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Acitretin


Pronunciation

 (a si TRE tin)


U.S. Brand Names

 Soriatane®


Generic Available

 No


Canadian Brand Names

 Soriatane®


Use

 Treatment of severe psoriasis


Pregnancy Risk Factor

 X


Pregnancy Implications

 Acitretin is teratogenic in humans. Severe birth defects have been reported when conception occurred during treatment or after therapy was complete. Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. In addition, because ethanol forms a teratogenic metabolite and would increase the duration of teratogenic potential, ethanol should not be consumed during treatment or for 2 months after discontinuation. Limited amounts of acitretin are found in seminal fluid; although it appears this poses little risk to a fetus, the actual risk of teratogenicity is not known. Any pregnancy which occurs during treatment, or within 3 years after treatment is discontinued, should be reported to the manufacturer at 1-888-500-3376 or to the FDA at 1-800-FDA-1088.


Lactation

 Enters breast milk/not recommended


Contraindications

 Hypersensitivity to acitretin, other retinoids, or any component of the formulation; patients who are pregnant or intend on becoming pregnant; ethanol ingestion; severe hepatic or renal dysfunction; chronically elevated blood lipid levels; concomitant use with methotrexate or tetracycline

Acitretin is contraindicated in females of childbearing potential unless all of the following conditions apply:

1) Patient has severe psoriasis unresponsive to other therapy or if clinical condition contraindicates other treatments.

2) Patient must have two negative urine or serum pregnancy tests prior to therapy.

3) Patient must commit to using two effective forms of birth control starting one month prior to acitretin treatment and for 3 years after discontinuation.

4) Patient is reliable in understanding and carrying out instructions.

5) Patient has received, and acknowledged understanding of a careful oral and printed explanation of the hazards of fetal exposure to acitretin and the risk of possible contraception failure; this explanation may include showing a line drawing to the patient of an infant with the characteristic external deformities resulting from retinoid exposure during pregnancy. Patient must sign an agreement/informed consent document stating that she understands these risks and that she should not consume ethanol during therapy or for 2 months after discontinuation.

6) All patients (male and female) should not donate blood during and for 3 years following treatment with acitretin.


Warnings/Precautions

 Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. All patients (male and female) should abstain from ethanol or ethanol-containing products during therapy and for 2 months after discontinuation. All patients should be advised not to donate blood during therapy or for 3 years following completion of therapy. Monitor for hepatotoxicity; discontinue if elevations of liver enzymes occur. Use with caution in patients at risk of hypertriglyceridemias. Rarely associated with pseudotumor cerebri. Discontinue if visual changes occur. May cause a decrease in night vision or decreased tolerance to contact lenses. All patients must be provided with a medication guide each time acitretin is dispensed. Female patients must also sign an informed consent prior to therapy. Safety and efficacy for pediatric patients have not been established; growth potential may be affected.


Adverse Reactions

>10%:

Central nervous system: Hyperesthesia (10% to 25%)

Dermatologic: Cheilitis (>75%), alopecia (50% to 75%), skin peeling (50% to 75%), dry skin (25% to 50%), nail disorder (25% to 50%), pruritus (25% to 50%), erythematous rash (10% to 25%), skin atrophy (10% to 25%), sticky skin (10% to 25%), paronychia (10% to 25%)

Endocrine & metabolic: Hypercholesterolemia (25% to 50%), hypertriglyceridemia (50% to 75%), HDL decreased (25% to 50%), phosphorus increased (10% to 25%), potassium increased (10% to 25%), sodium increased (10% to 25%), magnesium increased/decreased (10% to 25%), fasting blood sugar increased (25% to 50%), fasting blood sugar decreased (10% to 25%)

Gastrointestinal: Xerostomia (10% to 25%)

Hematologic: Reticulocytes increased (25% to 50%), hematocrit decreased (10% to 25%), hemoglobin decreased (10% to 25%), WBC increased/decreased (10% to 25%), haptoglobin increased (10% to 25%), neutrophils increased (10% to 25%)

