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 |
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
