药品详细
Acitretin(阿维A)
化学结构式图
中文名
阿维A
英文名
Acitretin
分子式
C21H26O3
化学名
(2E,4E,6E,8E)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoic acid
分子量
Average: 326.4293
Monoisotopic: 326.188194698
Monoisotopic: 326.188194698
CAS号
55079-83-9
ATC分类
D05B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of etretinate with the advantage of a much shorter half-life when compared with etretinate. [PubChem]
生产厂家
- Stiefel laboratories inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes | Not Available |
| Substructures | Not Available |
适应症
药理
| Indication | For the treatment of severe psoriasis in adults. |
| Pharmacodynamics | Acitretin is a retinoid. Retinoids have a structure similar to vitamin A and are involved in the normal growth of skin cells. Acitretin works by inhibiting the excessive cell growth and keratinisation (process by which skin cells become thickened due to the deposition of a protein within them) seen in psoriasis. It therefore reduces the thickening of the skin, plaque formation and scaling. |
| Mechanism of action | The mechanism of action of acitretin is unknown, however it is believed to work by targeting specific receptors (retinoid receptors such as RXR and RAR) in the skin which help normalize the growth cycle of skin cells. |
| Absorption | Oral absorption of acitretin is optimal when given with food, and is linear and proportional with increasing doses from 25 to 100 mg. Approximately 72% (range 47% to 109%) of the administered dose was absorbed after a single 50 mg dose of acitretin was given to 12 healthy subjects. |
| Volume of distribution | Not Available |
| Protein binding | Over 99.9% bound to plasma proteins, primarily albumin. |
| Metabolism |
Following oral absorption, acitretin undergoes extensive metabolism and interconversion by simple isomerization to its 13-cis form (cis-acitretin). Both parent compound and isomer are further metabolized into chain-shortened breakdown products and conjugates, which are excreted.
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| Route of elimination | Both parent compound and isomer are further metabolized into chain-shortened breakdown products and conjugates, which are excreted. The chain-shortened metabolites and conjugates of acitretin and cis-acitretin are ultimately excreted in the feces (34% to 54%) and urine (16% to 53%). |
| Half life | 49 hours (range 33 to 96 hours) |
| Clearance | Not Available |
| Toxicity | Oral, rat: LD50 = >4000 mg/kg. Symptoms of overdose include headache and vertigo. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Demeclocycline | Increased risk of intracranial hypertension |
| Doxycycline | Increased risk of intracranial hypertension |
| Methacycline | Increased risk of intracranial hypertension |
| Methotrexate | Acitretin/etretinate increases the effect and toxicity of methotrexate |
| Minocycline | Increased risk of intracranial hypertension. |
| Norethindrone | Acitretine may cause a loss of contraceptive effect |
| Oxytetracycline | Increased risk of intracranial hypertension |
| Rolitetracycline | Increased risk of intracranial hypertension |
| Tetracycline | Increased risk of intracranial hypertension |
| Vitamin A | Acitretin increases the risk of vitamin A toxicity. Avoid vitamin A supplementation while taking acitretin. |
食物相互作用
Not Available
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