ANTIBIOTIC REVIEW SHEET

Antibiotic
(classification)
Mechanism Resistance Antibacterial
Spectrum
Side Eects Metabolism !istribution
Adm" # CNS
Anti$M%cobacterial !ru&s'
(TB Treatment)
!ue to dru& resistanc( combo therap% is recommende )i"e" isonia*id( riampin( and p%ra*inamide +ith ethambutole i resistance to isonia*id is , -./
Isonia*id
(bactericidal) Activated by
mycobacterial KAT G (a catalase
peroxidase). It binds to InhA (an enoyl
acyl carrier protein NAD red!ctase).
InhA is involved in mycolic acid
sythesis and hence inhibits cell "all
synthesis.
#!tation in InhA.
$oss of KAT G activity
It penetrates macropha%es and is
effective a%ainst intra and extre&
cell!lar or%anisms
#ycobacteria
Kansasii
'eripheral ne!ritis
$iver dama%e
Glossitis
GI dist!rbance
Aller%ic rxn
(N) reversed by pyridoxine
(*&+ ho!rs) lon% or short is
%enetically determined (ethnic)
Activity of hepatic&N&acetyl
transferase inactivaiton
,xcreted via -idney
.ral
Dr!% interaction/
Al!min!m antacid
decreases absorption.
Decreases '012
phenytoin toxicity
3es
Riampin
(bactericidal) Inhibits initiation of
transcription by bindin% to the s!b!nit
of bacterial 4NA polymerase
#!tation of 4NA polymerase
res!ltin% in affinity or
permeability
$eprae
Kansasii
.ran%e5red feces6 !rine6
saliva6 and s"eat
$iver dama%e
GI dist!rbance
Aller%y
(7&1 ho!rs8 deacylation) ,xcreted
in bile and enterohepatic
circ!lation
.ral
Dr!% interaction/
'012
.ther dr!% activity
("arfarin6 prednisone6
contraception6
methadone)
Ethambutol
(bacteriostatic) Inhibits arabin o%alactan
sythesis (cell "all). This "ea-ens the
"all and enhances lipophillic dr!%s li-e
4ifampin
9n-no"n T!berc!losis
#A(
Kansasii
.ptic ne!ritis
vis!al ac!ity
red %reen vision
aller%ic rxn
exacerbate %o!t6 b!t less than
pyra:inamide
(0 ho!rs) !nchan%ed
-idney
oral
0%ra*inamide
(bactericidal) 9n-no"n
ydroly:ed into its active form6
pyra:inoic acid. Tho!%ht to tar%et fatty
acid synthase I6 "hich converts
%lycolipid to mycolic acid. ence6 the
cell "all is affected
$oss of pyra:in amidase action6
"hich activates pyra:inamide.
'enetrates the macropha%e
lysosome beca!se it operates best
at lo" p
T!berc!losis
$iver dama%e
GI dist!rbance
,xacerbates %o!t more than
ethamb!tol
Kidney .ral
Streptom%cin
Inhibits bacterial protein synthesis by
bindin% to ribosomes
'oint m!tation in ribosome 'oor diff!sion across plasma
membrane. ence6 it only affects
extracell!lar t!berc!losis.
;estib!lar f!nction
earin% loss
Aller%ic rxn
4ash
4enal dama%e
(+ ho!rs) 9nchan%ed
Kidney
I#
Riabutin
(bactericidal) Inhibits initiation of
transcription by bindin% to the s!b!nit
of bacterial 4NA polymerase
#!tation of 4NA polymerase
res!ltin% in affinity or
permeability
Atypical mycobacteri!m that
affects I; <
#A(
Kansasii
GI dist!rbance
4ash
Discolor body fl!ids
(0&1 ho!rs)
#etaboli:ed by liver
,xcreted in feces and !rine
.ral
D!r% interaction/
'012
Thereby6 other
dr!%t concentrations
li-e A=T
Antibiotic
(classification)
Mechanism Resistance
Antibacterial
Spectrum
Side Eects Metabolism
!istribution
Adm" # CNS
Sulonamides
)inhibits metabolism/
)tr!ct!ral analo%s of para&aminoben:oic
acid (pABA) that inhibits
dihydropteroate synthase (DHTS).
