Roflumilast
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Category：Active Pharmaceutical Ingredients Own Brand：MT /MOQ:100KG /From China/ B2B only.
Introduction
English Synonyms 3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
Catalog ID99798
CAS NO.162401-32-3
Purity 98%
MDL NumberMFCD00938270
EINEC Molecular FormulaC17H14Cl2F2N2O3
Molecular Weight 403.211
| Category | Content |
|---|---|
| Generic Name | Roflumilast |
| Brand Name | Daliresp, Zoryve (topical form) |
| Drug Class | Phosphodiesterase-4 (PDE4) Inhibitor |
| Mechanism of Action | Roflumilast selectively inhibits PDE4, increasing intracellular cAMP levels in inflammatory cells. This reduces the release of inflammatory mediators and cytokines, leading to decreased inflammation and improved lung function. |
| Indications | – Reduces the risk of exacerbations in patients with severe COPD associated with chronic bronchitis.<br>- Also used topically for certain skin conditions (e.g., plaque psoriasis) under the brand name Zoryve. |
| Dosage Forms | Oral tablets (250 mcg, 500 mcg) and topical formulations. |
| Pharmacokinetics | – Bioavailability: Approximately 80%.<br>- Tmax: 1 hour for roflumilast, 8 hours for its active metabolite.<br>- Half-life: Approximately 17 hours.<br>- Metabolism: Primarily via CYP1A2 and CYP3A4. |
| Side Effects | Common: Nausea, diarrhea, weight loss, headache.<br> Serious: Increased risk of infections, psychiatric events, and liver toxicity. |
| Precautions | – Monitor weight regularly; report significant or unexpected weight loss.<br>- Avoid coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, erythromycin).<br>- Caution in patients with liver impairment. |
| Storage | Store at room temperature (20°C to 25°C), protect from moisture. |
| Developer | AstraZeneca |
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