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

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

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Acitretin
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Chlormadinone
The therapeutic efficacy of Chlormadinone can be decreased when used in combination with Acitretin.
Clomocycline
The risk or severity of pseudotumor cerebri and elevated intracranial pressure can be increased when Acitretin is combined with Clomocycline.
Cyproterone acetate
The therapeutic efficacy of Cyproterone acetate can be decreased when used in combination with Acitretin.
Demeclocycline
The risk or severity of pseudotumor cerebri and elevated intracranial pressure can be increased when Acitretin is combined with Demeclocycline.
Demegestone
The therapeutic efficacy of Demegestone can be decreased when used in combination with Acitretin.
Desogestrel
The therapeutic efficacy of Desogestrel can be decreased when used in combination with Acitretin.
Dienogest
The therapeutic efficacy of Dienogest can be decreased when used in combination with Acitretin.
Diethylstilbestrol
The therapeutic efficacy of Diethylstilbestrol can be decreased when used in combination with Acitretin.
Doxycycline
The risk or severity of pseudotumor cerebri and elevated intracranial pressure can be increased when Acitretin is combined with Doxycycline.
Drospirenone
The therapeutic efficacy of Drospirenone can be decreased when used in combination with Acitretin.
Eravacycline
The risk or severity of pseudotumor cerebri and elevated intracranial pressure can be increased when Acitretin is combined with Eravacycline.
Estradiol
The therapeutic efficacy of Estradiol can be decreased when used in combination with Acitretin.
Estradiol cypionate
The therapeutic efficacy of Estradiol cypionate can be decreased when used in combination with Acitretin.
Estradiol valerate
The therapeutic efficacy of Estradiol valerate can be decreased when used in combination with Acitretin.
Ethanol
Ethanol may increase the teratogenic activities of Acitretin.
Ethinylestradiol
The therapeutic efficacy of Ethinylestradiol can be decreased when used in combination with Acitretin.
Ethynodiol diacetate
The therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Acitretin.
Gestodene
The therapeutic efficacy of Gestodene can be decreased when used in combination with Acitretin.
Gestrinone
The therapeutic efficacy of Gestrinone can be decreased when used in combination with Acitretin.
Hydroxyprogesterone caproate
The therapeutic efficacy of Hydroxyprogesterone caproate can be decreased when used in combination with Acitretin.