloxifene
– Prevention of postmenopausal osteoporosis
• teriparatide
– Used for those with highest risk of fracture
(prior history of fractures)
Drug Therapy for Osteoporosis
Adverse Effects
• SERMs
– Hot flashes, leg cramps
– Can increase risk of venous thromboembolism
– Not used if patient is near age of menopause
due to possible hot flashes
– Leukopenia
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
Fertility Drugs
• Various medical techniques used to treat
infertility
• Include:
– in vitro fertilization
– Medication therapy: ovulation stimulation
Fertility Drugs (cont’d)
• clomiphene (Clomid
– Nonsteroidal ovulation stimulant
– Blocks estrogen receptors in the uterus
and brain, resulting in a false signal of
low estrogen levels
• Causes increased production of GnRH, FSH, and LH
– As a result, maturation of ovarian follicles
is stimulated, leading to ovulation and
increased chance of conception
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
Fertility Drugs (cont’d)
• chorionic gonadotropin (Ovidrel)
– Recombinant form of human chorionic
gonadotropin
– Causes rupture and ovulation of mature
ovarian follicles, and maintenance of corpus
luteum
– Used to stimulate ovulation
Fertility Drugs:
Indications
• Used primarily to induce ovulation in
anovulatory patients
• Also may be used to promote
spermatogenesis in infertile men
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
Uterine-Active Medications
• Medications used to alter uterine
contractions
• Used to:
– Promote labor
– Prevent the start or progression of
labor
– Postpartum use: to reduce the risk of
postpartum hemorrhage
Uterine Stimulants
Also called oxytocics
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Ergot derivatives
Prostaglandins
Progesterone antagonist
oxytocin (hormonal drug)
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)
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)
Uterine Stimulants (cont’d)
Progesterone antagonist
• mifepristone (Mifeprex)
• RU-486, the “abortion pill”
• Stimulates uterine contractions to induce
abortion
• Given with a prostaglandin drug for elective
abortions
Uterine Stimulants:
oxytocin (Pitocin)
Synthetic Form
• Used to induce labor at or near full-term gestation, and
to enhance labor when contractions are weak and
ineffective
• Prevent or control postpartum uterine bleeding
• Complete an incomplete abortion (after miscarriage)
• Promote milk ejection during lactation
Uterine Stimulants:
Adverse Effects
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Hypotension or hypertension, chest pain
Headache, dizziness, fainting
Nausea, vomiting, diarrhea
Vaginal pain, cramping
Leg cramps, joint swelling, chills, fever,
weakness, blurred vision
Uterine Relaxants:
Tocolytics
• Used to stop labor that begins before term to prevent
premature birth
• Generally used after the 20th week of gestation to stop
uterine contractions that occur between the 20th and
37th weeks of gestation (considered premature labor)
• Nonpharmacologic measures:
– Bedrest, sedation,
– hydration
Uterine Relaxants:
Tocolytics (cont’d)
• Uterine contractions that occur between
the 20th and 37th weeks of gestation
are considered premature labor
• Nonpharmacologic measures
– Bedrest, sedation, hydration
Uterine Relaxants
• ritodrine (Yutopar) and terbutaline
(Brethine)
– Beta-adrenergic drugs
– 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
Uterine Relaxants:
Adverse Effects
• Palpitations, tachycardia, hypertension
• Tremors, anxiety, insomnia, headache, dizziness
• Nausea, vomiting, anorexia, bloating, diarrhea, constipation
• Hyperglycemia, hypokalemia
• Dyspnea, hyperventilation
Nursing Implications
• Assess baseline VS, weight, blood glucose
levels, renal and liver function studies
• Assess whether the patient smokes
• Assess history and medication history
• Assess contraindications, including
potential pregnancy
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
Nursing Implications (cont’d)
• For bisphosphonate, ensure that the patient
has no esophageal abnormalities and can
remain upright or in a sitting position for
30 minutes after the dose
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 patient about correct selfadministration and what to do if a dose is
missed
Nursing Implications (cont’d)
• Estrogens and progestins (cont'd)
– Increased susceptibility to sunburn may
occur—advise patient to wear sunscreen
or avoid sunlight
– Patients should report weight gain
– Annual follow-up exams should be
completed, including PAP smear and
breast exam
Nursing Implications (cont’d)
• Follow specific administration guidelines carefully
for IV administration of uterine relaxants or
stimulants
• Monitor the patient’s vital signs and fetal condition
during therapy
• Instruct patient taking fertility drugs to take the
medication as ordered
• Recommend the patient keep a journal while on
fertility drugs
Nursing Implications (cont’d)
• Biphosphonates
– Instruct patient to take medication upon
rising in the morning, with a full glass of
water, and
30 minutes before eating
– Emphasize that the patient should sit
upright for at least 30 minutes after
taking the medication
Nursing Implications (cont’d)
• SERMs
– Instruct patient that the medication will
need to be discontinued 72 hours before
and during any prolonged immobility
(such as surgery or a long trip)
Nursing Implications (cont’d)
• Monitor for therapeutic responses
• Monitor for adverse effects