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QuickView for Estropipate (compound)


PubChem
Name: estropipate
PubChem Compound ID: 23703
Molecular formula: C22H32N2O5S
Molecular weight: 436.566 g/mol
Synonyms:
Estrone hydrogen sulfate compound with piperazine (1:1); Ogen; Conjugated estrogens: piperazine estrone sulfate; Estropipate; 3-(SULFOOXY)ESTRA-1,3,5(10)-TRIEN-17-ONE, W/PIP*; Estra-1,3,5(10)-trien-17-one 3-sulphate, compound with piperazine (1:1); Piperazine, compd. with 3-(sulfooxy)estra-1,3,5(10)-trien-17-one (1:1) (9CI); 7280-37-7; Estra-1,3,5(10)-trien-17-one, 3-(sulfooxy)-, compd. with piperazine (1:1); Estropipate [USAN].
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DrugBank
Identification
Name: estropipate
Name (isomeric): DB04574
Drug Type: small molecule
Synonyms:
OGEN; Estropipate (usp); Ogen (TN); Ogen 2.5
Brand: ORTHO-EST, Ogen
Category: Estrogens, Hormone Replacement Agents
CAS number: 7280-37-7
Pharmacology
Indication: Estropipate is used for the treatment of moderate to severe vasomotor symptoms associated with the monopause, and moderate to severe symptoms of vulval and vaginal atrophy associated with the menopause. It is also used to treat hypoestrogenism due to hypogonadism, castration or primary ovarian failure, and prevent postmenopausal osteoporosis.
Pharmacology:
Estropipate is an estrogenic substance. It acts as naturally produced estrogen does. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism. E...
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Mechanism of Action:
Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce s...
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Absorption: Estropipate is well absorbed through the skin and gastrointestinal tract. When applied for a local action, absorption is usually sufficient to cause systemic effects.
Biotransformation: Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Circulating estrogens exist in a dynamic equilibrium of metabolic interconversions. These transformations take place mainly in the liver. Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is the major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the gut followed by reabsorption. In postmenopausal women, a significant proportion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens.
Route of elimination: Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food to decrease nausea
Drug interaction:
PhenobarbitalThe enzyme inducer, phenobarbital, decreases the effect of the hormone agent, estropipate.
RaloxifeneAssociation not recommended
FosphenytoinThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estropipate.
PrimidoneThe enzyme inducer, primidone, decreases the effect of the hormone agent, estropipate.
PrednisoneThe estrogenic agent, estropipate, may increase the effect of corticosteroid, prednisone.
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