UNIT 11: INTRO TO ANTIMICROBIALS Flashcards
Enumeration
Narrow-Spectrum Penicillins (2)
Penicillin G
Penicillin V
Enumeration
Antistaphylococcal penicillins (4)
Very-Narrow Spectrum
Cloxacillin, dicloxacillin
Nafcillin
Oxacillin
Methicillin
Isoxazolyl Penicillins
Enumeration
Extended-spectrum penicillins (3)
Wider-Spectrum
Aminopenicillins (Ampicillin, Amoxicillin)
Carboxypenicillins (Carbenicillin, Ticarcillin)
Ureidopenicillins (Piperacillin)
Enumeration
Aminopenicillins (2)
Ampicillin
Amoxicillin
Enumeration
Carboxypenicillins (2)
Carbenicillin
Ticarcillin
Piperacillin is what type of Penicillin?
Ureidopenicillins
First-generation cephalosporins (6)
Cefazolin
Cefadroxil
Cephalexin
Cephalothin
Cephapirin
Cephradine
Second-generation cephalosporins (9)
Cefaclor
Cefamandole
Cefonicid
Cefuroxime
Cefprozil
Loracarbef
Ceforanide
Cefotetan
Cefoxitin
Third-generation cephalosporins (12)
Cefoperazone
Cefotaxime
Ceftazidime
Ceftizoxime
Ceftriaxone
Cefixime
Cefpodoxime proxetil
Cefdinir
Cefditoren
Pivoxil
Ceftibuten
Moxalactam
Fourth-generation cephalosporins (1)
Cefepime
Cephalosporin–β-lactamase inhibitor combinations (2)
Effective against gram (-) infections
Ceftolozane-tazobactam
Ceftazidime-avibactam
Siderophore Cephalosporin
Cefiderocol
Cephalosporins Active Against Methicillin-Resistant Staphylococci (1)
Ceftaroline fosamil
Carbapenems (4)
Ertapenem
Imipenem
Meropenem
Doripenem (not available in USA)
Drugs with a monocyclic β-lactam ring
Monobactams
Enumeration
Glycopeptides (5)
Vancomycin
Teicoplanin
Telavancin
Dalbavancin
Oritavancin
DOT TV
The following are glycopeptides, EXCEPT:
Vancomycin
Teicoplanin
Telavancin
Daptomycin
Dalbavancin
Oritavancin
Daptomycin
Daptomycin is a lipopeptide
Drugs that inhibit the growth/replication, or kill microrganisms
Antimicrobials
Types of antimicrobials (5)
Antibacterial
Antifungal
Antiviral
Anti-protozoal
Anti-parasitic
First-line drug for syphillis
Benzathine Penicillin G
Penicillin G is the drug of choice for infections caused by:
Streptococci
Meningococci
Enterococci
Penicillin-susceptible pneumococci
Non-B-lactamase-producing staphylococci
Spirochetes (Treponema pallidum)
Actinomyces
Non-B-lactamase-producing Gram (-) anaerobic organisms
Oral form of penicillin, indicated only in minor infections due to poor bioavailability
Penicillin V
Most active of oral B-lactam antibiotics against pneumococci
Aminopenicillins (ampicillin & amoxicillin)
Given orally to treat:
Bacterial sinusitis
Otitis
Lower respiratory tract infections
Amoxicillin
Effective for shigellosis
Ampicillin
Ampicillin is effective against serious infections including: (5)
Anaerobes
Enterococci
L. monocytogenes
E. coli
Salmonella sp.
Ampicillin is not active against:
Klebsiella sp.
Enterobacter sp.
P. aeruginosa
Citrobacter sp.
Serratia marcescens
Indole-positive Proteus species
Gram (-) aerobes
Resistant agents of Penicillin G:
Penicillin-Resistant S. pneumoniae (PRSP) strains
S. aureus
N. gonorrhoeae
Used for oropharyngeal infections
Penicillin V
Developed to broaden spectrum of penicillins against gram (-) pathogens, including Pseudomonas aeruginosa
Carboxypenicillins (carbenicillin, tricarcillin)
Active against Gram (-) bacilli:
Klebsiella pneumoniae
Pseudomonas aeruginosa
Ureidopenicillin (piperacillin)
Available only as co-formulation with tazobactam
Ureidopenicillin (piperacillin)
Antipseudomonal B-lactams used in combination with Ureidopenicillin due to P. aeruginosa developing resistance (2)
Aminoglycoside
Fluoroquinolone
B-lactamase inhibitors used in combination with Ampicillin, Amoxicillin, Piperacillin, and Ticarcillin (3)
Clavulanic acid
Sulbactam
Tazobactam
B-lactamase inhibitors extends the activity of penicillins against:
B-lactamase-producing strains of S. aureus
B-lactamase-producing Gram-negative bacteria
Degradation products of penicillins and products of alkaline hydrolysis
Antigenic determinants
Penicilloic acid
Associated with neutropenia
Nafcillin
Causes hepatitis
Oxacillin
Causes interstitial nephritis
Methicillin
Associated with pseudomembranous otitis
Ampicillin
Associated with skin rashes
Ampicillin
Caused by large doses of oral penicillins
GI disturbances
Nausea, vomiting, diarrhea
When combined with vancomycin, associated with greater incidence of acute kidney injury
Piperacillin-tazobactam
Generation of Cephalosporins effective against:
Gram (+) cocci
E. coli
Klebsiella pneumoniae
Proteus mirabilis
Anaerobic cocci (peptococci, peptostreptococci)
1st Generation
1st Generation Cephalosporins are not effective against:
Gram (-) cocci
Enterococci
MRSA
Most gram (-) rods
Methicillin-resistant strains of staphylococci
Pseudomonas aeruginosa
Indole-positive Proteus species
Enterobacter sp.
