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Pharmacology > Chemotherapy Of Antimicrobial Infections > Flashcards

Chemotherapy Of Antimicrobial Infections Flashcards

1
Q

Antimicrobials MOA 2

A

Interference with physiological pathways inhibits growth and multiplication or kill microorganisms

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2
Q

Antimicrobials MOA 3

A

Biochemical processes commonly inhibited: cell wall sysnthesis, cell membrane function, sysnthesis of 30s and 50s ribosomal subunits; nucleic acid sysnthesis

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3
Q

Characteristics of an ideal anti-infection agent

A
  1. Selective toxicity (bactericidal> bacteriostatic)
  2. Capable of penetration in concentration that exceeds several folds the MIC/MBC of potential pathogen, high affinity for site of action
  3. Resistant to inactivation and must not readily stimulate microbial resistance
  4. Orally active
  5. Long elimination half-life
  6. Devoid of adverse drug-drug interaction
  7. Absence of major organ toxic effect
  8. Absence of developmental or behavioral toxic effects
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4
Q

Factors to consider in the choice of antibiotics

A
  1. Microbial factors
  2. Host-related factors
  3. Drug-related factors
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5
Q

Classification of antibacterial agents

A
  1. Based on spectrum of activity (narrow or broad)
  2. Based on antimicrobial action (bactericidal or bacteriostatic)
  3. Based on mechanism of action (inhibition of cell wall synthesis, cell membrane function, protein synthesis, nucleic acid synthesis)
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6
Q

Ex of drugs that inhibit cell membrane function

A

Polymixins, daptomycin, polyene antifungals

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7
Q

Ex of drugs that inhibit protein systhesis

A

Aminoglycosides

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8
Q

Ex of direct inhibitor of DNA synthesis

A

Fluoroquinolones

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9
Q

Rifampicin as nucleic acid synthesis inhibitor

A

Forms stable complex with beta sub-unit of DNA-dependent RNA polymerase thereby inhibiting RNA synthesis (blocks RNA transcription)

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10
Q

Nitro-imidazoles like metronidazole as nucleic acid synthesis inhibitor

A

The nitro group is chemically reduced intracellularly in anaerobic bacteria and sensitive protozoans, to a reactive reduction product which interacts with DNa to cause a loss of helical DNA structure and strand breakage resulting in cell death

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11
Q

Antibiotic PD

A
  1. concentration-dependent or dose-dependent killing

2. Time-dependent killing

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12
Q

Concentration-dependent killing

–most important determinant of efficacy

A

The higher the concentration, the greater the bactericidal effect
—cmax/MIC ratio: aminoglycosides
AUC/MIC ratio: fluoroquinolones

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13
Q

Tome-dependent killing

  • –most important determinant of efficacy:
  • –goal:
A

Bactericidal effect is dependent on the length of time the bacteria are exposed to serum concentrations of at least 4x the MIC

  • –time>MIC
  • –goal: attain serum concentration of at least 4x MIC ofnjnfecting organism at all times for at least 40-50% of the dosing interval
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14
Q

Antibiotic absorption

A

To be effective the antibiotic has to be absorbed and penetrate into the infected compartment/organ; oral for mild to moderate infection and Iv for serious infections

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15
Q

Drugs with decreased biovailability with food

A 
Ampicillin
Azithromycin
Didanosine, efavirenz, indinavir
Erythromycin base/ether
Isoniazid
Itraconazole
Norfloxacin
Oxacillin,cloxacillin, etc
Phenoxymethylpenicillin (penicillin V)
Rifampicin
Sulfisoxqzole
Tetracyclin/oxytetracyclin
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16
Q

Drugs with increased bioavailability with food

A

Cefuroxime axetil
Fusidic acid
Griseofulvin
Nitrofurantoin

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17
Q

Unchanged bioavailability. Taken with or without food)

A 
Amoxicillin, co-amoxiclav
Cefadroxil
Cefixime
Chloramphenicol
Ciprofloxacin
Clarithromycin
Clindamycin
Cotrimoxazole
Dapsone
Doxycycline/minicycline
Fluconazole
Flucytosine
Ketoconazole
Pyrazinamide
Linezolid
Metronidazole
Telithromycin
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18
Q

Distribution of antibiotics

A

Effectiveness of antimicrobial therapy is determined by the relationship of the concentration of drug reaching the site of infection and the MIC of the infecting organism

