Aminophylline

Aminophylline(Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.

Using pharmacokinetic modelling to improve prescribing practices of intravenous aminophylline in childhood asthma exacerbations.[Pubmed:28108402]

Pulm Pharmacol Ther. 2017 Apr;43:6-11.

OBJECTIVE: To evaluate physiologically based pharmacokinetic modelling (PBPK) software in paediatric asthma patients using intravenous Aminophylline. METHODS: Prospective clinical audit of children receiving iv Aminophylline (July 2014 to June 2016), and in-silico modelling using Simcyp software. RESULTS: Thirty-eight admissions (25 children) were included. Children with Aminophylline levels >/=10 mg/l had equivalent clinical outcomes compared to those <10 mg/L, and adverse effects occurred in 57%. Therapeutic drug monitoring (TDM) data correlated well with PBPK model. PBPK modelling of a 5 mg/kg iv loading dose ( 20 mg/L. For an Aminophylline infusion (0-12 y) of 1.0 mg/kg/h, the mean steady state infusion concentration was 16.4 mg/L, (5th-95th centiles 5.3-32 mg/L), with 26.8% having a serum concentration >20 mg/L. For 12-18yr receiving 0.5 mg/kg/h infusion, the mean steady state infusion concentration was 9.37 mg/L (5th-95th centiles 3.4-18 mg/L), with 59.8% having a serum concentration <10 mg/L. CONCLUSION: PBPK software modelling correlates well with clinical data. Current Aminophylline iv loading dosage recommendations achieve levels <10 mg/l in 70% of children. Routine TDM may need altering as low risk of toxicity (>20 mg/l).

Successful Reversal of Bradycardia and Dyspnea With Aminophylline After Ticagrelor Load.[Pubmed:27920235]

J Pharm Pract. 2018 Feb;31(1):112-114.

A 69-year-old male underwent elective percutaneous coronary intervention requiring placement of a drug-eluting stent to the first obtuse marginal artery. Four hours following the administration of a ticagrelor loading dose, he developed dyspnea and sinus pauses. Aminophylline was administered and resulted in immediate and sustained symptom resolution. Ticagrelor has been associated with dyspnea and bradyarrhythmias, both attributed to increased adenosine exposure. Ticagrelor inhibits reuptake of intracellular adenosine. Adenosine antagonists Aminophylline and theophylline have been utilized to reverse the effects of adenosine and may relieve adenosine-mediated adverse effects induced by ticagrelor therapy. Aminophylline may be considered for reversal of dyspnea and bradyarrhythmia associated with ticagrelor therapy through alterations in adenosine exposure.

Aminophylline suppresses stress-induced visceral hypersensitivity and defecation in irritable bowel syndrome.[Pubmed:28054654]

Sci Rep. 2017 Jan 5;7:40214.

Pharmacological therapy for irritable bowel syndrome (IBS) has not been established. In order to find candidate drugs for IBS with diarrhea (IBS-D), we screened a compound library of drugs clinically used for their ability to prevent stress-induced defecation and visceral hypersensitivity in rats. We selected the bronchodilator Aminophylline from this library. Using a specific inhibitor for each subtype of adenosine receptors (ARs) and phosphodiesterases (PDEs), we found that both A2BARs and PDE4 are probably mediated the inhibitory effect of Aminophylline on wrap restraint stress (WRS)-induced defecation. Aminophylline suppressed maternal separation- and acetic acid administration-induced visceral hypersensitivity to colorectal distension (CRD), which was mediated by both A2AARs and A2BARs. We propose that Aminophylline is a candidate drug for IBS-D because of its efficacy in both of stress-induced defecation and visceral hypersensitivity, as we observed here, and because it is clinically safe.

Aminophylline Effect on Renal Ischemia-Reperfusion Injury in Mice.[Pubmed:28219599]

Transplant Proc. 2017 Mar;49(2):358-365.

BACKGROUND: Aminophylline increases the intracellular concentration of cAMP and exerts an anti-inflammatory effect. The aim of this study was to investigate the effect of Aminophylline on renal ischemia-reperfusion (I/R) injury in mice. METHODS: Thirty C57BL/6 mice were divided into 3 groups. In the sham group (group S, n = 10), only right nephrectomy was performed. In the control group (group C, n = 10), after right nephrectomy, the mice were subjected to 30 minutes of left renal ischemia. In the Aminophylline group (group A, n = 10), an intraperitoneal injection of Aminophylline (5 mg/kg) was performed before renal ischemia. Twenty-four hours after reperfusion, the mice were euthanized, and plasma and kidney samples were obtained to analyze the serum creatinine, renal histology, and expression levels of nuclear factor-kappa B (NF-kB) and pro-inflammatory cytokines. RESULTS: The serum creatinine concentration in group C was markedly elevated at 24 hours after reperfusion. Aminophylline treatment significantly reduced serum creatinine, compared with group C. Aminophylline also reduced the histological evidence of renal damage. The expression levels of NF-kB, tumor necrosis factor-alpha (TNF-alpha), monocyte chemoattractant protein-1 (MCP-1), macrophage inflammatory protein-2 (MIP-2), and intercellular adhesion molecule-1 (ICAM-1) mRNA were significantly increased in group C (P < .001). Group A showed lower expression of NF-kB, TNF-alpha, MCP-1, MIP-2, and ICAM-1 mRNA than group C (P < .01). CONCLUSIONS: Aminophylline treatment improved the renal function and indexes of renal inflammation, which suggests that it provided reno-protection against renal I/R injury.

Aminophylline is a competitive nonselective phosphodiesterase inhibitor that is used to treat airway obstruction from asthma or COPD.

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