Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The efficacy and safety of different regimens of intravenously administered enprofylline, an anti-asthma xanthine, were evaluated in a randomized open study, including 155 patients with acute exacerbation of obstructive lung disease. The regimen 2.5 mg/kg i.v. over 10 min was canceled after seven patients had been included, due to two cases of hypotensive/vasovagal reactions. The regimens 2.0 mg/kg/20 min and 2.5 mg/kg/20 min were significantly more effective with regard to bronchodilation than 2.0 mg/kg/10 min (PEF increase +35%, +30% and +17% respectively). Nausea and headache were the most common side effects (16-33% and 23-33% of the patients respectively on different regimens) with the lowest frequency on 2.0 mg/kg/20 min. Four additional hypotensive reactions occurred; one on each 2.0 mg/kg regimen and two on 2.5 mg/kg/20 min. The regimen 2.0 mg/kg20 min was found to be the most favourable with regard to efficacy and side effects. Enprofylline i.v. was found to be an effective bronchodilating treatment of acute airway obstruction but the frequency of side effects has to be considered.
 ...
PMID:Efficacy of enprofylline in acute airway obstruction. 201 8

Enprofylline, a recently developed xanthine derivative, is a more potent bronchodilator than theophylline. This study compares the efficacy and safety of enprofylline with theophylline for chronic obstructive airways disease (COAD) in elderly subjects. The study was of a randomized double-blind parallel design and commenced with a 1-week reference period when oral bronchodilators were withdrawn. Patients were then treated with either enprofylline or theophylline 150 mg bd for 2 weeks (period 1) followed by 300 mg bd for a further 3 weeks (period 2). Patients recorded peak expiratory flow rate (PEFR) and adverse experiences, if any, in a diary, daily. Of 111 patients recruited for the study, 85 entered active treatment (theophylline, n = 44; enprofylline, n = 41). Mean age was 72 years and mean bronchodilator reversibility was 22%. Enprofylline increased mean morning PEFR by 11% (period 1) and 19% (period 2) whereas theophylline increased PEFR by 13% and 19%, respectively. From the enprofylline group 29% were withdrawn from the study due mainly to headache and nausea/vomiting and from the theophylline group 7% were withdrawn due mainly to nausea/vomiting. Mean plasma concentrations of enprofylline were 2.0 mg l-1 and 3.4 mg l-1, and with theophylline 5.4 mg l-1 and 10.0 mg l-1 at the end of periods 1 and 2, respectively. Enprofylline and theophylline produced similar improvements in lung functions and symptoms of chronic obstructive airways disease, but enprofylline was less well tolerated than theophylline.
 ...
PMID:Comparative assessment of enprofylline and theophylline for chronic obstructive airways disease in the elderly. 221 6

Enprofylline is a novel xanthine derivative with negligible adenosine antagonizing ability. It is eliminated almost exclusively by renal clearance with a half-life of about 2 h. Three i.v. infusions of enprofylline (1 mg/kg body weight over 10 min) were given at hourly intervals to 16 patients with stable, reversible airway obstruction. The patients were pretreated at random with i.v. terbutaline (4 micrograms/kg body weight) or placebo according to a double blind cross-over design. Lung function and drug concentrations in plasma were followed. Enprofylline produced significant and concentration-dependent bronchodilation between plasma levels of 1.24 and 3.22 mg/l. The improvement in ventilatory function was significantly enhanced by terbutaline pretreatment. At the highest plasma levels of enprofylline nausea and headache were found as subjective side effects. The results suggest that enprofylline and terbutaline might best be used in a low dose combination in the treatment of bronchial asthma.
 ...
PMID:Additive bronchodilator effects of terbutaline and enprofylline in asthma. 358 66

The bronchodilating effect of two doses of peroral enprofylline was compared with placebo in 24 asthmatic patients. Enprofylline produced significantly greater bronchodilatation than placebo. A dose of 2 mg/kg b.wt. and 4 mg/kg b.wt. caused a mean maximal increase in FEV1 of 26% and 35%, respectively. The degree and the incidence of headache and nausea were estimated by means of a scoring system. Dose-related effects on both parameters were observed. Other side effects were negligible. In seven patients the mean plasma half-life of enprofylline was found to be 113 min. It is suggested that enprofylline should be studied further in patients suffering from obstructive lung disease.
 ...
PMID:Enprofylline--effects of a new bronchodilating xanthine derivative in asthmatic patients. 634 May 52

Bronchodilating effects produced by increasing intravenously administered doses of enprofylline and theophylline compared to placebo were evaluated in 20 asthmatic outpatients. Three mean plasma plateaux of enprofylline of 1.5, 2.9 and 4.0 micrograms/ml produced a mean increase in forced expiratory volume in the first second (FEV1.0) as a percentage of baseline, of 12.8%, 18.8% and 30.1%, respectively. Comparable plasma plateaux of theophylline i.e. 5.5, 10.8 and 15.2 micrograms/ml produced a mean increase of FEV1.0 in percent of basal values of 12.4%, 21.6% and 28.2%, respectively. Enprofylline at plasma concentrations above 2.9 micrograms/ml induced more headache and slightly more nausea than theophylline and placebo. Theophylline infusion produced more tremor (finger oscillation) than enprofylline and placebo. Intravenously administered enprofylline produces bronchodilation comparable to theophylline in a mean dose ratio of 3.8.
 ...
PMID:Maximally effective plasma concentrations of enprofylline and theophylline during constant infusion. 648 99

The bronchodilator effect and side-effects of a single oral dose of enprofylline were compared with the corresponding actions of a therapeutic dose of theophylline in 20 asthmatic patients, in a randomized cross-over clinical trial. Enprofylline 4 mg/kg and theophylline 8 mg/kg produced mean maximum plasma levels of 4.40 +/- 0.91 micrograms/ml and 16.5 +/- 2.58 micrograms/ml and mean maximum increases in FEV1.0 of 38.5% and 34.8%, respectively. The degree of headache and nausea was estimated by a scoring system. Enprofylline produced significantly higher scores for headache than theophylline, and both drugs produced s light nausea. No other side-effects were seen. Enprofylline seems to have bronchodilating properties comparable to those of theophylline without producing severe side-effects.
 ...
PMID:Comparison of oral enprofylline and theophylline in asthmatic patients. 648 10

Enprofylline (3-propylxanthine), a novel bronchodilating xanthine derivative that seems to lack adenosine antagonistic potency was given intravenously to eight recumbent healthy male volunteers in the doses 0.5, 1 and 1.5 mg/kg body-weight and to six of them also orally in the doses 2, 4 and 6 mg/kg. Mean enprofylline plasma levels ranged between 1.6 and 4.4 mg/1 (8.2-22.2 mumol/1) after intravenous, and between 1.9 and 5.5 mg/1 (9.8-27.9 mumol/1) after oral administration. Enprofylline was rapidly and completely absorbed and had an elimination half-life of approximately 2 hrs. About 90% of the dose given by either route was recovered as unchanged drug in the urine. A slight but significant increase in heart rate was seen at peak plasma levels after each of the highest intravenous and oral doses. At these dose levels the heart rate response to orthostatic tests was significantly increased by enprofylline. Adverse reactions were mild and short-lasting and occurred most frequently after the two highest intravenous and oral doses. Headache and nausea were noted in 5 of the 24 intravenous experiments and in 9 of the 17 times that enprofylline was given orally. In conclusion, the circulatory effects of enprofylline were small and the adverse reactions mild. Further clinical studies with enprofylline seem warranted.
 ...
PMID:Tolerance and some circulatory effects of intravenous and oral enprofylline in healthy volunteers. 663 10