Mills Hilla, Acquah Ronald, Tang Nova, Cheung Luke, Klenk Susanne, Glassen Ronald, Pirson Magali, Albert Alain, Hoang Duong Trinh, Van Thang Nguyen
Department of Medical Science, University for Development, Accra, Ghana.
RD Lab, The Hospital Institute for Hebal Research, Toluca 50200, MEX, Mexico.
Emerg Med Int. 2022 Jul 18;2022:2593740. doi: 10.1155/2022/2593740. eCollection 2022.
Chronic obstructive pulmonary diseases (COPD) and asthma are fatal. The respiratory tract may be blocked, robbed of the adequate amounts of oxygen; hence, death ensues if a quick medical attention is not provided. The treatment available for the duo are inhaled corticosteroids (ICS). The ICS can work synergically with LABAS (long-acting -antagonists) and so many other medicines like bronchodilators. The drugs used for the treatment of asthma and COPD are metabolised once in the body system and at the same time exerting the therapeutic effect provided the concentration of the drug is within the therapeutic window. The CYP3A isoforms metabolise the ICS, in this case, salmeterol and fluticasone propionate (FP). Methods of administration are not limited to inhalation. Specific doses are prescribed accurately paying attention to factors like age, gender, race, and genetic makeup since these affect drug metabolisms. Generally, the ICS work by translocating glucocorticoid receptors to the nucleus from the cytosol. The mechanism is potentiated by the -antagonists and this brings about an anti-inflammatory effect which is greater than either of the two drugs alone. Once this happens, it is not necessary to increase ICS dose. The ICS, in addition, cause more production of -receptors by activating the -receptor genes. This mode of action begets the LABAs' bronchodilator-effects. The challenge is that ICS are not limited only to "double" therapy. Analysing such therapies is daunting since coadministration interferes with pharmacology and pharmacokinetics of drugs. This work focuses on salmeterol/fluticasone propionate combination and aspects which has to do with administration, monitoring, metabolism, toxicity, and adverse effects.
慢性阻塞性肺疾病（COPD）和哮喘是致命的。呼吸道可能会被阻塞，无法获得足够的氧气；因此，如果不迅速就医，就会导致死亡。用于治疗这两种疾病的药物是吸入性糖皮质激素（ICS）。ICS可以与长效β2受体激动剂（LABA）以及许多其他药物如支气管扩张剂协同作用。用于治疗哮喘和COPD的药物在体内系统中代谢一次，同时只要药物浓度在治疗窗内就会发挥治疗作用。在这种情况下，CYP3A同工酶会代谢ICS，即沙美特罗和丙酸氟替卡松（FP）。给药方法不限于吸入。会根据年龄、性别、种族和基因组成等因素准确开出特定剂量，因为这些因素会影响药物代谢。一般来说，ICS通过将糖皮质激素受体从细胞质转运到细胞核来发挥作用。β2受体拮抗剂可增强这一机制，从而产生比单独使用这两种药物中任何一种都更强的抗炎作用。一旦出现这种情况，就没有必要增加ICS的剂量。此外，ICS通过激活β2受体基因导致更多β2受体的产生。这种作用方式产生了LABA的支气管扩张作用。挑战在于ICS不仅限于“双重”疗法。分析此类疗法颇具难度，因为联合给药会干扰药物的药理学和药代动力学。这项工作聚焦于沙美特罗/丙酸氟替卡松组合以及与给药、监测、代谢、毒性和不良反应相关的方面。