Hepatic: Liver function tests increased (25% to 50%), alkaline phosphatase increased (10% to 25%), direct bilirubin increased (10% to 25%), GGTP increased (10% to 25%)

Neuromuscular & skeletal: Paresthesia (10% to 25%), arthralgia (10% to 25%), rigors (10% to 25%), CPK increased (25% to 50%), spinal hyperostosis progression (10% to 25%)

Ocular: Xerophthalmia (10% to 25%),

Renal: Uric acid increased (10% to 25%), acetonuria (10% to 25%), hematuria (10% to 25%), RBC in urine (10% to 25%)

Respiratory: Rhinitis (25% to 50%), epistaxis (10% to 25%)

1% to 10%:

Cardiovascular: Flushing, edema

Central nervous system: Headache, pain, depression, insomnia, somnolence, fatigue

Dermatologic: Skin odor, change in hair texture, bullous eruption, dermatitis, diaphoresis increased, psoriasiform rash, purpura, pyogenic granuloma, rash, seborrhea, ulcers, fissures, sunburn

Endocrine & metabolic: Hot flashes, potassium decreased, phosphorus decreased, sodium decreased, calcium increased or decreased, chloride increased or decreased

Gastrointestinal: Gingival bleeding, gingivitis, increased saliva, stomatitis, thirst, ulcerative stomatitis, abdominal pain, diarrhea, nausea, taste disturbance, anorexia, increased appetite, tongue disorder

Hepatic: Total bilirubin increased

Neuromuscular & skeletal: Arthritis, back pain, hypertonia, myalgia, osteodynia, peripheral joint hyperostosis, Bell's palsy

Ocular: Blurred vision, blepharitis, conjunctivitis, night blindness, photophobia, corneal epithelial abnormality, eye pain, eyebrow or eyelash loss, diplopia, cataract

Otic: Earache, tinnitus

Renal: BUN increased, creatinine increased, glycosuria, proteinuria

Respiratory: Sinusitis

<1%: Abnormal gait, acne, anal disorder, anxiety, bone disorder, bursitis, chalazion, chest pain, cirrhosis, conjunctival hemorrhage, constipation, corneal ulceration, cough, cyanosis, deafness, diplopia, dizziness, dyspepsia, dysphonia, dysuria, ectropion, eczema, esophagitis, ethanol intolerance, fever, flu-like syndrome, fungal infection, furunculosis, gastritis, gastroenteritis, glossitis, gum hyperplasia, hair discoloration, hemorrhage, hemorrhoids, hepatic dysfunction, hepatitis, hyperkeratosis, hypertrichosis, hypoesthesia, impaired healing, increased bleeding time, intermittent claudication, itchy eyes, jaundice, lacrimation abnormal, leukorrhea, libido decreased, malaise, melena, migraine, moniliasis, muscle weakness, nervousness, neuritis, olecranon bursitis, papilledema, peripheral ischemia, pharyngitis, photosensitivity, pseudotumor cerebri, recurrent sties, scleroderma, skin hypertrophy, spinal hyperostosis (new lesion), taste loss, tendonitis, tenesmus, tongue ulceration, urticaria, vaginitis, weight gain

Postmarketing and/or case reports: Aggression, MI, myopathy with peripheral neuropathy, nail fragility, pancreatitis, skin fragility or thinning, stroke, suicidal thoughts, thromboembolism, vulvovaginitis


Overdosage/Toxicology

 Symptoms of acute hypervitaminosis A would be expected (headache, vertigo); vomiting has also been reported. Pregnancy test for women of childbearing age; counseling regarding potential for birth defects and appropriate contraceptive use.


Drug Interactions

Ethanol: Etretinate (a retinoid with a much longer half-life) can be formed with concurrent use; contraindicated

Methotrexate: The concomitant administration of methotrexate and etretinate has been associated with hepatitis, a similar increased hepatitis risk may be expected with the combined use of acitretin and methotrexate; concomitant use is contraindicated

Progestins: Decreased contraceptive effect with concurrent use; use of "mini-pill" preparations are not recommended. Interactions with other progestational agents or hormonal contraceptives have not been established.

