Roflumilast (Tablet)

Generic Details

Generic Name

Roflumilast Tablet

Other Names

  • Daliresp

Drug Class

  • Phosphodiesterase-4 (PDE4) inhibitor

Chemical Formula

C17H14Cl2F2O3

Molecular Weight

403.20 g/mol

Mechanism of Action

  • Inhibition of PDE4 leading to decreased inflammation in the lungs

Indications

  • Treatment of severe chronic obstructive pulmonary disease (COPD)

Common Dosage Forms

  • Oral tablet

Typical Dosage

  • 500 mcg once daily

Pediatric Dosage

    Geriatric Dosage

      Side Effects

      • Diarrhea
      • Nausea
      • Headache
      • Weight loss
      • Insomnia

      Contraindications

      • Hypersensitivity to roflumilast or any components of the tablet

      Pregnancy Category

      • Category C - Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans

      Lactation Safety

      • Not recommended

      Drug Interactions

      • Strong CYP3A4 inhibitors
      • Theophylline

      Overdose Symptoms

        Antidote for Overdose

          Storage Conditions

          • Store at room temperature away from moisture and heat

          Pharmacokinetics

          • Absorption: Rapidly absorbed after oral administration
          • Distribution: Highly protein-bound
          • Metabolism: Metabolized in the liver mainly by CYP1A2 and CYP3A4 enzymes
          • Excretion: Mainly excreted in the feces

          Precautions

          • Monitor for neuropsychiatric events such as mood changes or suicidal thoughts

          Warnings

          • Not indicated for the treatment of acute bronchospasm

          Others

          • Avoid grapefruit and grapefruit juice while taking roflumilast due to potential drug interactions