*selectivity= bacteria synthesize folate
but humans cant
*. en:yme m!tations of DT)
7. Increase in pABA
+. permeability to dr!%
0. !tili:ation of preformed folate
Bacteriostatic. emolytic anemia ( G>'D)
ypersensitivity 4xn. (incl.
)teven ?ohnson )yndrome@)
Kernicter!s in infants
AdonBt !se in pre%nancy6
lactation
(rystall!ria
,xcreted via %lomer!lar filtration
Cdr!%D in !rine.
)pecial care in -idney dx5 renal
fail!re dose
Eell absorbed
peritoneal6 ple!ral
fl!ids F cross
placenta.
()G
Trimethoprim
)inhibits metabolism/
)tr!ct!ral analo% of pteridine portion of
dihydrofolic acid.
(ompetitive inhibitor of dihydrofolate
reductase (DH!").
*selectivity= affinity for bacterial
dihydrofolate reductase (#$%%%).
'lasmid mediated m!tations in
DG4 (rare)
Bacteriostatic ("hen !sed alone)
1 is bacteriocidal +hen used
+ith Sulametho2a*ole )SM3/
Golate deficiency.
Na!sea F vomitin%.
)-in er!ptions.
(N) dist!rbances.
AdonBt !se in pre%nancy@
)pecial care in -idney dx5 renal
fail!re dose
(oncentrates in
prostate.
9rine/Blood *22
Ahas hi%her ;D than
s!lfonamides
T#'/)#= of 0/72
is optimal
(N)
0enicillin
)inhibits cell +all
s%nthesis/
)tr!ct!ral analo% of D&ala D&ala "5
intact lactam rin%.
*.'revents peptido%lycan crosslin-in%
d!rin% cell "all phase of synthesis by
inhibitin% peptido&lycan transpeptidase.
7. Activates murine hydrolase.
*selectivity= cell 'all or
transpeptidase tar&ets in humans
*. lactamase inactivation.
7. Alterations in 'enicillin Bindin%
'roteins ('B')
+. permeability to 'enicillin
('N().
Bacteriocidal. $o" direct toxicity (so
specific to bacteria).
*. GI effects (diarrhea)
7. Thrombophlebitis post I;
inHection
+. (N) effects "5 very
dose.
0. )!perinfection
pse!domembrano!s colitis.
1. ,lectrolyte imbalance.
>. H%persensiti4it% r2n"
(immediate6 accelerated6
delayed)
Aonly 71I of oral dose is
absorbed in small intestine
(remainder feces)
4apid excretion by -idney ('T
secretion).
T
J
K +2m8 ("5 renal dx F
'robenecid)
)pecial care in renal fail!re
dose
$iver clearance Bs "5 renal dx
*. 'N( G/ .ral L
administer on empty
stomach.
7. 'N( ;/ I;
A'N( concentrates in
-idney.
'oor (N) penetration
not !sed for (N)
infections.
Cephalosporins
)inhibits cell +all
s%nthesis/
)tr!ct!ral analo% of D&ala D&ala.
'revents peptido%lycan crosslin-in%
d!rin% cell "all phase of synthesis by
inhibitin% peptido&lycan transpeptidase.
*. lactamase inactivation.
Ab!t are not as readily inactivated
as penicillin@
7. Alterations in 'enicillin Bindin%
'roteins ('B')
+. permeability to (ephalosporin
(()).
Bacteriocidal. H%persensiti4it% r2n" (cross
reactive to 'N( F ())
Aothers same as for 'N(
&for very ill pt6 often !sed "5
amino%lycoside ris- of
nephrotoxicity.
,xcretion by t!b!lar secretion F
%lomer!lar filtration.
T
J
K +2m&7 hrs. ("5 renal dx F
'robenecid)
)pecial care in renal fail!re
dose
*
st
F 7
nd
%eneration
() penetrate tiss!e
"ell.
+
rd
%eneration ()
penetrate (N) "ell
Vancom%cin
)inhibits cell +all
s%nthesis/
Glycopeptide6 not a lactam.
