Antibacterial Flashcards
What is the mechanism of action of beta-lactam antibiotics?
Inhibits transpeptidation
What is the mechanism of action of action of penicillin resistance in beta-lactams?
hydrolyze beta lactam ring by lactamases
What is the mechanism of action of penicillin resistance of pseudomonas?
change in porin structure in outer cell wall
What drug inhibits renal tubular reabsorption of penicillin?
probenecid
What are examples of long acting intramuscular preparations of penicillin?
Benzathine Penicillin and Procained Penicillin
What drug is given together with penicillin to exhibit an increased activity agains enterococci?
Aminoglycoside
Drugs that are anti-staphylococcal?
Cloxacillin Oxacillin Nafcillin Dicloxacillin Methicillin
Anti-staphylococcal drug that exhibits biliary clearance
Methicillin
Penicillin that are resistant to beta lactamase inhbitiion
Isoxazoyl penicillin
Cloxacillin Oxacillin Nafcillin Dicloxacillin Methicillin
An extended penicillin that can cause pseudomembranous colitis and rash
Ampicillin
Extended penicillins that undergoes enterohepatic recirculation
Ampicillin
Extended penicillin that is inactivated by beta-lactamase inhibitors
Ampicillin, Amoxicillin
Drugs that are susceptible to extended spectrum penicillin
HELPS
Haemophilus influenzae Escherichia coli Listeria monocytogenes Proteus mirabilis Salmonella sp Enterococci
Examples of antipseudomonal penicillins
- Carbenicillin
- Piperacillin
- Ticarcillin
Penicillins with greater activity agains gram negative infections
- Carbenicillin
- Piperacillin
- Ticarcillin
Penicillins that has a greater activity to pseudomonas, enterobacter and Klebsiella
- Carbenicillin
- Piperacillin
- Ticarcillin
Examples of antipseudomonal penicillins that are inactivated by penicillinase
- Carbenicillin
- Piperacillin
- Ticarcillin
These antipseudomonal penicillins has synergistic effect when combined with?
aminoglycosides
Different diseases associated with pseudomonas?
Pneumonia Sepsis Ecthyma gangrenosus UTI DM Otitis externa Mucopolysaccharidoses - cystic fibrosis Osteomyelitis Nosocomial infections Skin Infection
What are your first generation cephalosporins?
Cefadroxil Cefazolin Cephalothin Cephapirin Cepharadine Cephalexin
FADer, help me FAZ my PHarmacology boards
Indications for 1st generation cephalosporin
- Surgical prophylaxis
- Bone infections
- Skin and soft tissue infections
- UTI
Combining 1st generation cephalosporin and aminoglycosides can increase?
Nephrotoxicity
First generation cephalosporins are effective against?
PEK
Proteus mirabilis
Escherichia coli
Klebsiella pneumoniae
What are your second generation cephalosporins?
Cefamandole
Cefoxitin
Cefuroxime
Cefotetan
Foxy cousin wearing a Fur coat and drinking TEA
Second generation cephalosporins are effective agains what microorganisms?
Haemophilus
Proteus mirabilis
Escherichia coli
Klebsiella pneumoniae
This second generation cephalosporin has an improved action agains pneumococcos and H. influenza
Cefuroxime
This second generation cephalosporin has a good activity agains B. fragilis (used for abdominal and pelvic infections
Cefotetan and Cefoxitin
[What generation is this]
Cefaclor Loracarbef Cefprozil Cefmetazole Cefonicid
2nd generation
FAC LORA the PROfessional AZhOLE is still on the FONe
What are your third generation cephalosporins?
CefoTAXime
CefoPERAzone
CeftaziDIME
CefTIZOxime
CeFIXime
CefTRIAxone
Cefpodoxime proxetil Cefnidir Cefditoren pivoxil Ceftibuten Moxalactam
This generation of cephalosporin has a decreased gram positive coverage, and increased gram negative activity
Third generation
What cephalosporins are used for gonorrhea?
Ceftriaxone
Cefixime
What generation of cephalosporins are useful for pseudomonas, bacteroides, providencia, serratia?
third generation
Which third generation cephalosporin have renal excretion?
Cefoperazone
Ceftriaxone
Which third generation cephalosporin CANNOT cross the BBB
Cefoperazone
Cefixime
Which third generation cephalosporin are the most active against penicillin-resistant S. pneumoniae
Ceftriaxine
Cefotaxime
Which third generation cephalosporin are commonly used agains bacteroides?
Ceftizoxime
Which third generation cephalosporin has a good CNS penetration?
