Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.4.1 (phosphodiesterase)
 18,767 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

MDL 17.043, a nonglycoside, noncatecholamine imidazolone derivative with phosphodiesterase inhibiting activity, has been shown to possess both positive inotropic and vasodilator properties. In the present study, the electrophysiological effects of intravenous MDL 17.043 were assessed in 10 patients undergoing programmed right atrial stimulation for diagnostic purposes. MDL 17.043 was administered as a single intravenous bolus injection of 1.5 mg/kg body weight over 4 min followed by an intravenous infusion of 0.75 mg/kg body weight over 20 min. With the dosage schedule used, the MDL 17.043 plasma levels achieved were similar to those previously reported to be associated with significant hemodynamic improvement of congestive heart failure. Electrophysiological measurements were performed before and during MDL 17.043 administration. MDL 17.043 consistently shortened basic sinus cycle length, sinus node recovery time and sinuatrial conduction time and decreased Wenckebach cycle length, atrioventricular and atrial refractoriness leading to positive chronotropic and dromotropic effects.
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PMID:Electrophysiological effects of intravenous MDL 17.043. 294 83

Whether phosphodiesterase inhibitors increase the heart rate in patients with bradyarrhythmias is not known. We attempted to determine whether the oral phosphodiesterase inhibitor cilostazol exhibits beneficial chronotropic effects in patients with symptomatic bradyarrhythmias. Twenty patients comprising eight with bradycardic atrial fibrillation, eight with sick sinus syndrome, and four with Wenckebach-type atrioventricular block, whose 24-h total heart-beat count was < or =70,000 beats and whose maximal RR interval was > or =2.5 s, were enrolled. Holter recordings (24-h) were made before and 2 weeks after oral daily administration of 200 mg of cilostazol. Cilostazol increased the 24-h total heart-beat count from 77,429 +/- 11,168 to 107,981 +/- 13,536 (95% confidence interval, 24,605-36,497; p < 0.0001), the minimal heart rate from 33 +/- 9 47 +/- 13 beats/min (95% confidence interval, 9-19 beats/min; p < 0.0001), and the maximal RR interval from 3,149 +/- 1,018 to 2,087 +/- 601 ms (95% confidence interval, -1,517 to -608 ms; p = 0.0001). Only two patients had headaches as adverse effects. In conclusion, cilostazol had a beneficial positive chronotropic effect in patients with bradyarrhythmias, especially with bradycardic atrial fibrillation and sick sinus syndrome.
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PMID:Chronotropic effects of cilostazol, a new antithrombotic agent, in patients with bradyarrhythmias. 955 1