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Doxofylline, a derivative of methylxanthine and structurally related to theophylline, is classified as a bronchodilator. It is used to treat and prevent chronic obstructive pulmonary disease (COPD) and asthma. The drug was first approved in Italy in 1988, and in February 2014, it was granted orphan drug designation by the FDA for the treatment of bronchiectasis.
BRAND NAMES:
D-Fyal – It is an oral liquid containing the main active ingredient doxofylline 100mg/5ml.
Doxfree – Doxfree is available as a tablet, doxofylline is the main active ingredient with a strength of 400mg.
Doxobron – Doxofylline is the main active ingredient present in doxobron available as oral tablets with strength 400mg.
MECHANISM OF ACTION:
Doxofylline exerts its effects primarily by inhibiting phosphodiesterase enzymes, particularly the PDE4 isoenzyme. This inhibition prevents the breakdown of cyclic adenosine monophosphate (cAMP) within cells. cAMP plays a key role as a secondary messenger in numerous cellular processes, including the regulation of inflammation and the relaxation of smooth muscle. By increasing intracellular cAMP levels, doxofylline promotes bronchodilation, helping to relieve airway obstruction in patients with asthma or COPD.
PHARMACOKINETICS:
Absorption: Doxofylline is well absorbed following oral administration, with peak plasma concentrations typically reached within 2 to 3 hours.
Distribution: Approximately 40% is mainly bound to albumin. The volume of distribution is about 0.5 – 0.7L/Kg.
Metabolism: Doxofylline is mainly metabolized in the liver through cytochrome P450 enzymes, particularly CYP1A2, although to a lesser extent than theophylline.
Excretion: Renal excretion is about 50 – 60% of the drug is excreted through renal excretion. And unchanged drug in urine is less than 4%.
PHARMACODYNAMICS:
Doxofylline is a novel bronchodilator xanthine that differs from theophylline in the presence of a dioxalane group in position. Doxofylline appears to have decreased affinities toward adenosine A1 and A2 receptors which may account for the better safety profile of the drug.
DOSAGE AND ADMINISTRATION:
Doxofylline is available as tablets, syrups, powders, and injections. Tablets, syrup, and injections are recommended for adults while the sachet can be used for children below 6 years.
Tablets available in strengths 200mg, 400mg
Syrups available mostly 100mg/5ml
Intravenous Injections dose: 100 – 300mg diluted in 100ml normal saline, infused over 20 – 30 minutes.
The dose administered depends on the patient's tolerance, body weight, and the severity of the disease.
For adults,
The recommended dose oral dose is 400mg twice daily and the maximum recommended dose should not exceed 1200mgday.
For children, the dose should be 6mg/Kg twice daily or 100 -200mg twice daily.
DRUG INTERACTIONS:
Some medications should be avoided while taking doxofylline as they can lead to adverse effects. Before taking doxofylline it is a must to discuss with the doctor if the patient is going through any other medications. Below are a few medications that should be avoided while taking doxofylline.
Antibiotics – Erythromycin, Lincomycin, Clindamycin
Antigout Medications - Allopurinol
Stomach acid reducers – Cimetidine
Antihypertensives – Propranol
Anticonsulvants – Phenytoin
CONTRAINDICATIONS:
Doxofylline is contraindicated in individuals with known hypersensitivity to the drug, as well as in those experiencing acute myocardial infarction or hypotension.
ADVERSE EFFECTS:
Headache
Palpitations
Mild tachycardia
Headache
Nausea
Vomiting
Abdominal pain
Insomnia
Irritability
TOXICITY:
Overdose can cause some toxic effects like
Severe agitation or tremors
Cardiac arrhythmias
Convulsions
Hypotension
Nausea
