Roflumilast is a selective phosphodiesterase-4 (PDE-4) inhibitor primarily used for long-term maintenance therapy of adult chronic obstructive pulmonary disease (COPD).

1、 Drug name

Roflumilast, trade name DALIRESP ®。

2、 Indications

Used to reduce the risk of acute exacerbation of chronic obstructive pulmonary disease (COPD) in patients with a history of chronic bronchitis and exacerbation.

Restrictive statement: This product is not a bronchodilator and is not suitable for relieving acute bronchospasm.

3、 Specifications and characteristics

Specification: Each tablet contains 500 micrograms of roflumilast.

Appearance: White to off white circular tablets, with "D" embossed on one side and "500" embossed on the other side.

4、 Main components

Active ingredient: Rofistat.

5、 Usage and dosage

Recommended dosage: once daily, one tablet (500 micrograms) each time, can be taken with or without food.

6、 Dose adjustment

Patients with liver dysfunction: Mild liver dysfunction (Child Pugh A grade) patients need to weigh the risks and benefits when using it. Patients with moderate to severe liver dysfunction (Child Pugh B or C grade) are contraindicated.

Patients with renal insufficiency: No need to adjust dosage.

Elderly patients: No need to adjust dosage.

7、 Medication precautions

Before and after meals: can be taken with or without food. Food can delay the peak time of roflunomide by about 1 hour and reduce the peak concentration by about 40%, but it does not affect the total absorption.

Missed dose: It is usually recommended to take the missed dose as soon as possible, but if it is close to the next dose, skip the missed dose and take the next dose at the regular time, without doubling the dose.

Vomiting: If vomiting occurs shortly after taking medication, it may affect drug absorption. It is recommended to consult a doctor or pharmacist.

Other precautions:

This product cannot be used to relieve acute bronchospasm. Patients should have emergency bronchodilators available.

Treatment is associated with an increased risk of mental events, including suicide. Patients, caregivers, and family members should be alert to the occurrence or worsening of insomnia, anxiety, depression, suicidal thoughts, or other emotional changes. Once they occur, they should contact a doctor. Patients with a history of depression and/or suicidal thoughts or behaviors should carefully weigh the risks and benefits before use.

Weight loss is a common adverse reaction. Patients should regularly monitor their weight. If there is unexplained or clinically significant weight loss, the weight loss should be evaluated and medication discontinuation should be considered.

During medication, avoid co administration with potent cytochrome P450 enzyme inducers such as rifampicin, phenobarbital, carbamazepine, and phenytoin, as they may reduce exposure to roflunomide and potentially weaken efficacy.

When used in combination with CYP3A4 inhibitors or CYP3A4 and CYP1A2 dual inhibitors (such as erythromycin, ketoconazole, fluvoxamine, enoxacin, cimetidine) or oral contraceptives containing gestodene and ethinylestradiol, there may be an increased exposure to rosuvastatin and the risk of adverse reactions. Careful consideration should be given to balancing the risks and benefits of use.

8、 Medication for special populations

Pregnant women: Use only when the potential benefits outweigh the potential risks to the fetus. Animal experiments have shown adverse effects.

Breastfeeding women: Rofistat and/or its metabolites may be excreted into human milk, and there is no relevant human research data available. Breastfeeding women should not use it.

Children: COPD usually does not occur in children, and safety and efficacy have not yet been established.

Older adults: No overall difference in safety and efficacy was observed compared to younger patients, but it cannot be ruled out that some older adults have higher sensitivity.

9、 Adverse reactions

The most common adverse reactions (incidence ≥ 2%):

Diarrhea, weight loss, nausea, headache, back pain, flu, insomnia, dizziness, decreased appetite.

Other significant adverse reactions:

Psychological events: including insomnia, anxiety, depression, suicidal ideation, and behavior (rare).

Weight loss: Some patients may experience moderate (5-10% weight loss) or severe (>10%) weight loss.

The main adverse reactions leading to discontinuation of medication are diarrhea and nausea.

Serious adverse reactions (higher incidence): diarrhea, atrial fibrillation, lung cancer, prostate cancer, acute pancreatitis, acute kidney failure.

10、 Contraindications

Moderate to severe liver dysfunction (Child Pugh B or C grade).

11、 Drug interactions

Prohibition of co use: Strong cytochrome P450 enzyme inducers (such as rifampicin, phenobarbital, carbamazepine, phenytoin), as they may reduce efficacy.

Caution should be exercised when using it (which may increase exposure and adverse reactions):

CYP3A4 inhibitors or CYP3A4/CYP1A2 dual inhibitors (such as erythromycin, ketoconazole, fluvoxamine, enoxacin, cimetidine).

Oral contraceptives containing progesterone and ethinylestradiol.

Drugs with no apparent interactions: inhaled salbutamol, formoterol, budesonide, as well as oral montelukast, digoxin, theophylline, warfarin, sildenafil, midazolam, antacids.

12、 Storage method

Store at 20 ° C to 25 ° C (68 ° F to 77 ° F); Allow short distance transportation between 15 ° C and 30 ° C (59 ° F and 86 ° F).

Roflumilastinformation