Ceftriaxone
What are your fourth generation cephalosporins?
Ceftaroline
Cefpiro
Cefepime
Taro, Piro, Fepi
These cephalosporins have a wide coverage against gram positive and gram negative bacteria
Third generation
What fourth generation cephalosporin can be used for MRSA
Ceftaroline
What are you anti-pseudomonal cephalosporins?
Ceftazidime
Cefepime
Cefoperazone
A novel cephalosporin, combined with tazobactam, used for the treatment of complicated urinary tract infections and itraabdominal infections
Ceftolozone
a carbapenem inhibits the renal metabolism of imipinem
cislastated
Which carbapenem has no activity agains pseudomonas and acinetobacter
Ertapenem
What renal enzyme metabolize imipenem?
dihydropeptidase
A monobactam used to treat Klebsiella, Pseudomonas, Serratia
Aztreonam
Which beta-lactamase inhibitor is not a good inhibitor of inducible chromosomal B lactamase (enterobacter, Pseudomonas, Serratia)
Sulbactam
Glycopeptides inhibit cell wall synthesis by binding to___
D-Ala-D-Ala terminus; prevents elongation and cross-linking
Which drug class will you use for drug-resistant, gram positive organisms?
Glycopeptide
What are your glycopeptide?
Vancomycin
Teicoplanin
Dalbavancin
Telavancin
How will you manage red man syndrome?
Slow the rate of infusion
Glycopeptides that are used for bacterial enterocolitis
Teicoplanin
Televancin
since they are not absorbed in the GIT
Among the glycopeptides, which has the longest half life?
Dalbavancin
What drugs are considered to be drugs of last resort?
Imipenem Amikacin Meropenem Linezolid Streptogramins Vancomycin
___ is a peptide antibiotic that interferes with a late stage in cell wall synthesis in gram positive organism
bacitracin
___ blocks incorporation of D-ala into pentapeptide side chain of the peptidoglycan
cycloserine
An agent used as a second-line agent in TB
cycloserine
___ binds to the cell membrane causing depolarization and rapid cell death
daptomycin
Daptomycin cant be used against pneumonia since it is inactivated by ____
pulmonary surfactants
___ acts on the cell wall by inactivating UDP-N-acetyglucosamine-3-enol pyruvyltransferase thereby preventing formation of NAM
fosfomycin
A 50s protease inhibitor that is a backup drug for salmonella, Rickettsia and bacteroides
Chloramphenicol
a 50s protease inhibitor that can cause idiosyncratic aplastic anemia and gray baby syndrome
Chloramphenicol
Chloramphenicol is bactericidal to these microorganisms
- H. influenza
- Neisseria
- Bacteroides
- S. pneumoniae
Gray baby syndrome is due to a decrease in ____
hepatic glucoronyltransferase
What are the examaples of protein synthesis inhibitors?
Aminoglycoside Tetracycyclines Chloramphenicol Erythromycin Lincozamide Linezolid Streptogramins
A 50S inhibitor that can cross the placenta and BBB
Chloramphenicol
A 30s protease inhibitor that can be used in peptic ulcer disease
tetracycline
A 30s protease inhibitor that can be used in SIADH
Demeclocycline
A 30s protease inhibitor that can be used in bronchitis, chlamydia, Rickettsia
Doxycycline
A 30s protease inhibitor that can cause tooth enamel dysplasia
Tetracycline
A 30s protease inhibitor that can cause reversible vestibulotoxicity
minocycline
A 30s protease inhibitor that are considered divalent, concommitant milk intake is not advised
Tetracycline
A 30s protease inhibitor that is excreted via the bile
Doxycyline
What is the resistance mechanism of tetracycline?
- development of efflux pumps for active extrusion of tetracycline
- formation of ribosomal protection
A 50s protease inhibitor (macrolide) causes what ECG changes
QT prolongation
Which macrolide cannot inhibit CYP450
Azithromycin
What macrolide is used in rare fulminant hepatic failure?
Telithromycin
What macrolide has the highest Vd, slowest elimination
Azithomycin
What is the resistance mechanism for macrolides?
- Efflux pumps
2. production of methylase enzyme
What are examples of lincosamides?
Clindamycin
A 50s binder used for endocarditis prophylaxis
Clindamycin
A 50s binder that can lead to pseudomembranous colitis
clindamycin
What is the mechanism of clindamycin resistance?
