Beta-Lactam Antibiotics Overview

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Questions and Answers

Who discovered penicillin?

Alexander Fleming

Penicillin is a type of beta-lactam antibiotic.

True (A)

Which of the following is NOT a type of beta-lactam antibiotic?

  • Cephalosporins
  • Macrolides (correct)
  • Penicillins
  • Carbapenems

What is the primary mechanism of action of penicillin?

<p>Inhibition of cell wall synthesis</p> Signup and view all the answers

Which of the following is a major mechanism of bacterial resistance to penicillin?

<p>All of the above (D)</p> Signup and view all the answers

What is the common name for Benzylpenicillin?

<p>Penicillin G</p> Signup and view all the answers

Penicillin G is stable in acidic environments.

<p>False (B)</p> Signup and view all the answers

Which of the following penicillins is acid-resistant?

<p>Penicillin V (B)</p> Signup and view all the answers

Methicillin is still widely used to treat MRSA infections.

<p>False (B)</p> Signup and view all the answers

What are two examples of extended-spectrum penicillins?

<p>Amoxicillin and Ampicillin</p> Signup and view all the answers

Amoxicillin can be administered intravenously or orally.

<p>True (A)</p> Signup and view all the answers

What is the main adverse effect associated with ampicillin?

<p>Diarrhea</p> Signup and view all the answers

What is the name of the penicillinase resistant penicillin used in combination with clavulanate?

<p>Amoxicillin</p> Signup and view all the answers

Which of the following is a beta-lactamase inhibitor?

<p>Clavulanic acid (D)</p> Signup and view all the answers

Cilastatin is a beta-lactamase inhibitor.

<p>False (B)</p> Signup and view all the answers

What are the two main categories of cephalosporins based on their structure and activity?

<p>Generations and Activity</p> Signup and view all the answers

Which generation of cephalosporins has the broadest activity against gram-negative bacteria?

<p>Third generation (D)</p> Signup and view all the answers

Cefazolin belongs to the second generation of cephalosporins.

<p>False (B)</p> Signup and view all the answers

Which of the following cephalosporins is used intravenously?

<p>Cefotaxime (D)</p> Signup and view all the answers

Ceftriaxone has a long half-life, allowing for once-daily administration.

<p>True (A)</p> Signup and view all the answers

What is the mechanism of resistance to cephalosporins?

<p>Production of beta-lactamases</p> Signup and view all the answers

Which of the following cephalosporins is commonly used for dental infections?

<p>Cefuroxime axetil (A)</p> Signup and view all the answers

The most common adverse drug reaction to cephalosporins is hypersensitivity.

<p>True (A)</p> Signup and view all the answers

Which of the following cephalosporins is known to cause a disulfiram-like reaction when combined with alcohol?

<p>Cefoperazone (C)</p> Signup and view all the answers

What are the two main classes of carbapenems that are clinically relevant?

<p>Imipenem and Meropenem</p> Signup and view all the answers

Doripenem is a beta-lactam antibiotic with a narrow spectrum of activity.

<p>False (B)</p> Signup and view all the answers

What is the primary use of carbapenems?

<p>Treatment of serious, multidrug-resistant infections</p> Signup and view all the answers

Which of the following medications is a monobactam antibiotic?

<p>Aztreonam (D)</p> Signup and view all the answers

Monobacteria are not susceptible to beta-lactamases.

<p>True (A)</p> Signup and view all the answers

What are some common uses for aztreonam?

<p>Treatment of serious infections caused by gram-negative bacteria such as Pseudomonas aeruginosa.</p> Signup and view all the answers

Beta-lactamase inhibitors are effective against all types of beta-lactamases.

<p>False (B)</p> Signup and view all the answers

What is the mechanism of action of beta-lactamase inhibitors?

<p>They prevent the breakdown of beta-lactam antibiotics by bacterial enzymes.</p> Signup and view all the answers

Which of the following beta-lactam antibiotics is commonly combined with sulbactam?

<p>Amoxicillin (D)</p> Signup and view all the answers

Tazobactam is often combined with piperacillin for the treatment of serious infections.

<p>True (A)</p> Signup and view all the answers

What is the most common combination of amoxicillin and a beta-lactamase inhibitor?

<p>Amoxicillin-clavulanate (Augmentin)</p> Signup and view all the answers

Beta-lactam antibiotics are effective against viral infections.

<p>False (B)</p> Signup and view all the answers

Flashcards

Beta-Lactam Antibiotics

A class of antibiotics that are active against a broad spectrum of bacteria, including gram-positive, gram-negative, and anaerobic bacteria. Known for their efficacy in treating various infections.

