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Chemotherapy Of Antimicrobial Infections Flashcards

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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
Hepatobiliary excretion
``` Cefoperazone/ceftriaxone Chloramphenicol Clindamycon/doxycyclin Azithromycin Linezolod Metronidazole Most azole but nit fluconazole Mocifloxacin Nafcillin Quinupristi rifampicin ```
26
Renal and biliary excretion
``` Ampicillin Cefixime Isoniazid Oxacillin and related drugs Pyrazinamide Telithromycin ```
27
Renal excretion
``` Aciclovir Aminoglycosides Amphotericin B Aztreonam Carbapanemes Cephalosporins Clarithromycin Fluoroquinolones Penicillintetracyclin Vancomycin ```
28
Rationale for antibiotic combination therapy
1 provide broad spectrum for empiric therapy 2. Treat polymicrobial infection 3. Prevent/ delay emergence of resistance 4. Decrease dose-related toxicity 5. Obtain enhanced inhibition/killing synergism
29
Mechanism of antimicrobial synergism
1. Blockade of sequential steps in metabolic sequence 2. Inhibition of enzymatic inactivation 3. Enhancement of antimicrobial uptake
30
[synergism] | Blockade of sequential steps in metabolic sequence
Sulfamethoxazole + trimethoprim
31
[synergism] | Inhibition of enzymatic inactivation
1. Betalactamase inhibitor and beta lactam antibiotic 2. Clavulanate K and amoxicillin 3. Sulbactam and ampicillin 4. Tazobactam and piperacillin
32
[synergism] | Enhancement of antimicrobial uptake
1. Penicillin and aminoglycosides 2. Ampicillin and gentamycin 3. Ceftazidime and amikacin
33
Mechanism of antimicrobial antagonism and example
1. Inhibition of bactericidal activity by bacteriostatic antibiotic (betalactams and tetracycline) 2. Induction of enzymatic inactivation (rifampicin and protease inhibitors)
34
Mechanism of acquired drug resistance | 1. Decrease
Decreased drug uptake or increase efflux of the drug ( tetracycline, quinolones, aminoglycoside, macrolides, chloramphenicol)
35
Mechanism of acquired drug resistance | 2. Enz
2. Enzymatic inactivation of the drug ( penicillin, aminoglycosides, chloramphenicol)
36
Mechanism of acquired drug resistance | 3. Dec conv
Decreased conversion of a drug to the active growth inhibitory compound (flucytosine)
37
Mechanism of acquired drug resistance | 4. Inc
Increased concentration of the metabolite antagonizing the drug action (sulfonamides)
38
Mechanism of acquired drug resistance | 5. Altered
Altered amount of drug receptor (trimethoprim)
39
Mechanism of acquired drug resistance | 6. Dec aff
Decreased affinity of receptor for the drug ( lsulfonamides, streptomycin, rifampicin)
40
Prophylactic antibiotic therapy
To prevent infection in those exposed or to prevent development of potentially dangerous disease in those who already have evidence of infection
41
Surgical chemoprophylaxis
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
42
General adverse effects
``` 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 ```
43
Misuse or abuse practices
1. Use in self-limited infections 2. Empiric use in fever of undetermined origin 3! Misuse of chemoprophylaxis 4. Misuse of antibiotic combinations
44
Antimicrobials MOA 1
Ligands whose active chemical moiety binds with microbial protein receptors which are essential components of biochemical reactions in the microbes
45
Penicillin MOA
Binds with PBP causing selective inhibition of transpeptidase
46
Penicillin mechanism of resistance
Inactivation by beta lactamase
47
Penicillin drugs
``` Penicillin G (benzylpenicillin G) Penicillin V (phenoxymethylpenicillin) ```
48
Anti-staphylococcal penicillin
Methicillin Naphcillin, oxacillin Dicloxacillin, cloxacillin, flucloxacillin
49
Extended-spectrum penicillin
1. Aminopenicillin (amoxicillin, ampicillin) 2. Ureidopenicillin (piperacillin) 3. Carboxylenicillin (ticarcillin, carbenicillin)
50
Penicillin PD
High protein binding Highly distributed in body fluids and tissues Poor intracellular concentrations Urine excretion
51
PEnicillin PD
Time-dependent killing: efficacy is directly related to time above MIC and becomes independeny of concentration once the MiC has been reached
