Drugs Affecting The Reproductive System

DRUGS AFFECTING THE FEMALE REPRODUCTIVE SYSTEM

I. Sex Hormones & Estrogen Receptor Modulator

 The FRS functions in a cyclical fashion, not in the steady-state fashion seen with much of
the rest of the endocrine system.
 Altering any component of this cycle or the system can have a wide variety of effects on
the entire body.
 Hormones and hormonal-like agent
Common Estrogen Drugs:
1. Estradiol (Estrace)
2. Conjugated Estrogens (Premarin)
3. Esterified Estrogen (Menest)
4. Estropipate (Ogen)
5. Ethinyl Estradiol (found in various birth control pills)
Common Progestin Drugs:
1. Medroxyprogesterone (Provera)
2. Levonorgestrel (Mirena, Plan B)
3. Norethindrone (Aygestin)
4. Desogestrel (found in many contraceptive combinations)
5. Drospirenone (Yasmin, Yaz)
Common Fertility Drugs:
1. Clomiphene (Clomid)
2. Gonadotropins (e.g., Follistim, Gonal-F)
3. Letrozole (Femara)
4. Human Chorionic Gonadotropin (hCG)
5. Bromocriptine (Parlodel)
Common Uterine Motility Drugs:
1. Oxytocin
2. Prostaglandins (e.g., Dinoprostone, Misoprostol)
3. Magnesium Sulfate
4. Terbutaline (Brethine)
5. Hydralazine
Therapeutic Actions and Indications of Estrogen:
 Used for hormone replacement therapy (HRT)
 Used as palliation for the discomforts of menopause.
 Treat female hypogonadism and ovarian failure.
 Prevent postpartum breast engorgement.
 As part of combination contraceptives

Therapeutic Actions and Indications of Progestins:

 Used as contraceptives
 Treat primary and secondary amenorrhea and functional uterine bleeding and as part of
fertility programs
 Useful in treating specific cancers with specific receptor site sensitivity
 Transform the proliferative endometrium into a secretory endometrium
 Inhibit uterine contraction
Pharmacokinetics
Contraindications (ESTROGEN)
1. In the presence of any known allergies to estrogen.
2. Patients with idiopathic vaginal bleeding, breast cancer, or any estrogen-dependent cancer.
3. History of thromboembolic (blood vessel clot) disorders including CVA, or with heavy
smokers
4. Hepatic dysfunction

Cautions (ESTROGEN)
1. Metabolic bone disease
2. Renal insufficiency
3. Hepatic impairment
4. Breast feeding
Contraindications (PROGESTIN)
1. PID, STD, endometriosis, or pelvic surgery.
2. Drospirenone - risk for hyperkalemia (renal disorders, liver disease, adrenal dysfunction)
Cautions (PROGESTIN)
1. Epilepsy
2. Migraine Headaches
3. Asthma
4. Cardiac or Renal dysfunction
Adverse Effects

II. Estrogen Receptor Modulator

Available ERM are
Evista (chemical name: raloxifene) Fareston (chemical name: toremifene) Nolvadex,Soltamox
(tamoxifen)
Therapeutic Actions and Indications
● used to treat estrogen receptor-positive breast cancer in women — both pre- and post-
menopausal.
● block the effects of estrogen in breast cells to stop breast cancer cells from multiplying.
● produce an estrogen-like effect in many other types of cells
Pharmacokinetics
1. Administer orally
Tamoxifene readily absorbed on oral administration
Oral dose 20 mg/day
2. RALOXIFENE ---- absorbed from the GIT (gastrointestinal tract (GIT) is the system of organs
that allows for the consumption and digestion of food, absorption of nutrients) and is
metabolized in the liver.
Contraindications and Cautions
1. Allergy to raloxifene Allergic reactions—skin rash, itching, hives, swelling of the face, lips,
tongue, or throat
2. Blood clot—algia, swelling, or warmth in the leg, SOB, Angina pectoris
3. During pregnancy (Teratogenicity during the first trimester of pregnancy has always been of
particular interest. The data support this concern about teratogenicity, but malformations were
also reported following tamoxifen treatment after the first trimester) Teratogenicity- the ability
to cause defects in a developing fetus.
Adverse Effects
Like most cancer treatments, SERMs have side effects, some of which may cause serious medical
issues.
Common tamoxifen side effects include:
 Hot flashes.
 Night sweats.
 Irregular periods or spotting (uterine bleeding).
 Loss of sex drive.
 Vaginal discharge.
 Vaginal dryness or itching.
 Changes in your menstrual cycle if you haven’t gone through menopause.
 Deep venous thrombosis
Raloxifene side effects include:
 Hot flashes (more common in the first six months of raloxifene therapy).
 Leg cramps.
 Swollen hands, feet, ankles or lower legs.
 Flu-like syndrome.
lll. Fertility Drugs
FERTILITY DRUGS
 Enhances the reproductive fertility
 Used to stimulate follicle development of ovary
 Improve their chance of conceiving

