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
Aminoglycosides MOA: Clinical use: Adverse effects: Resistance:
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,
26
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,
Aminoglycosides
27
Tetracyclines MOA: Clinical use: Adverse effects: Resistance:
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
28
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
Tetracycline
29
Tigecycline MOA: Clinical use: Adverse effects: Resistance:
MOA: 30S inhibitor Clinical use: Broad spectrum for gram +ve & gram -ve MRSA & VRE Adverse effects: Gi upset (N/V) Bleeding (dose dependent)
30
MOA: 30S inhibitor Clinical use: Broad spectrum for gram +ve & gram -ve MRSA & VRE Adverse effects: Gi upset (N/V) Bleeding (dose dependent)
Tigecycline
31
Chloramphenicol MOA: Clinical use: Adverse effects: Resistance:
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
32
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
Chloramphenicol
33
Clindamycin MOA: Clinical use: Adverse effects: Resistance:
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
34
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
Clindamycin
35
Linezolid MOA: Clinical use: Adverse effects: Resistance:
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
36
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
Linezolid
37
Macrolides MOA: Clinical use: Adverse effects: Resistance:
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
38
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
Macrolides
39
Polymyxins MOA: Clinical use: Adverse effects: Resistance:
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
40
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
Polymyxins
41
Sulfonamides MOA: Clinical use: Adverse effects: Resistance:
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
42
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
Sulfonamides
43
Dapsone MOA: Clinical use: Adverse effects: Resistance:
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
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
Dapsone
45
Trimethoprim (TMP) MOA: Clinical treatment: Adverse effects:
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
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)
Trimethoprim (TMP)
47
Fluoroquinolones MOA: Clinical treatment: Adverse effects: Resistance:
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
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
Fluoroquinolones
49
Daptomycin MOA: Clinical treatment: Adverse effects: Resistance:
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
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
Daptomycin
51
Metronidazole MOA: Clinical treatment: Adverse effects: Resistance:
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
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
Metronidazole
53
Which drugs are used for M. Leprae?
Dapsone or Rifampin (TB form) Clofazimine (lepromatous form)
54
Which drugs are used for MAC?
Azithromycin or Clarithromycin + Ethambutol
55
Which drugs are used for M. TB?
Rifampin Isoniazid Pyrazinamide Ethambutol Streptogrammins
56
Which drugs inhibit 50S subunits?
Chloramphenicol Clindamycin Macrolides Linezolid Streptogramins
57
Which drugs inhibit 30S subunits?
Aminoglycosides TCAs Tigecycline
58
Which drugs inhibit mRNA via RNA polymerase?
Rifampin
59
Which drugs form free radicals to damage DNA?
Metronidazole
60
Which drugs inhibit DNA Gyrase (topoisomerase II)?
Fluoroquinolones & Quinolones
61
Which drugs disrupt membrane integrity?
Daptomycin (gram +ve) Polymyxins (gram -ve)
62
Which drugs inhibit Folic acid synthesis & reduction?
Sulfonamides Trimethoprim
63
Which drugs inhibit Peptidoglycan synthesis?
Vancomycin & Bacitracin
64
Which drugs inhibit Peptidoglycan cross-linking?
PSP PRP Antipseudomonal penicillin's Cephalosporins Carbapenems Monobactams
65
Which drugs inhibit mRNA synthesis?
Rifampin & Rifabutin
66
Which drugs works best in pH environments (phagosomes)?
Pyrazinamide
67
Which drug inhibits arabinogalactan synthesis?
Ethambutol
68
Which drugs inhibit mycolic acid synthesis?
