Acitretin

Class and Category

Pharmacologic class: Second-generation retinoid

Therapeutic class: Antipsoriatic

Indications and Dosages

👉 To treat severe psoriasis

CAPSULES

Adults. 25 to 50 mg once daily with the main meal.

Mechanism of Action

Binds to several retinoid receptors to regulate gene transcription. Exactly how the action of this second-generation retinoid allows normal growth and development of skin is unknown.

Contraindications

Alcohol consumption; blood donation; breastfeeding; chronic hyperlipidemia; concurrent use of etretinate, methotrexate, or tetracycline; hypersensitivity to acitretin, other retinoids, or their components; pregnancy; severe hepatic or renal impairment

Interactions

DRUGS

Methotrexate: Increased risk of hepatitis oral contraceptives containing only progestin: Possibly decreased effectiveness of oral contraceptive

Phenytoin: Possibly decreased protein binding of phenytoin

Sulfonylureas: Possibly increased risk of hypoglycemia

Tetracyclines: Possibly increased intracranial pressure

Vitamin A and other oral retinoids: Increased risk of hypervitaminosis A

ACTIVITIES

Alcohol use: Increased risk of adverse reactions and acitretin toxicity

Adverse Reactions

CNS: Aggression, CVA, depression, fatigue, headache, hyperesthesia, hypotonia, insomnia, intracranial hypertension, paresthesia, peripheral neuropathy, rigors, somnolence, suicidal ideation, thirst

CV: Chest pain, decreased high-density lipoproteins, edema, elevated cholesterol or triglyceride levels, MI, thromboembolism

EENT: Abnormal or blurred vision, blepharitis, conjunctivitis, corneal epithelial abnormality, decreased night vision, deafness, dry eyes or mouth, earache, epistaxis, eye pain, gingival bleeding, gingivitis, increased saliva, photophobia, sinusitis, stomatitis, taste perversion, tinnitus, ulcerative stomatitis

ENDO: Hot flashes, hyperglycemia

GI: Anorexia, abdominal pain, diarrhea, elevated liver enzymes, hepatitis, hepatotoxicity, nausea, pancreatitis

GU: Vulvovaginitis

HEME: Capillary leak syndrome, hemorrhage, increased bleeding time

MS: Arthralgia, arthrosis, back pain, hyperostosis, myalgia, myopathy

SKIN: Abnormal skin or hair texture, alopecia, bullous eruption, cold or clammy skin, dermatitis, diaphoresis, dry or peeling skin, erythematous rash, exfoliative dermatitis, erythroderma, flushing, fragility or thinning of skin, loss of eyelashes or eyebrows, photosensitivity, pruritus, purpura, pyogenic granuloma, rash, scaling, seborrhea, skin fissure or ulceration

Other: Hypervitaminosis A, increased appetite

Childbearing Considerations

PREGNANCY

• Drug causes fetal harm, especially severe fetal malformations.
• Drug is contraindicated in pregnant women and women of childbearing age who are not using reliable contraception.
• Patient of child bearing age must meet all of the following conditions before drug can be prescribed:

1. 2 negative urine or serum pregnancy tests with a sensitivity of at least 25 mIU/ml; first test done before initial prescription of drug and second test done during the first 5 days of the menstrual cycle immediately preceding the 7 days before drug therapy actually begins.
2. A negative pregnancy test before prescription is refilled monthly.
3. Patient agrees to have a pregnancy test done every 3 months for at least 3 years after drug is discontinued.
4. Patient has selected and is committed to using 2 effective forms of contraception simultaneously, for at least 1 month prior to drug therapy beginning, throughout drug therapy, and for at least 3 years after drug is discontinued.
5. Patient agrees to use at least 1 contraceptive of a primary form, unless absolute abstinence is the chosen method, patient has undergone a hysterectomy, or is clearly postmenopausal.
6. Patient makes a commitment to undergo counseling about contraception and behaviors associated with an increased risk of pregnancy on a monthly basis and every 3 months for at least 3 years following drug being discontinued.

• Patient agrees to participate in the “Do Your P.A.R.T.” (Pregnancy Prevention Actively required During and After Treatment) program.
• Patient understands drug may interfere with the contraceptive effect of microdosed progestin preparations and knows that the microdosed “minipill” is not recommended for use with the drug.
• Patient expresses an understanding that it is not known if there is an interaction between the drug and combined oral contraceptives.
• Patient agrees not to use St. John’s Wort during drug therapy and for at least 3 years following the discontinuation of the drug because pregnancies have occurred in users of combined hormonal contraceptives and St. John’s Wort.
• Patient agrees not to donate blood during and for at least 3 years following the completion of drug therapy because women of childbearing potential must not receive blood from patients being treated with drug.

LACTATION

• Drug may be present in breast milk.
• A decision should be made to discontinue breastfeeding or the drug to avoid potential serious adverse reactions in the breastfed infant.

