Endometriosis
Adult: 2 mg once daily given in a continuous regimen regardless of menstrual bleeding.
Child: ≥12 yr (postmenarche): Same as adult dose.
Child: ≥12 yr (postmenarche): Same as adult dose.
Chỉ định và Liều dùng
Oral
Endometriosis Adult: 2 mg once daily given in a continuous regimen regardless of menstrual bleeding.
Child: ≥12 yr (postmenarche): Same as adult dose. |
Suy gan
Severe: Contraindicated.
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Cách dùng
May be taken with or without food.
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Chống chỉ định
Active venous thromboembolic disorder, active or history of arterial and CV disease (e.g. MI, CVA, ischaemic heart disease), DM w/ vascular involvement, presence or history of liver tumour, sex-hormone dependent malignancies, undiagnosed vag bleeding, ocular lesion due to vascular ophth disease (e.g. partial or complete visual loss, defect in visual fields), migraine w/ focal aura. Severe hepatic (e.g. cirrhosis) impairment. Pregnancy and lactation.
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Thận trọng
Patient w/ multiple risk factors for CV disease (e.g. old age, HTN, DM, hypercholesterolemia, morbid obesity, smoker), history of depression or gestational DM. Childn.
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Tác dụng không mong muốn
Significant: Menstrual bleeding irregularity (e.g. amenorrhea, prolonged bleeding, frequent/infrequent bleeding), increased risk of venous thromboembolism, plateauing and loss of BMD, HTN, chloasma, ovarian cyst. Rarely, liver tumours.
Nervous: Depression, headache, dizziness, lethargy, sleep disorder, nervousness, irritability, migraine. GI: Nausea, vomiting, abdominal pain. Hepatic: Cholestatic jaundice. Genitourinary: Vag haemorrhage, spotting. Endocrine: Decreased libido, wt gain, breast discomfort. Musculoskeletal: Weakness. Dermatologic: Acne, alopecia, androgenic effects (e.g. hirsutism, greasy hair). Immunologic: Hypersensitivity. |
Thông tin tư vấn bệnh nhân
Avoid smoking.
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Chỉ số theo dõi
Perform pregnancy test prior to initiation of therapy. Assess BP, pap smear, breast exam, mammogram. Monitor BMD (adolescent females), signs and symptoms of thromboembolic disorders, vision changes.
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Tương tác
Increased exposure w/ CYP3A4 enzyme inhibitors (e.g. azole antifungals, verapamil, macrolides, diltiazem, antidepressants). Decreased therapeutic effect w/ CYP3A4 enzyme inducers (e.g. phenytoin, barbiturates, primidone, carbamazepine, rifampicin, topiramate, griseofulvin).
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Tương tác với thức ăn
Decreased therapeutic effect w/ St John’s wort. Increased exposure w/ grapefruit juice.
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Ảnh hưởng đến kết quả xét nghiệm
May interfere w/ LFT and endocrine function test.
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Tác dụng
Description:
Mechanism of Action: Dienogest, a nonethinylated progestogen, reduces oestradiol production, thereby suppressing oestradiol’s trophic effects on both eutopic and ectopic endometrium. It leads to hypoestrogenic, hyperestagenic endocrine environment causing initial decidualisation of endometrial tissue followed by atrophy of endometriotic lesions when continuously given. It also has immunologic, antiproliferative, and antiangionenic effects which inhibit cellular proliferation. Pharmacokinetics: Absorption: Rapidly and almost completely absorbed. Bioavailability: Approx 91%. Time to peak plasma concentration: Approx 1.5 hr. Distribution: Volume of distribution: 40 L. Plasma protein binding: Approx 90%. Metabolism: Metabolised in the liver by CYP3A4 enzyme to inactive metabolites. Excretion: Via urine, mainly as inactive metabolite. Elimination half-life: 14 hr. |
Đặc tính
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Bảo quản
Store between 15-30°C.
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Phân loại MIMS
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Phân loại ATC
G03DB08 - dienogest ; Belongs to the class of pregnadien derivative progestogens used in progestogenic hormone preparations.
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Tài liệu tham khảo
Anon. Dienogest. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/05/2017. Buckingham R (ed). Dienogest. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/05/2017.
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