Apremilast

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Information about Apremilast

  Apremilast is an orally available, small molecule inhibitor of phosphodiesterase-4 (PDE-4) and an immunomodulating agent that is used for treatment of refractory psoriatic arthritis. 

Liver safety of Apremilast

Apremilast has been linked to a low rate of serum enzyme elevations during therapy, but has not been implicated in cases of clinically apparent acute liver injury.

Mechanism of action of Apremilast

Apremilast (a pre' mi last) is a small molecule inhibitor of the enzyme phosphodiesterase-4 (PDE-4) that is responsible for the degradation of cyclic adenosine monophosphate (cAMP), thereby blocking an important step in the inflammatory signaling of immune effector cells including T lymphocytes, monocytes and macrophages.  Apremilast therapy has been shown to decrease the level of circulating proinflammatory cytokines and to improve symptoms in cases of psoriatic arthritis that have not responded to conventional therapies. 

FDA approval information for Apremilast

Apremilast was approved as oral therapy of active psoriatic arthritis and for moderate-to-severe plaque psoriasis in the United States in 2014.  It has been used experimentally and off-label to treat scalp and nail psoriasis and is under evaluation as therapy of other chronic inflammatory conditions. 

Dosage and administration for Apremilast

Apremilast is available in tablets of 10, 20 and 30 mg under the brand name Otezla.  The recommended initial dose is 10 mg twice daily, which can be increased based upon tolerance to the recommended maintenance dose of 30 mg twice daily. 

Side effects of Apremilast

Side effects include diarrhea, nausea, weight loss and headache which generally arise during the first few weeks of treatment and improve thereafter.  Rare, but potentially severe adverse events include reactivation of tuberculosis, depression, severe infections and increased risk of malignancy.

Antipsoriasis agents

Monoclonal Antibodies IL-17A Antagonists

Tumor Necrosis Factor Antagonists

Other

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