Acitretin information from DrugsUpdate
P - Contraindicated in pregnancy
L - Contraindicated in lactation
FI - Lab *
LI - Food *
Acitretin (trade name Soriatane) is a second generation retinoid. It is taken orally, and is typically used for psoriasis.
It is a metabolite of etretinate, which was used prior to the introduction of acitretin. Etretinate was discontinued because it had a narrow therapeutic index as well as a long elimination half-life (t1/2=120 days), making dosing difficult. In contrast, acitretin's half-life is approximately 2 days.
Because acitretin can be reverse metabolised into etretinate which has a long half life, women must avoid becoming pregnant for at least 2 years after discontinuing acitretin. Therefore, etretinate is generally not recommended at for women of child bearing age with risk becoming pregnant.
Acitretin is the least toxic systemic treatment for psoriasis. It is an oral retinoid of choice used in the treatment of severe resistant psoriasis. It binds to nuclear receptors that regulate gene transcription. They induce keratinocyte differentiation and reduce epidermal hyperplasia. Acitretin is readily absorbed and widely distributed after oral administration. A therapeutic effect occurs after 2 to 4 weeks or longer.
If a patient has received the medication, he/she is advised against giving blood indefinitely due to the risk of birth defects.
Pharmacodynamics
Pharmacokinetics
Absorption
Absorption is linear and proportional with increasing doses; approximately 72% is absorbed following a 50 mg dose. C max (mean 416 ng/mL) is achieved in 2 to 5 h.
Distribution
Plasma protein binding is 99.9%, primarily to albumin.
Metabolism
Undergoes extensive metabolism to cis-acitretin.
Elimination
Excreted in the feces (34% to 54%) and urine (16% to 53%). Terminal t ? of acitretin is 49 h; t ? of cis-acitretin is 63 h.
Special Populations
Elderly
Higher plasma concentrations are seen; however, no changes occur in the t ? .
Renal Failure
Plasma concentrations are lower in end-stage renal failure. Acitretin is not removed by dialysis.
Acitretin Indications / Acitretin Uses
Information Not Available
Acitretin Adverse Reactions / Acitretin Side Effects
Dryness of mucous membranes and skin; conjunctivitis, dry sore mouth; ophth disturbances; raised lipid level, pancreatitis; sticky skin, dermatitis. Severe headache; GI disturbances; dermatologic reactions, oedema, paronychia, granulomatous lesions, bullous eruptions; reversible hair thinning and alopoecia; CNS disturbances; sweating; taste disturbance, gingivitis; benign intracranial hypertension; photosensitivity; skeletal hyperostosis; extraosseous calcification; premature epiphyseal closure in child.
Potentially Fatal: Phototoxicity, jaundice, hepatitis and hepatotoxity.
Precautions
Acitretin must not be used by women who are pregnant or intend to become pregnant during therapy or at any time for at least 3 yr following discontinuation of therapy. Acitretin must not be used by women who may not use reliable contraception while undergoing treatment or for at least 3 yr following discontinuation of treatment. Women must sign a Patient Agreement/Information Consent Form that contains warnings about the risk of potential birth defects. An acitretin medication guide must be given to patients each time acitretin is dispensed, as required by law. If pregnancy occurs during therapy or at any time for at least 3 yr after stopping therapy, the prescriber and patient should discuss the possible effects on the pregnancy.
Special Precautions
Female patients to avoid alcohol during and 2 months after treatment. Avoid blood donation during therapy or at least 1-3 years after stopping therapy. Children. Radiographic treatment for prolonged therapy. Therapy should not last >6 months. Monitor plasma lipid and glucose levels (especially diabetics) regularly. Monitor LFTs.
Other Drug Interactions
Concomitant use with keratolytics or high dose vitamin A. Reduces anticoagulant effect of coumarins e.g. warfarin. Concomitant use of microdised progestin oral contraceptives. Concomitant use of methotrexate can potentiate hepatotoxicty. Concomitant use with tetracycline.
Other Interactions
Co-administration with food may increase oral bioavailability.
Dosage
Oral
Darier's disease
Adult: Initially, 10 mg daily for 2-4 wk. Max: 50 mg/day.
Child: 500 mcg/kg/day. Max dose: 35 mg/day.
Oral
Congenital icthyosis
Adult: Initially, 25-30 mg daily for 2-4 wk before dose adjustments are done. Usual range: 25-50 mg daily for further 6-8 wk. Max: 75 mg daily for short periods.
Child: 500 mcg/kg/day. Max: 35 mg daily.
Oral
Severe psoriasis
Adult: Initially, 25-30 mg daily for 2-4 wk before dose adjustments are done. Usual range: 25-50 mg daily for further 6-8 wk. Max: 75 mg daily for short periods.
Child: 500 mcg/kg/day. Max: 35 mg daily.
Oral
Severe lichen planus
Adult: Initially, 25-30 mg daily for 2-4 wk before dose adjustments are done. Usual range: 25-50 mg daily for further 6-8 wk. Max: 75 mg daily for short periods.
Child: 500 mcg/kg/day. Max: 35 mg daily.
Food(before/after)
Should be taken with food. (Take w/ main meals or w/ a glass of milk.)
List of Contraindications
Acitretin and Pregnancy
Contraindicated in pregnancy
Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Acitretin and Lactation
Contraindicated in lactation
Acitretin and Children
Safety and efficacy not established
Acitretin and Geriatic
Information Not Available
Acitretin and Other Contraindications
Pregnancy (before the start, during and at least 2-3 years after cessation of therapy), lactation. Hepatic and renal impairment. Hyperlipidaemia.
Storage
Oral: Store below 25°C.
Lab interference
Oral: Store below 25°C.
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