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38 Cards in this Set
- Front
- Back
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Tetracyclines |
Doxycycline Minocycline (half-life: 16-18 hours) Demeclocycline (for SIADH) |
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Tetracyclines mechanism of action |
reversibly binds to 30S preventing binding of amino acid charged tRNA Bacteriostatic |
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Tetracyclines active against |
Chlamydia trachromatis Rickettsia Brucellosis V. cholerae H. pylori Mycoplasma pneumoniae Meningococcal carrier states (Minocycline) Acne (Minocycline) |
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Tetracycline pharmacokinetics |
impaired absorption by Dairy Products and Antacids due to formation of non-absorbable chelates with Calcium. Distributed well in the body, except minocycline, which is not effective for CNS infection |
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Doxycycline |
Excreted in bile, therefore used for treating infections in really compromised patients |
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Tetracyclines adverse effects |
Teeth discolouration Bone growth inhibition Vestibular problems (Minocycline and Doxycycline) Phototoxicity Toxicity in liver and kidney |
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Glycylcyclines |
Tigecycline similar to Tetracyclines |
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Tigecycline spectrum |
Broad spectrum MRSA Multidrug resistant S. pneumonia Acintobacter |
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Tigecycline Clinical uses |
Complicated skin infections Complicated intra-abdominal infections Community Acquired Pneumonia |
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Aminoglycosides |
Streptomycin Gentamicin Amikacin Tobramycin Neomycin |
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Aminoglycosides mechanism of action |
binds irreversibly to 30S subunit changing its structure Bactericidal |
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Aminoglycosides spectrum |
Only against Gram - aerobes because they need an oxygen-dependent process to be transported across the cell membrane |
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Aminoglycosides pharmacokinetics |
Given Parentral or topical (Neomycin) Concentration-dependant effect Post-antibiotic effect ONCE daily dosing can be used |
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Aminoglycosides adverse effects |
Accumulated in the renal cortex and in the endolymph andperilymph of the inner ear causing Nephrotoxic and Ototoxiceffects. Respiratory paralysis Allergic skin reactions and contact dermatitis (Neomycin) |
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Aminoglycosides clinical uses |
TB Tularemia Plague P. aeruginosa Brucellosis (in common with Tetracycline) Endocarditis |
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Spectinomycin |
related to Aminoglycosides Treatment of Gonorrhea |
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Macrolides |
Erythromycin Clarithromycin Azithromycin (3 days half-life) |
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Macrolides mechanism of action |
binds to the 50S subunit; blocks translocation Bacteriostatic or Bactericidal, depends on concentration and bacteria |
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Erythromycin spectrum |
mainly effective against Gram + organisms
DOC for C. diphtheria and Pertussis |
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Clarithromycin spectrum
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similar to Erythromycin + G- bacteria H. pylori |
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Azithromycin |
mainly active against G- bacteria Intracellular pathogens Legionnaire's disease DOC (CAP) |
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Macrolides pharmacokinetics |
Orally All acid-stable, except Erythromycin, thus given as enteric-coated tablets Food delays absorption of erythromycin and azithromycin, BUT increase that of clarithromycin Not distributed to CSF and brain |
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Macrolides metabolism |
Erythromycin and Clarithromycin inhibit CYP450, thus CI with drugs that rely on this enzyme |
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Macrolides excretion |
Erythromycin and Azithromycin excreted in bile Clartihromycin excreted in urine |
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Macrolides adverse effects |
GIT effects Liver toxicity: Cholestatic jaundice with Erythromycin Estolate (CI in pregnancy) |
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Clindamycin |
similar to Macrolides |
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Clindamycin spectrum |
Anaerobes |
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Clindamycin adverse effects |
Pseudomembranous Colitis |
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Chloramphenicol mechanism of action |
binds to 50S ribosome subunit; inhibiting protein synthesis Bacteriostatic or bactericidal, depends on organism |
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Chloramphenicol adverse effects |
Aplastic anemia Gary Baby Syndrome |
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Chloramphenicol clinical use |
Conjunctivitis (Topical) |
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Streptogramins mechanism of action |
binds to 50S ribosome subunit; inhibiting protein synthesis Bactericidal |
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Streptogramins spectrum |
VRSA and VRE (faecium NOT faecalis) MRSA |
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Streptogramins pharmacokinetics |
IV inhibit CYP450 |
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Streptogramins adverse effects |
Venous irritation Arthralgia and myalgia |
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Linezolid mechanism of action |
binds to 50S ribosomal subunit and inhibits formation ofinitiation complex (70S) Bacteriostatic, but Cidal against Streptococci |
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Linezolid spectrum |
VRSA and VRE (faecium AND faecalis) MRSA |
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Linezolid pharmacokinetics |
Taken orally or IV Does not inhibit CYP450 enzyme |