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19
Q

Excellent with or without inflammation

A 
Chloramphenicol
Ethionamide
Fluconazole
Isoniazid
Metronidazole
Pyrazinamide
Rifampicin
Sulfonamides
Trimethoprim
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20
Q

Drugs good with inflammation

A 
3rd generatiob parenteral cephalosporins
Cefepime
Aztreonam
Ciprofloxacin, moxifloxacin
Linezolid
Meropenem
Penicillin
Vancomycin
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21
Q

Minimal or not good with inflammation

A 
Aminoglycosides
Lincosamides
Macrolides
Streptogramins
Tetracyclins
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22
Q

No passage even with inflammation

A

AmphotericinB
1st 2nd gem cephalosporins
Cefoperazone and ceftaroline
Polymixin E

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23
Q

Metabolism of antibiotics

A

Relatively few administered as prodrugs and have to undergo biotransformation to become active ( isoniazid, chloramphenicol succinate/palmitate)
Some active antibiotics undergo biotransformation to form still active metabolites
Inhibit metabolism of other (metronidazole)
some enhance (rifampicin)

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24
Q

Antibiotics excretion

A

Via the kidney, nonrenal

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25
Q

Hepatobiliary excretion

A 
Cefoperazone/ceftriaxone
Chloramphenicol
Clindamycon/doxycyclin
Azithromycin
Linezolod
Metronidazole
Most azole but nit fluconazole
Mocifloxacin
Nafcillin
Quinupristi
rifampicin
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26
Q

Renal and biliary excretion

A 
Ampicillin
Cefixime
Isoniazid
Oxacillin and related drugs
Pyrazinamide
Telithromycin
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27
Q

Renal excretion

A 
Aciclovir
Aminoglycosides
Amphotericin B
Aztreonam
Carbapanemes
Cephalosporins
Clarithromycin
Fluoroquinolones
Penicillintetracyclin
Vancomycin
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28
Q

Rationale for antibiotic combination therapy

A

1 provide broad spectrum for empiric therapy

  1. Treat polymicrobial infection
  2. Prevent/ delay emergence of resistance
  3. Decrease dose-related toxicity
  4. Obtain enhanced inhibition/killing synergism
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29
Q

Mechanism of antimicrobial synergism

A
  1. Blockade of sequential steps in metabolic sequence
  2. Inhibition of enzymatic inactivation
  3. Enhancement of antimicrobial uptake
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30
Q

[synergism]

Blockade of sequential steps in metabolic sequence

A

Sulfamethoxazole + trimethoprim

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31
Q

[synergism]

Inhibition of enzymatic inactivation

A
  1. Betalactamase inhibitor and beta lactam antibiotic
  2. Clavulanate K and amoxicillin
  3. Sulbactam and ampicillin
  4. Tazobactam and piperacillin
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32
Q

[synergism]

Enhancement of antimicrobial uptake

A
  1. Penicillin and aminoglycosides
  2. Ampicillin and gentamycin
  3. Ceftazidime and amikacin
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33
Q

Mechanism of antimicrobial antagonism and example

A
  1. Inhibition of bactericidal activity by bacteriostatic antibiotic (betalactams and tetracycline)
  2. Induction of enzymatic inactivation (rifampicin and protease inhibitors)
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34
Q

Mechanism of acquired drug resistance

1. Decrease

A

Decreased drug uptake or increase efflux of the drug ( tetracycline, quinolones, aminoglycoside, macrolides, chloramphenicol)

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35
Q

Mechanism of acquired drug resistance

2. Enz

A
  1. Enzymatic inactivation of the drug ( penicillin, aminoglycosides, chloramphenicol)
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36
Q

Mechanism of acquired drug resistance

3. Dec conv

A

Decreased conversion of a drug to the active growth inhibitory compound (flucytosine)

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37
Q

Mechanism of acquired drug resistance

4. Inc

A

Increased concentration of the metabolite antagonizing the drug action (sulfonamides)

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38
Q

Mechanism of acquired drug resistance

5. Altered

A

Altered amount of drug receptor (trimethoprim)

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39
Q

Mechanism of acquired drug resistance

6. Dec aff

A

Decreased affinity of receptor for the drug ( lsulfonamides, streptomycin, rifampicin)

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40
Q

Prophylactic antibiotic therapy

A

To prevent infection in those exposed or to prevent development of potentially dangerous disease in those who already have evidence of infection

