[3S] Protein Synthesis Inhibitors Flashcards
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Widely distributed to all tissues including the CNS/CSF and placenta
Chloramphenicol
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Chloramphenicol excretion
Renal; partly bile and feces
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS
Chloramphenicol ROA
IV
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS MOA
● Binds to 50S
● Inhibits peptide bond formation
● Drug interactions: Phenytoin, Tolbutamide, Chlorpropamide, Warfarin
Chloramphenicol
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Bacteriostatic
● Gr(+) aerobes
● Gr(+) anaerobes
● Gr(-) aerobes
● Gr(-) anaerobes
● Rickettsiae
Chloramphenicol
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Especially effective against:
● H. influenzae
● N. meningitidis
● Bacteroides
Chloramphenicol
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Inactive: Chlamydia
Chloramphenicol
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
GI disturbances & Oral or Vaginal Candidiasis
Chloramphenicol Tetracycline & Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
● Bone marrow: Inhibition of red cell maturation
● Aplastic anemia
● Gray Baby Syndrome
Chloramphenicol
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Absorption is affected by food
Tetracycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Tetracycline excretion
Renal & Biliary
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS
Tetracycline ROA
PO
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS MOA
● Bacteriostatic
● Bind to 30S
● Inhibits binding of aminoacyl-tRNA to the acceptor site
● Intracellular concentration
ALL Tetracyclines
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
H. pylori ulcers
Tetracycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
● Gram-positive and gram- negative + anaerobes
● Chlamydiae
● Mycoplasma pneumoniae
● Borrelia, spirochetes, Anaplasma phagocytophilum, Ehrlichia sp.
Tetracycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Mainly for ricketssiae (Rocky mountain spotted fever) and borrelia (Lyme disease)
Tetracycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
● Alters intestinal flora
● Esophageal ulceration
● Enterocolitis
Tetracycline & Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
● Bacterial superinfections (S. aureus, C. difficile)
● Bones and teeth damage: Enamel dysplasia Crown
deformation
● Hepatic toxicity
● Renal toxicity
Tetracyclin, Doxycycline & Demeclocycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
Fanconi Syndrome
Tetracycline & Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
● Renal tubular acidosis
● Nephrotoxicity
● Exacerbate pre-existing renal dysfunction
Tetracycline & Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Absorption is not affected by food
Doxycycline & Minocycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Doxycycline ROA
PO/IV
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Lyme disease
Tetracycline & Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Malaria prophylaxis
Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Amoebiasis
Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Primary & secondary syphilis (penicillin allergy)
Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
Vestibulotoxicity
Doxycycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Demeclocycline excretion
Biliary & renally
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Demeclocycline ROA
PO
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Off-label treatment for inappropriate secretion of antidiuretic hormones
Demeclocycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
ADH-secreting tumors
Demeclocycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
Photosensitivity (UV Light)
Demeclocycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Minocycline excretion
Mostly fecal
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS
Minocycline ROA
PO/IV
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Meningococcal carrier state
Minocycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS: Minocycline
____________ is preferred due to resistant cases
ciprofloxacin/rifampin
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
● Vestibular toxicity
● Exacerbate pre-existing renal dysfunction
Minocycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Tigecycline excretion
Nonrenal (biliary)
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS
Longest half-life
Tigecycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
● MDR organisms
● Treats skin and skin-structure infections, intra- abdominal infections and CAP
Tigecycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS
Tigecycline ROA
IV
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
● Gr(+)
o CoNS, MRSA, VRE, Strep, Enterococci,
● Gr(-)
o Enterobacteriaceae, MDR Acinetobacter, Chlamydia, L. pneumophilia
Tigecycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
Anaerobes, ricketssiae, mycobacteria
Tigecycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
INACTIVE AGAINST: Proteus, Providencia, Pseudomonas
Tigecycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
Nausea
● Significantly higher mortality rates
Tigecycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Eravacycline excretion
Bile & urine + feces (10-40%)
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS
Eravacycline ROA
IV
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
● MDR organisms
● Complicated intra-abdominal infections
● Tigecycline uses
Eravacycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS CLINICAL APPLICATIONS
NOT effective against UTI
Eravacycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS TOXICITIES
Tetracycline toxicities + dose adjusted if used alongside CYP3A inducers like rifampin
Eravacycline
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS
Omadacycline excretion
Bile
BROAD SPECTRUM PROTEIN SYNTHESIS INHIBITORS PKINETICS
Administered 4 hours after as these may decrease
before or meals/supplements absorption
Omadacycline