Aminoglycoside

Hexose ring + amino

sugar

Tetracycline

Chloramphenicol

Macrolide
Lactone ring + deoxy
sugar

Quinolone

MOA

-irreversible, cidal
-passive diff via porin
across OM
-O2-dep transport
-30S
-conc dep

-reversible
-passive diff & active
-30S
-prevent tRNA bind to
A site

-reversible, static
-50S
-inhibits peptidyl
transferase
-inhibits peptide bond
formation

PK

A: hydrophilic (IM/IV)
D: x cross BBB
M: E: glomerular filtration
-significant PAE

A: PO (--food, cation,
alkaline), IV
D: calc tissue,
placenta
M: enterohepatic
E: U&B

A: prodrug hydrolysed
D: CSF
M: glucuronyl
transferase
E: renal secretion
(90%)

-usually cidal
-G-ve: block DNA
gyrase (transcription,
repair, replication)
-G+ve: block
topoisomerase IV
(separation of
replicated DNA)
A: PO, IV
D: wide
M: liver
E: secretion, filtration

Clinical
uses

-aerobic, G-ve
-sepsis
-bact endocarditis
-tualraemia, plague
-TB
-infected burns

-cholera
-severe acne
-mixed resp infections
-periodontal
-H. pylori
-M. pneumonia,
chlamydiae,
rickettsiae

-for life-threatening,
serious infections
-bacterial meningitis
-rickettsial infections
-eye infections

-irreversible, cidal
-50S
-inhibit elongation of
peptide bond
(interfere initiation
complex formation,
blocks ribosome
translocation)
A: PO (ester, enteric
coating, stearate)
D: placenta, x cross
BBB
M: enterohepatic
E: U- 5% active
B- 95%
-strep & staph
infections
-syphilis
-whooping cough, CAP
-orodental infections
-prophylaxis for bact
endocarditis

SE

-ototoxicity
-acute renal failure
-nondepolarising
neuromuscular
blockade

-bones & teeth

-GIT
-hepatotoxicity
-others

-BM disturbance
(anaemia, erythroid
suppression)
-GIT
-Gray Baby Syndrome

-GIT (motilin agonist,

direct stimulate
motility)
-erythromycin induced
cholestatic hepatitis
(estolate ester HS)

-arthropathy,
tendinitis
-nausea, diarrhea
-avoid in pregnant
-avoid in prolong QR/
pt receiving
antiarrhythmia
-photosensitivity

Lincosamine

Vancomycin
Glycopeptide

Metronidazole

Sulfonamide
PABA analog

Trimethoprim

Structure

Structure

-GIT infections
(infectious diarrhea,
enterobact)
-resp infections (TB,
URTI, LRTI)
-GUT infections (UTI,
STD)

MOA

=macrolides

=-lactam
-cidal

-static
-inhibit
dihydropteroate
synthetase

-static
-inhibit dihydrofolate
reductase

A: IV (PO for AAPC)

D: wide
M: E: glomerular filtration

-cidal
-reacts with bact DNA
(inhibits replication,
fragmentize existing
DNA)
A: PO, IV, rectal
D: wide
M: liver
E: U

PK

A: PO, IV
D: plasma protein
bound, x cross BBB
M: liver
E: U&B

A: PO
D: CSF, placenta,
protein-bound
M: liver (variable)
E: glomerular filtration

A: PO
D: CSF
M:
E: U

Clinical
uses

-prophylaxis for bact

endocarditis
-orodental infections
-tx anaerobic
infections
+primaquine ->P.
jiroveci

-sepsis
-AAPC, MRSA
-endocarditis (+AG)

-antiprotozoa
-anaerobes
-periodontitis, ANUG

-oral absorbable (UTI,

2nd line malaria,
toxoplasmosis

-TMP alone (UTI)

-IV TMP-SMZ
(pneumocystis
pneumonia, G-ve
sepsis)
-PO TMP-SMZ (GIT
infections, P. jiroveci
in resp, prostatitis,
otitis media)

-oral non-absorbable
(inflammatory bowel
disease)
-topical ( bact
conjunctivitis,
trachoma, burn
wounds)

SE

AAPC (suppress
normal flora, allow
Clostridium difficile
overgrow, produce
exotoxin A&B, colon
tissue necrosis

-HS (flushing,
hypotension,
tachycardia)
-phlebitis
-nephrotoxicity,
ototoxicity

Structure

Penicillin
-lactam (6-aminopenicillanic
acid) + R

MOA

-mimic D-Ala-D-Ala

-disulfiram-like effect
-nausea, headache,
metallic
-oral candidiasis
-potentiates warfarin
effect

Monobactam
Monocyclic -lactam
ring

Carbapenem

-HS (skin rash, GIT,

Stevens-Johnson
syndrome)
-UT (crystalluria)
-hematopoietic
(anaemia, haemolysis
in G6PD def,
kernicterus)

-antifolate effect ( BM
depression,
megaloblast anaemia,
leuko- &
granulocytopenia, HS)
-TMP-SMZ
(=sulfonamide, GIT
upset, HS)

Cephalosporin
Thiazolidine ring +-lactam ring +
R1 + R 2
=-lactam

-covalent bond with PBP

(enzyme-penicillin complex)
-inactivate PBP-> compromise
cell wall intergrity
-trigger autolysin ->lysis
PK

Clinical
uses

SE

A: PO, IM
D: placenta; bone& CSF when
inflamed
M: liver insignificant
E: active tubular secretion (90%),
GFR, as active molecule,
inhibited by probenecid
Natural: G+ve, clostridium,
spirochete, G-ve anaerobe
Antistaph: staph with lactamase
Aminopen, antipseudo: UTI, LRTI,
sinusitis, otitis, pen-resistant
pneumococci, pseudomonal
infections

-acute interstitial nephritis

-HS (skin rash, anaphylactic
shock, serum sickness)

A: IV
D: CSF
M:
E:

A: IV
D:
M: dehydropeptidase
I (inhibited by
cilastatin)
E:

A: PO (*1st), IV (most)
D: good
M:
E: active secretion except
ceftriaxone (bile)

-anaerobic G-ve rods

--lactamase
-pen-allergic pt
-meningitis

-mixed aerobic
+anaerobic
-pseudomonal
infections
--lactamase
producing
enterobacter

1st gen: surgical prophylaxis,

staph/strep, UTI

-phlebitis

-GIT disturbances,
skin rash, rxn at
infusion site
-seizures in renal
failure

2nd gen: H. influenza/M. catarrhalis,

mixed anaerobic infections,
orodental infections
3rd gen: bact meningitis,
neutropenia +
immunocompromised,
pseudomonas infections, gonorrhea
4th gen: =3rd, enterobacter
5th gen: multidrug-resistant S.
aureus
-HS
-irritation (pain, thrombophlebitis)
-hematologic (disulfiram-like,
bleeding)
-GIT (PMC, anorexia, nausea, vomit)
-other