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| == '''What is Conjugated estrogens?''' == | | = Conjugated Estrogens = |
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| * Conjugated estrogens ('''Premarin''') is a mixture of [[estrogens]] used in [[menopausal hormone therapy]] and for various other indications.
| | [[File:Estrone_sulfate.svg|thumb|right|Chemical structure of Estrone sulfate]] |
| * It is a mixture of the sodium salts of estrogen conjugates found in horses, such as estrone sulfate and equilin sulfate.
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| * Purified orally bioavailable female sex hormones isolated from pregnant [[mare]] urine or synthetically derived from plant materials and primarily conjugated as sulfate esters.
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| | '''Conjugated estrogens''' are a mixture of estrogen hormones used primarily in [[hormone replacement therapy]] (HRT) for [[menopause|menopausal]] symptoms and in the treatment of certain conditions in women. These estrogens are derived from natural sources and are often used to alleviate symptoms such as [[hot flashes]], [[vaginal atrophy]], and [[osteoporosis]]. |
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| | == Composition == |
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| | Conjugated estrogens are composed of a mixture of several different estrogen compounds. The primary components include: |
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| == '''What are the uses of this medicine?''' ==
| | * '''Estrone sulfate''' |
| | * '''Equilin sulfate''' |
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| Conjugated estrogens ('''Premarin''') is used after [[menopause]] to:
| | [[File:Equilin_sulfate.svg|thumb|left|Chemical structure of Equilin sulfate]] |
| * Reduce moderate to severe [[hot flashes]]
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| * Treat menopausal changes in and around the vagina
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| * Help reduce your chances of getting [[osteoporosis]] (thin weak bones)
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| PREMARIN is also used to:
| | These compounds are derived from the urine of pregnant mares, which is why the medication is sometimes referred to as "[[Premarin]]" (from "pregnant mares' urine"). |
| * Treat certain conditions in women before [[menopause]] if their ovaries do not make enough estrogen naturally.
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| * Ease symptoms of certain cancers that have spread through the body, in men and women.
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| | == Mechanism of Action == |
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| == '''How does this medicine work?''' ==
| | Conjugated estrogens work by binding to estrogen receptors in various tissues throughout the body. This binding helps to modulate the expression of genes involved in the regulation of the [[menstrual cycle]], maintenance of [[bone density]], and the health of the [[urogenital system]]. |
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| <youtube>
| | == Clinical Uses == |
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| * Endogenous [[estrogens]] are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics.
| | Conjugated estrogens are primarily used in the following clinical scenarios: |
| * The primary source of estrogen in normally cycling adult women is the [[ovarian follicle]], which secretes 70 to 500 mcg of [[estradiol]] daily, depending on the phase of the [[menstrual cycle]]. After menopause, most endogenous estrogen is produced by conversion of [[androstenedione]], secreted by the [[adrenal cortex]], to [[estrone]] in the peripheral tissues. Thus, estrone and the sulfate-conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women.
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| * Estrogen binds to and activates specific nuclear receptors, which, in turn, bind to estrogen response elements (EREs) in target genes, resulting in [[histone]] acetylation, alteration of [[chromatin]] conformation, and initiation of transcription.
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| * Circulating estrogens modulate the pituitary secretion of the [[gonadotropins]], [[luteinizing hormone]] (LH) and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these gonadotropins seen in [[postmenopausal]] women.
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| | * '''Hormone Replacement Therapy (HRT):''' To alleviate symptoms of menopause such as hot flashes, night sweats, and vaginal dryness. |
| | * '''Osteoporosis Prevention:''' To help maintain bone density in postmenopausal women. |
| | * '''Hypoestrogenism:''' In cases where the body produces insufficient estrogen, such as in [[ovarian failure]]. |
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| == '''Who Should Not Use this medicine ?''' == | | == Side Effects == |
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| This medicine cannot be used in patients who:
| | The use of conjugated estrogens can lead to several side effects, including: |
| * have unusual vaginal bleeding
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| * currently have or have had certain cancers
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| * had a [[stroke]] or heart attack
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| * currently have or have had blood clots
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| * currently have or have had liver problems
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| * have been diagnosed with a bleeding disorder
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| * are allergic to PREMARIN or any of its ingredients
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| * think you may be pregnant
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| | * Increased risk of [[thromboembolism]] |
| | * [[Breast tenderness]] |
| | * [[Nausea]] |
| | * [[Headaches]] |
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| == '''What drug interactions can this medicine cause?''' == | | == Use in Men == |
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| * Inducers or inhibitors of CYP3A4 may affect estrogen drug metabolism. Inducers of CYP3A4, such as [[St. John's Wort]] (Hypericum perforatum) preparations, [[phenobarbital]], [[carbamazepine]], and [[rifampin]], may reduce plasma concentrations of estrogens, possibly resulting in a decrease in therapeutic effects and/or changes in the uterine bleeding profile.