'revents elon%ation of cell "all by
bindin% to D&ala D&ala end of the cell
"all b!ildin% bloc- inhibits
peptido&lycan synthetase d!rin% cell
membrane phase.
'lasma mediated modification of
D&ala D&ala to D&ala D&lactate6
"hich can be !sed to elon%ate cell
"all b!t canBt be affected by
vancomycin (;().
Bacteriocidal.
Aused to t2 pseudomembranous
colitis )metronida*ole can also
be used to do this/
*. Thrombophlebitis6 chills6
fever.
7. Ototo2ic"
Amonitor renal F a!ditory
f!nction d!rin% !se.
M2I excreted by %lomer!lar
filtration.
)pecial care in renal fail!re
dose.
A T
J
K >&*2 days in anephric pt.8
not removed by hemodialysis.
I;
If %iven rapidly6
ca!ses fl!shin%
(histamine release).
C%loserine
)inhibits cell +all
s%nthesis/
Inhibits ala "acemase (prevents $&ala
D&ala) and D(ala D(ala Synthetase
(D&ala D&ala formation) d!rin%
cytoplasmic synthesis phase.
Bacteriocidal.
1contraindicated in pt5s +ith
histor% o epileps% or mental
instabilit%"
*. (N) effects (conf!sion6
coma)
7. 'eripheral ne!ritis.
+. $iver dama%e.
0. Golate deficiency.
1. #alabsorption syndrome.
.ral (N)
Bacitracin
)inhibits cell +all
s%nthesis/
Inhibits re%eneration of the lipid carrier6
"hich is responsible for transportin%
peptido%lycan prec!rsors across the cell
membrane..
Bacteriocidal. 9sed topically b5c
oral !se is toxic.
Streptom%cin
)inhibits protein
s%nthesis/
Binds at5near domain of )*7 protein on
bacterial +2). *. Allo"s N2) initiation
complex to form b!t inhibits it from
movin% alon% m4NA. 7. prevents
peptide elon%ation (prevents bindin% of
aminoacyl t4NA) +. disr!pts bacterial
cell membrane
*selectivity= )%s only in bacteria
*. #!tation in )*7 protein in +2)
s!b!nit
7. 'lasmid mediated acetylation6
adenylation6 F phosphorylation
inactivates the dr!%.
Bacteriocidal.
1 has lo+ TI must monitor6
to2icit% +# prolon&ed use )78$9
da%s/6 to2icit% +# CN VIII"
11used rarel% b#c lots o
resistance to it no+"
*. Vestibular toxicity
(di::iness6 verti%o) O
ototo2icit% (deafness).
7. Nephroto2icit%"
+. M%oneural bloc:ade
Arare
0. 4ash5fever post parenteral
administration.
No metabolism.
,xcretion by %lomer!lar filtration.
T
J
K 7 hrs. ("5 renal dx F a%e)
adH!st dose.
)elective acc!m!lation in 'T of
-idney6 endo F perilymph of hair
cells.
$imited F slo" oral
absorption.
#!st be %iven
parenteral (I;) in
C)#D.
Acc. in ple!ral6
pericardial6 synovial
fl!ids F fet!s.
$ittle ()G
penetration.
*
!apsone
'ABA a%onist. ence6 folic acid
biosynthesis is bloc-ed. 'rod!ction of
methionine6 serine6 p!rines6 and N forml
met 4NA are inhibited
C'ABAD
,n:yme m!tation
$eprae 4ash
emolytic anemia
GI dist!rbance
$iver dama%e
'eripheral ne!ropathy
,limiated in free form and
%l!c!ronide
Kidney
.ral
Cloa*imine
Binds to DNA and inhibits template
f!nction and prod!ction of cytotoxic
oxy%en radicals.
