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|Estropipate |
Drugs search, click the first letter of a drug name: | A | B | C | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 9 Home Estropipate( Piperazine Estrone Sulfate ) Pronouncation: (ESS-troe-PIH-pate)Class: Estrogens Trade Names: Trade Names: Mechanism of ActionPharmacologyPromotes growth and development of female reproductive system and secondary sex characteristics; affects release of ovulation and prevents postpartum breast engorgement; conserves calcium and phosphorous and encourages bone formation; overrides stimulatory effects of testosterone. PharmacokineticsAbsorptionWell absorbed from the GI tract. DistributionLargely bound to sex hormone-binding globulin and albumin. Crosses the placenta. MetabolismUndergoes first-pass metabolism. Metabolic conversion occurs primarily in the liver, but also at local target tissue sites. Also undergoes enteriohepatic recirculation. EliminationA certain portion is excreted into the bile and then reabsorbed from the intestine. Excreted in the urine as conjugates. Indications and UsageManagement of moderate to severe vasomotor symptoms associated with menopause; female hypogonadism, female castration, primary ovarian failure, and atrophic conditions caused by deficient endogenous estrogen production; prevention and treatment of osteoporosis. ContraindicationsBreast cancer; estrogen-dependent neoplasia; undiagnosed abnormal genital bleeding; thrombophlebitis or thromboembolic disorders associated with previous estrogen use; known or suspected pregnancy. Dosage and AdministrationDosage is calculated as estrone sulfate. Vasomotor SymptomsAdults PO 0.625 to 5 mg/day given cyclically. Female Hypogonadism, Female Castration, Primary Ovarian FailureAdults PO 1.25 to 7.5 mg/day for 3 wk followed by 8 to 10 day drug-free period. OsteoporosisAdults PO 0.625 mg/day for 25 days of 31-day cycle. Atrophic Vaginitis, Kraurosis VulvaeAdults PO 0.625 to 5 mg/day. Give cyclically. Intravaginal 2 to 4 g/day. Give cyclically. Drug InteractionsAntidepressants, tricyclicEstrogens may alter effects and increase toxicity of these agents. Barbiturates, modafinil, rifampin, St. John"s wort, topiramateMay decrease estropipate concentration. CorticosteroidsAn increase in the pharmacologic and toxicologic effects of corticosteroids may occur. HydantoinsLoss of seizure control or decreased estrogenic effects may occur. Laboratory Test InteractionsEndocrine and LFT results may be affected; possible decreased PT and increased platelet aggregability; increased thyroid-binding globulin and total T 4 ; impaired glucose tolerance; decreased serum folate concentration; increased serum triglyceride and phospholipid concentrations; increased corticosteroid binding globulin and sex-hormone binding globulin; increased plasma HDL concentrations; reduced LDL cholesterol concentrations; increased triglyceride levels. Adverse ReactionsCardiovascularThrombosis; thrombophlebitis; increased BP; pulmonary embolism; MI. CNSHeadache; migraine; dizziness; depression; insomnia; anxiety; emotional lability. DermatologicChloasma; melasma; erythema nodosum/multiforme; scalp hair loss; hirsutism; urticaria; dermatitis; skin hypertrophy; pruritus. EENTIntolerance to contact lenses. GINausea; vomiting; abdominal cramps; bloating; colitis; acute pancreatitis; diarrhea; dyspepsia; flatulence; gastritis; gastroenteritis; enlarged abdomen; hemorrhoids. GenitourinaryIncreased risk of endometrial carcinoma; breakthrough bleeding; dysmenorrhea; amenorrhea; vaginal candidiasis; premenstrual-like syndrome; increased size of uterine fibromyomata; hemolytic uremic syndrome; urinary tract infection; vaginitis; vaginal discomfort/pain; cystitis; dysuria; genital pruritus; urinary incontinence. HepaticCholestatic jaundice. MetabolicHyperglycemia; hypercalcemia. RespiratoryUpper respiratory tract infection; sinusitis; rhinitis; pharyngitis; flu-like symptoms; allergy; bronchitis; chest pain. MiscellaneousIncrease or decrease in weight; edema; changes in libido; breast tenderness; acute intermittent porphyria; vaginal bleeding; hypersensitivity reactions; back pain; arthritis; arthralgia; hot flushes; otitis media; toothache. PrecautionsPregnancyCategory X . LactationExcreted in breast milk. ChildrenSafety and efficacy not established. Hepatic FunctionMetabolism may be impaired; use drug with caution. Calcium and phosphorus metabolismUse drug with caution in patients with metabolic bone diseases. Cardiovascular and other risksCompared with placebo, increased risks of MI, stroke, deep vein thrombosis, pulmonary emboli, and invasive breast cancer were reported in postmenopausal women during 5 yr of treatment with conjugated equine estrogens combined with medroxyprogesterone acetate. Other combinations of estrogens and progestins were not studied; however, in the absence of comparable data, assume these risks to be similar. Fluid retentionUse drug with careful observation when conditions that might be affected by this factor are present (eg, asthma, cardiac or renal dysfunction, epilepsy). Gallbladder diseaseRisk of gallbladder disease may increase in women receiving postmenopausal estrogens. Induction of malignant neoplasmsMay increase risk of endometrial or other carcinomas. Familial hyperlipoproteinemiaMay be associated with massive elevations of plasma triglycerides. Uterine leiomyomataPreexisting uterine leiomyomata may increase in size. Unopposed estrogen administration (eg, without progesterone)Increases risk of uterine cancer. Therefore, when using estrogens on long-term basis in a woman with intact uterus, consider cyclic therapy with progesterone (eg, estrogen on days 1 to 25 of mo with progesterone added for last 12 days) or daily coadministration of estrogen plus progesterone on daily basis. In a woman without uterus, use of cyclic therapy and/or therapy with progesterone is not necessary. OverdosageSymptomsNausea, withdrawal bleeding in women. Patient Information
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