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Doxofylline – Indication, Dosage, Adverse Effect, Drug Interaction

Available Doxofylline in Bangladesh

Fixolin – Beximco (200mg, 400mg)

Doxoven – Beacon (200mg, 400mg) + Syrup

Flindof – Square (200mg, 400mg)

Docopa – Aristopharma (200mg, 400mg) + Syrup

Doxorin – Opsonin (200mg, 400mg)

Dophylin – Acme (200mg, 400mg)

What is Doxofylline

Doxofylline is a new generation xanthine derivative which has a dioxolane group at the N-7 position of its chemical structure. Doxofylline inhibits phosphodiesterase activities. Moreover, Doxofylline appears to have a less affinity towards adenosine A1 and A2 receptors which is account for the better safety profile of the drug. Doxofylline also inhibits platelet activating factor and the generation of leukotrienes.

 

Pharmacology of Doxofylline

Doxofylline is a new generation xanthine derivative which has a dioxolane group at N-7 position of its chemical structure. Doxofylline inhibits phosphodiesterase activities. Moreover, Doxofylline appears to have a less affinity towards adenosine A1 and A2 receptors which is account for the better safety profile of the drug. Doxofylline also inhibits platelet-activating factor and the generation of leukotrienes. Doxofylline also has antitussive and bronchodilator effects and acts as a phosphodiesterase inhibitor.

Indication of Doxofylline

  • Doxofylline is mostly administered for maintenance treatment in subjects experiencing
  • COPD (Chronic Obstructive Pulmonary Disease) and bronchial asthma.
  • Doxofylline is not designed for use as an emergency treatment during an asthma attack.

Doxofylline offers

  • In COPD, effectively reduces exacerbations
  • In asthma, provides better symptom control
  • No effect on sleep pattern and awakenings
  • Safe for cardiac patients
  • Lesser effect on gastric secretion
  • Better patient compliance

Dosage and administration of Doxofylline

Adult dose: 400 mg (1 tablet) daily in the evening. However, in certain cases, 400 mg twice daily is recommended on the basis of the clinical response. Doses as high as 1200 mg/day (400 mg 3 times daily) may also be prescribed. In elderly patients with concomitant cardiovascular, hepatic and renal diseases recommended dosage should be 200 mg twice daily.

Children (above 6 years of age): The recommended dosage of Doxofylline is 6 mg/kg twice daily. The dose may be increased up to 18 mg/kg daily on the basis of clinical response.

Dosage Type: 6 mg/kg b.i.d

Weight of the Child: 10 kg > Dosage: 3 ml
Weight of the Child: 15 kg > Dosage: 4.5 ml
Weight of the Child: 20 kg > Dosage: 6 ml
Weight of the Child: 25 kg > Dosage: 7.5 ml
Weight of the Child: 30 kg > Dosage: 9 ml
Weight of the Child: 35 kg > Dosage: 10.5 ml
Weight of the Child: 40 kg > Dosage: 12 ml

Dosage Type: Total Daily Dose

Weight of the Child: 10 kg > Dosage: 6 ml
Weight of the Child: 15 kg > Dosage: 9 ml
Weight of the Child: 20 kg > Dosage: 12 ml
Weight of the Child: 25 kg > Dosage: 15 ml
Weight of the Child: 30 kg > Dosage: 18 ml
Weight of the Child: 35 kg > Dosage: 21 ml
Weight of the Child: 40 kg > Dosage: 24 ml

Doxofylline may be taken with or without food.

Adverse effects of Doxofylline

After xanthine administration, nausea, vomiting, epigastric pain, cephalalgia, irritability, insomnia, tachycardia, and occasionally hyperglycemia and albuminuria, may occur. If a potential oral overdose is established, the patient may present with severe arrhythmias and seizure; these symptoms could be the first sign of intoxication. Adverse reactions may cause the withdrawal of treatment; a lower dose rechallenge may start only after the advice of a physician.

Contraindications of Doxofylline

Individuals who have shown hypersensitivity to Doxofylline.
Patients with acute myocardial infarction and hypotension.

In Lactation use of Doxofylline

Doxofylline is contraindicated in nursing mothers.

In Pregnancy use of Doxofylline

Animal reproduction studies indicate that doxofylline does not cause fatal harm when administered to pregnant animals or can affect reproduction capacity.

However, since there is limited experience in humans during pregnancy, xanthines should be given to a pregnant woman only if clearly needed.

Special Precaution of Doxofylline

The t ½ of xanthine derivatives is influenced by a number of known variables. It may be prolonged in patients with liver disease, in patients with congestive heart failure (CHF), in those affected with chronic obstructive lung disease or concomitant infections and in those patients taking certain other drugs (erythromycin, troleandomycin, lincomycin and other antibiotics of the same group, allopurinol, cimetidine, propranolol and anti-flu vaccine). In these cases, a lower dose of doxofylline may be needed. Phenytoin, other anticonvulsants, and smoking may cause an increase in clearance with a shorter mean t ½.

In these cases, higher doses of doxofylline may be needed. Use with caution in patients with hypoxemia, hyperthyroidism, liver disease, renal disease, in those with a history of peptic ulcer and in elderly. Frequently, patients with CHF have markedly prolonged drug serum levels following discontinuation of doxofylline.

Drug Interactions of Doxofylline

Doxofylline should not be administered together with other xanthine derivatives, including beverages and foods containing caffeine. Toxic synergism with ephedrine has been documented for xanthines. Concomitant therapy with erythromycin, troleandomycin, lincomycin, clindamycin, allopurinol, cimetidine, propranolol, and the anti-flu vaccine may decrease the hepatic clearance of xanthines causing an increase in blood levels.

Overdosages of Doxofylline

Although no major arrhythmia have been documented with Doxofylline tablets the occurrence of major cardiac rhythm disturbances cannot be excluded in case of overdosage of xanthine compounds. If a potential oral overdose is established the patient may present with seizures; these symptoms could be the first sign of intoxication. Adverse reactions may cause the withdrawal from treatment. A lower dose re-challenge may start only after the advice of the physician. There is no specific antidote. It is suggested that the management principle should be instituted according to a symptomatic relief of cardiocirculatory shock. Doxofylline tablets do not cause any risk of tolerance or addiction.

About Dr. Toufiq Hassan

I am Dr. Toufiq Hassan Shawon, currently working as a medical officer at Trisal Upazilla Health Complex, Mymensingh. I have passed MBBS from Rajshahi Medical College in 2013 January, Batch - 49. My school was B.A.F. Shaheen College, Tejgaon, Dhaka, SSC-2005 and College was Notre Dame College, HSC-2007.

3 comments

  1. Thanks for sharing your thoughts oon doxofylline. Regards
    sekolah tinggi pariwisata ambarukmo

  2. Great article, just what I wanted to find.

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