Tetracyclines, Macrolides, Clindamycin, & others Flashcards
Tetracycline
Mechanism of action
Prevents bacterial protein synthesis by binding to the 30S ribosomal subunit
Tetracyclines
Tetracycline
Doxycycline
Minocycline
Tigecycline
Prevents bacterial protein synthesis by binding to the 30S ribosomal subunit
Tetracycline
Mechanism of action
Tetracycline
Effects
Bacteriostatic activity against susceptible bacteria
Tetracycline
Clinical applications
Infections caused by mycoplasma, chlamydiae, rickettsiae, some spirochetes, malaria, H pylori, acne
Infections caused by mycoplasma, chlamydiae, rickettsiae, some spirochetes, malaria, H pylori, acne
Tetracycline
Clinical applications
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
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
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
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
Minocycline
Oral; longer half-life (16 h) so dosed twice daily; frequently causes reversible vestibular toxicity
Oral; longer half-life (16 h) so dosed twice daily; frequently causes reversible vestibular toxicity
Minocycline
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
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
Macrolides
Erythromycin
Clarithromycin
Azithromycin
Telithromycin
Erythromycin
Mechanism of action
Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit
Erythromycin
Effects
Bacteriostatic activity against susceptible bacteria
Erythromycin
Clinical applications
Community-acquired pneumonia, pertussis, corynebacterial and chlamydial infections
Community-acquired pneumonia, pertussis, corynebacterial and chlamydial infections
Erythromycin
Clinical applications
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
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
Clarithromycin
Oral; longer half-life (4 h) so dosed twice daily; added activity versus M avium complex, toxoplasma, and M leprae
Oral; longer half-life (4 h) so dosed twice daily; added activity versus M avium complex, toxoplasma, and M leprae
Clarithromycin
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
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
Telithromycin
Oral; unaffected by efflux-mediated resistance so is active versus many erythromycine-resistant strains of pneumococci; rare cases of fulminant hepatic failure
Oral; unaffected by efflux-mediated resistance so is active versus many erythromycine-resistant strains of pneumococci; rare cases of fulminant hepatic failure
Telithromycin
Lincosamide
Clindamycin
Clindamycin
Lincosamide
Clindamycin (lincosamide)
Mechanism of action
Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit
Clindamycin (lincosamide)
Effects
Bacteriostatic activity against susceptible bacteria
Clindamycin (lincosamide)
Clinical applications
Skin and soft tissue infections, anaerobic infections
Skin and soft tissue infections, anaerobic infections
Clindamycin (lincosamide)
Clinical applications
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
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
Streptogramins
Quinupristin-dalfopristin
Quinupristin-dalfopristin
Streptogramins
Quinupristin-dalfopristin (streptogramins)
Mechanism of action
Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit
Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit
Quinupristin-dalfopristin (streptogramins)
Mechanism of action
Quinupristin-dalfopristin (streptogramins)
Effect
Rapid bactericidal activity against most susceptible bacteria
Rapid bactericidal activity against most susceptible bacteria
Quinupristin-dalfopristin (streptogramins)
Effect
Quinupristin-dalfopristin (streptogramins)
Clinical applications
Infections caused by staphylococci or vancomycin-resistant strains of E faecium
Infections caused by staphylococci or vancomycin-resistant strains of E faecium
Quinupristin-dalfopristin (streptogramins)
Clinical applications
Quinupristin-dalfopristin (streptogramins)
Pharmacokinetics, Toxicities, Interactions
IV, hepatic clearance, dosed every 8-12 h, cytochrome P450 inhibitor, TOXICITY: Severe infusion-related myalgias and arthalgias
IV, hepatic clearance, dosed every 8-12 h, cytochrome P450 inhibitor, TOXICITY: Severe infusion-related myalgias and arthalgias
Quinupristin-dalfopristin (streptogramins)
Pharmacokinetics, Toxicities, Interactions
Chlorampheicol
Mechanism of action
Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit
Chlorampheicol
Effect
Bacteriostatic activity against susceptible bacteria
Chlorampheicol
Clinical applications
Use is rare in the developed world because of serious toxicities
Use is rare in the developed world because of serious toxicities
Chlorampheicol
Clinical applications
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
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
Oxazolidinones
Linezolid
Linezolid
Oxazolidinones
Linezolid (oxazolidinones)
Mechanism of action
Prevents bacterial protein synthesis by binding to the 23S ribosomal RNA of 50S subunit
Prevents bacterial protein synthesis by binding to the 23S ribosomal RNA of 50S subunit
Linezolid (oxazolidinones)
Mechanism of action
Linezolid (oxazolidinones)
Effect
Bacteriostatic activity against susceptible bacteria
Linezolid (oxazolidinones)
Clinical applications
Infections caused by methicillin-resistant staphylococci and vancomycin-resistant enterococci
Infections caused by methicillin-resistant staphylococci and vancomycin-resistant enterococci
Linezolid (oxazolidinones)
Clinical applications
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)
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