The History Of Antibiotics - part 3

Penicillin showed marked efficiency in combating an assortment of infections, including septicemia, pneumonia, scarlet fever, diphtheria, strep throat, rheumatic fever as well as the sexually transmitted ailment gonorrhoea. In fact, people started believing that penicillin could be used to treat any ailment and, incidentally, this myth even exists till date. At the same time, this new magic medicament received fantastic publicity and Dr. Fleming, Dr. Florey and Dr. Chain were jointly awarded the Nobel Prize in Physiology and Medicine in 1945.

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Later, penicillin was produced in oral form and was also included in several products, such as throat lozenges, ointments, cosmetic creams and nasal ointments. Before 1955, the sale of penicillin was not restricted and, hence, anyone and everyone were able to purchase it without a prescription. However, the overuse and unrestricted use of penicillin resulted in increasing resistant to bacteria. In fact, the damage had already been done. Soon, resistance to antibiotics became a major problem in medical circles and victims of staphylococcal-resistant infections, which appeared in an epidemic form, started pouring into different hospitals.

In the meantime, in 1935, a German researcher demonstrated that a dye known as Prontosil Red was effective in treating mice infected with Streptococcus supp. - the bacteria responsible for strep throat. In fact, the dye Prontosil Red was the predecessor of a group of drugs similar to antibiotics and known as sulphonamides or sulfa drugs. Even to this day, these drugs are in use. For instance, Septra, which contains sulfamethoxazole, is given to patients suffering from infections of the respiratory as well as the urinary tract.

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For a long period, microbiologists have been familiar with the fact that soil includes only a few bacteria that have the aptitude to cause infections in humans. Examination of the soil bacteria and the grounds why they are not much able of to cause diseases was the lifetime work of Selman Waksman, a research scientist associated with the New Jersey-base Rutgers University. Merck and Company helped Waksman with funds in 1939 to begin an exploration for antibiotics with a view to offer optimism to patients suffering from tuberculosis (TB). Even to this day, the antibiotic is used to treat tuberculosis.

Soon after streptomycin was clinically used in tuberculosis patients, it was found that the use of the drug resulted in side effects that were absent in the case of using penicillin, counting kidney damage as well as deafness. Nevertheless, the major problem faced by patients in using streptomycin, and what actually limited efficiency, was resistance. In fact, the pace at which bacteria were capable of developing resistance to this drug surprised Waksman and his colleagues. Owing to this factor, they were encouraged to undertake research to find other antibiotics. This search actually led to the development of neomycin - a medicament generally used in a number of antibacterial ointments these days.

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The antibiotic chloramphenicol was used in a clinical test in 1947 to cure an epidemic of typhus in Bolivia. The success of this antibiotic drug in restraining the epidemic resulted in its use on another region of the globe - treating scrub typhus (a contagious ailment caused by the organism Rickettsia tsutsug) in Malaysia.

As many as 22 patients who received the antibiotic chloramphenicol in the Bolivian epidemic survived. Among the 50 patients who did not avail antibiotic, 14 succumbed to the epidemic. Actually, the trial of the antibiotic drug in Bolivia is not its sole connection in South America. In effect, the antibiotic medicament chloramphenicol was isolated for the first time from a soil sample in a place in Caracas, Venezuela. This discovery is significant in two ways. Firstly, it helped in detecting a new antibiotic substance and second, according to the findings of the clinical trial, chloramphenicol has the potential to treat diseases that were incurable earlier - for instance, typhus. Much later, this antibiotic medicament demonstrated outstanding results in treating typhoid fever. Finally, the scientists were being successful in discovering new and effectual substances, which could cure severe infections.

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The ecstasy involved with the discovery of chloramphenicol was rather diminished when it became clear that the use of the antibiotic resulted in grave side effects. By 1950, several researchers were worried by the increasing proof related to the drug's use to acute blood disorders, such as anaemia and even leukemia.

The use of the antibiotic drug chloramphenicol is presently restricted in the developed nations, as more expensive, but less harmful medications are available in these places. However, in developing nations this antibiotic is still in use since its production does not entail great expenses. Primarily, this drug is given to patients suffering from typhoid fever, typhus, meningitis and brucellosis also known as undulant fever. However, this antibiotic medicament may also be used for treating other infections. In fact, it is possible that you have used this drug either in your ear drops or eye drops.

During the middle of the 1940s, the rector of the Sardinia-based University of Cagliari, Giuseppe Brotzu had isolated a substance akin to an antibiotic from a mold. Brotzu undertook a number of clinical trials with the substance (although in mixed form) and obtained excellent results, especially in treating infections caused by the staphylococcal bacterium and also in curing typhoid.

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In 1948, Brotzu made the findings of this clinical trials public and his work drew the attention of the research group formed by Dr. Florey in Oxford University. After obtaining the samples of the fungus, members of the Oxford University research group could isolate as well as purify a number of antibiotics similar to penicillin, which were known as cephalosporins. It was found that the cephalosporins were highly effectual in curing an assortment of infections caused by bacteria. These antibiotics eliminate bacteria in a way that is comparable to the actions of penicillin and were considered as valuable options, particularly in cases where resistance to penicillin was a major worry. In addition, cephalosporins had very low toxicity and this was a great advantage of using these antibiotic medicaments. However, it is another matter that using cephalosporins resulted in allergic reactions in approximately five per cent of patients.

