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Pharm SJSM > Block 3 material simplified (Antibiotics) > Flashcards

Block 3 material simplified (Antibiotics) Flashcards

1
Q

Penicillin G & Penicillin V

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Penicillin G (natural) & Penicillin V (acid-resistant)

MOA:
D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis

Clinical use:
1) Mostly gram +ve (S. pneumoniae, S. pyogenes, Actinomyces)

2) Some gram -ve (N. meningitidis)

3) Some spirochetes (T. palladium)

Adverse effects:
Hypersensitivity
Direct +ve Coombs hemolytic anemia
Drug induced Interstitial Nephritis

Resistance:
Penicillinase or altered PBP

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2
Q

MOA:
D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis

Clinical use:
1) Mostly gram +ve (S. pneumoniae, S. pyogenes, Actinomyces)

2) Some gram -ve (N. meningitidis)

3) Some spirochetes (T. palladium)

Adverse effects:
Hypersensitivity
Direct +ve Coombs hemolytic anemia
Drug induced Interstitial Nephritis

Resistance:
Penicillinase or altered PBP

A

Penicillin G & Penicillin V

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3
Q

Penicillinase-Sensitive-Penicillin’s

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

Amoxicillin & Ampicillin (Aminopenicillins)
Penicillin G & V

MOA:
D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis

Give with penicillinase inhibitors (Clavulanate acid, Sulbactam, & Tazobactam)

Clinical use:
Wider spectrum coverage of
- H. pylori (amoxicillin)
- H. influenza
- Enterococci
- E. coli
- Listeria
- Proteus
- Salmonella
- Shigella

Adverse effects:
1) Hypersensitivity
2) Interstitial Nephritis
3) Pseudomembranous colitis
4) Direct coombs +ve hemolytic anemia

Resistance:
Penicillinase

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4
Q

Amoxicillin & Ampicillin (Aminopenicillins)
Penicillin G & V

MOA:
D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis

Give with penicillinase inhibitors (Clavulanate acid, Sulbactam, & Tazobactam)

Clinical use:
Wider spectrum coverage of
- H. pylori (amoxicillin)
- H. influenza
- Enterococci
- E. coli
- Listeria
- Proteus
- Salmonella
- Shigella

Adverse effects:
1) Hypersensitivity
2) Interstitial Nephritis
3) Pseudomembranous colitis
4) Direct coombs +ve hemolytic anemia

Resistance:
Penicillinase

A

Penicillinase-Sensitive-Penicillin’s

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5
Q

Penicillinase-Resistance-Penicillin’s

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

Dicloxacillin, Nafcillin, Oxacillin, & Methicillin

MOA:
D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis. They have bulky R groups to protect their Beta lactam rings

Clinical use:
Narrow spectrum for S. aureus (not MRSA)

Adverse effects:
1) Hypersensitivity
2) Interstitial Nephritis
3) Direct coombs +ve hemolytic anemia
4) Pseudomembranous colitis

Resistance:
Altered PBPs

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6
Q

Dicloxacillin, Nafcillin, Oxacillin, & Methicillin

MOA:
D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis. They have bulky R groups to protect their Beta lactam rings

Clinical use:
Narrow spectrum for S. aureus (not MRSA)

Adverse effects:
1) Hypersensitivity
2) Interstitial Nephritis
3) Direct coombs +ve hemolytic anemia
4) Pseudomembranous colitis

Resistance:
Altered PBPs

A

Penicillinase-Resistance-Penicillin’s

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7
Q

Antipseudomonal penicillin’s

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

Piperacillin, Ticarcillin, & Carbenicillin

MOA:
D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis

Give with penicillinase inhibitors (Clavulanate acid, Sulbactam, & Tazobactam)

Clinical use:
Extended spectrum for pseudomonas & gram -ve rods

Adverse effects:
1) Hypersensitivity
2) Interstitial Nephritis
3) Direct coombs +ve hemolytic anemia
4) Pseudomembranous colitis

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8
Q

1st Generation Cephalosporins

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Cefazolin & Cephalexin

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
Proteus mirabilis
E. coli
Klebsiella pneumonia
Post operation S. aureus infection

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

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9
Q

Cefazolin & Cephalexin

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
Proteus mirabilis
E. coli
Klebsiella pneumonia
Post operation S. aureus infection

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

A

1st Generation Cephalosporins

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10
Q

2nd Generation Cephalosporins

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Cefaclor, Cefoxitin, Cefuroxime, & Cefotetan

