Quinestrolo
Quinestrolo Uses, Dosage, Side Effects, Food Interaction and all others data.
The 3-cyclopentyl ether of ethinyl estradiol.
Quinestrolo is the 3-cyclopentyl ether of ethinyl estradiol (the active metabolite). After gastrointestinal absorption, it is stored in adipose tissue where it is slowly released and metabolized principally to the parent compound, ethinyl estradiol. Ethinyl estradiol is a synthetic derivative of the natural estrogen estradiol.
| Trade Name | Quinestrolo |
| Availability | Discontinued |
| Generic | Quinestrol |
| Quinestrol Other Names | Quinestrol, Quinestrolo, Quinestrolum |
| Related Drugs | estradiol, Premarin, Estrace, Prempro, ethinyl estradiol / norethindrone |
| Type | |
| Formula | C25H32O2 |
| Weight | Average: 364.5204 Monoisotopic: 364.240230268 |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Used in hormone replacement therapy, treating symptoms of menopause such as hot flashes. Also used to treat breast and prostate cancer.
How Quinestrolo works
Estrogens diffuse into their target cells and interact with a protein receptor (the estrogen receptor). Estrogen 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 specific proteins that express the effect of estradiol upon the target cell. 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. Target cells include 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. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).
Toxicity
Symptoms of overdose include nausea and vomiting, 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.
Quinestrolo Disease Interaction
Elimination Route
Absorbed following oral administration.
Innovators Monograph
You find simplified version here Quinestrolo
