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NUR1142 > Module 9 14 Macrolides Lincosamides Clindamycin > Flashcards

Module 9 14 Macrolides Lincosamides Clindamycin Flashcards

1
Q

Question

A

Answer

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2
Q

What are macrolides, and how do they work?

A

Macrolides are broad-spectrum antibiotics that inhibit bacterial protein synthesis.

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3
Q

Which macrolide is the oldest member of the family?

A

Erythromycin.

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4
Q

Name two newer macrolides that are derivatives of erythromycin.

A

Azithromycin and clarithromycin.

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5
Q

What are the routes of administration for azithromycin (Zithromax)?

A

Azithromycin can be administered orally (PO) and intravenously (IV).

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6
Q

What is the usual dosing interval for azithromycin (Zithromax)?

A

The usual dosing interval for azithromycin is every 24 hours.

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7
Q

What is the typical adult dosage for clarithromycin (Biaxin)?

A

The usual adult dosage for clarithromycin is 500-1000 mg.

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8
Q

How often is erythromycin administered orally (PO)?

A

Erythromycin is typically administered every 6 hours (PO).

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9
Q

What is the pediatric dosage range for erythromycin (PO)?

A

The pediatric dosage for erythromycin (PO) is 30-50 mg/kg.

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10
Q

What is the usual dosing interval for erythromycin administered intravenously (IV)?

A

Erythromycin is usually administered every 24 hours (IV).

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11
Q

What is the recommended dosage for azithromycin on day 1 for adults (PO)?

A

The recommended dosage for azithromycin on day 1 for adults is 500 mg.

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12
Q

What is the recommended pediatric dosage for azithromycin on days 1-2 (PO)?

A

The recommended pediatric dosage for azithromycin on days 1-2 is 10 mg/kg.

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13
Q

What is the recommended pediatric dosage for azithromycin on days 3-5 (PO)?

A

The recommended pediatric dosage for azithromycin on days 3-5 is 5 mg/kg.

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14
Q

What is the recommended dosage for azithromycin on day 2 for adults (PO)?

A

The recommended dosage for azithromycin on day 2 for adults is 250 mg.

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15
Q

What is the antimicrobial spectrum of erythromycin?

A

Erythromycin has a relatively broad antimicrobial spectrum.

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16
Q

In what types of infections is erythromycin considered a preferred or alternative treatment?

A

Erythromycin is considered a preferred or alternative treatment for various infections.

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17
Q

Is erythromycin generally considered a safe antibiotic?

A

Yes, erythromycin is considered one of the safer antibiotics.

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18
Q

Which antibiotic serves as a prototype for the macrolide family?

A

Erythromycin serves as a prototype for the macrolide antibiotic family.

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19
Q

What is tetracycline?

A

Tetracycline is a type of antibiotic.

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20
Q

Which class of antibiotics includes erythromycin?

A

Erythromycin belongs to the macrolide class of antibiotics.

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21
Q

What is linezolid?

A

Linezolid is an example of an oxazolidinone antibiotic.

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22
Q

What class of antibiotics does tigecycline belong to, and what is it used for?

A

Tigecycline belongs to the glycylcycline class of antibiotics and is used to treat various infections.

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23
Q

Which antibiotic falls into the “Other” category?

A

Clindamycin is a notable antibiotic in the “Other” category of antibiotics.

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24
Q

How does erythromycin inhibit bacterial protein synthesis?

A

Erythromycin inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit.

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25
Q

What is the usual effect of erythromycin on bacteria?

A

Erythromycin is usually bacteriostatic, but it can be bactericidal against highly susceptible organisms or at high concentrations.

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26
Q

Why is erythromycin selectively toxic to bacteria?

A

Erythromycin is selectively toxic to bacteria because it doesn’t bind to ribosomes in the cytoplasm of mammalian cells.

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27
Q

How does erythromycin differ from chloramphenicol in terms of mitochondrial inhibition?

A

Erythromycin cannot cross the mitochondrial membrane and, therefore, does not inhibit protein synthesis in host mitochondria, unlike chloramphenicol.

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28
Q

How does the antibacterial spectrum of erythromycin compare to that of penicillin?

A

Erythromycin has an antibacterial spectrum similar to penicillin.

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29
Q

What types of bacteria is erythromycin active against?

A

Erythromycin is active against most gram-positive bacteria and some gram-negative bacteria.

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30
Q

What factor determines the sensitivity of bacteria to erythromycin?

A

Bacterial sensitivity to erythromycin is determined in large part by the drug’s ability to gain access to the cell interior.

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31
Q

What is the role of erythromycin in treating Corynebacterium diphtheriae infections?