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
For gram +ve cocci
- H. influenza
- Enterobacter aerogenes
- Neisseria
- Serratia
- Proteus
- E. coli
- Klebsiella

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

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11
Q

Cefaclor, Cefoxitin, Cefuroxime, & Cefotetan

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
For gram +ve cocci
- H. influenza
- Enterobacter aerogenes
- Neisseria
- Serratia
- Proteus
- E. coli
- Klebsiella

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

A

2nd Generation Cephalosporins

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12
Q

3rd Generation Cephalosporins

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Ceftriaxone, Cefotaxime, Cefpodoxime, Ceftazidime, & Cefixime

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
1) Serious gram -ve infections that are resistant to other beta-lactams

2) Ceftriaxone (Meningitis, Gonorrhea, & disseminated Lyme disease)

3) Ceftazidime (pseudomonas)

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

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13
Q

Ceftriaxone, Cefotaxime, Cefpodoxime, Ceftazidime, & Cefixime

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
1) Serious gram -ve infections that are resistant to other beta-lactams

2) Ceftriaxone (Meningitis, Gonorrhea, & disseminated Lyme disease)

3) Ceftazidime (pseudomonas)

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

A

3rd Generation Cephalosporins

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14
Q

4th Generation Cephalosporins

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Cefepime

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
gram +ve & gram -ve species, especially PSUEDOMONAS!!!

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

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15
Q

Cefepime

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
gram +ve & gram -ve species, especially PSUEDOMONAS!!!

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

A

4th Generation Cephalosporins

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16
Q

5th Generation Cephalosporins

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Ceftaroline

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
Broad coverage of gram +ve & gram -ve MRSA & Enterococcus faecalis
(not pseudomonas)

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

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17
Q

Ceftaroline

MOA:
Beta-lactams that are penicillinase resistant & inhibit cell wall synthesis

Clinical use:
Broad coverage of gram +ve & gram -ve MRSA & Enterococcus faecalis
(not pseudomonas)

Adverse effects:
Hypersensitivity
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vitamin K deficiency
Nephrotoxicity with aminoglycosides

Resistance:
Inactivated by cephalosporinase or PBP mutations

A

5th Generation Cephalosporins

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18
Q

Carbapenems

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Doripenem, Imipenem, Meropenem, & Ertapenem

MOA:
A beta lactamase resistant D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis. It is always co-administered with Cilastin to reduce inactivation in the renal tubules by (dehydropeptidase I)

Clinical use:
gram +ve cocci
gram -ve rods
Anaerobes
Life-threatening pseudomonas infection

Adverse effects:
1) CNS toxicity (seizures) worst in imipenem better in meropenem

2) Rash
3) Gi distress

Resistance:
Carbapenemase via K. pneumonia, E. coli, & E. aerogenes

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19
Q

Doripenem, Imipenem, Meropenem, & Ertapenem

MOA:
A beta lactamase resistant D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis. It is always co-administered with Cilastin to reduce inactivation in the renal tubules by (dehydropeptidase I)

Clinical use:
gram +ve cocci
gram -ve rods
Anaerobes
Life-threatening pseudomonas infection

Adverse effects:
1) CNS toxicity (seizures) worst in imipenem better in meropenem

2) Rash
3) Gi distress

Resistance:
Carbapenemase via K. pneumonia, E. coli, & E. aerogenes

A

Carbapenems

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20
Q

Monobactam

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Aztreonam

MOA:
A beta lactamase resistant D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis.

Resistant to penicillinase & it has no cross-reactivity with other penicillin’s (good for penicillin allergies)

Clinical use:
Only gram -ve rods, Pseudomonas & E.coli

Adverse effects:
Occasional Gi upset

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21
Q

Aztreonam

MOA:
A beta lactamase resistant D-Ala D-Ala analog that binds PBP (transpeptidase) to block peptidoglycan cross-linking to inhibit cell wall synthesis.

