Dilarof Tablet

Dilarof Tablet 500 mcg is a phosphodiesterase-4 (PDE-4) inhibitor. Due to its selective inhibition of the PDE4 isoenzyme in lung cells, roflumilast is indicated for the management of chronic obstrtuctive pulmonary disease (COPD) exacerbations. Treatment with Dilarof Tablet 500 mcg is associated with an increase in psychiatric adverse reactions, including suicide and suicidal attempts.

Dilarof Tablet 500 mcg is a selective phosphodiesterase 4 inhibitor indicated to decrease the risk of exacerbations in patients with severe chronic obstructive pulmonary disease (COPD) associated with a history of exacerbations and chronic bronchitis.

Dilarof Tablet 500 mcg is indicated as a treatment to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. Dilarof Tablet 500 mcg is not a bronchodilator and is not indicated for the relief of acute bronchospasm.

• Chronic Obstructive Pulmonary Disease (COPD)

Dilarof Tablet 500 mcg (and its active metabolite, roflumilast N-oxide) increases cyclic adenosine-3′, 5′-monophosphate (cAMP) in lung cells by inhibiting PDE4. Increased cAMP activates PKA, which inactivates transcription factors involved in inflammation. Romflumilast also decreases the amount of sputum neutrophils and eosinophils in COPD patients.

Dilarof Tablet 500 mcg is a phosphodiesterase-4 (PDE-4) inhibitor which, due to its selective inhibition of the PDE4 isoenzyme, has potential antiinflammatory and antimodulatory effects in the pulmonary system. It is thought that the increased levels of intracellular cyclic AMP are responsible for the therapeutic actions of Dilarof Tablet 500 mcg.

After a 500mcg dose, the bioavailability of roflumilast is about 80%. In the fasted state, maximum plasma concentrations are reached in 0.5 to 2 hours. While in the fed state, Cmax is reduced by 40%, Tmax is increased by one hour, and total absorption is unchanged.

Dilarof Tablet 500 mcg has a Vd of 2.9L/kg with a dose of 500mcg. Permeability of roflumilast across the blood-brain barrier appears to be poor in rat studies.

Dilarof Tablet 500 mcg is 99% plasma protein bound.

Dilarof Tablet 500 mcg is excreted 70% in the urine as roflumilast N-oxide.

Plasma half-life of roflumilast is 17 hours and its metabolite is 30 hours (oral dose).

~9.6 L/hour.

Headache, weight loss, GI upset, insomnia, and loose stools.

• Take with or without food. Administering roflumilast with a high-fat meal reduced and delayed the Cmax and Tmax, respectively, but did not impact the AUC of roflumilast or its active metabolite (roflumilast N‐oxide).