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Beta-lactam drugs
Penicillins, Cephalosporins, Aztreonam, Imipenem
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able to kill the cell in any phase
Aminoglycosides and Fluoroquinolones
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Lincosamides
- Clindamycin, Lincomycin
- Protein synthesis inhibitors (50S)
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inhibits peptidyl transferase (50S)
Chloramphenicol
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dihydrofolate reductase inhibitor
trimethoprim
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Sulfa drug MOA
inhibits dihydropteroate synthetase
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Method of resistance to Chloramphenicol
Reduced uptake into cell
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Method of resistance to tetracycline
Active efflux from the cell
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resistance via low binding affinity for B-Lactam antibiotics
- Methicillin resistance by Staphylococci
- Penicillin resistance by Pneumococci and Enterococci
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method of resistance to aminoglycosides
Inactivation by enzymes
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method of resistance to sulfa
Overproduction of target
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blocks Alanine Racemase (1st step in cell wall synthesis)
Cycloserine
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binds the D-ala, D-ala terminus of the glycopeptide polymer and prevents the ultimate cross-linking accomplished by transpeptidase
Vancomycin
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inhibit transpeptidase --> block cross linking in cell wall synthesis
Beta lactams.
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-
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drugs w/ time-dependent bactericidal activity
Penicillins, carbapenems, cephalosporins, monobactams
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Lipopeptide that binds to membrane & cause rapid depolarization, resulting in a loss of membrane potential leading to inhibition of protein, DNA and RNA synthesis
Daptomycin
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Post antibiotic effect, t1/2 = 8 hr
Daptomycin
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Toxicity of Daptomycin
Myositis
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Which drug is alternate for Vancomycin?
Daptomycin
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Short t1/2 (30-60 mins), excreted in urine unchanged, poor penetration to CSF, Brain, Eye, Prostate, Phagocytic Cells
Penicillins
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cell wall synthesis inhibitors that dont have cross hypersensitivity w/ penicillins
aztreonam and vancomycin
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amoxicillin administered w/ what to inhibit beta lactamase?
Clavulanic acid
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Cefazolin, Cephalothin, Cephalexin
1st generation cephalosporins
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Cefuroxime, Cefamandole, Ceftoxitin, Cefotetan
2nd generation cephalosporin
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Cefotaxime, Ceftriaxone, Ceftazidime
3rd generation cephalosporin
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Cefepime
4th generation cephalosporin
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Disulfiram Reaction is present in...
Cefalozin, Cefamandole, Cefoperazone, metronidazole (Methylthiotetrazole ring)
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aztreonam is used to treat pseudomonas and serratia because..
it is resistance to beta lactamase
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metabolized in urinary tract brush border by dipeptidases to an inactive metabolite. Therefore, it will be ineffective in UTI
Imipenem
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Which drug need to be used w/ Cilastin in order to treat UTI?
Imipenem
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Not oral, but iv only. Renal out. Ototoxicity
Vancomycin
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Which condition would the use of Vancomycin orally be ok?
C diff enterocolitis
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regularly used to treat Sepsis, endocarditis caused by methicillin-resistant staphylococci
Vancomycin
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method of resistance replacement of the D-ala-D-ala with D-ala-D-lactate is towards which drug?
Vancomycin
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Sulfa drugs are bactericidal or bacterostatic?
bacterostatic
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Alteration of pteridine (dihydropteroate) synthase and Increased PABA or alternate pathway are resistant methods for which drug?
Sulfa
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Displace drugs from albumin binding sites for warfarin (antigoagulant), methotrexate (DFR blocker, Cancer drug), chlorpropamide (Insulin release), and tolbutamide (Insulin release)
sulfa
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Procaine and other drugs derived from PABA may interfere w/ activity of...
sulfa
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Stevens-Johnson rxn is induced by which drug?
fever, sore throat, and fatigue. Ulcers & other lesions begin to appear in mucous membranes, almost always in mouth & lips but also in genital & anal regions. Lesions in mouth usually extremely painful. Conjunctivitis. A rash of round lesions ~1inch arises on face, trunk, arms & legs, and soles of feet, but usually not on scalp.
sulfa
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Dihydrofolate reductase inhibitor
Trimethoprim
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DNA gyrase inhibitor
Cipro. Quinolones & fluoroquinolones
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How does aminoglycosides become bactericidal?
Cationic antibiotic molecules create fissures in the cell membrane
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Aminoglycosides
Streptomycin, gentamicin, tobramycin
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antibiotics w/ Post antibiotic effect
Daptomycin, aminoglycosides,
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Aminoglycoside side effects
Neuromuscular Blockade. Decr ACh release. Ototoxicity, nephrotoxicity
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Tetracycline toxicity
- Hypoplasia, teeth problems, hepatotoxicity in pregnant women, Fanconi's syndrome: impairmt in proximal tubular fxn
- of kidney and other renal dz
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Chloramphenicol toxicities
Gray baby syndrome. Bone marrow suppression --> asplastic anemia. optic neuritis
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