A

Erythromycin is the treatment of first choice for Corynebacterium diphtheriae infections.

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32
Q

When can erythromycin be used as an alternative to penicillin G?

A

Erythromycin can be used as an alternative to penicillin G in patients with penicillin allergy.

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33
Q

What is the preferred treatment for acute diphtheria, and what is its role in eliminating the diphtheria carrier state?

A

Erythromycin is the preferred treatment for acute diphtheria and is used to eliminate the diphtheria carrier state.

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34
Q

Which types of infections respond well to both macrolides and tetracyclines, and what are they used for in these cases?

A

Macrolides and tetracyclines are both first-choice drugs for certain chlamydial infections (urethritis, cervicitis) and pneumonia caused by Mycobacterium pneumoniae.

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35
Q

What are the three forms of oral erythromycin available, and what are their differences?

A

The three forms of oral erythromycin are erythromycin base, erythromycin stearate, and erythromycin ethylsuccinate. They differ in their stability in stomach acid and absorption characteristics.

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36
Q

Why were derivatives like erythromycin stearate and erythromycin ethylsuccinate developed?

A

Derivatives like erythromycin stearate and erythromycin ethylsuccinate were developed to improve the bioavailability of erythromycin.

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37
Q

How is bioavailability enhanced when erythromycin is administered as tablets with an acid-resistant coating?

A

Bioavailability is enhanced by the acid-resistant coating, which protects erythromycin in the stomach and allows it to dissolve in the duodenum for absorption in the small intestine.

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38
Q

How does the presence of food affect the absorption of different forms of erythromycin?

A

Generally, food reduces the absorption of erythromycin base and erythromycin stearate. However, it does not affect the absorption of erythromycin ethylsuccinate.

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39
Q

Which form of erythromycin is biologically active, and what is required for the derivatives to work?

A

Only erythromycin base is biologically active. The derivatives need to be converted to the base, either in the intestine or after absorption, to become effective.

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40
Q

Under what conditions do all the oral erythromycins produce equivalent responses?

A

All oral erythromycins produce equivalent responses when used properly, meaning the correct dosage and the effects of food are considered.

41
Q

What are the different forms in which erythromycin is available for administration?

A

Erythromycin is available in various oral forms, including the base and its derivatives. It is also available as erythromycin lactobionate for intravenous use.

42
Q

How do drug levels achieved with intravenous dosing of erythromycin compare to those achieved with oral dosing?

A

Intravenous dosing of erythromycin produces drug levels higher than those achieved with oral dosing.

43
Q

How well does erythromycin distribute in the body?

A

Erythromycin readily distributes to most tissues and body fluids in the body.

44
Q

What is the extent of erythromycin’s penetration into the cerebrospinal fluid (CSF)?

A

Erythromycin has poor penetration into the cerebrospinal fluid (CSF).

45
Q

Can erythromycin cross the placenta, and what are the observed effects on the fetus?

A

Erythromycin can cross the placenta, but no adverse effects on the fetus have been observed.

46
Q

How is erythromycin primarily eliminated from the body?

A

Erythromycin is primarily eliminated through hepatic (liver) mechanisms.

47
Q

Which enzyme in the liver is responsible for the metabolism of erythromycin?

A

Erythromycin is metabolized in the liver by the CYP3A4 isoenzyme of cytochrome P450.

48
Q

Where is erythromycin concentrated before its excretion, and how is it excreted from there?

A

Erythromycin is concentrated in the liver and then excreted in the bile.

49
Q

What percentage of erythromycin is excreted unchanged in the urine?

A

Approximately 10% to 15% of erythromycin is excreted unchanged in the urine.

50
Q

How is erythromycin generally regarded in terms of safety?

A

Erythromycin is generally considered safe and free of serious toxicity.

51
Q

Among antibiotics, how is erythromycin commonly characterized regarding its safety profile?

A

Erythromycin is often characterized as one of the safest antibiotics.

52
Q

What is the small but important risk associated with erythromycin?

A

Erythromycin carries a very small risk for sudden cardiac death due to QT prolongation.

53
Q

What are the most common side effects associated with erythromycin?

A

The most common side effects of erythromycin are gastrointestinal disturbances, including epigastric pain, nausea, vomiting, and diarrhea.

54
Q

How can the gastrointestinal side effects of erythromycin be reduced?

A

Administering erythromycin with meals can help reduce gastrointestinal side effects.

55
Q

Which erythromycin products are suitable for administration with meals to mitigate side effects?

A

Erythromycin products unaffected by food, like erythromycin ethylsuccinate and certain enteric-coated formulations of erythromycin base, can be administered with meals.

