Pharmacology 3: Antibacterial agents for systemic therapy Flashcards

1
Q

Minimum inhibitory concentration (MIC)

A

lowest concentration of drug that INHIBITS visible bacterial growth

ex. MIC90 = concen for INHIBITING 90% of the bacteria

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2
Q

Minimum Bactericidal Concentration (MBC)

A

KILLS

lowest concentration of a drug that KILLS 99.9% of bacteria

LARGER

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3
Q

Mutant Prevention Concentration (MPC)

A

LEAST susceptible single-step mutant

-theory, kills them all so mutants (resistant bacteria) can NOT form

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4
Q

What requires host immune response?
hint* something to do with infection

A

Elimination of infection

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5
Q

Bacteriostatic bacteria

A

STOP bacteria from multiplying; don’t kill them

MBC much LARGER that the MIC

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6
Q

Bacteriostatic NEED what to eliminate infection?

A

Requires host immune response

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7
Q

Bactericidal is preferred for what kin of patients?

A

Immunosuppressed

Severely ill patients
-sepsis
-neonates
-on glucocorticoids
-on cancer chemotherapy

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8
Q

Bactericidal

A

kill bacteria if concentration reach MBC for a certain period of time
- MBC at or near the MIC

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9
Q

A drug can be both Bacteriostatic and Bactericidal?

A

True

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10
Q

Bactericidal antimicrobials are or are NOT always bactericidal?

A

NOT

static at concentration below MBC
- dose dependent
- bacteria dependent

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11
Q

Bacteria must be dividing or multiplying for bactericidal to work

A

bacteria must be MULTIPLYING

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12
Q

Postantibiotic effect (PAE)

A

Persistent drug effect
- After plasma concentration decline below the MIC/MBC

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13
Q

What are mechanisms for Postantibiotic effect

A

decreased virulence of the bacteria

development of abnormal cell wall or septum

increased susceptibility to host defenses

Persistence at sites of infection

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14
Q

When does PAE occur?

A

Only with SOME drugs and is BACTERIA-dependent

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15
Q

What do we use pharmacokinetic and pharmacodynamic interactions for?

A

How we determine dosing

Drug bug interactions

PREDICT SUCCESS OF ANTIMICROBIAL THERAPIES
- Relate concentrations of drug to MIC of the pathogen
- vary by class of drug
- vary with each pathogen

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16
Q

PK refresher

A

Cmax: maximum plasma

AUC: area under the plasma concentration time curve

17
Q

Pharmacodynamic targets

A

Time dependent antibiotics
- T>MIC: duration plasma concentration is above the MIC over 24h

Concentration-dependent antibiotics
- Cmax: MIC ratio of the maximum plasma concentration (C max) to the MIC

Concentration/Time dependent antibiotics
- AUC:MIC: ratio of the AUC0-24 to the MIC

18
Q

Antibiotic mechanism of action

A

Cell wall: inhibit synthesis and function

NA: inhibit synthesis and function

Protein synthesis: inhibits 50s ribsomal, subunits
inhibt 30s ribosomal, subunits

19
Q

Spectrum activity

A

describing general activity of antimicrobial

  • narrow=limited subsets of bacteria
  • broad=treats a lot (not always well)
    –> may include mycoplasma, rickettsia, and chlamydia
20
Q

Individual isolates of bacteria may be resistant to an antibacterial even though they are part of the SPECTRUM?

21
Q

Antibacteral spectrum 4 quadrants

A

Aerobic
+ and -

Anaerobic
+ and -

Broad spectrum
- all four quadrants
- other categories

Intermediate spectrum (NOT *)
- 2-3/4 quadrants

Narrow spectrum
- 1-2/4 quadrants

22
Q

Davis 6 quadrants antibacterial spectrum

A

Aerobic bacteria
- gram +
(step and staph) ococci
- gram -
respiratory pathogens
enteric pathogens

Anaerobic bacteria
- gram +
- gram -

PENICILLINS
- activate against streptococci, NOT most staphylococci
- NOT active against gram -
- active against most gram + and gram - anaerobes

AMINOGLYCOSIDES
- active against staphylococci, NOT most streptococci
- active against respiratory and enteric gram -
- NO activity against anaerobes

MACROLIDES
- active against gram - aerobes
- active against respiratory gram - but NOT enteric
- active against most gram + anaerobes

23
Q

Facts about Facultative anaerobes

A

are AEROBES
-CAN grow in anaerobic conditions
-culture as aerobes
-test susceptibility in aerobic conditions
-In vitro susceptibility may NOT equal in vivo susceptibility
- when anaerobic conditions are present in the patient

24
Q

antimicrobial drug interactions

A

additive/indifferent
- used to extend the spectrum
- does NOT enhance activity of either

25
Synergism
is what we HOPE for -combo enhances in activity -trimethoprim/sulfnamide - static alone;-cidal together -ampicillin/clavulanic acid - CA prevents degradation by beta-lactamases -Beta-lactams and aminoglycosides - beta-lactams increases permeability of cell to aminoglycoside
26
Antagonism
is what we WORRY about activity of the combo is less than the sum ex. static plus cidal drug and bug dependent
27
Judicious use of Antibacterials refers to?
IS AN ANTIBACTERIAL NECESSARY in this case. What is most appropriate route: IV, IM/SQ, PO --> transdermal NOT recommended Yes = bacterial infection-systemic No=viral, fungal, and parasitic Maybe=protozoal, bacterial, and local
28
MICs may __________ activity of topically/locally applied antibacterial drugs!
UNDERESTIMATE
29
In general, MICs ___________ predict ___________ for infections in the ISF
Adequately SUCCESS
30
MIC testing will _________ activity of antibiotics!
Overestimate
31
What are the exceptions rule when it comes to site of infection (judicious use)?
CNS Eye Prostate Bronchus Testes -protective barriers that consist of tights junctions between the endothelial cells -Limited drug movement into these areas -Lipid solubility Significance during inflammation
32
What drugs have BETTER penetration into cells when theres INTRACELLULAR infections? Lipophilic or Hydrophilic
Lipophilic drugs
33
When it comes to abscesses and granulomas what factors are important to keep in mind?
Drug diffusion slow - lower Cmax - slower equilibrium Lower blood supply to the area Treatment unsuccessful without DRAINAGE If you can DRAIN and LAVAGE the abscesses, antibacterials may NOT be necessary **If you do NOT drain --> choose more LIPOPHILIC drugs -->treat for LONG periods
34
Local tissue factors are?
Affect the efficacy of some drugs purulent debris acidic environment hemoglobin/ hemorrhage Anaerobic conditions/necrotic tissue - decreased blood supply
35
MICs do NOT take into account ______ ______ ______ !
LOCAL TISSUE FACTORS
36
Judicious use summarized in three statements?
Cut it out Drain it Fix underlying disease
37
Choosing an antibiotic with the Empiric treatment
Know which bacteria commonly involved in which infections Choose drug that is likely to treat that bacteria NARROW SPECTRUM BASED ON RESULTS OF CULTURE AND SENSITIVITY WHEN POSSIBLE
38
When choosing an antibiotic what 5 things are important to keep in mind?
Availability - formulations Ease of use - client compliance - patient compliance Adverse effects Cost Species