Roflu 500 mcg

Description

Indications
Roflu is recommended as a long-term treatment for individuals suffering from severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis. It is specifically aimed at adults who have a history of frequent exacerbations and can be used as an additional therapy alongside bronchodilator medications.

Use this medication only under the guidance of a registered healthcare provider.

Pharmacology
Roflumilast acts as a selective inhibitor of the phosphodiesterase-4 (PDE-4) enzyme. This inhibition results in potential anti-inflammatory and immunomodulatory effects within the lungs, which help manage COPD symptoms. The therapeutic effects are believed to be linked to the increased levels of cyclic AMP inside cells, which contributes to the overall beneficial action of Roflumilast.

Dosage & Administration
For adults, the typical dosage is one tablet of 500 micrograms of Roflumilast, to be taken once daily. It may take several weeks of consistent use to notice its full effect. Clinical trials have shown that Roflumilast can be effective for up to one year.

• Elderly patients (65 years and older): No adjustment in dosage is required.
• Renal impairment: No change in dosage is necessary.
• Hepatic impairment: Roflumilast should be used with caution in patients with mild hepatic impairment (Child-Pugh A). In those with moderate or severe hepatic impairment (Child-Pugh B or C), Roflumilast is contraindicated.
• Pediatric population: Roflumilast is not recommended for use in children under 18 years of age. The tablet should be swallowed whole with water at the same time each day, and it can be taken with or without food.

Consult your healthcare provider before taking this medication.

Interaction
There have been no significant interactions reported. However, there is an isolated case report indicating a possible interaction with ethanol and compounds containing pyrimethamine or dapsone. Additionally, the use of betahistine with salbutamol has shown an enhanced effect when used together. It’s advisable to consult your healthcare provider about all other medications you are taking.

Contraindications
Roflumilast should not be used if there is a known hypersensitivity to Roflumilast or any of its ingredients. It is also contraindicated in patients with moderate to severe hepatic impairment.

Side Effects
Clinical studies on COPD treatment with Roflumilast have shown that about 16% of patients may experience side effects, compared to 5% with a placebo. Common side effects include diarrhea (5.9%), weight loss (3.4%), nausea (2.9%), abdominal pain (1.9%), and headache (1.7%). Most of these side effects are mild to moderate and typically resolve with continued use of the medication. A detailed breakdown of side effects based on frequency is as follows:

• Immune system: Uncommon cases of hypersensitivity reactions.
• Endocrine: Rare occurrences of gynaecomastia.
• Metabolism & Nutrition: Commonly observed weight loss and reduced appetite.
• Psychiatric: Common symptoms include insomnia, with rarer symptoms like anxiety, depression, and suicidal thoughts.
• Nervous system: Headaches are common, and tremors, vertigo, and dizziness can occur less frequently.
• Cardiac: Palpitations may occasionally occur.
• Respiratory: Rare respiratory tract infections (excluding pneumonia).
• Gastrointestinal: Common issues include diarrhea, nausea, and abdominal pain.
• Hepatobiliary: Rare elevations in liver enzymes (Gamma-GT, AST).
• Skin & Subcutaneous Tissue: Uncommon rash, rare urticaria.
• Musculoskeletal: Muscle spasms, weakness, and back pain may occur.
• General: Fatigue and malaise are reported.

Pregnancy & Lactation

• Pregnancy: Roflumilast should not be used during pregnancy due to potential risks, as animal studies have shown reproductive toxicity. It is not recommended for women of childbearing potential who are not using contraception.
• Lactation: Studies show that Roflumilast can pass into breast milk, and there is a potential risk to breastfeeding infants. It is not recommended for use during breastfeeding.

Precautions & Warnings

• Rescue therapy: Roflumilast is not intended for use as a rescue medication during acute bronchospasms.
• Weight loss: Prolonged use of Roflumilast may lead to weight loss, more frequently observed compared to placebo. Patients should regularly monitor their weight, and any significant unexplained weight loss should be addressed by discontinuing the medication.
• Special conditions: Roflumilast should not be used in patients with severe immunological conditions, serious infections, cancers (excluding basal cell carcinoma), or in those receiving long-term immunosuppressive treatment.
• Psychiatric conditions: There is a potential for psychiatric disorders, including suicidal ideation, especially during the early weeks of treatment. If any new or worsening psychiatric symptoms appear, treatment should be discontinued immediately.
• Lactose intolerance: Patients with rare hereditary conditions, such as galactose intolerance or lactase deficiency, should avoid this medication.

Overdose Effects
In clinical trials, overdoses of up to 5,000 micrograms (ten times the recommended dose) resulted in symptoms such as headache, dizziness, gastrointestinal issues, and palpitations. If an overdose occurs, supportive medical care should be provided. Since Roflumilast is highly protein-bound, haemodialysis may not be an effective method to remove it from the body.

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

Storage Conditions
Store at temperatures below 30°C. Keep away from light and moisture, and ensure the medication is kept out of the reach of children.