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41
Q

Surgical chemoprophylaxis

A
  1. Antibiotic should be active vs common surgical wound pathogens; unnecessarily broad coverage should be avoided
  2. Efficacy in clinical trials
  3. Achieve concentrations higher than the MiC of suspected pathogens and these concentrations must be present at the time of incision
  4. Shortest possible course
  5. Reserved for therapy of resistant infections
  6. The least expensive
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42
Q

General adverse effects

A 
1. Hypersensitivity
2 idiosyncratic 
3. Toxicity rxn
4. Biologic anf metabolic alterations in the host
5. Treatment failure/ relapse
6. Masking effect
7. Adverse drug interaction
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43
Q

Misuse or abuse practices

A
  1. Use in self-limited infections
  2. Empiric use in fever of undetermined origin
    3! Misuse of chemoprophylaxis
  3. Misuse of antibiotic combinations
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44
Q

Antimicrobials MOA 1

A

Ligands whose active chemical moiety binds with microbial protein receptors which are essential components of biochemical reactions in the microbes

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45
Q

Penicillin MOA

A

Binds with PBP causing selective inhibition of transpeptidase

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46
Q

Penicillin mechanism of resistance

A

Inactivation by beta lactamase

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47
Q

Penicillin drugs

A 
Penicillin G (benzylpenicillin G)
Penicillin V (phenoxymethylpenicillin)
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48
Q

Anti-staphylococcal penicillin

A

Methicillin
Naphcillin, oxacillin
Dicloxacillin, cloxacillin, flucloxacillin

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49
Q

Extended-spectrum penicillin

A
  1. Aminopenicillin (amoxicillin, ampicillin)
  2. Ureidopenicillin (piperacillin)
  3. Carboxylenicillin (ticarcillin, carbenicillin)
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50
Q

Penicillin PD

A

High protein binding
Highly distributed in body fluids and tissues
Poor intracellular concentrations
Urine excretion

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51
Q

PEnicillin PD

A

Time-dependent killing: efficacy is directly related to time above MIC and becomes independeny of concentration once the MiC has been reached

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52
Q

Penicllin G drug of choice for

Pemicillin V

A 
1. Strep pyogenes
Strep pneumoniae
Non beta lactamase producing staph aureus
Enterococcus faecalis
Neisseria meningitidis
Treponema pallidum
Leptospira spp
Clostridium tryani actinomyces
2. Strep pyogenes
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53
Q

Uses for anti staphylococcal penicillins

A

Methicillin-sensitive S. Aureus

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54
Q

Uses for aminopenicillin

A 
Strep pneumoniae
Shigella
Salmonella
E. Coli
Listeria monocytogenes
Enterococcus faecalis
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55
Q

Use for carboxypenicillins

A

Pseudomonas aeruginosa

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56
Q

Ureidopenicillin use

A

P. Aeruginosa

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57
Q

Penicillin AE common

A

Hypersensitivity, rash, GI disturbances

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58
Q

Penicillin AE occasional

A

Hematologic disturbances

Pseudomembranous colitis

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59
Q

Penicillin AE rare

A 
Anaphylactic shock
Serum sickness
Muscle irritability, seizure
Hemolytic anemia
Interstitial nephrittis
Hepatitis
Agranulocytosis, neutropenia
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60
Q

Beta lactamase inhibitor moa

A

Bind irreversibly to the catalytic site of beta lactamases rendering them inactive

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61
Q

First gen cephalosporins
Oral
Uses

A
  1. Cephalexin
    Cefadroxil
  2. Strep and staph; surgical prophylaxis; e. Coli
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62
Q

Second gen cephalosporin
Oral
Uses

A 
1. Cefuroxime
Cefaclor
Cefprozil
Loracarbef
2. Bacteroides fragilis; broader than first gen
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63
Q

3rd gen cephalosporin
Oral
Uses

A
  1. Cefixime
    Cefpodoxime
    Cefdinir
  2. Meningitis caused by penicillin-resistant strep pneumoniae; pseudomonas aeruginosa; neisseria gonorrhea; MDR salmonella typhi, etc
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64
Q

Cephalosporins AE common

A

GI disturbances, thrombophlebitis

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65
Q

Cephalosporins AE occasional

A

Hypersensitivity, serum sickness-like reactions, bile sludging, pseudocholelithiasis, hematologic disturbances, disulfram like rxns

