1. OverView:
(1) Dienogest was synthesised in 1979 in Jena, Germany under the leadership of Prof. Kurt Ponsold, was initially referred to as STS 557. It was found that its potency was 10 times that of levonorgestrel. The first product on the market to contain dienogest as a contraceptive pill Valette in 1995 made by Jenapharm. It has been little used outside of Germany.
(2) Dienogest is an orally-active semisynthetic, steroidal progestogen (or progestin). It is available for use as an oralcontraceptive in combination with ethinylestradiol. It has antiandrogenic activity and as a result can improve androgenicsymptoms. It is a non-ethinylated progestin which is structurally related to testosterone. Dienogest given in isolation is available for the treatment of endometriosis under the trade name Visanne.
2. Usage:
Dienogest is used primarily as a contraceptive in combination with ethinylestradiol. It is given as a tablet containing 2 mg of dienogest and 30 μg of ethinylestradiol. Dienogest is also available in a quadriphasic oral contraceptive pill combined with estradiol valerate, marketed as Natazia in the United States and Qlaira in some European countries. This formulation is also approved for the treatment of heavy menstrual bleeding.
The minimum dose required to inhibit ovulation has been found to be approximately 1 mg.
3. How does it work:
(1) Dienogest has moderate affinity for the progesterone receptor in human uterus tissue, in vitro, about 10% that of progesterone.
(2) Inhibition of ovulation
The minimum effective dose of oral dienogest required to inhibit ovulation is 1 mg/day. The inhibition of ovulation by dienogest occurs mainly via peripheral action as opposed to central action on gonadotrophin secretion. Oral treatment of dienogest 2 mg/day in cyclical women reduced serum progesterone levels to anovulatory levels, however serum levels of lutenising hormone and follicle-stimulating hormone are not significantly altered.
4. Adverse effects:
Adverse effects associated with dienogest are the same as those expected of a progestogen. These include weight gain, increased blood pressure, breast tenderness and nausea. It produces no androgenic side effects and has little effect on metabolic and lipid haemostatic parameters.
5. COA:
TEST
|
SPECIFICATIONS
|
RESULTS
|
Appearance
|
White to pale yellow crystalline powder
|
Conforms
|
Melting point
|
210°C-218°C
|
212°C-216°C
|
Clarity and Color of Solution
|
Conforms
|
Conforms
|
Specific Rotation
|
-338°~-358°
|
-351.1°
|
Total impurity
|
≤1.0%
|
0.08%
|
Max single impurity
|
≤0.1%
|
0.04%
|
Loss on drying
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≤1.0%
|
0.10%
|
Residue on Ignition
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≤0.1%
|
0.045%
|
Heavy Metal
|
≤10ppm
|
Conforms
|
Assay
|
≥98.0
|
98.6%
|
Conclusion: Conforms to the Enterprise Standards.
|

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