acitretin


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acitretin

 [as″e-tret´in]
a second generation retinoid used in treatment of severe psoriasis; administered orally.

acitretin

Neotigason (UK), Soriatane

Pharmacologic class: Second-generation retinoid

Therapeutic class: Antipsoriatic

Pregnancy risk category X

FDA Box Warning

• Drug may harm fetus and must not be used by pregnant patients, those who intend to become pregnant, or those who may not use reliable contraception during therapy and for at least 3 years afterward.

• Patient must commit to using two effective contraceptive forms simultaneously. At least one form must be primary, unless patient chooses absolute abstinence, has had a hysterectomy, or is postmenopausal.

• Drug should be prescribed only by clinicians with special competence in diagnosing and treating severe psoriasis, experience using systemic retinoids, and understanding of teratogenicity risk.

• Consider drug only for women with severe psoriasis unresponsive to other therapies or whose clinical condition contraindicates other therapies.

• Instruct patient not to donate blood during therapy and for at least 3 years afterward.

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.

acitretin

/ac·i·tret·in/ (as″e-tret´in) a second generation retinoid used in treatment of severe psoriasis.

acitretin

[as′e-tret′in]
a second-generation retinoid used in the treatment of severe psoriasis. It is administered orally.

Acitretin

A second-generation oral retinoid indicated for psoriasis which is an etretinate metabolite. While acitretin is regarded as the oral anti-psoriatic agent of choice, it is contraindicated for women of childbearing age, as it is reverse metabolised into etretinate, which has a long elimination half-life.

acitretin

Therapeutics A retinoid used for CA prevention and psoriasis. See Retinoids.

acitretin

vitamin A derivative used in the treatment of severe, resistant psoriasis, Darier's disease (keratosis follicularis) and ichthyosis

acitretin

an active metabolite of etretinate, with similar actions and also used in dermatology.
References in periodicals archive ?
Reliability of the system was checked by using acitretin as a control substance capable of penetrating the BBB (Holthoewer et al.
Acitretin is under study by the Take Action to Prevent Pregnancy (T.
In the case of severe patients, non-steroidal drugs such as methotrexate, cyclosporine, and acitretin are practiced as first-line treatment; however, they come with toxicity concerns and so cannot be prescribed for long durations.
Peripheral sensory neuropathy associated with short-term oral acitretin therapy.
Tsambaos D, Sakkis T, Chroni E, et al: Peripheral sensory neuropathy associated with short-term oral acitretin therapy.
Others include minocycline, an antibiotic for acne, and acitretin, which treats the skin condition psoriasis.
Hsu acknowledged that the guidelines are a bit bold because they directly state, for example, that acitretin doesn't work well for plaque psoriasis, and that evidence is scant to support the use of alefacept to achieve full clearance.
Vitamin A-derived drugs, such as acitretin and isotretinoin, may help too but have important side effects and are available only from dermatology departments.
Synthetic retinoids, etretinate (Tigason[R]) and acitretin (Neotigason[R]) were developed to overcome this side-effect.
This is a rare feature of isotretinoin treatment (Figure 7) and is more often observed with acitretin or etretinate.
acitretin in the treatment of ichthyosis: a phase II/III multicentre, double-blind, randomized, active-controlled study.
Additionally, acitretin and phototherapy have been shown to reduce associated symptoms.