Retinoids
Synonym(s)
DefinitionThis section has been translated automatically.
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)This section has been translated automatically.
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.
IndicationThis section has been translated automatically.
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 effectsThis section has been translated automatically.
InteractionsThis section has been translated automatically.
ContraindicationThis section has been translated automatically.
PreparationsThis section has been translated automatically.
Note(s)This section has been translated automatically.
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!
LiteratureThis section has been translated automatically.
- Boisnic S et al (2002) Topical retinaldehyde treatment in oral lichen planus and leukoplakia. Int J Tissue React 24: 123-30.
- 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
- Jones PH et al (2003) A phase 1 study of tazarotene in adults with advanced cancer. Br J Cancer 89: 808-815
- 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
- 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.
TablesThis section has been translated automatically.
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 |