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66
Q

Cephalosporins AE rare

A

Anaphylactic shock, interstitial nephritis and tubular necrosis, pseudomembranous colitis, hepatitis, seizure

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67
Q

Monobactam occasional AE

A

Hypersensitivity
GI disturbances
Transaminitis
Local reactiob

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68
Q

Monobactam rare AE

A

Hematologic disturbances

Pseudomembranous colitis

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69
Q

Carbapanem uses

A

ESBLs, serious miced aerobic and anaerobic infections

Enterobacter spo

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70
Q

Carbapanem AE common

A

GI disturbances

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71
Q

Carbapanem AE occasional

A

Hypersensitivity,
Hematologic disturbances,
Local reactions

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72
Q

Carbapanem AE rare

A

Seizure, hallucination, anaphylactic shock, serum sickness, pseudomembranous colitis

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73
Q

Glycopeotides MIA

A
  1. Inhibit cell wall synthesis

2. Inhibit transglycosylase

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74
Q

Glycopeptide PK

A

Tine-dependent killing: efficacy is directly related ti time above MIC, and becomes independent of concentration once the MIC has been reached

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75
Q

Vancomycin uses

A

Caused by MRSA; for coagulase negative staphylococci; enterococci; penicillin-resistant strep pneumoniae

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76
Q

Vancomycin AE common

A

Red man or red neck; phlebitis to injection site; GI disturbances

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77
Q

Vancomycin AE occasional

A

Ototoxicity and nephrotoxicity (reversible)

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78
Q

Vancomycin AE rare

A

Macular rash, hematologic disturbances

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79
Q

Lipopeptide (daptomycin) MOA

A

Bind to cell membrane via Ca dependent insertion of its lipid taol; depolarization of cell membrane with K efflux and rapid cell death

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80
Q

Lipopeptide PK

A

Poor oral absorption; distributed mainly into plasma and interstitial fluid; little CNS and bone penetration; excreted in urine

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81
Q

Lipopeptide PD

A

Concentration-dependent killing: as the serum concentration is increased above MIC, bactericidal activity is also increased and at a more rapid rate

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82
Q

Lipopeptide uses

A

Vancomycin-resistant strains of s. Aureus and enterococci; alternative drug for vancomycin for treatment of MRSA bacteremia

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83
Q

Lipopeptide common AE

A

Muscle toxicity(reversible)

84
Q

Lipopeptide occasional AE

A

Allergic pneumonitis

85
Q

Polymixin MOA

A

Attach and disrupt bacterial cell membrane; cationic detergent; bind to anionic lps molecules leading to permeability changes in cell membrane; leakage of intracellular metabolites and nucleosides, causing cell death

86
Q

Polymixin PD

A

Concentration-dependent killing: as the serum concentration is increased above MIC, the bactericidal activity is also increased and at a more rapid

87
Q

Polymixibs uses

A

Infections caused by multidrug-resistant organisms like pneumonia, skin and soft tissue infections, intraabdominal infections, bacteremia

88
Q

Polymixins AE common

A

Nephrotoxicity (reversible)

89
Q

Polymixins occasional AE

A

Neurotoxicity, neuromuscular blockade

90
Q

Polymixins AE rare

A

Hypersensitivity

91
Q

Aminoglycosides MOA

A
  1. Block formation of the initiation complex
  2. Block translocation
  3. Misreading of the mRNA
92
Q

Aminoglycosides mechanism of resistance

A

Inactivation by transferase enzymes; impaired entry into the cell; modification of ribosomal binding site/ribosomal protection

93
Q

Aminoglycosides PK

A
  1. Very poorly absorbed from intact Gi tract
  2. Poorly distributed in tissues, and non-inflamed meninges except in neonates
  3. Excreted in urine
  4. Synergism with beta lactam antibiotics if given sequentially
  5. Antagonism with other bacteriostatic antibiotic
94
Q

Aminoglycosides PD

A
  1. Concentration-dependent killing: as the serum comcentration increases above MIC, the bactericidal activity is also increased and at a more rapid rate
  2. Single large dose
  3. Post-antibiotic effect
95
Q

Aminoglycosides Uses

A

Used in combination with beta lactam antibiotics for serious infections; not recommended as monotherapy for P. Aeruginosa; not recommended for anaerobic infections; m. Tuberculosis; contraindicated for pregnancy

