Roxair 500 mcg

Description

Indications
Roxair 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.
Take the medication as prescribed by a registered physician.

Pharmacology
Roflumilast is a phosphodiesterase-4 (PDE-4) inhibitor that, due to its selective inhibition of the PDE4 isoenzyme, has potential anti-inflammatory and antimodulatory effects in the pulmonary system. It is thought that 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: Clinical data with Roflumilast in patients with mild hepatic impairment (Child-Pugh A) are insufficient to recommend a dose adjustment. Therefore, Roflumilast should be used with caution in these patients. Patients with moderate or severe hepatic impairment (Child-Pugh B or C) must not take Roflumilast.
• Pediatric population: Roflumilast is not relevant for use in the pediatric population (under 18 years). The tablet should be swallowed with water and taken at the same time every day. It can be taken with or without food.
  Take the medication as prescribed by a registered physician.

Interaction
There are no proven cases of hazardous interactions. There have been reports of interaction with ethanol and a compound containing pyrimethamine with dapsone. Another report indicated potentiation of betahistine with salbutamol. The concurrent administration of H1 antagonists may cause a mutual attenuation of the effect of active agents.

Contraindications

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

Side Effects
In clinical COPD studies, approximately 16% of patients experienced adverse reactions with Roxair (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%), and headache (1.7%). These were primarily mild or moderate and generally resolved with continued treatment. Adverse reactions are categorized as follows:

• Very common: 1/10
• Common: 1/100 to <1/10
• Uncommon: 1/1,000 to <1/100
• Rare: 1/10,000 to <1/1,000
• Very rare: <1/10,000
• Not known: cannot be estimated from available data

Other reported adverse reactions include:

• Immune system disorders: Uncommon: Hypersensitivity
• Endocrine disorders: Rare: Gynecomastia
• 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, Gastroesophageal reflux disease, Dyspepsia, Rare: Hematochezia, 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 is limited data on the use of Roflumilast in pregnant women. Animal studies have shown reproductive toxicity. Roflumilast is not recommended during pregnancy or in women of childbearing potential not using contraception. It has been shown to cross the placenta in pregnant rats.
• Lactation: Pharmacokinetic data in animals show the excretion of Roflumilast or its metabolites in milk. A risk to the suckling child cannot be excluded, so Roflumilast should not be used during breastfeeding.

Precautions & Warnings

• Rescue medicinal products: Roxair is not a rescue medication for the relief of acute bronchospasms.
• Weight decrease: Weight loss occurred more frequently in patients treated with Roxair compared to those treated with a placebo. If significant weight loss is observed, Roxair should be discontinued and further follow-up on body weight is recommended.
• Special clinical conditions: Roxair should not be initiated in patients with severe immunological diseases, severe acute infections, cancers (except basal cell carcinoma), or those receiving immunosuppressive therapy. Caution should be used in patients with latent infections like tuberculosis or viral hepatitis.
• Psychiatric disorders: Roxair is associated with an increased risk of psychiatric disorders like insomnia, anxiety, nervousness, and depression. Rare instances of suicidal ideation and behavior have been observed, especially within the first weeks of treatment. Discontinue if new or worsening psychiatric symptoms occur.
• Persistent intolerability: If adverse reactions like diarrhea, nausea, abdominal pain, and headache persist, reconsider the treatment plan.
• Theophylline: Concomitant treatment with theophylline is not recommended.
• Lactose: Roxair tablets contain lactose, so patients with lactose intolerance should not use this product.

Overdose Effects
In Phase I studies, symptoms such as headache, gastrointestinal disorders, dizziness, palpitations, light-headedness, clamminess, and arterial hypotension were observed at increased rates after single oral doses of 2,500 micrograms and one dose of 5,000 micrograms (ten times the recommended dose). In case of overdose, appropriate supportive medical care should be provided. Roxair is highly protein-bound, so hemodialysis is unlikely to be effective in its removal.

Therapeutic Class
Antihistamines, anti-allergies, and hypo-sensitization.

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