Competitive Inhibition
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The document discusses the concept of competitive inhibition, highlighting its crucial role in the development of life-saving drugs, including antibiotics and cancer treatments. It explains the mechanism, effects on enzyme kinetics, and applications of various inhibitors like sulphonamides, methotrexate, statins, and allopurinol. The conclusion emphasizes the significance of competitive inhibition in medicine and the responsibility of medical professionals to further explore its principles.
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Competitive Inhibition
- 1. HEY! That’s MY enzyme Whatever. Don’t see Your name on it. INDRANI SAHA DARAKSHA SAJID KHAN FARHAJ SULTANA BIKRANT ROY COMPETITIVE INHIBITION
- 2. INTRODUCTION We are here to highlight the majestic impact of Competitive Inhibition which has given the world innumerable life saving drugs. Most antibiotics are based on the principles of Competitive Inhibition. Drugs against cancer and other deadly diseases utilize the mechanisms of Competitive Inhibition.
- 3. DEFINITION: The type of inhibition where the inhibitor is structural analogue of substrate and it binds reversibly to the same site that substrate will occupy normally, is called Competitive Inhibition. EFFECT ON Vmax : Vmax remains unchanged EFFECT ON Km: Km is increased In presence of a competitive inhibitor more substrate is needed to reach ½Vmax. Competitive Inhibition
- 4. The plots of the inhibited and uninhibited reactions intersect on the y- axis at 1/Vmax. The inhibited and uninhibited reactions show different X-axis intercepts, indicating that the apparent Km is increased in the presence of the competitive inhibitor because - 1/Km moves closer to zero from a negative value.
- 7. EP
- 10. Applications of Competitive Inhibition It has helped in the manufacture of innumerable life saving drugs. Sulphonamides Methotrexate Dicoumarol Isonicotinic acid hydrazide Alcohol dehydrogenase Statin Allopurinol Captopril
- 11. SULPHONAMIDES Bacteria synthesize tetra hydro folic acid by combining Para amino benzoic acid with pteroyl glutamic acid. Sulpha drugs are structural analogs of Para amino benzoic acid. Enzyme dihydro pteroate synthetase is inhibited. All sulpha drugs are bacteriostatic.
- 12. METHOTREXATE It inhibits Dihydrofolate reductase enzyme. It is a structural analog of folic acid. This is essential for DNA synthesis and cell division. It is used as an anticancer drug.
- 13. ALCOHOL DEHYDROGENASE In methanol poisoning, methanol is acted upon by alcohol dehydrogenase. It is converted to formic acid which leads to toxicity. This leads to metabolic acidosis, retinal oedema, COMA and death. For treatment ethanol is used as it can competitively bind to alcohol dehydrogenase.
- 14. CASE STUDY : METHANOL POISONING •Doctors at a Vietnam hospital pumped 5 litres of beer into 48 year old Nyugen Van Nhat’s stomach to save him from dying of alcohol poisoning. •Doctors decided to take the step after the methanol level in his blood was found 1,119 times higher than normal. •The beer(ethanol) slowed down his liver’s methanol processing. •Competitive inhibition provides a novel technique to combat alcohol with alcohol.
- 15. STATIN Statins lower cholesterol levels by inhibiting HMG CoA reductase. Statins can lower LDL cholesterol by 70 mg/dl. This leads to an estimated 60% decrease in cardiac events. 17% reduced risk of stroke.
- 16. ALLOPURINOL Allopurinol inhibits xanthine oxidase . Xanthine oxidase catalyzes the oxidation of hypoxanthine to xanthine . It further catalyzes the oxidation of xanthine to uric acid. Allopurinol blocks the production of uric acid in the body. It is, therefore, used in the treatment for gout.
- 17. ISONICOTINIC ACID HYDRAZIDE It inhibits Beta ketoacyl carrier protein reductase which is involved in elongation of mycolic acid. It results in the inhibition of cell wall leading to cell death. It is an anti tuberculosis drug.
- 18. ANGIOTENSIN CONVERTING ENZYME INHIBITORS ACE inhibitors prevent the conversion of Angiotensin I to Angiotensin II. They inhibit the Angiotensin Converting Enzyme. Angiotensin II is a potent vasoconstrictor. Drugs like Captopril, Enalapril, Lisinopril, Ramipril and Fosinopril are ACE inhibitors. They are used in hypertension acute myocardial infarction.
- 19. DICOUMAROL Dicoumarol is a competitive inhibitor of Vitamin K epoxide reductase. It inhibits Vitamin K recycling and causes depletion of active Vitamin K in blood. Thus, it acts as an anticoagulant.
- 20. CONCLUSION •Competitive Inhibition has profound applications in the field of medicine. •Hence Competitive Inhibition is a boon to mankind. •So as medicos it is our responsibility to explore the principles the Competitive Inhibition further and exploit its potential.
- 21. THANK YOU