ACITRETIN

ACITRETIN (a-ci-tree'tin) Soriatane Classifications: antiacne; retinoid; Therapeutic: antiacne Prototype: Isotretinoin Pregnancy Category: X

Availability

10 mg, 25 mg capsules

Action

Acitretin binds to the retinoic acid receptors in the skin, thus modifying gene expression, epithelial cell growth, and cell differentiation.

Therapeutic Effect

Acitretin is a highly toxic metabolite of retinol (vitamin A).

Uses

Treatment of severe, recalcitrant psoriasis in adults.

Contraindications

Sensitivity to parabens, papilledema, severe renal impairment or renal failure, pregnancy (category X) for at least 3 y after use, lactation.

Cautious Use

Patients with impaired hepatic function, hepatitis, diabetes mellitus, obesity, alcoholism, history of pancreatitis, hypertriglyceridemia, hypercholesterolemia, coronary artery disease, retinal disease, degenerative joint disease.

Route & Dosage

Psoriasis Adult: PO 25–50 mg q.d. with main meal

Administration

Oral

• Administer as single dose with main meal because food enhances absorption.
• Store at 15°–25° C (59°–77° F) and protect from light. After opening, avoid exposure to high temperatures and humidity.

Adverse Effects (≥1%)

Body as a Whole: Hyperesthesia, paresthesias, arthralgia, progression of existing spinal hyperostosis, rigors, back pain, hypertonia, myalgia, fatigue, hot flashes, increased appetite. CNS: Headache, depression, aggressive feelings and thoughts of self-harm, insomnia, somnolence. CV: Flushing, edema. GI: Dry mouth, increased liver function tests, increased triglycerides and cholesterol, hepatitis, gingival bleeding, gingivitis, increased saliva, stomatitis, thirst, ulcerative stomatitis, abdominal pain, diarrhea, nausea, tongue disorder. Special Senses: Blurred vision, blepharitis, conjunctivitis, decreased night vision/night blindness, eye pain, photophobia; earache, tinnitus; taste perversion. Respiratory: Sinusitis. Skin: Alopecia, skin peeling, dry skin, nail disorders, pruritus, rash, cheilitis, skin atrophy, paronychia, abnormal skin odor and hair texture, cold/clammy skin, increased sweating, purpura, seborrhea, skin ulceration, sunburn. Other: Rhinitis, epistaxis, xerophthalmia.

Interactions

Drug: Combination with ethanol can create etretinate, which has a significantly longer half-life than acitretin; interferes with the contraceptive efficacy of progestin-only oral contraceptives. Use with methotrexate increases the risk of heptatitis. Food: Avoid excess vitamin A.

Pharmacokinetics

Absorption: Rapidly from GI tract, optimal absorption when taken with food. Peak: 2–5 h. Distribution: Crosses placenta, distributed into breast milk. Metabolism: Active metabolite, cis-acitretin. Elimination: In both urine and feces. Half-Life: 49 h acitretin, 63 h cis-acitretin.

Nursing Implications

Assessment & Drug Effects

• Monitor for S&S of pancreatitis or loss of glycemic control in diabetics. Report either condition immediately to physician.
• Lab tests: Before initiating therapy and at 1- to 2-wk intervals until response to drug is known, do lipid profile and liver function tests. Monitor blood glucose and HbA_1C periodically.

Patient & Family Education

• Note: Transient worsening of psoriasis may occur during early therapy.
• Review common adverse effects of drug; lag time of 2–3 mo may be necessary before drug effect is evident.
• Discontinue drug and report immediately to physician if visual problems develop.
• Note: Dry eyes with decreased tolerance for contact lenses may occur.
• Do not drink alcohol while taking this drug; it increases risk of hepatotoxicity and hypertriglyceridemia; females should avoid alcohol during and for 2 mo following therapy.
• Do not donate blood for 3 y following therapy.
• Avoid excessive exposure to sunlight or UV light.
• Use two forms of effective contraception for 1 mo before and at least 3 y following therapy because of the serious risk of fetal deformities that could result from exposure to this medication.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug