Aminophylline: Clinical Applications and Adverse Effects

Applications

Aminophylline, a combination of theophylline and ethylenediamine, has historically been used for asthma and COPD but has recently shown promise in pain management, particularly for renal colic and post-dural puncture headache. Studies indicate its efficacy as an adenosine antagonist, providing significant pain relief, including rapid improvement in migraine cases. Its dual role as a bronchodilator and analgesic highlights its therapeutic versatility. 

Treatment with aminophylline, as an antagonist of nonspecific adenosine receptor, increases renal filtration and urine flow and reduces the dialysis necessity. Aminophylline in cardiac surgery can reduce the frequency of acute kidney injury according to RIFLE criteria and could be used in the prevention of AKI as a safe and efficient modality in high-risk patients. Also, the use of this drug may reduce the need for inotropic medication at the time of surgery, intensive care unit stay length, and extubation time.

Gaffney et al. found that AKI could not significantly be reduced after cardiac surgery. In another study, aminophylline showed no effect to prevent acute kidney injury in children recovering from cardiac surgery performed with cardiopulmonary bypass. The association between perioperative use of aminophylline infusion and lower incidence of deterioration in renal function following cardiacsurgery in high-risk patients has been suggested by Mahaldar et al. ¹

Figure 1. Aminophylline

Adverse Effects

Iain Drummond provided 3 cases of drug toxicity that were due to aminophylline overdosage.²

These cases all have a remarkably similar presentation, but it must be noted also that they mimic closely organic reactions to such things as urinary infection or hypoglycemia and also the most common chronic organic syndromes such as multi-infarct dementia. The problem is, of course, that serum concentrations of aminophylline may be difficult to obtain, so if there is any suspicion of toxicity by aminophylline it might be best simply to give supportive treatment and observe for three or four days and delay any investigations. There are few published reports on aminophylline toxicity and no previous description of what appears to be a discrete and specific response, at least in the elderly.

Reference

1. Evaluation of the Effect of Aminophylline in Reducing the Incidence of Acute Kidney Injury After Cardiac Surgery. Anesth Pain Med. 2017 August; 7(4):e21740.

2. Aminophylline toxicity in the elderly. doi: 10.1136/bmj.285.6344.779-a

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