Antibiotic development

Antibiotic development
An ideal antibiotic stops the growth of or kills all dangerous bacteria in a patient’s body while leaving the normal bacteria in the body alone and not harming the tissues of the host body. Even though there isn’t such an antibiotic, these things must be taken into account when making antibiotics so that, even if they aren’t perfect, a drug close to these qualities can be made. First of all, the spectrum of coverage is very important. An antibiotic that works well against both gram-positive and gram-negative bacteria is better than a drug that only works on one group of bacteria because it lowers antibiotic resistance. (Palomino & Palomino 2011). For example, the fourth-generation drug Cefepime is effective against both gram-positive and gram-negative bacteria, which makes it a recommended drug.

Second, I would think about how important it is to have more than one goal as a site of action. Having one site of action helps get rid of drug resistance. For example, a drug that works by stopping the production of both the 30s and 50s subunit proteins would be more effective because its effects add up. Also, if the bacteria are resistant to one mode of action (MOA), the other MOA makes up for the difference, so the bacteria don’t become resistant to the drug. Also, knowing the makeup of the bacteria is important. If you know its strengths and weaknesses, it’s easy to figure out where your drug should go in that microorganism. ( Kaye & Pogue 2015). For example, it is easy to make an antibiotic that stops cell wall production once you know how the walls of bacteria are made. For example, penicillin works against a wide range of bacteria because it stops bacteria from making peptidoglycans.

Also, the antibiotic shouldn’t hurt the host too much. When used by pregnant women, some antibiotics can cause birth defects. (Khadka et al., 2014). In terms of how the bacteria affect the body’s systems and how well the drug works, the disease process is an important factor. Some drugs stick strongly to proteins in the blood, like globulins, so that not enough of the drug is at the sites where it works. So, absorption is an important thing to consider when making these drugs so that they work.

Several theories about what causes drug resistance have been tested and found to be true. Some bacteria make enzymes that can stop some medicines from doing their job. For example, beta-lactamases are enzymes that work against drugs with a beta-lactam ring, making them useless. Drugs like penicillin, cephalosporins, carbapenems, etc., are affected by beta-lactamases. In these cases, these drugs are given with other drugs that protect them from beta-lactamases. For example, Amoxicillin is given with clavulanic acid, which keeps beta-lactamases from breaking down Amoxicillin. (Richter & Hergenrother 2019). Also, some bacteria have genes that tell them how to make efflux pumps. These pumps can get rid of drugs so they don’t stop growth or kill the organism.Some bacteria have proteins called porins that control which chemicals can get inside the bacteria. Because of this, some antibiotics can’t get into the organism’s interior surroundings. This makes the organism resistant to the drug. D’Costa et al. (2011) found that antibiotic resistance is also caused in part by changes in the drug targets. For example, some quinolones work by stopping topoisomerase IV and DNA gyrase from doing their jobs. If the genes that make these enzymes change, the enzymes they make will be different, and antibiotics may not work on the new enzymes. This makes bacteria resistant to antibiotics.

References

Almeida Da Silva, P. E., & Palomino, J. C. (2011). Molecular basis and mechanisms of drug resistance in Mycobacterium tuberculosis: classical and new drugs. Journal of antimicrobial chemotherapy, 66(7), 1417-1430.

D’Costa, V. M., King, C. E., Kalan, L., Morar, M., Sung, W. W., Schwarz, C., … & Golding, G. B. (2011). Antibiotic resistance is ancient. Nature, 477(7365), 457-461.

Kaye, K. S., & Pogue, J. M. (2015). Infections caused by resistant gram‐negative bacteria: epidemiology and management. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 35(10), 949-962.

Khadka, P., Ro, J., Kim, H., Kim, I., Kim, J. T., Kim, H., … & Lee, J. (2014). Pharmaceutical particle technologies: An approach to improve drug solubility, dissolution and bioavailability. Asian journal of pharmaceutical sciences, 9(6), 304-316.

Richter, M. F., & Hergenrother, P. J. (2019). The challenge of converting Gram-positive-only compounds into broad-spectrum antibiotics. Annals of the New York Academy of Sciences, 1435(1), 18.

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