Estradiol Drospirenone Tablets

Estradiol: Estradiol drospirenone tablets contain synthetic 17β-estradiol, which has the same chemical properties and biological functions as endogenous human estradiol. It can supplement the insufficient estrogen secretion in postmenopausal women and relieve postmenopausal symptoms. Estrogen can prevent bone loss caused by menopause or oophorectomy. Drospirenone: Drospirenone is a synthetic progestin. Because estrogen can promote the growth of the endometrium, unopposed estrogens increase the risk of endometrial hyperplasia and endometrial cancer. For women with an intact uterus, progestins can reduce but not eliminate the risk of estrogen-induced endometrial hyperplasia. Drospirenone has anti-aldosterone activity, increases water and sodium excretion, and reduces potassium excretion. In animal experimental studies, drospirenone has no estrogenic, glucocorticoid, or anti-glucocorticoid activity.

Each tablet contains estradiol 1.0 mg and drospirenone 2.0 mg

This product is a medium red round film-coated tablet with a regular hexagon printed on one side and the letters DL engraved in the middle. It appears white after removing the coating.

Used to treat moderate to severe vasomotor symptoms such as vulvar and vaginal atrophy caused by menopause in women.

Each package contains 28 days of treatment. Treatment should be continued continuously, i.e. immediately start taking the next box after finishing one, without any intervals. Swallow the tablet whole with a small amount of liquid, and the time of taking the medicine is not affected by food. It is best to take the medicine at the same time every day.

Serious adverse reactions associated with hormone replacement therapy are also described in [Precautions]. The table below lists adverse reactions according to the MedDRA system organ class (MedDRAS0Cs). The determination of their frequency is based on clinical trials. Adverse reactions are from 7 Phase III clinical studies (n=2524 women). The most common adverse reactions are breast pain (>10%) and bleeding and spotting (>10%) that occur in the first few months of treatment. Irregular bleeding often improves with continuous treatment (see "Effects of drospirenone" in [Pharmacology and Toxicology]. The frequency of bleeding decreases with the course of treatment. Additional instructions for special populations: 1. The following are adverse reactions in 2 clinical trials conducted in women with hypertension. (1) Metabolic and nutritional diseases: hyperkalemia (2) Cardiac diseases: heart failure, atrial flutter, QT interval prolongation, cardiac hypertrophy; (3) Laboratory tests: increased blood aldosterone 2. The following are adverse reactions that have been reported in other HRT drugs: (1) erythema nodosum, erythema multiforme, chloasma and hemorrhagic dermatitis, etc. (2) In women with hereditary angioedema, exogenous estrogen may induce or aggravate the symptoms of angioedema (see [Precautions]).

Hormone replacement therapy should not be used when any of the following conditions exist. If any of the following conditions occur during the use of hormone replacement therapy, it should be stopped immediately: unexplained abnormal genital bleeding; known or suspected breast cancer; known or suspected sex hormone-dependent precancerous lesions or malignant tumors; current or previous liver tumors (benign or malignant); severe liver disease; untreated endometrial hyperplasia; acute liver disease, or a history of liver disease and liver function has not yet returned to normal; porphyria; severe renal insufficiency or acute renal failure; acute arterial thromboembolism (such as myocardial infarction and stroke); active deep vein thrombosis; thromboembolic disease, or a history of these diseases; severe hypertriglyceridemia; pregnancy or lactation, known allergy to the active ingredients or excipients in the drug.

Precautions for children: Estradiol drospirenone tablets cannot be used in children. Precautions for pregnancy and lactation: Estradiol drospirenone tablets are absolutely prohibited for use during pregnancy and lactation (see [Contraindications]). If you become pregnant while using estradiol drospirenone tablets, you must stop taking the drug immediately. There is no clinical data related to pregnancy while using this product. Animal experiments have shown that the use of estradiol drospirenone tablets during pregnancy and lactation has adverse effects (see "Preclinical Safety Data" under [Pharmacology and Toxicology]). The potential risk to humans is unclear. Current epidemiological research data do not suggest that women who accidentally take estrogen-progestin combination preparations during pregnancy have teratogenic effects on the fetus. Drospirenone can be excreted in small amounts through breast milk. Precautions for the elderly: There is no special dosage recommendation for the elderly.

1. Effects of other drugs on estradiol drospirenone tablets The induction of liver enzymes can increase the clearance of sex hormones, which may reduce the effect of drugs and lead to irregular bleeding. Drugs known to have liver enzyme induction activity include hydantoins, barbiturates, deoxyphenobarbital, carbamazepine and rifampicin, while oxcarbazepine, topiramate, felbamate and griseofulvin are also suspected to have liver enzyme induction activity. The mechanism of interaction may be based on the characteristics of these drugs in inducing liver enzymes. The peak of liver enzyme induction occurs at 2 to 3 weeks of medication and can last for 4 weeks after discontinuation of medication. Although ritonavir and nelfinavir are known to be strong inhibitors of drug-metabolizing enzymes, the enzymes will be induced when these two drugs are used simultaneously with steroid hormone therapy. Chinese patent medicine preparations containing St. John's wort may induce the metabolism of estrogen and progesterone. In rare cases, a decrease in estradiol levels occurs when certain antibiotics (such as penicillin and tetracycline) are used at the same time. The cytochrome P450 system is not involved in the formation of the main metabolites of drospirenone. Therefore, inhibitors of this enzyme system may not affect the metabolism of drospirenone. However, inhibitors of CYP3A4 such as cimetidine and ketoconazole may inhibit the metabolism of estradiol. 2. Interaction with alcohol Rapid drinking during HRT can increase the level of circulating estradiol. 3. Interaction between estradiol drospirenone tablets and other drugs In vitro inhibition studies using a steady-state dose of 3 mg drospirenone per day and omeprazole, simvastatin or midazolam as labeled substrates and in vivo interaction studies in female volunteers showed that drospirenone has little effect on clinically relevant interactions with other drugs metabolized by cytochrome P450 enzymes. 4. Pharmacodynamic interactions with antihypertensive drugs and nonsteroidal anti-inflammatory drugs (NSAIDs) Women who are treated with estradiol drospirenone tablets and antihypertensive drugs such as ACE inhibitors, angiotensin II receptor antagonists, and hydrochlorothiazide may experience additional blood pressure drops. The combined use of estradiol drospirenone tablets and non-steroidal anti-inflammatory drugs (NSAIDs) or antihypertensive drugs is unlikely to increase blood potassium. The simultaneous use of three drugs may lead to a slight increase in blood potassium, which is more obvious in diabetic women. 5. Laboratory tests The use of steroid sex hormones may affect certain laboratory test results, including biochemical parameters of liver, thyroid, adrenal and renal function, plasma (carrier) protein levels such as sex hormone binding globulin and blood lipid/lipoprotein ratio, and coagulation and fibrinolysis parameters. Changes in these parameters are usually within the normal range. Estradiol drospirenone tablets have no effect on glucose tolerance.

Store below 30°C. Store properly and keep out of reach of children.

Each tablet contains estradiol 1.0 mg and drospirenone 2.0 mg

60 months