Antibacterial
Group Drugs MOA Uses ADR Resistance Pharmacokinetics Additional info
Bactericidal – disturb cell wall synthesis
Penicillin Penicillin G Inhibit cell wall synthesis DOC for syphilis Hypersensitivity Beta lactamase A – not acid stable (IV) ROA depends on: -
- Acid stability
Bind to PBP Streptococci Nephritis Efflux pump E- Rapidly excreted by kidney - Bioavailability
- Infection severity
Inhibit transpeptidation Meningococci GI upset Impaired penetration Allergy – give tetracycline
(cross-link) (x100% effective) Probenecid inhibits excretion of
Pneumococci Change in PBP penicillin
W/O peptidoglycan synthesis
Gram+ bacillus
Penicillin V Weak & endosmosis Oropharyngeal infection Acid stable (oral) Narrow spectrum
Methicillin Suspected S. aureus IV If MRSA, give vancomycin instead
Bacteria burst infection
Nafcillin Serious S. aureus infection
Ampicillin Production of autolysin Sore throat Oral Extended
Cause lesions Enterococci
E. coli (resistant ald)
Salmonella spp.
Amoxicillin UTI Extended
Sinusitis & otitis Better absorbed than ampicillin
Lower respiratory tract
infection
Piperacillin P. aeruginosa IV Extended
Frequently used with aminoglycoside
W penicillinase inhibitor
Cephalosporin Cephalexin Gram+ cocci Allergy Oral 1st gen
E. coli Toxicity Kidney excretion
K. pneumonia Bleeding disorder (give
Cefuroxime Both gram Vit K) Oral 2nd gen
IV (serious)
H. influenzae
Ceftriaxone Both gram IV/IM 3rd gen
H. influenzae Pass BBB Empirical for serious
, N. spp.
Cefepime Both gram IV 4th gen
H. influenzae Pass BBB & CSF
N. spp. 2h HL
P. aeruginosa Kidney excretion
S. aureus
S. pneumonia
Monobactem Aztreonam Aerobic gram – rods only Uncommon IV Alternative to penicillin allergy
(P. aeruginosa)
1-2h HL
Prolonged in kidney failure
Carbapenem Imipenem Gram – rods (P. GI upset IV 1st class
aeruginosa)
Skin rash Prolonged in kidney failure
Gram+
Infusion reaction
Anaerobes
Seizure (excess in renal
failure)
No effect
Beta-lactamase inhibitor Clavulanic acid Bind to beta-lactamase Plasmid encoded beta- No bactericidal effect
lactamase
Inactivate it - Gonococci Clavulanic acid & amoxicillin
- Streptococci (Augmentin)
- E. coli
- H. influenzae Salbactam & ampicillin (Unasyn)
Tazobactam & pipercillin (Zosyn)
Clavulanic acid & ticarcillin
(Timentin)
Glycopeptide Vancomycin Inhibit cell wall synthesis MRSA Infusion reaction IV/oral (enterocolitis) Narrow
Bind to D-Ala peptidoglycan Enterococcal endocarditis Fever Accumulate in renal Alternative in penicillin allergy
(w gentamicin) insufficiency
Inhibit transglycosylase Ototoxicity DOC for C. difficile is metronidazole
Infection of bones, joints &
Inhibit elongation of peptidoglycan soft tissue Nephrotoxicity
, Weak wall & lysis Pneumonia Hypotension
Septicemia Red-man syndrome
Pseudomembranous colitis Erythematous rashes
(backup)
Bacteriostatic – inhibit protein synthesis
Lincomycin Clindamycin Binds to the 23s of the 50s MRSA GI upset 50s binding site Oral/IV
methylation
Inhibit ribosome assembly & Anaerobic Skin rashes Extensive distribution (x BBB
translocation Enzymatic & CSF)
Endocarditis prophylaxis Colitis (C. difficile take inactivation
over normal flora) Liver metabolism
AIDs related
toxoplasmosis (w Bile/urine excretion
pyrimethamine)
Oxazolidinones Linezolid Binds to 23s of the 50s Multidrug resistant Gram+
Tedizolid
Inhibit 70s formation & translation MRSA
VREF
Tetracycline Tetracycline Inhibit protein synthesis Both gram GI upset Variable oral absorption Broad
- Chlamydia
Bind to 30s - Mycoplasma Natural flora disturbance Wide tissue distribution Used in penicillin allergy
- Rickettsia (oral/vaginal candidiasis) - Cross placenta
Blocks aminoacyl-tRNA to A site
