Aminophylline Injection, USP is a sterile, nonpyrogenic solution of aminophylline in water for injection. Aminophylline (dihydrate) is approximately 79% of anhydrous theophylline by weight. Aminophylline Injection is administered by slow intravenous injection or diluted and administered by intravenous infusion. The solution contains no bacteriostat or antimicrobial agent and is intended for use only as a single-dose injection. When smaller doses are required the unused portion should be discarded. Aminophylline is a 2:1 complex of theophylline and ethylenediamine. Theophylline is structurally classified as a methylxanthine. Aminophylline occurs as a white or slightly yellowish granule or powder, with a slight ammoniacal odor. Aminophylline has the chemical name 1H-Purine-2, 6-dione, 3,7-dihydro-1,3-dimethyl-, compound with 1,2-ethanediamine (2:1).
Intravenous theophylline is indicated as an adjunct to inhaled beta-2 selective agonists and systemically administered corticosteroids for the treatment of acute exacerbations of the symptoms and reversible airflow obstruction associated with asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.
Published Studies Related to Aminophylline
Attenuation of the side effect profile of regadenoson: a randomized double-blind
placebo-controlled study with aminophylline in patients undergoing myocardial
perfusion imaging and have severe chronic kidney disease--the ASSUAGE-CKD trial. 
A subgroup analysis of the ASSUAGE trial suggested that the standardized
intravenous aminophylline administration following regadenoson-stress leads to
substantial attenuation of regadenoson adverse-effects in patients with severe
chronic kidney disease (CKD)... In conclusion, the routine standardized
administration of intravenous aminophylline in patients with severe CKD
substantially reduces the frequency and severity of the adverse-effects
associated with regadenoson-stress without changing the ischemic burden.
Attenuation of the side effect profile of regadenoson: a randomized
double-blinded placebo-controlled study with aminophylline in patients undergoing
myocardial perfusion imaging. "The ASSUAGE trial". 
other adverse effects associated with regadenoson... CONCLUSIONS: This trial supports the routine administration of IV-aminophylline
Effects of aminophylline on cognitive recovery after sevoflurane anesthesia. 
clinical recovery after sevoflurane anesthesia... CONCLUSION: The administration of escalating doses of aminophylline accelerates
Efficacy of N-acetylcysteine and aminophylline in preventing contrast-induced nephropathy. [2010.03]
CONCLUSIONS: These results suggest that both prophylactic NAC and aminophylline administration are effective in preventing CIN, but not with hydration alone. It appears that the two compounds work in different ways against CIN. Copyright 2009 Japanese College of Cardiology. Published by Elsevier Ltd. All rights reserved.
Pharmacokinetics of aminophylline delivered to the small intestine and colon using remote controlled capsules. [2010.02.05]
BACKGROUND: A patented remote controlled capsule (RCC) has recently been developed to provide noninvasive drug delivery to selected sites in the human gut that allows assessment of regional gastrointestinal (GI) drug absorption under a normal physiological environment. The objective of this study was to investigate the rate and extent of aminophylline absorption after site-specific delivery of the drug in the GI tract using RCC and a magnetic marker monitoring (MMM) technique... CONCLUSIONS: The proprietary of the RCC and MMM technique offer the opportunity to obtain data on the intestinal absorption of a drug in humans under noninvasive conditions. Aminophylline is rapidly and efficiently absorbed from the small bowel. While colonic absorption was limited by the poor water condition although effective absorption was observed from the ascending colon. This provides an opportunity for rational development of modified-release formulations as well as alternative dosage forms.
Clinical Trials Related to Aminophylline
The Safety Evaluation of Aminophylline and Ambrisentan When Administered Orally Alone and in Combination to Healthy Volunteers [Completed]
This is a Phase I, three period, two sequence, open-label, randomized, crossover study, with
the primary objective of testing the safety and tolerability of combined oral doses of
aminophylline and ambrisentan in healthy human subjects. The secondary objective is to
assess the pharmacokinetic profiles of theophylline (aminophylline) and ambrisentan when
administered alone or in combination. It is hypothesized that the combination of these drugs
is generally safe, and that no drug interaction can be observed.
Attenuation of the Side Effect Profile of Regadenoson: Study With Aminophylline in Patients With Severe Kidney Disease Undergoing Myocardial Perfusion Imaging [Completed]
The routine administration of 75 mg of intravenous aminophylline in patients with severe
chronic kidney disease undergoing a nuclear stress test with regadenoson (Lexiscan®) can
reduce or eliminate the incidence of diarrhea and other side effects related to regadenoson.