Alterations in the fundamental chemical structure of cephalosporin have resulted in the development of an entire variety of these antibiotic drugs for clinical use. In fact, further research into the development of latest cephalosporin is continuing even to this day. Benjamin M. Duggar was successful in isolating chlortetracycline from a mud sample obtained from a river in Missouri. While chlortetracycline was the first ever tetracycline, the discovery of Duggar has resulted in the isolation and then the development of numerous very potent antibiotics. Currently, these antibiotic drugs are only second to penicillin in terms of worldwide sales.

Since these antibiotic drugs are extremely effective against an assortment of bacteria and they are also comparatively cheaper to produce, the tetracyclines gained favour very quickly and currently, they are used to cure several different types of infections.

It must be accepted that the wide ranging research conducted on tetracyclines has definitely found them to be extremely effectual in combating infections. At the same time, use of tetracyclines is also known to result in a number of noxious side effects. Tetracyclines results in the formation of calcium complexes in developing bone, which may cause permanent discoloration and enamel imperfections in the teeth and, at the same time, lessen the growth of bone. In addition, tetracyclines penetrate the placenta and have an immense toxic effect on the fetus. Owing to these adverse and toxic side effects, use of tetracyclines is banned in treating infections among pregnant women and children under the age of seven years, since they have the potential to slow down the growth of kids.

Tetracyclines also cause a number of other toxic side effects, such as the rapid multiplication of the Staphylococcus spp. and Candida spp. bacteria in the bowel resulting in chronic infections with these micro-organisms. Some patients using these antibiotic medicaments may also experience kidney and liver damages, while tetracyclines are also known to cause allergic reactions, including hives, skin rash, contact dermatitis and even asthma.

As the use of tetracyclines result in the formation of complexes with magnesium, calcium and iron, they should never be taken concurrently with dairy products or any vitamin or mineral supplements that may enclose magnesium, calcium or iron. Additional research undertaken in the 1960s led to the development of the second generation antibiotic drugs. These second generation antibiotics included methicillin, a partially synthetic derivative of penicillin produced to especially beat the problems of penicillin resistance. In effect, scientists hailed methicillin as a vital advancement in the fight against bacterial resistance to penicillin. Scientists were now of the view that they would be able to win the battle against bacterial infections. However, unfortunately, they were proved wrong and bacteria had the final word and today we have bacteria that are also resistant to the second generation antibiotic methicillin.

In addition to methicillin, ampicillin is another second generation antibiotic that has been derived from penicillin. This antibiotic was developed to widen the range of infections that could be cured by penicillin and now, to a great extent, ampicillin, it has substituted penicillin. In fact, today ampicillin is the first choice of physicians while treating an assortment of infections, counting infections of the respiratory and urinary tracts.

In effect, today amoxicillin is the yet another extensively used antibiotic drug that has been derived from penicillin. Similar to ampicillin, amoxicillin also has a wide range of actions. It is effective in treating Gram-positive bacteria (those bacteria that preserves the brutal stain in a procedure known as Gram's method or Gram's stain, used to classify bacteria, for instance, Staphylococcus spp. and Streptococcus spp.) as well as Gram-negative bacteria (the bacteria that do not keep the violent stain used in Gram's method, for instance E.coli and Haemophilus influenza).

Gentamicin is another antibiotic drug belonging to the same family of antibiotics like streptomycin (the anti-tuberculosis drug that was discovered in 1943). This antibiotic drug is usually kept aside for treating acute infections, since gentamicin has the potential to cause grave toxic side effects in the ears and the kidneys.

In recent times, pharmaceutical companies have developed antibiotic drugs belonging to a new family called fluoroquinolones. Besides being very effectual in combating a wide range of bacteria, when taken orally, the drugs in this family of antibiotics have the aptitude to reach a high concentration in the bloodstream. This denotes that several infectious diseases that required to be cured by staying in hospitals can now be treated at home.

Very frequently, fluoroquinolones are used to treat cases which require taking long courses of antibiotic drugs, some times even for several weeks or several months. Currently, an entire range of antibiotic drugs belonging to the fluoroquinolones are available and they are highly effective against bacteria that were difficult to treat some time back. This type of bacteria includes the leprosy bacteria.

The future

While several new types of antibiotic medicaments have been discovered over the ages, the hunt for discovering latest and further effectual drugs that started with Dr. Florey, Dr. Chain and Waksman continues to this day. However, the pace of the search has slowed down significantly, since it is additionally difficult for pharmaceutical firms to get new drugs approved these days now. The delay in time between the discovery of a new antibiotic drug in the laboratory and the authorization needed to produce the drug commercially is often so great that it has resulted in some companies abandoning the marketplace for good. The pharmaceutical firms that are engaged in the search for discovering the latest antibiotic drugs are also finding it more and more difficult to maintain the rate at which bacterial resistance makes their findings ineffective. Hence, it may be said that the future of discovering new antibiotics that would be highly effective against bacteria and overcome bacterial resistance appears to be bleak.


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