Penicillins

Among the most commonly prescribed antibiotics, they work by inhibiting bacterial cell wall synthesis, ultimately leading to bacterial death. Highly effective against gram-positive bacteria, but some are also effective against gram-negative bacteria.

Penicillin G (Benzyl Penicillin)

The most common type of penicillin. It is effective against gram-positive bacteria, but is susceptible to breakdown by bacterial enzymes. This type is not acid stable..

Procaine Penicillin G, Benzathine Penicillin G

These forms of penicillin G are designed for longer-lasting effects, allowing for less frequent administration.

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Acid-Resistant Penicillins

These penicillins, like Phenoxymethylpenicillin, are a special subtype that can withstand stomach acids, enabling oral administration.

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Penicillinase-Resistant Penicillins

A group of penicillins specially designed to overcome the breakdown by certain bacterial enzymes. Effective against bacteria producing lactamases.

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Extended Spectrum Penicillins

These penicillins are designed to effectively target a broader range of bacteria, including those resistant to traditional penicillin options. They are subdivided into aminopenicillins and antipseudomonal penicillins.

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Aminopenicillins (Amoxicillin, Ampicillin, Bacampicillin)

This type of penicillin is effective against a broader spectrum of bacteria, including gram-negative bacteria. They are commonly used to treat urinary tract infections, respiratory tract infections, and other infections.

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Antipseudomonal Penicillins

These penicillins, like Piperacillin and Mezlocillin, are particularly effective against Pseudomonas aeruginosa, a type of bacteria that can be difficult to treat with other antibiotics.

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Penicillin G - Uses

This penicillin is used to treat several types of infections, including bacterial infections of the ear, throat, skin, and lungs.

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Amoxicillin - Dental Uses

Amoxicillin is a popular choice for treating various dental infections.

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Amoxicillin - Other Uses

Amoxicillin is widely used for a variety of infections, spanning several body systems.

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Superinfection

A possible side effect of penicillin use is an overgrowth of a different type of bacteria that is resistant to the antibiotics, potentially leading to a new infection. It is important to use antibiotics appropriately and complete the entire course of treatment to prevent this.

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Jarisch-Herxheimer Reaction

This rare reaction to penicillin can occur during syphilis treatment and involves a rapid destruction of the syphilis bacteria releasing toxins, leading to a sudden and severe illness.

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Cephalosporins

Another class of antibiotics that are structurally similar to penicillins and also work by inhibiting bacterial cell wall synthesis.

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First Generation Cephalosporins

These cephalosporins typically target gram-positive bacteria and are often used for skin infections, respiratory tract infections, and urinary tract infections. They are often the first choice for treating bacterial infections, particularly those affecting the urinary tract.

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Second Generation Cephalosporins

These cephalosporins have a broader spectrum of activity than their first generation counterparts, targeting not only gram-positive bacteria, but also some gram-negative bacteria.

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Third Generation Cephalosporins

This generation of cephalosporins offers even greater potency against a wide range of bacteria, including many gram-negative bacteria.

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Fourth Generation Cephalosporins

These cephalosporins are designed to overcome resistance to existing cephalosporins and are effective against many clinically significant gram-negative organisms.

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Fifth Generation Cephalosporins

This latest generation of cephalosporins is characterized by their even broader spectrum of activity and effectiveness against various resistant bacteria. They are particularly prominent in tackling drug-resistant infections.

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Mechanism of Action of Cephalosporins

They work by disrupting the synthesis of bacterial cell walls, leading to bacterial cell death. It is a primary mechanism by which many antibiotics work.

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Mechanism of Resistance to Cephalosporins

This refers to the ability of bacteria to develop resistance to cephalosporins. This can occur through various mechanisms, including producing enzymes that degrade the antibiotic or altering the bacterial cell wall to prevent the antibiotic from entering.

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Therapeutic and Prophylactic Uses of Cephalosporins

Cephalosporins have a variety of uses in treating infections, especially in both therapeutic and preventative scenarios. They are frequently used to treat a wide range of infections, including those involving the respiratory system, urinary tract, skin, and bones and joints. They can also be used as prophylactics, which means they can prevent infections from developing in the first place.

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Dental Use of Cephalosporins

Because of their effectiveness against various bacterial infections, first-generation cephalosporins are widely used in dentistry.

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Choice Cephalosporins for Serious Infections

They are particularly valuable for treating infections caused by certain types of bacteria such as Klebsiella, Enterobacter, Proteus, Serratia, and Haemophilus, commonly known as Enterobacteriaceae, which cause a variety of infections, particularly in the urinary tract and respiratory system.

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Cephalosporins for Typhoid Fever

Ceftriaxone, Cefotaxime, and Cefoperazone are effective against Salmonella typhi, the bacterium responsible for typhoid fever.

