Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0040822 (tremor)
 18,428 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

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.
 ...
PMID:Effects of enprofylline, a xanthine lacking adenosine receptor antagonism, in patients with chronic obstructive lung disease. 628 96

Enprofylline is a potent bronchodilating xanthine derivative that has been shown to have little or no ability to antagonize adenosine in a variety of cell types. In eight patients with chronic obstructive lung disease, a single dose of enprofylline (3.5 mg/kg) was given orally. A double blind, randomized, crossover comparison was made with oral theophylline (9.5 mg/kg) which is a potent and general adenosine receptor antagonist. Forced expiratory volume (FEV1), vital capacity, tremor of hands, heart rate, and blood pressure were followed for 6 h. Plasma concentrations of both drugs were monitored. At doses producing significant bronchodilation, theophylline caused a significant increase in tremor of hands whereas enprofylline did not. There were no significant changes in heart rate or blood pressure after either drug. It is suggested that the lack of tremorogenic effect of enprofylline is related to its lack of CNS-stimulating behavioural effects and, hence, may reflect its low tendency to antagonize neuro-depressant actions of adenosine. The adenosine-blocking mechanism may not be important for the bronchodilating effects of xanthines.
 ...
PMID:A novel bronchodilator xanthine apparently without adenosine receptor antagonism and tremorogenic effect. 630 42

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

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. Enprofylline was given i.v. to 8 patients with partially reversible chronic airway obstruction in a double blind cross-over trials with placebo. Three infusions of drug (1 mg/kg in 10 min) were given at hourly intervals. Spirometry (FEV1x0 and FVC) and drug analyses showed that enprofylline produced significant and concentration-dependent bronchodilation between plasma levels of 1 and 4 mg/L. The maximum effect obtained was similar to that produced by 5 doses of terbutaline aerosol. Heart rate was significantly increased by enprofylline. No change in tremor of hand and no subjective side effects were recorded. It is concluded that enprofylline given i.v. is well tolerated and produces marked and dose-dependent bronchodilation.
 ...
PMID:Intravenous enprofylline in asthma patients. 670 55