96
Q

Aminoglycosides AE common

A

Ototoxicity( irreversible); nephrotoxicity (reversible)

97
Q

Aminoglycosides AE rare

A

Hypersensitivity, anaphylacis; loval reaction; neuromuscular blockade (results in respiratory paralysis)

98
Q

Penicillin MOA

A

Binds with PBP causing selective inhibition of transpeptidase

99
Q

Penicillin mechanism of resistance

A

Inactivation by beta lactamase

100
Q

Penicillin drugs

A 
Penicillin G (benzylpenicillin G)
Penicillin V (phenoxymethylpenicillin)
101
Q

Anti-staphylococcal penicillin

A

Methicillin
Naphcillin, oxacillin
Dicloxacillin, cloxacillin, flucloxacillin

102
Q

Extended-spectrum penicillin

A
  1. Aminopenicillin (amoxicillin, ampicillin)
  2. Ureidopenicillin (piperacillin)
  3. Carboxylenicillin (ticarcillin, carbenicillin)
103
Q

Penicillin PD

A

High protein binding
Highly distributed in body fluids and tissues
Poor intracellular concentrations
Urine excretion

104
Q

PEnicillin PD

A

Time-dependent killing: efficacy is directly related to time above MIC and becomes independeny of concentration once the MiC has been reached

105
Q

Penicllin G drug of choice for

Pemicillin V

A 
1. Strep pyogenes
Strep pneumoniae
Non beta lactamase producing staph aureus
Enterococcus faecalis
Neisseria meningitidis
Treponema pallidum
Leptospira spp
Clostridium tryani actinomyces
2. Strep pyogenes
106
Q

Uses for anti staphylococcal penicillins

A

Methicillin-sensitive S. Aureus

107
Q

Uses for aminopenicillin

A 
Strep pneumoniae
Shigella
Salmonella
E. Coli
Listeria monocytogenes
Enterococcus faecalis
108
Q

Use for carboxypenicillins

A

Pseudomonas aeruginosa

109
Q

Ureidopenicillin use

A

P. Aeruginosa

110
Q

Protein synthesis inhibitor

A 
Tetracyclines
Glycyckine
Macrolides
Lincosamide
Chloramphenicol
Oxazolidinone
Streptogramins
111
Q

[tetracycline]

Short-acting 6-8 hrs

A

Chlortetracycline

Tetracycline

Oxytetracycline

112
Q

[tetracycline]

Intermediate acting 12 hrs

A

Demeclocycline
Methacycline
Lymecycline

113
Q

[tetracycline]

Long-acting 16-18 hours

A

Doxyxycline

Minocycline

114
Q

[tetracycline]

Moa– most imprtant

A

To 30s subunit

Prevent binding of incoming charged trna unit ti the acceptor site

Efflux pump– most important

Modification of ribosomal binding site/ ribosomal protection

115
Q

[tetracycline]

PK

A

Absorption impaired by food except long acting, antacids, dairy products, and divalent cations
High protein binding

Widely distributed

Intracellular penetration
Excreted in bile and urine except doxycycline

Pass placenta and excreted in milk

116
Q

[tetracycline]

PD

A

Time dependent

117
Q

[tetracycline]

Uses- Deoxycycline

A

Doc for ricketssiae

118
Q

[tetracycline]

Common AE

A

Gi disturbance, local reaction (thrombophlebitis),
Oral candidiasis, permanent teeth discoloration and enamel hypoplasia
Bone deformity and growth retardation

119
Q

[tetracycline]

Occasional AE

A

Hepatitis, liver failure

Photosensitivity (demeclocycline)

Esophageal ulceration

Pancreatitis (tetracycline)

Visual disturbances -tetra

Vestibular toxicity, vertigo -mino

Pseudomembranous colitis

Aggravate preexisting renal failure

120
Q

[tetracycline]

Rare AE

A

Hypersensitivity, drug eruption

Pseudomotor cerebri

DI

Interstitial nephritis

Lupus like sydrome

Black pigmentation of thyroid

Gray pigmentation of nail, skin, sclera

121
Q

[glycycline]

A

Tigecycline

Third gen tetracycline

122
Q

[glycycline]

Moa

A

Bind to 30s subunit

Prevent binding of incoming charged trna unit

123
Q

[glycycline]

