Antimicrobials Flashcards
Which drugs have DNA replication as their site of antimicrobial action?
Quinolones
Metronidazole
Which drugs have cell wall synthesis as their site of antimicrobial action?
Beta lactams Vancomycin Daptomycin Isoniazid Ethambutol
Which drugs have protein synthesis (ribosome S30) as their site of antimicrobial action?
Aminoglycosides
Tetracyclines
Tigecycline
Which drugs have protein synthesis (ribosome S50) as their site of antimicrobial action?
Chloramphenicol Macrolides Clindamycin Linezolid Streptogramins
Which drugs have antimetabolites as their site of antimicrobial action?
Sulfonamides
Trimethoprim
Which drugs have RNA synthesis as their site of antimicrobial action?
Rifampicin
Which drugs have membrane permeability as their site of antimicrobial action?
Polymixen
What is the site of antimicrobial action of beta lactams?
Cell wall synthesis
What is the site of antimicrobial action of vancomycin?
Cell wall synthesis
What is the site of antimicrobial action of isoniazid?
Cell wall synthesis
What is the site of antimicrobial action of ethambutol?
Cell wall synthesis
What is the site of antimicrobial action of aminoglycosides?
Protein synthesis (ribosome S30) Reversible
What is the site of antimicrobial action of tetracyclines?
Protein synthesis (ribosome S30) Reversible
What is the site of antimicrobial action of chloramphenicol?
Protein synthesis (ribosome S50) Irreversible
What is the site of antimicrobial action of macrolides?
Protein synthesis (ribosome S50) Irreversible
What is the site of antimicrobial action of clindamycin?
Protein synthesis (ribosome S50) Irreversible
What is the site of antimicrobial action of sulfonamides?
Antimetabolites
What is the site of antimicrobial action of trimethoprim?
Antimetabolites
What is the site of antimicrobial action of polymixen?
Membrane permeability
What is the site of antimicrobial action of rifampicin?
RNA synthesis
What are the four kinds of beta lactams?
Penicillin
Cephalosporins
Carbapenems
Monobactams
Name the kinds of penicillins
Natural
Beta-lactamase resistant
Broad-spectrum
Extended-spectrum (antipseudomonal)
Name natural penicillins
Benzylpenicillin (pen G)
Phenoxymethylpenicillin (pen V)
Name beta-lactamase resistant penicillins
Oxacillin Cloxacillin Flucloxacillin Dicloxacillin Methicillin Nafcillin
Name broad-spectrum penicillins
Amoxicillin
Ampicillin
Name extended-spectrum (antipseudomonal) penicillins
Piperacillin
Ticarcillin
Indanyl carbenicillin
Name thee kinds of cephalosporins
1st generation
2nd generation
3rd generation
4th generation
Name 1st generation cephalosporins
Cefadroxil
Cefazolin
Cephalexin
Cephalothin
Name 2nd generation cephalosporins
Cefaclor Cefamandole Cefprozil Cefuroxime Cefotetan Cefoxitin
Name 3rd generation cephalosporins
Cefdinir Cefixime Cefoperazone Cefotaxime Ceftazidime Ceftibuten Ceftizoxime Ceftriazone
Name 4th generation cephalosporins
Cefepime
Name carbapenems
Imipenem
Meropenem
Ertapenem
Why is imipenem combined with cilastatin?
Cilastatin inhibits dehydropeptidase, the enzyme which renally degrades imipenem. It is combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect.
Name monobactams
Aztreonam
What is the spectrum of monobactams?
Aerobic gram -
Name beta lactamase inhibitors
Clavulanic acid
Sulbactam
Tazobactam
What is the spectrum of natural penicillins?
Gram + cocci Gram + bacilli Gram - cocci Anaerobes Spirochetes
What is the spectrum of beta lactamase resistant penicillins?
Strep
Step
NOT enterococci, anaerobes, gram- cocci, gram - bacilli
What is the spectrum of broad-spectrum penicillins
Gram + cocci Gram + bacilli Gram - cocci Anaerobes Spirochetes AND Gram - bacilli - salmonella, shigella (2GIT) - e coli, proteus mirabilis (2UTI) - H influenza, pertussis (2 resp)
What is the spectrum of extended-spectrum penicillins?
Gram + cocci Gram + bacilli Gram - cocci Anaerobes Spirochetes AND Pseudomonas AND Gram - bacilli (KEEPS) - klebsiella - ecoli - enterobacter - proteus - serratia
What coverage extends with increasing cephalosporin generation?
Gram -
What is the spectrum of 1st generation cephalosporins?
Gram(+) cocci: • Staph. aureus* (* Except MRSA) • Staph. epidermidis • Strep. pneumoniae • Strep. pyogenes • Anaerobic streptococci
Gram(-) bacilli:
• E. coli
• Klebsiella pneumoniae
• Proteus mirabilis
What is the spectrum of 2nd generation cephalosporins?
