Antibiotics

C

Aminoglycosides

Streptomycin is the oldest of the aminoglycosides. The aminoglycosides inhibit bacterial protein synthesis in many gram-negative and some gram-positive organisms. They are sometimes used in combination with penicillin. The members of this group tend to be more toxic than other antibiotics. Rare adverse effects associated with prolonged use of aminoglycosides include damage to the vestibular region of the ear, hearing loss, and kidney damage.

D

Tetracyclines

Tetracyclines are bacteriostatic, inhibiting bacterial protein synthesis. They are broad-spectrum antibiotics effective against strains of streptococci, gram-negative bacilli, rickettsia (the bacteria that causes typhoid fever), and spirochetes (the bacteria that causes syphilis). They are also used to treat urinary-tract infections and bronchitis. Because of their wide range of effectiveness, tetracyclines can sometimes upset the balance of resident bacteria that are normally held in check by the body's immune system, leading to secondary infections in the gastrointestinal tract and vagina, for example. Tetracycline use is now limited because of the increase of resistant bacterial strains.

E

Macrolides

The macrolides are bacteriostatic, binding with bacterial ribosomes to inhibit protein synthesis. Erythromycin, one of the macrolides, is effective against gram-positive cocci and is often used as a substitute for penicillin against streptococcal and pneumococcal infections. Other uses for macrolides include diphtheria and bacteremia. Side effects may include nausea, vomiting, and diarrhea; infrequently, there may be temporary auditory impairment.

F

Sulfonamides

The sulfonamides are synthetic bacteriostatic, broad-spectrum antibiotics, effective against most gram-positive and many gram-negative bacteria. However, because many gram-negative bacteria have developed resistance to the sulfonamides, these antibiotics are now used only in very specific situations, including treatment of urinary-tract infection, against meningococcal strains, and as a prophylactic for rheumatic fever. Side effects may include disruption of the gastrointestinal tract and hypersensitivity.

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V

Production

The production of a new antibiotic is lengthy and costly. First, the organism that makes the antibiotic must be identified and the antibiotic tested against a wide variety of bacterial species. Then the organism must be grown on a scale large enough to allow the purification and chemical analysis of the antibiotic and to demonstrate that it is unique. This is a complex procedure because there are several thousand compounds with antibiotic activity that have already been discovered, and these compounds are repeatedly rediscovered. After the antibiotic has been shown to be useful in the treatment of infections in animals, larger-scale preparation can be undertaken.

Commercial development requires a high yield and an economic method of purification. Extensive research may be needed to increase the yield by selecting improved strains of the organism or by changing the growth medium. The organism is then grown in large steel vats, in submerged cultures with forced aeration. The naturally fermented product may be modified chemically to produce a semisynthetic antibiotic. After purification, the effect of the antibiotic on the normal function of host tissues and organs (its pharmacology), as well as its possible toxic actions (toxicology), must be tested on a large number of animals of several species. In addition, the effective forms of administration must be determined. Antibiotics may be topical, applied to the surface of the skin, eye, or ear in the form of ointments or creams. They may be oral, or given by mouth, and either allowed to dissolve in the mouth or swallowed, in which case they are absorbed into the bloodstream through the intestines. Antibiotics may also be parenteral, or injected intramuscularly, intravenously, or subcutaneously; antibiotics are administered parenterally when fast absorption is required.

In the United States, once these steps have been completed, the manufacturer may file an Investigational New Drug Application with the Food and Drug Administration (FDA). If approved, the antibiotic can be tested on volunteers for toxicity, tolerance, absorption, and excretion. If subsequent tests on small numbers of patients are successful, the drug can be used on a larger group, usually in the hundreds. Finally a New Drug Application can be filed with the FDA, and, if this application is approved, the drug can be used generally in clinical medicine. These procedures, from the time the antibiotic is discovered in the laboratory until it undergoes clinical trial, usually extend over several years.

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