Roflumilast

DALIRESP

What it isSelective PDE4 inhibitor with anti-inflammatory action; severe COPD with chronic bronchitis and exacerbations.

Why this oneIt reduces exacerbations in the chronic bronchitis phenotype, which bronchodilators alone do not.

What limits itWeight loss, diarrhea and psychiatric effects limit tolerability. It is not a bronchodilator and does nothing acutely.

FDA-approved for

FDA dosing	Population	Start	Target	Max
Reduce risk of COPD exacerbations	Adults	250 mcg QD x 4 weeks (to improve tolerability), then 500 mcg QD	500 mcg QD	500 mcg QD

Renal No dosage adjustment needed

Hepatic Mild (Child-Pugh A): weigh risk-benefit; contraindicated in moderate-severe (Child-Pugh B or C)

250 mcg is a starting/tolerability dose only and is not the effective (therapeutic) dose

Take once daily with or without food
Not a bronchodilator - do not use for relief of acute bronchospasm
Avoid strong CYP450 inducers (rifampicin, phenobarbital, carbamazepine, phenytoin)

Psychiatric events including suicidality - weigh risk in patients with depression/suicidal history
Weight decrease - monitor weight; evaluate and consider discontinuation if clinically significant loss
Not for acute bronchospasm
Use with strong CYP450 inducers not recommended

Pregnancy No human data; should not be used during labor and delivery; animal adverse effects at high multiples of MRHD.

Lactation Excretion into human milk probable; should not be used while nursing.

NO BOXED WARNINGS

Principal riskWeight loss and psychiatric effects

Cost, est. cash$30–$500/month

Generic entry2018

Therapeutic safety burden1 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityTremor, tachycardia or anticholinergic effects; excessive beta-agonist exposure can cause hypokalemia and arrhythmia.