Contraindications (FD)
 Presence of primary ovarian failure
 Thyroid or adrenal dysfunction
 Ovarian cysts
 Pregnancy
 Idiopathic uterine bleeding
 Allergy to any fertility drug
Cautions (FD)
 Cautions should be used in women who are breastfeeding
 Those with thromboembolic (thrombo embolism - a circulating blood clot that gets stuck
and causes an obstruction) disease
 With respiratory diseases
Adverse Effects (FD)
 Increased risk of multiple births and birth defects
 Ovarian overstimulation (abdominal pain, distention, ascites, pleural effusion)
 Headache
 Gynecomastia (enlargement of a man's breasts)
 Nausea (being sick to your stomach)
 Bloating
 Uterine bleeding
 Ovarian enlargement
IV. Uterine Motility Drugs
A. Oxytocics
Stimulate contraction of the uterus, much like the action of the hypothalamus hormone
oxytocin, stored in the posterior pituitary.
• Methylergonovine (Methergine), oxytocin (Pitocin)
Therapeutic Actions and Indications (Oxytocics)
1. Directly affect neuroreceptor site to stimulate contraction of the uterus.
2. Stimulate the lacteal glands in the breast to contract.
3. Indicated for the prevention and treatment of uterine atony after delivery
Pharmacokinetics (Oxytocics)
• Rapidly absorbed after parenteral or oral administration.
• Metabolized in the liver
• Excreted in the urine and feces
• Cross the placenta and enter breast milk
• Administered IM or IV
• Methylergonovine - administered as such directly after delivery and then continued in
the oral
form to promote uterine involution.
• Oxytocin-used in nasal form to stimulate "let down" in lactating women.
Contraindications (Oxytocics)
1. Allergy to oxytocics
2. Cephalopelvic disproportion, unfavorable fetal position, complete uterine atony, or
early pregnancy.
Cautions (Oxytocics)
1. Coronary disease and HPN
2. Previous CS births
3. Hepatic or Renal impairment
Adverse Effects (Oxytocics)
1. Related to excessive effects (uterine hypertonicity and spasm, uterine rupture,
postpartum hemorrhage, decreased FHR)
2. Gl upset (nausea, headache, and dizziness)
3. Methylergonovine - ergotism (n/v, BP changes, weak pulse, dyspnea, chest pain,
numbness and coldness in extremities, confusion, delirium and even coma)
4. Severe water intoxication with coma and maternal death.

B. Abortifacients
Therapeutic Actions and Indications (Abort)
Stimulate uterine activity, dislodging any implanted trophoblasts and preventing
implantation of any fertilized egg
Approved for use to terminate pregnancy at 12 to 20 weeks from the date of the LMP

Pharmacokinetics (Abort)
• Well absorbed when administered.
• Metabolized in liver and excreted in the urine.
• Mifepristone-administered orally and takes 5-7 days to produce the desired effect.
• Carboprost-IM injection, onset of 15 minutes and a duration of 2 hours.
• Dinoprostone-intravaginal suppository, onset of effects in 10 minutes and a duration
of effects of 2 hrs.

Contraindications (Abort)
1. Allergy to abortifacients or prostaglandin
2. After 20 weeks from the last menstrual period
3. Active PID or acute CV, hepatic, renal, or pulmonary disease.
4. Not recommended during lactation.
Cautions (Abort)
1. Caution should be used with any history of asthma, HPN, or adrenal disease.
2. With acute vaginitis (describes various disorders that cause your vagina to become infected) or scarred
uterus.

Adverse Effects (Abort)

1. Abdominal cramping
2. Heavy uterine bleeding
3. Perforated uterus
4. Uterine rupture Headache, n/v, diarrhea, diaphoresis(excessive sweating), backache, and rash.
DRUGS AFFECTING THE MALE REPRODUCTIVE SYSTEM
• Drugs that are used to affect the MRS include androgens (male steroid hormones), anabolic
steroids, and drugs that act to improve penile dysfunction.
• The male steroids are produced in the teste s and affects the entire MRS.

ANDROGEN
• male sex hormone and includes testosterone and androgens
• testosterone (Durates, Testoderms and others),the primary natural hydrogen
• used for replacement therapy in cases of hypogonadism and to treat certain breast cancers

Common Androgen Drugs

• Danazol
• Fluoxymesterone
• Methyltestosterone
• Testosterone

Therapeutic Actions and Indications (ANDROGEN)

1. Responsible for growth and development of male sex organ
2. Maintenance of secondary male sex characteristics
3. Act to increase the retention of nitrogen, sodium, potassium, and phosphorus and to
decreased the urinary excretion of calcium
4. Testosterone increased protein anabolism and decreased protein catabolism
5. Increased the production of RBC

Pharmacokinetics (ANDROGEN)
• Depot (deep, slow-release) injections, buccal system, topical gels, topical sprays, urethral
pellets and a dermal patch.
• Danazol : synthetic androgen (long-acting) available only in oral form.
• Methyltestosterone and Fluoxymesterone : long half-lives and available in the oral form.
• Well-absorbed and widely distributed throughout the body.
• Metabolize in the liver and excreted in the urine.

Contraindications (ANDROGEN)
1. Any known allergy to the drug or ingredients in the drug
2. During pregnancy and lactation
3. Presence of prostate or breast cancer in men
Cautions (ANDROGEN)
1. Presence of any liver dysfunction or cardiovascular disease
2. The topical forms of testosterone have a black box warning alerting the user to the risk of
virilization in children who come in contact with the drug from touching the clothes and the skin
of the man using the drug
3. Danazol : have black box warning regarding the risk for thromboembolic events, fetal
abnormalities, hepatitis and intracranial HPN

Adverse Effects (ANDROGEN)

A. Androgenic effects
• acne
• edema
• hirsutism
• deepening of the voice
• oily skin and hair
• weight gain
• testicular atrophy
B. Antiestrogen effects
• flushing
• sweating
• vaginitis
• nervousness
• emotional lability
C. Common Effects
• headache
• dizziness
• sleep disorder
• fatigue
• rashes
D. Potentially Life—threatening Effects
• Hepatocellular Cancer
• Cardiovascular events: stroke and venous embolic events