Pharmacology 2.

Estrogen Receptor Modulators

2yr - 1st sem, Finals 3. Fertility Drugs
4. Uterine Motility Drugs
Drugs Affecting the Female & Male 1. Sex Hormones
1. Estrogen
Reproductive System ▸ Used for hormone replacement therapy
(HRT)
Review of the Female RS ▸ palliation for the discomfort of
STRUCTURES menopause
- 2 Ovaries ▸ dev't of female RS & 2° sex
- 2 Fallopian tubes Uterus characteristics
- Accessory structures ▹ Estradiol
▹ Estrogen, conjugated
▹ Estrogen, esterified
◈ C/I & Cautions
Estrogen
- Allergies
- Idiopathic vaginal bleeding
- Breast Ca
- Estrogen-dependent Ca
- Hepatic Dysfunction
- CVA
- Pregnancy & lactation
❑ HORMONES - Bone Dse.
1. Estrogen - Renal Insufficiency
- produced by the ovaries, placenta, and 2. Progesterone
adrenal glands development of female ▸ contraceptives (inhibit the secretions of
characteristics prepares the body for FSH & LH)
pregnancy. ▸ amenorrhea & functional uterine
2. Progesterone bleeding
- produced by the ovaries, placenta, and Progestin
adrenal glands promotes maintenance - Drospirenone
of pregnancy - Etonogestrel
- Levonorgestrel
❑ MENSTRUAL CYCLE
- progesterone (generic)
- Each cycle starts with the release of Follicle
- medroxyprogesterone (Provera)
Stimulating Hormone (FSH), Luteinizing
◈ C/I & Cautions
Hormone (LH), and stimulation of the ovarian
Progestin
follicles.
- PID
MENARCHE → MENOPAUSE
- STIs
❑ PREGNANCY
- Endometriosis
- When ovum is fertilized by sperm → embryo
- Pelvic Sx
- Renal and Hepatic D/O
Drugs Affecting the Reproductive System
- Epilepsy
❖ Drug Classifications
- Asthma
1. Sex Hormones
- Migraine HA

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 ◈ Adverse Reactions (ARs) - Allery
- Corneal Changes - Primary ovarian failure
- Photosensitivity - Thyroid or adrenal dysfunction.
- Peripheral edema - Ovarian cysts
- Chloasma - Pregnancy
- Hepatic Adenoma - Idiopathic uterine bleeding.
- N/V - Lactation. R
- Abdl cramps - Thromboembolic disease.
- Bloatedness - Women with respiratory diseases
- Breakthrough bleeding ◈ ARs
- Change in menstrual flow - Greatly increased risk of multiple births
2. Estrogen Receptor Agonists and birth defects
➢ are agents that either stimulate or block specific - Ovarian overstimulation: abdominal
estrogen receptor sites. plain, distention, ascites, pleural
INDICATION effusion
- Prevention and treatment of - Others: headache, fluid retention,
osteoporosis in postmenopausal nausea, bloating, uterine bleeding,
women. ovarian enlargement, gynecomastia,
- HRT is no longer commonly used by and febrile reactions
postmenopausal women 4. Uterine Motility Drugs
e.g. tamoxifen, raloxifene ➢ stimulate uterine contractions to
◈ C/I & Cautions - induce labor (oxytocics)
- Allergy to estrogen. - induce abortion (abortifacients)
- Pregnancy, lactation ➢ slow down contractions (tocolytics)
- History of venous thrombosis or Tocolytics
smoking ▸ use to slow down uterine activities
◈ ARs (preterm labor)
- GI upset, N/V ▸ e.g. terbutaline
- headache, dizziness, visual changes, and Oxytocics
mental changes. ▸ stimulates contraction of the uterus
- hot flashes, skin rash, edema, and (induction of labor)
vaginal bleeding. ▸ stimulates lacteal glands → lactation
- Depression INDICATION
- Lightheadedness - Prevention and treatment of uterine
3. Fertility Drugs atony after delivery, thus reducing the
➢ are agents that stimulate the female reproductive risk of postpartum hemorrhage.
system. e.g.
INDICATION - methylergonovine
- stimulates follicles and ovulation by (Methergine)
stimulating the hypothalamus to ↑ - oxytocin (Syntocinon)
GnRH that ↑ FSH & LH levels ◈ C/I & Cautions
- chorionic gonadotropin - Allergy
- clomiphene citrate - Cephalopelvic disproportion
- follitropin alfa, follitropin beta - unfavorable fetal position (breech,
- menotropins footling)
◈ C/I & Cautions

