Question

Which drug inhibits extended-spectrum \(\beta\)-lactamases including some cephalosporinases? (A) avibactam (B) clavulanate (C) sulbactam (D) tazobactam (E) monobactam

Short answer

The drug avibactam inhibits extended-spectrum β-lactamases including some cephalosporinases.

Step-by-step solution

Understanding the Question

We need to identify which drug from the options provided inhibits extended-spectrum β-lactamases (ESBLs) including some cephalosporinases. These enzymes are responsible for antibiotic resistance in bacteria, and certain inhibitors can block their action.

Analyzing Each Option

Let's assess each option: (A) Avibactam: A non-β-lactam β-lactamase inhibitor known to inhibit a broad range of β-lactamases, including ESBLs and some cephalosporinases. (B) Clavulanate: Commonly used to inhibit β-lactamases, but less effective on ESBLs and cephalosporinases. (C) Sulbactam: Acts as a β-lactamase inhibitor but not known for inhibiting ESBLs effectively. (D) Tazobactam: Effective against some β-lactamases, but not primarily for ESBLs. (E) Monobactam: This is more of an antibiotic rather than a β-lactamase inhibitor.

Selecting the Appropriate Answer

From our analysis, avibactam (Option A) is the only inhibitor known to effectively work against extended-spectrum β-lactamases as well as some cephalosporinases.

Key concepts

extended-spectrum β-lactamases (ESBLs)

Extended-spectrum β-lactamases, often abbreviated as ESBLs, are enzymes produced by certain bacteria. These enzymes can break down a wide variety of β-lactam antibiotics, which makes infections difficult to treat. ESBLs can hydrolyze the common penicillins and cephalosporins, rendering them ineffective. This situation poses a significant challenge in treating bacterial infections, as it limits the number of effective antibiotics. ESBL-producing bacteria are often found in hospital settings and can spread between patients if proper hygiene practices are not followed. To address this issue, scientists have developed β-lactamase inhibitors, like avibactam, which can block the action of ESBLs and restore the effectiveness of antibiotics.

antibiotic resistance

Antibiotic resistance is when bacteria develop the ability to survive exposure to antibiotics that would usually kill them. This is a natural phenomenon, but the misuse and overuse of antibiotics in both humans and animals have accelerated the process. Antibiotic resistance occurs when bacteria mutate or acquire resistance genes from other bacteria. This creates "superbugs" that are difficult to treat with standard medicines, leading to longer hospital stays, higher medical costs, and increased mortality. The presence of enzymes like ESBLs further complicates treatment options, as they destroy common antibiotics. Maintaining strict antibiotic prescription guidelines and promoting research for new medications are vital steps in combating antibiotic resistance.

cephalosporinases

Cephalosporinases are another type of β-lactamase enzyme. They specifically target cephalosporin antibiotics, breaking down their structure and nullifying their effectiveness. These enzymes are prevalent in certain bacteria, providing them with an advantage against numerous antibacterial treatments. Cephalosporinases are a concern because they contribute to antibiotic resistance patterns observed in clinical settings. Inhibitors like avibactam are crucial therapeutic agents. These can block the actions of cephalosporinases, making antibiotics effective once again. Using these inhibitors allows blocked bacterial enzymes to be bypassed, providing doctors with more choices to treat resistant infections.

pharmacological mechanism

The pharmacological mechanism explains how a drug works in conjunction with the body's biological systems. In the case of β-lactamase inhibitors, the pharmacological mechanism often involves directly binding to and inactivating the target enzyme. Avibactam, for example, binds to β-lactamases, including both ESBLs and cephalosporinases, stopping them from breaking down important antibiotics. By inhibiting these enzymes, avibactam allows antibiotics to continue their job of attacking harmful bacteria. This mode of inhibition can vary among different β-lactamase inhibitors, showcasing the specificity and range that certain medications might have. This variety underscores the importance of selecting the right inhibitor in clinical treatments.