Ne". ence6 fe" cases -no"n $eprae 4ed discolori:ation o s-in6
!rine6 sp!t!m6 and s"eat
GI dist!rbance
.ral
Thalidomide
9n-no"n
Gl!tamin acid derivative
It has anti&inflammatory and imm!no&
mod!latin% effects
Ne" ,rethema
Nodos!m lepros!m
$eprae
Terato%en
'eripheral ne!ropathy
)edation
(onstipation
9n-no"n .ral
Anti$;un&al A&ents'
Antibiotic
(classification)
Mechanism Resistance
Antibacterial
Spectrum
Side Eects Metabolism
!istribution
Adm" # CNS
Amphotericin B
(polyene)
Binds to er%osterol of the cell membrane
and ma-es a pore that allo"s ionic fl!x
and cell lysis
4are 9sef!l a%ainst all f!n%i6 b!t !se
limited to systemic
'ro%ressive infections
$ife threatenin% infection
Asper%ill!s
Ac!te febrile rxn !pon
inf!sion
4enal dama%e
A:otemia
ypo-alemia
Thrombophlebitis
Anorexia
M2I protein bo!nd )lo" I; No
N%statin
(polyene)
Binds to er%osterol of the cell membrane
and ma-es a pore that allo"s ionic fl!x
and cell lysis
4are )!perficial mycosis
#ostly candida
Aller%ic rxn
GI dist!rbance
Topical No
;luc%tosine
(pyrimidine)
Deaminated by cytosine deaminase to 1
fl!oro!racil and anaboli:ed into a
n!cleotide6 1&Gd9#' or 1&G9T'. The
n!cleotide binds to thymidilate
synthetase and deprives the cell of
thymidilic acid6 an essential DNA
component. 1&G9T' incorporates into
4NA and disr!pts n!cleic acid and
protein synthesis.
$oss of cytosine permease
9#' phophorlyase or
cytosine deaminase
(rytococc!s Neoformans
)ome candida
(hromobastomycosis
(dermitacio!s mold)
Intestinal conversion to
fl!oro!racil ca!ses bone
marro" toxicity6 le!-openia6
thrombocytopenia
GI dist!rbance
9nchan%ed
Kidney
.ral 3es
<etocona*ole
(imida:ole)
(G!n%icidal) 4ed!ction of er%osterol
synthesis by inhibition of f!n%al '012.
The sterol affected is *0 demethylase.
The res!lt is a disr!ption of the
membrane permeability and f!nction.
)!perficial
#!coc!taneo!s candidiasis
Non&menin%ial coccidiodomycosis
)ele tive than ne" a:oles
'012
Adrenal and %onadal
steroids (man&boobs)
Na!sea6 vomit6 pr!iritic6 GI6
verti%o6 headache6 fever6 chill
epatotoxicity
,xtensive liver metabolism
,xcreted into bile
4ifamyc hepatic metabolism
%astric p reP!ired
for .ral absorption
No
7
Clotrima*ole
(imida:ole)
(G!n%icidal) 4ed!ction of er%osterol
synthesis by inhibition of f!n%al '012.
The sterol affected is *0 demethylase.
The res!lt is a disr!ption of the
membrane permeability and f!nction.
)!perficial mycosis ,rythema
'r!ritis
B!rnin%
GI irritation
Topical
.ral
Anti$;un&al A&ents' )continued/
Antibiotic
(classification)
Mechanism Resistance
Antibacterial
Spectrum
Side Eects Metabolism
!istribution
Adm" # CNS
Micona*ole
(imida:ole)
(G!n%icidal) 4ed!ction of er%osterol
synthesis by inhibition of f!n%al '012.
The sterol affected is *0 demethylase.
The res!lt is a disr!ption of the
membrane permeability and f!nction
)!perficial mycosis B!rnin%
Irritation
Topical
;lucona*ole
(tria:ole)
(G!n%icidal) 4ed!ction of er%osterol
synthesis by inhibition of f!n%al '012.
The sterol affected is *0 demethylase.
The res!lt is a disr!ption of the
membrane permeability and f!nction.
.ral and esopha%eal candidiasis
)!perficial mycosis ("idest of
a:oles)
(ryptococcal menin%itis
Dimorphic f!n%i
Q side effects than imida:ole
No interaction "ith liver
en:yme
GI
ypo-alemia
,dema
ypertension
9nchan%ed
Kidney
.ral
I;
3es
Itracona*ole
(tria:ole)
(G!n%icidal) 4ed!ction of er%osterol
synthesis by inhibition of f!n%al '012.
The sterol affected is *0 demethylase.
The res!lt is a disr!ption of the
membrane permeability and f!nction.
