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1st generation cephalosporins clinical uses (name the drugs)
Sugical prophylaxis Soft tissue infections Cefazolin (p) Cephalexin (o) Cefadroxil (o)
2nd generation cephalosporins clinical uses (name the drugs)
intra-abdominal infections Cefoxitin (p) Cefotetan (p) Cefuroxime (o) Cefprozil (o) 3b .
what is the purpose of this? 4a .All lactams have sulfur in their structure.
increase lipid solubility and hypersensitivity 4b .
Aminoglycoside toxicity 5a .
nephrotoxicity ototoxicity not for pregnant neuromuscular blockade 5b .
Aminoglycosides Chloramphenicol Macrolides Tetracyclines Streptogramins Linezolid Clindamycin Tigecycline 6a .
Inhibit bacterial protein synthesis (translation) 6b .
Aminoglycosides are bacteriostatic? 7a .
..False.unique to this group Cause misreading of mRNA template 7b ...Bacteriocidal.
Aminoglycosides demonstrate concentration dependent killing? Does it demonstrate post-antibiotic effect? 8a .
high levels of antibiotic facilitate entry through cell wall and membrane Yes 8b .True .
Ampicillin Amoxicillin Ticarcillin Piperacillin 9a .
Extended Range Penicillins Think (more gram .use) amoxicillin = oral mode ampicilin = parenteral/oral 9b .
As one moves down the generations of cephalosporins what is the general trend in terms of spectrum of activity? 10a .
bacteria 10b .Tend to be more effective against Gram .
Augmentin 11a .
amoxicillin + clavulonic acid 11b .
Bacteroides infection would be suitable to be treated with Aztreonam 12a .
.False..NO Anaerobes 12b ..
clostridium and actinomyces are all relevant organisms to be treated with aminoglycosides 13a .Bacteroides.
False.dont treat anaerobes Killing mechanism is O2 dependent uptake 13b ...
Besides Clavulonic acid what are other Beta-Lactamase inhibitors? 14a .
Unasyn P Piperacillin/Tazobactam .Augmentin 0 Ticarcillin/Clavulanic Acid .Timentin P Ampicillin/Sulbactam .Zosy P 14b .Sulbactam Tazobactam Amoxicillin-Clavulanic Acid .
Blurred vision GI disturbances Prolonged QT interval Exacerbation of Myasthenia gravis 15a .
Telithromycin Toxicity symptoms 15b .
Cefatrixone treats what the best? 16a .
Lyme 16b .3rd generation -> H Influenzae and Gram -.
Cefazolin (p) Cephalexin (o) Cefadroxil (o) 17a .
First generation Cephalosporins 17b .
Cefepime (p) 18a .
4th generation cephalosporin 18b .
Cefepime is used to tx what? 19a .
4th generation cepha--> pseudomonas 19b .
Cefotaxime (p) Ceftriaxone (p) Ceftazidime (p) Cefdinir (o) 20a .
3rd generation cephalosporins 20b .
Cefotetan tx what the best? 21a .
2nd generation --> Bacteriodes 21b .
Cefoxitin (p) Cefotetan (p) Cefuroxime (o) Cefprozil (o) 22a .
Second generation cephalsporins 22b .
Ceftazidime used to tx what? 23a .
3rd generation --> pseudom 23b .
Cephalosporin Toxicity 24a .
abdominal pain) Bleeding diathesis Phlebitis Biliary obstruction 24b . vomiting. nausea.Allergic/Hypersensitivity Cross allergy/sensitivity bw penicillins and cephalosporins is uncommon Disulfiram-like reaction (cefoperazone) (ingestion with alcohol produced headache.
Cephalosporins DO NOT tx what? 25a .
LAME listeria atypicals MRSA enterococci 25b .
Cephalosporins excreted into biliary tract 26a .
Ceforperazone (3rd generation) Ceftriaxone (3rd) 26b .
Chloramphenicol's mechanism of action 27a .
binds 50s subunit inhibits peptidyl transferase bacteriostatic 27b .
Chloramphenicol's mechanism or resistance 28a .
plasmid mediated production of antibiotic inactivating enzyme (acetyl transferase) Reduced permeability of bacterial organism to drug 28b .
Clavulonic Acid 29a .
beta-lactamase inhibitor often used with penicillins to enhance action 29b .
Clindamycin is primary absorbed? 30a .
Orally and has has good tissue penetration (but not to CNS/eye) blocks translocation 30b .
Clindomycin used against what spectrum
Gram + and Anaerobes NOT ENTEROCOCCI
Clinical uses of aminoglycosides
less potent when used alone...often in combination synergistic with cell wall active drugs gram - nosocomial empirically for neonatal infections 1st and 2nd line against mycobacterial infections
Clinical Uses of penicillin
strep pharyngitis rheumatic fever prophylaxis syphilis 33b .