56
Q

What should patients do if they experience persistent or severe gastrointestinal reactions while taking erythromycin?

A

Patients who experience persistent or severe gastrointestinal reactions should notify their prescriber.

57
Q

What is the risk associated with high concentrations of erythromycin and prolonged QT intervals?

A

High concentrations of erythromycin can increase the risk of torsades de pointes, a potentially fatal ventricular dysrhythmia.

58
Q

What happens when erythromycin is combined with a CYP3A4 inhibitor, and how does it affect the risk of sudden cardiac death?

A

When erythromycin is combined with a CYP3A4 inhibitor, the risk of sudden cardiac death is increased by fivefold, resulting in approximately 6 extra deaths for every 100,000 patients using the drug.

59
Q

Who should avoid using erythromycin to minimize the risk of cardiac complications?

A

Erythromycin should be avoided by patients with congenital QT prolongation and those taking class IA or III antidysrhythmic drugs.

60
Q

Which specific drugs or categories of medications should patients avoid when using erythromycin due to the risk of cardiac complications?

A

Patients should avoid erythromycin if they are taking CYP3A4 inhibitors, including certain calcium channel blockers (verapamil and diltiazem), azole antifungal drugs (e.g., ketoconazole, itraconazole), HIV protease inhibitors (e.g., ritonavir, saquinavir), and nefazodone (an antidepressant) to minimize the risk of cardiac complications.

61
Q

How can erythromycin affect the plasma levels and half-lives of certain drugs, and what is the underlying mechanism?

A

Erythromycin can increase the plasma levels and half-lives of certain drugs by inhibiting hepatic cytochrome P450 drug-metabolizing enzymes, which poses a risk of toxicity.

62
Q

Name three drugs that may have elevated levels when combined with erythromycin, and why is this a concern?

A

Theophylline (used for asthma), carbamazepine (used for seizures and bipolar disorder), and warfarin (an anticoagulant) can have elevated levels when combined with erythromycin, raising the risk of toxicity. Close monitoring for signs of toxicity is necessary.

63
Q

How does erythromycin affect the antibacterial effects of chloramphenicol and clindamycin, and what is the recommendation for concurrent use?

A

Erythromycin prevents the binding of chloramphenicol and clindamycin to bacterial ribosomes, antagonizing their antibacterial effects. Consequently, concurrent use of erythromycin with these two drugs is not recommended.

64
Q

Name some drugs that should not be combined with erythromycin due to their potential to inhibit erythromycin metabolism.

A

Drugs that can inhibit erythromycin metabolism and should not be combined with it include verapamil, diltiazem, HIV protease inhibitors, and azole antifungal drugs.

65
Q

What are the therapeutic goals of erythromycin?

A

The therapeutic goals of erythromycin include the treatment of respiratory infections, infections caused by H. pylori, disseminated Mycobacterium, and serving as an alternative to penicillin in patients with penicillin allergy.

66
Q

Is there any specific baseline data recommended for patients using erythromycin?

A

No specific baseline data are indicated for patients using erythromycin.

67
Q

What type of monitoring is recommended for patients on erythromycin therapy?

A

No specific monitoring is recommended for patients on erythromycin therapy.

68
Q

In which patient population should erythromycin be used with caution, and why?

A

Erythromycin should be used with caution in patients with QT prolongation due to potential cardiac risks.

69
Q

How can you evaluate the therapeutic effects of erythromycin treatment?

A

You can monitor for indications of antimicrobial effects, such as a reduction in fever, pain, or inflammation.

70
Q

How can adverse gastrointestinal effects of erythromycin be minimized?

A

Adverse gastrointestinal effects can be reduced by administering erythromycin with meals.

71
Q

What is the potential risk associated with clindamycin use?

A

Clindamycin can increase the risk of severe Clostridium difficile-associated diarrhea (CDAD), which can be fatal.

72
Q

How are the indications for clindamycin affected by the risk of CDAD?

A

The indications for clindamycin are limited due to the risk of CDAD.

73
Q

For what type of infections is systemic use of clindamycin currently indicated?

A

Systemic use of clindamycin is currently indicated only for certain anaerobic infections located outside the central nervous system (CNS).

74
Q

What is the primary mechanism of action of clindamycin in bacterial cells?

A

Clindamycin binds to the 50S subunit of bacterial ribosomes, inhibiting protein synthesis.

75
Q

Why is concurrent use of clindamycin, erythromycin, and chloramphenicol not recommended?

A

The binding site of clindamycin overlaps with the binding sites for erythromycin and chloramphenicol, which may lead to antagonism of their effects.

