Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 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.
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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a randomized double-blind parallel design and commenced with a 1-week reference period when oral bronchodilators were withdrawn.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 From the enprofylline group 29% were withdrawn from the study due mainly to headache and nausea/vomiting and from the theophylline group 7% were withdrawn due mainly to nausea/vomiting.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.
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PMID:Comparative assessment of enprofylline and theophylline for chronic obstructive airways disease in the elderly. 221 6

Fifteen asthmatic outpatients were randomly treated during two periods of 14 days each with sustained-release preparations of either enprofylline (3-propyl-xanthine) or theophylline (Theo-Dur) in a double-blind crossover study. After 4 days of treatment the mean daily doses of enprofylline and theophylline, which were 14.1 and 16.2 mg/kg/day, produced mean plasma concentrations of 4.9 and 12.7 micrograms/ml, respectively. Taking into account all the parameters used to evaluate the antiasthmatic effects, the peak expiratory flow, the number of puffs used from a beta-agonist aerosol, the asthma symptom score and the patients' preferred period, enprofylline was found to be better than theophylline. Enprofylline produced more headaches during the 1st week than theophylline did. However, during the 2nd week the score for headaches decreased to the same level as in the theophylline treatment group. Thus, enprofylline and theophylline seem to have comparable bronchodilator properties and side-effects in the long-term treatment of asthma.
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PMID:Enprofylline and theophylline slow-eroding tablets in the treatment of asthma: a comparison. 352 64

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.
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PMID:Additive bronchodilator effects of terbutaline and enprofylline in asthma. 358 66

Enprofylline, a xanthine-derivative shown experimentally to lack universal adenosine receptor antagonism, has been examined in patients with partly reversible, chronic, obstructive lung disease. Significant bronchodilation was produced by enprofylline 2 mg/kg, giving a peak plasma concentration of 3.0 +/- 0.6 microgram/ml (mean +/- SD). A dose of 2 + 4 mg/kg dilated the bronchi at least to the same extent as theophylline 9.2 +/- 0.9 mg/kg (plasma level 18.5 +/- 4.7 micrograms/ml). Neither at the low nor at the high dosage (2 +/- 4 mg/kg), giving plasma concentrations of 8.5 +/- 1.4 microgram/ml, did enprofylline produce theophylline-like CNS effects, such as restlessness and tremor, but it did exhibit some of the innocuous side effects expected with xanthine derivatives, such as epigastric discomfort and headache. The comparison with theophylline was limited because different dosage forms had to be used (solution an tablets), which for example, resulted in different absorption rates. Nevertheless, the present findings indicate enprofylline to be potent bronchodilator in patients with obstructive lung disease, suggesting that adenosine-receptor antagonism is not involved in the bronchodilator effects of xanthines.
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PMID:Effects of enprofylline, a xanthine lacking adenosine receptor antagonism, in patients with chronic obstructive lung disease. 628 96

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.
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PMID:Enprofylline--effects of a new bronchodilating xanthine derivative in asthmatic patients. 634 May 52

In 6 asthmatic patients, the possibility of obtaining a steady state plasma level of 5 mg/l of enprofylline by administration of two constant rate infusions was examined. The simulated plasma concentration curves, based on information from preassessment of individual pharmacokinetic parameters, were in good agreement with the plasma levels obtained. The side-effects and bronchodilatation produced by enprofylline were compared to those obtained with theophylline at a steady state level of 15 mg/l. Enprofylline and theophylline caused a mean maximal increase in FEV1.0 of 14% and 2.6% per mg/l in plasma, respectively. Side-effects, headache, nausea and vomiting, became pronounced in 2 patients in whom the plasma enprofylline level was about 6 mg/l. No other serious adverse reaction was seen. It is suggested that enprofylline should be further evaluated as a possible anti-asthmatic drug.
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PMID:Intravenous administration of enprofylline to asthmatic patients. 634 76

Twenty-five asthmatic outpatients were treated for 3 one-week periods with either enprofylline slowly eroding 300 mg tablets t.i.d., theophylline 300 mg tablets (Theo-Dur) t.i.d., or placebo in a double-blind, cross-over, randomized trial. Sixteen patients were able to complete 2 or 3 one-week periods. Evaluation of bronchodilating properties by home recordings of peak expiratory flow (PEF) and side effects suggested that enprofylline was an effective antiasthmatic xanthine derivative for continuous treatment, as it improved mean morning PEF significantly. Continuous treatment with the 2 xanthine derivatives resulted in mean steady state plasma levels within therapeutic range for theophylline, and 3-4 times lower mean plasma levels for enprofylline. Enprofylline induced headache in 13 of 16 patients, theophylline in 9 of 19 patients, and placebo in 2 of 18 patients. No serious side effects were seen.
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PMID:Continuous treatment of asthmatic patients with enprofylline and theophylline. 638 11

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.
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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.
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PMID:Comparison of oral enprofylline and theophylline in asthmatic patients. 648 10


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