Dimorphic/ blastomycosis6
histoplasma6 sporothrix
#ost potent of tria:ole6 b!t
bioavailability Q "th rifampin
Asper%ill!s
Dermatophytosis
.nchomycosis
Interat "ith some hepatic
en:ymes
GI
ypo-alemia
,dema
ypertension
$iver
,xcreted in bile and !rine
.ral
Terbinaine
(allylamine)
Inhibits the en:yme sP!aline epoxidase
"hich inhibits er%osterol prod!ction and
cell "all inte%rity
)!perficial mycosis
R* dermatophyte
.nchomycosis
Irritation Topical
=riseoul4in
(%risan)
#ytotic inhibitor
Binds to microt!b!les to bloc- assembly
and f!nction
)!perficial mycosis GI dist!rbance
Aller%ic rxn
'hotosensitivity
Ind!ce '012. o"ever6 it
tar%ets -eratin cells and
effects are minimal
eadache
$iver
,xcreted in feces and !rine
.ral
0entamidine
'ne!mocystic carinni pne!monia
Blastomycosis
Ato4a>uone
'ne!mocystic carinni pne!monia
Blastomycosis
+
0
Cell Wall Inhibitors'
Antibiotic
(classification)
Mechanism Resistance
Antibacterial
Spectrum
Side Eects Metabolism
!istribution
Adm" # CNS
0enicillin =
& (idal
?/ Inhibits peptido&l%can transpeptidase
(a 'B' that forms crosslin-s b5t
NA#5NAG in the cell "all)
& mimics the D&ala&D&ala end of NA#
(!s!al s!bstrate) bindin% covalently to the
en: and inhibitin% it
@/ activates endo%eno!s a!tolytic en:yme
murein h%drolase "hich de%rades the cell
"all f!rther
Beta$lactamase
& hydroly:es the beta&lactam
bond
& most common esp in Gpos
& Gpos secrete o!tside cell "all
& Gne% -eep in periplasmic
space
!ecreases perm to 0EN
& Gne% can chan%e the porin so
it dosent let ',N in
Alterations in 0B0 s!ch as
alterin% the transpeptidases L ex
is #4)A
Narro" )pectr!m
& 'rimarily active
a%ainst =pos
aerobes and
anaerobes
Ao+ direct to2icit% b5c tar%et is spec to bact
& GI6 Thrombophelbitis after I;6 (N) "5 very hi%h doses6 )!perinf ().
enterocolitis)6 pse!domembrano!s colitis6 Ne!tropenia6
,lectrolyte imbalance (K
<
5 Na
<
"5 I; doses)6 (;5ne!ro toxicity "5 renal
impairment
H%persensiti4it% r2ns 1111
Immediate (2&+2 min) L rare ac!te anaphylactic rxn & I%, mediated
Also/ !rticaria6 an%ioedema6 rhinitis6 asthma6 laryn%eal edema
Accelerated (*&N7 hrs) & similar (b!t6 severe anaphylaxis6 hypotension6
death are rare)
Delayed 4eactions (+&+2 days) L self&limitin% L mostly rashes
Also/ ser!m sic-ness6 hemolytic anemia6 thrombocytopenia6
nephropathies6 )tevens&?ohnson syn6 exfoliatave dermatitis
Cross$h%persensiti4it% occ!rs "ith all the penicillins L ie yo! are
sensiti:ed to other ',NBs and cephalosporins
& 71I of oral dose absorbed L
th!s !s!ally %iven parentally
& "ide distrib!tions in body L
conc in -idney
& excreted by :idne% mainly 0T
$ t?#@ B 8C min6 probenecid
slo"s excretion
& liver inactivation minor !nless
renal dysf!nction
0arentall%
!s!ally I; or I#6
not orally b5c
stomach p
inactivates N1I

0oor CNS
penetration6
!nless the
menin%es
are inflamed
L as "ith
infection
Nacillin
& a ',Nase resistant ',N & #4)A & (an -ill ',Nase
prod!cin% Gpos
(',Nase prod!cin%
strains of ). a!re!s)
& Ineffective a%ainst
Gne%
