Valest

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

Valest was first synthesized in 1938 by Hans Herloff Inhoffen and Walter Hohlweg at Schering. It was developed in an effort to create an estrogen with greater oral bioavailability. These properties were achieved by the substitution of an ethinyl group at carbon 17 of estradiol. Valest soon replaced mestranol in contraceptive pills.

Valest was granted FDA approval on 25 June 1943.

Valest is a synthetic estrogen that decreases luteinizing hormone to decrease endometrial vascularization, and decreases gonadotrophic hormone to prevent ovulation. It has a long duration of action as it is taken once daily, and a wide therapeutic index as overdoses are generally not associated with serious adverse effects. Patients should be counselled regarding the risks of thrombotic events.

Trade Name Valest
Generic Ethinylestradiol
Ethinylestradiol Other Names 17-ethinylestradiol, 17alpha-Ethinyl estradiol, Ethinyl estradiol, Ethinylestradiol, Ethinylestradiolum, Ethinyloestradiol, Ethynyl estradiol, Etinilestradiol
Weight 2mg, 1mg
Type Tablet
Formula C20H24O2
Weight Average: 296.4034
Monoisotopic: 296.177630012
Protein binding

Enthinylestradiol is 98.3-98.5% bound to albumin in serum but also exhibits binding to sex hormone binding globulin.

Groups Approved
Therapeutic Class
Manufacturer Walter Bushnell Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Valest
Valest

Uses

Valest is an estradiol used as a contraceptive.

Valest is combined with other drugs for use as a contraceptive, premenstrual dysphoric disorder, moderate acne, moderate to severe vasomotor symptoms of menopause, prevention of postmenopausal osteoporosis.

Valest is also used to associated treatment for these conditions: Menopausal Osteoporosis, Mild to Moderate Acne, Premenstrual Dysphoric Disorder ( PMDD), Moderate Acne vulgaris, Moderate, severe, Vasomotor Symptoms caused by Menopause, Contraception, Folate supplementation therapy

How Valest works

Valest is a synthetic estrogenic compound. Use of estrogens have a number of effects on the body including reduced bone density. Combined oral contraceptives suppress ovulation by suppressing gonadotrophic hormone, thickening cervical mucus to prevent the travel of sperm, and preventing changes in the endometrium required for implantation of a fertilized egg. Valest decreases luteinizing hormone, decreasing vascularity in the endometrium. It also increases sex hormone binding globulin.

Toxicity

Female patients experiencing and overdose may present with withdrawal bleeding, nausea, vomiting, breast tenderness, abdominal pain, drowsiness, and fatigue. Overdose should be treated with symptomatic and supportive care including monitoring for potassium concentrations, sodium concentrations, and signs of metabolic acidosis.

Food Interaction

  • Avoid St. John's Wort. St. John's Wort may decrease the effectiveness of ethinylestradiol.

Volume of Distribution

A 30µg oral dose has an apparent volume of distribution of 625.3±228.7L and a 1.2mg topical dose has an apparent volume of distribution of 11745.3±15934.8L.

Elimination Route

A 30µg oral dose of ethinylestradiol reaches a Cmax of 74.1±35.6pg/mL, with a Tmax of 1.5±0.5h, and an AUC of 487.4±166.6pg*h/mL. A 1.2mg dose delivered via a patch reaches a Cmax of 28.8±10.3pg/mL, with a Tmax of 86±31h, and an AUC of3895±1423pg*h/mL.

Half Life

A 30µg oral dose has a half life of 8.4±4.8h and a 1.2mg topical dose has a half life of 27.7±34.2h.

Clearance

Valest has an intravenous clearance of 16.47L/h, and an estimated renal clearance of approximately 2.1L/h. A 30µg oral dose has a clearance of 58.0±19.8L/h and a 1.2mg topical dose has a clearance of 303.5±100.5L/h.

Elimination Route

Valest is 59.2% eliminated in the urine and bile, while 2-3% is eliminated in the feces. Over 90% of ethinylestradiol is eliminated as the unchanged parent drug.

Innovators Monograph

You find simplified version here Valest

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/C0003570
http://classyfire.wishartlab.com/tax_nodes/C0003027
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/C0004646
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:4903
http://www.genome.jp/dbget-bin/www_bget?cpd:C07534
http://www.lipidmaps.org/data/LMSDRecord.php?LMID=LMST02010036
http://www.hmdb.ca/metabolites/HMDB0001926
http://www.genome.jp/dbget-bin/www_bget?drug:D00554
http://www.genome.jp/dbget-bin/www_bget?cpd:C07534
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5991
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508618
https://www.chemspider.com/Chemical-Structure.5770.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50187243
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=4124
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=4903
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL691
https://zinc.docking.org/substances/ZINC000003812897
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP001018
http://www.pharmgkb.org/drug/PA449527
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/3WF
http://www.rxlist.com/cgi/generic/estinyl.htm
https://en.wikipedia.org/wiki/Ethinylestradiol
*** Taking medicines without doctor's advice can cause long-term problems.
Share