| | Conjugated estrogens are sometimes used in men, particularly in the treatment of [[prostate cancer]]. Estrogens can help reduce [[testosterone]] levels, which can slow the growth of prostate cancer cells. |
| * Inhibitors of CYP3A4, such as [[erythromycin]], [[clarithromycin]], [[ketoconazole]], [[itraconazole]], [[ritonavir]] and [[grapefruit juice]], may increase plasma concentrations of estrogens and may result in side effects.
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| | [[File:Testosterone_levels_with_different_estrogen_therapies_in_men_with_prostate_cancer.png|thumb|right|Testosterone levels with different estrogen therapies in men with prostate cancer]] |
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| == '''Is this medicine FDA approved?''' == | | == Related Pages == |
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| * Premarin, the major brand of CEEs in use, is manufactured by Pfizer and was first marketed in 1941 in Canada and in 1942 in the United States. | | * [[Estrogen]] |
| * It is the most commonly used form of estrogen in [[menopausal hormone therapy]] in the United States. | | * [[Hormone replacement therapy]] |
| | * [[Menopause]] |
| | * [[Prostate cancer]] |
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| == '''How should this medicine be used?''' ==
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| '''Recommended dosage:'''
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| '''Treatment of Moderate to Severe Vasomotor Symptoms due to Menopause:'''
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| * Patients should be treated with the lowest effective dose.
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| * Generally, women should be started at 0.3 mg PREMARIN daily.
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| * Subsequent dosage adjustment may be made based upon the individual patient response.
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| '''Treatment of Moderate to Severe Symptoms of Vulvar and Vaginal Atrophy due to Menopause:'''
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| * Patients should be treated with the lowest effective dose.
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| * Generally, women should be started at 0.3 mg PREMARIN daily.
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| * Subsequent dosage adjustment may be made based upon the individual patient response.
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| '''Treatment of Hypoestrogenism due to Hypogonadism, Castration, or Primary Ovarian Failure:'''
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| * PREMARIN therapy should be initiated and maintained with the lowest effective dose to achieve clinical goals.
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| * Female hypogonadism: 0.3 mg or 0.625 mg daily, administered cyclically (e.g., three weeks on and one week off).
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| * Female castration or primary ovarian failure: 1.25 mg daily, cyclically.
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| '''Treatment of Breast Cancer (for Palliation Only) in Appropriately Selected Women and Men with Metastatic Disease:'''
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| * Suggested dosage is 10 mg three times daily, for a period of at least three months.
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| '''Treatment of Advanced Androgen-Dependent Carcinoma of the Prostate (for Palliation Only):'''
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| * 1.25 mg to 2 × 1.25 mg three times daily.
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| * The effectiveness of therapy can be judged by phosphatase determinations as well as by symptomatic improvement of the patient.
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| '''Prevention of Postmenopausal Osteoporosis:'''
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| * PREMARIN therapy may be given continuously, with no interruption in therapy, or in cyclical regimens (regimens such as 25 days on drug followed by 5 days off drug), as is medically appropriate on an individual basis.
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| * Patients should be treated with the lowest effective dose.
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| * Generally, women should be started at 0.3 mg PREMARIN daily.
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| '''Administration:'''
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| * Take one PREMARIN tablet at the same time each day
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| * If you miss a dose, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your normal schedule. Do not take 2 doses at the same time.
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| * Estrogens should be used at the lowest dose possible for your treatment only as long as needed. You and your healthcare provider should talk regularly (for example, every 3 to 6 months) about the dose you are taking and whether you still need treatment with PREMARIN.
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| * If you see something that resembles a tablet in your stool, talk to your healthcare provider.
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| * Take PREMARIN with or without food.
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| == '''What are the dosage forms and brand names of this medicine?''' ==
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| This medicine is available in fallowing doasage form:
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| * As Premarin, are available in the form of oral tablets (0.3 mg, 0.625 mg, 0.9 mg, 1.25 mg, or 2.5 mg), creams for topical or vaginal administration (0.625 mg/g), and vials for [[intravenous]] or [[intramuscular]] injection (25 mg/vial).