Clinical uses of Tetracyclines 34a .
prostatitis gingavitis SIADH 34b .
Concentrates in phagocytic cells and other tissues 35a .
Azithromycin 35b .
Concentrates in respiratory secretions 36a .
Daptomycin is used in all age groups?
False..not approved for children
Daptomycin mechanism of action and clinical uses
new lipopeptide antibiotic...IV only Cidal --> disrupts multiple aspects of bacterial plasma membrane function --> inhibits cell wall Resistance mechanism not yet defined Skin and soft tissue infections, sepsis, endocarditis (resistant gram + infections)
Difference in excretion bw tetracycline and doxycycline 39a .
tetra = urine doxy = feces 39b .
Do penicillin crosses into CNS. prostate and eye 40a .
Minimally 40b .
DOC for borellia bergdorfi? 41a .
Ceftriaxone --> 3rd generation 41b .
DOC for legionella 42a .
think atypical Think Macrolide KAPLAN FACT 42b .
DOC for nosocomial life threatening diseases 43a .
Imipenem/Meropenem 43b .
DOC for oral treatment of animal bites 44a .
Augmentin (ampicillin + clavulonic) 44b .
DOC for Rocky Mountain Spotted Fever 45a .
tetracycline 45b .
TB and Bubonic blague 46a .DOC for tularemia.
Streptomycin aminoglycoside KAPLAN FACT 46b .
DOC of Atypical Mycobacteria 47a .
Clarithromycin (macrolide) 47b .
DOC of Atypical Organisms 48a .
macrolides/ketolides 48b .
DOC of C Diff 49a .
Metronidazole May have to use it after ampicillin side effect 2nd DOC = oral vancomycin KAPLAN FACT 49b .
DOC of Salmonella (typhoid) and bordatella pertussis 50a .
Azythromycin (macrolide) 50b .
DOC to treat syphillis 51a .
Benzathine-Penicillin (Penicillin G) Penicillinasesensitive 51b .
Drugs that are contraindicated in children 52a .
Daptomycin Tetracycline (tigecycline) 52b .
Enterococcus infection would be suitable to be treated with Aztreonam 53a .
.False..only use this drug with gram .rods 53b .
Extended Range Ampicillin/Amoxicillin Penicillins Tx what bugs? what clinical uses? 54a .
H influenzae.H. Strep pneumo Otitis media. HEELS Borrelia. H pylori. UTI. lyme 54b .B. Entorocci. pneumonia. Listeria. E coli. sinusitis.
Give an example of an oxazolidione 55a .
Linezolid = first in class Blocks 50s initiation Bacteriostatic 55b .
Gray-Baby Syndrome 56a .
Chloramphenicol can be conjugated because of immaturity/decreased levels of glucuronsyl transferase 56b .
Groups/Names of drugs that inhibit bacterial protein synthesis (translocation) 57a .
Aminoglycosides Chloramphenicol Macrolides Tetracyclines Streptogramins Linezolid Clindamycin Tigecycline 57b .
Idiosyncratic/dose related aplastic anemia 58a .
chloramphenicol toxicity 58b .
If i use combo a tetracycline with a beta lactam how would you describe the relationship? 59a .
Antagonistic Static and Cidal 59b .
If it ends in "thromycin" 60a .
Administered with Cilastatin which inhibits renal inactivation (dehydropeptidase effect) to prevent kidney metabolism from occurring too quickly Dont mix...co-administer Possible seizure side effect
Imipenem toxicity can cause
seizures and/or renal failure
Inhibit cell wall synthesis (6 categories/drugs) 63a .
Penicillins Cephalosporins Aztreonam Meropenem/Imipenem Vancomycin Daptomycin 63b .
Inhibits cytochrome P450 64a .
Chloramphenicol Macrolides (exception = azithromycin) 64b .
Jarish Herxheimer 65a .
Systemic side effects results from penicillin during treatment of syphillis Also seen with Tetracyclines 65b .
Linezolid has oral bioavailability? 66a .
yes 100% 66b .
Linezolid mechanism of resistance 67a .
decreased affinity of antimicrobial agent to bacterial target site (target alteration) 67b .
Linezolid would be preferred over which cell wall inhibitor? 68a .
Vancomycin It has better penetration into the lung to fight pneumonias 68b .
Loves the bone and stays active Used to tx osteomyelitis 69a .
Clindamycin Kaplan fact 69b .
Macrolides mechanism of action 70a .
bind to 50s subunit prevents ribosomal translocation down mRNA Bacteriostatic 70b .
Mechanism of action of Aminoglycosides 71a .
Binds to 30s subunit of bacterial ribosome Bacteriocidal Inhibitor of protein synthesis 71b .
Mechanism of action of synercid 72a .
binds to 50 s prevents translocation Bacteriocidal 72b .
