Transcript Women`s Health Agents

NUR 210:
Women’s Health Agents
Pharmacology:
Wanda Lovitz, APRN
Objectives: Women’s Health Agents

Describe the roles of the hypothalamus, pituitary,
and ovaries in maintaining female reproductive
function.
 Describe the benefits and risks associated with use
of estrogens in hormone replacement therapy.
 Describe the nurse’s role in the pharmacologic
management of disorders and conditions of the
female reproductive system.
 Explain the concept of selective estrogen receptor
modulation as it relates to drug therapy.
DRUGS TO KNOW

estrogen/Premarin
– Prempro/Premphase

progesterone/ Provera and DepoProvera

tamoxifen/Novadex

megestrol/Megace
Role of the hypothalamus and pituitary
in secretion of female hormones

The hypothalmus secretes GnRH which
stimulates the pituitary to secrete
FSH and LH  FSH/LH act upon
the ovary and cause development of
ovarian follicles  The ovarian follicles
then secrete estrogen and progesterone
HYPOTHALMIC -PITUITARY
AXIS
NEGATIVE Feedback System:
•estrogen FSH/LH
•Is the body’s attempt to maintain estrogen
levels.
•Will see  FSH/LH levels as the woman
goes through menopause
•estrogen and progesterone levels in
the last half of the cycle shut off GnRH,
LH, and FSH preventing another follicle
from developing
Estrogen Sources: endogenous

Endogenous Estrogens
(produced WITHIN the body)
1.
Estradiol**
2.
Estrone
Estriol
3.

All are synthesized from cholesterol in the ovarian follicles and have
the basic structure of a steroid= Steroid Hormones

** is the primary estrogen
Estrogen sources: exogenous

Exogenous Estrogens
(produced outside the body)

Natural form obtained from a
pregnant
mare’s
 urine (PREMARIN)


Exogenous hormones were developed for therapeutic use
b/c endogenous forms are inactive orally.
Effects of estrogen on body organs
The ovaries stop
secreting estrogen when
women enter menopause at
about age 50 -55.
FSH/LH  is an attempt
to get the ovaries
to secrete estrogen
Estrogenic Agents
po, transdermal, vaginal

Formulations of estrogen are similar chemically, but vary
in potency.
– Mimic effects of estrogen in estrogen
sensitive target tissue


DRUGS BIND TO ESTROGEN RECEPTOR
*estrogen /Premarin
– Commonly used to alleviate menopausal s


Vasodilation, hot flashes, and vaginal dryness
Smallest dose that alleviates sx for the shortest possible period
of time is used
*prototype drug
COMBINATION estrogen and
progesterone
Prempro/Premphase

Contraindicated in women
with breast cancer because
estrogen may promote
growth of estrogen
sensitive tumors

There are fixed
combinations of
estrogen/progesterone

(Prempro and Premphase)
Estrogenic Agents:
PRECAUTIONS

Estrogen should ALWAYS be
given with a progesterone in a
woman with a uterus to prevent
endometrial hyperplasia

Endometrial hyperplasia is a
precursor of Endometrial Cancer

Estrogen may also
risk for BREAST CANCER,
STROKE, AND UTERINE
CANCER

May exacerbate endometriosis

Smoking greatly increases the risk
for serious SE
Estrogen: CONTRAINDICATIONS








Pregnancy
Lactation
Smoker->15 Cigarettes/day
CVA hx
DVT/PE hx or risks
Breast cancer
Endometrial cancer
Migraine
Progestins
affect the endometrium (uterine lining)

Natural progestin
– Progesterone

Produced by the corpus luteum during the menstrual
cycle
– produced by the placenta during pregnancy

Inhibits the secretion of pituitary gonadotropins
preventing follicular maturation and ovulation (
progesterone  LH)
Synthetic progestins:
Provera/Depoprovera

Synthetic progestins
– Developed because oral natural progestins are
inactive
– *medroxyprogesterone
Provera (po)
 DepoProvera (IM) Q 3months

– Mainly used for birth control by inhibiting pituitary
gonadotropins FSH/LH
– Also used to tx uterine bleeding, endometrial cancer, and
secondary amenorrhea
Menstrual Cycle
High doses of progestins
SUPPRESS BLEEDING of the
endometrium.
Used to treat
endometriosis and
hypermenorrhea.
It is the WITHDRAWAL of
Progestin that causes sloughing of
the endometrial lining.
Synthetic Progestin: Megace
 megestrol
(Megace)
– Structurally a little different from progesterone, has a
methyl group on the steroid nucleus
– Primarily used in palliative management of metastatic
breast or endometrial cancer
– SE is an increase in appetite

IS OFTEN ALSO USED AS AN APPETITE STIMULANT
Medications

megestrol (Megace)
– Synthetic progesterone
– Treatment of breast and endometrial cancer

Effects hormones related to cancer growth
– Relieve symptoms of advanced forms of these cancers
– Treats loss of appetite and weight loss

Increases appetite by unknown mechanisms
Progestins: Major Side Effects


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Nausea/vomiting
**Amenorrhea
BTB (break through
bleeding)
Edema
fatigue

Depression
 Liver dysfunction
(alters lipid metabolism)

Delay in return to
fertility
 Increased appetite
with weight gain
Anti-estrogen: Tamoxifen

tamoxifen (Novadex)
– Used for many years in the treatment of breast cancer by blocking
estrogen receptors in the breast
– IT REDUCES THE OCCURRENCE OF CONTRALATERAL
BREAST CANCER
– Also used to prevent breast CA in high risk women
Tamoxifen: blocks the estrogen
receptors

Expert Quote:
“Breast cancer cells
can grow only if
you feed them
normal estrogen,
which is like
‘sirloin steak’.
Taking tamoxifen is
like feeding them
watery soup.”
Lisa Weissma
Medications

Alendronate (Fosamax)
– Fosamax Plus D
– Treat or prevent postmenopausal osteoporosis
– 10mg/day without food, minimal water
– Inhibits normal and abnormal bone resorption

Premarin
– Conjugated estrogen (HRT)
– Treatment of moderate to severe vasomotor symptoms (night sweats,
hot flashes)
– 0.3 – 0.625 mg/day cyclic 3 wks on/1 wk off
– Estrogen can stimulate growth of hormone responsive breast CA cells
 Increased risk CVD, CVA, veno-thromboembolism, breast CA
Medications

tamoxifen (Nolvadex)
– 1st line therapy advanced breast CA pre- post-
menopause
– First drug approved to prevent breast CA in high-risk
women

Competes with estrogen for binding sites in tissues high in
estrogen receptors (breast cancer cells)
– Deprives estrogen-sensitive tumors of estrogen
– Post-menopausal women
• Increases bone mineral density
• Decreases cholesterol levels