Roflumilast Tablets (Daxas) are a selective phosphodiesterase 4 (PDE4) inhibitor, primarily indicated for reducing the risk of acute exacerbations in patients with severe chronic obstructive pulmonary disease (COPD) who have chronic bronchitis and a history of prior acute exacerbations.

Dosage and Administration, Recommended Dosage of Roflumilast Tablets (Daxas)

Initial and Maintenance Dosage

Initially, administer roflumilast 250 mcg tablets orally, once daily, for 4 consecutive weeks.

This is an initial titration dose rather than an effective therapeutic dose, designed to improve patients' tolerance to the medication and reduce the rate of treatment discontinuation due to adverse reactions.

After completing the 4-week initial treatment course, the dosage should be increased to roflumilast 500 mcg tablets, once daily, which shall be used as the long-term maintenance dose.

Administration Method

Roflumilast Tablets should be taken once daily. They can be administered with food or on an empty stomach, as diet does not affect the overall absorption of the drug.

Dosage Adjustment of Roflumilast Tablets (Daxas)

Conditions Requiring Dosage Adjustment or Avoidance

Hepatic impairment: This is a key area for dosage adjustment.

Mild hepatic impairment (Child-Pugh Class A): Exposure to roflumilast and its metabolites may be increased. Physicians need to carefully evaluate the risks and benefits of administration.

Moderate to severe hepatic impairment (Child-Pugh Class B or C): Increased drug exposure leads to a higher risk of adverse reactions. Roflumilast is contraindicated in patients with moderate to severe hepatic insufficiency.

Dosage Adjustment Due to Drug Interactions

Concomitant use with potent CYP450 enzyme inducers: Co-administration with potent enzyme inducers such as rifampicin, phenobarbital, carbamazepine and phenytoin is prohibited. These agents can significantly decrease the plasma concentration of roflumilast, resulting in treatment failure.

Concomitant use with CYP3A4 or CYP1A2 inhibitors: Co-administration with drugs including erythromycin, ketoconazole, fluvoxamine, enoxacin and cimetidine may increase roflumilast exposure, thereby elevating the risk of adverse reactions.

Use in Special Populations of Roflumilast Tablets (Daxas)

Pregnant and Lactating Women

Pregnant women: The use of roflumilast during pregnancy should be decided by physicians after a comprehensive assessment of potential risks and benefits. It should not be used during labor and delivery.

Lactating women: Roflumilast and its metabolites are likely to be excreted in human milk, and the effects on breastfed infants are unknown. The use of roflumilast is not recommended for lactating women. If administration is deemed necessary, breastfeeding must be discontinued.

Pediatric and Geriatric Patients

Pediatric patients: COPD rarely occurs in children. The efficacy of roflumilast in pediatric patients has not been established.

Geriatric patients (≥ 65 years old): No overall differences in efficacy have been observed between geriatric and younger patients, and dosage adjustment is not required under the conventional dosage regimen. However, individual variations should still be taken into account.