Drospirenone ethinyl estradiol tablets (Ⅱ)

Pharmacological action Drospirenone ethinyl estradiol tablets (II) are a combination oral contraceptive consisting of drospirenone and ethinyl estradiol. Drospirenone has anti-mineralocorticoid activity, counteracts sodium retention associated with estrogen, and has anti-androgenic activity. Drospirenone does not counteract the increase in sex hormone binding globulin (SHBG) associated with ethinyl estradiol, which is conducive to binding with endogenous androgens and inactivating them. Ethinyl estradiol is a steroid hormone oral contraceptive that works mainly by inhibiting ovulation and changing the properties of cervical mucus. Toxicological studies Drospirenone The results of the drospirenone Ames test, mammalian cell gene mutation test, human hepatocyte DNA test, and mouse micronucleus test were all negative; the results of the human peripheral lymphocyte chromosome aberration test and rat hepatocyte DNA test were positive. When drospirenone was orally administered to pregnant rats and rabbits, drospirenone and/or its metabolites could pass through the placenta and enter the fetus. No evidence of teratogenicity of drospirenone was found in rats or rabbits. No increase in tumor incidence was observed in mice and rats given drospirenone for 2 years. The exposure of drospirenone (based on AUC) is 3 times (mice) and 8 times (rats) the exposure at the recommended clinical dose in humans. Ethinyl estradiol In the use of other drugs containing ethinyl estradiol, ethinyl estradiol has been observed to induce tumors in rodents, which is believed to be due to the species-specific effects of estrogen on prolactin secretion in rodents. In the combination study, the co-administration of drospirenone and ethinyl estradiol to female rats in the third third of pregnancy can cause feminization of male fetuses and masculinization of female fetuses in a dose-dependent manner. The feminization of male fetuses is related to the anti-androgenic effect of drospirenone, and the systemic exposure is approximately 8-13 times the expected clinical exposure (based on AUC). The systemic exposure of drospirenone when masculinization of female fetuses occurs is approximately 2-5 times the expected clinical exposure (based on AUC). After daily administration of drospirenone and ethinyl estradiol to pregnant monkeys during the stage of organ development and sexual organ differentiation, the abortion rate increased in a dose-dependent manner, but no teratogenic effects were observed. Administration of drospirenone and ethinyl estradiol to pregnant rabbits can lead to a dose-dependent increase in embryonic mortality and increased pre-implantation and post-implantation loss. In a 2-year oral carcinogenicity study in rats and mice, mice or rats were given drospirenone 10 mg/kg/d or drospirenone: ethinyl estradiol at a ratio of 1:0.01, 3:0.03, 10:0.1 mg/kg/day. The drospirenone exposure (AUC) of mice was 0.1 to 2 times that of humans when given a single contraceptive. In the drospirenone alone group, the incidence of cancer in the Harderian gland increased; the exposure of rats was 0.8 to 10 times that of humans when given a single contraceptive. The incidence of benign and malignant adrenal pheochromocytoma increased in the high-dose drospirenone test group. After co-administration of drospirenone and ethinyl estradiol, the incidence of tumors in the following sites increased: mammary gland and uterus of mice and rats and pituitary gland of mice. The tumor incidence was similar when ethinyl estradiol was given alone, but the incidence was further increased, suggesting that ethinyl estradiol is associated with an increased tumor incidence. The co-administration of drospirenone and ethinyl estradiol reduced the carcinogenic potential of ethinyl estradiol to the pituitary gland of mice and the uterus and mammary gland of rats. It should be noted that sex steroid hormones can promote the growth of certain hormone-dependent tissues and tumor growth.

24 light pink film-coated tablets containing hormones: each tablet contains 0.02 mg of ethinyl estradiol (in the form of b-cyclodextrin inclusion complex) and 3 mg of drospirenone. 4 white film-coated tablets without hormones.

Tablets containing hormones are light pink film-coated tablets, which appear white after the coating is removed. Tablets without hormones are white film-coated tablets with a regular hexagon engraved on one side and the word "DP" engraved in the middle.

