Tetracyclines, Macrolides, Clindamycin, & others Flashcards

0
Q

Tetracycline

Mechanism of action

A

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

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1
Q

Tetracyclines

A

Tetracycline
Doxycycline
Minocycline
Tigecycline

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2
Q

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

A

Tetracycline

Mechanism of action

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3
Q

Tetracycline

Effects

A

Bacteriostatic activity against susceptible bacteria

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4
Q

Tetracycline

Clinical applications

A

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

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5
Q

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

A

Tetracycline

Clinical applications

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6
Q

Tetracycline

Pharmacokinetics, Toxicities, Interactions

A

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

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7
Q

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

A

Tetracycline

Pharmacokinetics, Toxicities, Interactions

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8
Q

Docycycline

A

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

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9
Q

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

A

Docycycline

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10
Q

Minocycline

A

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

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11
Q

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

A

Minocycline

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12
Q

Tigecycline

A

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

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13
Q

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

A

Tigecycline

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14
Q

Macrolides

A

Erythromycin
Clarithromycin
Azithromycin
Telithromycin

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15
Q

Erythromycin

Mechanism of action

A

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

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16
Q

Erythromycin

Effects

A

Bacteriostatic activity against susceptible bacteria

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17
Q

Erythromycin

Clinical applications

A

Community-acquired pneumonia, pertussis, corynebacterial and chlamydial infections

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18
Q

Community-acquired pneumonia, pertussis, corynebacterial and chlamydial infections

A

Erythromycin

Clinical applications

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19
Q

Erythromycin

Pharmacokinetics, Toxicities, Interactions

A

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

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20
Q

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

A

Erythromycin

Pharmacokinetics, Toxicities, Interactions

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21
Q

Clarithromycin

A

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

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22
Q

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

A

Clarithromycin

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23
Q

Azithromycin

A

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

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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
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Lincosamide
Clindamycin
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Clindamycin
Lincosamide
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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
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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
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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
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Quinupristin-dalfopristin
Streptogramins
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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
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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
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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