The exact mechanism of action is not known,possible explanation is altered gene expression through nuclear retinoic acid receptors (RARs) and binding to DNA to cause transcription or transrepression changes in protein synthesis.
藥動學
-Absorption Systemic:Bioavailability: 59% (range 36 to 95%); Food: increases absorption.
-Metabolism: Systemic:Active metabolites: 13-cis acitretin and etretinate.
-Excretion:Systemic:Fecal: 16 to 53%; Renal: 34 to 54%
-Elimination Half Life:ystemic: Acitretin: 49 h (range 33 to 96 h); 13-cis acitretin 63 hours (range 28 to 157 h); Etretinate: 120 d (range up to 168 d)
禁忌症
-Chronically abnormal lipid elevations.
-Concomitant use with methotrexate,tetracyclines.
-Hypersensitivity to acitretin, its excipients, or other retinoids.
-Pregnancy at initiation, during treatment, and for at least 3 years after treatment discontinuation; women of childbearing potential must use 2 forms of contraception, except the minipill; pregnancy tests required prior to, during, and for at least 3 years after treatment discontinuation.
Severe hepatic or renal impairment.
懷孕分類
X
哺乳分類
Infant risk cannot be ruled out.(Micromedex)
Acitretin is excreted in breast milk. Due to the potential for serious adverse reactions in the breastfeeding infant, the manufacturer does not recommend acitretin prior to or during breastfeeding(Uptodate).
副作用
Common
-Dermatologic: Alopecia (50% to 75%), Cheilitis (greater than 75%), Disorder of nail (25% to 50%), Dry skin (25% to 50%), Peeling of skin (50% to 75%), Pruritus (25% to 50%).
-Endocrine metabolic: Hypertriglyceridemia, Lipids abnormal.
-Gastrointestinal: Xerostomia (10% to 25%).
-Musculoskeletal: Arthralgia (10% to 25%).
-Neurologic: Hyperesthesia (10% to 25%), Paresthesia (10% to 25%).
-Ophthalmic: Dry eye syndrome (23%), Xerophthalmia (10% to 25%).
-Respiratory: Epistaxis (10% to 25%), Nasal mucosa dry, Rhinitis (25% to 50%).
Serious
-Cardiovascular: Myocardial infarction.
-Hepatic: Hepatotoxicity, Increased liver aminotransferase level.
-Neurologic: Pseudotumor cerebri.
-Otic: Ototoxicity - deafness (less than 1%).
-Psychiatric: Depression (1% to 10%).
-Other: Capillary leak syndrome.
劑量和給藥方法
General Dosage Information:
Prescribe and dispense only a 1-month supply at a time.
Disorder of skin, Nonpsoriatic:
30 mg orally once daily for 8 weeks (off-label dosage).
Lichen planus:
30 mg/day orally for up to 16 weeks (off-label dosage).
Psoriasis (Severe):
Initial, 25 to 50 mg ORALLY once daily with main meal; maintenance, 25 to 50 mg ORALLY once daily based on response; decrease concomitant phototherapy dose per patient response.
Skin cancer; Prophylaxis - Transplant of kidney, High-risk recipients:
30 mg ORALLY daily was used in a clinical trial
小兒調整劑量
The safety and efficacy of acitretin have not been established in pediatric patient
腎功能調整劑量
There are no dosage adjustments provided in manufacturer's labeling; use is contraindicated in patients with severely impaired renal function.
(Hemodialysis: Not removed by hemodialysis.)
肝功能調整劑量
There are no dosage adjustments provided in manufacturer’s labeling; use is contraindicated in patients with severely impaired liver function.