Oestrone

Oestrone Uses, Dosage, Side Effects, Food Interaction and all others data.

Oestrone, one of the major mammalian estrogens, is an aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone. It is produced in vivo from androstenedione or from testosterone via estradiol. It is produced primarily in the ovaries, placenta, and in peripheral tissues (especially adipose tissue) through conversion of adrostenedione. Oestrone may be further metabolized to 16-alpha-hydroxyestrone, which may be reduced to estriol by estradiol dehydrogenase.

Oestrone, a synthetically prepared or naturally occurring steroidal estrogen obtained from pregnant equine urine, is the primary circulating estrogen after menopause. Oestrone is naturally derived from the peripheral conversion of androstenedione by an aromatase enzyme found in adipose tissues and is converted to estradiol in peripheral tissues. The estrogenic potency of estrone is one third that of estradiol. Estropipate is piperazine-stabilized estrone sulfate. Oestrone, and estropipate are used to treat abnormalities related to gonadotropin hormone dysfunction, vasomotor symptoms, atrophic vaginitis, and vulvar atrophy associated with menopause, and for the prevention of osteoporosis due to estrogen deficiency.

Oestrone
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Oestrone
Availability	Discontinued
Generic	Estrone
Estrone Other Names	Estrona, Estrone, Estronum, Follicular hormone, Folliculin, Oestrone
Type
Formula	C₁₈H₂₂O₂
Weight	Average: 270.3661 Monoisotopic: 270.161979948
Protein binding	> 95%
Groups	Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Oestrone is an estrogen used to treat perimenopausal and postmenopausal symptoms.

For management of perimenopausal and postmenopausal symptoms.

Oestrone is also used to associated treatment for these conditions: Vulvovaginal Atrophy

How Oestrone works

Estrogens enter the cells of responsive tissues (e.g. female organs, breasts, hypothalamus, pituitary) where they interact with estrogen receptors. Hormone-bound estrogen receptors dimerize, translocate to the nucleus of cells and bind to estrogen response elements (ERE) of genes. Binding to ERE alters the transcription rate of affected genes. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) release from the anterior pituitary.

Toxicity

Symptoms of overdose include nausea and vomiting. Estrogen related side effects include nausea, breast tenderness, fluid retention and edema, headaches and/or migraines, chloasma and poor contact lens fit. Estrogen hormone deficiency is associated with breakthrough bleeding, hypomenorrhea, irritability, depression and menopausal symptoms. Withdrawal bleeds may occur in females.

Food Interaction

Avoid alcohol. Ingesting alcohol may increase serum concentrations of estradiol.
Avoid grapefruit products. Grapefruit inhibits CYP3A4 and therefore, may increase estrone concentrations, potentially increasing its adverse effects.

[Minor] Coadministration with grapefruit juice may increase the bioavailability of oral estrogens.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall induced by certain compounds present in grapefruits.

In a small, randomized, crossover study, the administration of ethinyl estradiol with grapefruit juice (compared to herbal tea) increased peak plasma drug concentration (Cmax) by 37% and area under the concentration-time curve (AUC) by 28%.

Based on these findings, grapefruit juice is unlikely to affect the overall safety profile of ethinyl estradiol.

However, as with other drug interactions involving grapefruit juice, the pharmacokinetic alterations are subject to a high degree of interpatient variability.

Also, the effect on other estrogens has not been studied.

Oestrone Cholesterol interaction

[Moderate] Although estrogens have generally favorable effects on plasma lipids, including increases in HDL and decreases in total cholesterol and LDL, they have also been associated with significant elevations in triglyceride levels, particularly when high dosages are used.

Severe hyperlipidemia is known to sometimes cause pancreatitis.

Patients with preexisting hyperlipidemia may require closer monitoring during estrogen therapy, and adjustments made accordingly in their lipid-lowering regimen.

Oestrone Hypertension interaction

[Major] The risk of myocardial infarction and strokes, including those associated with oral contraceptive use and some estrogen use, is increased in patients with hypertension.

Moreover, estrogens (and progestogens) may elevate blood pressure and worsen the hypertension, thus compounding the risk.

Clinically significant blood pressure increases have been reported during estrogen therapy, particularly in patients receiving high dosages or treated with oral contraceptive combinations having high progestational activity.

These effects also increase with duration of therapy and patient age.

Therapy with estrogens should be administered cautiously in patients with preexisting hypertension.

Patients should be monitored for changes in cardiovascular status, and their antihypertensive regimen adjusted or estrogen therapy withdrawn as necessary.

In patients requiring contraception, alternative methods should be considered for those who are hypertensive, over age 35, and smoke.