Module 9 14 Cephalosporin Flashcards

1
Q

Question

A

Answer

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2
Q

What are cephalosporins?

A

Cephalosporins are a class of antibiotics with a structure and mode of action similar to penicillins.

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3
Q

How do cephalosporins affect bacteria?

A

Cephalosporins are bactericidal, meaning they kill bacteria.

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4
Q

What is one of the key advantages of cephalosporins in terms of their effectiveness?

A

Cephalosporins often show resistance to β-lactamases, enzymes that can inactivate β-lactam antibiotics.

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5
Q

What is the spectrum of activity for cephalosporins?

A

Cephalosporins are effective against a broad spectrum of pathogens, making them versatile antibiotics.

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6
Q

Are cephalosporins associated with high toxicity?

A

No, cephalosporins have low toxicity and are well-tolerated.

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7
Q

Which class of antibiotics is considered one of the most widely used groups in clinical practice?

A

Cephalosporins are among the most widely used groups of antibiotics in clinical practice.

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8
Q

Are cephalosporins bactericidal or bacteriostatic?

A

Cephalosporins are bactericidal antibiotics.

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9
Q

What is the mechanism of action of cephalosporins?

A

Cephalosporins bind to penicillin-binding proteins (PBPs) in bacterial cells.

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10
Q

What are the two main effects of cephalosporin binding to PBPs?

A

The two main effects of cephalosporin binding to PBPs are (1) disruption of cell wall synthesis and (2) activation of autolysins, which cleave bonds in the cell wall.

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11
Q

How does the damage to the bacterial cell wall lead to cell death?

A

Damage to the bacterial cell wall leads to cell lysis, resulting in bacterial death.

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12
Q

When are cephalosporins most effective against bacterial cells?

A

Cephalosporins are most effective against bacterial cells that are actively growing and dividing.

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13
Q

What is the mechanism of action of cephalosporins?

A

Cephalosporins bind to penicillin-binding proteins (PBPs) in bacterial cells.

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14
Q

What are the two main effects of cephalosporin binding to PBPs?

A

The two main effects of cephalosporin binding to PBPs are (1) disruption of cell wall synthesis and (2) activation of autolysins, which cleave bonds in the cell wall.

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15
Q

How does the damage to the bacterial cell wall lead to cell death?

A

Damage to the bacterial cell wall causes cell lysis, resulting in bacterial death.

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16
Q

When are cephalosporins most effective against bacterial cells?

A

Cephalosporins are most effective against bacterial cells that are actively growing and dividing.

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17
Q

How does bacterial resistance to cephalosporins occur?

A

Bacterial resistance can result from producing altered penicillin-binding proteins (PBPs) with low affinity for cephalosporins.

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18
Q

What is the significance of methicillin-resistant staphylococci (MRSA) in cephalosporin resistance?

A

MRSA produces altered PBPs, which makes it resistant to most cephalosporins.

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19
Q

Which cephalosporin has demonstrated activity against MRSA?

A

Ceftaroline, a fifth-generation cephalosporin, has shown activity against MRSA.

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20
Q

How are cephalosporins categorized into different “generations”?

A

Cephalosporins are categorized into generations based on the order of their introduction to clinical use.

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21
Q

What are the key differences between cephalosporin generations?

A

Each generation of cephalosporins differs in terms of antimicrobial spectrum, susceptibility to β-lactamases, and the ability to reach the cerebrospinal fluid (CSF).

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22
Q

How do characteristics change as you progress from the first-generation to the fifth-generation cephalosporins?

A

Generally, as you move from the first-generation to the fifth-generation cephalosporins, there is an increase in activity against gram-negative bacteria and anaerobes, resistance to destruction by β-lactamases, and the ability to reach the CSF.

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23
Q

What are the key differences between cephalosporin generations in terms of activity against gram-negative bacteria?

A

Activity against gram-negative bacteria generally increases as you move from the first generation to the fifth generation.

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24
Q

How does resistance to β-lactamases change across cephalosporin generations?

A

Resistance to β-lactamases generally increases as you progress from the first generation to the fifth generation of cephalosporins.

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25
Q

What is the difference in distribution to the cerebrospinal fluid (CSF) among cephalosporin generations?

A

The distribution to CSF generally improves as you move from the first generation to the fifth generation of cephalosporins.

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26
Q

Why are many cephalosporins administered parenterally (IM or IV) rather than orally?

A

Many cephalosporins have poor absorption from the gastrointestinal (GI) tract, making parenteral administration necessary.

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27
Q

How many cephalosporins can be administered orally in the United States?

A

There are 10 cephalosporins that can be administered orally in the United States.

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28
Q

Which cephalosporin can be administered both orally and by injection?

A

Cefuroxime is the cephalosporin that can be administered both orally and by injection in the United States.

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29
Q

What is the major route of elimination for cefazolin, a first-generation cephalosporin?