Aminophylline and Cognitive Function After Sevoflurane Anaesthesia [Completed]
Early postoperative recovery of neurologic and cognitive functions is especially
advantageous after fast-tracking ambulatory procedures to hasten home discharge after
surgery. 1 It is well known that volatile anaesthetic agents may generate adverse
postoperative cognitive effects and even traces of it may affect task performance in healthy
volunteers. 2Hence, rapid elimination of the volatile anaesthetics may help reduce
postoperative confusion and cognitive impairment in surgical patients by facilitating a
faster recovery from general anaesthesia. 3 Sevoflurane has been advocated for the routine
anesthesia for ambulatory surgery patients. It activates adenosine A1 receptors in primary
rat hippocampal cultures through the liberation of adenosine secondary to the interaction of
with adenosine transport or key enzymes in adenosine metabolism. 4 However; sevoflurane
anaesthesia is associated with slower emergence and delayed early postoperative cognitive
recovery than desflurane5 and xenon2 anaesthesia.
Aminophylline, which is a hydrophilic cyclic adenosine mono-phosphate (cAMP) dependent
phosphodiesterase inhibitor has been used for long time to antagonize the sedative effects
of morphine, diazepam, and barbiturates. 6-7Aminophylline in doses of 2-5 mg/kg shortens the
recovery from sevoflurane anaesthesia and improves bispectral index scores (BIS) with
concurrent increases in heart rate which might have a detrimental effect in patients with
ischaemic heart disease. 8-11However, the use of smaller doses of 2-3 mg/kg is associated
with less increases in heart rate. 10-11 The use of 1 mg/kg of Doxapram is comparable to 2
mg/kg of aminophylline in improvement of early recovery from sevoflurane anaesthesia
secondary to its central nervous system stimulating effect rather than increased ventilatory
elimination of sevoflurane. 11 Currently, there is no available published studies have
investigated the effects of either theophylline or doxapram on early postoperative cognitive
recovery after balanced anaesthesia with sevoflurane.
We hypothesized that the use of small doses of aminophylline [2-3 mg/kg] may be comparable
to larger doses in improvement of the early postoperative cognitive recovery from
sevoflurane anaesthesia with associated non-significant increases in heart rate.
The present study investigated the effects of 1 mg/kg of doxapram, and 2, 3, 4, and 5 mg/kg
of aminophylline on the early postoperative cognitive recovery using the Short Orientation
Memory Concentration Test (SOMCT), response entropy (RE) state entropy (SE), difference
between RE and SE (RE-SE), end-tidal sevoflurane concentration, haemodynamics, the times to
eyes opening and to extubation and degree of sedation after sevoflurane anaesthesia in
patients undergoing ambulatory surgery.
A Study to Test the Safety of Combined Dosing With Aminophylline and Ambrisentan in Exercising Healthy Human Volunteers at Simulated High Altitude [Completed]
Acute exposure of the unacclimatized human body to high altitude leads to health
complications, such as loss of exercise performance capacity and fatigue. The investigators
have found that the combination of the xanthine drug theophylline and the endothelin
receptor antagonist ambrisentan improves the exercise performance capacity of rats under
simulated high altitude. In young, healthy human volunteers, this combination of drugs has
not increase toxicity over the single compounds under sea-level conditions. The aim of this
study is to test whether the combination of theophylline, supplied as its more soluble
formulation aminophylline, and ambrisentan, are also safe to take under simulated high
altitude of 4,267 meters, under both resting and exercising conditions. The study also aims
to test whether this drug combination improves exercise capacity in humans. In this study,
human subjects will be randomized to one of four treatment sequences and receive the same
study drug(s) throughout all procedures. The study consists of an initial exercise test,
followed by two cycles of drug testing at simulated high altitude: Cycle 1 - resting
subjects receiving study drug at simulated altitude and continually monitored for safety
with pharmacodynamic and pharmacokinetic assessments; and Cycle 2, the same as Cycle 1, with
the addition of exercise testing. It is hypothesized that the combination of aminophylline
and ambrisentan is not only safe under simulated high altitude, but also improves exercise
performance capacity, in comparison with placebo.
Perioperative Aminophylline to Improve Early Kidney Function After a Kidney Transplant [Recruiting]
The aim of this study is to evaluate whether peri-transplant administration of a drug named
aminophylline to children undergoing a kidney transplant from deceased donors improves early
graft function and also projects on long term graft function.
Reports of Suspected Aminophylline Side Effects
Confusional State (2),
Respiratory Depression (2),
Multi-Organ Failure (2),
Streptococcal Sepsis (2),
Metabolic Acidosis (2),
Tachyarrhythmia (2), more >>
Page last updated: 2014-11-30