REPRODUCTION

• Pregnancy must be avoided.
• Advise patient to use reliable contraception for at least one month before, during drug therapy, and for at least 3 years following drug discontinuation as outlined above.

Nursing Considerations

WARNING Don’t give acitretin to a pregnant woman, a woman contemplating pregnancy, or a woman who may not use reliable contraception during drug therapy and for at least 3 years afterward because acitretin causes major fetal abnormalities.

• Make sure patient has had 2 negative urine or serum pregnancy tests with a sensitivity of at least 25 mIU/ml before receiving acitretin. First test should be obtained when decision is made to use acitretin and second test during first 5 days of the menstrual period just before acitretin therapy starts. For patients with amenorrhea, second test should be done at least 11 days after the last act of unprotected sexual intercourse (which means without using two effective forms of contraception simultaneously).
• Check to make sure female patient of childbearing age has signed the patient agreement and informed consent form before starting acitretin therapy.
• Obtain a lipid profile, as ordered, before acitretin therapy starts and every 1 to 2 weeks for up to 8 weeks or until lipid effects are known. In high-risk patients, such as those with diabetes, obesity, or a history of alcohol abuse and those taking acitretin long-term, check lipid profile periodically throughout therapy.
• Monitor liver enzymes, as ordered. If hepatotoxicity is suspected, expect to stop drug and investigate cause.
• Monitor patient closely for capillary leak syndrome demonstrated by localized or generalized edema, weight gain, fever, hypotension, and myalgias. If present, notify prescriber and expect to obtain laboratory studies for evidence of neutrophilia, hypoalbuminemia, and an elevated hematocrit. If confirmed, discontinue acitretin therapy, as ordered.
• Prepare patient for periodic bone radiography if she takes acitretin long term or she develops a skeletal disorder because ossification abnormalities can occur, especially of the vertebral column, knees, and ankles.
• Monitor patient’s eyes for abnormalities throughout therapy. Expect patient to stop drug and have an ophthalmologic examination if eye abnormalities occur.
• Monitor patient for evidence of increased intracranial pressure, such as papilledema, headache, nausea, vomiting, and visual disturbances. If papilledema occurs, stop drug therapy immediately and obtain a neurologic evaluation, as ordered. Patient should never receive a tetracycline while taking acitretin because combined use can increase intracranial pressure.

• Assess patient for suicidal ideation because depression and other psychiatric symptoms, including thoughts of self-harm, may occur with acitretin use. Expect drug to be discontinued if psychiatric symptoms develop.
• Be aware that significantly lower doses of phototherapy are needed during acitretin therapy because drug increases the risk of erythema. If patient develops serious skin reactions, notify prescriber and expect acitretin therapy to be discontinued.

PATIENT TEACHING

WARNING: Warn women of childbearing age that acitretin causes major fetal abnormalities.

• Inform woman of childbearing age that she must have a pregnancy test before acitretin therapy starts, every month during acitretin therapy, and every 3 months for 3 years after therapy stops.
• Emphasize to woman of childbearing age that she must use two effective forms of contraception simultaneously unless she has chosen absolute abstinence or has had a hysterectomy. This must begin at least 1 month before acitretin therapy starts and continue throughout therapy and for at least 3 years after therapy ends.
• Caution women taking oral contraceptives that some prescribed and OTC drugs, including herbal supplements such as St. John’s wort, may interfere with oral contraceptives. Urge her to tell prescriber about all drugs she takes.
• Alert female patient of childbearing age that any method of birth control can fail, including tubal ligation, and that microdose progestin “minipill” preparations are not recommended to be taken with acitretin. Tell her to seek immediate medical care on how to obtain emergency contraception if sexual intercourse occurs without using 2 effective forms of contraception simultaneously.
• Caution patient not to consume alcohol or products that contain alcohol during acitretin therapy and for 2 months after therapy ends.
• Inform patient that regular blood tests will be needed to monitor liver function. Tell him to notify prescriber if any of the following develops: nausea and vomiting, loss of appetite, dark urine, or whites of eyes or skin turns yellow.
• Warn patient, male or female of any age, not to donate blood during acitretin therapy and for at least 3 years after it ends.
• Review acitretin medication guide with patient, and answer the patient’s questions.
• Inform patient that psoriasis may worsen during initial treatment and that full effects of drug may not be seen for up to 3 months.
• Caution patient to avoid hazardous activities until drug’s CNS and ophthalmic effects are known.
• Inform the patient that tolerance to contact lenses may decrease during acitretin therapy and for a period of time after treatment ends.
• Advise the patient not to take more than the minimum recommended daily allowance of vitamin A during acitretin therapy because of the risk of vitamin A toxicity.
• Caution patient not to use sun lamps and to avoid excessive exposure to sunlight because the effects of UV light are enhanced by retinoids such as acitretin.
• Tell patient to notify prescriber of any new skin changes that become serious or prolonged, as acitretin therapy may need to be discontinued, if present.