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Synthesis of new annellated flavonoid derivatives possessing spasmolytic activity--VII.

7,8-Dihydroxyflavone reacts with ethyl 2,3-dibromopropanoate to form the new, annellated, 1,4-benzodioxanes 1 containing a flavone structural unit. The regioisomers 1a and 1b thus obtained were separated and 1a was converted to the amides 2a-2f. The constitutions of 1 and 2 were elucidated by 500 MHz 1H-NMR spectroscopy. In the spasmolysis test, 2e showed significant antagonistic effect towards the agonists acetylcholine, barium chloride, and histamine.

Chemical Phenomena↗

Evaluation of a spasmolytic cocktail to prevent radial artery spasm during coronary procedures.

Radial artery spasm is a frequent complication of the transradial approach for coronary angiography and angioplasty. Recently, we have been able to quantify spasm using the automatic pullback device. The objective of this study was to assess the efficacy of an intra-arterial vasodilating cocktail in reducing the incidence and severity of radial artery spasm. A hundred patients undergoing coronary procedures via the radial artery were divided into two groups of 50 each. Patients in group A received intra-arterial cocktail (5 mg of verapamil plus 200 micro g nitroglycerine in 10 ml of normal saline), while patients in group B did not receive any vasodilating drug. The pullback device was used for sheath removal at the end of the procedure. Seven (14%) patients in group A experienced pain (i.e., pain score of III-V) during automatic sheath removal, as compared to 17 (34%) in group B (P = 0.019). The mean pain score was significantly lower in group A than in group B (1.7 +/- 0.94 vs. 2.08 +/- 1.07; P = 0.03). The maximal pullback force (MPF) was also significantly lower for group A (0.53 +/- 0.52 kg; range, 0.10-3.03 kg) as compared to group B (0.76 +/- 0.45 kg; range, 0.24-1.99 kg; P = 0.013). Only 4 (8%) patients in group A had an MPF value greater than 1.0 kg, suggesting the presence of significant radial artery spasm, as opposed to 11 (22%) in group B (P = 0.029). Administration of an intra-arterial vasodilating cocktail prior to sheath insertion reduces the occurrence and severity of radial artery spasm.

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