Resistant to penicillinase & it has no cross-reactivity with other penicillin’s (good for penicillin allergies)

Clinical use:
Only gram -ve rods, Pseudomonas & E.coli

Adverse effects:
Occasional Gi upset

A

Monobactam

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22
Q

Match the Beta-lactamase inhibitor with the penicillin:

Amoxicillin
Ampicillin
Piperacillin

A

Amoxicillin-Clavulanate acid
Ampicillin-Sulbactam
Piperacillin-Tazobactam

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23
Q

Vancomycin

MOA:

Clinical use:

Adverse effects:

Resistance:

A

MOA:
Binds D-Ala D-Ala to prevent cell wall peptidoglycan formation & resistant to penicillinase

Clinical use:
Only gram +ve MRSA, S. epidermidis, & C. difficile

Adverse effects:
1) Nephrotoxicity
2) Ototoxicity
3) Thrombophlebitis
4) Red man syndrome
5) DRESS

Resistance:
AA mutation to D-Lac

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24
Q

MOA:
Binds D-Ala D-Ala to prevent cell wall peptidoglycan formation & resistant to penicillinase

Clinical use:
Only gram +ve MRSA, S. epidermidis, & C. difficile

Adverse effects:
1) Nephrotoxicity
2) Ototoxicity
3) Thrombophlebitis
4) Red man syndrome
5) DRESS

Resistance:
AA mutation to D-Lac

A

Vancomycin

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25
Q

Aminoglycosides

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Gentamicin, Amikacin, Neomycin, Streptomycin, & Tobramycin

MOA:
30S inhibitor to prevent bacterial protein synthesis (synergistic with beta lactams)

Clinical uses:
1) Aerobic organisms (needs O2 for uptake)
2) gram -ve rods
3) Bowel surgery prophylaxis (Neomycin)
4) Mycobacterium TB (Streptomycin RIPES)

Adverse effects:
1) Nephrotoxicity (Acute tubular necrosis)
2) Ototoxicity (loop diuretics)
3) Neuromuscular block (avoid in myasthenia gravis)
4) Teratogenicity

Resistance:
Enzyme modification of the drug via acetylation, phosphorylation, & adenylation,

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26
Q

Gentamicin, Amikacin, Neomycin, Streptomycin, & Tobramycin

MOA:
30S inhibitor to prevent bacterial protein synthesis (synergistic with beta lactams)

Clinical uses:
1) Aerobic organisms (needs O2 for uptake)
2) gram -ve rods
3) Bowel surgery prophylaxis (Neomycin)
4) Mycobacterium TB (Streptomycin RIPES)

Adverse effects:
1) Nephrotoxicity (Acute tubular necrosis)
2) Ototoxicity (loop diuretics)
3) Neuromuscular block (avoid in myasthenia gravis)
4) Teratogenicity

Resistance:
Enzyme modification of the drug via acetylation, phosphorylation, & adenylation,

A

Aminoglycosides

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27
Q

Tetracyclines

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Tetracycline, Doxycycline, & Minocycline

MOA:
30S inhibitor

Avoid with milk, antacids, or iron chelators

Clinical use:
Acne
B. burgdorferi
Chlamydia
Community acquired MRSA
M. pneumoniae
Rickettsia (rmsf)

Adverse effects:
1) Gi distress
2) Teeth discoloration
3) Inhibited bone growth (avoid in kids)
4) Photosensitivity

Resistance:
Efflux pumps

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28
Q

Tetracycline, Doxycycline, & Minocycline

MOA:
30S inhibitor

Avoid with milk, antacids, or iron chelators

Clinical use:
Acne
B. burgdorferi
Chlamydia
Community acquired MRSA
M. pneumoniae
Rickettsia (rmsf)

Adverse effects:
1) Gi distress
2) Teeth discoloration
3) Inhibited bone growth (avoid in kids)
4) Photosensitivity

Resistance:
Efflux pumps

A

Tetracycline

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29
Q

Tigecycline

MOA:

Clinical use:

Adverse effects:

Resistance:

A

MOA:
30S inhibitor

Clinical use:
Broad spectrum for gram +ve & gram -ve
MRSA & VRE

Adverse effects:
Gi upset (N/V)
Bleeding (dose dependent)

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30
Q

MOA:
30S inhibitor

Clinical use:
Broad spectrum for gram +ve & gram -ve
MRSA & VRE

Adverse effects:
Gi upset (N/V)
Bleeding (dose dependent)

A

Tigecycline

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31
Q

Chloramphenicol

MOA:

Clinical use:

Adverse effects:

Resistance:

A

MOA:
50S inhibitor via (peptidyl transferase)

Clinical use:
1) Meningitis (H.influenzae, N.meningitidis, strep. pneumoniae)

2) Rickettsia (rmsf)

Adverse effects:
Anemia
Aplastic anemia
Gray baby syndrome

Resistance:
Plasmid encoded acetyltransferase which inactivates it

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32
Q

MOA:
50S inhibitor via (peptidyl transferase)

