Class: Second generation retinoid
- Capsules 10 mg
- Capsules 25 mg
Absorption is linear and proportional with increasing doses; approximately 72% is absorbed following a 50 mg dose. C max (mean 416 ng/mL) is achieved in 2 to 5 h.
Plasma protein binding is 99.9%, primarily to albumin.
Undergoes extensive metabolism to cis-acitretin.
Excreted in the feces (34% to 54%) and urine (16% to 53%). Terminal t ½ of acitretin is 49 h; t ½ of cis-acitretin is 63 h.
Higher plasma concentrations are seen; however, no changes occur in the t ½ .Renal failure
Plasma concentrations are lower in end-stage renal failure. Acitretin is not removed by dialysis.
Indications and Usage
Treatment of severe psoriasis.
Pregnancy; severe liver or kidney function impairment; chronic abnormal elevation in blood lipid values; concurrent use of methotrexate or tetracyclines; hypersensitivity to other retinoids or any component of the product.
Dosage and AdministrationAdults
PO Start with 25 to 50 mg/day given as a single dose with the main meal. Maintenance doses of 25 to 50 mg/day may be given dependent upon the patient's response to initial treatment.Relapse
PO Relapses may be treated as outlined for initial treatment.Phototherapy
PO When used with phototherapy, the phototherapy dose should be decreased by the prescriber based upon the patient's individual response.
Store capsules at controlled room temperature (59° to 77°F). Protect from light. Avoid exposure to high temperatures and humidity after bottle is opened.
Concurrent use of alcohol and acitretin may lead to the formation of etretinate, which increases the duration of teratogenic potential in women.Glyburide
The glucose-lowering effect of glyburide may be potentiated.Methotrexate
Because the risk of hepatitis may be increased, concurrent use is contraindicated.Phenytoin
Protein binding of phenytoin may be reduced.Progestin “minipill”
Acitretin may interfere with the contraceptive effect.Tetracyclines
Because acitretin and tetracyclines can cause increased intracranial pressure, concurrent use is contraindicated.Vitamin A, oral retinoids
Because the risk of hypervitaminosis A is increased, concurrent use is contraindicated.
Laboratory Test Interactions
None well documented.
Acute MI, thromboembolism, stroke (postmarketing).
Rigors (10% to 25%); headache, pain, depression, insomnia, somnolence (1% to 10%); myopathy with peripheral neuropathy, aggressive feelings and/or suicidal thoughts (postmarketing).
Alopecia, skin peeling (60% to 75%); dry skin, nail disorder, pruritus (25% to 50%); erythematous rash, hyperesthesia, paresthesia, paronychia, skin atrophy, sticky skin (10% to 25%); abnormal skin odor, abnormal hair texture, bullous eruption, cold/clammy skin, dermatitis, increased sweating, psoriasiform rash, purpura, pyogenic granuloma, rash, seborrhea, skin fissures, skin ulceration, sunburn, infection (1% to 10%); skin thinning, skin fragility and scaling (postmarketing).
Rhinitis (25% to 50%); dry eyes (23%); xerophthalmia, epistaxis (10% to 25%); eye irritation (9%); brow and lash loss (5%); Bell palsy, blepharitis, crusting of eye lids, blurred vision, conjunctivitis, corneal epithelial abnormality, cortical cataract, decreased night vision/night blindness, diplopia, itchy eyes or eyelids, nuclear cataract, pannus, papilledema, photophobia, posterior subcapsular cataract, recurrent sties, subepithelial corneal lesions (less than 5%); eye pain, sinusitis, earache, taste perversion, tinnitus (1% to 10%).
Increased phosphorus, potassium, sodium, magnesium, decreased magnesium (10% to 25%); increased calcium, chloride, decreased calcium, chloride, phosphorus, potassium, sodium (1% to 10%).
Cheilitis (greater than 75%); dry mouth (10% to 25%); abdominal pain, diarrhea, nausea, tongue disorder, stomatitis, ulcerative stomatitis (1% to 10%).
White blood cells in urine (25% to 50%); acetonuria, hematuria, red blood cells in urine (10% to 25%); glycosuria, proteinuria (1% to 10%); vulvo-vaginitis from Candida albicans (postmarketing).
Increased reticulocytes (25% to 50%); decreased hematocrit, hemoglobin, WBC (10% to 25%); increased haptoglobin, neutrophils, WBC (10% to 25%); increased bands, basophils, eosinophils, hematocrit, hemoglobin, lymphocytes, monocytes, platelets, red blood cells, decreased haptoglobin, lymphocytes, neutrophils, reticulocytes, platelets, RBC (1% to 10%).
Increased cholesterol, LDH, AST, ALT, decreased HDL (25% to 50%); increased alkaline phosphatase, direct bilirubin, gamma-glutamyl transpeptidase (10% to 25%); increased globulin, total bilirubin, total protein, serum albumin, decreased serum albumin (1% to 10%).
