Bartkowiak-Emeryk Małgorzta, Breborowicz Anna, Emeryk Andrzej, Kulus Marek, Kurzawa Ryszard, Lis Grzegorz, Mazurek Henryk, Niedziela Marek
Zakład Immunologii Klinicznej Akademii Medycznej w Lublinie.
Pol Merkur Lekarski. 2004;17 Suppl 2:11-8.
Inhaled administration of glucocorticoid doesn't mean lack of systemic effects of drug. Bioavailability of steroid depends on oral absorption and absorption from respiratory system. In case of fluticasone propionate (FP) swallowed dose can be neglected because almost total (>99%) inactivation in liver during first pass. In second part of paper the most important safety parameters of therapy with FP are discussed, it means; influence on hypothalamic-pituitary-adrenal axis, growth and bone metabolism. Interpretation of potential side effects should differentiate between abnormal value of laboratory test and clinically important symptoms. Adrenal suppression depends on dose of FP and was found even after low dose (about 200 microg per day), but clinical value of this findings is unknown. Prolonged administration of high doses can suppress hypothalamic-pituitary-adrenal axis; exceptionally, it can induce adrenal insufficiency. Recommended doses of FP given 1 to 2 years doesn't cause growth retardation. Long term studies on influence of drug on final height are needed. FP as other inhaled corticosteroids, may transiently alter bone metabolism. Till now there are no evidences that this drug, when prescribed appropriately in standard doses for asthma control, may decrease the bone mineral density or induce osteoporosis and may increase the risk of bone fractures in asthmatic children. Effective asthma control achieved with FP therapy permits normal activity and development of asthmatic children which prevails over exceptionally noticed side effects.
吸入糖皮质激素并不意味着药物没有全身作用。类固醇的生物利用度取决于口服吸收和呼吸系统吸收。就丙酸氟替卡松(FP)而言,吞咽剂量可忽略不计,因为其在首过效应期间几乎在肝脏中完全(>99%)失活。在本文的第二部分,讨论了FP治疗的最重要安全参数,即对下丘脑-垂体-肾上腺轴、生长和骨代谢的影响。对潜在副作用的解读应区分实验室检查异常值和具有临床意义的症状。肾上腺抑制取决于FP的剂量,即使在低剂量(约每天200微克)后也有发现,但这一发现的临床价值尚不清楚。长期高剂量给药可抑制下丘脑-垂体-肾上腺轴;罕见的情况下,可诱发肾上腺功能不全。推荐剂量的FP使用1至2年不会导致生长迟缓。需要对药物对最终身高的影响进行长期研究。与其他吸入性糖皮质激素一样,FP可能会短暂改变骨代谢。到目前为止,尚无证据表明,当以标准剂量适当地用于控制哮喘时,这种药物会降低骨矿物质密度或诱发骨质疏松症,也不会增加哮喘儿童骨折的风险。通过FP治疗实现的有效哮喘控制可使哮喘儿童正常活动和发育,这比罕见的副作用更为重要。