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?

A

true

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
Q

Synergism

A

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
Q

Antagonism

A

is what we WORRY about

activity of the combo is less than the sum

ex. static plus cidal

drug and bug dependent

27
Q

Judicious use of Antibacterials refers to?

A

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
Q

MICs may __________ activity of topically/locally applied antibacterial drugs!

A

UNDERESTIMATE

29
Q

In general, MICs ___________ predict ___________ for infections in the ISF

A

Adequately

SUCCESS

30
Q

MIC testing will _________ activity of antibiotics!

A

Overestimate

31
Q

What are the exceptions rule when it comes to site of infection (judicious use)?

A

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
Q

What drugs have BETTER penetration into cells when theres INTRACELLULAR infections?

Lipophilic or Hydrophilic

A

Lipophilic drugs

33
Q

When it comes to abscesses and granulomas what factors are important to keep in mind?

A

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
Q

Local tissue factors are?

A

Affect the efficacy of some drugs

purulent debris

acidic environment

hemoglobin/ hemorrhage

Anaerobic conditions/necrotic tissue
- decreased blood supply

35
Q

MICs do NOT take into account ______ ______ ______ !

A

LOCAL TISSUE FACTORS

36
Q

Judicious use summarized in three statements?

A

Cut it out

Drain it

Fix underlying disease

37
Q

Choosing an antibiotic with the Empiric treatment

A

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
Q

When choosing an antibiotic what 5 things are important to keep in mind?

A

Availability
- formulations

Ease of use
- client compliance
- patient compliance

Adverse effects

Cost

Species