OTEZLA trade name.
First oral therapy for the treatment of adults with active psoriatic arthritis.
In phase III studies, demonstrated clinically significant improvements across multiple manifestations of psoriatic arthritis and a consistent safety profile.
In patients with oral ulcers with Behcet’s syndrome it resulted in a greater reduction in the number of oral ulcers than placebo, but was associated with adverse effects including diarrhea, nausea, and headache.
Routine laboratory monitoring is not required
Modulates inflammation through intracellular inhibition of PDE4
Oral, selective inhibitor of phosphodiesterase 4 (PDE4), for the treatment of adult patients with active psoriatic arthritis.
An oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP).
PDE4 inhibition results in increased intracellular cAMP levels.
Prevents degradation of cyclic adenosine monophosphate, decreasing the production of pro inflammatory cytokines and increases the production of anti-inflammatory mediators.
Psoriatic arthritis is a chronic disorder characterized by pain, stiffness, swelling and tenderness of the joints, inflammation of specific ligaments and tendons, and a decrease in physical functioning.
Presently is the only FDA-approved oral treatment for psoriatic arthritis.
Also useD as a treatment for the treatment of plaque psoriasis.
Three multi-center, randomized, double-blind, placebo-controlled trials conducted in adult patients with active psoriatic arthritis who were inadequately controlled by disease-modifying anti-rheumatic drugs (DMARDs) and/or biologics: 38 percent of patients treated with apremilast 30 mg twice daily achieved an ACR 20 response at week 16 versus 19 percent of patients on placebo.
Treatment results in improvement in dactylitis, and enthesitis, which is inflammation at sites where tendons or ligaments insert into bone.
Adverse reactions include: nausea, headache, upper respiratory tract infection, vomiting, nasopharyngitis, and upper abdominal pain.
10 percent of patients compared with 3.3 percent of patients taking placebo, reported weight loss of five to ten percent, such that patients should have their weight checked regularly.
Associated with an increase in adverse reactions of depression.
During clinical trials, 1.0% of patients reported depression or depressed mood, and 0.3% of patients discontinue treatment due to depression or depressed mood.
Drug exposure is decreased when co-administered with strong CYP450 inducers, such as rifampin, which may result in loss of efficacy.
Concomitant use with CYP450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended.
May be efficacious in the current aphthous stomatitis.
Adverse reactions reported in at least 2% of patients.
Adverse reactions include: diarrhea, nausea, headache, upper respiratory tract infection, vomiting, nasopharyngitis, and upper abdominal pain.
Not been studied in pregnant women.
Dosage should be reduced in patients with severe renal impairment.