Antimicrobials 2
Subclass, Drug Mechanism of Action
Inhibitors of Protein Ribosomal resistance to this
Sythesis: drug develops readily,
limiting its role as a single
30S Inhibitors: agent
Aminoglycosides: IM/IV for mycobacterial
Streptomycin infection
Used mainly in severe
infections (sepsis,
pneumonia) caused by gram
(-) bacteria
Gentamicin In combination with nafcillin
in selected cases of
staphylococcal endocarditis
Antimicrobial spectrum and
pharmacokinetics are
virtually identical to
gentamicin
Tobramycin Blood levels should be
monitored in renal
insufficiency
Semisynthetic derivative of
kanamycin
Amikacin Resistant to many
inactivating enzymes
Multi-drug resistant TB
Shares many characteristics
with gentamycin and
Netilmicin tobramycin
Multi-drug resistan TB
Used for bowel preparation
Kanamycin and for elective surgery
Neomycin There is complete cross-
resistance between
Effects
nd
Mainly used as a 2 -line
agent for the tx of TB
Used in combination with
Pen G for bactericidal activity
in endocarditis due to
viridans streptococci or
enterococci
Slightly more active against
pseudomonas
Strains of multi-drug resistan
M. tuberculosis are usually
susceptible
Serum concentrations should
be monitores
Not significantly absorbed
from the GIT
Too toxic for parenteral use
Limited to topical and oral
Clinical Applications
Plague, tularemia, brucellosis
Antidotes: calcium gluconate,
neostigmine
P, T, I
Pain at injection site, fever,
skin rashes, vestibular
dysfunction, nephrotoxic,
ototoxic
Nephrotoxicity (reversible),
irreversible ototoxicity
(manifests as vestibular
dysfunction), hypersensitivity
reactions
Nephrotoxic, autditory
dysfunction
Nephrotoxic and ototoxic
(auditory dysfunction),
curare-like muscular
blockade and respiratory
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 kanamycin and neomycin route arrest
Chemically related to Dispensed as Used as an alternative for the Pain at injection site, fever,
aminoglycosides dihydrochloridepentahydrate tx of gonorrhea for patients nausea, nephrotoxicity,
Spectinomycin Binds to 30S subunit for IM injection that are allergic to penicillin anemia
(bacteriostatic) or whose gonococci are
resistant to other drugs
Tetracyclines: Discolors teeth, inhibits bone
Short-acting: growth in children

Tetracycline
Oxytetracycline
Chlortetracycline
Intermediate-acting: Inhibits the action of ADH in
the renal tubule and been
Demeclocycline used in the tx of SIADH
certain tumors
Methacycline
Long-acting: Eliminated through the feces
Can be combined with
Doxycycline ceftriaxone = tx of
gonococcal infection
Carrier state of Meningococcemia Dizziness, vertigo
meningococcal infections, N. 200 mg daily orally for 5 days
Minocycline asteroids, N. gonorrhea can eradicate the
meningococcal carrier state
Parenteral only
Tigecycline
50S Inhibitors: Attaches to P sites of Bactericidal = H. influenza, N. Meningitis, ricketssia, Gray baby syndrome, oral
microbial ribosomes and meningitides, B. fragilis salmonella, anaerobic and vaginal candidiasis,
inhibits the functional Bacteriostatic = S. infections irreversible aplastic anemia,
Chloramphenicol attachment of aminoacyl end epidermidis, S. aureus, M. Occasionally used topically in reversible BM depression
of AA-Trna to 50S subunit pneumonia, L. the tx of eye infections due
monocytogenes etc. to its good penetration into
ocular tissue and aqueous
humor
Macrolides:

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Old generation: Binds to P site of the 50S Food interferes with Metabolites can inhibit
bacterial subunit absorption cytochrome p450 enzymes
Prototype Not removed by dialysis and increase the serum
Traverses the placenta and concentrations of
reaches the fetus theophylline, oral
Erythromycin anticoagulants, cyclosporine,
methylprednisolone, GIT
dysfunction, intrahepatic
cholestatic jaundice
Oleandomycin
Troleandomycin
Spiramycin
Josamycin
New generation:
Rosamycin
Roxithromycin
Derived from erythromycin More active against gram (+)
by addition of methyl group pathogens, legionella and
Clarithromycin and has improved acid chlamydia than erythromycin
stability and oral absorption
15 atom lactone macrolide Active against M. avium and Does not inactivate
Derived from erythromycin T. gondii cytochrome p450 enzymes
Azithromycin by addition of a methylated Long half-life allows once and free of drug interactions
nitrogen into the lactone ring daily oral administration that occur with erythromycin
and clarithromycin
Dirithromycin
Hepatitis, renal failure
Ketolides
[Telithromycin]
Lincosamides: Attaches to the 50S Narrow gram (+) spectrum, Most important indication: tx Diarrhea, nausea, skin rashes,
ribosomal subunit, inhibits excellent activity against of severe anaerobic impaired liver function and
protein synthesis by anaerobes infections caused by neutropenia, antibiotic
Clindamycin interfering with the Prophylaxis of endocarditis in bacteroides and other associated colitis caused by
formation of initiation patients with valvular heart anaerobes that often toxigenic C. difficile

3
 complexes and translocation disease for dental procedures participate in mixed
reaction infections
Lincomycin
Oxazolidinones: Inhibits protein synthesis by Unique binding site located Tx of infections caused by Hematologic,
preventing formation of the on the 23S ribosomal RNA of vancomycin resistant E. thrombocytopenia,
ribosome complex that the 50S subunit, results in no faecium and other infection serotonin-syndrome
Linezolid initiates protein synthesis cross resistance with other by multiple drug resistant
drug classes organisms
Metabolic Synthesis Structural analogs of PABA Inhibits groth by reversibly Inhibits the growth of both Hemolytic reaction in patient
Inhibitors: Competitively inhibits blocking folic acid synthesis gram (+) and gram (-) with G6PD deficiency,
dihydropteroate synthase Crosses placenta and bacteria kernicterus
and folate production secreted breastmilk, should Ricketssia are not inhibited
not be given to pregnant but rather stimulated in their
Sulfonamides women growth
Inhibits bacterial dihydrofolic Some nontuberculous UTI Kernicterus
Trimethoprim- acid reductase mycobacterial infections Shigellosis
Sulfamethoxazole DOC pneumocystis carinii Systemic salmonella infection
pneumonia caused by ampicillin and
(Cotrimoxazole) chloramphenicol resistant
organisms
Inhibitors of Nucleic
Acid Syntheis:
Flouroquinolones:
st
1 generation:
Nalidixic Acid
nd
2 generation: Most widely used Synergistic with beta lactams
DOC for anthrax M. tuberculosis
Ciprofloxacin Most potent for P.
aeruginosa
Not effective in systemic
Norfloxacin infections
Ofloxacin
rd
3 generation:
Levofloxacin Prostatitis, E. coli, STD, skin

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 and lower infection, S.
pneumonia
Moxifloxacin
Gatifloxacin
th
4 generation:
Trovafloxacin