Oral isotretinoin (13-cis-retinoic acid) therapy in severe acne: drug and vitamin A concentrations in serum and skin.

Oral isotretinoin (13-cis-retinoic acid) therapy in severe acne: drug and vitamin A concentrations in serum and skin.
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口服异维A酸(13-顺式视黄酸)治疗严重痤疮:血清和皮肤中的药物和维生素 A 浓度。

DOI:
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发表时间:
1986
影响因子:
6.5
通讯作者:
A. Vahlquist
A. Vahlquist
中科院分区:
医学1区
文献类型:
--
作者:
O. Rollman;A. Vahlquist

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本文研究了17例结节性痤疮患者口服异维甲酸对皮肤的影响及其对血清和皮肤中维生素A水平的影响。所有患者均接受0.5 mg/kg/天的治疗,持续3个月,8例患者继续接受0.75 mg/kg/天的治疗,持续3个月。采用高压吸附液相色谱法对未受累皮肤的血清和活检组织中母体药物、主要代谢物(4-氧-异维甲酸)和2种天然类维甲酸(视黄醇和脱氢视黄醇)进行监测。在治疗的最初3个月,血清中异维甲酸的平均水平为145 ng/ml,表皮中为73 ng/g。4-氧-异维甲酸对应值分别为615和113 ng/g。即使在最高剂量下,血清、表皮或皮下也没有异维甲酸的进行性积累。停药后2-4周内血清和皮肤中的药物消失。通过视黄醇、视黄醇结合蛋白和前白蛋白(转甲状腺素)浓度监测的血清维生素A转运不受治疗影响。相比之下,治疗3个月后,表皮中视黄醇水平平均上升53% (p < 0.01),脱氢视黄醇水平平均下降79% (p < 0.001)。这两种变化都是可逆的。结果表明,异维甲酸治疗干扰皮肤内源性维生素A代谢。
The disposition of oral isotretinoin to the skin and the effects of the drug on the vitamin A levels in serum and skin were studied in 17 patients with nodulocystic acne. All patients received 0.5 mg/kg/day for 3 months and 8 patients continued treatment with 0.75 mg/kg/day for another 3 months. The parent drug, the major metabolite (4-oxo-isotretinoin), and 2 natural retinoids (retinol and dehydroretinol) were monitored in serum and biopsies of uninvolved skin, using adsorption high-pressure liquid chromatography. During the initial 3 months of treatment the mean isotretinoin level in the serum was 145 ng/ml and in the epidermis 73 ng/g. The corresponding values for 4-oxo-isotretinoin were 615 and 113 ng/g, respectively. Even at the highest dosage there was no progressive accumulation of isotretinoin in serum, epidermis, or subcutis. After discontinuation of therapy the drug disappeared from both serum and skin within 2-4 weeks. The serum transport of vitamin A, monitored by the concentrations of retinol, retinol-binding protein, and prealbumin (transthyretin), was not affected by the treatment. By contrast, the retinol level in the epidermis increased by an average of 53% (p less than 0.01) and the dehydroretinol level decreased by 79% (p less than 0.001) as a result of 3 months of treatment. Both changes were reversible. The results suggest that isotretinoin therapy interferes with the endogenous vitamin A metabolism in the skin.
DOI: --
发表时间: 1982
期刊: The Journal of biological chemistry
影响因子: --
作者:
Zile,MH;Inhorn,RC;DeLuca,HF
通讯作者: DeLuca,HF