Conjugated Estrogens vaginal cream is indicated in the treatment of atrophic vaginitis, dyspareunia and kraurosis vulvae. Conjugated Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia.
Conjugated estrogens for oral administration is a mixture of estrogens, obtained exclusively from natural sources, blended to represent the average composition of material derived from pregnant mares’ urine. It contains the sodium salts of water-soluble sulfate esters of estrone, equilin, and 17alpha-dihydroequilin, together with smaller amounts of 17 alpha-estradiol, equilenin, 17 alpha-dihydroequilenin, 17 beta-dihydroequilin, 17 beta-dihydroequilenin, 17beta-estradiol, and delta 8,9-dehydroestrone.
Estrogens are important in the development and maintenance of the female urogenital system and secondary sex characteristics. They promote growth and development of the vagina, uterus, and fallopian tubes, and enlargement of the breasts. Indirectly, they contribute to the shaping of the skeleton, maintenance of tone and elasticity of urogenital structures, changes in the epiphyses of the long bones associated with the pubertal growth spurt and its termination, growth of axillary and pubic hair, and pigmentation of the nipples and genital tissues. Decline of ovarian estrogenic and progestogenic activity at the end of the menstrual cycle can result in menstruation, although the cessation of progesterone secretion is the most important factor in the mature ovulatory cycle. However, in the preovulatory or anovulatory cycle, estrogen is the primary determinant in the onset menstruation. Eestrogen also affects the release of pituitary gonadotropins. The pharmacologic effects of conjugated estrogens are similar to those of endogenous estrogens. In responsive tissues (female urogenital organs, breasts, hypothalamus, pituitary) estrogens enter the cell and are transported into the nucleus. As a result of estrogenic activity, specific RNA and protein synthesis occurs. Oral administration of Conjugated Estrogens to postmenopausal women increases serum high density lipoprotein cholesterol (HDL-C) levels and decreases low density lipoprotein cholesterol (LDL-C) levels. This improves the lipid profile and is recognized as a factor responsible for the beneficial effects of Conjugated Estrogens on the risk of coronary heart disease in postmenopausal women. Conjugated Estrogens are soluble in water and are well absorbed from the gastrointestinal tract. Metabolism and inactivation occur primarily in the liver. Some estrogens are excreted in bile; however, they are reabsorbed from the intestine and returned to the liver through the portal venous system. Water-soluble estrogen conjugates are strongly acidic and are ionized in body fluids, which favors excretion through the kidneys since tubular reabsorption is minimal.
Menopausal vasomotor symptoms: 0.45 mg/day, up to 1.25 mg/day. Attempt to discontinue medication at 3-6-mth intervals. Vulvular and vaginal atrophy: 0.3 mg/day. Female hypogonadism: 0.3-0.625 mg/day in a cyclical regimen. Add progestin treatment once skeletal maturity is achieved. Female castration, Primary ovarian failure: 1.25 mg/day in a cyclical regimen. Palliation in prostate carcinoma 1.25-2.5 mg 3 times/day. Osteoporosis prophylaxis in postmenopausal women: Initial: 0.3 mg/day in a cyclical or continuous regimen depending on patient's condition.
Rifampin reportedly decreases estrogenic activity during concomitant use with estrogen. This effect has been attributed to enhanced metabolism of estrogen, presumably by induction of hepatic microsomal enzymes.
Known or suspected pregnancy; undiagnosed abnormal uterine bleeding; known, suspected, or history of past breast cancer; known or suspected estrogen-dependent neoplasia (e.g., endometrial cancer, endometrial hyperplasia); active or history of arterial thromboembolic disease (e.g., stroke, myocardial infarction or venous thromboembolism (such as deep venous thrombosis, pulmonary embolism); active or chronic liver dysfunction or disease; known thrombophilic disorders (e.g., protein C, protein S, or antithrombin deficiency); hypersensitivity to any component of this medication.
Breast pain, tenderness or enlargement, Headache/migraine, Gut disturbances, such as nausea, abdominal pain, bloating, flatulence, indigestion, Legcramps, Fatigue, Weightchanges, Vaginalthrush, Depression, Anxiety, Dizziness, Changes in sex drive, Rise in blood pressure, Gall bladder disease, Swelling of the ankles due to to fluid retention (peripheral oedema), Skin reactions such as rash and itch, Steepening of corneal curvature which may make contact lenses uncomfortable, Premenstrual-like symptoms, Disturbance in liver function, Irregular brown patches on the skin, usually of the face (chloasma), Blood clots in the blood vessels.
For women with a uterus: If pregnancy occurs during medication with Conjugated Oestrogens treatment should be withdrawn immediately. The results of most epidemiological studies to date relevant to inadvertent foetal exposure to estrogens indicate no teratogenic or foetotoxic effects. Lactation: Conjugated Oestrogens is not indicated during lactation.
Symptoms of overdosage of estrogen containing products in adults and children may include nausea, vomiting, breast tenderness, dizziness, abdominal pain, drowsiness/fatigue; withdrawal bleeding may occur in females. There is no specific antidote and further treatment if necessary should be symptomatic.
Store in a cool and dry place, protected from light and moisture, temperature below 25ºC.
.png&w=384&q=75)