A

Renal elimination.

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30
Q

What is the half-life of cefprozil, a second-generation cephalosporin, in normal renal function?

A

1.3 hours.

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31
Q

In which generation of cephalosporins is ceftriaxone found, and what is its major route of elimination?

A

Ceftriaxone is a third-generation cephalosporin, and its major route of elimination is hepatic.

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32
Q

What is the half-life of cefepime, a fourth-generation cephalosporin, in normal renal function?

A

2 hours.

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33
Q

What is the half-life of ceftaroline, a fifth-generation cephalosporin, in normal renal function?

A

2.6 hours.

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34
Q

Do first- and second-generation cephalosporins reliably penetrate the cerebrospinal fluid (CSF) for the treatment of bacterial meningitis?

A

No, their penetration to the CSF is unreliable.

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35
Q

Which generations of cephalosporins generally achieve sufficient CSF levels for bactericidal effects?

A

Third, fourth, and fifth generations.

36
Q

How are most cephalosporins eliminated from the body?

A

Most cephalosporins are eliminated by the kidneys.

37
Q

What is the typical excretion mechanism for cephalosporins?

A

Excretion involves both glomerular filtration and active tubular secretion.

38
Q

How can probenecid affect the elimination of some cephalosporins?

A

Probenecid can decrease the tubular secretion of certain cephalosporins, prolonging their effects.

39
Q

Why do patients with renal insufficiency often require reduced dosages of most cephalosporins?

A

Reduced dosages are necessary to prevent the accumulation of cephalosporins to toxic levels.

40
Q

Is dosage reduction necessary for ceftriaxone in patients with renal impairment?

A

No, ceftriaxone is primarily eliminated by the liver, and dosage reduction is unnecessary in patients with renal impairment.

41
Q

What is the most common adverse event associated with cephalosporin use?

A

Hypersensitivity reactions, including maculopapular rash.

42
Q

When does a maculopapular rash typically develop in response to cephalosporin treatment?

A

Several days after the onset of treatment.

43
Q

Are severe immediate reactions, like bronchospasm and anaphylaxis, common with cephalosporin use?

A

No, severe immediate reactions are rare but can occur.

44
Q

What action should be taken if signs of allergy (e.g., urticaria, rash, hypotension, difficulty breathing) appear during cephalosporin treatment?

A

The cephalosporin should be discontinued immediately.

45
Q

What is the recommendation for patients with a history of cephalosporin allergy?

A

They should avoid cephalosporin drugs.

46
Q

Why is there potential for cross-reactivity between penicillins and cephalosporins?

A

Because of their structural similarities.

47
Q

What is the typical incidence of cross-reactivity in penicillin-allergic patients when given a cephalosporin?

A

Approximately 1%.

48
Q

Can patients with mild penicillin allergies use cephalosporins with safety?

A

Yes, they can often use cephalosporins with minimal concern.

49
Q

What is the recommendation regarding cephalosporin use for patients with a history of severe allergic reactions to penicillins?

A

Cephalosporins should not be given to such patients due to the potential for fatal anaphylaxis.

50
Q

Which cephalosporins can induce alcohol intolerance and a disulfiram-like reaction?

A

Cefazolin and cefotetan.

51
Q

What is the disulfiram effect, and what causes it?

A

The disulfiram effect is a reaction caused by the accumulation of acetaldehyde, and it results from the inhibition of aldehyde dehydrogenase.

52
Q

What is the recommendation for patients taking cefazolin and cefotetan concerning alcohol consumption?

A

They must avoid consuming alcohol in any form to prevent a disulfiram-like reaction.

53
Q

Which cephalosporins can interfere with Vitamin K metabolism and potentially inhibit the formation of clotting factors?

A

Cefotetan, cefazolin, and ceftriaxone.

54
Q

Why is caution necessary when combining these cephalosporins with other agents?

A

Because they can promote bleeding, and when combined with agents like anticoagulants, thrombolytics, NSAIDs, or antiplatelet drugs, the risk of bleeding increases.

55
Q

What are the key characteristics of cephalosporins as antimicrobial drugs?

A

Cephalosporins are broad-spectrum, bactericidal drugs with a high therapeutic index.

56
Q

How have cephalosporins been historically employed in the treatment of infections?

A

Cephalosporins have been widely and successfully used against a variety of infections.

57
Q

For which group of patients can cephalosporins be valuable alternatives, especially if they have a mild penicillin allergy?

A

Patients with mild penicillin allergy can consider cephalosporins as alternatives.

58
Q

How do the five generations of cephalosporins differ in their applications?

A

The five generations of cephalosporins have distinct applications.

59
Q

Are first- and second-generation cephalosporins commonly the preferred choice for most active infections?

A

No, first- and second-generation cephalosporins are rarely the preferred choice for active infections, except for infections caused by sensitive staphylococci.