PK

A

Iv

Poorly absorbed, oral

Widely distributed

Excellent intracellular penetration

Low urinary concentration

Bile and urine

124
Q

[glycycline]

Uses

A

Infxns caused by multidrug resistant organisms– skin and soft tissue infection, intraabdominal infections

125
Q

[glycycline]

AE

A

Same as tetracyclines- pregnancy risk category D

Hematologic disturbances

Pancreatitis

Transaminitis

Somnolence

126
Q

[macrolides]

Moa

A

Bind to 50s subunit

Block peptide chain elongation

127
Q

[macrolides]

Mechanism of resistance

A
  1. Modification of ribosomal binding site/ribosomal protection
  2. Efflux pump
  3. Production of esterases
128
Q

[macrolides]

Pk-erythromycin

A
  1. Absorption impaired by food
  2. Widely distributed
  3. Good intracellular penetration
  4. Bile
  5. Pass the placenta: excreted in milk
  6. Inhibit cytochrome p450
129
Q

[macrolides]

Pd

A

Time dependent

130
Q

[macrolides]

Uses- erythromycin

A

Doc for legionella pneumophilia, mycoplasma pneumoniae, chlamydia spp.; corynebacterium spp.; bordetella pertusis

Penicillin substitute for strep pyogenes to those with allergy

131
Q

[macrolides]

Common AE

A

Gi disturbances - diarrhea abdominal cramps due to motilin and dose related

132
Q

[macrolides]

Occasinal AE

A

Acute cholestatic hepatitis (estolate)

Stomatitis

Thrombophlebitis

133
Q

[macrolides]

Rare AE

A

Hypersensitivity

Infantile hypertrophic pyloric stenosis

Prolonged QT interval, arrythmia

Transient hearing loss

Pseudomembranous colitis

134
Q

[clarithromycin]

Compared to erythromycin

A
  • most active against H. Influenza amd mycobacterium avium
  • longer half life
  • absorption less affected by food
  • urine
  • less gi disturbance
135
Q

[azithromycin]

A

Same with clarithromycin but add[macrolides]d coverage for salmonella and shigella

Doc for bartonella henselae

136
Q

[azithromycin]

Compared to other macrolides

A

Absorptin is impaired with food

Best tissue penetratin

Concentration dpendent killing

Does not inhibit cyp450

Less gi disturbances

137
Q

[lincosamide]

A

Clindamycin

138
Q

[lincosamide]

Moa

A

Bind to 50s subunit

Block peptide bond formation

Block translocation

139
Q

[lincosamide]

Mechanism of resistance

A

Modification of ribosomal binding site/ribosomal protection

Enzymatic inactivation

140
Q

[lincosamide]

PD

A

Time dependent

141
Q

[lincosamide]

PK

A

Absorption not affected by food

High protein binding

Good distribution to tissues

Can penetrate abscesses

Bile and urine

Cross placenta

142
Q

[lincosamide]

Uses

A

Doc for community acquired MRSA (skin and soft tissue infection)

Anaerobic infxns above the level of the diaphragm except cns

Alternative for staph infxns

143
Q

[lincosamide]

Common AE

A

Gi disturbances -diarrhea, nausea or vomiting

Hypersensitivity

144
Q

[lincosamide]

Occasional AE

A

Pseudomembranous colitis, toxic megacolon

145
Q

[lincosamide]

Rare AE

A

Esophageal ulceratin

Transaminitis, hepatitis

Hematologic disturbamces - neutropenia, thrombocytopenia

146
Q

[chloramphenicol]

Moa

A

Bind to 50s subunit

Block peptide formation

147
Q

[chloramphenicol]

MOR

A

Production of chloramphenicol acetyltransferase

148
Q

[chloramphenicol]

PK

A

Available as prodrug

Low pb

Widely distributed

Good ontracellular penetration

Metab in liver

Urine and bile

Pass placenta; excreted in milk

Inhibit cyp450

149
Q

[chloramphenicol]

PD

A

Time dependent

150
Q

[chloramphenicol]

Use

A

Alternative drug for beta lactam

Salmonella typhi, shigella, ricketssia

151
Q

[chloramphenicol]

Common AE

A

Dose related anemia reversible - due to inhibition of mitochondrial protein synthesis

Gray baby syndrome- due to lack pf effective glucuronic acid conjugatin

152
Q

[chloramphenicol]

