Female reproductive system drugs(*estrogens/Estradiol*) (Indications (Used…
Female reproductive system drugs(
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.
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.
Mechanism of action
Estrogen mediates its effects across the body through potent agonism of the Estrogen Receptor (ER), which is located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain
Estradiol binds to both subtypes of the Estrogen Receptor: Estrogen Receptor Alpha (ERα) and Estrogen Receptor Beta (ERβ
Estradiol also acts as a potent agonist of G Protein-coupled Estrogen Receptor (GPER), which has recently been recognized as a major mediator of estradiol's rapid cellular effects
When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell
regulate gene transcription which leads to formation of messenger Rma
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.
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
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.
Do not store unpouched. Apply immediately upon removal from the protective pouch.
Store at controlled room temperature 15 to 30 deg C (59 to 86 deg F).
Route of administraction
Hormone replacement therapy (HRT) can be administered orally and non-orally
Providing equivalent doses are given, all forms of HRT can equally relieve menopausal symptoms and prevent bone loss and osteoporosis
Different routes of administration will have differing metabolic effects, with oral HRT producing a hepatic first-pass effect not seen with non-oral HRT