Oxtriphylline; Uses, Dosage, Side Effects, Drug Interactions

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Oxtriphylline is the choline salt of theophylline with an anti-asthmatic property. Oxtriphylline appears to inhibit phosphodiesterase and prostaglandin production, regulates calcium flux and intracellular calcium distribution, and antagonizes adenosine. Physiologically, this agent causes relaxation of the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the cardiac muscle, as well as induces diuresis and gastric acid secretion. It may also suppress inflammation and improve contractility of the diaphragm.

Theophylline also is known as oxtriphylline, is a cough medicine derived from xanthine that acts as a bronchodilator to open up airways in the lung. Chemically, it is a salt of choline and theophylline. It classifies as an expectorant. Oxtriphylline is the choline salt form of theophylline. Once in the body, theophylline is released and acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Its main physiological response is to dilate the bronchioles. As such, oxtriphylline is indicated mainly for asthma, bronchospasm, and COPD (i.e. all the same indications as for the other theophyllines). It is marketed under the name Choledyl SA, and several forms of oxtriphylline have been discontinued. In the US, oxtriphylline is no longer available.

Mechanism of action of Oxtriphylline

Oxtriphylline is a choline salt of theophylline. After ingestion, theophylline is released from oxtriphylline, and theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, an allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine-mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.

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Indications of Oxtriphylline

Contra-Indications of Oxtriphylline

Dosage of Oxtriphylline

Strengths: 200 mg ; 400 mg ; 600 mg

Asthma – Maintenance

  • 4.7 mg/kg orally every 8 hours.

Pediatric Asthma – Maintenance

  • Child 1-9 years: 6.2 mg/kg orally every 6 hours.
  • Child 9-16 years: 4.7 mg/kg orally every 6 hours.

Side Effects of Oxtriphylline

The most common

 Common

Rare/Less common

  • Confusion
  • Fever or a sore throat
  • Rash
  • Slowed breathing or breathing difficulties
  • Sores in the mouth
  • Broken blood vessels under the skin
  • Easy bruising or bleeding
  • Swelling of the eyes, lips, or cheeks
  • Blistering or peeling of the skin
  • Restless muscle movements in the eyes, tongue, jaw, or neck

Drug Interactions of Oxtriphylline

Oxtriphylline may interact with following drugs, supplements & may change the efficacy of drugs

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Pregnancy & Lactation of Oxtriphylline

 FDA Pregnancy Category C

Pregnancy

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.

Lactation

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

References

Voriconazole

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