Mechanism of Resistance of Macrolides 73a .
production of inactivating enzyme (methyltransferases) Target alteration that alters 50s binding increased efflux decrease permeability 73b .
Most potent lactam 74a .
Imipenem/meropenem 74b .
Name 3 tetracyclines 75a .
doxycycline minocycline (tigecycline) tetracycline Kaplan fact: demeclocyline 75b .
Only one in its class (protein translation inhibitor) Rarely used today in the US because of feared toxicity 76a .
Chloramphenicol 76b .
Oxacillin Nafacillin Dicloxacillin Methicillin Cloxacillin 77a .
PenicillinaseResistant Penicillin 77b .
Penicillin G and V used to tx all strains of 78a .
Syphilis GAS (strp pyogenes) 78b .
Pharmacology of Aminoglycosides? Oral? excretion? activity is _____ dependent 79a .
acidosis may decrease activity 79b .Not absorbed orally. they are polar Renal excretion pH dependent .
Precludes widespread use: drug interactions. phlebitis 40%. jaundice 30%. arthralgia and myalgia 20% 80a .
Synercid Toxicity 80b .
Probenecid 81a .
Blocks Penicillin Excretion 81b .
Protein Inhibitors Contraindicated in pregnancy 82a .
Aminoglycosides Tetracycline Macrolides (except azithromycin) 82b .
These protein synthesis inhibitors work on the 30s subunit 83a .
Aminoglycosides block initiation Tetraclycines block A site 83b .
These Protein Synthesis inhibitors work on the 50s subunit 84a .
Linezolide .blocks initiation Streptogramins block A site Chloramphenicol blocs peptide bond Macrolides/Clindamycin blocks translocation 84b .
Psuedotumor Cebri 85a .
Tetracycline toxicity (tigecycline) impairs CSF reabsorption -> increase cranial pressure 85b .
Pyloric Stenosis when used in infants 86a .
Macrolide toxicity KAPLAN FACT --> macrolides increase GI distress by stimulating motlin receptors --> increased peristalsis 86b .
Red Man syndrome.other side effects in same drug? 87a ...
Hypersensitivity Type 1 Ameliorated by slow infusion Vancomycin Toxicity Nephrotoxicity Ototoxicity 87b .
Side effect of this drug can be contact dermatitis 88a .
aminoglycoside Found in triple Ab ointment (neosporin) used topically KAPLAN FACT 88b .Neomycin .
Side effects include transient muscle weakness. myalgias 89a .
Daptomycin 89b .
Side effects of Penicililn Toxicity 90a .
anemia (coombs +) nephritis (especially Methicillin) drug fever 90b . diarrhea Seizures Hametologic -penias.Allergic hypersensitivity. urticaria GI distress. rash.
Single most effective antibiotic in terms of ease of distribution (very lipophilic) 91a .
Chloramphenicol 91b .
.Someone has a macrolide resistnat strain of pneumococci..what drug do I give 92a .
Telithromycin 92b .
Someone Has a Staph infection. what would be the progression of drugs to use to try to cure? 93a .
Penicillin/Methicillin --> Vanco --> Linezolide --> Daptomycin 93b .
.Someone is allergic to Penicillin.what drug should i give them? 94a . and has a Pseudomonal infection..
rods NO CROSS ALLERGENICITY WITH PENICILLS/CEPHALOSPORINS 94b .AZTREONAM resistant to beta lactamases Tx gram .
Specturm of Linezolid 95a .
All aerobic gram + organisms especially resistant strains 95b .
Streptogramins (Synercid) typically used to treat? 96a .
VRSA/VRE according to Kaplan 96b .
Streptomycin (p) Tobramycin (p) Amikacin (p) Gentamicin (p/t) Neomycin (p/t) 97a .
examples of aminoglycosides 97b .
Tetracycline mechanism of action 98a .
Bacteriostatic Binds reversible to 30s subunit of ribosome Inhibits A-site 98b .
Tetracycline mechanism of resisitance 99a .
facilitated efflux of drug decreased entry 99b .
Tetracycline toxicity 100a .
nausea.GI . diarrhea Fetal and childhood effects on bones and teeth Liver necrosis with doxy Nephrotoxic Photosensitivity/toxicity --> get rash in sun 100b . abd pain.
why? 101a ...Tetracyclines cannot be taken with food.
chelators (ca/mg) 101b .
Tetracyclines usually used to tx? 102a .
chlamydia. borrelia. entamoeba) **macrolides are preferred DOC for atypicals 102b . rickettsia. chancroid.Atypicals (mycoplasma.
This cell wall inhibitor is known to have a "postantibiotic effect" 103a .
Daptomycin 103b .
This cell wall inhibitor is not a lactam 104a .
Vancomycin 104b .