Serratia marcescens
Citrobacter sp.
Acinetobacter sp.
Drug of choice for surgical prophylasxis
Cefazolin
1st Generation
Effective for serious staphylococcal infections such as bacteremia
Cefazolin
Suitable for urinary tract infections and staphylococcal or streptococcal infections, including cellulitis or soft tissue absess
Oral cephalosporins
A heterogenous group with individual differences in activity, pharmacokinetcs, and toxicity
2nd Generation Cephalosporins
2nd Generation Cephalosporins effective against Haemophilus influenzae but NOT Serratia and Bacteroides fragilis (2)
Cefuroxime
Cefaclor
2nd Generation Cephalosporins effective against Bacteroides fragilis and Serratia but NOT Haemophilus influenzae (2)
Cefoxitin
Cefotetan
True or False
2nd Generation Cephalosporins are active against enterococci and P. aeruginosa
False
No member is active
True or False
2nd Generation Cephalosporins can be used to treat Enterobacter infections
False
Should not be used
2nd Generation Cephalosporin effective against extended-spectrum B-lactamases produced by E. coli and Klebsiella sp.
Cefoxitin
2nd Generation
Most commonly used oral cephalosporin
Cefuroxime axetil
2nd generation cephalosporins used to treat mixed anaerobic infections such as: (2)
Peritonitis
Diverticulitis
Pelvic inflammatory disease
Cefoxitin
Cefotetan
2nd Generation
Used to treat community-acquired pneumonia
Cefuroxime
2nd Generation Cephalosporins are effective against: (4)
Extended gram (-) activity
Klebsiella
H. influenzae
Bacteroides fragilis
Serratia
2nd Generation Cephalosporins are NOT effective against: (2)
Enterobacter
P. aeruginosa
3rd Generation Cephalosporins are effective against: (4)
Citrobacter
Serratia
Providencia
Pseudomonas
The only 3rd Generation Cephalosporin effective against P. aeruginosa
Ceftazidime
3rd Generation Cephalosporins are NOT effective against:
Enterobacter
3rd Generation Cephalosporins less active against pneumococci and S. aureus (2)
Cefixime
Ceftibuten
Generation of Cephalosporins that penetrate body fluids and tissues well, and can reach cerebrospinal fluid
3rd Generation
3rd Generation Cephalosporins
____ combined with ____ is the preferred regimen for treating most gonococcal infections
Intramuscular Ceftriaxone + azithromycin
The only 3rd Generation Cephalosporin excreted through the biliary tract
Ceftriaxone
The only penicillin excreted through the billiary tract
Nafcillin
3rd Generation
Most active cephalosporins against penicillin-non-susceptible strains of pneumococci (2)
Ceftriaxone
Cefotaxime
3rd Generation
Approved for treating meningitis caused by pathogens such as: (2)
Pneumococci
Meningococci
H. influenzae
Enteric Gram-negative rods (except L. monocytogenes)
Ceftriaxone
Cefotaxime
3rd Generation
Recommended for empirical therapy of serious infections caused by penicillin-non-susceptible strains of pneumococci (2)
Ceftriaxone
Cefotaxime
The only available fourth generation cephalosporin
Cefepime
4th generation cephalosporins are effective against: (6)
P. aeruginosa
Enterobacteriaceae
Methicillin-susceptible S. aureus (MRSA)
S. pneumoniae
Haemophilus sp.
Neisseria sp.
Valuable for treating Enterobacter infections due to good activity against most penicillin-resistant strains of streptococci
Cefepime
4th Generation
Commonly used empirically in patients with febrile neutropenia
Cefepime
4th Generation
First-beta-lactam antibiotic approved in the USA with activity against MRSA
Prodrug of ceftaroline
Ceftaroline fosamil
Used off-label to treat bacteremia, endocarditis, and osteomyelitis
Ceftaroline
Ceftolozane-tazobactam and Ceftazidime-avibactam are effective against:
P. aerugnosa
AmpC and extended-spectrum B-lactamase-producing Enterobacterieae
Ceftolozane-tazobactam and Ceftazidime-avibactam are combined with ____ when treating complicated intra-abdominal infections
Metronidazole
Effective for carbapenemase-producing organisms
Ceftazidime-avibactam
Ceftolozane-tazobactam and Ceftazidime-avibactam are NOT effective against:
Organisms producing metallo-B-lactamases
Patients with history of penicillic anaphylaxis should avoid which generations of cephalosporins?