Sulfonylureas: Glucose-lowering effect may be potentiated. Effect seen with glibenclamide.

Tetracycline: Acitretin and tetracyclines may both cause increased intracranial pressure; concomitant use is contraindicated.

Vitamin A: Concomitant administration of vitamin A and other systemic retinoids must be avoided due to the risk of possible additive toxic effects


Ethanol/Nutrition/Herb Interactions

 Ethanol: Use leads to formation of etretinate, a teratogenic metabolite with a prolonged half-life; concomitant use of ethanol or ethanol-containing products is contraindicated.


Stability

 Store between 15°C to to 25°C (59°F to 77°F) and protect from light; avoid high temperatures and humidity


Pharmacodynamics/Kinetics

 Etretinate has been detected in serum for up to 3 years following therapy, possibly due to storage in adipose tissue.

Onset: May take 2-3 months for full effect; improvement may be seen within 8 weeks.

Absorption: Oral: ~72% absorbed when given with food

Protein binding: >99% bound, primarily to albumin

Metabolism: Metabolized to cis -acitretin; both compounds are further metabolized. Concomitant ethanol use leads to the formation of etretinate (active).

Half-life elimination: Acitretin: 49 hours (range: 33-96); cis -acitretin: 63 hours (range: 28-157); etretinate: 120 days (range: 84-168 days)

Excretion: Feces (34% to 54%); urine (16% to 53%)


Dosage

 Oral: Adults: Individualization of dosage is required to achieve maximum therapeutic response while minimizing side effects

Initial therapy: Therapy should be initiated at 25-50 mg/day, given as a single dose with the main meal

Maintenance doses of 25-50 mg/day may be given after initial response to treatment; the maintenance dose should be based on clinical efficacy and tolerability


Monitoring Parameters

 Lipid profile (baseline and at 1- to 2-week intervals for 4-8 weeks); liver function tests (baseline, and at 1- to 2-week intervals until stable, then as clinically indicated); blood glucose in patients with diabetes; bone abnormalities (with long-term use)


Dietary Considerations

 Administer with food. Avoid ingestion of additional sources of exogenous vitamin A (in excess of RDA); use of ethanol and ethanol-containing products is contraindicated.


Patient Education

 Take with food. Do not drink alcohol during therapy and for 2 months after discontinuation. Use contraception for 1 month before, during, and for 3 years after discontinuation. You may not be able to tolerate contact lenses during treatment. Do not donate blood during treatment and for 3 years after discontinuation. Avoid exposure to sunlight. Wear protective clothing and sunscreens. Avoid use of other vitamin A products. Pregnancy/breast-feeding precautions: Females: Use two effective forms of birth control. If you have had your tubes tied, then use an additional form of birth control. If you become pregnant, contact your prescriber immediately. Breast-feeding is not recommended.


Additional Information

 Female patients are required to use two forms of birth control, at least one of which is a primary form, unless they have undergone a hysterectomy or are postmenopausal. Both forms of birth control must be used simultaneously for at least 1 month prior to therapy and for at least 3 years after discontinuation. Primary forms of birth control include tubal ligation, partner's vasectomy, IUD, or hormonal birth control products. Microdosed progestin products, referred to as "mini-pills," have been shown to be less effective when used with acitretin, and are not recommended. Secondary forms of contraception include diaphragms, latex condoms and cervical caps, all if used with a spermicide.


Dental Health: Effects on Dental Treatment

 No significant effects or complications reported


Dental Health: Vasoconstrictor/Local Anesthetic Precautions

 No information available to require special precautions


Mental Health: Effects on Mental Status

 None reported


Mental Health: Effects on Psychiatric Treatment

 None reported


Dosage Forms

 Capsule: 10 mg, 25 mg


International Brand Names

 Neotigason® (AR, AT, AU, BE, CH, CL, CO, CZ, DE, DK, ES, FI, GB, HR, HU, IE, IL, IT, LU, NL, NO, NZ, PL, PT, RO, RU, SE, SG, SI); Neo-Tigason® (TH); Neotigason® (TR, YU, ZA); Soriatane® (CA, FR)


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