Acitretin

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 19.01.2021

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Definition
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Derivative of vitamin A acid, see also retinoids.

Pharmacodynamics (Effect)
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Inhibition of the hyperproliferation of keratinocytes in the psoriatic epidermis. Anti-keratinizing. The exact mechanism of action has not yet been elucidated. After uptake into the target cell, acitretin activates all 3 subtypes of the nuclear vitamin A acid receptors (RAR alpha, beta, gamma). Acitretin possibly reduces the enzymatic conversion of retinol into vitamin A acid by inhibiting interferon gamma. The reduction of the cellular vitamin A acid level leads to an inhibition of cellular proliferation. In addition, synthetic retinoids inhibit ribonuclease P (RNase P) to varying degrees depending on the dose.

Limited indication
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Sicca Syndrome.

Notice! Control of values: transaminases, alkaline phospatase, gamma-GT, creatinine, triglycerides, cholesterol, glucose. In patients with a history of abnormal kidney, liver or lipid metabolism: urea, uric acid, urine status, bilirubin, lipid electrophoresis (every 4 weeks).

Pregnancy/nursing period
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Contraindicated.

Dosage and method of use
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The effective dose is above 10 mg/day. The optimum effective dose is about 50 mg/day depending on body weight.
  • Adults initially 3 Kps./day neotigasone 10, over 2-4 Wo., then depending on the effect increase to a maximum 3 Kps./day neotigasone 25. maintenance dose usually 30 mg/day for another 6-8 Wo.
  • Children: Very strict indication, careful benefit-risk assessment. Initial 0.5 mg/kg bw/day. Maintenance dose 0.1 mg/kg bw/day, in no case > 0.2 mg/kg bw/day or > 35 mg/day.
Effect onset after 4-6 weeks at the earliest. Duration until complete healing 2-3 months. Therapy failure is to be expected in about 20% of treated cases.

Notice! Pregnancy must be ruled out before therapy begins. During therapy and up to 2 years after discontinuation of the preparation, effective contraception must be used, although the effect of oral contraceptives may be impaired. Low-dose progesterone preparations (so-called minipills) should not be used for contraception as the contraceptive effect of these preparations can be reduced by interaction with acitretin. Regular monitoring of the skeleton during long-term therapy. In children, carefully monitor growth (bone development)!

Undesirable effects
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  • Skin and mucous membranes: Depending on the dose: dry, possibly inflamed lips, dry nose, dry eyes, especially when wearing contact lenses, xerosis cutis, classic retinoid dermatitis, granulation tissue in the nail wall, hyperhidrosis.
  • Systemic: Substance is teratogenic: No prescription in women of childbearing potential; if there are no treatment options prescription only with simultaneous administration of anticontraceptives up to 2 years after taking the last tablet. Reversible increase in transaminases, possibly hepatotoxic (< 1%), centrilobular toxic liver necrosis, hyperostoses, osteoporosis, bone pain, calcification of muscles and ligaments, increase in triglycerides and cholesterol levels (in 20% of cases), increase in VLDL and decrease in HDL.

Notice! Special caution should be taken in patients with a history of hepatitis, diabetes mellitus, hyperlipidemia, pancreatitis and known retinal diseases! In rare cases a capillary leak syndrome has been reported.

Interactions
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  • Alcohol: Possible conversion of Acitretin to Etretinate.
  • Colestyramine: Simultaneous administration should be avoided as the absorption of etretinate is reduced. Acitretin should be given 1 hour before and > 4 hours after colestyramine intake. Effect on glucose tolerance readjustment of diabetes.
  • Tetracyclines: danger of intracranial hypertension.
  • Methotrexate: Possible additive hepatotoxic effect.
  • Isotretinoin and vitamin A: cumulative vitamin A toxicity!

Contraindication
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Because of teratogenicity contraindicated in pregnancy, lactation and in all women of childbearing potential! Liver dysfunction, lipometabolic disorders, diabetes mellitus, combination with tetracyclines or methotrexate, renal insufficiency, hypersensitivity to acitretin.

Preparations
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Neotigason, acicutane

Literature
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  1. Estival JL et al (2004) Capillary leak syndrome induced by Acitretin. Br J Dermatol 150: 150-52
  2. Kuenzli S, Saurat JH (2001) Retinoids for the treatment of psoriasis: outlook for the future. Curr Opin Investig Drugs 2: 625-630
  3. Farewell M et al (2003) Acitretin suppression of squamous cell carcinoma: Case report and literature review. J Dermatolog Treat 14 Suppl2: 3-6
  4. Papadimou E et al (2003) Retinoids inhibit human epidermal keratinocyte RNase P activity. Biol Chem 384: 457-462
  5. Rim JH et al (2003) The efficacy of calcipotriol + acitretin combination therapy for psoriasis: comparison with acitretin monotherapy. Am J Clin Dermatol 4: 507-510
  6. Spuls Pet al. (2003) Retrospective analysis of the treatment of psoriasis of the palms and soles. J Dermatolog Treat 14(Suppl2): 21-25
  7. Tsambaos D et al (2003) Peripheral sensory neuropathy associated with short-term oral acitretin therapy. Skin Pharmacol Appl Skin Physiol 16: 46-49
  8. Vos LE et al (2007) Acitretin induces capillary leak syndrome in a patient with pustular psoriasis. J Am Acad Dermatol 56: 339-342
  9. Zouboulis CC et al (2001) Retinoids--which dermatological indications will benefit in the near future? Skin Pharmacol Appl Skin Physiol 14: 303-315

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Last updated on: 19.01.2021