Block 3 material simplified (Antibiotics) Flashcards
Penicillin G & Penicillin V
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
Penicillin G & Penicillin V
Penicillinase-Sensitive-Penicillin’s
MOA:
Clinical uses:
Adverse effects:
Resistance:
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
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
Penicillinase-Sensitive-Penicillin’s
Penicillinase-Resistance-Penicillin’s
MOA:
Clinical uses:
Adverse effects:
Resistance:
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
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
Penicillinase-Resistance-Penicillin’s
Antipseudomonal penicillin’s
MOA:
Clinical uses:
Adverse effects:
Resistance:
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
1st Generation Cephalosporins
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
1st Generation Cephalosporins
2nd Generation Cephalosporins
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
2nd Generation Cephalosporins
3rd Generation Cephalosporins
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
3rd Generation Cephalosporins
4th Generation Cephalosporins
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
4th Generation Cephalosporins
5th Generation Cephalosporins
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
5th Generation Cephalosporins
Carbapenems
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
Carbapenems
Monobactam
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
Monobactam
Match the Beta-lactamase inhibitor with the penicillin:
Amoxicillin
Ampicillin
Piperacillin
Amoxicillin-Clavulanate acid
Ampicillin-Sulbactam
Piperacillin-Tazobactam
Vancomycin
MOA:
Clinical use:
Adverse effects:
Resistance:
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
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
Vancomycin
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,
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
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
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
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)
MOA:
30S inhibitor
Clinical use:
Broad spectrum for gram +ve & gram -ve
MRSA & VRE
Adverse effects:
Gi upset (N/V)
Bleeding (dose dependent)
Tigecycline
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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)
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)
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
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
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
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
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
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
Which drugs are used for M. Leprae?
Dapsone or Rifampin (TB form)
Clofazimine (lepromatous form)
Which drugs are used for MAC?
Azithromycin or Clarithromycin + Ethambutol
Which drugs are used for M. TB?
Rifampin
Isoniazid
Pyrazinamide
Ethambutol
Streptogrammins
Which drugs inhibit 50S subunits?
Chloramphenicol
Clindamycin
Macrolides
Linezolid
Streptogramins
Which drugs inhibit 30S subunits?
Aminoglycosides
TCAs
Tigecycline
Which drugs inhibit mRNA via RNA polymerase?
Rifampin
Which drugs form free radicals to damage DNA?
Metronidazole
Which drugs inhibit DNA Gyrase (topoisomerase II)?
Fluoroquinolones & Quinolones
Which drugs disrupt membrane integrity?
Daptomycin (gram +ve)
Polymyxins (gram -ve)
Which drugs inhibit Folic acid synthesis & reduction?
Sulfonamides
Trimethoprim
Which drugs inhibit Peptidoglycan synthesis?
Vancomycin & Bacitracin
Which drugs inhibit Peptidoglycan cross-linking?
PSP
PRP
Antipseudomonal penicillin’s
Cephalosporins
Carbapenems
Monobactams
Which drugs inhibit mRNA synthesis?
Rifampin & Rifabutin
Which drugs works best in pH environments (phagosomes)?
Pyrazinamide
Which drug inhibits arabinogalactan synthesis?
Ethambutol
Which drugs inhibit mycolic acid synthesis?
Isoniazid
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
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
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
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
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
MOA:
works in acidic pH (bacterial phagosomes)
Clinical uses:
M. TB (RIPES)
Adverse effects:
1) Hyperuricemia/Gout
2) Hepatotoxicity
3) Arthralgias
Pyrazinamide
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)
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
Streptomycin
MOA:
Clinical uses:
Adverse effects:
Resistance:
30S inhibitor
Clinical uses:
M. TB (RIPES)
Adverse effects:
1) Tinnitus
2) Ataxia
3) Nephrotoxicity
30S inhibitor
Clinical uses:
M. TB (RIPES)
Adverse effects:
1) Tinnitus
2) Ataxia
3) Nephrotoxicity
Streptomycin
Prophylaxis drugs for exposure to Meningitis?
Ceftriaxone
Ciprofloxacin
Rifampin
Prophylaxis drugs for exposure to Endocarditis & dental surgery?
Amoxicillin
Prophylaxis drugs for recurrent UTI’s?
TMP-SMX
Prophylaxis drugs for exposure to Strep B when pregnant?
Intrapartum, Penicillin G or Ampicillin
Prophylaxis drugs for Gonorrhea conjunctivitis in newborns?
Erythromycin
Prophylaxis drugs for post op S. aureus?
Cefazolin or Vancomycin (MRSA)
Prophylaxis drugs for Strep pharyngitis in children with post rheumatic fever?
Benzathine (penicillin G) or oral penicillin V
What are the drugs used to treat MRSA?
Vancomycin, Daptomycin, Linezolid, Tigecycline, Ceftaroline (5th) , Doxycycline
What are the drugs used to treat VRE?
Daptomycin, Linezolid, Tigecycline, Streptogramins
What are the drugs used to treat multi-drug resistant P. aeruginosa?
Acinetobacter baumannii (Polymyxin B & Colistin (polymyxin E))
What are the drugs used to treat HIV infection/aids?
CD4<200 = TMP-SMX
(Pneumocystis pneumoniae)
CD4<100 = TMP-SMX
(Pneumocystis pneumoniae & Toxoplasmosis)
Chlamydia (Mucopurulent discharge, pleomorphic gram-negative, intracellular) is treated with which drugs?
Azithromycin or Doxycycline.
Gonorrhea (Yellow-green discharge, gram-negative intracellular diplococci) is treated with which drugs?
Ceftriaxone plus Azithromycin or Doxycycline.
Syphilis (Painless chancre, gram-negative spiral-shaped bacteria) treated with which drugs?
Penicillin G
Trichomoniasis (Foul-smelling, yellow -green purulent discharge, trophozoites w/multiple flagella) Which drugs treat this?
Metronidazole or Tinidazole.
Herpes (Pain, pruiritis, rash)
Antivirals like Acyclovir, Valacyclovir
Candida Vaginosis (Milky, curdy white discharge, yeast infection) treat with which drugs?
Fluconazole, clotrimazole
Bacterial Vaginosis (Gardnerella) ( Grayish milky discharge, whiff test: fishy odour, clue cells, pleomorphic gram negative
rods.) treated with which drugs?
Metronidazole
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.
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.
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),
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.
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
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
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
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
● 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
