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Solutions For An Introduction to Medicinal Chemistry Chapter 19 Problem 4Q

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Sulfa drugs or sulpha drugs, also known as sulphonamide are the basis of many drug groups. The authentic antibacterial sulphonamides are the simulated antimicrobial agents, which constitute the sulfonamide group. Certain sulphonamides also lack antibacterial activity.

In bacteria, sulphonamides functions as competitive inhibitors of the enzyme DHPS (dihydropteroate synthase), they are therefore bacteriostatic and prevent multiplication and growth of bacteria, but do not kill them.

Procaine is a native anesthetic drug of the group of amino ester. It is used mainly to minimize the intramuscular injection pain of penicillin, and it is has application in dentistry. Generically it is used in some regions as Novocain. It generally acts as a blocker of the sodium channel. Presently, it is therapeutically in certain nations because of its anti-inflammatory, sympatholytic, mood enhancing, and perfusion enhancing influences.

However, the activity of sulphonamides is reduced if they are consumed at the similar time with procaine. The body modifies procaine to PABA (para-aminobenzoic acid). This PABA has an antagonistic influence on antibiotic sulfonamides, which reduce its activity. Some of these antibiotics are Gantanol (sulfamethaxazole), Azulfidine (sulfasalazine), and Gantrisin (sulfisoxazole).

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Solutions For Problems in Chapter 19