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    13 views4 pages

    Viagra

    Uploaded by

    Daniel Conway
    biosci

    Copyright:

    © All Rights Reserved
    Download as PDF or read online from Scribd
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    of 4
    Hon scece works looks at examples fhe waysin which sins work and ‘he potenti impact of ter werk fages isa familiar name, instantly recognised, ten with amusement, worldwide. This disinctve litle blue pill has revolutionised the teatment of erectile dysfunction ~ the inability to sustain an evetion of the penis. Viagra ‘was launched in 1998, and was so siccesfal that i 1999 ‘worklwide sles exceeded $1 billion. Cleary there is truth in the old advertising saying that ‘sex sells. Despite is phenomenal commercial success, however, the effects of Viagra were discovered almost by chance. The scientist who fist produced it never intended to create 2 treatment for crectle dysfunction ll. Viagra was developed in the UK by the pharmaceutical company fier, x part of drug development programme aimed 3¢ treating cardiovascular disease. Cardiovascular problems are the biggest ill n the UK, According tothe British Heart Foundation, cardiovascular problems caused 340 of all deaths in 2007. The pharmaceutical industry twies constantly to develop new treatments for cardio. vascular disease, Pfizer orginally wanted to help sufferers of angina, a ceushing chest pain that can oceut upon exercise ‘or sires (Gee pp. 34-37), Angina Is a symptom of diseased Coronaty arteries, These essential blood vessels supply ‘xygen-tich Blood to the heart muscle itself I they are blocked, damage to the heart may result often with fatal consequences. Partial blockages inthe coronary arteries ar, however, common, Atheroma is a misture of cholesterol, cells and other material that develops in the vlls of arteries in people suffering from vascular disease. tntally there are no symptom but a the disease progiesses and the deposits Increase in size the supply of blood to the heart muscle may be affected. Even then the oeygen demands ofthe heart can sualy be met, Hovsever, when the heart's ned for oxygen increases during exercise, for example, the diseased blood vessels are no longer able to cope. Pat of the heart muscle is starved of oxygen and the result i the agonising pain of an angina attack ‘Many people live with angina for years — it atects 2 million in the UK alone. The pain is reduced by resting, 2nd provided the cells ae not deprive of exygen for too long the heart, recovers rapidly. However, drugs that reduce the likelihood of an angina attack greatly improve the quality of life for sufferers, One Cardvasu close Endthela el roup of such drugs used for over a century, te the organic nitrates. These medicines reduce the workload of the heat, decreasing the chances of its demands outstripping the ability ofthe coronary arteries o deliver oxygen. However, they have the major disadvantage that people taking them regularly may develop tolerance, so the drugs hse their effectiveness ifused too fequentl. Pfizer sought to find an effete alternative and developed Viagra with this in mind ‘The intended target Reseaichers at Pfizer alteady knew a lt about the way fonginie nitrates act. They cause involuntary muscle cll in blood vessel walls (vascular musele) to relax (Figure 1) ‘When the muscle contracts, te diameter of the blood vessels secreaes. This increases the lood pressure and reduces, the blood flow. In contast, muscle relaxation increases ‘vessel diameter This has the effet both of lowering blood pressure and of reducing the amount of blood retuining to the heart though the vein because the dilated veins are able a contain more blond, As result the heat is stretched less during filling, and this reduces the amount af force it reeds to produce when it next contracts, The heart muscle thus requires les oxygen, reducing the chances of an angina attack Tes not the mizate drug itself that helps angina patents but a breakdown-product — a smal, unstable molecule called nitric oxide. Nitricoxideis also produced inthe body as part ofits normal function, Wis released by cells lining ‘the blood vse (the endothelium) and by certain nerves. Ik acts assign causing the muscle inthe blood vessel wallto relay, increasing blood vessel diameter and reducing blood pressure (Figure 1) Nitric oxide docs not cause muscle relaxation directs ‘When i enters dhe cells it binds to and activates an enzyme called guanylate eyease (Figure 2} Guanslate cyclase then catalyses the production of cyclic GMP (¢GMP), which binds, and setivates, 2 number of specifi protein args September 2011 ‘vest constricted ‘vessel ated Reed aod ow Increased ood Howe Ineresied presse edced presure Figure 1 Vascular muscle and its role in regulating blood flow. (a Section trough a blood vessel showing the location ofthe muscle els (8) When the muscle inthe blood vessel ‘wal contrets, the vessel constrict Mii oxide dives muscle ‘elastin and verse! diaton ‘Figure 2 Function of nitvic oxide in blood vessel muscle relaxation and ‘theetfeet of Viogra. (A) Inthe absence of nitric oxide, guanylate cease is inactive. When tric oxides preset activated guanate cyclase “converse substrate GTP to cGMP Thi eatces changes that raul in loss of Ca fons, and muscle relaxation. PES reverses this process by converting cGti to inactive GMP (6) By blocking CGMP breakdown, ‘Viogre boosts level of cGMP. This makes more likely thatthe muscle ‘wiley allowing on erection to occu Inthe penis, niticande is ‘eleased by sexual simulation, so without 2 sexual stimulus, Viagra haemo effect inbiting PDES hon thei no eGUP inthe cells doos 15, “Angin irters chest pain tht ocurs when heart muses deprived of cxygen. Endothelium Cols hate bod veils, GGuanylate cyclase The enzyme ha makes

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