Clinical use:
1) Meningitis (H.influenzae, N.meningitidis, strep. pneumoniae)

2) Rickettsia (rmsf)

Adverse effects:
Anemia
Aplastic anemia
Gray baby syndrome

Resistance:
Plasmid encoded acetyltransferase which inactivates it

A

Chloramphenicol

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33
Q

Clindamycin

MOA:

Clinical use:

Adverse effects:

Resistance:

A

MOA:
50S inhibitor

Clinical use:
For anaerobic infections ABOVE the diaphragm
- Bacteroides
- Clostridium per fringes
- Aspiration pneumonia
- Lung abscess
- Bacterial vaginosis
- Oral infections
- Strep pyogenes

Adverse effects
1) Pseudomembranous colitis (C. diff)
2) Fever
3) Diarrhea

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34
Q

MOA:
50S inhibitor

Clinical use:
For anaerobic infections ABOVE the diaphragm
- Bacteroides
- Clostridium per fringes
- Aspiration pneumonia
- Lung abscess
- Bacterial vaginosis
- Oral infections
- Strep pyogenes

Adverse effects
1) Pseudomembranous colitis (C. diff)
2) Fever
3) Diarrhea

A

Clindamycin

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35
Q

Linezolid

MOA:

Clinical use:

Adverse effects:

Resistance:

A

MOA:
50S inhibitor (blocks the initiation complex formation)

Clinical use:
gram +ve (MRSA & VRE)

Adverse effects:
1) Bone marrow suppression (thrombocytopenia, anemia, & leukopenia)

2) Peripheral neuropathy (optic neuritis & peripheral neuropathy)

3) Serotonin syndrome (partial monoamine oxidase inhibition)

Resistance:
Point mutation of ribosomal RNA

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36
Q

MOA:
50S inhibitor (blocks the initiation complex formation)

Clinical use:
gram +ve (MRSA & VRE)

Adverse effects:
1) Bone marrow suppression (thrombocytopenia, anemia, & leukopenia)

2) Peripheral neuropathy (optic neuritis & peripheral neuropathy)

3) Serotonin syndrome (partial monoamine oxidase inhibition)

Resistance:
Point mutation of ribosomal RNA

A

Linezolid

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37
Q

Macrolides

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Azithromycin, Clarithromycin, & Erythromycin

MOA:
50S inhibitor via binding 23S rRNA to prevent bacterial protein synthesis

Clinical use:
1) Atypical pneumonia (Mycoplasma, Chlamydia, & Legionella)
2) STI’s (Chlamydia & N. gonorrhea)
3) B. pertussis
4) gram +ve cocci in penicillin allergic patients

Adverse effects: MACRO
1) gi Motility issues

2) Arrythmias (Prolonged QT interval & Torsade’s de points risk)

3) acute Cholestatic hepatitis
4) Rash
5) eOsinophilia

Resistance:
Methylation of 23s rRNA binding sites

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38
Q

Azithromycin, Clarithromycin, & Erythromycin

MOA:
50S inhibitor via binding 23S rRNA to prevent bacterial protein synthesis

Clinical use:
1) Atypical pneumonia (Mycoplasma, Chlamydia, & Legionella)
2) STI’s (Chlamydia & N. gonorrhea)
3) B. pertussis
4) gram +ve cocci in penicillin allergic patients

Adverse effects: MACRO
1) gi Motility issues

2) Arrythmias (Prolonged QT interval & Torsade’s de points risk)

3) acute Cholestatic hepatitis
4) Rash
5) eOsinophilia

Resistance:
Methylation of 23s rRNA binding sites

A

Macrolides

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39
Q

Polymyxins

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Colistin (polymyxin E) & Polymyxin B

MOA:
Create cation polypeptides that bind cell membranes & cause holes (intracellular leakage)

Clinical use:
Multidrug resistant P. aeruginosa, E.coli, & K. pneumonia

Adverse effects:
1) Nephrotoxicity
2) Neurotoxicity
3) Respiratory failure

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40
Q

Colistin (polymyxin E) & Polymyxin B

MOA:
Create cation polypeptides that bind cell membranes & cause holes (intracellular leakage)

Clinical use:
Multidrug resistant P. aeruginosa, E.coli, & K. pneumonia

Adverse effects:
1) Nephrotoxicity
2) Neurotoxicity
3) Respiratory failure

A

Polymyxins

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41
Q

Sulfonamides

MOA:

