Differential effect of regadenoson versus dipyridamole on heart rate in patients with left bundle branch block: How does it affect the results of pharmacological nuclear stress testing?

Background Myocardial perfusion imaging (MPI) stress test is performed either using exercise as a stress modality or through the use of pharmacological vasodilator agents in those who cannot exercise. Regadenoson and dipyridamole are some of the most common vasodilator agents used. We aim to study the effect of these agents on the heart rate and the imaging results. Methods This was a retrospective study which included 187 patients with left bundle branch block. Patients received either dipyridamole or regadenoson during the myocardial perfusion imaging stress test. Charts were reviewed, and patient characteristics were recorded, as well as baseline heart rate, peak heart rate during stress, and angiographic data if available. Results Regadenoson increased peak, absolute and relative heart rates significantly more compared to dipyridamole. The peak heart rate for Regadenoson was 94.1 ± 17.36 and for dipyridamole it was 85.38 ± 16.48 BPM (P < 0.001). The relative and absolute heart rate increase in the regadenoson group were 40.75 ± 23.01% and 26.06 ± 13.44 BPM, respectively. The relative and absolute heart rate increase in the dipyridamole group were 24.61 ± 18.25% and 16.23 ± 10.97 BPM. The frequency of reversible septal defects was similar in both groups (54% for Regadenoson vs. 63% for Dipyridamole; P = 0.24). Conclusions There is a statistically significant increase in heart rate with the use of regadenoson for MPI compared to dipyridamole. However, the number of septal perfusion defects was similar between the two groups. The effect of this increase in heart rate, while statistically significant, is likely of no clinical significance.

Synthesis and vasodilator activity of 3,4-dihydropyrimidin-2(1H)-ones bearing urea, thiourea, and sulfonylurea moieties

A series of novel 3,4-dihydropyrimidin-2(1H)-ones bearing urea, thiourea, and sulfonylurea moieties were synthesized and pharmacologically evaluated as vasodilator agents. The most interesting vasodilators were the thiourea derivatives 6a and 6b and the urea derivatives 6f–6i and 7f–7h, although the ureas were relatively more active than thioureas. Twenty-fold more active than diazoxide, the urea 6g was the most potent vasodilator (EC50 = 0.983 ± 0.061 μmol/L) and proved to act as a voltage-gated calcium channel blocker. The lack of activity of sulfonylureas, 6k and 7j, could be attributed to their partial ionization at the physiological pH because of their acidic character. It should be interesting to investigate a larger number of compounds, including N-methylated sulfonylureas, to increase the vasodilator activity and to explore other biological models.