Perry M D, McEvoy G K
Clin Pharm. 1983 Jan-Feb;2(1):12-9.
The chemistry, pharmacology, pharmacokinetics, clinical use, adverse effects, dosage and administration, and FDA-approved indications of isotretinoin, a new agent used for treating acne, are reviewed. Isotretinoin is a synthetic retinoid compound with pharmacologic actions similar to those of other retinoids. Isotretinoin's effects on nodulocystic acne lesions apparently result from its reduction of the size of sebaceous glands, inhibition of sebum production, and inhibition of follicular keratinization. Isotretinoin is administered orally; peak serum drug concentrations occur approximately three hours after ingestion. The drug is widely distributed throughout body tissues and metabolized by the liver by oxidation and glucuronidation; both parent drug and metabolites are excreted in the urine and feces. Clinical trials of isotretinoin have shown the drug to be effective in treating cystic or conglobate acne that is unresponsive to therapy with oral or topical antibiotics, topical tretinoin, or topical benzoyl peroxide. Isotretinoin is unique in that acne remission continues after discontinuance of therapy. The most frequent adverse effects involve mucocutaneous tissues and include cheilitis, xerosis, xerostomia, dry nose, epistaxis, and pruritus. Other adverse effects--including some serious ones--have been found rarely in humans or animals receiving isotretinoin. The usual oral dosage of isotretinoin for patients with cystic acne is 1-2 mg/kg/day in two divided doses; administration should continue for 15-20 weeks. Isotretinoin is currently more expensive than other acne treatments. Isotretinoin is an effective agent for treating cystic acne; pending accumulation of further data, its use should be limited to patients with severe conditions that do not respond to older therapies because of isotretinoin's cost and sometimes serious adverse effects.
本文综述了异维A酸这一治疗痤疮新药的化学性质、药理学、药代动力学、临床应用、不良反应、剂量与用法以及美国食品药品监督管理局（FDA）批准的适应症。异维A酸是一种合成类视黄醇化合物，其药理作用与其他类视黄醇相似。异维A酸对结节囊肿性痤疮损害的作用，显然源于其减小皮脂腺大小、抑制皮脂分泌以及抑制毛囊角化。异维A酸口服给药；服药后约三小时达到血清药物浓度峰值。该药广泛分布于全身组织，并在肝脏中通过氧化和葡萄糖醛酸化代谢；母体药物及其代谢产物均经尿液和粪便排出。异维A酸的临床试验表明，该药对口服或外用抗生素、外用维甲酸或外用过氧化苯甲酰治疗无效的囊肿性或聚合性痤疮有效。异维A酸的独特之处在于停药后痤疮缓解仍会持续。最常见的不良反应累及皮肤黏膜组织，包括唇炎、皮肤干燥、口干、鼻干、鼻出血和瘙痒。在接受异维A酸治疗的人类或动物中，很少发现其他不良反应，包括一些严重的不良反应。囊肿性痤疮患者异维A酸的常用口服剂量为每日1 - 2mg/kg，分两次服用；给药应持续15 - 20周。异维A酸目前比其他痤疮治疗药物更昂贵。异维A酸是治疗囊肿性痤疮的有效药物；在积累更多数据之前，由于异维A酸的成本以及有时出现的严重不良反应，其使用应限于对传统疗法无反应的重症患者。
