Description
Indications for use Premarin
Climacteric syndrome, estrogen deficiency in the menopausal and postmenopausal period, postmenopausal osteoporosis, dysfunctional uterine bleeding, dysmenorrhea, amenorrhea, prostate cancer.
Form of issue
Tablets coated with 0.625 mg; blister 28 package 1;
Pharmacodynamics
Regulate the development and preservation of the function of the female reproductive system, the formation of secondary sexual characteristics.
Relieve or stop manifestations of climacteric syndrome – vasomotor disorders, emotional (irritability, anxiety, depression) and urogenital (atrophic vaginitis, progressive diffuse atrophy of the vulva) symptoms.
Prevent the development of postmenopausal osteoporosis, increase the level of HDL, reduce – LDL and total cholesterol, reduce the risk of developing cardiovascular diseases.
Premarin: Pharmachologic effect
Estrogenic means, regulates the development and preservation of the function of the female reproductive system, the formation of female secondary sexual characteristics. Once in the bloodstream, it forms a complex with a specific receptor (in the fallopian tubes, cervix, ducts of the mammary glands, vagina, urethra, breast, liver, hypothalamus, pituitary), stimulates the synthesis of DNA and proteins. In this case, the proliferation of the epithelium is noted, the sensitivity of the muscles of the uterus and the tubes to the LS motivating them increases.
Reduces bone resorption of Ca2 + during the menopause, prevents the involution of the genitals. Has hypolipidemic action, reduces the concentration in the blood of LDL, increases – HDL, sensitivity to the action of insulin, improves the utilization of glucose; stimulates the production of liver globulins, binding sex hormones, renin and clotting factors; affects the exchange of Ca2 + and phosphorus (contributes to the preservation of the normal structure of bones, indirectly contributes to the formation of the skeleton and its final growth). In large doses delays water and Na + in the body, inhibits erythropoiesis. Due to participation in the realization of positive and negative feedback in the hypothalamic-pituitary-ovarian system, the Premarin causes moderately pronounced central effects. It alleviates (eliminates) manifestations of climacteric syndrome: a feeling of heat, increased sweating, dizziness, irritability, depression; prevents the development of postmenopausal osteoporosis. Promotes the normalization of the menstrual cycle in women. In men, it lowers the concentration of testosterone. indirectly contributes to the formation of the skeleton and its final growth). In large doses delays water and Na + in the body, inhibits erythropoiesis.
Due to participation in the realization of positive and negative feedback in the hypothalamic-pituitary-ovarian system, the Premarin causes moderately pronounced central effects. It alleviates (eliminates) manifestations of climacteric syndrome: a feeling of heat, increased sweating, dizziness, irritability, depression; prevents the development of postmenopausal osteoporosis. Promotes the normalization of the menstrual cycle in women. In men, it lowers the concentration of testosterone. indirectly contributes to the formation of the skeleton and its final growth). In large doses delays water and Na + in the body, inhibits erythropoiesis. Due to participation in the realization of positive and negative feedback in the hypothalamic-pituitary-ovarian system, the Premarin causes moderately pronounced central effects. It alleviates (eliminates) manifestations of climacteric syndrome: a feeling of heat, increased sweating, dizziness, irritability, depression; prevents the development of postmenopausal osteoporosis.
Promotes the normalization of the menstrual cycle in women. In men, it lowers the concentration of testosterone. Due to participation in the realization of positive and negative feedback in the hypothalamic-pituitary-ovarian system, the Premarin causes moderately pronounced central effects. It alleviates (eliminates) manifestations of climacteric syndrome: a feeling of heat, increased sweating, dizziness, irritability, depression; prevents the development of postmenopausal osteoporosis. Promotes the normalization of the menstrual cycle in women. In men, it lowers the concentration of testosterone. Due to participation in the realization of positive and negative feedback in the hypothalamic-pituitary-ovarian system, the Premarin causes moderately pronounced central effects. It alleviates (eliminates) manifestations of climacteric syndrome: a feeling of heat, increased sweating, dizziness, irritability, depression; prevents the development of postmenopausal osteoporosis. Promotes the normalization of the menstrual cycle in women. In men, it lowers the concentration of testosterone.
Pharmacokinetics
The components of the Premarin are soluble in water and well absorbed in the digestive tract, penetrate into the target tissues (genitalia, mammary glands, bones, hypothalamus, pituitary gland), cytoplasm and cell nuclei, where they stimulate the synthesis of RNA and protein.
Biotransformation occurs mainly in the liver, estrogens are excreted with bile, but are reabsorbed from the intestine and return to the portal vein system. Water-soluble conjugates of estrogens with acidic properties are ionized in the body and excreted by the kidneys with minimal reabsorption in the tubules.
Use during pregnancy
Contraindicated in pregnancy.
Contraindications for use
Breast cancer and estrogen-dependent neoplasms; uterine bleeding of unclear etiology; thrombophlebitis, a disorder of the blood coagulation system, thromboembolic diseases; severe diseases of the cardiovascular system; marked violations of the liver or kidneys; sickle-cell anemia; congenital hearing loss; prolonged immobilization.
Side effects of Premarin
Headache, nausea, vomiting, weight gain, swelling, uterine bleeding, facial skin pigmentation, erythema nodosum, transient elevation of transaminase levels in blood plasma, hyperbilirubinemia; allergic reactions (rash); rarely – hemorrhagic rashes on the skin, neoplasms of the endometrium.
Dosing and Administration Premarin
Inside. For cyclic use – 625 mcg – 1.25 mg per day, alternating with the reception for 3 weeks with a break in 1 week, menstrual bleeding begins with the 5th day of the menstrual cycle, and from the 15th to the 21st day in addition use a gestagenic the Premarin (with prolonged absence of menstruation, treatment is started any day).
If necessary, on the 5th-7th day of treatment, the daily dose can be increased to 3.75 mg, then it is reduced to 1.25 mg. Treatment of malignant neoplasms is 3.75-7.5 mg.
Overdose Premarin
Symptoms: nausea, vomiting, uterine bleeding.
Treatment: gastric lavage, maintenance therapy.
Interactions Premarin with other drugs
The effect is reduced by barbiturates, hydantoins, butadione, rifampicin.
Precautions for admission
Caution is prescribed for diabetes mellitus, arterial hypertension, epilepsy, multiple sclerosis, porphyria, tetany, mastopathy, thyrotoxicosis.
Storage conditions
List B .: In the dark place at a temperature of 15-25 ° C.
Shelf life
60 months