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Cephalosporins for Meningitis

Ceftriaxone, Cefotaxime, and Ceftizoxime are effective against different types of bacteria that can cause bacterial meningitis, including Neisseria meningitidis, Haemophilus influenzae, and Streptococcus pneumoniae.

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Cephalosporins for Meningitis - Pseudomonas

Combination therapy with aminoglycosides, such as gentamicin, is used to treat Pseudomonas aeruginosa-related meningitis, an infection often difficult to manage.

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Cephalosporins for Pneumonia

Ceftriaxone and Cefotaxime are effective against pneumococci and H. influenzae, common causes of bacterial pneumonia, making them suitable medications for pneumonia treatment.

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Cephalosporins for Anaerobic Infections

Cefoxitin, Cefotetan, and Cefotaxime are effective against Bacteroides fragilis, an anaerobic bacterium often responsible for infections in the abdomen, pelvic region, and other areas. Aminoglycosides may be necessary due to the anaerobic nature of the infection.

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Cephalosporins for Surgical Prophylaxis

Cefazolin is often used as a single-dose prophylactic measure before surgery to decrease the risk of post-surgical infections. Administering cephalosporins before surgery can help prevent infections that commonly develop in the surgical site or surrounding areas.

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Cephalosporins for Gonorrhea

Ceftriaxone and Cefixime, often given as a single dose, are effective treatments for gonorrhea, a sexually transmitted infection.

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Cephalosporins for Biliary Tract Infections

Cefoxitin, Cefotaxime, Cefuroxime, and Cefazolin are effective against various bacteria causing biliary tract infections, which are infections affecting the gallbladder, bile ducts, and surrounding areas.

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Cephalosporins for Bone and Joint Infections

Third-generation cephalosporins are often used for bone and joint infections, which can be difficult to treat. They are often effective against the bacteria causing these infections.

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Cephalosporins for Leptospirosis

Ceftriaxone and Cefotaxime are effective intravenously against Leptospira interrogans, the bacterium causing leptospirosis, a serious bacterial infection that can affect multiple organs.

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Cephalosporins for Lyme Disease

Cefuroxime is effective against Borrelia burgdorferi, the bacterium causing Lyme disease, a multisystem infectious disease transmitted through ticks.

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Study Notes

Beta-Lactam Antibiotics

  • Beta-lactam antibiotics are a class of antibiotics
  • They contain a beta-lactam ring
  • Key examples are Penicillins, Cephalosporins, Monobactams, and Carbapenems

History of Beta-Lactam Antibiotics

  • Alexander Fleming discovered penicillin
  • Penicillin played a crucial role in wartime medical care

Classification of Penicillins

  • Penicillin G (Benzylpenicillin):
    • Administered intravenously, intramuscularly, or orally
    • Effective against various gram-positive bacteria:
      • Streptococci, staphylococci, and some bacilli
    • Acid-labile and not effective orally in some forms
  • Penicillin V: Acid-resistant, can be taken orally; less potent, used for infections less susceptible to penicillin G
  • Penicillinase-resistant penicillins:
    • Examples: Methicillin, Cloxacillin, Dicloxacillin, Oxacillin, Flucloxacillin, Nafcillin
    • Resistant to penicillinase enzymes produced by some bacteria
    • Active against staphylococci (excluding MRSA)
  • Extended-spectrum penicillins:
    • Examples: Amoxicillin, Ampicillin, Bacampicillin
    • Active against a broader range of bacteria, including some gram-negative bacteria
    • Anti-pseudomonal penicillins (e.g., Piperacillin, Mezlocillin) are effective against Pseudomonas.
  • Repository Penicillins (Longer-acting):
    • Examples: Procaine penicillin, Benzathine penicillin, Fortified procaine penicillin
    • Release slowly when injected, providing prolonged antibiotic effects

Mechanism of Action of Penicillin

  • Bactericidal drug
  • Inhibits bacterial cell wall synthesis
  • Rapid action on growing and multiplying bacteria
  • Binds to penicillin-binding proteins (PBPs) interfering with peptidoglycan cross-linking
  • Cell wall deficient bacteria undergo lysis

Mechanism of Bacterial Resistance to Penicillins

  • Modification of penicillin-binding proteins (PBPs)
  • Inability of the drug to reach the target site (due to impermeability) in gram-negative bacteria
  • Active efflux pumps to remove the drug from the bacterial cell
  • Production of bacterial enzymes (e.g., β-lactamases) that inactivate the antibiotic by breaking the beta-lactam ring

Penicillins – Uses

  • Streptococcal infections (otitis media, pharyngitis, rheumatic fever, scarlet fever)
  • Pneumococcal infections
  • Meningococcal infections
  • Gonorrhea
  • Syphilis
  • Tetanus
  • Gas gangrene
  • Etc.

