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Antimicrobial Agents. Antimicrobial agents. Antibiotics – bacteria Antifungals – fungus Antiprotozoans – protozoa Antihelminths – worms. Infection. It has only been in the last 150 years that we have realized that infections were caused by other living organisms residing in the host.
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Antimicrobial agents • Antibiotics – bacteria • Antifungals – fungus • Antiprotozoans – protozoa • Antihelminths – worms
Infection • It has only been in the last 150 years that we have realized that infections were caused by other living organisms residing in the host
Infection • Localized – limited to one area like skin, eyes, ears or mucosa • Systemic – infection involves the body
Infectious Disease • There are many, many disease processes that are caused by infection • There are many, many terms to describe infection
Microbiology • The study of these microbes is covered in microbiology (microscopic biology).
Basic Micro Terms for Antibiotics • Bacteriostatic – prevent bacteria reproduction • Bacteriolytic – cause bacteria death
The age of antibiotics • Although there have been cultures that used plants and minerals to treat infectious diseases for centuries • Our understanding of infectious disease and the scientific use of antibiotics is less than a century old
Many horrible diseases are no longer killing the masses worldwide • Learn the history of infectious disease and the human suffering it has caused
Proper sanitation and clean water have done more to combat infectious disease than anything else
Sulfonamides • Sulfonamide drugs were the first antimicrobial drugs • Paved the way for the antimicrobial revolution in medicine
Sulfonamides • The first sulfonamide was trade named Protonsil, which is a prodrug of an active sulfonamide. • Experiments with Prontonsil began in 1932 in the laboratories in the laboratories of Bayer AG.
Sulfonamides • Prontonsil was the first medicine ever discovered that could effectively treat a range of bacterial infections. • It had no effect at all in a test tube or petri dish, exerting its antibacterial action only in live animals.
Sulfonamides • Antibacterial sulfonamides act to prevent a key step in folate synthesis • Since folate is necessary for cells to synthesize nucleic acids… • Preventing folate acid synthesis prevents cells from dividing
Sulfonamides • Because the sulfonamide antibacterial prevent reproduction of the bacteria they are…
Sulfonamides • Folate is synthesized in mammalian cells, it is a dietary requirement • This explains the selective toxicity in bacteria
Sulfonamides • Sulfacetamide as topical for bacterial conjunctivitis • Silver sulfadiazine cream for burn wounds
BactrimSeptraSMX/TMP • Sulfamethoxazole with Trimethoprim are used in combination as a potent antibiotic combination • Trimethoprim is also a folate synthesis inhibitor
Sulfonamide • Sulfonamides led to the development of many sulfa-based drugs: • Sulfonylureas – for diabetes mellitus • Thiazide diuretics – for hypertension
Sulfonamide • Unfortunately, sulfonamides cause allergic reactions in nearly 5% of the population • Is a leading cause of a drug induced Stevens-Johnson syndrom – a type of allergic reaction
Polyketides • Polyketides are metabolites from bacteria, fungi, plants and animals.
Polyketides • Ancient wisdom gave us the knowledge that certain plants and molds were helpful in preventing what we call infection
Penicillin • It has been known since the ancients that certain molds had healing properties • Modern scientific investigation of these properties emerged as early as 1875.
Penicillin • Although the antimicrobial properties of penicillin were well accepted • Mass production of penicillin was difficult until 1940s. • It was common procedure to collect the urine from patients being treated so that the penicillin could be isolated and reused.
Penicillin • Thanks to a lot of researchers, and a moldy cantaloupe in Peoria, Illinois… • By 1944, PCN was in full mass production
Penicillin • Penicillin was used to treat Gonorrhea before but now it is no longer being used since the bacteria evolved to resist the antibiotic
However… • Some bacteria, which had never caused infections before penicillin, emerged as pathogens…
Beta-lactam antibiotics • Penicillins • Cephalosporins • Carbapenems