UNIT 12: PROTEIN SYNTHESIS INHIBITORS Flashcards
Protein Synthesis Inhibitors
Should not be taken with milk/dairy, antacids, or ferrous sulfate
Tetracyclins
Primary uses of Tetracyclins
Mycoplasma pneumoniae (in adults)
Chlamydiae
Rickettsiae
Vibrios
Spirochetes
Drug of choice for Vibrios
Tetracyclins
Secondary uses of Tetracyclins
Alternative to:
- Community-acquired pneumonia (CAP)
- Syphilis
Chronic bronchitis
Leptospirosis
Acne
The alternative to macrolides in treatment of syphilis
Doxycycline
Gastrointestinal ulcers caused by H. pylori
Tetracycline
Meningococcal carrier state
Minocycline
Lyme disease
Doxycycline
Malaria prophylaxis
Doxycycline
Amebiasis
Doxycycline
Tetracyclines (5)
Doxycycline
Minocycline
Tigecycline
Eravacycline
Omadacycline
The only tetracyclines excreted through the fecal route (2)
Doxycycline
Tigecycline
Short-acting (6-8 hours)
Tetracycline
Intermediate-acting (12 hrs)
Demeclocycline
Long-acting (16-18 hrs)
Doxycycline
Minocycline
Longer half-lives than long-acting tetracyclins (3)
Tetracycline (30-36 hrs)
Eravacycline
Omadacycline
Tetracycline resistance mechanisms (3)
Impaired influx/Increased efflux
Ribosome protection proteins
Enzymatic inactivation
Given to patients with excessive antidiuretic hormone (ADH)-secreting tumors
Demeclocycline
Cytochrome P450 inhibitors (2)
Erythromycin (Macrolides)
Quinupristin-dalfopristin (Streptogramins)
Gray baby syndrome
Chloramphenicol
Photosensitivity
Tetracyclines
Deposition in bone and teeth
Tetracyclines
Severe infusion-related myalgias and arthralgias (arthralgia-myalgia syndrome)
Quinupristin-dalfopristin
Streptogramins
Dose-related anemia
Idiosyncratic aplastic anemia
Chloramphenicol
Serotonin syndrome
Linezolid
Oxazolidinones
Duration-dependent bone marrow suppression
Linezolid
Oxazolidinones
Optic neuritis
Linezolid
Oxazolidinones
Cytochrome P450 3A4 substrate
Lefamulin
Pleuromutilins
Binds to 23S ribosomal RNA of 50S subunit
Linezolid
Oxazolidinones
Clinical use:
Pertussis
Corynebacterial and chlamydial infections
Erythromycin
Hematologic toxicity (thrombocytopenia)
Linezolid
Oxazolidinones
Activity against STI-causing organisms
Lefamulin
Pleuromutilins
Lefamulin
Pleuromutilins
Oxazolidinones (2)
Linezolid
Tedizolid
Quinupristin-dalfopristin
Streptogramins
Used with Penicillin G for toxic shock syndrome, necrotizing fasciitis
Clindamycin
Chlorine-substituted derivative of lincomycin
Clindamycin
Clinical use:
Skin and soft tissue infections
Clindamycin
Used with aminoglycoside or cephalosporin for:
Septic abortion
Penetrating wounds
Pelvic abscesses
Pelvic inflammatory disease
Lung and periodontal abscesses
Clindamycin
Clinical use:
Infections caused by staphylococci or vancomycin-resistant strains of enterococci (E. faecium)
Quinupristin-dalfopristin
Streptogramins
Effective alternate for Pneumocystis jiroveci pneumonia in patients with AIDS
Clindamycin + Primaquine
For AIDS-related toxoplasmosis of the brain
Clindamycin + Pyrimethamine
Toxicity:
Colitis due to C. difficile
Clindamycin
Ketolides (2)
Telithromycin
Solithromycin
Minimally absorbed macrolide used to treat C. difficile infections
Fidaxomicin
Macrolides (4)
Erythromycin
Clarithromycin
Azithromycin
Fidaxomicin
Characterized by a macrocyclic lactone ring
Macrolides
Prototype drug of macrolides
Erythromycin
Prevents transpeptidation by blocking the polypeptide exit tunnel
Erythromycin
Destroyed by stomach acid and must be administered with enteric coating
Erythromycin
Traditional DOC for:
Corynebacterial infections (diptheria, corynebacterial sepsis)
Respiratory, neonatal, ocular, or genital chlamydial infections
Erythromycin
Combined with oral neomycin and kanamycin for colon preoperative operation
Oral erythromycin base
True or False
A higher dose of erythromycin is recommended for treating pneumonia caused by Legionella pneumophila
True
Causes gastroparesis (off-label use)
Erythromycin
Causes acute cholestatic hepatitis
Erythromycin
Causes gastrointestinal intolerance
Erythromycin
Derived from erythromycin by addition of a methyl group
Clarithromycin
Derived from erythromycin by addition of a methylated nitrogen
Azithromycin
Torsades de pointes arrhythmia
Azithromycin
Exacerbates myasthenia gravis
Telithromycin
Ketolides
Ketolide used for treatment of community-acquired pneumonia
Solithromycin
Increased risk of death with hospital-acquired and ventilator-associated pneumonia
Tigecycline
Drug of choice for most infections caused by Rickettsiae and Borrelia sp.:
Rocky Mountain Spotted fever
Lyme disease
Tetracycline
Oral tetracycline of choice for most indications
Doxycycline
Tooth enamel dysplasia
Tetracyclines
Fanconi syndrome
Outdated tetracyclines
Candidiasis (oral and vaginal)
Tetracyclines
Chloramphenicol
Neither an inducer nor an inhibitor of cytochrome P450 enzymes
Linezolid
Oxazolidinones
Inhibits protein synthesis by interfering with the formation of initiation complexes and with aminoacyl translocation reactions
Clindamycin