Syphilis Hepatoxicity Excreted in bile & urine
Inhibit addition of new AAs
Cholera Renal tubular acidosis
Helicobacter pylori (gastric Permanent yellowing of
& duodenal ulcer) bone & teeth (in youngs)
Prophylaxis of protozoa Photosensitivity
Acne
Doxycycline Lyme disease (B. >95% oral absorption Broad
burgdorferi)
Bile excretion Used in renal impairment
Chlamydia
Mycoplasma
Cholera
Bactericidal ([]-dependent killing & PAE)
, Aminoglycosides Streptomycin Porin channel diffusion/O2- Enterococcal endocarditis Deafness in newborn Efflux pump Aminoglycoside IV well absorbed
dependent transport system (strep)
nd
2 line for TB ↓d uptake
Gentamicin Binds to 30s Gram – rods Ototoxicity Aminoglycoside HL 2-3H – x renal
- x Initiation complex formation (synergistic with beta- Modification & impairment
- mRNA misreading lactam) Nephrotoxicity inactivation by
- Polysome → non-functional plasmid enzyme
monosomes E. coli Allergy
K. pneumoniae Neuromuscular blockade
Tobramycin Gram- → respiratory paralysis Aminoglycosides normally x2/day
with normal renal (now 1/day)
P. aeruginosa
Synergistic with penicillin/
glycopeptide
Chloramphenicol Chloramphenicol Bind to 50s Serious rickettsia GI upset IV X need to change in renal
insufficiency but in hepatic failure
Inhibit peptide bond formation Meningitis (alternative to Aplastic anemia Widely distributed
penicillin) Rarely systemic due to
Gray baby syndrome Conjugated in liver - Toxicity
Eye (topical) - Resistance
Urine excretion - Other alternatives
Inhibit hepatic
drug metabolizing enzyme
Warfarin & phenytoin elevate its
effect
Macrolides Azithromycin Bind to 50s Urethritis (C. trichomonas) GI upset Efflux pump 2-4 days HF Alternative to ceftriaxone for
gonorrheae
Interfere with transpeptidation N. gonorrheae Ototoxicity ↓ 50s binding Bile excretion
Clarithromycin H. influenzae affinity Urine excretion Macrolides has long PAE
Inhibit translocation & complex
dissociate M. leprae ↓d absorption
T. gondii Esterase
Erythromycin Both gram Good oral bioavailability (w Moderate
enteric coating)
Chlamydia No CNS entry
Bile excretion
Mycoplasma Disturb normal flora that inactivate
digoxin → high reabsorption of
Legionella digoxin
Group Drugs MOA Uses ADR Resistance Pharmacokinetics Additional info
Bactericidal – disturb cell wall synthesis
Penicillin Penicillin G Inhibit cell wall synthesis DOC for syphilis Hypersensitivity Beta lactamase A – not acid stable (IV) ROA depends on: -
- Acid stability
Bind to PBP Streptococci Nephritis Efflux pump E- Rapidly excreted by kidney - Bioavailability
- Infection severity
Inhibit transpeptidation Meningococci GI upset Impaired penetration Allergy – give tetracycline
(cross-link) (x100% effective) Probenecid inhibits excretion of
Pneumococci Change in PBP penicillin
W/O peptidoglycan synthesis
Gram+ bacillus
Penicillin V Weak & endosmosis Oropharyngeal infection Acid stable (oral) Narrow spectrum
Methicillin Suspected S. aureus IV If MRSA, give vancomycin instead
Bacteria burst infection
Nafcillin Serious S. aureus infection
Ampicillin Production of autolysin Sore throat Oral Extended
Cause lesions Enterococci
E. coli (resistant ald)
Salmonella spp.
Amoxicillin UTI Extended
Sinusitis & otitis Better absorbed than ampicillin
Lower respiratory tract
infection
Piperacillin P. aeruginosa IV Extended
Frequently used with aminoglycoside
W penicillinase inhibitor
Cephalosporin Cephalexin Gram+ cocci Allergy Oral 1st gen
E. coli Toxicity Kidney excretion
K. pneumonia Bleeding disorder (give
Cefuroxime Both gram Vit K) Oral 2nd gen
IV (serious)
H. influenzae
Ceftriaxone Both gram IV/IM 3rd gen
H. influenzae Pass BBB Empirical for serious
, N. spp.