Arthralgia, spinal hyperostosis (10% to 25%); arthritis, arthrosis, back pain, hypertonia, myalgia, osteodynia, peripheral joint hyperostosis (1% to 10%).
Increased uric acid (10% to 25%); increased BUN, creatinine (1% to 10%).
Increased triglycerides (50% to 75%); increased CPK, fasting blood glucose (25% to 50%); decreased fasting blood sugar, high occult blood (10% to 25%); anorexia, edema, fatigue, hot flashes, increased appetite, gingival bleeding, gingivitis, increased salivation, thirst, infection, decreased and increased iron, flushing (1% to 10%).
Acitretin must not be used by women who are pregnant or intend to become pregnant during therapy or at any time for at least 3 yr following discontinuation of therapy. Acitretin must not be used by women who may not use reliable contraception while undergoing treatment or for at least 3 yr following discontinuation of treatment. Women must sign a Patient Agreement/Information Consent Form that contains warnings about the risk of potential birth defects. An acitretin medication guide must be given to patients each time acitretin is dispensed, as required by law. If pregnancy occurs during therapy or at any time for at least 3 yr after stopping therapy, the prescriber and patient should discuss the possible effects on the pregnancy.Hepatotoxicity
Hepatotoxicity, hepatitis, and hepatitis related deaths may occur.
Category X .
Excreted in breast milk.
Safety and efficacy not established.
May occur; avoid excessive use of sunlamps, exposure to sunlight, and ultraviolet light.
Patients should not donate blood during and for at least 3 yr following completion of acitretin therapy.
Examine patient for possible ossification abnormalities.
Lipid effects and CV risk
Elevation in triglycerides and cholesterol may occur; decreased HDL may occur. CV risk status may be increased.
Pancreatitis (including fatal fulminant pancreatitis) with or without elevated triglyceride levels may occur.
Depression and other psychiatric symptoms such as aggressive feeling or thought of self-harm may occur.
Night vision and tolerance to contact lenses may be decreased.
Identical to acute hypervitaminosis A (headache, vertigo).
- Advise patient to review the Medication Guide before starting therapy and with each refill.
- Advise patient that dose may be adjusted based on tolerance and effectiveness.
- Instruct patient to take prescribed dose every day with main meal. Advise patient that food increases absorption and beneficial effects.
- Advise patient that if a dose is missed to skip the missed dose and resume the normal schedule. Caution patient not to double the dose to try to catch up.
- Advise patient that psoriasis may worsen during the initial treatment period but that gradual improvement should follow and max benefit may not be noted for 2 to 3 mo. Advise patient to notify health care provider if symptoms do not improve as expected or continue to worsen.
- Caution women of childbearing potential not to consume alcohol or products containing alcohol during and for 2 mo following cessation of therapy.
- Instruct sexually active women who are not clearly menopausal or have undergone a hysterectomy to use 2 reliable forms of contraception beginning 1 mo before starting therapy, during therapy, and for 3 yr following cessation of therapy. Caution patient that micro-dosed progestin “minipills” are not recommended during therapy with acitretin.
- Advise women of childbearing potential to notify health care provider immediately if pregnant, miss a period, or have sex without using 2 effective forms of birth control either while taking acitretin or for 3 yr following cessation of therapy.
- Caution both men and women not to donate blood during and for at least 3 yr following cessation of therapy because women of childbearing potential must not receive blood from patients being treated with acitretin.
- Advise patient, family, or caregiver to inform health care provider of the following: persistent severe headache; persistent nausea and/or vomiting; yellowing of the skin or eyes; dark urine; persistent appetite loss; frequent urination; great thirst or unexplained hunger; sudden vision changes; severe skin or mucus membrane dryness; depression or other mental symptoms; shortness of breath; dizziness; chest pain; sudden weakness; trouble speaking; swelling of a leg.
- Advise patient that medication can cause chapped lips, peeling of the fingertips, palms, and soles, itching or scaly skin, runny or dry nose, or nosebleeds and to inform health care provider if any of these occur and are bothersome. Advise patient that health care provider or pharmacist can recommend a lotion or cream to help treat drying or chapping.
- Advise patient that drug may cause decreased night vision and to avoid driving at night if any sudden vision problems occur.
- Advise diabetic patient to monitor blood sugars more frequently when medication is started or after a dose adjustment and to inform health care provider if significant changes in blood sugar are noted.
- Caution patient that medication can increase sensitivity to UV light and to avoid use of sun lamps and unnecessary exposure to sunlight while undergoing treatment.
- Advise patient wearing contact lenses that decreased tolerance to lenses may be experienced during treatment and after therapy has been stopped.
- Caution patient against taking vitamin A supplements in excess of recommended daily allowances.
Copyright © 2009 Wolters Kluwer Health.
More about acitretin
- Other brands: Soriatane