Conjugated Estrogens Usp (Premarin)
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Other names of Premarin
Apo-Conest, Belestar, CES, Carentil, Cenestin, Climarest, Climopax, Climopax mono, Congest, Conjugen, DNA-EC, Dagynil, Elredin, Emopremarin, Enjuvia, Equifan, Equin, Esonovag, Estrinolon, Estrogenon, Estroplus, Fahifem, Femavit, Gestrocon, Livomarin, Longaplex, Mannest, Menoprin, Menosedan, Neradin, Oestrofeminal, Prem, PremarinLite, Premarina, Premauclair, Premphase, Prempro, Presomen, Presomen spezial, Repogen, Six Din, Sultrona, Terapova, Transannon.
What Is Premarin (Conjugated Estrogens Usp)?
Premarin, or Conjugated estrogen USP, contains a mixture of estrogen hormones derived from pregnant mares’ urine (horses). It is commonly prescribed to treat symptoms associated with menopause, such as hot flashes, vaginal dryness, and other hormonal imbalances. Premarin can also be used to prevent osteoporosis in postmenopausal women and as part of hormone replacement therapy (HRT). It comes in various forms, including oral tablets and topical creams. As with any hormone therapy, the use of Premarin should be carefully monitored by a healthcare professional, considering individual health factors and potential risks, such as an increased risk of certain cancers and cardiovascular issues. Regular check-ups and discussions with a healthcare provider are essential for Premarin users.
Conjugated estrogens taken orally are hydrolyzed by enzymes present in the intestine that remove the sulfate group and allow absorption of the unconjugated estrogen. Metabolism occurs primarily in the liver, with some enterohepatic recycling.
Uses and Administration
Conjugated estrogens have actions and uses similar to those described for estradiol. When used as menopausal, HRT doses of 0.3 to 1.25 mg daily are given orally, either cyclically or continuously, with a progestogen in women with a uterus. Doses of 0.3 to 1.25 mg may also prevent postmenopausal osteoporosis. Still, estrogen therapy is generally reserved for women who are at significant risk and who cannot be given non-hormonal treatment.
Topical vaginal therapy may be used specifically for menopausal atrophic vaginitis, atrophic urethritis, and kraurosis vulvae 0.5 to 2 g of a 0.0625% cream may be used daily for three weeks of a 4-week cycle. For women with a uterus, the addition of cyclical progestogen is generally not required during topical vaginal estrogen therapy. However, the use of a progestogen may be considered, and during long-term therapy, these women should be monitored for evidence of endometrial hyperplasia.
When given as replacement therapy on a cyclical basis, oral doses of 1.25 mg daily are used for primary ovarian failure, adjusted according to response. Doses of 300 to 625 micrograms daily are usually given for female hypogonadism, although higher doses were formerly used.
For the palliative treatment of prostatic carcinoma, an oral dose of 1.25 to 2.5 mg three times daily has been used. A dose of 10 mg three times daily for at least three months has been used for palliative treatment of breast carcinoma in men and postmenopausal women.
Abnormal uterine bleeding has been treated acutely by giving 25 mg of conjugated estrogens by slow intravenous injection, repeated if required after 6 to 12 hours. The intramuscular route has also been used. Synthetic conjugated estrogens are derived from plant material and are not a generic equivalent of Conjugated Estrogens described in the United States Pharmacopeia 31, 2008. Synthetic conjugated estrogens, A, contains nine derivatives of estrone, equilin, estradiol, and equilenin. It is used in oral doses of 0.45 to 1.25 mg daily for the relief of vasomotor symptoms associated with menopause.
A dose of 300 micrograms daily may be used for menopausal vulvar and vaginal atrophy, but an alternative topical therapy should be considered if this is the only symptom being treated. Synthetic conjugated estrogens, B, contains ten derivatives of estrone, equilin, estradiol, and equilenin. It is used in oral doses of 0.3 to 1.25 mg daily for the relief of vasomotor symptoms associated with menopause. A dose of 300 micrograms daily may be used for menopausal vulvar and vaginal atrophy, but an alternative topical therapy should be considered if this is the only symptom being treated.
Administration in Children
Conjugated estrogens have been used to reduce final height in girls with constitutional tall stature. They have also been used in children for some hemorrhagic disorders.
Case reports and small studies have described the use of high-dose conjugated estrogens in the management of hemorrhagic disorders associated with renal failure. However, it is unclear how estrogens might reduce prolonged bleeding times in these patients. Treatment has been given orally, but an intravenous dose of 600 micrograms/kg given over 30 to 40 minutes, once daily for five days, has been reported most often.
