Name | Dienogestrel |
Synonyms | STS 557 Dienogest Endometrion Dienogestril Dienogestrel 17a-Cyanomethyl-17-hydroxyestra-4, 9-dien-3-one (17a)-17-Hydroxy-3-oxo-19-norpregna-4,9-diene-21-nitrile (17R)-17-Hydroxy-3-oxo-19-norpregna-4,9-diene-21-nitrile [(17beta)-17-hydroxy-3-oxoestra-4,9-dien-17-yl]acetonitrile |
CAS | 65928-58-7 |
EINECS | 639-448-2 |
InChI | InChI=1/C20H25NO2/c1-19-8-6-16-15-5-3-14(22)12-13(15)2-4-17(16)18(19)7-9-20(19,23)10-11-21/h12,17-18,23H,2-10H2,1H3/t17-,18+,19+,20-/m1/s1 |
Molecular Formula | C20H25NO2 |
Molar Mass | 311.43 |
Density | 1.0899 (rough estimate) |
Melting Point | 210-2140C |
Boling Point | 451.46°C (rough estimate) |
Specific Rotation(α) | D25 -290° (c = 0.5 in pyridine) |
Flash Point | 285.8°C |
Solubility | Chloroform (Slightly), Pyridine (Slightly) |
Vapor Presure | 2.42E-14mmHg at 25°C |
Appearance | powder |
Color | white to beige |
Merck | 14,3106 |
pKa | 13?+-.0.40(Predicted) |
Storage Condition | 2-8°C |
Refractive Index | 1.5614 (estimate) |
Use | Dienogest is a synthetic, orally effective progesterone (progesterone). |
RTECS | RC8899500 |
Toxicity | LD50 oral in mouse: 4gm/kg |
Reference Show more | 1. [IF=7.514] Suo Decheng et al."Trace analysis of progesterone and 21 progestins in milk by ultra-performance liquid chromatography coupled with high-field quadrupole-orbitrap high-resolution mass spectrometry."Food Chem. 2021 Nov;361:130115 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.211 ml | 16.055 ml | 32.111 ml |
5 mM | 0.642 ml | 3.211 ml | 6.422 ml |
10 mM | 0.321 ml | 1.606 ml | 3.211 ml |
5 mM | 0.064 ml | 0.321 ml | 0.642 ml |
Overview | dienoest is a kind of selective luteinizing hormone drugs newly listed in recent years, it can play a role in stabilizing endometrial tissue by specifically binding to ethylene, demethyltestosterone and progesterone derivatives. Studies have found that tumor necrosis factor (TNF). And interleukin (IL-8) in patients with endometriosis have increased trend. |
Use | denopetin is a mixed progestogen, at the same time, it has the dual properties of 19-to testosterone derivatives and progesterone derivatives; Therefore, it has the pharmacological advantages of natural and synthetic progesterone, and has high progesterone activity. A large randomized, double-blind, placebo-controlled clinical trial conducted by Harada et al. showed that after 24 weeks of taking 2mg/d of denogestin, it improved Abdominal Pain, the curative effect of low back pain and sexual intercourse pain is equivalent to that of buserelin, but the rate of adverse reactions such as vaginal bleeding and bone mineral density decrease is significantly lower, and the tolerance is better. |
pharmacological properties | denopetin is a mixed progestogen with the pharmacological advantages of both natural and synthetic progestins. Denopressin has a high progestin activity with a semi-effective oral dose of 0.11mg/kg. The endocrine pharmacological properties of the endocrine pharmacological properties of the hormone is very ideal, it is only bound to the progesterone receptor, so there is no estrogen, anti estrogen and androgen activity, the anti-gonadotropin effect (inhibition of the secretion of follicle-stimulating hormone and luteinizing hormone) is also weak. |
pharmacological mechanism | absorption of oral dinoprox is complete and rapid, with absolute bioavailability greater than 90%, the time to maximum serum and plasma concentrations is approximately 2 and 1-2 hours, respectively. In plasma, about 10% of the denopeptide is present in free form, and the proportion of this biologically active moiety is quite high compared to progesterone (0.5-4%). The other 90% of denogestin in plasma is bound to plasma albumin. denogin is metabolized mainly by aromatization and 11 β-hydroxylation, and the metabolites are rapidly eliminated from the urine within 24 hours of administration. The plasma half-life of dinoprogine is shorter than that of other progestins, only 6.5 ~ l2 hours, so there is no accumulation in daily administration, and this property is also better than that of levonorgestrel. |
contraceptive drugs | dinogest is a synthetic contraceptive drug, belonging to the class of 19-demethyltestosterone progestins, has a strong progestogen and antiandrogen activity. The drug can reduce sperm motility by affecting the energy metabolism of the sperm. denopetin was successfully developed by Schering, Germany, and has been applied to oral contraception due to its strong ovulation inhibition effect. It has the characteristics of definite curative effect and little side effect, and is becoming the first choice for oral contraception. |
side effects | denopetin is used together with estradiol (artificial estrogen) for contraception. Hormonal contraception works by preventing the ovaries from releasing eggs and reducing the chances of fertilization. It also affects the lining of the uterus to prevent implantation of the egg. Women can take these pills as prescribed to reduce their chances of becoming pregnant. There are several side effects associated with the use of dinopetin and estradiol. These include breast tenderness, minor bleeding between menstrual periods, and Head Pain. Also patients reported Nausea, Abdominal Pain or bloating, as well as problems with weight gain. In addition, this drug also makes some people long acne, the whole body Fatigue and Diarrhea. More serious side effects require immediate treatment, including shortness of breath, severe chest pain, and sudden partial or complete blindness. Occasionally, persistent leg pain, abnormal Head Pain, and difficulty speaking may also occur. In addition, jaundice, numbness or weakness also requires a doctor. |