Romilast 500 mcg

Description

Indications
Romilast 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, which, due to its selective inhibition of the PDE4 isoenzyme, has potential anti-inflammatory and anti-modulatory 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: Clinical data with Roflumilast in patients with mild hepatic impairment classified as Child-Pugh A are insufficient to recommend a dose adjustment, so 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 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 an interaction with ethanol and a compound containing pyrimethamine with dapsone, and another report of potentiation of betahistine with salbutamol. Since Betahistine is a histamine analogue, concurrent administration of H1 antagonists may cause mutual attenuation of the effects 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 Romilast (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 adverse reactions were mostly mild or moderate, typically occurring within the first weeks of therapy and generally resolving with continued treatment.
Adverse reactions are ranked under the MedDRA frequency classification:

• 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, Gastro-esophageal 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: Limited data on the use of Roflumilast in pregnant women are available. Studies in animals 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: Available pharmacokinetic data in animals show that Roflumilast or its metabolites are excreted in milk. The risk to the suckling child cannot be excluded, so Roflumilast should not be used during breastfeeding.

Precautions & Warnings

• Rescue medicinal products: Romilast is not indicated as a rescue medicine for acute bronchospasms.
• Weight decrease: Weight loss occurred more frequently in patients treated with Romilast compared to placebo-treated patients in studies. Patients’ body weight should be monitored regularly. In case of unexplained and clinically concerning weight loss, Romilast should be discontinued, and body weight should be followed up further.
• Special clinical conditions: Romilast should not be used in patients with severe immunological diseases, severe acute infections, cancers (except basal cell carcinoma), or patients receiving immunosuppressive therapy. Caution is advised in patients with latent infections such as tuberculosis or viral hepatitis.
• Psychiatric disorders: Romilast has been associated with an increased risk of psychiatric disorders such as insomnia, anxiety, depression, and suicidal ideation. If any new or worsening psychiatric symptoms are observed, or if suicidal thoughts or attempts occur, the treatment should be discontinued.
• Persistent intolerability: In patients who experience persistent adverse reactions like diarrhea, nausea, abdominal pain, or headache, Romilast treatment should be reassessed.
• Theophylline: Romilast is not recommended in conjunction with theophylline for maintenance therapy.
• Lactose: Romilast tablets contain lactose, so patients with galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take this product.

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

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

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