Retinoids

Author: Prof. Dr. med. Peter Altmeyer

All authors of this article

Last updated on: 26.07.2024

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Synonym(s)

Retinoid

Definition
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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.

Indication
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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.

Interactions
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See Table 3.

Contraindication
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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.

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

Note(s)
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The risk of PUVA-treated psoriatic patients developing spinocellular squamous cell carcinoma is reduced if retinoids are taken at the same time!

Please note! 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 doctor. In principle, women of childbearing age must have a negative pregnancy test before starting treatment and effective contraception must be used 4 weeks before starting treatment. Pregnancy tests must be carried out regularly during therapy. Pregnancy must be ruled out up to 12 weeks after the end of treatment with isotretinoin (e.g. Isotretinoin-ratiopharm; Acnenormin) and 2 years after acitretin (Neotigason). Patients must not donate blood during treatment with retinoids!

Caution! Conception protection by oral contraceptives is impaired!

Literature
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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.

Tables
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Indications for systemic retinoids

Indication

Isotretinoin

Acitretin

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)

Airways

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

eyes

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)

Blood

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

Vessels

Vasculitis, triggering Wegener's granulomatosis

GIT

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)

Skin

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

Ears

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

CNS

Depression, behavioural disorders, seizures


Significant interactions of retinoids

Carbamazepine

Carbamazepine bioavailability ↓

Contraceptives, oral

Contraception ↓

Phenytoin

Phenytoin levels ↑

Tetracyclines

Intracranial pressure increase, combination contraindicated

vitamin A

Vitamin A toxicity ↑, combination contraindicated

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Last updated on: 26.07.2024