Clinical use:

Adverse effects:

Resistance:

A

Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine

MOA:
PABA analogs that bind & block dihydropteroate synthase to inhibit folate synthesis

Clinical use:
Broad coverage with trimethoprim (TMP-SMX)
- gram +ve (nocardia)
- gram -ve
- UTI

Adverse effects:
1) Hypersensitivity (sulfa allergy)
2) Nephrotoxicity (tubulointerstitial nephritis)
3) Hemolysis in G6PD deficiency
4) Photosensitive rash (SJS)
5) Infant Kernicterus
6) Inhibited CYP450 (warfarin toxicity)

Resistance:
Increased PABA levels
Reduced drug uptake
Mutated dihydropteroate synthase

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42
Q

Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine

MOA:
PABA analogs that bind & block dihydropteroate synthase to inhibit folate synthesis

Clinical use:
Broad coverage with trimethoprim (TMP-SMX)
- gram +ve (nocardia)
- gram -ve
- UTI

Adverse effects:
1) Hypersensitivity (sulfa allergy)
2) Nephrotoxicity (tubulointerstitial nephritis)
3) Hemolysis in G6PD deficiency
4) Photosensitive rash (SJS)
5) Infant Kernicterus
6) Inhibited CYP450 (warfarin toxicity)

Resistance:
Increased PABA levels
Reduced drug uptake
Mutated dihydropteroate synthase

A

Sulfonamides

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43
Q

Dapsone

MOA:

Clinical use:

Adverse effects:

Resistance:

A

MOA:
Inhibits dihydropteroate synthase to inhibit folate synthesis

Clinical use:
Leprosy (lepromatous & TB forms)
PJP

Adverse effects:
1) Hemolysis in G6PD deficiency
2) Methemoglobinemia
3) Agranulocytosis

44
Q

MOA:
Inhibits dihydropteroate synthase to inhibit folate synthesis

Clinical use:
Leprosy (lepromatous & TB forms)
PJP

Adverse effects:
1) Hemolysis in G6PD deficiency
2) Methemoglobinemia
3) Agranulocytosis

A

Dapsone

45
Q

Trimethoprim (TMP)

MOA:

Clinical treatment:

Adverse effects:

A

MOA:
Inhibits folate synthesis by blocking dihydrofolate reductase (DHFR)

Clinical:
Board spectrum when given with sulfonamides
- Shigella
- Salmonella
- Pneumocystis Jirovecii pneumoniae
- Toxoplasmosis prophylaxis
- Community acquired MRSA

Adverse effects:
1) Hyperkalemia
2) Megaloblastic anemia
3) Leukopenia
4) Granulocytopenia (give leucovorin to avoid)
5) Teratogenic (NTD)
6) Inhibits CYP450 (warfarin toxicity)

46
Q

MOA:
Inhibits folate synthesis by blocking dihydrofolate reductase (DHFR)

Clinical:
Board spectrum when given with sulfonamides
- Shigella
- Salmonella
- Pneumocystis Jirovecii pneumoniae
- Toxoplasmosis prophylaxis
- Community acquired MRSA

Adverse effects:
1) Hyperkalemia
2) Megaloblastic anemia
3) Leukopenia
4) Granulocytopenia (give leucovorin to avoid)
5) Teratogenic (NTD)
6) Inhibits CYP450 (warfarin toxicity)

A

Trimethoprim (TMP)

47
Q

Fluoroquinolones

MOA:

Clinical treatment:

Adverse effects:

Resistance:

A

Ciprofloxacin, Enoxacin, & Ofloxacin

Gemifloxacin, Levofloxacin, Monifloxacin:
Respiratory fluoroquinolones

MOA:
Inhibits topoisomerase II (DNA gyrase) & Topoisomerase IV

AVOID antacids

Clinical use:
gram -ve rods (UTI’s, GIT, & Pseudomonas)
gram -ve (Otitis externa)

Adverse effects:
1) Gi upset
2) Prolonged QT
3) Tendonitis/Ruptured (Achilles)
4) Superinfection
5) Cartilage damage (avoid in kids)

Resistance:
Mutated DNA gyrase & Efflux pumps

48
Q

Ciprofloxacin, Enoxacin, & Ofloxacin

Gemifloxacin, Levofloxacin, Monifloxacin:
Respiratory fluoroquinolones

MOA:
Inhibits topoisomerase II (DNA gyrase) & Topoisomerase IV

AVOID antacids

Clinical use:
gram -ve rods (UTI’s, GIT, & Pseudomonas)
gram -ve (Otitis externa)