Isoniazid
69
Rifamycin's MOA: Clinical uses: Adverse effects: Resistance:
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
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
Rifamycin's
71
Isoniazid MOA: Clinical uses: Adverse effects: Resistance:
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
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
Isoniazid
73
Pyrazinamide MOA: Clinical uses: Adverse effects: Resistance:
MOA: works in acidic pH (bacterial phagosomes) Clinical uses: M. TB (RIPES) Adverse effects: 1) Hyperuricemia/Gout 2) Hepatotoxicity 3) Arthralgias
74
MOA: works in acidic pH (bacterial phagosomes) Clinical uses: M. TB (RIPES) Adverse effects: 1) Hyperuricemia/Gout 2) Hepatotoxicity 3) Arthralgias
Pyrazinamide
75
Ethambutol MOA: Clinical uses: Adverse effects: Resistance:
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
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)
Ethambutol
77
Streptomycin MOA: Clinical uses: Adverse effects: Resistance:
30S inhibitor Clinical uses: M. TB (RIPES) Adverse effects: 1) Tinnitus 2) Ataxia 3) Nephrotoxicity
78
30S inhibitor Clinical uses: M. TB (RIPES) Adverse effects: 1) Tinnitus 2) Ataxia 3) Nephrotoxicity
Streptomycin
79
Prophylaxis drugs for exposure to Meningitis?
Ceftriaxone Ciprofloxacin Rifampin
80
Prophylaxis drugs for exposure to Endocarditis & dental surgery?
Amoxicillin
81
Prophylaxis drugs for recurrent UTI's?
TMP-SMX
82
Prophylaxis drugs for exposure to Strep B when pregnant?
Intrapartum, Penicillin G or Ampicillin
83
Prophylaxis drugs for Gonorrhea conjunctivitis in newborns?
Erythromycin
84
Prophylaxis drugs for post op S. aureus?
Cefazolin or Vancomycin (MRSA)
85
Prophylaxis drugs for Strep pharyngitis in children with post rheumatic fever?
Benzathine (penicillin G) or oral penicillin V
86
What are the drugs used to treat MRSA?
Vancomycin, Daptomycin, Linezolid, Tigecycline, Ceftaroline (5th) , Doxycycline
87
What are the drugs used to treat VRE?
Daptomycin, Linezolid, Tigecycline, Streptogramins
88
What are the drugs used to treat multi-drug resistant P. aeruginosa?
Acinetobacter baumannii (Polymyxin B & Colistin (polymyxin E))
89
What are the drugs used to treat HIV infection/aids?
CD4<200 = TMP-SMX (Pneumocystis pneumoniae) CD4<100 = TMP-SMX (Pneumocystis pneumoniae & Toxoplasmosis)
90
Chlamydia (Mucopurulent discharge, pleomorphic gram-negative, intracellular) is treated with which drugs?
Azithromycin or Doxycycline.
91
Gonorrhea (Yellow-green discharge, gram-negative intracellular diplococci) is treated with which drugs?
Ceftriaxone plus Azithromycin or Doxycycline.
92
Syphilis (Painless chancre, gram-negative spiral-shaped bacteria) treated with which drugs?
Penicillin G
93
Trichomoniasis (Foul-smelling, yellow -green purulent discharge, trophozoites w/multiple flagella) Which drugs treat this?
Metronidazole or Tinidazole.
94
Herpes (Pain, pruiritis, rash)
Antivirals like Acyclovir, Valacyclovir
95
Candida Vaginosis (Milky, curdy white discharge, yeast infection) treat with which drugs?
Fluconazole, clotrimazole
96
Bacterial Vaginosis (Gardnerella) ( Grayish milky discharge, whiff test: fishy odour, clue cells, pleomorphic gram negative rods.) treated with which drugs?
Metronidazole
97
Streptogramins
(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
Antimalarial: Chloroquine MOA Resistance Adverse effects
● 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
Antimalarial: Primaquine MOA: Clinical uses Adverse effects
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
Antimalarial: Mefloquine MOA Clinical uses:
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
Antimalarial: Artensuate MOA Clinical uses
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
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
Antimalarial: Artensuate
103
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.
Mefloquine
104
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
Primaquine
105
● 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.
Chloroquine