Dilarof 500 mcg

Description

Indications
Dilarof is indicated for the maintenance treatment of severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis in adult patients with a history of frequent exacerbations, as an add-on to bronchodilator treatment.
Use only as directed by a registered healthcare professional.

Pharmacology
Roflumilast, the active ingredient in Dilarof, is a phosphodiesterase-4 (PDE-4) inhibitor. By selectively inhibiting the PDE4 isoenzyme, it has potential anti-inflammatory and modulatory effects in the pulmonary system. This leads to increased intracellular cyclic AMP levels, which are believed to mediate its therapeutic effects.

Dosage & Administration

• Adult dose: The recommended dose is one tablet (500 micrograms) once daily. Roflumilast may take several weeks to show effects and has been studied in clinical trials for up to one year.
• Elderly (65 years and older): No dose adjustment is required.
• Renal impairment: No dose adjustment is required.
• Hepatic impairment: Roflumilast should be used with caution in patients with mild hepatic impairment (Child-Pugh A). It is contraindicated in patients with moderate or severe hepatic impairment (Child-Pugh B or C).
• Pediatric population: Not recommended for use in individuals under 18 years.

The tablet should be swallowed whole with water, at the same time each day, with or without food.
Use only as directed by a registered healthcare professional.

Interaction
No proven hazardous interactions. However, there are case reports of interactions with ethanol, pyrimethamine, dapsone, and betahistine. Concomitant use with H1 antagonists may reduce the effectiveness of the active agents.

Contraindications

• Hypersensitivity to Roflumilast or any of its excipients.
• Moderate or severe hepatic impairment.

Side Effects
Common adverse reactions observed in COPD studies include:

• Gastrointestinal: Diarrhoea (5.9%), nausea (2.9%), abdominal pain (1.9%)
• Other: Weight decreased (3.4%), headache (1.7%)

These side effects were mostly mild to moderate and occurred mainly in the first weeks of therapy.
Other possible side effects include:

• Immune system disorders: Hypersensitivity (Uncommon)
• Psychiatric: Insomnia (Common), Anxiety (Uncommon), Suicidal ideation (Rare)
• Nervous system: Headache (Common), Dizziness (Uncommon)
• Gastrointestinal: Vomiting, Gastritis (Uncommon)
• Musculoskeletal: Myalgia, Back pain (Uncommon)
• Skin: Rash (Uncommon)

Pregnancy & Lactation

• Pregnancy: Limited data available. Animal studies indicate reproductive toxicity. Roflumilast is not recommended during pregnancy or for women of childbearing potential who are not using contraception.
• Lactation: Roflumilast is excreted in animal milk. Use during breastfeeding is not recommended.

Precautions & Warnings

• Rescue medicinal product: Dilarof is not intended for acute bronchospasm relief.
• Weight loss: Regular monitoring of body weight is recommended, particularly in underweight patients. Discontinue Dilarof if there is unexplained, clinically concerning weight loss.
• Special conditions: Not recommended for patients with severe immunological diseases, infectious diseases, cancers (except basal cell carcinoma), or those on long-term immunosuppressive therapy.
• Psychiatric disorders: Increased risk of psychiatric disorders, including depression and suicidal ideation. Discontinue treatment if new or worsening psychiatric symptoms occur.
• Theophylline: Not recommended for use in combination with theophylline for maintenance therapy.
• Lactose: Contains lactose; not suitable for patients with galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.

Overdose Effects
Symptoms of overdose include headache, gastrointestinal disorders, dizziness, palpitations, and hypotension. In case of overdose, provide appropriate supportive care. Hemodialysis is not effective for removal due to high protein binding.

Therapeutic Class
Antihistamines, Anti-allergies, & Hypo-sensitisation

Storage Conditions
Store below 30°C, away from light and moisture. Keep out of reach of children.