- Methylation of binding sites
2. Enzymatic inactivation
Clindamycin is used for anaerobes ___ (above/below) the diaphragm
above
Metronidazole is used for anaerobes ___ (above/below) the diaphragm
below
What are examples of streptogramin?
Quinupristin-Dalfoprisin
A 50s subunit binder used to treat drug-resistant staphylococcus and E. faecium
Quinupristin-Dalfopristin
What are examples of your Oxazolidinone
Linezolid
Tedizolid
What is the mechanism of action of you linezolid?
Binds to the 23S rRNA of 50s subunit
What will you give to treat drug-resistant Listeria, Corynebacterium?
Linezolid
Taking of linezolid and SSRIs can cause what syndrome
Serotonin Syndrome
What is the resistance pattern of linezolid?
decreased affinity of drug to binding site
Aminoglycosides exhibit these unique killing action
- Concentration-dependent killing action
- Time-dependent killing action
- Post-antibiotic effect
What is the major mode of excretion of aminoglycosides?
renal excretion
Among the aminoglycosides, this has the narrowest therapeutic window
Amikacin
What ribosomal subunit dies aminoglycosides bind to?
30S
What is the mechanism of resistance of aminoglycosides
plasmid-mediated
Streptomycin resistance is due to?
changes in the ribosomal binding site
What are examples of aminoglycosides?
Gentamicin Neomycin Amikacin Tobramycin Streptomycin
GNATS
What are the side effects of your aminoglycosides?
Nephrotoxicity
Ototoxicity
Teratogenicity
Aminoglycosides used for ocular infections
- Tobramycin
2. Gentamicin
Aminoglycosides can cause irreversible ___
ototoxicity
Amikacin can be used for ____
- Proteus
- E. coli
- Klebsiella
PEK - Enterics (Providencia, Pseudomonas, Serratia)
What aminoglycoside is used as second line drug for MDRTB
Amikacin
Aminoglycoside effective for bubonic plague
Streptomycin
Aminoglycoside effective for tularemia
Streptomycin
What aminoglycoside can cause congenital deafness
Streptomycin
Drug of choice used in elective bowel surgery
- Neomycin
- Kanamycin
- Paromomycin
What is the drug of choice for Kala-azar?
Kala-azar = Visceral Leishmaniasis
Paromomycin
Aminoglycosides that cause neuromuscular blockade
- Kanamycin
- Neomycin
- Paromomycin
How will you reverse the neuromuscular blockade caused by kanamycin, neomysin and paromomycin?
- Calcium gluconate
2. Neostigmine
What is the drug of choice for drug-resistant gonorrhea?
Spectinomycin
Harvey specter
What is the drug of choice for patients with gonorrhea but are allergic to penicillin?
Spectinomycin
Can cause anemia
This amonoglycoside has no cross resistance to other anti-gonorrheal drug
Spectinomycin
Can cause anemia
This amonoglycoside has no cross resistance to other anti-gonorrheal drug
Spectinomycin
Can cause anemia
Among the aminoglycosides, which is the most ototoxic?
- Kanamycin
2. Amikacin
Among the aminoglycosides, which is the most vestibulotoxic?
- Tobramycin
2. Gentamicin
Among the aminoglycosides, which is the most nephrotoxic?
- Tobramycin
2. Gentamicin
Among the aminoglycosides, that can usually cause skin reactions?
- Neomycin
2. Streptomycin
A protease inhibitor that inhibits the protein translocation used as topical agent against S. aureus
Fusidic acid
____ are weakly acidic compounds that have a common chemical nucleus resembling PABA
sulfonamides
What are your short acting sulfonamides
- Sulfacytine
- Sulfisoxazole
- Sulfamethizole
Site, Socks, Methi
What are your intermediate acting sulfonamides
- Sulfadiazine
- Sulfamethoxazole
- Sulfapyridine
Azine, metho, fire
What are you long acting sulfonamides?
Sulfadoxine
Antifolate drug structurally similar to folic acid; weak base that is trapped in acidic environment
Trimethoprim
Trimethoprim reaches high concentrations in these bodily fluids
- Prostatic fluids
2. Vaginal fluids
Sulfonamides are bacteriostatic inhibitors of folic acid synthesis. It competitively inhibits what enzyme
dihydropteroate synthase
___ are selective inhibitor of bacterial dihydrofolate reductase
Trimethoprim
Combination of TMP-SMX is ___ bactericidal/bacteriostatic?
bactericidal
___drug competes with PABA
sulfonamides
Resistance to TMP-SMX is due to?
plasmid-mediated
A sulfonamide used in burn infection that can cause metabolic acidosis and can penetrate eschar
Mefenide acetate
A sulfonamide used to treat P. jirovecii
Co-trimoxazole
What is the ration of TMP-SMX in co-trimoxazole?
