Norgestimate

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

Norgestimate was first described in the literature in 1977. It was developed by Ortho Pharmaceutical Corporation as part of an effort to develop new hormonal contraceptives with reduced adverse effects. It is commonly formulated with ethinylestradiol as a combined oral contraceptive that can also be used to treat moderate acne vulgaris.

Norgestimate was granted FDA approval on 29 December 1989.

Norgestimate is a progestin that suppresses ovulation for contraception and reduces free testosterone to treat moderate acne vulgaris. The therapeutic index is wide as overdoses are rare. Patients should be counselled regarding the risk of vascular problems, liver disease, hypertension, metabolic effects, headaches, and bleeding irregularities.

Trade Name Norgestimate
Generic Norgestimate
Norgestimate Other Names Dexnorgestrel Acetime, Norgestimate, Norgestimato, Norgestimatum
Type
Formula C23H31NO3
Weight Average: 369.4971
Monoisotopic: 369.230393863
Protein binding

17-desacetylnorgestimate is 97.2% bound to albumin and Norgestrel is >97% protein bound, including 92.5% bound to sex hormone binding globulin.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Norgestimate
Norgestimate

Uses

Norgestimate is a progesterone used as a contraceptive and to treat acne vulgaris.

Norgestimate is formulated with ethinylestradiol as a combined oral contraceptive. It can also be given with low dose ethinylestradiol for contraception as well as the treatment of moderate acne vulgaris in women ≥15 years old.

Norgestimate is also used to associated treatment for these conditions: Hypermenorrhea, Idiopathic Hirsutism, Menstrual Distress (Dysmenorrhea), Postmenopausal Osteoporosis, Moderate Acne vulgaris, Moderate Menopausal Vasomotor Symptoms, Moderate Vulvovaginal atrophy, Severe Vasomotor Symptoms Associated With Menopause, Severe menopausal vulvovaginal atrophy, Oral Contraceptives

How Norgestimate works

Progesterone analogs like norgestimate decrease the frequency of gonadotropin releasing hormone pulses from the hypothalamus, decreasing follicle stimulating hormone and luteinizing hormone. These actions prevent ovulation.

Norgestimate suppresses the hypothalamo-pituitary-axis, reducing androgen synthesis. It also induces production of sex hormone binding globulin, which decreases free testosterone. These actions together result in less testosterone being available to stimulate sebaceous glands, resulting in effective treatment of some forms of acne.

Toxicity

Data regarding overdoses of norgestimate are rare. However, the majority of patients overdosing on oral contraceptives do not become seriously ill. Treat overdoses with symptomatic and supportive care.

Food Interaction

  • Take at the same time every day.
  • Take with or without food.

Volume of Distribution

Data regarding the volume of distribution of norgestimate are not readily available.

Elimination Route

Oral norgestimate has a Tmax of 0.5-2h.

On day 21 of cycle 3, 17-desacetylnorgestimate reaches a Cmax of 1.82ng/mL, with a Tmax of 1.5h, and an AUC of 16.1h*ng/mL. At the same time, norgestrel reaches a Cmax of 2.79ng/mL, with a Tmax of 1.7h, and an AUC of 49.9h*ng/mL.

Half Life

Norgestimate is rapidly deacetylated. The active metabolites of norgestimate, 17-desacetyl norgestimate, has a half life of 12-30h, while norgestrel has a half life of 36.4±10.2h.

Clearance

Data regarding the clearance of norgestimate is not readily available.

Elimination Route

Norgestimate is 45-49% eliminated in urine and 16-49% eliminated in feces. Unchanged norgestimate is not detected in urine.

Innovators Monograph

You find simplified version here Norgestimate

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/C0001691
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http://classyfire.wishartlab.com/tax_nodes/C0001466
http://classyfire.wishartlab.com/tax_nodes/C0002978
http://classyfire.wishartlab.com/tax_nodes/C0001373
http://classyfire.wishartlab.com/tax_nodes/C0003079
http://classyfire.wishartlab.com/tax_nodes/C0001238
http://classyfire.wishartlab.com/tax_nodes/C0001137
http://classyfire.wishartlab.com/tax_nodes/C0004478
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:50815
http://www.hmdb.ca/metabolites/HMDB0015092
http://www.genome.jp/dbget-bin/www_bget?drug:D05209
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=6540478
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507381
https://www.chemspider.com/Chemical-Structure.5022837.html
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=31994
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=50815
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1200934
https://zinc.docking.org/substances/ZINC000003938695
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP001210
http://www.pharmgkb.org/drug/PA164744346
http://www.rxlist.com/cgi/generic/norgestimest.htm
https://en.wikipedia.org/wiki/Norgestimate
*** Taking medicines without doctor's advice can cause long-term problems.
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