Pharmacokinetics and Therapeutic Efficacy of Retinoids in Skin Diseases
Pharmacokinetics and Therapeutic Efficacy of Retinoids in Skin Diseases
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类维生素A在皮肤病中的药代动力学和治疗效果
DOI：
10.2165/00003088-199223010-00004
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发表时间：
1992
影响因子：
4.5
通讯作者：
K. Kragballe
中科院分区：
文献类型：
--
作者：
F. G. Larsen;F. Nielsen‐Kudsk;P. Jakobsen;K. Weismann;K. Kragballe
维甲酸是一类化合物，包括维生素A的天然形式和合成类似物。异维甲酸通常被称为第一代维甲酸，可能对严重的顽固性痤疮患者有相当大的好处。代表第二代的两种芳香族化合物埃维甲酸酯和阿维A酸在治疗牛皮癣方面取得了重大成功，特别是与更传统的疗法相结合。维生素A增多症的典型不良反应与维甲酸治疗有关；因此，接受维甲酸治疗的育龄妇女坚持避孕方案尤为重要。这些药物被广泛代谢，只有微量的未改变的药物在尿液中被清除。异维A酸、乙酸乙酯和阿维A在长期治疗后的消除半衰期分别为20h、120d和48h。由于这些药物的血药浓度和预期药理作用之间缺乏明确的相关性，再加上口服这些药物后个体间和个体内的系统利用度差异非常显著(15%到90%)，因此只能根据这些药物的一般药代动力学来粗略地判断个体患者的初始剂量。以后的剂量调整应根据血药浓度(和可能的代谢物)浓度以及药物的有效性和耐受性进行监测。
SummaryThe retinoids are a class of compounds that includes the natural forms and synthetic analogues of vitamin A. Isotretinoin, often referred to as a first generation retinoid, may be of considerable benefit to patients with severe, recalcitrant acne. Etretinate and acitretin, 2 aromatic compounds representing the second generation, have found their major success in the treatment of psoriasis, particularly in combination with more traditional therapies. Retinoid therapy is associated with a distinctive adverse effect profile typical of hypervitaminosis A; thus, it is especially important that fertile women undergoing retinoid therapy adhere to a contraceptive regimen. These drugs are extensively metabolised and only traces of unchanged drugs are eliminated in urine. The terminal elimination half-lives of isotretinoin, etretinate and acitretin after long term treatment are up to 20h, 120 days and 48h, respectively. Because of lack of definite correlation between plasma concentration and desired pharmacological effects, in conjunction with the very pronounced inter- and intraindividual variation in systemic availability (15 to 90%) after oral administration of these drugs, initial dosages in individual patients can only be roughly judged on the basis of the general pharmacokinetics of the agents. Later dosage adjustments should be made on the basis of monitoring of both plasma drug (and possible metabolite) concentrations, and the efficacy and tolerability of the drugs.
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三种剂量水平的口服 13-顺式视黄酸对皮脂分泌可持续率和痤疮的影响。
影响因子：
13.8
作者：
Stewart,ME;Benoit,AM;Stranieri,AM;Rapini,RP;Strauss,JS;Downing,DT
通讯作者：
Downing,DT
13-顺式视黄酸在晚期癌症患者中的药代动力学。
影响因子：
11.2
作者：
Goodman,GE;Einspahr,JG;Alberts,DS;Davis,TP;Leigh,SA;Chen,HS;Meyskens,FL
通讯作者：
Meyskens,FL
致畸生物测定中阿维A酯的生物转化以及阿维A酯和其他芳香族视黄醇的发育毒性。
DOI：
--
发表时间：
1989
期刊：
Drug metabolism and disposition: the biological fate of chemicals
影响因子：
--
作者：
Kochhar,DM;Penner,JD;Minutella,LM
通讯作者：
Minutella,LM
异维A酸治疗长期皮脂产生的变化。
影响因子：
13.8
作者：
Strauss,JS;Stranieri,AM
通讯作者：
Stranieri,AM
异维A酸对囊性痤疮患者体内的单核细胞和中性粒细胞趋化性产生显着的抑制作用。
DOI：
10.1111/1523-1747.ep12580370
发表时间：
1987
期刊：
The Journal of investigative dermatology
影响因子：
--
作者：
Norris,DA;Osborn,R;Robinson,W;Tonnesen,MG
通讯作者：
Tonnesen,MG