& very rare ca!se of hepatitis & mainly biliary excretion 0arentall% d!e
to variable GI
absorption
Ampicillin
& an aminopenicillin L extended spectr!m & inactivated by beta&lactamase & Gpos
& effective a%ainst
some Gne% AA
& GI distress6 diarrhea
& delayed reactions
& s-in rashes (mac!lopap!lar5!rticaria)
& mac!lopap!lar L StoxicT rxn "5o imm!ne basis
& !rticaria & tr!e ',N hypersensitivity rxn
& acid stabile and
"ell absorbed via
=I
Amo2icillin
& an aminopenicillin L extended spectr!m & inactivated by beta&lactamase & same as Ampicillin & better tolerated than Ampicillin & better =I
absorption than
Ampicillin
(almost
completely
absorbed)
& food does not
impair absorption
0iperacillin
& an Antipse!domonal ',N L (also has an
extended spectr!m)
& !sef!l in tx of septicemia d!e to
s!sceptible or%anisms in patients "ith
impared imm!ne defenses (%iven "ith an
amino%lycoside)
& inactivated by beta&lactamase & Gpos
& enhanced activity
a%ainst select Gne%
(esp 'se!domonas)
& 0arentall%
(inactivated by
%astric p)
Cla4ulonic
acid 7
beta$lactam
a&ent
& (lav!lanic acid inhibits beta&lactamase
b!t has no intrinsic anti&microbial activity A
& "hen %iven "ith a ',N the spectr!m of
',N is extended
& note/ not all beta&lactamases
are bloc-ed by (lav!lonic acid
& resistance can occ!r by a mech
other than beta&lactamase
prod!ction
& Gpos
& Beta&lactamse
prod!cin% strains of
). a!re!s
& Gne% bacilli
Vancom%cin
& Inhibits peptido&l%can s%nthetase (en:
that extends the cell "all) by bindin% to the
D&ala&D&ala termin!s of disaccharide
b!ildin% bloc-s and bloc-in% their addition
to the %ro"in% peptido%lycan strands
& note/ this is not a Beta&lactam antibiotic
& 'lasmid&mediated
modification of D&ala&D&ala to
D&ala&D&lactate "hich can be
incorporated into the
peptido%lycan stands L this
doesnBt affect str!ct!ral
inte%rity of the cell "all
& Gro"in% n!mber of ;(
resistant strains of ,nterococci
and #4)A
& Gpos
Incl!din%/
& #4)A
& )trep pne!moniae
strains resistant to
beta&lactams
& GreP!ent/ Thrombophlebitis8 chills and feber
& .totoxic L esp in lar%e5contin!o!s doses6 in the presence of renal
dama%e or in the elderly L esp if co&administered "ith another ototoxic
dr!%
& ne!tropenia6 renal dama%e
& #onitor renal and a!ditory f!nction !se.
& ,xcreted via -idney & =i4en IV( not
absorbed orall%.
& %iven orally to
tx (. dificile
1
Antibiotic
(classification)
Mechanism Resistance
Antibacterial
Spectrum
Side Eects Metabolism
!istribution
Adm" # CNS
Ciprolo2acin
(fl!oroP!inolone)
Inhibit DNA Gyrase and Topoisomerase #!tation in Gyrase
,ffl!x
Gram Ne%
Gram 'os not some anaerobes
#ycobacteria
Inhibit GABA
(N) effects
4,NA$ .ral (N) ,GG,(T)
Norlo2acin
(fl!oroP!inolone)
Inhibit DNA Gyrase and Topoisomerase #!tation in Gyrase
,ffl!x
Gram Ne%
'oor tiss!e penetration
9TI only
Inhibit GABA
(N) effects
4,NA$ .ral (N) ,GG,(T)
Nitrourantoin
(!nrinary
antiseptic)
9n-no"n
DNAU
.xy%en free radicalU
)lo" resistance
4are
Gram 'ost
Ge" Gram Ne%
Not 'se!domonas or 'rote!s
Bro"n 9rine
Na!sea and ;omitin%
'!lmonary Gibrosis