52
Penicllin G drug of choice for | Pemicillin V
``` 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 ```
53
Uses for anti staphylococcal penicillins
Methicillin-sensitive S. Aureus
54
Uses for aminopenicillin
``` Strep pneumoniae Shigella Salmonella E. Coli Listeria monocytogenes Enterococcus faecalis ```
55
Use for carboxypenicillins
Pseudomonas aeruginosa
56
Ureidopenicillin use
P. Aeruginosa
57
Penicillin AE common
Hypersensitivity, rash, GI disturbances
58
Penicillin AE occasional
Hematologic disturbances | Pseudomembranous colitis
59
Penicillin AE rare
``` Anaphylactic shock Serum sickness Muscle irritability, seizure Hemolytic anemia Interstitial nephrittis Hepatitis Agranulocytosis, neutropenia ```
60
Beta lactamase inhibitor moa
Bind irreversibly to the catalytic site of beta lactamases rendering them inactive
61
First gen cephalosporins Oral Uses
1. Cephalexin Cefadroxil 2. Strep and staph; surgical prophylaxis; e. Coli
62
Second gen cephalosporin Oral Uses
``` 1. Cefuroxime Cefaclor Cefprozil Loracarbef 2. Bacteroides fragilis; broader than first gen ```
63
3rd gen cephalosporin Oral Uses
1. Cefixime Cefpodoxime Cefdinir 2. Meningitis caused by penicillin-resistant strep pneumoniae; pseudomonas aeruginosa; neisseria gonorrhea; MDR salmonella typhi, etc
64
Cephalosporins AE common
GI disturbances, thrombophlebitis
65
Cephalosporins AE occasional
Hypersensitivity, serum sickness-like reactions, bile sludging, pseudocholelithiasis, hematologic disturbances, disulfram like rxns
66
Cephalosporins AE rare
Anaphylactic shock, interstitial nephritis and tubular necrosis, pseudomembranous colitis, hepatitis, seizure
67
Monobactam occasional AE
Hypersensitivity GI disturbances Transaminitis Local reactiob
68
Monobactam rare AE
Hematologic disturbances | Pseudomembranous colitis
69
Carbapanem uses
ESBLs, serious miced aerobic and anaerobic infections | Enterobacter spo
70
Carbapanem AE common
GI disturbances
71
Carbapanem AE occasional
Hypersensitivity, Hematologic disturbances, Local reactions
72
Carbapanem AE rare
Seizure, hallucination, anaphylactic shock, serum sickness, pseudomembranous colitis
73
Glycopeotides MIA
1. Inhibit cell wall synthesis | 2. Inhibit transglycosylase
74
Glycopeptide PK
Tine-dependent killing: efficacy is directly related ti time above MIC, and becomes independent of concentration once the MIC has been reached
75
Vancomycin uses
Caused by MRSA; for coagulase negative staphylococci; enterococci; penicillin-resistant strep pneumoniae
76
Vancomycin AE common
Red man or red neck; phlebitis to injection site; GI disturbances
77
Vancomycin AE occasional
Ototoxicity and nephrotoxicity (reversible)
78
Vancomycin AE rare
Macular rash, hematologic disturbances
79
Lipopeptide (daptomycin) MOA
Bind to cell membrane via Ca dependent insertion of its lipid taol; depolarization of cell membrane with K efflux and rapid cell death
80
Lipopeptide PK
Poor oral absorption; distributed mainly into plasma and interstitial fluid; little CNS and bone penetration; excreted in urine
81
Lipopeptide PD
Concentration-dependent killing: as the serum concentration is increased above MIC, bactericidal activity is also increased and at a more rapid rate
82
Lipopeptide uses
Vancomycin-resistant strains of s. Aureus and enterococci; alternative drug for vancomycin for treatment of MRSA bacteremia
83
Lipopeptide common AE
Muscle toxicity(reversible)
84
Lipopeptide occasional AE
Allergic pneumonitis
85
Polymixin MOA
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
Polymixin PD
Concentration-dependent killing: as the serum concentration is increased above MIC, the bactericidal activity is also increased and at a more rapid
87
Polymixibs uses
Infections caused by multidrug-resistant organisms like pneumonia, skin and soft tissue infections, intraabdominal infections, bacteremia
88
Polymixins AE common
Nephrotoxicity (reversible)
89
Polymixins occasional AE
Neurotoxicity, neuromuscular blockade
90
Polymixins AE rare
Hypersensitivity
91
Aminoglycosides MOA
