acitretin

Action

Unclear. Promotes normal growth cycle of skin cells, possibly by targeting retinoid receptors in these cells and adjusting factors that affect epidermal proliferation and synthesis of RNA and DNA.

Availability

Capsules: 10 mg, 17.5 mg, 25 mg

Indications and dosages

➣ Severe psoriasis

Adults and elderly patients: Initially, 25 to 50 mg/day P.O. as a single dose with main meal. If initial response is satisfactory, give maintenance dosage of 25 to 50 mg/day P.O.

Off-label uses

• Darier's disease (keratosis follicularis)

• Lamellar ichthyosis (in children)

• Lichen planus

• Nonbullous and bullous ichthyosiform erythroderma

• Palmoplantar pustulosis

• Sjögren-Larsson syndrome

Contraindications

• Hypersensitivity to drug or paraben (used as preservative in gelatin capsule)

• Pregnancy or anticipated pregnancy within 3 years after drug discontinuation (drug has teratogenic and embryotoxic effects)

• Women of childbearing age who may not use reliable contraception during therapy and for at least 3 years after drug discontinuation

• Breastfeeding

Precautions

Use cautiously in:

• hepatic or renal impairment, diabetes mellitus, obesity

• elevated cholesterol or triglyceride levels

• elderly patients.

Administration

☞ Verify that patient isn't pregnant before giving drug.

• Give as a single dose with main meal.

Adverse reactions

CNS: headache, depression, insomnia, drowsiness, fatigue, migraine, rigors, abnormal gait, nerve inflammation, hyperesthesia, paresthesia, pseudotumor cerebri

EENT: abnormal or blurred vision, dry eyes, eye irritation, eyebrow and eyelash loss, eyelid inflammation, cataract, conjunctivitis, corneal epithelial abnormality, reduced night vision, photophobia, recurrent styes, earache, tinnitus, hearing loss, epistaxis, rhinitis, sinusitis, papilledema

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, gastritis, stomatitis, esophagitis, melena, painful straining at stool, pancreatitis, lip inflammation and cracking, dry mouth, anorexia

GU: abnormal urine, dysuria, atrophic vaginitis, leukorrhea

Hepatic: abnormal hepatic function, jaundice, hepatitis

Metabolic: poor blood glucose control

Musculoskeletal: joint, muscle, back, and bone pain; arthritis; bone disorders; spinal bone overgrowth; increased muscle tone or rigidity; tendinitis

Respiratory: coughing, increased sputum, laryngitis

Skin: dry skin, pruritus, skin atrophy, skin peeling, abnormal skin odor, sticky skin, seborrhea, dermatitis, diaphoresis, cold clammy skin, skin infection, rash, pyrogenic granuloma, skin ulcers, skin fissures, sunburn, flushing, purpura, nail disorder, inflammation of tissue surrounding nails, abnormal hair texture, alopecia

Other: abnormal taste, glossitis, tongue ulcers, gingival bleeding, gingivitis, edema, thirst, hot flashes

Interactions

Drug-drug. Glyburide: increased blood glucose clearance

Methotrexate: increased risk of hepatotoxicity

Oral contraceptives ("minipill"): decreased contraceptive efficacy

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, triglycerides: increased levels

Low-density lipoproteins: decreased level

Drug-behaviors. Alcohol use: interference with acitretin elimination, possible drug toxicity

Patient monitoring

• Monitor patient who has early signs or symptoms of pseudotumor cerebri, such as headache, nausea, vomiting, and visual disturbances. Discontinue drug immediately if papilledema occurs.

• Check blood lipid levels before therapy begins and every 1 to 2 weeks during therapy.

• Monitor blood glucose levels and kidney and liver function test results.

• If drug causes open skin lesions resulting from dermatitis or blisters, watch for signs and symptoms of infection.

• Assess for pain, stinging, and itching. Apply cool compresses as needed for relief.

☞ Be aware that women taking this drug must avoid alcohol-containing foods, beverages, medications, and over-the-counter products during therapy and for 2 months afterward.

Patient teaching

• Instruct patient to take drug with main meal to minimize GI upset.

• Tell patient to avoid driving and other hazardous activities until he knows how drug affects concentration, alertness, and vision.

• Caution patient not to drink alcohol during therapy.

☞ Advise females to use effective contraception for at least 1 month before starting drug, throughout entire course of therapy, and for 3 years after discontinuing drug.

• Explain that disease may seem to worsen at start of therapy.

• Tell contact lens wearers that lens intolerance may develop.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.