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| This medicine is available in fallowing brand namesː
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| * '''Premarin'''; '''Premarin vaginal'''
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| =='''What side effects can this medication cause?'''==
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| The most common side effects of this medicine include:
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| * [[Headache]]
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| * Breast pain
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| * Irregular vaginal bleeding or [[spotting]]
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| * Stomach or abdominal [[cramps]], [[bloating]]
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| * [[Nausea]] and vomiting
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| * [[Hair loss]]
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| * Fluid retention
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| * Vaginal [[yeast infection]]
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| * Reactions from inserting PREMARIN Vaginal Cream, such as vaginal burning, irritation, and itching
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| Serious, but less common side effects include:
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| * [[Heart attack]]
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| * [[Stroke]]
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| * [[Blood clot]]s
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| * [[Dementia]]
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| * [[Breast cancer]]
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| * Cancer of the lining of the uterus (womb)
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| * Cancer of the ovary
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| * High blood pressure
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| * High blood sugar
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| * [[Gallbladder]] disease
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| * Liver problems
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| * Enlargement of benign tumors of the uterus ("[[fibroids]]")
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| * Severe allergic reaction
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| ==''' What special precautions should I follow?''' ==
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| * [[Estrogens]] increase the risk of gallbladder disease.
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| * Discontinue estrogen if severe [[hypercalcemia]], loss of vision, severe [[hypertriglyceridemia]] or [[cholestatic jaundice]] occurs.
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| * Monitor thyroid function in women on [[thyroid replacement therapy]].
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| * Estrogen administration may lead to severe [[hypercalcemia]] in women with [[breast cancer]] and [[bone metastases]]. If hypercalcemia occurs, use of the drug should be stopped and appropriate measures taken to reduce the serum calcium level.
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| == '''What to do in case of emergency/overdose?''' ==
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| Symptoms of overdosage may include:
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| * [[nausea]]
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| * vomiting
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| * breast tenderness
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| * abdominal pain
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| * [[drowsiness]]
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| * [[fatigue]]
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| * [[withdrawal bleeding]]
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| '''Treatment of overdosage:'''
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| * Treatment of overdose consists of discontinuation of PREMARIN therapy with institution of appropriate symptomatic care.
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| == '''Can this medicine be used in pregnancy?''' ==
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| * PREMARIN should not be used during pregnancy.
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| * There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins as an [[oral contraceptive]] inadvertently during early pregnancy.
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| =='''Can this medicine be used in children?'''==
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| * Safety and effectiveness in pediatric patients have not been established.
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| == '''What are the active and inactive ingredients in this medicine?''' ==
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| * PREMARIN contains a mixture of conjugated estrogens, which are a mixture of sodium estrone sulfate and sodium equilin sulfate and other components including sodium sulfate conjugates, 17 α-dihydroequilin, 17 α-estradiol, and 17 β-dihydroequilin.
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| * PREMARIN 0.3 mg, 0.45 mg, 0.625 mg, 0.9 mg, and 1.25 mg tablets also contain the following inactive ingredients: calcium phosphate tribasic, hydroxypropyl cellulose, microcrystalline cellulose, powdered cellulose, hypromellose, lactose monohydrate, magnesium stearate, polyethylene glycol, sucrose and titanium dioxide.
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| == '''Who manufactures and distributes this medicine?''' ==
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| * '''Packager:''' [[Wyeth Pharmaceuticals LLC]], a subsidiary of [[Pfizer Inc]].
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| == '''What should I know about storage and disposal of this medication?''' ==
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| * Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F).
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| * Dispense in a well-closed container, as defined in the USP.
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| {{coststubd}}
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| {{Estradiol}}
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| {{Estrogens and antiestrogens}}
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| {{Estrogen receptor modulators}}
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| {{Portal bar | Medicine}}
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| [[Category:Antigonadotropins]]
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| [[Category:Bioethics]]
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| [[Category:Combination drugs]]
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| [[Category:Estranes]]
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| [[Category:Estrogens]] | | [[Category:Estrogens]] |
| [[Category:Hormonal antineoplastic drugs]] | | [[Category:Hormone replacement therapy]] |
| [[Category:Horse products]]
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| [[Category:Ketones]]
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| [[Category:Organic sodium salts]]
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| [[Category:Prodrugs]]
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| [[Category:Prolactin releasers]]
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| [[Category:Sulfate esters]]
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| [[Category:Wyeth brands]]
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| [[Category:Pfizer brands]]
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