1. Block formation of the initiation complex 2. Block translocation 3. Misreading of the mRNA
92
Aminoglycosides mechanism of resistance
Inactivation by transferase enzymes; impaired entry into the cell; modification of ribosomal binding site/ribosomal protection
93
Aminoglycosides PK
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
Aminoglycosides PD
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
Aminoglycosides Uses
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
Aminoglycosides AE common
Ototoxicity( irreversible); nephrotoxicity (reversible)
97
Aminoglycosides AE rare
Hypersensitivity, anaphylacis; loval reaction; neuromuscular blockade (results in respiratory paralysis)
98
Penicillin MOA
Binds with PBP causing selective inhibition of transpeptidase
99
Penicillin mechanism of resistance
Inactivation by beta lactamase
100
Penicillin drugs
``` Penicillin G (benzylpenicillin G) Penicillin V (phenoxymethylpenicillin) ```
101
Anti-staphylococcal penicillin
Methicillin Naphcillin, oxacillin Dicloxacillin, cloxacillin, flucloxacillin
102
Extended-spectrum penicillin
1. Aminopenicillin (amoxicillin, ampicillin) 2. Ureidopenicillin (piperacillin) 3. Carboxylenicillin (ticarcillin, carbenicillin)
103
Penicillin PD
High protein binding Highly distributed in body fluids and tissues Poor intracellular concentrations Urine excretion
104
PEnicillin PD
Time-dependent killing: efficacy is directly related to time above MIC and becomes independeny of concentration once the MiC has been reached
105
Penicllin G drug of choice for | Pemicillin V
``` 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
Uses for anti staphylococcal penicillins
Methicillin-sensitive S. Aureus
107
Uses for aminopenicillin
``` Strep pneumoniae Shigella Salmonella E. Coli Listeria monocytogenes Enterococcus faecalis ```
108
Use for carboxypenicillins
Pseudomonas aeruginosa
109
Ureidopenicillin use
P. Aeruginosa
110
Protein synthesis inhibitor
``` Tetracyclines Glycyckine Macrolides Lincosamide Chloramphenicol Oxazolidinone Streptogramins ```
111
[tetracycline] Short-acting 6-8 hrs
Chlortetracycline Tetracycline Oxytetracycline
112
[tetracycline] Intermediate acting 12 hrs
Demeclocycline Methacycline Lymecycline
113
[tetracycline] Long-acting 16-18 hours
Doxyxycline Minocycline
114
[tetracycline] | Moa-- most imprtant
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
[tetracycline] PK
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
[tetracycline] PD
Time dependent
117
[tetracycline] Uses- Deoxycycline
Doc for ricketssiae
118
[tetracycline] Common AE
Gi disturbance, local reaction (thrombophlebitis), Oral candidiasis, permanent teeth discoloration and enamel hypoplasia Bone deformity and growth retardation
119
[tetracycline] Occasional AE
Hepatitis, liver failure Photosensitivity (demeclocycline) Esophageal ulceration Pancreatitis (tetracycline) Visual disturbances -tetra Vestibular toxicity, vertigo -mino Pseudomembranous colitis Aggravate preexisting renal failure
120
[tetracycline] Rare AE
Hypersensitivity, drug eruption Pseudomotor cerebri DI Interstitial nephritis Lupus like sydrome Black pigmentation of thyroid Gray pigmentation of nail, skin, sclera
121
[glycycline]
Tigecycline Third gen tetracycline
122
[glycycline] Moa
Bind to 30s subunit Prevent binding of incoming charged trna unit
123
[glycycline] PK
Iv Poorly absorbed, oral Widely distributed Excellent intracellular penetration Low urinary concentration Bile and urine
124
[glycycline] Uses
Infxns caused by multidrug resistant organisms-- skin and soft tissue infection, intraabdominal infections
125
[glycycline] AE
Same as tetracyclines- pregnancy risk category D Hematologic disturbances Pancreatitis Transaminitis Somnolence
126
[macrolides] Moa
Bind to 50s subunit Block peptide chain elongation
127
[macrolides] Mechanism of resistance
1. Modification of ribosomal binding site/ribosomal protection 2. Efflux pump 3. Production of esterases
128
[macrolides] Pk-erythromycin
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
[macrolides] Pd
Time dependent
130
