Antimicrobial Drugs Part 1

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1
What is therapeutic dose?
dose per kg required to achieve MIC (minimum inhibitory concentration)
2
What is the therapeutic index? What does it indicate?
(toxic dose/therapeutic dose)
greater the #=safer the drug
lower the #=more toxic drug
3
What must be maintained in order to provide effective drug tx?
*need to maintain minimum effective concentration of the drug
4
What is toxic dose?
*maximum tolerated dose (dose when you start to see toxic effects)
5
What is therapeutic index? Why do we use it?
*TD50/ED50 (toxic dose in 50% of pts/effective dose in 50% of patients)
*space between efficacy and toxicity curve midpoints
6
What is margin of safety? Why do we use it?
*Toxic dose 1/effective dose 99
(toxic dose in 1 % of patients/effective dose in 99% of patients)
used to help determine patient dosages
7
What is chemotherapy? when used?
*use of drugs to treat disease
*cancer tx, antibiotics against bacteria, etc..
8
What do antimicrobial drugs do?
interfere with growth of microbes within a host
9
What does "selective toxcitiy" mean?
*drug that kills harmful microbes without damaging the host
10
What is the therapuetic window?
concentration range that a drug will work (upto the toxicity point)
11
When was PCN discovered? By whom?
*1928 by Fleming
12
When and whom performed the frist clinical trial of PCN?
*1940 by HOward Florey and Ernst Chain
13
Where do most antibiotics come from?
*bacteria
*over half originate from Streptomyces
14
What is a broad spectrum drug?
*antibioitic that is effective against a wide range of both gram-positive and/or gram negative bacteria
15
Bactericidal?
killing of bacteria
16
Bacteriostatic?
*inhibiting bacterial growth
17
In what ways can disk diffusion test be applied?
*antibiotics
*drug
*chemicals (disinfectants)
*other biologicals (pt's serum etc...)
18
What values must be evaluated to determine when 2nd antibiotic dose must be given?
must know the serum antimicrobial concentration, want the amount of antibiotic in serum above the minimum inhibitory concentration
19
What must be taken into consideratino when determining dosage and schedule?
*margin of safety
*metabolism (and rate of metabolism) of drug
20
What are the 4 ways broad spetrum antibiotics act against microbes?
*Metabolic inhibitors
*DNA replication inhibitors
*RNA polymerase inhibitors
*protein synthesis inhibitors
21
What do cell wall inhibitors impact?
*peptidoglycan synthesis
22
What are 5 cell wall inhibitors?
*PCN
*cephalosporins
*vancomycin
*bacitracin
*monobactams
23
What are 2 metabolic inhibitors?
*sulfonamides
*trimethoprim
24
What is one DNA replication inhibitor?
*quinolones
25
What are two RNA polymerase inhibitors?
*rifampin
*pyronins
26
What are 5 protein synthesis inhibitors (affect larger portion 50S of ribosome)?
*chloramphenicol
*macrolides (erythromycin)
*clindamycin
*oxazolidinones (linezolid)
*Streptogramins (synercid)
27
What are 2 protein sythesis inhibitors (affects smaller 30S portion of ribosome)?
*Aminoglycosides (gentamicin)
*Tetracyclines (doxycycline)
28
How do antibitoics target the cell wall?
prevents specific proteins/enzymes from creating peptidotetrad linkages for the NAG and NAM chains within the cell wall
(prevents cell wall synthesis)
*keep in mind, more than one way to accomplish this
29
What are B-lactam antibiotics?
*class of antibiotics that contain beta-lactam ring as their common structure
*PCN (natural and semisynthetic)
30
What are B-lactamase inhibitors?
*destroy the enzyme (produced by bacteria) that would harm the antibiotics
31
Action of penicillinase enzyme?
produced by bacteria, destroys beta-lactum ring of antibiotic rendering it useless (ineffective)
32
What antibiotics are resistant to penicillinase (enzyme produced by bacteria)?
*Ampicillin
*Amoxicillin
*Amoxicillin + clavulanic acid = Augmentin
those with betalactamase
33
What are B-lactamase inhibitors?
*destroy the enzyme that would harm the antibiotic (destory the B-lactum ring)
34
What are Cephalosporin antibiotics?
*Cephalexin (1st gen)
*Cephoxatin (2nd gen)
*Ceftriaxone (3rd gen)
35
What are Carbapenems?
*class of B-lactam antibiotics
*single sulfur in place of carbon (double bond included)
36
What are Monobactam?
*single ring B-lactam antibiotics
37
How can penicillin inactivated?
*use penicillinase (break the B-lactam ring)
38
What two drugs target the bacterial membrane?
*Gramicidin
*Polymixin (detergent action)
39
What is platensimycin?
*B-lactam antibiotic drug that inhibits fatty acid synthesis (damages bacterial membrane)
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