Alitretinoin

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 04.05.2024

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Synonym(s)

9-cis-retinoic acid

Definition
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Retinoid.

Pharmacodynamics (Effect)
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Endogenous physiological ligand and sole panagonist for retinoic acid receptor (RAR) and retinoid X receptor (RXR). The activated receptors act as transcription factors that regulate gene expression, which in turn controls cell differentiation and proliferation in healthy and neoplastic cells. In vitro, alitretinoin can inhibit the growth of Kaposi's sarcoma cells. The exact mechanism of action in vivo is not known.

Anti-inflammatory effect in skin by inhibiting cytokine production in keratinocytes. Inhibition of leukocyte activity and inhibition of leukocyte and antigen-presenting cell (APC)-mediated chemotaxis with down-regulation of chemokines and other molecules important for the immune response (immunomodulation).

Indication
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Treatment of severe refractory chronic hand eczema.

Treatment of skin lesions in patients with HIV-related Kaposi's sarcoma when the lesions are not ulcerated or lymphedematous, treatment of systemic Kaposi's sarcoma lesions is not required, the lesions do not respond to systemic antiretroviral therapy, and radio- or chemotherapy is not adequate.

Individual case reports exist of success in Darier 's disease and lichen planus of the nails.

Pregnancy/nursing period
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Contraindicated.

Dosage and method of use
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Panretin: Kaposi's sarcoma: Apply 2 times/day initially, 2-4 times/day thickly to each lesion as therapy progresses. Therapy for 12 weeks. Skin lesions that respond to topical therapy with alitretinoin continue beyond that time.

Toctino: Chronic hand eczema: In this setting, the drug is shown to be effective at doses between 10-30 mg/day p.o.. Depending on clinical findings, a reduction to 10 mg/day can be made.

Undesirable effects
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Topical: Erythema, edema or blistering at the site of application in up to 70% of patients.

With oral medication: exsiccation of skin and mucous membranes especially cheilitis simplex; rhinitis, dermatitis, headache, trigyceride increases, hair frizz.

Preparations
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Topical: Panretin gel. The marketing authorization for Panretin has been withdrawn at the request of the marketing authorization holder.

Systemic: Toctino.

Note(s)
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According to the findings of the BACH study, alitretinoin can also be used in long-term therapy.

Literature
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  1. Alsenaid A et al. (2014) Successful treatment of nail lichen planus with alitretinoin: report of 2 cases and review of the literature. Dermatology 229:293-296.
  2. Barnstedt SE (2012) Successful therapy of Darier's disease with alitretinoin. Dermatologist 63:139-141
  3. HerinkC(2015) Hair frizz under systemic therapy with alitretinoin. Dermatologist 66: 617-619
  4. Molin S, Ruzicka T (2008) Alitretinoin. Dermatologist 59: 703-709
  5. Ruzicka T (2010) Alitretinoin also applicable in long-term therapy. Results of a specialist press conference in Munich in July 2010. Akt Dermatol 36: 494

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Last updated on: 04.05.2024