Tetracyclines, Macrolides, Clindamycin, & others Flashcards Preview

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Flashcards in Tetracyclines, Macrolides, Clindamycin, & others Deck (60):
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Tetracyclines

Tetracycline
Doxycycline
Minocycline
Tigecycline

1

Tetracycline

Mechanism of action

Prevents bacterial protein synthesis by binding to the 30S ribosomal subunit

2

Prevents bacterial protein synthesis by binding to the 30S ribosomal subunit

Tetracycline

Mechanism of action

3

Tetracycline

Effects

Bacteriostatic activity against susceptible bacteria

4

Tetracycline

Clinical applications

Infections caused by mycoplasma, chlamydiae, rickettsiae, some spirochetes, malaria, H pylori, acne

5

Infections caused by mycoplasma, chlamydiae, rickettsiae, some spirochetes, malaria, H pylori, acne

Tetracycline

Clinical applications

6

Tetracycline

Pharmacokinetics, Toxicities, Interactions

Oral, mixed clearance (half-life 8 h), dosed every 6 h, divalent cations impair oral absorption, TOXICITY: Gastrointestinal upset, hepatotoxicity, photosensitivity, deposition in bone and teeth

7

Oral, mixed clearance (half-life 8 h), dosed every 6 h, divalent cations impair oral absorption, TOXICITY: Gastrointestinal upset, hepatotoxicity, photosensitivity, deposition in bone and teeth

Tetracycline

Pharmacokinetics, Toxicities, Interactions

8

Docycycline

Oral and IV; longer half-life (18 h) so dosed twice daily; nonrenal elimination; absorption is minimally affected by divalent cations; used to treat community-acquired pneumonia and exacerbation of bronchitis

9

Oral and IV; longer half-life (18 h) so dosed twice daily; nonrenal elimination; absorption is minimally affected by divalent cations; used to treat community-acquired pneumonia and exacerbation of bronchitis

Docycycline

10

Minocycline

Oral; longer half-life (16 h) so dosed twice daily; frequently causes reversible vestibular toxicity

11

Oral; longer half-life (16 h) so dosed twice daily; frequently causes reversible vestibular toxicity

Minocycline

12

Tigecycline

IV; unaffected by common tetracycline resistance mechanisms; very broad spectrum of activity against gram-positive, gram-negative, and anaerobic bacteria; nausea and vomiting are the primary toxicities

13

IV; unaffected by common tetracycline resistance mechanisms; very broad spectrum of activity against gram-positive, gram-negative, and anaerobic bacteria; nausea and vomiting are the primary toxicities

Tigecycline

14

Macrolides

Erythromycin
Clarithromycin
Azithromycin
Telithromycin

15

Erythromycin

Mechanism of action

Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit

16

Erythromycin

Effects

Bacteriostatic activity against susceptible bacteria

17

Erythromycin

Clinical applications

Community-acquired pneumonia, pertussis, corynebacterial and chlamydial infections

18

Community-acquired pneumonia, pertussis, corynebacterial and chlamydial infections

Erythromycin

Clinical applications

19

Erythromycin

Pharmacokinetics, Toxicities, Interactions

Oral, IV, hepatic clearance (half-life 1.5 h), dosed every 6 h, cytochrome P450 inhibitor, TOXICITY: Gastrointestinal upset, hepatotoxicity, QTc prolongation

20

Oral, IV, hepatic clearance (half-life 1.5 h), dosed every 6 h, cytochrome P450 inhibitor, TOXICITY: Gastrointestinal upset, hepatotoxicity, QTc prolongation

Erythromycin

Pharmacokinetics, Toxicities, Interactions

21

Clarithromycin

Oral; longer half-life (4 h) so dosed twice daily; added activity versus M avium complex, toxoplasma, and M leprae

22

Oral; longer half-life (4 h) so dosed twice daily; added activity versus M avium complex, toxoplasma, and M leprae

Clarithromycin

23

Azithromycin

Oral, IV; very long half-life (68 h) allows for once- daily dosing and 5-day course of therapy of community-acquired pneumonia; does not inhibit cytochrome P450 enzymes

24

Oral, IV; very long half-life (68 h) allows for once- daily dosing and 5-day course of therapy of community-acquired pneumonia; does not inhibit cytochrome P450 enzymes

Azithromycin

25

Telithromycin

Oral; unaffected by efflux-mediated resistance so is active versus many erythromycine-resistant strains of pneumococci; rare cases of fulminant hepatic failure

26

Oral; unaffected by efflux-mediated resistance so is active versus many erythromycine-resistant strains of pneumococci; rare cases of fulminant hepatic failure

Telithromycin

27

Lincosamide

Clindamycin

28

Clindamycin

Lincosamide

29

Clindamycin (lincosamide)

