Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Retinoids are chemical substances related to vitamin A. This group of substances is used in dermatology both for local (cream/ointment/gel) and systemic therapy.

Retinoids are most frequently used in the treatment of severe acne or various forms of psoriasis. Retinoids are also used in the treatment or prevention of certain tumour diseases of the skin. The therapy of advanced stages of cutaneous T-cell lymphoma is the main focus here.

Pharmacodynamics (Effect)
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The exact mechanism of action of retinoids is not yet fully understood. The activation of selective retinoid X-receptors (RXRs) or RAR (retiniod-acid receptor), which are important in cell metabolism (vitamin D3, thyroid hormone receptor, proliferation-activating receptor in peroxysomes), is being discussed. The retinoid-activated retinoid receptors form homo- or heterodimers which bind to specific DNA sequences and act as transcription factors for genes. RAR regulates cell growth and differentiation, RXR regulates apoptosis.

  • Retinoids act on:
  • cell division (antiproliferative)
  • Stability of the lysosomal membranes
  • Integrity of cell membranes
  • Arachidonic acid metabolism
  • RNA Synthesis
  • Protein Synthesis
  • Glycosidation of proteins.

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The indications for systemic retinoids vary depending on the preparation, see Table 1, and the indication "cutaneous T-cell lymphomas" for the preparation Bexaroten.

Approved active ingredients are:

Undesirable effects
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See Table 2.

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See Table 3.

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Pregnancy, lactation, blood donation, liver dysfunction, pre-existing lipometabolic disorders, contact lens wearers, manifest diabetes mellitus, renal insufficiency, hypersensitivity to the preparation, combination with vitamin A or other retinoids, tetracyclines, methotrexate. S.u. Acitretin, Isotretinoin, Tazarotene, Tretinoin.

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acenormin, isoderm, isotrex, isotrexine (combination with erythromycin), neotigason, bexarotene, zorac, isotretinoin, tazarotene

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The risk of PUVA-treated psoriatics to get a spinocellular squamous cell carcinoma is reduced if retinoids are taken at the same time!

Notice! Due to their pronounced teratogenicity, retinoids are not approved for the treatment of women of childbearing age. The consequences under civil and criminal law lie exclusively with the prescribing physician. In principle, women of childbearing age must have a negative pregnancy test before initiating therapy and effective contraception must be carried out 4 weeks before initiating therapy. Regular pregnancy tests must be carried out during therapy. Pregnancy must be ruled out up to 12 weeks after the end of therapy with isotretinoin (e.g. isotretinoin-ratiopharm; acne normin) and 2 years after acitretin

(neotigason). Patients must not donate blood while under retinoid therapy!Cave! Conceptional protection by oral contraceptives is impaired!

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  1. Boisnic S et al (2002) Topical retinaldehyde treatment in oral lichen planus and leukoplakia. Int J Tissue React 24: 123-30.
  2. Duvic M et al (2003) Analysis of long-term outcomes of combined modality therapy for cutaneous T-cell lymphoma. J Am Acad Dermatol 49: 35-49
  3. Jones PH et al (2003) A phase 1 study of tazarotene in adults with advanced cancer. Br J Cancer 89: 808-815
  4. Nijsten TE, Stern RS (2003) Oral retinoid use reduces cutaneous squamous cell carcinoma risk in patients with psoriasis treated with psoralen-UVA: a nested cohort study. J Am Acad Dermatol 49: 644-650
  5. Xu D et al (2016) Binding characterization, synthesis and biological evaluation of RXRα antagonists targeting the coactivator binding site. Bioorg Med Chem Lett 26:3846-3849.

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Indications for systemic retinoids




Keratinization disorders

acne conglobata



acne fulminans



M. Darier



ichthyosis vulgaris



Palmo-Plantar Keratoses



Disseminated actinic porokeratosis


Inflammatory dermatoses

psoriasis vulgaris



pustular psoriasis


Psoriatic Erythroderma


Subcorneal pustulose


lichen planus


Side effects of retinoids (modified, from Red List)

Organ System

Undesirable side effects (ADR)


Dryness of the nasal mucosa, nosebleeds, hoarseness, dry throat mucosa


conjunctivitis, inflammation of the conjunctiva, passagere corneal opacity (rare), opacity of the lens, corneal inflammation

Increased corneal vulnerability, corneal ulcers (rare)

visual disorders (reduction of night vision (isotretinoin), temporary reduction of visual acuity, deterioration of light/dark vision, reduced sensitivity to glare)


thrombocytopenia, anemia, thrombocytosis, neutropenia, BSG ↑, leukopenia


Vasculitis, triggering Wegener's granulomatosis


dryness of the lips or oral mucosa, cheilitis

Gastrointestinal disorders (abdominal pain, diarrhoea, intestinal bleeding), discontinuation in the event of colitis/ivitis (isotretinoin)

nausea, vomiting, gastrointestinal ulcers

Liver dysfunction, hepatitis (individual cases)


Increased tissue formation (granulation tissue)

Skin desquamation, skin redness, skin thinning with increased vulnerability

Skin peeling on palms of hands and soles of feet, rhagade formation

feeling of "burning" or "sticky" skin, itching, skin irritation on the face, sweating

Nailwall inflammation, nail dystrophy

Change of the hair growth rate, pigment shift of skin and hair, hair loss

Increased light sensitivity of the healing skin, intensification of the signs of disease at the beginning of treatment

exanthema, eczema, urticaria, purpura, blistering, skin ulcers, Staphylococcus aureus infections

Nervous System

Increase in intracranial pressure, pseudotumour cerebri (rare), headache


Hearing disorders

Metabolism, Endocrine

Blood lipid values ↑, HDL cholesterol ↓, blood sugar ↑ (connection questionable), diabetes or worsening of diabetes, thirst, freezing, creatine phosphokinase ↑, prolactin and uric acid values ↑, gynecomastia, edema

Support apparatus

muscle and joint pain, bone changes, skeletal hyperostoses, premature closure of the bone growth joints (rare), bone pain, soft tissue calcification, functional movement restrictions

Urogenital tract

Non-specific urethritides and vulvitides, menstrual disorders, hematuria, proteinuria


Depression, behavioural disorders, seizures

Significant interactions of retinoids


Carbamazepine bioavailability ↓

Contraceptives, oral

Contraception ↓


Phenytoin levels ↑


Intracranial pressure increase, combination contraindicated

vitamin A

Vitamin A toxicity ↑, combination contraindicated


Last updated on: 29.10.2020