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1 reference

Sulfa drug, in full SULFONAMIDE DRUG, sulfa also spelled SULPHA, any member of a group of synthetic antibacterial drugs containing the sulfanilamide molecular structure, and including sulfanilamide, sulfadiazine, sulfapyridine, sulfathiazole, and other substances.

The antibacterial effects of sulfonamides were first observed in 1932, when Gerhard Domagk a German bacteriologist and pathologist, noted the effects of Prontosil (a red dye) on streptococcal infections in mice. French investigators were first to prove that sulfonamide was the active principle in the dye. American researchers later helped create a rational basis for sulfonamide chemotherapy. Sulfonamides were the first chemical substances that were systematically used to cure and prevent bacterial infections in humans.

They are bacteriostatic drugs; i.e., they inhibit the growth and multiplication of bacteria but do not kill them. They act by interfering with enzyme systems essential to normal metabolic and growth patterns of bacteria. Although more than 5,000 sulfa drugs have been prepared and tested, fewer than 20 continue to have therapeutic value because resistant strains of bacteria have developed.

Sulfa drugs are assigned to four groups based on the rapidity with which they are absorbed and excreted. The most common side effects of sulfa drugs include nausea, vomiting, and mental confusion. Other side effects include fever, skin eruptions, anemia, leukopenia, and irritation of the liver or kidneys. More potent antibacterial drugs have largely replaced the sulfa drugs. They are still used, however, in the treatment of urinary tract infection.

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Any of a class of synthetic chemical substances derived from sulfanilamide, or para-amino-benzene-sulfonamide. Sulfa drugs are used to treat bacterial infections, although they have largely been replaced for this purpose by antibiotics some are also used in the treatment of diabetes. Because sulfa drugs were first used to elucidate ways in which substances can interfere with the metabolism of invading microorganisms, they are of historical interest. The parent compound, para-aminobenzenesulfonamide, was synthesized in 1908 by Paul Gelmo, an Austrian industrial chemist. In 1932 the German chemist Gerhard Domagk discovered that the dye Prontosil had antagonistic properties against a wide range of bacteria, and in 1935 it was found that the sulfanilamide portion of the Prontosil molecule was responsible for its antibacterial effect. In 1940 it was shown that sulfanilamide inhibited the action of the physiological substance para-amino-benzoic acid, which bacteria need to synthesize folic acid. The idea that the two substances were antagonists led to a theory of the mechanism of action of drugs: Many chemotherapeutic substances compete with structurally similar substances that are necessary to the metabolism of invading microorganisms. Since sulfanilamide first came into use, more than 150 different derivatives have appeared on the market, chemically modified to achieve more effective antibacterial activity, wider spectrum of microorganisms affected, or more prolonged action. Because of their low cost they are still used in many parts of the world. However, resistance to sulfa drugs has emerged among many microorganisms, especially streptococci, meningococci, and shigella, making them less effective than formerly . The substances are still used to treat some urinary tract infections, leprosy, and in combination with other drugs, fungal diseases such as toxoplasmosis.