ATC Group: D11A Other dermatological preparations

Abrocitinib is a Janus kinase (JAK)1 inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of haematopoiesis and immune cell function. JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Inhibition of JAK1 modulates the signalling pathways by preventing the phosphorylation and activation of STATs.

Alitretinoin is a naturally-occurring endogenous hormone related to vitamin A, binds to and activates all known intracellular retinoid receptor subtypes (RAR, RAR, RAR, RXR, RXR, RXR). The efficacy of alitretinoin in treating KS lesions may be related to the demonstrated ability of alitretinoin to inhibit the in vitro growth of KS cells.

Brimonidine is an alpha₂-adrenergic receptor agonist that is 1000-fold more selective for the alpha₂-adrenoceptor than the alpha₁-adrenoreceptor. This selectivity results in no mydriasis and the absence of vasoconstriction in microvessels associated with human retinal xenografts.

Caffeine is structurally related to the methylxanthines theophylline and theobromine. Caffeine’s main action is as a CNS stimulant.

Calcium gluconate is the gluconate salt of calcium. An element or mineral necessary for normal nerve, muscle, and cardiac function, calcium as the gluconate salt helps to maintain calcium balance and prevent bone loss when taken orally.

Cetrimide is a quaternary ammonium cationic disinfectant with bactericidal activity against gram-positive and some gram-negative organisms. Cetrimide is relatively ineffective against viruses.

Crisaborole is an anti-inflammatory benzoxaborole phosphodiesterase-4 (PDE4) inhibitor that suppresses secretion of certain cytokines, such as tumour necrosis factor-α (TNF-α), interleukins (IL-2, IL-4, IL-5), and interferon gamma (IFNγ), and improves skin barrier function as measured by transepidermal water loss (TEWL). It is used for treatment of mild to moderate atopic dermatitis in adults and paediatric patients.

Sodium cromoglicate (Cromoglicic acid) inhibits the activation of many of the cell types involved in the development and progression of asthma. Thus, sodium cromoglicate inhibits the release of inflammatory mediators including cytokines from mast cells and reduces the chemotactic activity of eosinophils and neutrophils.

Deoxycholic acid is a cytolytic drug, which when injected into localized subcutaneous fat, physically disrupts the cell membrane of adipocytes. The destruction of adipocytes elicits a tissue response in which macrophages are attracted to the area to eliminate cellular debris and lipids, which are then cleared through natural processes.

Diclofenac is a non-steroidal anti-inflammatory drug. The mechanism of action of diclofenac in AK may be related to the inhibition of the cycloxygenase pathway leading to reduced prostaglandin E₂ (PGE₂) synthesis. In addition, immunohistochemistry (IHC) from skin biopsies ac revealed that the clinical effects of diclofenac in AK are primarily due to anti-inflammatory, anti-angiogenic and possibly anti-proliferative effects and apoptosis-inducing mechanisms.

Dupilumab is a recombinant human IgG4 monoclonal antibody that inhibits interleukin-4 and interleukin-13 signaling. Dupilumab inhibits IL-4 signaling via the Type I receptor (IL-4Rα/γc), and both IL-4 and IL-13 signaling through the Type II receptor (IL-4Rα/IL-13Rα). IL-4 and IL-13 are major drivers of human type 2 inflammatory disease, such as atopic dermatitis, asthma, and CRSwNP. Blocking the IL-4/IL-13 pathway with dupilumab in patients decreases many of the mediators of type 2 inflammation.

Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme involved in the production of the hair shaft by the hair follicle. Eflornithine has been shown to reduce the rate of hair growth.

Finasteride is a competitive inhibitor of human 5α-reductase, an intracellular enzyme which metabolises testosterone into the more potent androgen, dihydrotestosterone (DHT). In benign prostatic hyperplasia (BPH), enlargement of the prostate gland is dependent upon the conversion of testosterone to DHT within the prostate. Finasteride is highly effective in reducing circulating and intraprostatic DHT. Finasteride has no affinity for the androgen receptor.