Adverse effects:
1) Gi upset
2) Prolonged QT
3) Tendonitis/Ruptured (Achilles)
4) Superinfection
5) Cartilage damage (avoid in kids)

Resistance:
Mutated DNA gyrase & Efflux pumps

A

Fluoroquinolones

49
Q

Daptomycin

MOA:

Clinical treatment:

Adverse effects:

Resistance:

A

MOA:
Disrupts the cell membrane via Na+ transmembrane channels that cause intracellular leakage & membrane depolarization (cell death)

Clinical use:
gram +ve cocci
- S. aureus & MRSA (skin infections)
- VRE

(NOT for pseudomonas)

Adverse effects:
1) Myopathy
2) Rhabdomyolysis (Elevated CK)
3) Retinopathy

50
Q

MOA:
Disrupts the cell membrane via Na+ transmembrane channels that cause intracellular leakage & membrane depolarization (cell death)

Clinical use:
gram +ve cocci
- S. aureus & MRSA (skin infections)
- VRE

(NOT for pseudomonas)

Adverse effects:
1) Myopathy
2) Rhabdomyolysis (Elevated CK)
3) Retinopathy

A

Daptomycin

51
Q

Metronidazole

MOA:

Clinical treatment:

Adverse effects:

Resistance:

A

MOA:
Forms free radicals to damage DNA

Clinical use:
Giardia
Entamoeba
Trichomonas
Gardnerella vaginallis
Anaerobes (Bacteroides & c.diff)
h. Pylori

“GET GAP”

Adverse effects:
1) Disulfiram-like reaction with alcohol
2) Metallic taste
3) Neuropathy (paresthesia’s)
4) Headache/Gi upset

52
Q

MOA:
Forms free radicals to damage DNA

Clinical use:
Giardia
Entamoeba
Trichomonas
Gardnerella vaginallis
Anaerobes (Bacteroides & c.diff)
h. Pylori

“GET GAP”

Adverse effects:
1) Disulfiram-like reaction with alcohol
2) Metallic taste
3) Neuropathy (paresthesia’s)
4) Headache/Gi upset

A

Metronidazole

53
Q

Which drugs are used for M. Leprae?

A

Dapsone or Rifampin (TB form)

Clofazimine (lepromatous form)

54
Q

Which drugs are used for MAC?

A

Azithromycin or Clarithromycin + Ethambutol

55
Q

Which drugs are used for M. TB?

A

Rifampin
Isoniazid
Pyrazinamide
Ethambutol
Streptogrammins

56
Q

Which drugs inhibit 50S subunits?

A

Chloramphenicol
Clindamycin
Macrolides
Linezolid
Streptogramins

57
Q

Which drugs inhibit 30S subunits?

A

Aminoglycosides
TCAs
Tigecycline

58
Q

Which drugs inhibit mRNA via RNA polymerase?

A

Rifampin

59
Q

Which drugs form free radicals to damage DNA?

A

Metronidazole

60
Q

Which drugs inhibit DNA Gyrase (topoisomerase II)?

A

Fluoroquinolones & Quinolones

61
Q

Which drugs disrupt membrane integrity?

A

Daptomycin (gram +ve)
Polymyxins (gram -ve)

62
Q

Which drugs inhibit Folic acid synthesis & reduction?

A

Sulfonamides
Trimethoprim

63
Q

Which drugs inhibit Peptidoglycan synthesis?

A

Vancomycin & Bacitracin

64
Q

Which drugs inhibit Peptidoglycan cross-linking?

A

PSP
PRP
Antipseudomonal penicillin’s
Cephalosporins
Carbapenems
Monobactams

65
Q

Which drugs inhibit mRNA synthesis?

A

Rifampin & Rifabutin

66
Q

Which drugs works best in pH environments (phagosomes)?

A

Pyrazinamide

67
Q

Which drug inhibits arabinogalactan synthesis?

A

Ethambutol

68
Q

Which drugs inhibit mycolic acid synthesis?

