protein synthesis inhibitors Flashcards
Chloramphenicol binds reversibly to which subunit
50S
Tetracyclines bind reversibly to which subunit
30S
Inhibits peptide bond formation
Chloramphenicol
Prevents addition of amino acids to the growing peptide
Blocks binding of aminoacyl-tRNA to the acceptor site of the mRNA ribosome complex
Tetracyclines
Protein synthesis inhibitors active against chlamydia
Tetracyclines (Tigecycline, Eravacycline, Omadacycline)
Macrolides (Erythromycin, Azithromycin)
CAP, Syphilis, Leptospirosis, Acne, Lyme disease, Malaria prophylaxis, Amoebiasis
Doxycycline
Gastrointestinal ulcers caused by H. pylori
Tetracycline
Meningococcal carrier state
Minocycline
Inhibits renal actions of ADH (non microbial func)
Demeclocycline
Active against CONS, MRSA strains, VRE strains
Strep, Entero, gram (+) rods, Acinetobacter sp., anaerobes, Rickettsiae, Chlamydia sp., L. pneumophila, mycobacteria
Tigecycline, Eravacycline, Omadacycline
3rd line drug for TB
Tetracyclines
Penetrates Placenta and BBB
Chloramphenicol
Crosses placental barrier and is excreted in breast milk
Tetracyclines
Absorption impaired by multivalent cations (Ca, Mg, Fe, Al), dairy products, antacids, and alkaline pH
Tetracyclines
Tetracyclines eliminated nonrenally
Doxycycline and Tigecycline
Tetracyclines given IV
Tigecycline and Eravacycline
Bone marrow toxicity
Inhibition of RBC maturation
Aplastic Anemia
Gray Baby Syndrome
Chloramphenicol
Tooth enamel dysplasia
Irregularities in bone growth
Crown deformation (permanent teeth)
Fanconi syndrome
Tetracyclines
Photosensitivity
Demeclocycline
Vestibular toxicity
Doxycycline and Minocycline
Macrolides and Clindamycin bind to which subunit
50S
Backup drug for MRSA
Clindamycin
Toxic shock syndrome
Clindamycin + Penicillin G
Necrotizing fasciitis
Clindamycin
Penetrating wounds to the abdomen and gut
Clindamycin + Aminoglycoside or cephalosporin
Prophylaxis of endocarditis in valvular disease
Pelvic, lung, and periodontal abscesses
Clindamycin
PJP in Aids
Clindamycin + Primaquine
AIDS-related toxoplasmosis
Clindamycin + Pyrimethamine
Dosage reduction is recommended for patients with creatinine clearances less than 30 mL/min
Clarithromycin
Torsades de pointes arrhythmia
Macrolides
Traverses the placenta and reaches the fetus but cannot enter BBB
Erythromycin
Penetrates into most tissues and phagocytic cells extremely well except for CSF
Azithromycin
Acute Cholestatic Hepatitis
Erythromycin
Pseudomembranous colitis
Clindamycin
Streptogramins and Lefamulin bind to which subunit
50S
Linezolid binds to which subunit
23S ribosomal RNA of the 50S subunit
Linezolid MOA
Prevents the formation of ribosome complex that initiates protein synthesis
Lefamulin MOA
Inhibits bacterial protein synthesis
Binding pocket closes around drug molecule, preventing tRNA from binding
Protein synthesis inhibitors with MRSA activity
Tedizolid
Quinupristin-Dalfopristin
Protein synthesis inhibitor active against gonorrhea
Lefamulin
Primarily eliminated in feces
Quinupristin-Dalfopristin
Arthralgia-myalgia
Quinupristin-Dalfopristin
Treatment of VRE infections, HCAP, CAP, skin and soft tissue infections, MDR-TB and Nocardia infections
Linezolid
Oxazolidinone that is 100% bioavailable
Linezolid
Thrombocytopenia
Anemia
Neutropenia
Optic and peripheral neuropathy
Lactic acidosis
Serotonin syndrome
Linezolid
Oxazolidinone for skin and soft tissue infection
Tedizolid
Which is higher protein binding: Linezolid or Tedizolid
Tedizolid (70%-90%)
For CAP and lower respiratory tract infections
Lefamulin
Protein synthesis inhibitor active against Lower respi infections, Atypical pathogens, Aerobic gram (+) and STI’s
Lefamulin
Causes congenital malformations
Lefamulin
Protein synthesis inhibitor that requires dose adjustments
Lefamulin