Doxofylline; Uses, Dosage, Side effects, Drug Interactions

Doxofylline
If this article seems to be helpful, please rate/review us & share to others









User Review


5
(4 votes)


Doxofylline is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has shown similar efficacy to theophylline but with significantly fewer side effects in animal and human studies. Unlike other xanthines, doxofylline lacks any significant affinity for adenosine A1 or A2 receptors and does not produce stimulant effects. Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline. Unlike theophylline, doxofylline does not affect calcium influx and does not antagonize the actions of calcium channel blockers which could explain reduced cardiac adverse reactions associated with the drug . The anti-asthmatic effects of doxophylline are mediated by other mechanisms, primarily through inhibiting the activities of the phosphodiesterase (PDE) enzyme.

Unlike other xanthines, doxofylline lacks any significant affinity for adenosine A1 or A2 receptors and does not produce stimulant effects. Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline  Unlike theophylline, doxofylline does not affect calcium influx and does not antagonize the actions of calcium channel blockers which could explain reduced cardiac adverse reactions associated with the drug.

Mechanism of action of doxofylline

The main mechanism of action of doxofylline is unclear. One of the mechanisms of action of is thought to arise from the inhibition of phosphodiesterase activity thus increasing the levels of cAMP and promoting smooth muscle relaxation.

The interaction of doxofylline with beta-2 adrenoceptors was demonstrated by a study using nonlinear chromatography, frontal analysis and molecular docking . Serine 169 and serine 173 residues in the receptor are thought to be critical binding sites for doxofylline where hydrogen bonds are formed . Via mediating the actions of beta-2 adrenoceptors, doxofylline induces blood vessel relaxation and airway smooth muscle relaxation.

You Can Also Like   Itraconazole; Uses, Dosage, Side Effects, Interactions, Pragnancy

There is also evidence that doxofylline may exert anti-inflammatory actions by reducing the pleurisy induced by the inflammatory mediator platelet activating factor (PAF) according to a rat study . It is suggested that doxofylline may play an important role in attenuating leukocyte diapedesis, supported by mouse preclinical studies where doxofylline administration was associated with inhibited leukocyte migration across vascular endothelial cells in vivo and in vitro .Unlike theophylline, doxofylline does not inhibit tumor necrosis factor-induced interleukin (IL)-8 secretion in ASM cells

Indications of doxofylline

It has antitussive and bronchodilator effects, and acts as a phosphodiesterase inhibitor.

Contraindications of doxofylline

Hypersensitivity to Doxofylline is a contraindication. In addition, Doxofylline should not be used if you have the following conditions:

Dosages 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
You Can Also Like   Antihistamines; Latest Classification of Antihistamine

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.

Side Effects of doxofylline

The most common

Common

Less common

Drug Interactions of doxofylline

Doxofylline may interact with following drugs,suppliment & may change the efficasy of drugs

You Can Also Like   Narcotics; Types, Indications/ Uses, Side Effects

Pregnancy & Lactation of doxofylline

FDA Pregnancy Category B

Pregnancy

When phenytoin is taken during pregnancy, it may cause harm to the developing baby. This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

This medication passes into breast milk. If you are a breast-feeding mother and are taking phenytoin, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding

References 

 

Print Friendly, PDF & Email

Sharing to Spread to the World

14 thoughts on “Doxofylline; Uses, Dosage, Side effects, Drug Interactions”

Leave a Reply

Your email address will not be published.