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PubChem
Name: Acitretin
PubChem Compound ID: 41317
Description: 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.
Molecular formula: C21H26O3
Molecular weight: 326.429 g/mol
DrugBank
Identification
Name: Acitretin
Name (isomeric): DB00459
Drug Type: small molecule
Description: 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.
Brand: Acetretin, Soriatane
Category: Keratolytic Agents
CAS number: 55079-83-9
Pharmacology
Indication: For the treatment of severe psoriasis in adults.
Pharmacology:
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 ...
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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.
Biotransformation: 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.
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)
Toxicity: Oral, rat: LD50 = >4000 mg/kg. Symptoms of overdose include headache and vertigo.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TetracyclineIncreased risk of intracranial hypertension
MethotrexateAcitretin/etretinate increases the effect and toxicity of methotrexate
MethacyclineIncreased risk of intracranial hypertension
RolitetracyclineIncreased risk of intracranial hypertension
NorethindroneAcitretine may cause a loss of contraceptive effect
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