SORIATANE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SORIATANE (SORIATANE).
Retinoid that binds to nuclear retinoic acid receptors (RARs), modulating gene expression involved in cell proliferation, differentiation, and apoptosis.
| Metabolism | Primarily metabolized via CYP450 isoenzymes, including CYP3A4, 2C8, and 2C9, to active metabolites acitretin and cis-acitretin. Undergoes hepatic glucuronidation and excretion. |
| Excretion | Primarily hepatic metabolism; eliminated via feces (≈60%) and urine (≈15%) as metabolites; parent drug not excreted unchanged. |
| Half-life | Terminal elimination half-life of etretinate (active form) is ≈100–125 days due to storage in adipose tissue; clinically relevant for prolonged teratogenicity. |
| Protein binding | >99% bound to plasma proteins, primarily albumin and lipoproteins (etretinate). |
| Volume of Distribution | Very large Vd (≈2–10 L/kg) due to extensive distribution and accumulation in adipose tissue. |
| Bioavailability | Oral: Absolute bioavailability is variable, estimated ≈40–60% (increased with food); avoid administration with alcohol. |
| Onset of Action | Oral: Clinical improvement in psoriasis usually observed within 2–4 weeks; maximal effect after 2–3 months. |
| Duration of Action | Therapeutic effects persist for weeks to months after cessation due to long half-life; adverse effects (e.g., mucocutaneous) may resolve over similar timeframe. |
Initial: 25-50 mg orally once daily; maintenance: 25-50 mg orally once daily; not to exceed 75 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | No specific dose adjustment provided for renal impairment; use caution in severe impairment. |
| Liver impairment | Contraindicated in significant hepatic impairment; Child-Pugh class C: contraindicated; class A or B: avoid or use with extreme caution, no specific dose adjustment established. |
| Pediatric use | Not recommended for use in children due to risk of long-term skeletal toxicity. |
| Geriatric use | No specific dose adjustment, but consider increased risk of adverse effects; use lowest effective dose. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SORIATANE (SORIATANE).
| Breastfeeding | Contraindicated. Acitretin is excreted into human milk. The milk-to-plasma ratio is approximately 0.4. Due to potential for severe adverse effects in the nursing infant, breastfeeding is contraindicated during therapy and for at least 3 years after last dose. |
| Teratogenic Risk | Pregnancy Category X. Acitretin is a retinoic acid derivative and a potent teratogen. First trimester exposure causes major congenital malformations including CNS, cardiovascular, and facial defects (e.g., microcephaly, hydrocephalus, cardiovascular anomalies, microphthalmia). Second and third trimester exposure may lead to persistent teratogenic effects. Contraindicated in pregnancy and for 3 years post-discontinuation (acitretin is stored in adipose tissue and undergoes slow elimination). |
■ FDA Black Box Warning
SORIATANE must not be used by females who are pregnant or who may become pregnant during therapy or at any time for at least 3 years after discontinuation. There is an extremely high risk of severe birth defects.
| Serious Effects |
["Pregnancy (females of childbearing potential must avoid pregnancy during and for 3 years after therapy).","Nursing mothers (potential for serious adverse reactions in infants).","Severe hepatic impairment or active hepatitis.","History of pancreatitis (unless clearly unrelated to prior retinoid therapy).","Concomitant use of methotrexate (increases risk of hepatotoxicity).","Known hypersensitivity to acitretin or any component of the formulation."]
| Precautions | ["Hepatotoxicity: Monitor hepatic function before and during therapy. Avoid in patients with pre-existing liver disease.","Lipid abnormalities: Elevations in triglycerides and cholesterol; monitor lipid profiles.","Pseudotumor cerebri: Discontinue if signs of intracranial hypertension (headache, visual disturbances).","Pancreatitis: Discontinue if abdominal pain or elevated pancreatic enzymes.","Depression: Use caution in patients with history of depression; monitor mood changes.","Photosensitivity: Use sun protection; avoid UV light.","Ophthalmic effects: Risk of dry eyes, corneal opacities, and decreased night vision.","Hyperostosis: Long-term use may cause skeletal abnormalities (DISH)."] |
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| Fetal Monitoring | Maternal monitoring: Baseline and periodic liver function tests, serum lipids (fasting), renal function, and CBC. Pregnancy testing: Two negative pregnancy tests (with sensitivity of at least 25 mIU/mL) before initiation, monthly during therapy, and 3 years after discontinuation. Fetal monitoring: Ultrasound for detection of teratogenic effects if inadvertent exposure occurs. |
| Fertility Effects | Acitretin may impair fertility in females by disrupting menstrual cycles (e.g., anovulation) and in males by affecting spermatogenesis (reversible upon discontinuation). Patients should be counseled on contraception. |