4,NA$ .ral
Methenamine
(!rinary
antiseptic)
Decomoses at p V1.1 to
G.4#A$D,3D,
4are #ost Bacteria
,xcept !rease splittin% bacteria
ie. 'rote!s
Toxic to GI
Bladder irritation
4,NA$ .ral
>
;luoro>uinilones and Drinar% Antiseptics'
Amino&l%cosides'
Tetrac%clines'
Antibiotic
(classification)
Mechanism Resistance
Antibacterial
Spectrum
Side Eects Metabolism
!istribution
Adm" # CNS
=entamicin
Inhibit +2) Decrease 9pta-e Gram Ne%
)yner%y "ith Beta $actams
.totoxic
Nephrotoxic
;estib!lar
4,NA$ I;
Neom%cin
Inhibit +2) +2) m!tation
4arely active a%ainst Gram 'os
T.'I(A$ .4
INT,)TINA$ G$.4A
Too nephrotoxic for
parenteral
Intestinal #alabsorption
(not absorbed "ell)
Geces T.'I(A$
.4A$ for red!cin%
intestinal flora
Streptom%cin
Inhibit +2) Decrease 9pta-e
,xtensive 4esistance
4arely !sed b!t for TB
TB .totoxic
Nephrotoxic
;estib!lar
4,NA$ I;
Ami:acin
Inhibit +2) Decrease 9pta-e Gram Ne%
)yner%y "ith Beta $actams
'otent a%ainst 'se!domonas
.totoxic
Nephrotoxic
;estib!lar
4,NA$ I;
N
Miscellaneous Anti$Bacterial !ru&s'
Antibiotic
(classification)
Mechanism Resistance
Antibacterial
Spectrum
Side Eects Metabolism
!istribution
Adm" # CNS
Chloramphenicol
binds 12 ) and
inhibits peptidyl
transferase no
protein elon%ation
'lasmid ma-es (AT
(cholrampenicol
acetyl transferase)
acetylation
inactivation
Ne4er irst choice6
b!t !sed for
salmonella6 h. fl!
(menin%ial inf.) and
GN aerobes that
ca!se brain abscesses
4apid and complete
absorption6 especially
to (N)6 inhibits p0126
ca!ses hepatic
ins!fficeintcy
,xcreted M2I as
non&toxic
%l!c!ronide by
t!b!lar secretion6
*2I as parent
dr!%
.phthalmic
sol!tion and
ointment
3es L !sed
for treatment
of menin%ial
infections and
brain abcesses
Er%throm%cin
)EM/
Binds $*1 protein
of 12) and bloc-s
translocation from
the A site to the '
site
'lasmid/
methylation6 decrease
permeability6
hydrolysis by
esterases
(hromosomal/
alternation of 12s
protein at ,#&
bindin% site
*. corny infections
7. chlamydial
infections
+. (A pne!monia
Gram positives
(pneumococci* strep*
staph and corny)8
pne!monia from
myco and le&ionella
Abdominal crampin%6
increase stomach
motility6 cholestatic
hepatitis6 ototoxicity
Activity
enhanced at
al-aline p8
absorption
inhibited by
food8
concentrated in
liver and
excreted in bile
.rally or
parentally
(I; as ,#
%l!ceptate
or ,#
lactobionate
)
No
Clarithrom%cin
Binds $*1 protein
of 12) and bloc-s
translocation from
the A site to the '
site
'lasmid/
methylation6 decrease
permeability6
hydrolysis by
esterases
(hromosomal/
alternation of 12s
protein at ,#&
bindin% site
(ombo therapy for
AID)6 #A( (myco
avium)6 strep and
myco and le&ionella
pne!monia
GI probs6 inhibits p0126
terato%enic
More stable to
acid than EM(
lon&er hal lie
than ,#
t"ice daily
dosin%8
metaboli:ed in
liver6 excreted
by -idney
.rally No
A*ithrom%cin
Binds $*1 protein
of 12) and bloc-s
translocation from
the A site to the '
site
'lasmid/
methylation6 decrease
permeability6
hydrolysis by
esterases
(hromosomal/
alternation of 12s
protein at ,#&
bindin% site
