Rofumil 500 mcg

Description

Indications
Rofumil is primarily prescribed for the ongoing treatment of severe chronic obstructive pulmonary disease (COPD), particularly when associated with chronic bronchitis, in adult patients with a history of frequent exacerbations. It is used as an adjunct to bronchodilator therapy for better management of the condition.
Note: Always follow the guidance of a registered healthcare professional when using this medication.

Pharmacology
Roflumilast functions as a phosphodiesterase-4 (PDE-4) inhibitor. By selectively blocking the PDE4 isoenzyme, Roflumilast exerts anti-inflammatory and immunomodulatory effects within the respiratory system. Its therapeutic effects are believed to be linked to elevated levels of cyclic AMP inside cells, contributing to the management of COPD symptoms.

Dosage & Administration

• Adult dosage: The typical recommended dosage is 500 micrograms of Roflumilast once daily. It may take several weeks for patients to notice the effects of the medication. Roflumilast has been tested in clinical trials for up to a year.
• Elderly patients (65 years and older): No dose adjustment is necessary for this group.
• Renal impairment: No dosage changes are required for patients with renal issues.
• Hepatic impairment: Patients with mild hepatic impairment (classified as Child-Pugh A) have insufficient clinical data to justify a dosage adjustment. Caution is recommended in these cases. Roflumilast must not be used in patients with moderate or severe hepatic impairment (classified as Child-Pugh B or C).
• Pediatric use: The medication is not indicated for use in children or adolescents under the age of 18.
  The tablet should be taken whole with water, ideally at the same time each day. It can be consumed with or without food.
  Note: Always follow the advice of a registered healthcare professional.

Interaction
No significant interactions have been reported. However, there have been isolated cases of interaction with ethanol and compounds containing pyrimethamine with dapsone, and with betahistine potentiated by salbutamol. Concomitant use of H1 antagonists with betahistine may reduce the effectiveness of both medications.

Contraindications

• Hypersensitivity to Roflumilast or any of its ingredients.
• Moderate to severe liver impairment.

Side Effects
In clinical studies for COPD, around 16% of patients experienced adverse reactions, compared to 5% with placebo. Common side effects included diarrhea (5.9%), weight loss (3.4%), nausea (2.9%), abdominal pain (1.9%), and headache (1.7%). Most of these side effects were mild to moderate and often resolved after continued use.
Adverse reactions are categorized based on frequency:

• 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)
• Unknown (cannot be estimated from the data)

Pregnancy & Lactation

• Pregnancy: There is limited data on the use of Roflumilast during pregnancy. Animal studies have shown reproductive toxicity. Roflumilast is not recommended for use in pregnant women or those of childbearing potential who are not using contraception.
• Lactation: Roflumilast is excreted in animal milk. The potential risk to a breastfeeding infant cannot be excluded, so it should not be used during lactation.

Precautions & Warnings

• Rofumilast is not intended for use as a rescue medication for acute bronchospasms.
• Weight loss: Patients on Roflumilast may experience weight loss. This is more common in the first year of treatment. Regular monitoring of body weight is recommended, particularly in underweight patients. If unexplained or clinically significant weight loss occurs, Roflumilast should be discontinued, and weight should be monitored closely.
• Patients with severe immunological conditions or active infectious diseases should not begin or continue treatment with Roflumilast due to the lack of sufficient clinical experience.
• Psychiatric risks: Roflumilast has been associated with psychiatric issues, including insomnia, anxiety, depression, and rare instances of suicidal thoughts or behavior. Patients with a history of depression or suicidal tendencies should not use Roflumilast. If any psychiatric symptoms or changes in behavior are observed, the treatment should be discontinued.
• Persistent adverse reactions: While most side effects like diarrhea, nausea, and headache resolve over time, Roflumilast should be reevaluated if intolerable side effects persist, especially in specific populations or when combined with other medications that may increase side effects.

Overdose Effects
In studies, higher doses of Roflumilast (2,500–5,000 micrograms) led to symptoms such as headache, gastrointestinal issues, dizziness, and light-headedness. In case of overdose, supportive medical care should be administered. Hemodialysis is unlikely to be effective in removing Roflumilast due to its high protein binding, and it is uncertain whether peritoneal dialysis would be helpful.

Therapeutic Class
Roflumilast is classified under antihistamines, specifically used for anti-allergy and hypo-sensitization purposes.

Storage Conditions
Store the medication in a cool, dry place below 30°C, away from light and moisture. Keep it out of the reach of children.