药品信息:
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--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201191922522625.pdf、201112418011324.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文曲洛司坦处方资料(仅供参考)
分类名称 一级分类:内分泌系统药物 二级分类:肾上腺皮质激素类药 三级分类: 药品英文名 Trilostane 药品别名 腈环乙雄烷、Modrenal 药物剂型 胶囊:60mg。 药理作用 主要抑制皮质激素合成过程中的3β-脱氢酶,使皮质醇、醛固酮合成减少。本品也有明显的降低血睾酮水平作用,可能与抑制其合成有关。 药动学 本品口服吸收容易,血药浓度高峰约4h,代谢产物主要经尿排出。 适应证 主要用于治疗库欣综合征(皮质醇增多症)和原发性醛固酮增多症,但治疗库欣综合征(皮质醇增多症)的疗效不如美替拉酮。 禁忌证 肝、肾功能不良及孕妇不宜使用。 注意事项 用药期间应监测血皮质醇水平、电解质和血压。出现应激时应停药,必要时补充皮质激素。如同时使用保钾利尿药要注意发生高钾血症。 不良反应 不良反应较轻,部分病人可有脸红、恶心、呕吐、腹泻和胃肠不适。 用法用量 口服,每次60mg,2次/d。3~7天后,可根据病人对疗效反应调整剂量。一般的剂量范围是120~360mg/d,最大不超过480mg。
MODRENAL Drug Class Description : Steroid synthesis inhibitors.
Generic Name : Trilostane - neoplastic disorders
Drug description : Each Modrenal capsule contains either 60 mg or 120 mg Trilostane (4?, 5-epoxy -17? - hydroxy -3 -OXO -5? -androstane -2? -carbonitrile.)
Presentation : 60 mg capsules: opaque pink/black Size 3 hard gelatine capsules marked with 60 on one end. 120 mg capsules: opaque pink/yellow Size 1 hard gelatine capsules marked with 120 on one end
Indications : (a) For the control of the manifestation of adrenal cortical hyperfunction in such conditions as hypercortisolism and primary aldosteronism. (b) For the treatment of postmenopausal advanced breast cancer following relapse to initial hormone therapy e.g. oestrogen receptor antagonists.
Adult Dosage : Modrenal for oral administration only.
Adrenal Cortical Hyperfunction - 240 mg/day in divided doses for at least three days, then dose adjustment according to the patient's clinical response and appropriate biochemical monitoring. The usual dose is 120–480 mg/day but may be increased to 960 mg.
Postmenopausal Breast Cancer - The daily dose given in divided doses should increase stepwise every three days from 240 mg to 480 mg to 720 mg to 960 mg. This dose should be maintained but if it cannot be tolerated it may be reduced to 720 mg/day. From the start of Trilostane therapy a physiological replacement dose of a glucocorticoid (e.g. Hydrocortisone 30 mg/day in divided doses) should be given to prevent activation of the HPA axis.
Elderly - There are no special dosage recommendations.
Child Dosage : Not recommended.
Contra Indications : Trilostane is contraindicated in pregnancy and children.
Special Precautions : Pregnancy should be excluded before beginning treatment and nonhormonal contraceptive methods should be used during therapy where appropriate.
As with all drugs that are metabolised by the liver and excreted by the kidney, caution should be exercised when treating patients with gross hepatic or renal impairment. It is advisable to monitor response when treating adrenal cortical hyperfunction, by regular assays of blood electrolytes and circulating corticosteroids, and adjust the dose accordingly. In some patients the suppression of aldosterone production may cause hyperkalaemia and hyponatraemia with subsequent hypotension – under these circumstances a mineralocorticoid should be given, e.g. Fludro-cortisone 0.1 mg/day. In other patients it is possible to produce corticosteroid insufficiency, especially if the production of ACTH is limited, and then a glucocorticoid may be necessary.
When treating hypercortisolism due to excess ACTH production (whether ectopic or pituitary), an initial response may be followed by a relapse if the hypophyseal/pituitary/adrenal (HPA) axis is still intact and is not suppressed. If, however, the excessive steroid production is due to an adrenal cortical tumour, or the HPA axis is no longer able to respond to lowered levels of circulating glucocorticoids, the condition will remain responsive to Trilostane.
Interactions : When administered concurrently with thiazide diuretics the inhibition of aldosterone production caused by Trilostane reduces potassium loss whilst maintaining the natriuretic effect.
Adverse Reactions : Flushing, tingling in mouth, palatal swelling, rhinorrhoea, sickness, vomiting, diarrhoea, and cramps have been reported commonly. These are generally mild and reversible on adjusting dose, administering with food, stopping therapy and/or symptomatic treatment (e.g. antacid, antidiarrhoeal with a small dose of aspirin). More severe signs of stomach upset, e.g. bleeding or ulcer, usually occur with concurrent administration of nonsteroidal anti-inflammatory drugs – reducing the dose of these latter drugs and/or adding an H2 blocker will usually resolve these problems.
Skin rashes can occur occasionally but are usually self limiting.
Very rarely, in cancer patients whose bone marrow is compromised by disease or chemotherapy, granulocytopenia has been reported - it is reversible on stopping therapy.
Manufacturer : Genzyme Therapeutics
Drug Availability : (POM)
Drug Updated : 03 June 2009
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201191922522625.pdf、201112418011324.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- |