• To ↓ the risk of exacerbations in severe COPD patients that have a history of chronic bronchitis with exacerbations.

Contraindicated in:

• Acute bronchospasm
• Moderate to severe hepatic impairment
• Concurrent use of strong inducers of CYP3A4 and CYP1A2 enzymes
• Lactation: Lactation.

Use Cautiously in:

• History of depression/suicidal thoughts
• OB: Use only if potential maternal benefit justifies potential fetal risk
• Pedi: Safety and effectiveness not established in children.

Derm: rash.

GI: diarrhea, abdominal pain, ↓ appetite, dyspepsia, gastritis, nausea, vomiting.

Metab: weight loss.

MS: muscle spasms.

Neuro: tremor , SUICIDAL THOUGHTS/BEHAVIOR, anxiety, depression, dizziness, headache, insomnia.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA) .

Drug-Drug:

• Strong CYP3A4 and CYP1A2 inducers, including rifampicin, phenobarbital, carbamazepine, and phenytoin may ↓ levels and effectiveness; avoid concurrent use.
• Concurrent use of CYP3A4 inhibitors and dual CYP3A4 and CYP1A2 inhibitors, including erythomycin, ketoconazole, fluvoxamine, and cimetidine may ↑ levels and risk of toxicity.
• Ethinyl estradiol may ↑ levels and risk of toxicity.

(Generic available)

• Tablets: 250 mcg; 500 mcg;

• PO (Adults): 250 mcg once daily for 4 wk, then ↑ to 500 mcg once daily.

Daliresp

• Roflumilast and one active metabolite (roflumilast N-oxide) act as selective inhibitors of phosphodiesterase 4 (PDE4), responsible for breaking down 3', 5'-adenosine monophosphate (cAMP). Resulting intracellular accumulation of cAMP in lung tissue.
• Reduces cells (neutrophils, eosinophils and total cells) in sputum.

• ↓exacerbations in COPD patients.

Therapeutic Classification:

Pharmacologic Classification: phosphodiesterase inhibitors

Absorption: Well absorbed following oral administration.

Distribution: Parent drug and metabolites probably enter breast milk.

Protein Binding: Roflumilast — 99%; roflumilast N-oxide — 97%.

Metabolism/Excretion: Mostly metabolized (87.5%), primarily by CYP3A4 and CYP1A2 enzyme systems One metabolite, roflumilast N-oxide in pharmacologically active. Inactive metabolites excreted in urine.

Half-life: Roflumilast — 17 hr; roflumilast N-oxide — 30 hr.

Daxas

(blood levels)

†For roflumilast N-oxide.

• Instruct patient to take roflumilast as directed. Advise patient to read Medication Guide before starting therapy and with each Rx refill; new information may be available.
• Inform patient that roflumilast is not a bronchodilator and should not be used for treating sudden breathing problems.
• Advise patient to monitor weight regularly. If weight loss occurs, notify health care professional; may require discontinuation of therapy.
• Advise patient and family to notify health care professional if thoughts about suicide or dying, attempts to commit suicide, trouble sleeping, new or worse depression, new or worse anxiety, acting on dangerous impulses, or other unusual changes in behavior or mood or signs and symptoms of hypersensitivity reactions occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of Rx, OTC, and herbal products without consulting health care professional.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

row-FLOO-mi-last

NDC Code^*

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0088- Daliresp
    • 0310-0088-28- 1 BLISTER PACK in 1 BOX, UNIT-DOSE (0310-0088-28) > 28 TABLET in 1 BLISTER PACK

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0088- Daliresp
    • 0310-0088-39- 10 BLISTER PACK in 1 BOX, UNIT-DOSE (0310-0088-39) > 2 TABLET in 1 BLISTER PACK

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0088- Daliresp
    • 0310-0088-95- 1 BLISTER PACK in 1 BOX, UNIT-DOSE (0310-0088-95) > 28 TABLET in 1 BLISTER PACK

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0095- Daliresp
    • 0310-0095-30- 30 TABLET in 1 BOTTLE, PLASTIC (0310-0095-30)

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0095- Daliresp
    • 0310-0095-39- 10 BLISTER PACK in 1 BOX, UNIT-DOSE (0310-0095-39) > 2 TABLET in 1 BLISTER PACK

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0095- Daliresp
    • 0310-0095-90- 90 TABLET in 1 BOTTLE, PLASTIC (0310-0095-90)

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0095- Daliresp
    • 0310-0095-95- 7 BLISTER PACK in 1 BOX, UNIT-DOSE (0310-0095-95) > 1 TABLET in 1 BLISTER PACK