Aminophylline
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| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a601015 |
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| Routes of administration |
By mouth, IV |
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| Pharmacokinetic data | |
| Protein binding | 60% |
| Biological half-life | 7–9 hours |
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| ECHA InfoCard | 100.005.696 |
| Chemical and physical data | |
| Formula | C16H24N10O4 |
| Molar mass | 420.427 g/mol |
| 3D model (Jmol) | |
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Aminophylline is a compound of the bronchodilator theophylline with ethylenediamine in 2:1 ratio. The ethylenediamine improves solubility, and the aminophylline is usually found as a dihydrate.
Aminophylline is less potent and shorter-acting than theophylline. Its most common use is in the treatment of airway obstruction from asthma or COPD. It is used off-label as a reversal agent during nuclear stress testing. Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor.
Aminophylline is used to reverse regadenoson, dipyridamole or adenosine based infusions during nuclear cardiology stress testing.
Aminophylline has shown some promise as a bodyfat reducer when used as a topical cream. Aminophylline is also a treatment option for anaphylactic shock.
While it has been suggested for use in cardiac arrest evidence does not support a benefit.
Aminophylline can lead to theophylline toxicity. Aminophylline has been found to decrease the sedative effects of propofol and decrease topiramate antiseizure action.
It is more soluble in water than theophylline. White or slightly yellowish granules or powder, having a slight ammoniacal odor and a bitter taste. Upon exposure to air, it gradually loses ethylenediamine and absorbs carbon dioxide with the liberation of free theophylline. Its solutions are alkaline. 1 g dissolves in 25 mL of water to give a clear solution; 1 g dissolved in 5 mL of water crystallizes upon standing, but redissolves when a small amount of ethylenediamine is added. Insoluble in alcohol and in ether.
Like other methylated xanthine derivatives, aminophylline is both a
Aminophylline causes bronchodilation, diuresis†, central nervous system and cardiac stimulation, and gastric acid secretion by blocking phosphodiesterase which increases tissue concentrations of cyclic adenosine monophosphate (cAMP) which in turn promotes catecholamine stimulation of lipolysis, glycogenolysis, and gluconeogenesis, and induces release of epinephrine from adrenal medulla cells.
†Note that diuresis is caused by an increase in cAMP which acts in the CNS to inhibit the release of antidiuretic hormone (arginine-vasopressin).
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Wikipedia