A

Isoniazid

69
Q

Rifamycin’s

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

Rifampin, Rifabutin, & Rifapentine

MOA:
Inhibits DNA-dependent-RNA polymerase

Clinical uses:
M. TB (RIPES)

Adverse effects:
1) Red/Orange body fluids
2) Ramped up CYP450 (Rifampin)
3) Hepatotoxicity
4) Nephrotoxicity (Acute Interstitial Nephritis)

Resistance:
Rapid resistance in monotherapy (mutated RNA polymerase)

4 R’s
RNA polymerase inhibitor
Red/Orange body fluids
Rapid resistance in monotherapy

70
Q

Rifampin, Rifabutin, & Rifapentine

MOA:
Inhibits DNA-dependent-RNA polymerase

Clinical uses:
M. TB (RIPES)

Adverse effects:
1) Red/Orange body fluids
2) Ramped up CYP450 (Rifampin)
3) Hepatotoxicity
4) Nephrotoxicity (Acute Interstitial Nephritis)

Resistance:
Rapid resistance in monotherapy (mutated RNA polymerase)

4 R’s
RNA polymerase inhibitor
Red/Orange body fluids
Rapid resistance in monotherapy

A

Rifamycin’s

71
Q

Isoniazid

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

MOA:
Activated by bacterial catalase peroxidase (Kat G) to inhibit mycolic acid synthesis

Clinical use:
M. TB monotherapy (RIPES)

Adverse effects:
1) Hepatotoxicity
2) Drug-induced SLE
3) Vit B6 deficiency (Peripheral neuropathy & sideroblastic anemia & seizures)
5) Metabolic anion gap acidosis

Resistance:
Mutations to reduce the expression of KatG

72
Q

MOA:
Activated by bacterial catalase peroxidase (Kat G) to inhibit mycolic acid synthesis

Clinical use:
M. TB monotherapy (RIPES)

Adverse effects:
1) Hepatotoxicity
2) Drug-induced SLE
3) Vit B6 deficiency (Peripheral neuropathy & sideroblastic anemia & seizures)
5) Metabolic anion gap acidosis

Resistance:
Mutations to reduce the expression of KatG

A

Isoniazid

73
Q

Pyrazinamide

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

MOA:
works in acidic pH (bacterial phagosomes)

Clinical uses:
M. TB (RIPES)

Adverse effects:
1) Hyperuricemia/Gout
2) Hepatotoxicity
3) Arthralgias

74
Q

MOA:
works in acidic pH (bacterial phagosomes)

Clinical uses:
M. TB (RIPES)

Adverse effects:
1) Hyperuricemia/Gout
2) Hepatotoxicity
3) Arthralgias

A

Pyrazinamide

75
Q

Ethambutol

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

MOA:
Inhibits arabinosyltransferase to reduce carbohydrate polymerization in the cell wall

Clinical use:
M. TB (RIPES)
MAC

Adverse effects:
1) Optic neuropathy (red-green color blindness)

76
Q

MOA:
Inhibits arabinosyltransferase to reduce carbohydrate polymerization in the cell wall

Clinical use:
M. TB (RIPES)
MAC

Adverse effects:
1) Optic neuropathy (red-green color blindness)

A

Ethambutol

77
Q

Streptomycin

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

30S inhibitor

Clinical uses:
M. TB (RIPES)

Adverse effects:
1) Tinnitus
2) Ataxia
3) Nephrotoxicity

78
Q

30S inhibitor

Clinical uses:
M. TB (RIPES)

Adverse effects:
1) Tinnitus
2) Ataxia
3) Nephrotoxicity

A

Streptomycin

79
Q

Prophylaxis drugs for exposure to Meningitis?

A

Ceftriaxone
Ciprofloxacin
Rifampin

80
Q

Prophylaxis drugs for exposure to Endocarditis & dental surgery?

A

Amoxicillin

81
Q

Prophylaxis drugs for recurrent UTI’s?

A

TMP-SMX

82
Q

Prophylaxis drugs for exposure to Strep B when pregnant?

A

Intrapartum, Penicillin G or Ampicillin

83
Q

Prophylaxis drugs for Gonorrhea conjunctivitis in newborns?

A

Erythromycin

84
Q

Prophylaxis drugs for post op S. aureus?

A

Cefazolin or Vancomycin (MRSA)

85
Q

Prophylaxis drugs for Strep pharyngitis in children with post rheumatic fever?

A

Benzathine (penicillin G) or oral penicillin V

86
Q

What are the drugs used to treat MRSA?

A

Vancomycin, Daptomycin, Linezolid, Tigecycline, Ceftaroline (5th) , Doxycycline

87
Q

What are the drugs used to treat VRE?