Conjugated estrogens have also been used in various doses in the management of hemorrhagic cystitis, particularly that caused by high-dose cyclophosphamide therapy. The successful use of 25 mg intravenously for two consecutive days has been reported, as has a regimen consisting of a 1 mg/kg intravenous dose followed by 5 mg orally for three weeks. A treatment report in 10 patients described the use of oral conjugated estrogens in doses of 6 to 12 mg daily, usually in three divided doses, for durations of 5 days to 16 weeks. Another report of therapy in 10 children aged between 8 and 19 years described intravenous doses of 12.5 to 50 mg twice daily, often for 2 or 3 days, followed by oral doses ranging from 2.5 mg twice daily to 5 mg four times daily for durations of a few days to about three weeks.
Estrogens have also been used in the treatment of other bleeding disorders.
Adverse Effects and Precautions
Side effects are the same as for estrogens in general.
Effects on the Cardiovascular System
In an early study of men with a previous myocardial infarction, treatment with conjugated estrogens 5 mg daily was stopped because of a higher incidence of subsequent coronary events. Moreover, treatment with the lower 2.5 mg dose was later also stopped because of suggestions of adverse trends, including a greater incidence of venous thromboembolism.
Effects on the Nervous System
Reversible chorea has been described in 2 women given conjugated estrogens with a progestogen as postmenopausal HRT. In 1 case, the patient had a history of migraine and Sydenham’s chorea. Chorea also recurred in a postmenopausal woman with a history of chorea gravidarum when she was given vaginal conjugated estrogens.
Hypersensitivity. An anaphylactic reaction after intravenous conjugated estrogens has been reported.
Premarin (Conjugated Estrogens USP) can interact with various medications, and it’s essential to inform your healthcare provider about all the drugs you are taking, including prescription, over-the-counter, herbal products, and supplements. Some medications may either enhance or diminish the effects of Premarin, leading to potential complications or reduced efficacy.
Interactions may occur with aromatase inhibitors, certain anticonvulsants, corticosteroids, and tamoxifen. Additionally, smoking while using Premarin may increase the risk of severe cardiovascular side effects.
Always consult your healthcare provider to ensure a comprehensive understanding of potential interactions, and only adjust your medication regimen with professional guidance. Regular check-ups with your healthcare provider are crucial to monitor and manage any potential complications associated with Premarin use.
Synonyms: Conjugated Estrogens; Conjugated Oestrogens; Estrógenos conjugados; Estrogeenit, konjugoidut; Estrogena Coniugata; Estrogenai, konjuguoti; Estrogener, konjugerade; Estrogeni Coniunct; Estrogeni Coniuncti; Estrogeny konjugované; Konjugált ösztrogének
ATC code: G03CA57
Read code: y02ar; y08DY [Endocrine Use]
Pharmacopoeias. In Europe and the US.
European Pharmacopoeia, 6th ed. (Estrogens, Conjugated). A mixture of various conjugated forms of estrogens obtained from pregnant mares’ urine or by synthesis dispersed in a suitable powdered diluent. It contains two principal components, 52.5 to 61.5% sodium estrone sulfate, and 22.5 to 30.5% sodium equilin sulfate; the total of the combined two is 79.5 to 88.0%. It also contains 2.5 to 9.5% sodium 17a-estradiol sulfate, 13.5 to 19.5% sodium 17a-dihydroequilin sulfate, and 0.5 to 4.0% sodium 17p-dihy-droequilin sulfate. All percentages are related to the labeled content.
An almost white-brownish amorphous powder.
The United States Pharmacopeia 31, 2008 (Conjugated Estrogens). A mixture of sodium estrone sulfate and sodium equilin sulfate, derived wholly or in part from equine urine or synthetically from estrone and equilin. It contains other conjugated oestrogenic substances of the type excreted by pregnant mares. It contains 52.5 to 61.5% sodium estrone sulfate and 22.5 to 30.5% sodium equilin sulfate; the combined two should comprise 79.5 to 88.0% of the labeled content of conjugated estrogens.
It should contain, as sulfate conjugates, 13.5 to 19.5% of 17a-dihydro equilin, 2.5 to 9.5% of 17a-estradiol, and 0.5 to 4.0% of 17p-dihydro equilin, relative to the labeled content of conjugated estrogens. If obtained from natural sources, it is a buff-colored amorphous powder that is odorless or has a slight characteristic odor. The synthetic form is a white to light buff-colored crystalline or amorphous powder, odorless or with a slight odor. Store at a temperature of 25°; excursions permitted between 15° and 30°.