[macrolides] Uses- erythromycin
Doc for legionella pneumophilia, mycoplasma pneumoniae, chlamydia spp.; corynebacterium spp.; bordetella pertusis Penicillin substitute for strep pyogenes to those with allergy
131
[macrolides] Common AE
Gi disturbances - diarrhea abdominal cramps due to motilin and dose related
132
[macrolides] Occasinal AE
Acute cholestatic hepatitis (estolate) Stomatitis Thrombophlebitis
133
[macrolides] Rare AE
Hypersensitivity Infantile hypertrophic pyloric stenosis Prolonged QT interval, arrythmia Transient hearing loss Pseudomembranous colitis
134
[clarithromycin] Compared to erythromycin
- most active against H. Influenza amd mycobacterium avium - longer half life - absorption less affected by food - urine - less gi disturbance
135
[azithromycin]
Same with clarithromycin but add[macrolides]d coverage for salmonella and shigella Doc for bartonella henselae
136
[azithromycin] Compared to other macrolides
Absorptin is impaired with food Best tissue penetratin Concentration dpendent killing Does not inhibit cyp450 Less gi disturbances
137
[lincosamide]
Clindamycin
138
[lincosamide] Moa
Bind to 50s subunit Block peptide bond formation Block translocation
139
[lincosamide] Mechanism of resistance
Modification of ribosomal binding site/ribosomal protection Enzymatic inactivation
140
[lincosamide] PD
Time dependent
141
[lincosamide] PK
Absorption not affected by food High protein binding Good distribution to tissues Can penetrate abscesses Bile and urine Cross placenta
142
[lincosamide] Uses
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
[lincosamide] Common AE
Gi disturbances -diarrhea, nausea or vomiting Hypersensitivity
144
[lincosamide] Occasional AE
Pseudomembranous colitis, toxic megacolon
145
[lincosamide] Rare AE
Esophageal ulceratin Transaminitis, hepatitis Hematologic disturbamces - neutropenia, thrombocytopenia
146
[chloramphenicol] Moa
Bind to 50s subunit Block peptide formation
147
[chloramphenicol] MOR
Production of chloramphenicol acetyltransferase
148
[chloramphenicol] PK
Available as prodrug Low pb Widely distributed Good ontracellular penetration Metab in liver Urine and bile Pass placenta; excreted in milk Inhibit cyp450
149
[chloramphenicol] PD
Time dependent
150
[chloramphenicol] Use
Alternative drug for beta lactam Salmonella typhi, shigella, ricketssia
151
[chloramphenicol] Common AE
Dose related anemia reversible - due to inhibition of mitochondrial protein synthesis Gray baby syndrome- due to lack pf effective glucuronic acid conjugatin
152
[chloramphenicol] Occasional AE
Gi disturbances Oral candidiasis
153
[chloramphenicol] Rare AE
Aplastic anemia- idiosyncratic, irreversible Hypersen Peripheral neuropathy Optic neuritis Pseudomembranous colitis
154
[oxazolididone]
Linezolid
155
[oxazolididone] MOa
Bind to 50s Inhibit formatin of ribosome complex that initiates protein syntesis No cross resistance
156
[oxazolididone] PK
100% F oral Widely distributed Urine Time dependent
157
[oxazolididone] Uses
Multidrug resistant gram positive cocci -MRSA, VRE
158
[oxazolididone] Common AE
Hematologic disturbances reversible- thrombocytopenia mostcommon, anemia, neutropenia
159
[oxazolididone] Occasional AE
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
[streptogramins]
Srep B- quinupristin A- dalfropristin Synergism
161
[streptogramins] MOA
Bind to 50s su unit Interfere with peptidyl transferase -dalfo Inhibit peptide chain elongation -quin
162
[streptogramins] MOR
Modificatinof ribosomal binding site or ribosomal protection Efflux pump
163
[streptogramins] PK
Widely distributed Excreted in stool Inhibit cyp3A4
164
[streptogramins] PD
Concentration-dependent
165
[streptogramins] Uses
Infxns caused bu multidrug resistant gram positive cocci except enterococcus faecalis- skin and soft tissue infections, pneumonia, bacteremia
166
[streptogramins] Common AE
Infusion related reactions Arthralgia-myalgia syndrome Direct hyperbilirubinemia
167
NUCLEIC ACID SYNTHESIS INHIBITORS
Antifolate drugs- trimethoprim - sulfamethoxazole (cotrimoxazole) DNA Gyrase inhibitors -fluoroquinolones
168
[cotrimoxazole]