A

Daptomycin, Linezolid, Tigecycline, Streptogramins

88
Q

What are the drugs used to treat multi-drug resistant P. aeruginosa?

A

Acinetobacter baumannii (Polymyxin B & Colistin (polymyxin E))

89
Q

What are the drugs used to treat HIV infection/aids?

A

CD4<200 = TMP-SMX
(Pneumocystis pneumoniae)

CD4<100 = TMP-SMX
(Pneumocystis pneumoniae & Toxoplasmosis)

90
Q

Chlamydia (Mucopurulent discharge, pleomorphic gram-negative, intracellular) is treated with which drugs?

A

Azithromycin or Doxycycline.

91
Q

Gonorrhea (Yellow-green discharge, gram-negative intracellular diplococci) is treated with which drugs?

A

Ceftriaxone plus Azithromycin or Doxycycline.

92
Q

Syphilis (Painless chancre, gram-negative spiral-shaped bacteria) treated with which drugs?

A

Penicillin G

93
Q

Trichomoniasis (Foul-smelling, yellow -green purulent discharge, trophozoites w/multiple flagella) Which drugs treat this?

A

Metronidazole or Tinidazole.

94
Q

Herpes (Pain, pruiritis, rash)

A

Antivirals like Acyclovir, Valacyclovir

95
Q

Candida Vaginosis (Milky, curdy white discharge, yeast infection) treat with which drugs?

A

Fluconazole, clotrimazole

96
Q

Bacterial Vaginosis (Gardnerella) ( Grayish milky discharge, whiff test: fishy odour, clue cells, pleomorphic gram negative
rods.) treated with which drugs?

A

Metronidazole

97
Q

Streptogramins

A

(e.g., Quinupristin/Dalfopristin):

■ MOA: 50S inhibitors
Quinupristin inhibits the early phase of protein synthesis,
Dalfopristin inhibits the late phase to produce a synergistic bactericidal effect

■ Note: Used mainly for resistant Gram-positive infections.

98
Q

Antimalarial: Chloroquine

MOA

Resistance

Adverse effects

A

● MOA:
Chloroquine inhibits heme polymerization

● Resistance: Chloroquine resistance due to efflux pump.

● Side Effects: retinopathy (Chloroquine).

● Clinical Use:
○ Chloroquine for primarily P. vivax and P. ovale, and some strains of P. falciparum.

99
Q

Antimalarial: Primaquine

MOA:

Clinical uses

Adverse effects

A

MOA:
Primaquine interferes with the electron transport in the mitochondria of the malaria parasite

Clinical uses:
○ Primaquine is used for radical cure (elimination of liver stages) of P. vivax and P. ovale infections, preventing relapses.

Adverse effects:
G6PD deficiency hemolysis (Primaquine),

100
Q

Antimalarial: Mefloquine

MOA

Clinical uses:

A

MOA:
Mefloquine disrupts heme detoxification within the parasite’s food vacuole

Clinical uses:

○ Mefloquine is the treatment of chloroquine-resistant P. falciparum and P. vivax. Used in
pregnant females.

101
Q

Antimalarial: Artensuate

MOA

Clinical uses

A

MOA:
Artesunate is rapidly hydrolyzed to dihydroartemisinin, which generates free radicals that damage proteins and membranes in the malaria parasite.

Clinical uses:

○ Artesunate is used for the treatment of severe and complicated P. falciparum malaria

102
Q

MOA:
is rapidly hydrolyzed to dihydroartemisinin, which generates free radicals that damage proteins and membranes in the malaria parasite.

Clinical uses:

○ is used for the treatment of severe and complicated P. falciparum malaria

A

Antimalarial: Artensuate

103
Q

MOA:
disrupts heme detoxification within the parasite’s food vacuole

Clinical uses:

○ is the treatment of chloroquine-resistant P. falciparum and P. vivax. Used in
pregnant females.

A

Mefloquine

104
Q

MOA:
interferes with the electron transport in the mitochondria of the malaria parasite

Clinical uses:
○ is used for radical cure (elimination of liver stages) of P. vivax and P. ovale infections, preventing relapses.

Adverse effects:
G6PD deficiency hemolysis

A

Primaquine

105
Q

● MOA:
inhibits heme polymerization

● Resistance: resistance due to efflux pump.

● Side Effects: retinopathy

● Clinical Use:
○ for primarily P. vivax and P. ovale, and some strains of P. falciparum.

A

Chloroquine

Pharm SJSM (23 decks)

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