Occasional AE

A

Gi disturbances

Oral candidiasis

153
Q

[chloramphenicol]

Rare AE

A

Aplastic anemia- idiosyncratic, irreversible

Hypersen

Peripheral neuropathy

Optic neuritis

Pseudomembranous colitis

154
Q

[oxazolididone]

A

Linezolid

155
Q

[oxazolididone]

MOa

A

Bind to 50s

Inhibit formatin of ribosome complex that initiates protein syntesis

No cross resistance

156
Q

[oxazolididone]

PK

A

100% F oral

Widely distributed

Urine

Time dependent

157
Q

[oxazolididone]

Uses

A

Multidrug resistant gram positive cocci -MRSA, VRE

158
Q

[oxazolididone]

Common AE

A

Hematologic disturbances reversible- thrombocytopenia mostcommon, anemia, neutropenia

159
Q

[oxazolididone]

Occasional AE

A

Gi disturbances- nausea, vomiting, diarrhea

Optic and peripheral neuropathy - mitochondrial protein symthesis, mag lead to blindness

Lactic acidosis-mitochondrial protein syn

Serotonin syndrome - fever, agitation, confusion, tremors. Diaphoresis– due to monoamine oxidase inhibition, cause hypertensive crisis; risk factors include intake with tyramine rich food, pseudohedrine, phenylpropanolamine

160
Q

[streptogramins]

A

Srep B- quinupristin

A- dalfropristin

Synergism

161
Q

[streptogramins]

MOA

A

Bind to 50s su unit

Interfere with peptidyl transferase -dalfo

Inhibit peptide chain elongation -quin

162
Q

[streptogramins]

MOR

A

Modificatinof ribosomal binding site or ribosomal protection

Efflux pump

163
Q

[streptogramins]

PK

A

Widely distributed

Excreted in stool

Inhibit cyp3A4

164
Q

[streptogramins]

PD

A

Concentration-dependent

165
Q

[streptogramins]

Uses

A

Infxns caused bu multidrug resistant gram positive cocci except enterococcus faecalis- skin and soft tissue infections, pneumonia, bacteremia

166
Q

[streptogramins]

Common AE

A

Infusion related reactions

Arthralgia-myalgia syndrome

Direct hyperbilirubinemia

167
Q

NUCLEIC ACID SYNTHESIS INHIBITORS

A

Antifolate drugs- trimethoprim - sulfamethoxazole (cotrimoxazole)

DNA Gyrase inhibitors -fluoroquinolones

168
Q

[cotrimoxazole]

A

SMX- sulfanilamide nucleus
TMP- benzypyrimidine

Combi is bactericidal

169
Q

[cotrimoxazole]

MOA smx

A

Smx inhibit dihydropteroate synthase- inhibit production of dihydrofolic acid

170
Q

[cotrimoxazole]

Moa tmp

A

Inhibit dihydrofolate reductase

- inhibit prod of terahydrofolic acid

171
Q

[cotrimoxazole]

Combi moa

A

Blocks sequential step in folic acid synthesis

172
Q

[cotrimoxazole]

Smx mor

A

Overproduction of PABA

Overprod of dihydropteroate synthase with reduced drug binding

Impaired entry into cell

173
Q

[cotrimoxazole]

Tmp mor

A

Overprod of dihydropteroate synthase with reduced drug binding

Impaired entry into cell

174
Q

[cotrimoxazole]

PK

A

Widely distributed in body fluids and tissues including csf and prostate

Metabolized in the liver

Pass placenta

Excreted in urine

175
Q

[cotrimoxazole]

PD

A

Time dependent

176
Q

[cotrimoxazole]

Uses

A

Doc for stenotrophomonas maltophilia

Susceptible mrsa, burkholderia sepacia, salmonella, shigella, nocardia

Prostasis

177
Q

[cotrimoxazole]

Common AE

A

Rash, exfoliative dermatitis, photosen in smx

178
Q

[cotrimoxazole]

Occasinal AE

A

Hematologic disturbances: smx- aplastic anemia, hemolytic anemia, granulocytopenia, thrombocytopenia

Tmp: megaloblastic ane ia, leukopenia, granulocytopenia

179
Q

[cotrimoxazole]

Occasional AE non hema

A

Kerniaterus - pregnancy risk category C – due to lack ofeffective glucuronic acid conjugation in newborn infants; not tecommended during term pregnancy and lactation, and in neonates