Synthetic Conjugated Estrogens, A
Synthetic Conjugated Oestrogens, A.
Синтетические Конъюгированные Эстрогены, A
Synthetic Conjugated Estrogens, B
(US Adopted Name)
CE-10 Synthetic Conjugated Oestrogens, B.
Синтетические Конъюгированные Эстрогены, B.
CAS — 746658-13-9.
The United States Pharmacopeia 31, 2008: Conjugated Estrogens Tablets.
Argentina: Belestar Livomarin Premarin
Austria: Conjugen Oestro-Feminal Premarin
Brazil: Estrogenon Estroplus Gestrocon Menoprin Menosedan Prem Premarin Repogen
Canada: CES Congest Premarin
Chile: Climatrol E Conpremin Estrarona Profemina
Czech Republic: Oestrofeminal Premarin Presomen
Germany: Climarest Climopax mono Femavit Oestrofeminal Presomen Transannon
Hong Kong: Equin Premarin
India: Espauz Estrin Premarin
Israel: Premaril Prevagin-Premaril
Italy: Emopremarinl Premarin
Mexico: Equifan Fahifem Neradin Premarin Six Din Sultrona Terapova
The Netherlands: Dagynil Premarin PremarinLite
New Zealand: Premarin
Philippines: Menpoz Premarin
South Africa: Premarin
Singapore Equin Premarin
Spain: Equin Longaplex Premarin
Switzerland: Premarin Transannon
Thailand: Estromon Premarin
USA: Cenestin Enjuvia Premarin
Venezuela: Biostrogen Climatrol E Menostat Premarin.
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
Argentina: Periofem Ciclico¤; Periofem Continuo¤; Premelle Ciclico; Premelle Continuo;
Australia: Menoprem¤; Premia Continuous; Premia Low; Premia; Provelle¤;
Austria: Cyclo-Premarin-MPA¤; Cyclo-Premella¤; Perennia; Premarin compositum; Premarin MPA¤; Premarin Plus; Premella¤; Sequennia;
Belgium: Premelle Cycle; Premelle; Premplus¤;
Brazil: Ero Test¤; Menosedan Ciclo; Menosedan Fase; Menosedan MPA; Menostress¤; Menotensil; Premarin MPA¤; Premelle Ciclo; Premelle; Prempro Bifasico; Prempro Monofasico; Repogen Ciclo; Repogen Conti; Selecta;
Canada: Premarin with Methyltestosterone¤; Premplus;
Chile: Climatrol Continuo; Climatrol HT Continuo; Climatrol HT; Conpremin Pak Plus; Conpremin Pak; Novafac 30; Novafac CC; Novafac; Prempak; Profemina CC; Profemina MP;
Czech Republic: Cyclo-Premella; Premella; Presomen Compositum;
Germany: Climopax Cyclo; Climopax; Ovaribran¤; Presomen Compositum; Seda-Presomen¤; Transannon comp.¤; Transannon Plus¤;
Greece: Premelle Cycle; Premelle;
Hong Kong: Premelle Cycle; Premelle; Prempak¤;
Hungary: Cyclo-Premella; Premella;
Ireland: Premique Cycle; Premique; Prempak-C;
Israel: Premaril MP; Premaril Plus MP;
Italy: Premelle Combinato; Premelle S¤; Premelle Sequenziale; Prempak;
Malaysia: Plentiva Cycle 5; Plentiva; Premelle; Prempak;
Mexico: Premarin Pak¤; Premelle;
Netherlands: Premarin Plus; Premelle Cycle; Premelle; PremelleLite; Prempak-C;
New Zealand: Menoprem; Premia Continuous; Premia; Prempak-C¤; Provette Continuous¤; Provette Sequential¤;
Portugal: Premarin Plus; Premelle Cycle; Premelle;
South Africa: PMB¤; Premelle; Prempak N;
Singapore: Premelle Cycle; Premelle; Prempak-C; Spain: Premelle Ciclico; Premelle;
Sweden: Premelle Sekvens; Premelle; Switzerland: Cyclo-Premella ST; Cyclo-Premella¤; Premarin Plus; Premella; Premia;
Thailand: Premelle Cycle; Premelle; Prempak¤;
United Kingdom: Premique Cycle; Premique; Prempak-C;
United States: Mediatric¤; PMB¤; Premarin with Methyltestosterone¤; Premphase; Prempro;
Venezuela: Climatrol HT Ciclico; Climatrol HT Continuo; Cyclogesterin; Premelle Ciclico; Premelle Continuo; Premelle Plus Continuo