76
Q

What are the consequences of the binding site overlap among clindamycin, erythromycin, and chloramphenicol?

A

Clindamycin, erythromycin, and chloramphenicol can antagonize each other’s effects when used concurrently, so there are no indications for such combination therapy.

77
Q

Which types of bacteria are susceptible to clindamycin?

A

Clindamycin is effective against most anaerobic bacteria, including gram-positive and gram-negative anaerobes, and most gram-positive aerobes.

78
Q

Are gram-negative aerobes generally susceptible to clindamycin?

A

No, gram-negative aerobes are generally resistant to clindamycin.

79
Q

Can you name some of the susceptible anaerobic bacteria to clindamycin?

A

Susceptible anaerobic bacteria to clindamycin include Bacteroides fragilis, Fusobacterium species, Clostridium perfringens, and anaerobic streptococci.

80
Q

Is clindamycin typically bacteriostatic or bactericidal?

A

Clindamycin is usually bacteriostatic, but it can be bactericidal if the target organism is especially sensitive.

81
Q

What can be a significant problem regarding resistance with clindamycin?

A

Resistance can be a significant problem, particularly with Bacteroides fragilis.

82
Q

Why is clindamycin frequently used as an alternative to penicillin?

A

Clindamycin is a common alternative to penicillin because of its effectiveness against gram-positive cocci.

83
Q

For which type of infections is clindamycin primarily employed, and why?

A

Clindamycin is primarily used for anaerobic infections located outside the central nervous system (CNS) because it does not cross the blood-brain barrier.

84
Q

What makes clindamycin the drug of choice for severe group A streptococcal infections and gas gangrene caused by Clostridium perfringens?

A

Clindamycin is the preferred treatment for these infections because it can rapidly suppress the synthesis of bacterial toxins.

85
Q

What is the mechanism of action of clindamycin?

A

Clindamycin is a lincosamide antibiotic that binds to the 50S subunit of bacterial ribosomes.

86
Q

What are the primary therapeutic uses of clindamycin?

A

Clindamycin is used for anaerobic infections located outside the central nervous system (CNS), including Clostridium perfringens and group A streptococcus.

87
Q

How does clindamycin metabolize and eliminate from the body?

A

Clindamycin undergoes hepatic metabolism and renal elimination, with poor distribution to cerebrospinal fluid (CSF).

88
Q

What is a notable adverse effect associated with clindamycin use?

A

Clindamycin is associated with the risk of Clostridium difficile-associated diarrhea (CDAD) and may decrease oral contraceptive activity.

89
Q

What class of antibiotics does linezolid belong to, and how does it affect bacterial ribosomes?

A

Linezolid is an oxazolidinone antibiotic that binds to the 23S portion of the 50S ribosomal subunit.

90
Q

What are the therapeutic uses of linezolid, and against which types of bacteria is it effective?

A

Linezolid is effective against certain gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium.

91
Q

What is CDAD, and what is its association with clindamycin use?

A

CDAD (Clostridium difficile-associated diarrhea) is the most severe toxicity linked to clindamycin use.

92
Q

What causes CDAD, and what type of bacterium is involved?

A

CDAD results from a superinfection of the bowel by Clostridium difficile, an anaerobic gram-positive bacillus.

93
Q

What are the typical symptoms of CDAD?

A

CDAD is characterized by profuse watery diarrhea, abdominal pain, fever, leukocytosis, and stools containing mucus and blood.

94
Q

When can CDAD symptoms develop in relation to clindamycin use?

A

CDAD symptoms can occur during clindamycin treatment or develop as long as 4 to 6 weeks after clindamycin withdrawal.

95
Q

What is the potential consequence of untreated CDAD?

A

Left untreated, CDAD can be fatal.

96
Q

What should patients on clindamycin be advised to report, and why?

A

Patients should report significant diarrhea (more than five watery stools per day) because it may indicate CDAD.

97
Q

What is the recommended course of action if C. difficile superinfection is diagnosed in a patient taking clindamycin?

A

Clindamycin should be discontinued, and the patient should be given oral vancomycin or metronidazole, which are the drugs of choice for eliminating C. difficile from the bowel.

98
Q

How soon does diarrhea typically cease after starting vancomycin for CDAD?

A

Diarrhea usually stops within 3 to 5 days after initiating vancomycin treatment for CDAD.

99
Q

What additional therapy is often necessary for CDAD, and what should be avoided?

A

Fluid and electrolyte replacement is usually indicated, and drugs that decrease bowel motility (e.g., opioids, anticholinergics) should be avoided as they may worsen symptoms.

NUR1142 (112 decks)

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