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 - complete uterine atony, early
pregnancy. Obstetric Medications
- Coronary disease, hypertension. ❑ PREECLAMPSIA
- Hepatic & Renal impairment ➢ pregnancy-specific new-onset hypertension and
◈ ARs proteinuria, with or without severe features.
- Excessive effects: uterine hypertonicity
❑ ECLAMPSIA
and spasm, uterine rupture,
➢ seizures that cannot be attributable to other
postpartum hemorrhage, decreased
causes in a woman with preeclampsia.
fetal heart rate
➢ HELP syndrome (hemolysis, elevated liver
- Common effects: GI upset, nausea,
enzymes, low platelet count) may complicate
headache, dizziness
severe preeclampsia.
- Ergotism caused by ergonovine and
magnesium sulfate (MgSO4)
methylergonovine: nausea, blood
▸ to prevent seizure.
pressure changes, weak pulse, dyspnea,
▸ The usual dose for severe preeclampsia is 4g
chest pain, numbness and coldness in
deep IM on each buttocks, then 1gm VERY
extremities, confusion, excitement,
SLOWLY thru IV push
delirium, convulsions, coma
▸ Other med given : Hydralazine (vasodilator)
- Oxytocin has caused severe water
❖ NURSING CONSIDERATIONS
intoxication with coma and even
1. Monitor maternal VS hourly.
maternal death when used for a
2. Criteria before administration:
prolonged period.
a. Respirations not less than 12 CPM
Abortifacients (Prostaglandins)
b. DTR is present.
- evacuate uterine contents via
c. Urine output is not less than 30
intensified uterine contractions →
mL/hour.
induced abortion
3. Standby calcium gluconate on hand.
e.g.
4. Continuous fetal monitoring.
- carboprost
5. Keep room as cool as possible.
- dinoprostone
- mifepristone
Drugs Affecting the Male Reproductive System
- misoprostol (Cytotec)
STRUCTURES
◈ C/I & Cautions
- 2 testes
- Allergy
- vas deferens
- After 20 weeks from the last menstrual
- prostate gland
period.
- penis
- Active PID, CV, hepatic, renal,
- urethra
pulmonary disease.
- Lactation.
- Asthma, hypertension, adrenal disease.
- Acute vaginitis, scarred uterus.
◈ ARs
- abdominal cramping, heavy uterine
bleeding, perforated uterus, uterine
rupture
- Others: headache, nausea, vomiting,
diarrhea, diaphoresis, backache, rash

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❑ HORMONES
1. Testosterone
⬝ responsible for many sexual and
metabolic effects in male
⬝ produced by interstitial or Leydig cells
of the testes.
❑ ANDROPAUSE
⬝ Male climacteric
⬝ production of testosterone declines
Drugs Affecting the Reproductive System
❖ Drug Classifications
1. Androgens
2. Anabolic Steroids
3. Drugs for treating Penile Erectile Dysfunction
1. Androgens
➢ Male sex hormones: G&D of male organs and 2°
male sex characteristics
1. Testosterone - produced in the testes (male
characteristics before puberty)
E.g.
- Depo-testosterone
- methyltestosterone (Virilon)
2. Androgens - produced in the adrenal glands (
sustains male characteristics after puberty)
e.g.
- danazol (Danocrine) - endometriosis
- fluoxymesterone (Androxyl)
◈ C/I & Cautions
- Allergy
- Pregnancy & lactation
- Presence of prostate or breast cancer in
men.
- Liver dysfunction, CV disease.
- Topical forms of testosterone have a
Black Box Warning alerting user to the
risk of virilization in children.
- Danazol has Black Box warning
regarding the risk of thromboembolic
events, fetal abnormalities, hepatitis,
and intracranial hypertension.
◈ ARs
- Androgenic effects: acne, edema,
hirsutism, deepening of the voice, oily
skin and hair, weight gain, decrease in
breast size, and testicular atrophy.
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- Antiestrogen effects: flushing, sweating,
vaginitis, nervousness, and emotional
lability.
- Common effects: headache. dizziness,
sleep disorders, fatigue, rash, and
altered serum electrolytes.
- Hepatocellular cancer
2. Anabolic Steroids
Anabolic Steroids
- testosterone analogues that have been
developed to produce the
tissue-building effects of testosterone
with less androgenic effect.
E.g.
- oxandrolone (Oxandrin)
◈ C/I & Cautions
- Allergy
- Pregnancy, lactation.
- Liver dysfunction.
- Coronary disease.
- Prostate/breast cancer in males
NOTE: Also known to be used illegally for the
enhancement of athletic performance by
promoting increased muscle mass, hematocrit,
strength, and endurance.
◈ ARs
- In prepubertal males: virilization (e.g.
phallic enlargement, hirsutism,
increased skin pigmentation).
- In post pubertal males: inhibition of
testicular function, gynecomastia,
testicular atrophy, priapism (painful
and continual erection of the penis),
baldness, and change in libido.
- In women: hirsutism, hoarseness,
deepening of the voice, clitoral
enlargement, baldness, menstrual
irregularities.
3. Drugs for Erectile Dysfunction
➢ Penile erectile dysfunction is a condition in
which the corpus cavernosum does not fill with
blood to allow for penile erection.
1. Alprostadil
- acts locally to relax the vascular
smooth muscle and allow
filling of the corpus
 cavernosum, causing penile
erection.
2. PDE5 receptor inhibitors
- act to increase nitrous oxide
levels in the corpus
cavernosum.

alprostadil (Caverject, Muse)

PDE5 receptor inhibitors

- sildenafil (Viagra)
◈ C/I & Cautions
- Priapism
- Penile implants
- Bleeding disorders, CV diseases, optic
neuropathy, severe hepatic and renal
disorders.
◈ ARs
- Local effects associated with
alprostadil: pain at injection site,
infection, priapism, fibrosis, rash.
- Effects associated with PDE5
inhibitors: headache, flushing,
dyspepsia, urinary tract infection,
diarrhea, dizziness, possible eight
cranial nerve toxicity, and loss of
hearing.
- Hepatocellular cancer.

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