Cefepime Both gram IV 4th gen
H. influenzae Pass BBB & CSF
N. spp. 2h HL
P. aeruginosa Kidney excretion
S. aureus
S. pneumonia
Monobactem Aztreonam Aerobic gram – rods only Uncommon IV Alternative to penicillin allergy
(P. aeruginosa)
1-2h HL
Prolonged in kidney failure
Carbapenem Imipenem Gram – rods (P. GI upset IV 1st class
aeruginosa)
Skin rash Prolonged in kidney failure
Gram+
Infusion reaction
Anaerobes
Seizure (excess in renal
failure)
No effect
Beta-lactamase inhibitor Clavulanic acid Bind to beta-lactamase Plasmid encoded beta- No bactericidal effect
lactamase
Inactivate it - Gonococci Clavulanic acid & amoxicillin
- Streptococci (Augmentin)
- E. coli
- H. influenzae Salbactam & ampicillin (Unasyn)
Tazobactam & pipercillin (Zosyn)
Clavulanic acid & ticarcillin
(Timentin)
Glycopeptide Vancomycin Inhibit cell wall synthesis MRSA Infusion reaction IV/oral (enterocolitis) Narrow
Bind to D-Ala peptidoglycan Enterococcal endocarditis Fever Accumulate in renal Alternative in penicillin allergy
(w gentamicin) insufficiency
Inhibit transglycosylase Ototoxicity DOC for C. difficile is metronidazole
Infection of bones, joints &
Inhibit elongation of peptidoglycan soft tissue Nephrotoxicity
, Weak wall & lysis Pneumonia Hypotension
Septicemia Red-man syndrome
Pseudomembranous colitis Erythematous rashes
(backup)
Bacteriostatic – inhibit protein synthesis
Lincomycin Clindamycin Binds to the 23s of the 50s MRSA GI upset 50s binding site Oral/IV
methylation
Inhibit ribosome assembly & Anaerobic Skin rashes Extensive distribution (x BBB
translocation Enzymatic & CSF)
Endocarditis prophylaxis Colitis (C. difficile take inactivation
over normal flora) Liver metabolism
AIDs related
toxoplasmosis (w Bile/urine excretion
pyrimethamine)
Oxazolidinones Linezolid Binds to 23s of the 50s Multidrug resistant Gram+
Tedizolid
Inhibit 70s formation & translation MRSA
VREF
Tetracycline Tetracycline Inhibit protein synthesis Both gram GI upset Variable oral absorption Broad
- Chlamydia
Bind to 30s - Mycoplasma Natural flora disturbance Wide tissue distribution Used in penicillin allergy
- Rickettsia (oral/vaginal candidiasis) - Cross placenta
Blocks aminoacyl-tRNA to A site
Syphilis Hepatoxicity Excreted in bile & urine
Inhibit addition of new AAs
Cholera Renal tubular acidosis
Helicobacter pylori (gastric Permanent yellowing of
& duodenal ulcer) bone & teeth (in youngs)
Prophylaxis of protozoa Photosensitivity
Acne
Doxycycline Lyme disease (B. >95% oral absorption Broad
burgdorferi)
Bile excretion Used in renal impairment
Chlamydia
Mycoplasma
Cholera
Bactericidal ([]-dependent killing & PAE)
, Aminoglycosides Streptomycin Porin channel diffusion/O2- Enterococcal endocarditis Deafness in newborn Efflux pump Aminoglycoside IV well absorbed
dependent transport system (strep)
nd
2 line for TB ↓d uptake
Gentamicin Binds to 30s Gram – rods Ototoxicity Aminoglycoside HL 2-3H – x renal
- x Initiation complex formation (synergistic with beta- Modification & impairment
- mRNA misreading lactam) Nephrotoxicity inactivation by
- Polysome → non-functional plasmid enzyme
monosomes E. coli Allergy
K. pneumoniae Neuromuscular blockade
Tobramycin Gram- → respiratory paralysis Aminoglycosides normally x2/day
with normal renal (now 1/day)
P. aeruginosa
Synergistic with penicillin/
glycopeptide
Chloramphenicol Chloramphenicol Bind to 50s Serious rickettsia GI upset IV X need to change in renal
insufficiency but in hepatic failure
Inhibit peptide bond formation Meningitis (alternative to Aplastic anemia Widely distributed
penicillin) Rarely systemic due to
Gray baby syndrome Conjugated in liver - Toxicity
Eye (topical) - Resistance
Urine excretion - Other alternatives
Inhibit hepatic
drug metabolizing enzyme
Warfarin & phenytoin elevate its
effect
Macrolides Azithromycin Bind to 50s Urethritis (C. trichomonas) GI upset Efflux pump 2-4 days HF Alternative to ceftriaxone for
gonorrheae
Interfere with transpeptidation N. gonorrheae Ototoxicity ↓ 50s binding Bile excretion
Clarithromycin H. influenzae affinity Urine excretion Macrolides has long PAE
Inhibit translocation & complex
dissociate M. leprae ↓d absorption
T. gondii Esterase
Erythromycin Both gram Good oral bioavailability (w Moderate
enteric coating)
Chlamydia No CNS entry
Bile excretion
Mycoplasma Disturb normal flora that inactivate
digoxin → high reabsorption of
Legionella digoxin