Penicillins – Adverse Reactions

  • Hypersensitivity (allergic reactions)
  • Anaphylaxis (severe allergic reaction)
  • Suprainfection (superinfection by other resistant bacteria)

Methicillin (Penicillinase Resistant Penicillin)

  • Highly penicillinase-resistant
  • Narrow spectrum – used to treat some Gram-positive bacteria.
  • Should be administered parenterally
  • Induces penicillinase production
  • Adverse effects: interstitial nephritis, hematuria, albuminuria

MRSA (Methicillin-Resistant Staphylococcus Aureus)

  • Insensitive to penicillinase-resistant penicillins, other β-lactams
  • Evolved through horizontal gene transfer → altered PBPs → fail to bind to penicillins
  • Treatment: Vancomycin, Linezolid, Ciprofloxacin

Cloxacillin

  • Highly penicillinase and acid-resistant
  • More active than methicillin
  • Less active against gram-negative bacteria than some other penicillins

Extended Spectrum Penicillins (ex. Ampicillin, Amoxicillin)

  • Retain the antibacterial spectrum of penicillin with activity against gram-negative organisms
  • Relatively susceptible to beta-lactamases

Ampicillin and Amoxicillin

  • These penicillins have similar properties:
  • Acid stable
  • Incomplete oral absorption
  • Food interference
  • Good spectrum against gram-positive pathogens
  • Partial excretion in bile
  • Primary excretion through kidney

Amoxicillin – Uses (Dental)

  • Pulpitis
  • Peri-apical Periodontitis
  • Periodontitis
  • Pericoronitis
  • Dental caries
  • Peri-apical abscess
  • Post-surgical infections
  • Gingivitis
  • Acute necrotizing ulcerative gingivitis

Amoxicillin – Uses (Other)

  • UTI, RTI, Meningitis, Gonorrhoea, typhoid fever, bacillary dysentery, Cholisystitis, etc.

Piperacillin

  • Increased activity against Pseudomonas and Klebsiella species
  • Acid-labile
  • Administered parenterally
  • Rapid excretion in the urine
  • Used for serious Pseudomonas or Klebsiella infections like UTIs

Cephalosporins

  • General class details
    • Beta-lactam antibiotics
    • Divided into four main generations (First through Fourth)
  • Mechanism of action: inhibit bacterial cell wall synthesis

Cephalosporin Classes

  • First generation:
    • Examples: Cephalexin, Cephradine, Cefadroxil, Cephaloridine
    • Primarily effective against gram-positive bacteria
    • Limited activity against gram-negative bacteria
    • Used in uncomplicated community-acquired infections
  • Second generation:
    • Examples: Cefaclor, Cefuroxime, Cefprozil, Loracarbef
    • Improved activity against gram-negative bacteria compared to first generation
    • Used for Infections such as UTIs
  • Third generation:
    • Examples: Cefotaxime, Ceftriaxone, Cefdinir, Cefixime, Cefpodoxime
    • Better gram-negative coverage
    • Used in various infections, including those requiring broader spectrum coverage against more resistant pathogens
  • Fourth generation:
    • Examples: Cefepime, Cefpirome, Cefacloridine
    • Broad-spectrum activity against both gram positive and negative bacteria
    • High resistance

Carbapenems (ex. Imipenem, Meropenem, etc.)

  • Very broad-spectrum activity against gram-positive and gram-negative bacteria, including many resistant organisms
  • Susceptible to bacterial beta-lactamases
  • Treatment for serious infections; combined with cilastatin for stability

Monobactams (ex. Aztreonam)

  • Monocyclic beta-lactams and resistant to beta-lactamases
  • Primarily active against aerobic gram-negative bacteria and Pseudomonas.

Beta-Lactamase Inhibitors

  • Clavulanic acid, sulbactam, and tazobactam
  • Given with beta-lactam antibiotics, such as penicillins or cephalosporins
  • Inhibits bacterial beta-lactamases, thereby improving the effectiveness of beta-lactams against bacteria that produce these enzymes

Combination Drugs (ex. Augmentin, Sulbactam + antibiotics)

  • Combining a beta-lactam antibiotic with a beta-lactamase inhibitor increases effectiveness against bacteria that produce these enzymes
  • Example combinations include: Clavulanic acid + amoxicillin (Augmentin), sulbactam + ampicillin.

General information (Uses, Adverse Effects, etc.)

  • Specific uses (e.g., skin infections, pneumonia, and surgical prophylaxis) are discussed for each antibiotic class and specific drugs mentioned.
  • Adverse effects (e.g., hypersensitivity, anaphylaxis, nephrotoxicity) are also highlighted for various agents.

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