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Product details
It is the most progestationally active contraceptive pill with the lowest dose. Its progestogen activity is 2 times that of levothyroxine, and has no androgenic and estrogenic activity, with anti-estrogenic effects. Oral absorption is rapid and complete, after 1~2 hours blood concentration peak, bioavailability 100%, elimination t1/28 hours. Clinically, it is used as a short-acting oral contraceptive with ethinylestradiol as a composite tablet or three photos. Because of its reliable contraceptive effect, good cycle control, can have a favourable effect on lipid metabolism, improve hdl, so it is currently the most ideal oral contraceptive.
Uses and functions of Gestodene.
Progesterone, stronger than other 19 nortestosterone derivatives, with little or no androgenic effect at effective doses. With ethinylestradiol, it forms a new combined oral contraceptive.
Pharmacological Action of Gestodene.
1, this product is norethindrone progestin, can inhibit the secretion of gonadotropins, inhibit the strength of the effect of ovulation is similar to norethindrone. It can inhibit the growth of endometrium and thicken the cervical mucus, so as to achieve the effect of anti-sperm penetration and anti-attachment.
2、The mechanism of action of this product as a short-acting compound oral contraceptive is as follows.
(1) Inhibition of ovarian ovulation: estrogen inhibits the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus through a negative feedback mechanism, which reduces the secretion of follicle stimulating hormone and inhibits follicle growth and maturation, and progesterone inhibits the release of luteinising hormone from the pituitary gland through a negative feedback mechanism, which hinders the maturation of the ovum and ovulation.
(2) Changing the morphology of the endometrium: due to the anti-estrogenic effect of progesterone, the endometrium becomes thinner, the glands are reduced, and premature secretion of dysfunctional secretion occurs, which is not conducive to the implantation of fertilised eggs.
(3) Changing the physicochemical properties of cervical mucus: under the influence of progesterone, the secretion of cervical glands is inhibited, and the amount of cervical mucus is small, sticky, turbid, and the biochemical properties are changed, which is not conducive to the penetration of spermatozoa.
Drug interactions of Bulk Gestodene Powder.
1, antibiotics inhibit intestinal bacterial reproduction, reduce the decomposition of hormone conjugates, reduce intestinal and hepatic circulation, the blood concentration of this product increases.
2、Drugs that induce hepatic enzymes such as rifampicin, hypnotic and anticonvulsant drugs, antipyretic and analgesic drugs can reduce the effect of this product.
3、Tricyclic antidepressants compete with this product in the liver for common metabolic enzymes, which can increase the blood concentration of this product.
4, amphetamine ester can enhance the clearance of this product in low-dose combined oral contraceptives, which may reduce the effect of contraceptives.
5, and contraceptive drugs combined application, the efficacy of the drug is affected as follows.
(1) Decreased antihypertensive effect of antihypertensive drugs.
(2) The anticoagulant effect of anticoagulants is reduced.
(3) The efficacy of hypoglycaemic drugs (such as insulin and oral hypoglycaemic drugs) in controlling diabetes is reduced.
(4) Increased effectiveness of tricyclic antidepressants.
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