Gram(+) cocci: • Strep. pneumoniae • Strep. pyogenes • Anaerobic streptococci Gram(-) cocci: • N. gonorrhoeae
Gram(-) bacilli: • Enterobacter aerogenes • E. coli • H. influenza • Klebsiella pneumoniae • Proteus mirabilis
What is the spectrum of 3rd generation cephalosporins?
Gram(-) cocci: • N. gonorrhoeae Gram(-) bacilli: • Enterobacter aerogenes • E. coli • H. influenza • Klebsiella pneumoniae • Proteus mirabilis • Pseudomonas aeruginosaGram(-) cocci: • N. gonorrhoeae
Gram(-) bacilli: • Enterobacter aerogenes • E. coli • H. influenza • Klebsiella pneumoniae • Proteus mirabilis • Pseudomonas aeruginosa
What is the spectrum of 4th generation cephalosporins?
Wide antibacterial spectrum and
excellent coverage of gram(+) and
gram(-) organisms
What are cephamycins active against and which is the most potent?
Anaerobes eg bacteroides fragilis
Cefoxitin
What is the spectrum of carbapenems?
Broadest of all beta lactams
Gram +
Gram -
Anaerobes
Which beta lactams have the broadest bacterial coverage and why?
Carbapenems
[ ] dependent killing and postantibiotic effect
vs
Other beta lactams
Time dependent killing and no antibiotic effect
What is the spectrum of imipenem?
GRAM(-) BACILLI: • Acinetobacter species • Citrobacter species • Enterobacter species • E. coli • Gardnerella vaginalis • H. influenza • Klebsiella species • Proteus species • Providencia species • Salmonella species • Serratia species • Pseudomonas aeruginosa*** (*** Resistant strains reported)
GRAM(-) COCCI:
• Neisseria meningitidis** (** Including penicillinase producing
strains.)
• Neisseria gonorrhoeae
GRAM(+) COCCI: • Staph. aureus* (*MRSA are resistant) • Staph. epidermidis • Enterococcus faecalis • Streptococcus Group A, B & C • Strep. pneumoniae
ANAEROBIC ORGANISMS: • Clostridium species • Peptococcus species • Peptostreptococcus species • Propionibacterium species • Bacteroides species (e.g. B. fragilis) • Fusobacterium species
OTHER:
• Actinomyces
• Nocardia species
Name macrolides
Erythromycin
Clarithryomycin
Azithromycin
Telithromycin
How is erythromycin excreted?
Bile -> enterohepatic -> urine
How is azithromycin excreted?
Bile -> enterohepatic -> urine
How is clarithromycin excreted?
Renal + hepatic -> urine
Name side effects of macrolides
GIT disturbances
Cholestatic jaundice
Ototoxicity
Name contraindications for macrolides
Liver dysfunction
Renal dysfunction
What is important about 30S vs 50S
30S = reversible 50S = irreversible
Name tetracyclines
Tetracycline
Doxycyline
Minocycline
Demeclocycline
Which tetracycline provides therapeutic levels in CSF?
Minocycine
Name side effects of tetracyclines
GIT discomforty
Bone deposition
Phototoxicity
Vestibular problems
Name contraindications for tetracyclines
Pregnancy
Breastfeeding
Children <8yo
Name side effects of cotrimoxazole
Skin rash NV Haematological disturbances - megaloblastic anemia - leukopenia - thrombocytopenia
What does trimethroprim inhibit?
Dihydrofolate reductase
Which drug is linked to Gray baby syndrome?
Chloramphenicol
Name the side effects of chloramphenicol
Anemias
Gray baby syndrome
Drug interactions (CYP450)
What is important concerning lipophilic drugs and the brain?
They cross the BBB
What is clostridium difficile always resistant to?
Clindamycin
Name side effects of clindamycin
Skin rashes
Pseudomembranous colitis
Name aminoglycosides
Amikacin Gentamicin Tobramycin Streptomycin Neomycin
Name side effects of aminoglycosides
Ototoxicity
Nephrotoxicity
Neuromuscular paralysis
Skin rash w/ neomycin
Name 1st generation fluoroquinolones
Nalidixic acid
Name 2nd generation fluoroquinolones
Ciprofloxacin
Norfloxacin
Ofloxacin
Name 3rd generation fluoroquinolones
Gatifloxacin
Levofloxacin
Moxifloxacin
Sparfloxacin
Name 4th generation fluoroquinolones
Trovafloxaci
Name side effects of fluoroquinolones
GIT disturbances
Headaches and dizziness
Phototoxicity
Drug interaction (CYP450)
Name contraindications for fluoroquinolones
Pregnancy
Breast feeding
<18 yo
Arrythmias
Which drugs inhibit DNA gyrase?
Quinolones
Which drugs inhibit folate synthesis?
Trimethoprim
Sulfamethoxazole
Which drugs create free radicals?
Metronidazole
Nitrofurantoin