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Route of AdministrationOral Dosage ScheduleHow to TakeThis product is taken orally as one tablet at the same time each day. If a dose is missed or taken incorrectly, the failure rate will increase. To achieve the greatest contraceptive effect, this product must be taken correctly in the order specified on the package insert. If a dose is missed, take a tablet as soon as you remember. How to Start Taking This ProductInform the patient to start taking this product on the first day of menstruation. During the first cycle of using this product, tell the patient to take one light pink tablet daily, starting on day 1 of the menstrual cycle (day 1 refers to the first day of menstruation). One light pink tablet should be taken daily for 24 consecutive days, followed by one white inactive tablet daily on days 25-28. The tablets must be taken with a small amount of liquid at approximately the same time each day in the order indicated on the package, preferably on the 24th day of the menstrual cycle.

The following serious adverse reactions that occur when using COCs are discussed in the [Precautions] section of the instructions: cardiovascular events and stroke, vascular events, liver disease, common adverse reactions reported by COC users; irregular uterine bleeding, nausea, breast tenderness, headache. Please refer to the instructions for detailed information.

Women with the following conditions should not use this product: · Renal impairment · Adrenal insufficiency · Increased risk of arterial or venous thromboembolic disease. This includes women with the following conditions: . Smoking and over 35 years old . Current or past deep vein thrombosis or pulmonary embolism . Cerebrovascular disease . Coronary heart disease . Thrombotic valvular heart disease or thrombotic heart rhythm disease (such as subacute bacterial endocarditis with valvular disease or atrial fibrillation) . Hereditary or acquired hypercoagulable disease . Uncontrolled hypertension . Diabetes with vascular disease . Headache with focal neurological symptoms; or migraine with or without aura, and over 35 years old . Undiagnosed abnormal uterine bleeding . Current or past breast cancer or other estrogen- or progesterone-sensitive cancer . Benign or malignant liver tumors

Precautions for children: The safety and efficacy of this product have been established in women of childbearing age. In adolescent girls under 18 years of age, the expected safety and efficacy are the same as those for women ≥ 18 years of age. This product cannot be used before menarche. Precautions during pregnancy and lactation: Pregnancy There is little or no increased risk of birth defects in women who accidentally took COCs in early pregnancy. Epidemiological studies and meta-analyses have found that there is no increased risk of genital or non-genital birth defects (including cardiac anomalies and short limb defects) after exposure to low doses of COCs before conception or in early pregnancy. Withdrawal bleeding induced by COC administration should not be used as a pregnancy test. COCs should not be used to treat threatened or habitual abortion during pregnancy. Postpartum women who are not breastfeeding should take COCs no earlier than 4 weeks after delivery. Lactation If possible, breastfeeding women are advised to use other contraceptive measures before weaning. Estrogen-containing COCs can reduce milk production in breastfeeding women. Once a lactation pattern is established, this is less likely to occur, however, Elderly Note: This product has not been studied in postmenopausal women and is not suitable for use in this population.

Effects of other drugs on combined hormonal contraceptives Substances that reduce the effectiveness of COCs: Drugs or herbal remedies that induce specific enzymes (including CYP3A4) may reduce the effectiveness of COCs or increase breakthrough bleeding. Drugs or herbal remedies that may reduce the effectiveness of hormonal contraceptives include: phenytoin, barbiturates, carbamazepine, bosentan, felbamate, griseofulvin, oxcarbazepine, rifampin, topiramate, and products containing St. John's wort (Hypericum perforatum). Interactions between oral contraceptives and other drugs may lead to breakthrough bleeding and/or contraceptive failure. Advise women to use an alternative contraceptive or back-up method when using enzyme inducers with COCs and to continue using back-up contraception for 28 days after discontinuation of the enzyme inducer to ensure contraceptive reliability. Can increase the effectiveness of COCs

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Ethinylestradiol 0.020 mg and drospirenone 3.000 mg

24 months