Vasodilators – Pentaerythritol tetranitrate, Isosorbide dinitrate & Dipyridamole | YR Pharma Tube
Hi this is dr rajeshwar from yr pharma tube in the previous video we discussed two vasodilator drugs such as amyl nitrite and nitroglycerin if you did not watch the video hit the i button on top right of this video to watch it for the other topics of anti-anginal agents and medicinal chemistry links are given in the description below this video watch them in this
Lesson we shall discuss few other vasodilators namely penta erythritol tetra nitrate isocarbide dinitrite and dipyridamole the first drug is penta erythritol tetra nitrate pento erythritol tetra nitrate is an organic compound first reported by a german chemist ben hard tollens in 1891 with the formula c ch2o no2 taken 4 times it is chemically 2 2 bis hydroxy
Methyl 1 3 propane diol tetra nitrate it is classified as a polyol or tetral which is a primary alcohol that is white in solid the word penta erythritol is a blend of penta in reference to its five carbon atoms and erythritol which also possess four alcoholic groups penta erythritol is a chemical intermediate used in the synthesis and production of explosives
Plastics paints appliances cosmetics and many other commercial products it has a role as a flame retardant and a laxative it derives from a hydride of neopentane penta erythritol tetra nitrate may be synthesized by a simple nitration reaction of a penta erythritol with nitric acid but using two two bis hydroxy methyl one three propane diol instead of glycerol as
The starting material it is an odourless white solid with a melting point of 140 degree centigrade it is insoluble in water slightly soluble in alcohol and readily soluble in acetone the mechanism of action of penta erythritol tetra nitrate is similar to glycerol tri nitrate but its duration of action is more prolonged it relaxes smooth muscle of smaller vessels
In the coronary vascular tree penta erythritol is a vasodilator and explosive it is a versatile building block for the preparation of many poly functionalized compounds derivatives of penta erythritol are components of alkyd resins varnishes polyvinyl chloride stabilizers tall oil esters antioxidants for example anoxic 20. it can be found in transformer oil
Plastics paints cosmetics and many other applications it is given as tablets the second drug is iso carbide dinitrate iso carbide dinitrate abbreviated isdn is a nitrate vasodilator it is chemically 1436-diahydro deglusital dinitrate the physiologic effect of iso carbide is by means of vasodilation it is a nitrate ester and a glucitol derivative it has a role
As a vasodilator agent and a nitric oxide donor isocarbide dinitrate was first written about in 1939. iso-carbide dinitrate is synthesized by intermolecular dehydration of disorbate into iso carbide using the paratoline sulfonic acid and subsequent nitration of the two alcoholic groups by nitric acid it occurs as a white crystalline powder its water solubility
Is about 1 mg per ml it is stored in a well closed container and protected from light iso carbide dye nitrate is the dye nitrate salt form of iso carbide and organic nitrate with vasodilator activity isosarbide dinitrate relaxes vascular smooth muscle by formation of free radical nitric oxide which is identical to the endothelium derived relaxing factor nitric
Oxide activates guanycyclase enzyme thereby increasing the synthesis of cgmp within smooth muscle resulting in de-phosphorylation of light chain myosin and relaxation of peripheral arteries and veins in addition isosurbide dinitrate relaxes coronary arteries thereby increasing the blood circulation through the ischemic area iso carbide dinitrate is sold in the u.s
Under the brand names dielectric sr and isordil it is in the nitrate family of medications and works by dilating blood vessels that is as a vasodilator it is a medication used for heart failure eusophagal spasms and to treat and prevent chest pain from not enough blood flow to the heart it has been found to be particularly useful in heart failure due to systolic
Dysfunction together with hydralazine it is taken by mouth or under the tongue the last drug of this lesson is a dipyridamole dipyridamole is a synthetic derivative of pyrimidopyrimidine with anti-platelet properties it has a role as an adenosine phosphodiesterase inhibitor and adenosine d-aminos inhibitor a platelet aggregation inhibitor and a vasodilator agent
It is a member of piperidines a pyramidopyrimidine a tertiary amino compound and a tetral dipyridamole is a nucleoside transport inhibitor and a pde3 inhibitor medication that inhibits blood clot formation when given chronically and causes blood vessel dilation when given at high doses over a short time dipyridamole is easily synthesized from phi nitro orotic
Acid which is prepared from 2-4 dihydroxymethyl pyrimidine which in turn is usually prepared by the condensation of urea with acetoacetic ether reduction of the nitro group in phi nitro orotic acid by various reducing agents give 5 amino urotic acid which is reacted with urea or with potassium cyanide to give 2468 tetrahydroxy pyrimidopyridine this undergoes a
Reaction with a mixture of phosphorus oxychloride and phosphorus pentochloride which forms 2468 tetrachloropyrimidal pyrimidine reacting the resulting tetrachloride with piparidine replaces the chlorine atoms at c4 and c8 with the piperidine giving 2 6 dichloropyramidal 4 8 dipiparydinopyrimidine reacting this with diethanolamine gives the desired product that is a
Diperitamole dipyridamole has two known effects acting via different mechanisms of action number one dipyridamole inhibits the phosphodiesterase enzymes that normally break down cyclic amp or cyclic gmp and number two dipyridamole inhibits the cellular reuptake of adenosine into platelets rbcs and endothelial cells leading to increased extracellular concentrations
Of adenosine dipyridamole is sowed in the name parasantine it is used to dilate blood vessels in people with peripheral arterial disease and coronary artery disease it has been shown to lower pulmonary hypertension without a significant drop of systemic blood pressure it can be used for myocardial stress testing as an alternative to exercise induced stress methods
Such as treadmills this is the list of references followed for the lesson that’s all in this lesson the vasodilators such as penta erythritol tetra nitrate iso carbide dinitrite and dipyridamole in the next lesson we will discuss the calcium channel blockers till then never stop learning and never stop watching my videos thank you for watching this video
Transcribed from video
Vasodilators – Pentaerythritol tetranitrate, Isosorbide dinitrate & Dipyridamole | YR Pharma Tube By YR Pharma Tube