This cephalosporin is known to cause biliary obstruction when rapidly infused 105a .
Ceftriaxone (3rd generation) --> excreted in bile 105b .
This macrolide is considered to be safer for use during pregnancy because it is more water soluble then the rest of its class and does not inhibit p450 106a .
Azithromycin 106b .
This penicillin causes interstital nephritis 107a .
Methicillin 107b .
This penicillin is mostly excreted into the biliary tract 108a .
Nafcillin 108b .
This protein synthesis inhibitor may be associated with incidence of pseudomembranous colitis? which cell wall inhibitor is related? 109a .
Clindamycin Ampiciliin 109b .
This specific tetracycline is metabolized in liver and can cause hepatic necrosis 110a .
Doxycycline 110b .
neutropenia Reversible Bone marrow suppression weak MAO inhibitor 111a .Thrombocytopenia.
Linezolid toxicity 111b .
Ticarcillin and Piperacillin tx what? 112a .
Proteus Piper > Ticar Tx mixed-intra abdominal abscesses 112b . Bacteroides and E.Gram negative microbes Especially Pseudomonas. Coli.
Tigecycline is used for what spectrum of diseases? and what clinical uses 113a .
MRSA. VRE Acinetobacter and other gram aerobes/anaerobes NOT PSEUDO synergistic with Rifampin Use: skin/stricture infections. MRSE.no kids 113b .. intra-abdominal infections..
Tigecycline mechanism of action 114a .
new glycylcycline derivative of minocycline for IV use only High affinity binding to 30s unit of ribosome to block A site No known resistance yet 114b .
Toxicity of this drug can lead to Neuromuscular Blockade 115a .
Aminoglycoside decrease ACh. similar to Botulism Gentamycin specifically 115b .
Treats gram bone infections 116a .
quinilones (dont confuse with clindamycin) KAPLAN FACT 116b .
Used for bell's palsy 117a .
tetracycline 117b .
Vancomycin mechanism of action 118a .
binds to D-ala-D-ala muramyl pentapeptide --> blocks transglycosylation -> block elongation of peptidoglycal cell wall 118b .
Vancomycin used to tx what organisms 119a .
MRSE..that is metronidazole) 119b ... Pnemococci (Gram +) C Diff (but not DOC.MRSA.
What are mechanisms of microbial resistance to penicillin? 120a .
formation of beta-lactamases (penicillinases) mutation of PBP targets (mrsa) change in porin structure (pseudo) 120b .
What are the carbapenems? What is a monobactam example? 121a .
Meropenem (p) Imipenem (p) Ertapenem (p) ex of mono = aztreonam (p) 121b .
What does first generation cephalosporins treat best? 122a .
Gram + (strep/staph). some Gram Cefazolin (p) 122b .
imipenem.What is a unique characteristic of aztreonam. and meropenem 123a .
All are resistant to beta-lactamases 123b .
What is penicillin's chief mechanism of action? 124a .
Bind PBPs in bacterial cytopalsmic membrane --> inhibit transpeptidation --> inhib crosslinking Bactericidal 124b .
What is reccommended dosage of Aminoglycosides to avoid toxicity? 125a .
1 or 2 large daily doses each day 125b .
What is Synercid? 126a .
streptogramin combinaton (quinupristin/dalfopristin) metabolized and excreted by the liver Only IV 126b .
What is the mechanism of reaction for aminoglycosides 127a .
Plasmid mediated formation of inactivating enzymes --> group transferases porin protein mutation decreased affinity of 30s subunit target 127b .
What is the mechanism of resistance of Vancomycin 128a .
D-ala-D-lactate mutation 128b .
What is unique about vancomycin 129a .
it is not a lactam used to tx Gram + IV only NO CNS 129b .
What organisms do Aminoglycosides work on? 130a .
aerobes Pseudo-Keeps Pseudomonas Klebsiella E coli Enterobacter Proteus Serratia some gram + 130b .Gram .
Where is tigecycline metabolized/excreted? 131a .
Liver/biliary tract 131b .
Which carbapenem is known to penetrate the CNS 132a .
Which carbapenem is not effective against anaerobes?
Which cephalosporins have been proven to reach good CNS levels?
3rd generation Cefotaxime (p) Ceftriaxone (p) Ceftazidime (p) Cefdinir (o)
Which generation cephalosporins used to tx meningitis? name the drugs? 135a .
3rd generation 3rd generation Cefotaxime (p) Ceftriaxone (p) Ceftazidime (p) Cefdinir (o) 135b .
Which generation of cephalosporins has the best effect against anaerobes? 136a .
2nd Cefoxitin (p) Cefotetan (p) Cefuroxime (o) Cefprozil (o) 136b .
Which penicillin is known to cause GI distress and lead to C DIFF superinfection (pseudomembrane collitis) 137a .
Ampicillin 137b .
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