Mechanism of action

Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit

30

Clindamycin (lincosamide)

Effects

Bacteriostatic activity against susceptible bacteria

31

Clindamycin (lincosamide)

Clinical applications

Skin and soft tissue infections, anaerobic infections

32

Skin and soft tissue infections, anaerobic infections

Clindamycin (lincosamide)

Clinical applications

33

Clindamycin (lincosamide)

Pharmacokinetics, Toxicities, Interactions

Oral, IV, hepatic clearance (half-life 2.5 h, dosed every 6-8 houres, TOXICITY: Gastrointestinal upset, C difficil colitis

34

Oral, IV, hepatic clearance (half-life 2.5 h, dosed every 6-8 houres, TOXICITY: Gastrointestinal upset, C difficil colitis

Clindamycin (lincosamide)

Pharmacokinetics, Toxicities, Interactions

35

Streptogramins

Quinupristin-dalfopristin

36

Quinupristin-dalfopristin

Streptogramins

37

Quinupristin-dalfopristin (streptogramins)

Mechanism of action

Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit

38

Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit

Quinupristin-dalfopristin (streptogramins)

Mechanism of action

39

Quinupristin-dalfopristin (streptogramins)

Effect

Rapid bactericidal activity against most susceptible bacteria

40

Rapid bactericidal activity against most susceptible bacteria

Quinupristin-dalfopristin (streptogramins)

Effect

41

Quinupristin-dalfopristin (streptogramins)

Clinical applications

Infections caused by staphylococci or vancomycin-resistant strains of E faecium

42

Infections caused by staphylococci or vancomycin-resistant strains of E faecium

Quinupristin-dalfopristin (streptogramins)

Clinical applications

43

Quinupristin-dalfopristin (streptogramins)

Pharmacokinetics, Toxicities, Interactions

IV, hepatic clearance, dosed every 8-12 h, cytochrome P450 inhibitor, TOXICITY: Severe infusion-related myalgias and arthalgias

44

IV, hepatic clearance, dosed every 8-12 h, cytochrome P450 inhibitor, TOXICITY: Severe infusion-related myalgias and arthalgias

Quinupristin-dalfopristin (streptogramins)

Pharmacokinetics, Toxicities, Interactions

45

Chlorampheicol

Mechanism of action

Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit

46

Chlorampheicol

Effect

Bacteriostatic activity against susceptible bacteria

47

Chlorampheicol

Clinical applications

Use is rare in the developed world because of serious toxicities

48

Use is rare in the developed world because of serious toxicities

Chlorampheicol

Clinical applications

49

Chlorampheicol

Pharmacokinetics, Toxicities, Interactions

Oral, IV, hepatic clearance (half-life 2.5 h), dosage is 50-100 mg/kg/d in four divided doses, TOXICITY: Dose-related anemia, idiosyncratic aplasic anemia, gray baby syndrom

50

Oral, IV, hepatic clearance (half-life 2.5 h), dosage is 50-100 mg/kg/d in four divided doses, TOXICITY: Dose-related anemia, idiosyncratic aplasic anemia, gray baby syndrom

Chlorampheicol

Pharmacokinetics, Toxicities, Interactions

51

Oxazolidinones

Linezolid

52

Linezolid

Oxazolidinones

53

Linezolid (oxazolidinones)

Mechanism of action

Prevents bacterial protein synthesis by binding to the 23S ribosomal RNA of 50S subunit

54

Prevents bacterial protein synthesis by binding to the 23S ribosomal RNA of 50S subunit

Linezolid (oxazolidinones)

Mechanism of action

55

Linezolid (oxazolidinones)

Effect

Bacteriostatic activity against susceptible bacteria

56

Linezolid (oxazolidinones)

Clinical applications

Infections caused by methicillin-resistant staphylococci and vancomycin-resistant enterococci

57

Infections caused by methicillin-resistant staphylococci and vancomycin-resistant enterococci

Linezolid (oxazolidinones)

Clinical applications

58

Linezolid (oxazolidinones)

Pharmacokinetics, Toxicities, Interactions

Oral, IV, hepatic clearance (half-life 6 h), dosed twice-daily, TOXICITY: Duration-dependent bone marrow suppression, neuropathy, and optic neuritis, serotonin syndrome may occur when coadministered with other serotonergic drugs (eg, selective serotonin reuptake inhibittors)

59

Oral, IV, hepatic clearance (half-life 6 h), dosed twice-daily, TOXICITY: Duration-dependent bone marrow suppression, neuropathy, and optic neuritis, serotonin syndrome may occur when coadministered with other serotonergic drugs (eg, selective serotonin reuptake inhibittors)

Linezolid (oxazolidinones)

Pharmacokinetics, Toxicities, Interactions