1/30/17 SMITH Antibiotics 1 TEST #1 Flashcards
What are the two types of antimicrobial classes that target the cell wall synthesis?
- Beta Lactams
- Vancomycin
- Bacitracin
What must the B-lactam drugs bind to, to be effective?
-Transpeptidase enzyme (penicillin-binding protein) on the bacteria’s cytoplasmic membrane
What must B-lactam drugs evade to be effective?
-Bacterial defenses
What must B-lactam drugs pentrate to be effective?
-Outer cell layers to reach inner cytoplasmic membrane
What must B-lactams keep in their structure to be efective?
B-lactam ring structure
What on the B-lactam drugs resembles the D-ala-D-ala end of the peptidie that serves as a substrate for transpeptidase enzymes?
B-lactam region
What are 6 subclasses of B-lactam antimicrobials?
- Natural Penicillins
- Aminopenicillins
- Penicillinase-resistant penicillins
- Anti-Pseudomonal
- Cephalosporins
- Carbapenems: Impinem
What is the ultimate goal of the B-lactam antibiotics?
-Reach the transpeptidase enzyme
What does the binding of the B-lactam drugs to the transpeptidase penicillin binding proteins prevent?
-Transpeptidation (last step in new peptidoglycan (cell wall) synthesis)
Are B-lactam drugs bacterocidal or bacteriostatic?
-Bacterocidal
What do all B-lactam drugs require?
-Active proliferating microorganisms to maximally effective
What are B-lactam drugs inactive against?
-Organisms devoid of peptidoglycans (virus, mycobacteria, and fungi)
What type of drug is a B-lactam drug?
-Type II
What are two examples of Natural Penicillins?
- Penicillin G
- Penicillin V
What are natural penicillins highly active against?
-Gram + organisms
What are natural penicillins very susceptible to?
-Bacterial B-lactamases
What are two examples of Aminopenicillins?
- Ampicillin
- Amoxicillin
What did the aminopenicillins add to the penicillins?
-An amine group
What did the addition of the amino group on the penicllins to create aminopenicillins do for the targets of aminopenicillins?
-Extended spectrum to include the Gram - as well as the Gram +
T/F Aminopenicillins are still susceptible to B-lactamases
-True
What are 4 examples of penicillinase-resistant penicillins (anti-staphylococcal penicillin)?
- Methicillin
- Nafcillin
- Oxacillin
- Dicloxacicillin
What are the Penicillinase resistant penicillins relatively resistant to?
-B-lactamases
What penicillinase resistant penicillins is used as a first line treatment of choice for staphylococcal endocarditis?
-Nafcillin
What are 3 examples of Anti-Pseudomonal penicillins?
- Monobactams (aztreonam)
- Ureidopenicillins (piperacillin)
- Carboxypenicillins (Ticarcillin, indanyl carbenicillum)
What type of bacteria do Anti-Psudomonal penicillins have no activity against?
- Gram +
- Anaerobes
Of all the anti-psudomonal penicillins what two have the broadest spectrums of activity?
- Ticarcillin
- Peperacillin
T/F Cephalosporins are built on a 7-aminocephalosporanic acid instead of penicillins traditional 6-aminopenecillinic acid
True
Cephalosporins: Bacteriostatic or Bacteriocidal
Bactericidal
What is the broadest antibacterial available?
-Carbapenems
Of the two natural penicillins what is the only true naturally occurring penicillin?
-Penicillin G
What separates Penicillin G and Penicillin V?
-Penicillin V is acid stable so you can take it orally because the acid won’t chew it up
Are penicillins considered broad or narrow spectrum?
-Narrow
What is Penicillin G rapidly hydrolyzed by?
-Penicillinase enzymes (B-lactamase enzymes)
What is the drug of choice when prolonged low concentrations are required for example syphilis?
-Benzathine penicillin (Durapen)
What is the drug of choice for listeria monocytogenes, prophylaxis of infective endocarditis, or treatment of UTIs caused by susceptible enterococci?
-Aminopenicillins
Which of the aminopenicillins has a higher oral absorption?
-Amoxicillin
What aminopenicillins has a longer half-life and is less likely to cause adverse GI effects?
-Amoxicillins
What gram - strains does aminopenicillins work against?
- H. influenzae
- Enterics