1st and 2nd generation
Cephalosporins that may cause hypoprothrombinemia and bleeding disorders (4)
Cephalosporins containing a methylthiotetrazole group:
Cefamandole
Cefmetazole
Cefoperazone
Cefotetan
Drugs with a monocyclic B-lactam ring
Monobactams
Monobactams are effective against:
Aerobic Gram-negative organisms (including P. aeruginosa)
Monobactams are NOT effective against:
Gram-positive bacteria or anaerobes
Monobactams
Can be given to penicillin-allergic patients without reaction
Aztreonam
Beta-lactamase Inhibitors (4)
Clavulanic acid
Sulbactam
Tazobactam
Avibactam
CATS
Beta-lactamase Inhibitors are most effective against:
Ambler class A B-lactamases produced by:
Staphylococci
H. influenzae
N. gonorrhoeae
Salmonella
Shigella
Escherichia coli
Klebsiella pneumoniae
Non-B-lactam B-lactamase inhibitor active against Ambler class A, Ambler class C, and some class D B-lactamases
Avibactam
Active against B-lactamase-producing S. aureus and H. influenzae but not against Serratia
Ampicillin-Sulbactam
Trrue or False
Piperacillin-Tazobactam is active against P. aeruginosa
False
Carbapenem effective against:
Gram-negative rods (P. aeruginosa)
Gram-positive organisms
Anaerobes
Imipenem
Imipenem is NOT active against:
Enterococcus faecium
MRSA
Clostridium difficile
Burkholderia cepacia
Stenotrophomonas maltophilia
Inactivates Imipenem, resulting in low urinary concentrations
Dehydropeptidases
An inhibitor of renal dehydropeptidase, administered with Imipenem for clinical use against pneumonia and sepsis
Cilastatin
Clinical use:
Streptococcal infections
Meningococcal infections
Neurosyphilis
Penicillin G
Narrow-spectrum Penicillin
Clinical use:
Skin and soft tissue infections
Urinary tract infections
Surgical prophylaxis
Cefazolin
1st Generation Cephalosporin
Clinical use:
Infections caused by aerobic, Gram-negative bacteria in patients with hypersensitivity to penicillins
Aztreonam
Monobactam
Clinical use:
Serious infections such as pneumonia and sepsis
Imipenem-cilastatin
Intravenous carbapenem, stable to renal dehydropeptidase, lowers incidence of seizures
Meropenem
Clinical use:
Infections caused by Gram-positive bacteria including sepsis, endocarditis, and meningitis
C. difficile colitis
Vancomycin
Narrow-Spectrum Penicillins
Penase-susceptible
(2)
Penicillin G
Penicillin V
Narrrow-Spectrum Penicillins
Penase-resistant
(2)
Nafcillin
Oxacillin
Monobactam active only against Gram-negative bacteria:
Klebsiella
Pseudomonas
Serratia spp
Aztreonam
Novel cyclic lipopeptide fermentation product of Streptomyces roseusporus
Daptomycin
Active against vancomycin-resistant strains of enteroccoci and S. aureus
Daptomycin
Binds to the cell membrane via calcium-dependent insertion of its lipid tail
Daptomycin
Can cause myopathy
Daptomycin
Inhibits the cytpolasmic enzyme enolpyruvate transferase
Fosfomycin
Fosfomycin is active against:
Both gram-positive and gram-negative organisms
Approved for use against uncomplicated lower urinary tract infections in women
Fosfomycin
Cyclic peptide mixture obtained from the Tracy strain of Bacillus subtilis
Bacitracin
Inhibits cell wall formation by interfering with dephosphorylation
Bacitracin
An antibiotic produced by Streptomyces orchidaceous
Cycloserine
Almost exclusively used to treat tuberculosis caused by strains of Mycobacterium tuberculosis resistant to first-line agents
Cycloserine
Causes serious dose-related CNS toxicity with headaches, tremors, acute psychosis, and convulsions
Cycloserine
An antibiotic isolated from Amycolatopsis orientalis
Vancomycin
Inhibits cell wall synthesis by binding to the d-Ala-d-Ala terminus of nascent peptidoglycan pentapeptide
Vancomycin
Synergistic with vancomycin against Enterococcus faecium and Enterococcus faecalis strains (2)
Gentamicin
Streptomycin
Combined with vancomycin as an alternative regimen for treating enterococcal endocarditis in patients with serious penicillin allergy
Gentamicin