Description

Simple

A medication used to treat patients who have severe psoriasis.

Clinical

An oral retinoid used in the treatment of severe psoriasis.

Overview

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.

Pharmacology

Indication

For the treatment of severe psoriasis in adults.

Pharmacodynamic

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... Read more

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.

Protein binding

Over 99.9% bound to plasma proteins, primarily albumin.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

49 hours (range 33 to 96 hours)

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%).

Toxicity

Oral, rat: LD50 = >4000 mg/kg. Symptoms of overdose include headache and vertigo.

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Increased triglycerides US
  • Kind: experimental
    • Percent: 50-75%
  • Clinical Trial
    Cheilitis US
  • Kind: experimental
    • Percent: >75%
  • Clinical Trial
    Alopecia US
  • Kind: experimental
    • Percent: 50-75%
  • Clinical Trial
    Skin peeling US
  • Kind: experimental
    • Percent: 50-75%
  • Clinical Trial
    WBCs in urine US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased CPK US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased fasting blood sugar US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Decreased HDL cholesterol US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased SGPT US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased LDH US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased SGOT US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased cholesterol US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased reticulocytes US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Dry Skin US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Nail disorder US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Pruritis US
  • Kind: experimental
    • Percent: 25-50%
  • Clinical Trial
    Increased haptoglobin US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Decreased WBC US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Decreased hemoglobin US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Decreased hematocrit US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Decreased magnesium US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased magnesium US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased sodium US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased potassium US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased phosphorus US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Acetonuria US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Hematuria US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    RBCs in urine US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Decreased high occult blood US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased uric acid US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased direct bilirubin US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased GGTP US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Decreased fasting blood sugar US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased neutrophils US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased WBC US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased alkaline phosphatase US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Skin atrophy US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Paronychia US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Sticky skin US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Rigors US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Xerophthalmia US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Epistaxis US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Spinal hyperostosis US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Erythematous rash US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Hyperesthesia US
  • Kind: experimental
    • Percent: 10-25%
  • Clinical Trial
    Increased basophils US
  • Kind: experimental
    • Percent: 1-10%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Regions: US
    • With Drugs Coadmin:
        • Name: Methotrexate
        • Drugbank Id: DB00563
    • Route:
      • Oral
    • Regions: US
    • With Categories Coadmin:
        • Name: Tetracyclines
        • Drugbank Id: DBCAT002418
        • Mesh Id: D013754

    Food Interactions

    Avoid alcohol. Women of childbearing age should avoid ingesting any alcohol during treatment and two months after discontinuation of acitretin. Alcohol intake increases the duration of risk for birth defects to beyond three years post acitretin discontinuation.

    Take with food. Taking acitretin with the main meal of the day improves oral absorption.