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Relugolix blocks the GnRH receptor in the anterior pituitary gland, reducing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby lowering estrogen levels in the body. This mechanism is very effective in treating uterine fibroids and endometriosis, because the development and progression of these diseases are closely related to high levels of estrogen.
1. Generic name :Relugolix
2. Trade name u2 00c:MYFEMBREE® (compound preparation, containing relugolix, estradiol and norethindrone acetate)
3. Dosage form :Oral film-coated tablet
4. Main ingredients :Each tablet contains 40 mg of relugolix, 1 mg of estradiol (E2), and 0.5 mg of norethindrone acetate (NETA)
1. Severe bleeding related to uterine fibroids: For patients whose fibroids cause menstrual flow >80ml/cycle or cause anemia (Hb<110g/L);
2. Pain related to endometriosis: Suitable for pelvic pain with VAS score ≥ 4 points, with or without deep infiltrating nodules.
3. Limitation of use : The treatment time shall not exceed 24 months (because it may cause irreversible decrease in bone density).
1. Specifications : Each tablet contains 40mg/E21mg/NETA0.5mg of relugolix. It is a light yellow to yellow round film-coated tablet with "MVT" engraved on one side and "415" on the other side.
2. Packaging : 28 pieces/bottle (including desiccant), equipped with child-safe bottle cap.
1. Conventional dose : Take 1 tablet once a day, swallow the whole tablet, with food or on an empty stomach.
2. Treatment of missed doses : If you miss a dose, you should take it as soon as possible on the same day, and take it at the original planned time the next day; there is no need to make up the dose after vomiting.
3. Special medication : When combined with P-gp inhibitors (such as erythromycin), an interval of at least 6 hours is required (take MYFEMBREE first).
1. Monitoring requirements :
Monitor bone density (DXA scan), liver function, blood pressure, blood lipids and blood sugar regularly before and during treatment.
If you develop jaundice, chest pain, sudden vision changes, or severe headache, seek medical attention immediately.
2. Contraceptive measures : Non-hormonal contraception (such as condoms) must be used during treatment and within 1 week after stopping the drug.
3. Diet : Avoid grapefruit juice (may interfere with metabolism).
1. Pregnant women: : Absolute contraindications (can cause early miscarriage).
2. Lactation : Breastfeeding is prohibited during treatment and within 1 week of drug withdrawal.
3. Liver damage : Contraindicated for moderate to severe liver damage (Child-PughB/C).
4. U200c for the elderly: No dosage adjustment is required, but monitoring is required.
1. Common (≥3%) : Hot flashes (10.6%), abnormal uterine bleeding (6.3%), hair loss (3.5%), and loss of sexual desire (3.1%).
2. Severe reactions : Thrombotic events (DVT/PE), liver toxicity, depression or suicidal tendencies, and prolapse of uterine fibroids.
1. History or high risk of thrombotic diseases (such as smoking and age >35 years, uncontrolled hypertension).
2. Pregnancy, breast cancer or other hormone-sensitive tumors.
3. Osteoporosis or severe liver disease.
4. Those who are allergic to ingredients.
1. P-gp inhibitor : Increase the exposure of relugolix and require an interval of 6 hours;
2. Strong CYP3A inducer (such as rifampicin):Reduce efficacy, avoid combined use;
3. Hormonal contraceptive :May reduce efficacy and increase adverse reactions.
Save at room temperature (15-30°C). The original bottle should be protected from light and moisture, and the desiccant cannot be removed.