Xanthine derivatives

• Xanthine derivative overview

  works by inhibiting phosphodiesterase which increases cAMP which leads to smooth muscle relaxation
• Xanthine derivative examples

  Methylxanthines: theophylline, aminophylline, caffeine
• Xanthine action

  inhibits phosphodiesterase which in turn increases cAMP which results in smooth muscle relaxation

  theophylline and caffeine have effects on the CNS as stimulants

  theophylline stimulates myocardium and increases contractility and heart rate

  increases gastric acid secretion

  stimulate skeletal muscle leading to tremors

  can also lead to increased sodium and chloride excretion which also leads to diuresis
• Caution and contraindication to xanthines

  hypersensitivity, PUD, seizures are contraindications

  caution in HTN, stroke, arrhythmias

  too much can lead to toxicity
• Adverse reaction of xanthines

  uncommon but may have CNS stimulation, GERD, cardiovascular stimulation, n/v
• Theophylline use

  not generally recommended unless no other option works