Chlorestrolo

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

A powerful synthetic, non-steroidal estrogen. [PubChem]

Chlorestrolo is a nonsteroidal synthetic estrogen. After menopause, when the body no longer produces estrogen, chlorotrianisene is used as a simple replacement of estrogen. The estrogen-stimulated endometrium may bleed within 48-72 hours after discontinuance of estrogen therapy. Paradoxically, prolonged estrogen therapy may cause shrinkage of the endometrium and an increase in size of the myometrium. Estrogens have a weak anabolic effect and may cause sodium retention with associated fluid retention and edema. Estrogens may also decrease elevated blood cholesterol and phospholipid concentrations. Estrogens affect bone by increasing calcium deposition and accelerating epiphyseal closure, following initial growth stimulation. During the preovulatory or nonovulatory phase of the menstrual cycle, estrogen is the principal determinant in the onset of menstruation. A decline of estrogenic activity at the end of the menstrual cycle also may induce menstruation; however, the cessation of progesterone secretion is the most important factor during the mature ovulatory phase of the menstrual cycle. The benefit derived from estrogen therapy in the prevention of postpartum breast engorgement must be carefully weighed against the potential increased risk of puerperal thromboembolism associated with the use of large doses of estrogens.

Chlorestrolo
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	Chlorestrolo
Availability	Discontinued
Generic	Chlorotrianisene
Chlorotrianisene Other Names	Chloortrianisestrol, Chlorestrolo, Chlorotrianisene, Chlorotrianisenum, Chlorotrianisine, Chlorotrianizen, Chlortrianisen, Chlortrianisestrol, Chlortrianisoestrolum, Chlortrianizen, Clorotrianiseno
Related Drugs	estradiol, Premarin, Estrace, Prempro, ethinyl estradiol / norethindrone
Type
Formula	C₂₃H₂₁ClO₃
Weight	Average: 380.864 Monoisotopic: 380.117922245
Protein binding	50-80%
Groups	Investigational, Withdrawn
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Used to treat symptoms of menopause, deficiencies in ovary function (including underdevelopment of female sexual characteristics and some types of infertility), and in rare cases, prostate cancer. Chlorestrolo may also be used to prevent breast engorgement following childbirth.

How Chlorestrolo works

Chlorestrolo binds to the estrogen receptor on various estrogen receptor bearing cells. Target cells include cells in the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. 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) from the anterior pituitary.

Toxicity

Acute overdosage of large doses of oral contraceptives in chidren reportedly produces almost no toxicity except nausea and vomiting. Acute overdosage of estrogens may cause nausea, and withdrawal bleeding may occur in females.

Food Interaction

[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.

Chlorestrolo 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.

Chlorestrolo 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.