Dear Readers, welcome to medicinal chemistry. This time we will be exploring cardiovascular drugs in detail. Surprisingly, cardiovascular diseases are the second leading cause of death. These can be treated using cardiovascular drugs, which are any agents that affect the function of the heart and blood vessels. These drugs save many lives, but how?
What are cardiovascular drugs?
As mentioned earlier, cardiovascular drugs are chemicals or agents that affect the function of the heart and the blood vessels- but there is a wide, wide range of chemicals used to treat cardiovascular diseases- these consist of anticoagulants(or blood thinners), antiplatelet agents, diuretics and so many more- but our article will focus on the more common ones- b-blockers, organic nitrates(which are used in many drugs) and a-blockers.
B-Blockers
B-Blockers are one of the most commonly used drugs to treat cardiovascular diseases- a widely used example is propranolol. Let's use this as a case study: Propranolol is an androgenic blocker that inhibits the brain’s sympathetic functions. That’s some complicated jargon, but let’s break it down together. What a b-blocker does, essentially, is bind to adrenoreceptors, which are the neuroreceptors(read our Neurochemistry issue for more info!) for neurotransmitters that induce effects similar to those of adrenaline- examples include norepinephrine and epinephrine. By binding to these receptors before the neurotransmitters, b-blockers inhibit their effects- therefore, they prevent sympathetic effects, which refer to the fight or flight responses our body makes to certain scenarios. Hydrogen bonds can be observed when b-blockers bind to b-androgenic receptors, which are strong forces between oxygen and hydrogen atoms in different molecules. The most important end result of the usage of this blocker is reduced blood pressure, which thereby reduces the effects of cardiovascular diseases. The chemical structures of some b-blockers are shown below:
A-blockers
You, dear Reader, are probably pondering the difference between a-blockers and b-blockers. Well, a-blockers deal with neurotransmitters like norepinephrine and noradrenaline, resulting in reduced blood pressure, like the b-blockers. They work in almost the exact same way, but with different receptors. The a-blockers bind to alpha-adrenergic receptors, which guarantee smooth constriction of muscles. A-blockers stimulate these receptors by binding to them and can cause various effects- most importantly it relaxes blood vessels, causing vasodilation and thereby reducing blood pressure. Below are the chemical structures for some commonly used a-blockers.
Organic Nitrates
Organic nitrates are molecules capable of releasing NO and they have been used for many years in the treatment of cardiovascular diseases such as angina and heart failure. Many medicines contain organic nitrates such as nitroglycerin and isosorbide. In fact, nitrates have been the basis for the treatment of angina for decades. Angina is an uncomfortable feeling, tightening or pain in your chest. Essentially, nitrates dilate, either widen or relax the arteries and veins in the body. By dilating the blood vessels of the heart, nitrates can reduce the stress on the heart by improving blood flow to the heart muscle. Organic nitrates oxidize the haemoglobin and myoglobin to release NO. The donation of NO by organic nitrates and the activation of the pathway is described as the main mechanism of action of these drugs.
And that’s the end of this article! We hope you enjoyed reading and learning as much as we did provide this content. Now you know more about the chemistry and working mechanisms of cardiovascular drugs, and there’s more to come in Medicinal Chemistry. Keep an eye out for our next issue!
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Written by:
Mythri Subash and Malaya Parwani
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