Angina pectoris coronary vasodilators

Prenyl amine (66) was long used in the treatment of angina pectoris, in which condition it was believed to act by inhibiting the uptake and storage of catecholamines in heart tissue. Droprenilamine (69), an analogue in which the phenyl ring is reduced, acts as a coronary vasodilator. One of several syntheses involves simple reductive alkylation of 1,1-diphenyl-propylamine (67) with cyclohexyl acetone (68)... 

DHPs are potent arterial vasodilators. They act on resistance vessels and therefore reduce peripheral vascular resistance, lower arterial blood pressure, and antagonize vasospasms in coronary or peripheral arteries. By reducing afterload, DHPs also reduce cardiac oxygen demand. Together with their vascular spasmolytic effect, this explains most of the beneficial actions of DHPs in angina pectoris. Most DHPs are only licensed for the therapy of hypertension, some of them also for the treatment of angina pectoris and vasospastic (Prinzmetal) angina. 

Papaverine is an opium alkaloid initially isolated in the mid-1800s. It relaxes smooth muscle and is a potent vasodilator. As such it is used to dilate pulmonary and other arteries. It is therefore sometimes of use in the treatment of angina pectoris (usually caused by partial blockage of the coronary artery), heart attacks and bronchial spasms. 

PETN was introduced into clinical medicine for the treatment of angina pectoris as a long-acting coronary vasodilator [24]. The administration of PETN has very little effect on peripheral arterial vasodilation [25]. 

The coronary vasodilating effect of various substances was compared (142, 147-149). Persch and Nitz (149) studied the therapeutic application of parakhelline for angina pectoris in dogs and cats. Papaverine brought about a maximum blood flow in the coronary arteries much more rapidly than that of khelline which was, however, of longer duration. Fekete and Borsy (150) studied the effect of pheno-thiazine derivatives and of papaverine on the dilation of coronary arteries. 

Ettriol trinitrate) - se coronary vasodilator (angina pectoris)... 

Dipyridamole is also a potent coronary arteriolar vasodilator, perhaps by opening of vascular K tp channels (2). However, the Food and Drug Administration withdrew conditional approval for certain drug products containing dipyridamole, because of a lack of sufficient evidence of effectiveness in the long-term therapy of angina pectoris (3). 

Prenylamine is a coronary vasodilator that depletes myocardial catecholamine stores and has some calcium-channel blocking activity. It has been used in the treatment of angina pectoris, but it often causes ventricular dysrhythmias and has been superseded by less toxic drugs. 

Verapamil. Verapamil. S-. T.4-dimcthoxyphcnethyl -methylamino)-2-(3.4-dimcthoxyphenyl)-2-isopropylvalcro-nitrile (Calan. Isoptin). was introduced in 1962 as a coronary vasodilator and is the prototype of the Ca antagonists u.sed in cardiova.sculur diseases. It i.s u.scd in the treatment of angina pectoris, arrhythmias from Lschcmic myocardial. syndromes, and supraventricular airhythmia.s. 

Iopanoic acid (3-amino-0(-ethyl-2,4,6-rn7o(3 o-hydrocinnamic acid) is a radiopaque iodine compound used as a contrast medium in cholecystography. Amiodarone (2-butyl-3-benzofuranyl) [4- [2- (diethylamino) ethoxyl]-3,5-diVocoronary vasodilator used in the control of ventricular arrhythmias, and in the management of angina pectoris. 

In the course of their work on a canine heart model for angina, Szentivanyi and co-workers claim to have found evidence for the existence of a substance, hyperemin, which regulates coronary vessel responsiveness to metabolic requirements. In the absence of hyperemin, vasodilation could no longer be produced by metabolic stimuli or by adrenalin. Administration of hyperemin from a donor heart reestablished normal responses. -Presumably, angina pectoris may involve a lack or insufficiency of a hyperemin type material in the human heart. 

Dipyridamole is a potent coronary vasodilator. Despite the fact that it causes a substantial increase in CBF, its value for the acute relief or prevention of angina pectoris has been seriously questioned. Considerable effort has been expended in the study of this drug. Deutllcke reports dipyridamole to inhibit adenosine deaminase which results in an accumulation of adenosine. Since adenosine is a potent vasodilator, there is an increase in CBF. Emmons found dipyridamole to inhibit platelet agglutination and proposed that dipyridamole prevents the uptake of adenosine by red blood cells, thereby delaying its deamination. Stafford feels that dipyridamole inhibition of adenosine deaminase is unlikely, as high concentrations are necessary to produce inhibition of deaminase from intestinal mucosa. Much lower concentrations of dipyridamole potentiate the action of adenosine on myocardial tissue. Stafford proposes that dipyridamole prevents the uptake of adenosine by myocardial tissue or red blood... 

Prenylamine (I) was introduced in Europe as a coronary vasodilator which reduces the noradrenaline and serotonin content of the heart. Initial double blind studies have shown a decrease in the pain of angina pectoris. Results using objective methods, based on ECG changes and Masters Two-Step techniques, have been equivocal. Ito found prenylamine, dipyridamole, and 7-chloroethyltheophylline to increase diastolic pressure as well as CBF. Ito states that factors other than increased diastolic... 

A number of compounds have been reported which have coronary dilator properties or other activities which have culminated in their clinical trial for use in angina pectoris. Lidoflazlne (IV) is claimed to be a specific, long acting coronary vasodilator. This agent appears to reduce coronary vascular resistance in dogs and causes an Increase in coronary venous pO. ... 

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