Urinary tact disturbamces- crystalluria, he,atueia,

Hyperkalemia

Pseudomembranous colitis

180
Q

[cotrimoxazole]

Rare AE

A

Stevens-jh sons syndrome smx

Hepatitis, cholestasis

Cns disturbances

Methemoglobinemia

Pancreatitis

Lupus like syndrome

181
Q

[fluoroquinolones]

First gen

A

Norfloxacin

182
Q

[fluoroquinolones]

Second

A

Ciprofloxacin, of.oxacin, pefloxacin

183
Q

[fluoroquinolones]

Trd

A

Levofloxacin, gatifloxacin, gemif

Oxacin, moxifloxacin

184
Q

[fluoroquinolones]

MOA

A

Inhibit bacterial topoisomerase II(dna gyrase)- prevents relaxatin of positively superco led DNA

Inhibit topoisomerase IV- interferes with separation of replicated chromosomal DNA into respective daughter cells during cell division

185
Q

[fluoroquinolones]

Mor

A

Modificatin of target enzyme dna gyrase

Impaired entry into the cell

186
Q

[fluoroquinolones]

PK

A

80-95% F oral

Absorption impaired by divalent cations

Widely distributed in body fluids a d tissues including csf amd prostate
High intracellular or tissue penetration

Urine except gemi urine and bile a f moxi bile

187
Q

[fluoroquinolones]

PD

A

Comcentration dpendent

188
Q

[fluoroquinolones]

Uses

A

Pseudomonas aeruginosa, salmonella, shigella, e. Coli, neisseria me ingitidis

189
Q

[fluoroquinolones]

Occasional AE

A

Gi disturbances, cns disturbances, rash, oral candidiasis, transaminitis, hepa, hematologic, hypergly in diabetics, hypogly

190
Q

[fluoroquinolones]

Rare AE

A

Tendinitis, tendon rupture

Retinal detach,ent

Anaphylaxis
Cns disturbances

Peripheral neurpathy

Pseudomembranous colitis

Interstitial nephritis

Vasculitis

Prolonged qt interval, torsades de pointes, ventricular tach

191
Q

Miscellaneous antibiotics

A

Metronidazole
Nitrofurantoin
Fosfomycin

192
Q

[metronidazole]

moa

A

Nitro group reduced intracellular,y by reacting eith reduced ferredoxim

Produce toxic metabolites which are taken up into bacterial dna

193
Q

[metronidazole]

PK

A

Oral iv rectal 100% F

Widely distributed

Penetrate abscesses including those in the brain

Urine and feces

194
Q

[metronidazole]

PD

A

Concentratin dependent

195
Q

[metronidazole]

Uses

A

Clostridium difficile colitis

Anaerobic infxns below the level of the diaphragm

Brain anscesses

196
Q

[metronidazole]

Common AE

A

Gi disturbances

Dry mouth, furrytongue

197
Q

[metronidazole]

Occasinal AE

A

Insomnia

Urethral burnimg

Darkening of urine

Phlebitis

Disulfiram like effect

198
Q

[metronidazole]

Rare AE

A

Cns disturbances - seizure. Ata ia, dysarthria

Peripheral and optic neuropathy

Pancreatitis

199
Q

[nitrofurantoin]

Moa

A

Rapid intracellular conversion to highly reactive intermediates by bacterial reductased

200
Q

[nitrofurantoin]

PK

A

Well absorbed oral

Very rapid excretion in urine, no systemic antibacterial effect

201
Q

[nitrofurantoin]

Use

A

Urinary antiseptic - uncomplicated acute cystisis)

202
Q

[nitrofurantoin]

Common AE

A

Gi disturbances - nausea, vomiting, diarrhea

203
Q

[nitrofurantoin]

Occasional AE

A

Neuropathy

Hemolytic anemia

Rash

Pulmonary infiltratin, fibrosis

204
Q

[fosfomycin]

Moa

A

Inhibit the very early stage of cell wall synthesis - inhibit enolpyruvate transferase, block addition of phosphoenolpyruvatr to UDP-N-acetylglucosamine

205
Q

[fosfomycin]

Pk

A

40% F after oral administration

Poorly distributed in tissues

Excreted in urine

206
Q

[fosfomycin]

Use

A

Uncomplicated acute cystisis

Not for first line agent for treatment for mdr infection

Pharmacology (2 decks)

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