1:5
Sulfonamide used only for lower UTI
Sulfisoxazole
What is the DOC for toxoplasmosis?
Sulfadiazine-Pyrimethamine
What sulfonamide is the 2nd line for malaria?
Sulfadoxine-Pyrimethamine
Sulfonamide that is co-administered with leucovorin to limit bone marrow toxicity
Pyrimethamine
Sulfonamide can displace protein binding affecting levels of these drugs?
- Warfarin
2. Methotrexate
DNA gyrase (Topoisomerase II) in gram negative organism prevents what in the DNA
prevents relaxation of supercoiled DNA
Topoisomerase IV in gram positive bacteria interferese with
separation of replicated chromosomal DNA during cell division
What are the resistance pattern of fluoroquinolones?
- Efflux pump
- Porin structure
- changes the sensitivity of the target enzyme via point mutation
What are example of your first generation fluoroquinolones?
- Nalidixic acid
- Oxolinic acid
- Cinoxacin
- Rosoxacin
What are example of your second generation fluoroquinolones?
- Ciprofloxacin
- Ofloxacin
- Norfloxacin
- Lomefloxacin
- Enoxacin
What are example of your third generation fluoroquinolones?
- Levofloxacin
- Gemflixacin
- Moxifloxacin
- Sparfloxacon
- Grepafloxacin
- Gatifloxacin
- Pazufloxacin
- Tosufloxacon
- Balofloxacin
What are example of your fourth generation fluoroquinolones?
- Trovafloxacin
- Alatrofloxacin
- Prulifloxacin
- Clinafloxacin
[What generation of FQ]
Urinary tract infections
1st generation
[What generation of FQ]
gram negative, gonococci, mycoplasma
2rd generation
[What generation of FQ]
gram positives, stretococci, enterococci
3rd generation
[What generation of FQ]
broad specturm, anaerobes
4th generation
2nd generation FQ used as 2nd line drug for TB
Ciprofloxacin
Intake of this anti-asthmatic drug enhances the toxicity of 2nd generation FQ
methylxanthinse (theophylline)
FQ that does not compete with probenecid
Moxifloxacin
3rd generation FQ used as 2nd line treatment for TB
Levofloxacin
What is the mode of clearance for moxifloxacin>
hepatic
3rd generation FQ used to treat C. trachomatis
Ofloxacin
What generation of FQ is also called respiratory quinolones
third generation
Levofloxacin can be used in CAP that is caused by
- Chlamydia
- Mycoplasma
- Legionella
Third generation FQ that can cause QT prolongation
- Levofloxacin
- Gemfloxacon
- Moxifloxacin
Third generation FQ that can cause hyperglycemia in DM patients
Gatifloxacon
Metronidazole belongs to what class of drugs
- Nitroimidazole
2. Antiprotozoal
What is the MOA of metronidazole?
Reactive reduction by ferredoxin forming free radicals that disrupt ETC
What is the DOC for amebiasis and giardiasis?
metronidazole
Used to treat Trichomonas and Garnerella
metronidazole
This forms reactive intermediate when acted upon by bacterial nitrofuran reductase
Nitrofurantoin
nitrofurantoin can be used in UTI except if it is caused by what organisms?
- Proteus
2. Pseudomonas
___ inhibits staphylococcal isoleucyl tRNA synthetase
mupirocin
topical DOC for impetigo
mupirocin
__ are cationic detergents that disrupt bacterial cell membrane, bind and inactivate endotoxin
polymixin
Polymixin is used are salvage therapy of these organisms
- Acinetobacter
- Enterobacteriacease
- Pseudomonas
These organism are resistant to polymixin
- Proteus
2. Neisseria
____ binds to the sigma subunit of RNA polymerase
Fidaxomycin
DOC for C. difficile colitis in adults
Fidaxomicin
What is the outpatient regimen of PID?
- Ceftriaxine 250mgIM
- Doxycyclin 100 mg BID PO x14
- Metronidazole 500mg PO BID for 14 days
What is the regimen A for parenteral treatment of PID
- Cefotetan 2g IV q12h or Cefoxitin 2g IV q6h
PLUS
- Doxycycline 100mg IV PO q12h
What is the regimen B for parenteral treatment of PID
- Clindamycin 900mg IV q8h
2. Gentamicin LD 2mg/kg then maintainance dose 1.5mg/kg q8h