Glycopyrronium is an inhaled long-acting muscarinic receptor antagonist (anticholinergic) for once-daily maintenance bronchodilator treatment of COPD. Glycopyrronium works by blocking the bronchoconstrictor action of acetylcholine on airway smooth muscle cells, thereby dilating the airways.

Hydroquinone is a skin bleaching agent. Topical application of hydroquinone produces a reversible depigmentation of the skin by inhibition of the enzymatic oxidation of tyrosine to 3,4-dihydroxyphenylalanine (dopa).

Ivermectin is a member of the avermectin class and has high affinity with glutamate-gated chloride channels present in invertebrate nerve and muscle cells. Its binding to these channels promotes an increase in membrane permeability to chloride ions, leading to hyperpolarization of the neural or muscle cell. This results in neuromuscular paralysis and may lead to the death of certain parasites.

Lebrikizumab is an immunoglobulin (IgG4) monoclonal antibody that binds with high affinity to interleukin (IL)-13 and selectively inhibits IL-13 signalling through the IL-4 receptor alpha (IL-4Rα)/ IL-13 receptor alpha 1 (IL-13Rα1) heterodimer, thereby inhibiting the downstream effects of IL-13. Inhibition of IL-13 signalling is expected to be of benefit in diseases in which IL-13 is a key contributor to the disease pathogenesis. Lebrikizumab does not prevent the binding of IL-13 to the IL-13 receptor alpha 2 (IL-13Rα2 or decoy receptor), which allows the internalisation of IL-13 into the cell.

Little is known about the way the lithium ion can modify neurotransmission within the CNS. Many of the proposed mechanisms have suggested an inhibitory effect on components of various neurotransmitter signalling pathways, such as cyclic AMP formation, cyclic GMP formation, G-proteins or inositol phosphate metabolism.

Magnesium sulfate is a saline purgative. It can be employed locally in various inflammatory conditions, due to its osmotic action.

Topical administration of minoxidil stimulates hair growth in men and women with androgenic alopecia. The mechanism of stimulating hair growth from minoxidil is not fully understood, but some actions of minoxidil include increasing hair diameter, stimulating new growth and prolonging the developmental phase, and stimulating hair follicle transition from resting phase (telogen) in the growth phase (regenerative).

Pimecrolimus is a lipophilic anti-inflammatory ascomycin macrolactam derivative and a cell selective inhibitor of the production and release of pro-inflammatory cytokines.

Povidone iodine is an iodophore that has an established use as a broad-spectrum antiseptic, mainly for the treatment of contaminated wounds and for the preoperative preparation of the skin, mucous membranes and the ocular surface. The organic complex contains approximately 10% of active available iodine. Solutions of povidone iodine gradually release iodine to exert an antimicrobial effect against bacteria, fungi, viruses, and spores. Although povidone iodine is less potent than preparations containing free iodine, it is also less toxic.

Ruxolitinib is a selective inhibitor of the Janus Associated Kinases (JAKs) JAK1 and JAK2 (IC₅₀ values of 3.3 nM and 2.8 nM for JAK1 and JAK2 enzymes, respectively). These mediate the signalling of a number of cytokines and growth factors that are important for haematopoiesis and immune function. Ruxolitinib inhibits cytokine-induced STAT3 phosphorylation in whole blood from healthy subjects, MF patients and PV patients.

Tacrolimus is a highly potent immunosuppressive agent. In particular, tacrolimus inhibits the formation of cytotoxic lymphocytes, which are mainly responsible for graft rejection. Tacrolimus suppresses T-cell activation and T-helper-cell dependent B-cell proliferation, as well as the formation of lymphokines (such as interleukins-2, -3, and γ-interferon) and the expression of the interleukin-2 receptor.

Tralokinumab is a fully human IgG4 monoclonal antibody that specifically binds to the type 2 cytokine interleukin-13 (IL-13) and inhibits its interaction with the IL-13 receptors. Tralokinumab neutralises the biological activity of IL-13 by blocking its interaction with the IL-13Rα1/IL-4Rα receptor complex. IL-13 is a major driver of human type 2 inflammatory disease, such as atopic dermatitis and inhibiting the IL-13 pathway with tralokinumab in patients decreases many of the mediators of type 2 inflammation.