SMX- sulfanilamide nucleus TMP- benzypyrimidine Combi is bactericidal
169
[cotrimoxazole] MOA smx
Smx inhibit dihydropteroate synthase- inhibit production of dihydrofolic acid
170
[cotrimoxazole] Moa tmp
Inhibit dihydrofolate reductase | - inhibit prod of terahydrofolic acid
171
[cotrimoxazole] Combi moa
Blocks sequential step in folic acid synthesis
172
[cotrimoxazole] Smx mor
Overproduction of PABA Overprod of dihydropteroate synthase with reduced drug binding Impaired entry into cell
173
[cotrimoxazole] Tmp mor
Overprod of dihydropteroate synthase with reduced drug binding Impaired entry into cell
174
[cotrimoxazole] PK
Widely distributed in body fluids and tissues including csf and prostate Metabolized in the liver Pass placenta Excreted in urine
175
[cotrimoxazole] PD
Time dependent
176
[cotrimoxazole] Uses
Doc for stenotrophomonas maltophilia Susceptible mrsa, burkholderia sepacia, salmonella, shigella, nocardia Prostasis
177
[cotrimoxazole] Common AE
Rash, exfoliative dermatitis, photosen in smx
178
[cotrimoxazole] Occasinal AE
Hematologic disturbances: smx- aplastic anemia, hemolytic anemia, granulocytopenia, thrombocytopenia Tmp: megaloblastic ane ia, leukopenia, granulocytopenia
179
[cotrimoxazole] Occasional AE non hema
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
[cotrimoxazole] Rare AE
Stevens-jh sons syndrome smx Hepatitis, cholestasis Cns disturbances Methemoglobinemia Pancreatitis Lupus like syndrome
181
[fluoroquinolones] First gen
Norfloxacin
182
[fluoroquinolones] Second
Ciprofloxacin, of.oxacin, pefloxacin
183
[fluoroquinolones] Trd
Levofloxacin, gatifloxacin, gemif | Oxacin, moxifloxacin
184
[fluoroquinolones] MOA
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
[fluoroquinolones] Mor
Modificatin of target enzyme dna gyrase Impaired entry into the cell
186
[fluoroquinolones] PK
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
[fluoroquinolones] PD
Comcentration dpendent
188
[fluoroquinolones] Uses
Pseudomonas aeruginosa, salmonella, shigella, e. Coli, neisseria me ingitidis
189
[fluoroquinolones] Occasional AE
Gi disturbances, cns disturbances, rash, oral candidiasis, transaminitis, hepa, hematologic, hypergly in diabetics, hypogly
190
[fluoroquinolones] Rare AE
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
Miscellaneous antibiotics
Metronidazole Nitrofurantoin Fosfomycin
192
[metronidazole] | moa
Nitro group reduced intracellular,y by reacting eith reduced ferredoxim Produce toxic metabolites which are taken up into bacterial dna
193
[metronidazole] PK
Oral iv rectal 100% F Widely distributed Penetrate abscesses including those in the brain Urine and feces
194
[metronidazole] PD
Concentratin dependent
195
[metronidazole] Uses
Clostridium difficile colitis Anaerobic infxns below the level of the diaphragm Brain anscesses
196
[metronidazole] Common AE
Gi disturbances Dry mouth, furrytongue
197
[metronidazole] Occasinal AE
Insomnia Urethral burnimg Darkening of urine Phlebitis Disulfiram like effect
198
[metronidazole] Rare AE
Cns disturbances - seizure. Ata ia, dysarthria Peripheral and optic neuropathy Pancreatitis
199
[nitrofurantoin] Moa
Rapid intracellular conversion to highly reactive intermediates by bacterial reductased
200
[nitrofurantoin] PK
Well absorbed oral Very rapid excretion in urine, no systemic antibacterial effect
201
[nitrofurantoin] Use
Urinary antiseptic - uncomplicated acute cystisis)
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[nitrofurantoin] Common AE
Gi disturbances - nausea, vomiting, diarrhea
203
[nitrofurantoin] Occasional AE
Neuropathy Hemolytic anemia Rash Pulmonary infiltratin, fibrosis
204
[fosfomycin] Moa
Inhibit the very early stage of cell wall synthesis - inhibit enolpyruvate transferase, block addition of phosphoenolpyruvatr to UDP-N-acetylglucosamine
205
[fosfomycin] Pk
40% F after oral administration Poorly distributed in tissues Excreted in urine
206
[fosfomycin] Use
Uncomplicated acute cystisis Not for first line agent for treatment for mdr infection

Pharmacology (2 decks)

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