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. |
| Molecular Weight | 326.43 |
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 | Teratogenic; absolutely contraindicated due to high risk of major fetal malformations including CNS, cardiovascular, and facial abnormalities. |
| 2nd trimester | Contraindicated; continued risk of teratogenicity. |
| 3rd trimester | Contraindicated; risk persists throughout pregnancy. |
Clinical note
Comprehensive clinical and safety monograph for SORIATANE (SORIATANE).
| Placental transfer | Crosses the placenta readily; demonstrated in animal studies and human case reports. |
| Breastfeeding | Excreted in human milk; potential for serious adverse reactions in nursing infants. Breastfeeding is contraindicated during therapy and for at least 2 months after discontinuation. |
| Lactation Rating |
■ 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 |
PregnancyFemales of childbearing potential not using effective contraceptionHistory of pancreatitisHypertriglyceridemiaHepatic dysfunctionHypersensitivity to acitretin or retinoids
| 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). |
| Food/Dietary |
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| L5 |
| 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). |
| 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. |
| Take with food (especially fatty meal) to enhance absorption. Avoid alcohol entirely as it may cause formation of etretinate, prolonging teratogenic risk. No other significant food interactions. |
| Clinical Pearls | Soriatane (acitretin) is a systemic retinoid used for severe psoriasis. It is highly teratogenic with a long elimination half-life; women of childbearing potential must avoid pregnancy for at least 3 years after discontinuation. Avoid concurrent use with methotrexate due to increased hepatotoxicity risk. Monitor liver function tests and fasting lipids regularly. May cause pseudotumor cerebri, especially when combined with tetracyclines. |
| Patient Advice | Do not become pregnant while taking this medication or for at least 3 years after stopping; use two reliable forms of contraception. · Avoid alcohol consumption because it can convert acitretin to etretinate, which stays in the body much longer. · Report any severe headache, vision changes, or nausea/vomiting immediately (signs of pseudotumor cerebri). · Do not donate blood during therapy and for 3 years after stopping. · Expect dry lips, skin, and eyes; use moisturizers and lip balm regularly. · Avoid vitamin A supplements to prevent additive toxicity. · Take with food to improve absorption. |