Roflast 500 mcg

Description

Indications

Roflast is indicated for maintenance treatment of severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis in adult patients with a history of frequent exacerbations as add-on to bronchodilator treatment.
Take medication as per the advice of a registered physician.

Pharmacology

Roflumilast is a phosphodiesterase-4 (PDE-4) inhibitor which, due to its selective inhibition of the PDE4 isoenzyme, has potential anti-inflammatory and immunomodulatory effects in the pulmonary system. It is thought that the increased levels of intracellular cyclic AMP are responsible for the therapeutic actions of Roflumilast.

Dosage & Administration

Adult dose: The recommended dose is one tablet of 500 micrograms Roflumilast once daily. Roflumilast may need to be taken for several weeks to achieve its effect. Roflumilast has been studied in clinical trials for up to one year.

Elderly (65 years and older): No dose adjustment is necessary.

Renal impairment: No dose adjustment is necessary.

Hepatic impairment: The clinical data with Roflumilast in patients with mild hepatic impairment classified as Child-Pugh A are insufficient to recommend a dose adjustment and therefore Roflumilast should be used with caution in these patients. Patients with moderate or severe hepatic impairment classified as Child-Pugh B or C must not take Roflumilast.

Pediatric population: There is no relevant use of Roflumilast in the paediatric population (under 18 years).

The tablet should be swallowed with water and taken at the same time every day. The tablet can be taken with or without food.
Take medication as per the advice of a registered physician.

Interaction

There are no proven cases of hazardous interactions. There is a case report of an interaction with ethanol and a compound containing pyrimethamine with dapsone and another of potentiation of betahistine with salbutamol. Betahistine is a histamine analogue, concurrent administration of H1 antagonists may cause a mutual attenuation of effect of the active agents.

Contraindications

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

Side Effects

In clinical COPD studies, approximately 16% of patients experienced adverse reactions with Roflast (compared to 5% in placebo). The most commonly reported adverse reactions were:

• Diarrhea (5.9%)
• Weight decreased (3.4%)
• Nausea (2.9%)
• Abdominal pain (1.9%)
• Headache (1.7%)

The majority of these adverse reactions were mild or moderate. These adverse reactions mainly occurred within the first weeks of therapy and mostly resolved on continued treatment.

Adverse reactions classified by MedDRA frequency:

• Immune system disorders: Uncommon: Hypersensitivity
• Endocrine disorders: Rare: Gynaecomastia
• Metabolism and nutrition disorders: Common: Weight decreased, Decreased appetite
• Psychiatric disorders: Common: Insomnia; Uncommon: Anxiety; Rare: Suicidal ideation and behavior, Depression, Nervousness
• Nervous system disorders: Common: Headache; Uncommon: Tremor, Vertigo, Dizziness; Rare: Dysgeusia
• Cardiac disorders: Uncommon: Palpitations
• Respiratory, thoracic and mediastinal disorders: Rare: Respiratory tract infections (excluding Pneumonia)
• Gastrointestinal disorders: Common: Diarrhea, Nausea, Abdominal pain; Uncommon: Gastritis, Vomiting, Gastro-esophageal reflux disease, Dyspepsia; Rare: Haematochezia, Constipation
• Hepatobiliary disorders: Rare: Gamma-GT increased, Aspartate aminotransferase (AST) increased
• Skin and subcutaneous tissue disorders: Uncommon: Rash; Rare: Urticaria
• Musculoskeletal and connective tissue disorders: Uncommon: Muscle spasms and weakness, Myalgia, Back pain; Rare: Blood creatine phosphokinase (CPK) increased
• General disorders and administration site conditions: Uncommon: Malaise, Asthenia, Fatigue

Pregnancy & Lactation

Pregnancy: There are limited amount of data from the use of Roflumilast in pregnant women. Studies in animals have shown reproductive toxicity. Roflumilast is not recommended during pregnancy and in women of childbearing potential not using contraception. Roflumilast has been demonstrated to cross the placenta in pregnant rats.

Lactation: Available pharmacokinetic data in animals have shown excretion of Roflumilast or its metabolites in milk. A risk to the suckling child cannot be excluded. Roflumilast should not be used during breastfeeding.

Precautions & Warnings

All patients should be informed about the risks of Roflast and the precautions for safe use.

• Rescue medicinal products: Roflast is an anti-inflammatory substance; it is not indicated as a rescue medicinal product for the relief of acute bronchospasms.
• Weight decrease: In 1-year studies, a decrease of body weight occurred more frequently in patients treated with Roflast compared to placebo-treated patients. After discontinuation of Roflast, the majority of patients had regained body weight after 3 months. Body weight of underweight patients should be checked at each visit. Patients should be advised to check their body weight regularly. If unexplained and clinically concerning weight loss occurs, Roflast should be stopped and body weight should be monitored.
• Special clinical conditions: Due to lack of relevant experience, Roflast should not be initiated or continued in patients with severe immunological diseases (e.g. HIV infection, multiple sclerosis, lupus erythematosus, progressive multifocal leukoencephalopathy), severe acute infectious diseases, cancers (except basal cell carcinoma), or patients being treated with immunosuppressive drugs.
• Psychiatric disorders: Roflast is associated with increased risk of psychiatric disorders such as insomnia, anxiety, nervousness, and depression. Rare instances of suicidal ideation and behavior, including completed suicide, have been observed. Patients should be monitored closely for mood changes, and treatment should be discontinued if symptoms worsen.
• Persistent intolerability: If adverse reactions persist, reassessment of Roflast treatment is recommended.
• Theophylline: No clinical data support concomitant use with theophylline for maintenance therapy. Concurrent use is not recommended.
• Lactose intolerance: Roflast contains lactose. Patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicine.

Overdose Effects

In Phase I studies, symptoms observed at an increased rate after single doses of 2,500 micrograms and 5,000 micrograms (ten times the recommended dose) included headache, gastrointestinal disorders, dizziness, palpitations, light-headedness, clamminess, and arterial hypotension. Supportive medical care is recommended in case of overdose. Since Roflumilast is highly protein-bound, hemodialysis is unlikely to be effective in removing the drug. It is unknown whether Roflumilast is dialyzable via peritoneal dialysis.

Therapeutic Class

Antihistamines, anti-allergies & hypo-sensitization

Storage Conditions

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