Apremilast is a drug used under the trade name Otezla in the treatment of plaque psoriasis and active psoriatic arthritis. It is an active substance from the group of PDE4 inhibitors. The effect of apremilast is based on inhibition of the enzyme phosphodiesterase-4.
What is apremilast?
Apremilast is a drug used under the trade name Otezla in the treatment of plaque psoriasis and active psoriatic arthritis. Otezla is used for moderate to severe plaque psoriasis. This is a disease that causes red and scaly patches on the skin. The drug apremilast is also used to treat the inflammation of the joints associated with psoriasis.
psoriatic arthritis, an inflammation of the joints associated with psoriasis. Otezla is used in patients for whom other systemic therapies do not achieve the desired effect. Otezla can also be used in combination with other disease-modifying antirheumatic drugs. The drug with the active ingredient apremilast requires a prescription and should be used only under the supervision of an experienced physician. Treatment is initiated gradually. Apremilast is commercially available as a film-coated tablet. It was first approved in the United States in 2014 under the trade name Otezla.
Pharmacologic action
Apremilast inhibits the enzyme phosphodiesterase-4, thereby increasing intracellular cyclic adenosine monophosphates (cAMP), biochemically derived molecules from adenosine triphosphates (ATP). They serve cellular signal transduction. This increase is followed by decreased formation of inflammatory mediators in inflammatory cells. The intracellular enzyme phoshodiesterase-4 (PDE4) plays an important role in the natural defense system of the human body, the immune system. It triggers the production of cytokines. These are messenger substances that are appropriately involved in inflammatory processes and processes that trigger psoriasis. By inhibiting PDE4, the concentration of these cytokines in the body is reduced. Inflammation and other symptoms of psoriasis are mitigated by this inhibitory effect. Apremilast is an oral small molecule PDE4 inhibitor. It acts intracellularly through the modulation already named. In the network of pro- and anti-inflammatory mediators, PDE4 is a dominant PDE. Inhibition results in downregulation of the inflammatory response. Presumably, the pro- and anti-inflammatory mediators are involved in the disease pattern of psoriasis and are positively manipulated by apremilast accordingly. In clinical studies, a significant modulation was observed in patients treated with apremilast. However, complete inhibition of plasma protein levels did not occur. In addition, apremilast reduced epidermis thickness in affected skin areas in patients. Furthermore, infiltration by inflammatory cells and expression of proinflammatory genes were significantly decreased. At doses of 50 mg twice daily, no prolongation of the QT interval was observed in patients.
Medical Application and Uses
Psoriasis is also called psoriasis. In this disease of the skin, nails or joints may also be affected. This chronic inflammatory skin disease is not contagious. Causes include a genetically inherited predisposition to psoriasis. Symptoms include the reddish inflamed skin areas, itching and silvery-white skin scales, which can have a size of several centimeters. This disease is usually chronic or with recurrent episodes. Clinical studies have demonstrated the efficacy of the drug apremilast in psoriasis and psoriatic arthritis, respectively. Apremilast has been used as monotherapy and as combination therapy with small molecule DMARDs, a basic therapy for inflammatory rheumatic diseases. As a result, treatment with apremilast significantly improved symptoms and signs of psoriasis and psoriatic arthritis, respectively. Response data were approximately equal in the group of patients receiving monotherapy and the group of patients receiving combination therapy. A treatment benefit was seen in different manifestations of psoriasis. Patients’ quality of life was significantly improved with apremilast.
Risks and Side Effects
The most common side effect of Otezla involves the digestive system. Diarrhea and nausea are very common symptoms.Upper respiratory tract infections, headache, especially tension headache, are also among the common side effects. Apremilast should not be used during pregnancy. Also, women should use effective contraceptive measures while taking it. Otezla was approved because the benefits outweigh the risks. Side effects are predominantly mild to moderate. The drug can be taken orally, is available up to 30 mg.