60
Q

Which generation of cephalosporins is often preferred for treating several infections?

A

Third-generation cephalosporins are often the preferred therapy for various infections.

61
Q

In what capacity are fourth- and fifth-generation cephalosporins particularly effective?

A

Fourth- and fifth-generation agents are effective against resistant organisms.

62
Q

For which types of infections is the fifth-generation cephalosporin commonly used?

A

The fifth-generation agent is used to treat skin infections, including MRSA, and health care-associated pneumonias.

63
Q

Which generation of cephalosporins has the highest activity against gram-positive organisms such as staphylococci and streptococci?

A

The first-generation cephalosporins have the highest activity against gram-positive organisms.

64
Q

What is the preferred use of first-generation cephalosporins?

A

First-generation cephalosporins are used in patients with mild penicillin allergy and for surgical prophylaxis.

65
Q

Which organisms are targeted by second-generation cephalosporins?

A

Second-generation cephalosporins have a broader spectrum, including gram-positive and gram-negative organisms like Haemophilus influenzae, Klebsiella, pneumococci, and staphylococci.

66
Q

What are the preferred uses of second-generation cephalosporins?

A

Second-generation cephalosporins are used for otitis, sinusitis, and respiratory tract infections.

67
Q

Which generation of cephalosporins is preferred for treating meningitis and has broad activity against gram-negative organisms?

A

Third-generation cephalosporins are preferred for treating meningitis and have a broad spectrum against gram-negative organisms.

68
Q

Against which organisms are fourth-generation cephalosporins mainly effective, and what infections are they used for?

A

Fourth-generation cephalosporins are mainly effective against Pseudomonas aeruginosa and are used for hospital-acquired pneumonia and complicated intra-abdominal and urinary tract infections.

69
Q

What is the primary target of fifth-generation cephalosporins, and what types of infections are they used for?

A

Fifth-generation cephalosporins primarily target gram-positive organisms, especially methicillin-resistant Staphylococcus aureus (MRSA), and are used for MRSA-associated infections.

70
Q

What is the category of drugs that inhibit cell wall synthesis, and name the prototype drugs in this category?

A

The category of drugs that inhibit cell wall synthesis includes cephalosporins, carbapenems, and vancomycin.

71
Q

Which drug is a prototype of cephalosporins?

A

Cephalexin is a prototype of cephalosporins.

72
Q

Which drug is a prototype of carbapenems?

A

Imipenem is a prototype of carbapenems.

73
Q

Name a drug in the “other” category of drugs that inhibit cell wall synthesis.

A

Vancomycin belongs to the “other” category of drugs that inhibit cell wall synthesis.

74
Q

How many cephalosporins are currently available in the United States?

A

There are 19 cephalosporins available in the United States.

75
Q

Why can selecting among cephalosporins be challenging?

A

The similarities among cephalosporins within each generation are more pronounced than the differences.

76
Q

What is often the primary basis for choosing one cephalosporin over another in the outpatient setting?

A

Cost is often the primary basis for choosing a cephalosporin over another in the outpatient setting.

77
Q

Into which three main categories can the differences between cephalosporins be grouped?

A

The differences between cephalosporins can be grouped into three main categories: antimicrobial spectrum, adverse effects, and pharmacokinetics.

78
Q

What is the dosage range for Cefadroxil (PO) in adults, and what is the recommended dosage for children?

A

Adults: 1-2 g every 12-24 hours; Children: 30 mg/kg

79
Q

How often is Cefazolin (IM, IV) typically administered in adults, and what is the dosage range for children?

A

Adults: 2-12 g every 6-8 hours; Children: 80-160 mg/kg

80
Q

What is the recommended dosage and dosing interval for Cephalexin (PO) in adults and children?

A

Adults: 1-4 g every 6 hours; Children: 25-100 mg/kg

81
Q

What is the therapeutic goal of cephalosporin treatment?

A

The therapeutic goal of cephalosporin treatment is to treat infections caused by susceptible organisms.

82
Q

Why is it important to collect baseline data in cephalosporin therapy, and what type of data should be collected?

A

Baseline data helps identify the infecting organism and its sensitivity. Collect samples for culture.

83
Q

Is routine laboratory monitoring necessary during cephalosporin treatment?

A

No, routine laboratory monitoring is not required.

84
Q

Who should avoid cephalosporin treatment due to contraindications?

A

Patients with a history of allergic reactions to cephalosporins or severe reactions to penicillin should avoid cephalosporin treatment.

85
Q

How can you evaluate the therapeutic effects of cephalosporin treatment?

A

Monitor for indications of antimicrobial effects, such as reduced fever, pain, edema, and inflammation.

86
Q

What potential adverse effect should patients be instructed to report during cephalosporin treatment?

A

Patients should report any increase in stool frequency, as cephalosporins can increase the risk of Clostridium difficile infection.