Female Sex Hormones

Exact mechanism of action in its function as a contraceptive is not known but it it thought that circulating progestins and estrogens “trick” the hypothalamus and pituitary and prevent the release of gonadotropin-releasing hormone (GnRH), FSH, and LH. Therefore, follicle development and ovulation are prevented

THERAPEUTIC ACTIONS:

Therapeutic Action

The desired and beneficial actions of female sex hormones are as follows:

ESTROGEN:

The most potent endogenous female sex hormone responsible for estrogen effects on the body.

Affect the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH).

Responsible for the proliferation of the endometrial lining and are known to compete with androgens for receptor sites.

The loss of estrogen is responsible for the signs and symptoms of menopause in the uterus, vagina, breasts, and cervix.

PROGESTINS:

Transform the proliferative endometrium into a secretory endometrium. They also inhibit the secretion of FSH and LH.

Prevent follicle maturation and ovulation as well as uterine contraction.

INDICATIONS:

Female sex hormones are indicated for the following medical conditions:

Estrogens

Used for hormone replacement therapy (HRT) in small doses when ovarian activity is blocked or absent.

Used as palliation for the discomforts of menopause in the first few years of menopause, when many of the beneficial effects of estrogen are lost.

Treat female hypogonadism and ovarian failure; to prevent postpartum breast engorgement.

To slow bone loss in osteoporosis.

Palliation of cancers that have known receptor sensitivity.

Progestins

Transform the proliferative endometrium into a secretory endometrium. They also inhibit the secretion of FSH and LH.

Prevent follicle maturation and ovulation as well as uterine contraction.

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Children

Have undergone little testing in children. They can cause premature closure of epiphysis so caution is important in growing children.

Smallest dose possible is used for prescribed oral contraceptives in teenage girls.

Adults

Women receiving any of these drugs should receive an annual medical examination, including breast examination and Pap smear, to monitor for adverse effects and underlying medical conditions.

Women taking estrogen should be advised not to smoke because of the increased risk of thrombotic events.

Women who are receiving these drugs for fertility programs should receive a great deal of psychological support and comfort measures to cope with the many adverse effects associated with these drugs. The risk of multiple births should be explained.

Drugs are used in treatment of specific cancers in males and they should be advised about the possibility of estrogenic effects.

Not indicated during pregnancy or lactation because of potential for adverse effects on the fetus or neonate.

Older adults

HRT is no longer commonly used by postmenopausal women.

INDICATIONS IN DIFFERENT STAGES:

CONTRAINDICATIONS AND CAUTIONS

Contraindications and Cautions

ESTROGEN:

The following are contraindications and cautions for the use of estrogens and progestins:

Allergy to estrogens. Prevent hypersensitivity reactions.

Idiopathic vaginal bleeding, breast cancer, estrogen-dependent cancer. Can be exacerbated by drug.

History of thromboembolic disorders, cerebrovascular accident, heavy smokers.Increased risk of thrombus and embolus development

Hepatic dysfunction. Estrogen have effects on liver function.

Pregnancy. Estrogen are linked to serious fetal defects

Lactating women. Possible effects to the neonate

Metabolic bone disease. Estrogen has bone-conserving effect and could exacerbate the disease.

Renal insufficiency. Can interfere with the renal excretion of the drug and increase the risk for potential adverse effects on fluid and electrolyte balance

Hepatic impairment. Can alter the metabolism of the drug and increase the risk for the adverse effects, including those on the liver and GI tract.

PROGESTINS:

Pelvic inflammatory disease (PID), sexually transmitted diseases, endometriosis, pelvic surgery. Progestins have effects on the vasculature of the uterus.

Drosperinone is contraindicated in patients who are at risk for hyperkalemia due to its antimineralocorticoid effects and the risk of hyperkalemia.

Epilepsy, migraine headaches, asthma, cardiac or renal dysfunction. Potential exacerbation of these conditions

ADVERSE EFFECTS:

Use of female sex hormones may result to these adverse effects:

Estrogen

GI: nausea, vomiting, abdominal cramp, bloating, colitis, acute pancreatitis, cholestatic jaundice, hepatic adenoma

GU: breakthrough bleeding, menstrual irregularities, dysmenorrhea, amenorrhea, changes in libido

Systemic effects: fluid retention, electrolyte disturbances, headache, dizziness, mental changes, weight changes, edema

Progestins

Systemic effects are similar to estrogen.

Dermal patch contraceptives are associated with same systemic effects, as well as local skin irritation.

Vaginal gel use is associated with headache, nervousness, constipation, breast enlargement, and perineal pain.

Intrauterine systems are associated with abdominal pain, endometriosis, abortion PID, and expulsion of the intrauterine device.

Vaginal use is associated with local irritation and swelling.

INTERACTIONS

Interactions

The following are interactions involved in the use of female sex hormones:

Estrogen

Barbiturates, rifampin, tetracyclines, phenytoin: decreased serum estrogen levels

Corticosteroids: increased therapeutic and toxic effects of corticosteroids.

Nicotine: Increased risk of thrombi and emboli

Grapefruit juice: inhibition of metabolism of estradiols

St. John’s wort: can affect metabolism of estrogens and can make estrogen-containing contraceptives less effective.

Progestins

Barbiturates, carbamazepine, phenytoin, griseofulvin, penicillin, tetracyclines, rifampin: reduced effectiveness of progestins

St. John’s wort: can affect the metabolism of progestins and can make progestin-containing contraceptives less effective.

Female sex hormones both can be used to replace missing hormones or to decrease the release of endogenous hormones. The female sex hormones include estrogen and progesterone.
It Is An Oral Drug.

Related Drugs

Classifications Generic Name Brand Name

Sex Hormones

Estrogens estradiol Estrace

estrogens, conjugated C.E.S, Premarin

estrogens, esterified Menest

estropipate Ortho-Est, Ogen

Progestins desogestrel Kariva, Cyclessa

drospirenone Yasmin, YAZ

etonogestrel Implanon

levonorgestrel Mirena, Plan B

medroxyprogesterone Provera

norethindrone acetate Aygestin

norgestrel Ovrette

progesterone (generic)

ulipristal Ella