Estrovis 4000

Estrovis 4000 Uses, Dosage, Side Effects, Food Interaction and all others data.

The 3-cyclopentyl ether of ethinyl estradiol.

Estrovis 4000 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 Estrovis 4000
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
Estrovis 4000
Estrovis 4000

Uses

Used in hormone replacement therapy, treating symptoms of menopause such as hot flashes. Also used to treat breast and prostate cancer.

How Estrovis 4000 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.

Estrovis 4000 Disease Interaction

Moderate: angioedema, melasma, retinal thrombosis

Elimination Route

Absorbed following oral administration.

Innovators Monograph

You find simplified version here Estrovis 4000

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0000012
http://classyfire.wishartlab.com/tax_nodes/C0000258
http://classyfire.wishartlab.com/tax_nodes/C0001466
http://classyfire.wishartlab.com/tax_nodes/C0001466
http://classyfire.wishartlab.com/tax_nodes/C0003236
http://classyfire.wishartlab.com/tax_nodes/C0000025
http://classyfire.wishartlab.com/tax_nodes/C0000048
http://classyfire.wishartlab.com/tax_nodes/C0000128
http://classyfire.wishartlab.com/tax_nodes/C0001373
http://classyfire.wishartlab.com/tax_nodes/C0001670
http://classyfire.wishartlab.com/tax_nodes/C0001292
http://classyfire.wishartlab.com/tax_nodes/C0004478
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8716
http://www.genome.jp/dbget-bin/www_bget?cpd:C07619
http://www.lipidmaps.org/data/LMSDRecord.php?LMID=LMST02010037
http://www.hmdb.ca/metabolites/HMDB0015579
http://www.genome.jp/dbget-bin/www_bget?drug:D00576
http://www.genome.jp/dbget-bin/www_bget?cpd:C07619
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=9046
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508939
https://www.chemspider.com/Chemical-Structure.8694.html
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=9066
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=8716
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1201165
https://zinc.docking.org/substances/ZINC000003875993
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP001016
http://www.pharmgkb.org/drug/PA164749042
https://en.wikipedia.org/wiki/Quinestrol
*** Taking medicines without doctor's advice can cause long-term problems.
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