(ombo therapy for
AID)6 #A(* strep6
myco and le&ionella
pne!monia6
chlamydia
GI6 reversible hearin%
loss "hen !sed to treat
#A(
No inhibition o p-9C
.nce daily
dosin%( no dru&$
dru&
interactions
orally No
Tetrac%cline
Inhibit +2) at A& )ite Decrease 9pta-e
Increase ,GG$9W
#!tation +2)
Gram 'os
Gram Ne%
GI
BROWN TEETH
)!perinfection
4ed!ce bioavail. .f .ral
(ontraceptives
(a ion6 antacids and food
Inhibit absorption
.4A$
!o2%c%cline
Inhibit +2) at A& )ite Decrease 9pta-e
Increase ,GG$9W
#!tation +2)
Gram 'os
Gram Ne%
GI
4ed!ce bioavail. .f .ral
(ontraceptives
(a ion6 antacids and food
Inhibit absorption
#ore $ipid sol!ble
$o" renal clearance
.4A$
Minoc%cline
Inhibit +2) at A& )ite Decrease 9pta-e
Increase ,GG$9W
#!tation +2)
Gram 'os
Gram Ne%
GI
Vestibular
4ed!ce bioavail. .f .ral
(ontraceptives
(a ion6 antacids and food
Inhibit absorption
#ore $ipid sol!ble
$o" renal clearance
Retained in lipids and CNS
.4A$
X
Clindam%cin
)CAM/
Binds $*1 protein
of 12) and bloc-s
translocation from
the A site to the '
site
'lasmid/
methylation6 decrease
permeability6
hydrolysis by
esterases
(hromosomal/
alternation of 12s
protein at ,#&
bindin% site
Anaerobic infections
(b. fra&ilis)* staph
and strep
'rophylaxis of
endocarditis "5
valv!lar heart
disease8 penetratin%
"o!nds
pse!domembrano!s
colitis (c. difficile)
Absorbed in
liver
.rally and
parentally
No
Metronida*ole
)MTN/
In anaerobes6
bacterial
nitrored!ctase
forms red!ced
#TN "hich
disr!pt bacterial
DNA
$o" nictrored!ctase
lo" red!ced #TN
red!ced bacterial
disr!ption
$. +iardiasis*
,mebiasis*
Trichomoniasis-
7. Anaerobic
infections (b.
fra&iles)
+ pse!domembrano!s
colitis from c.
difficile
Metallic taste6 na!sea6
headache6
dar: reddish$bro+n
urine(
inhibits p012
#etaboli:ed by
liver
oral 3es
Aine*olid
Binds 7+) of 12)
and prevents
formation of
f!nctional N2)
4are/ m!tation of
bindin% site
Aast resort
treatment for
vancomycin&resistant
enterococcus* staph
and strep (%ram <Bs)
Diarrhea6 na!sea(
not or pts +ith 0<D(
doesn5t inhibit p-9C(
fatal if ta-en "ith
tyramine (inhibits
monoamine oxidase)6
administer
pse!dophedrome and
))4IBs "ith ca!tion
#etaboli:ed by
liver
.rally
(s!spension
"ith
phenylalani
ne) and
parentally
S%nercid
)8C.Euinupristin #
FC.!alopristin/
Y!in!pristin binds
the 12)6
Dalfopristin binds
nearby and
enhances bindin%
protein
synthesis inhibition
#odification of
P!ni!pristin bindin%
site (#$)&B type)
vancomycin&resistant
enterococcus
faecium (not
faecalis)*
staph and strep
(%ram <Bs)
'ain6 inflammation6
arthral%ias6 myal%ias6
increased conH!%ated
bilir!bin6
pse!domembrano!s
colitis
#etaboli:ed by
liver
I;
M
Alcohol and Related !ru&s'
Antibiotic
(classification)
Acute 0h%sical
Eects#Mech
Chronic Eects
!ru&
Interactions
Metabolism
CNS
Ethanol
Beha4ioral
& )edation6 inhibition loss6 impaired H!d%ment6 sl!rred
speech6 ataxia
12&X2 m%5d$ drivin% impairment
*72&*>2 m%5d$ dr!n-enness
O122 m%5d$ death
0eripheral Eects
& cardiac fcn6 relaxes vasc!lar (and !terine) smooth
m!scle vasodilation6 hypothermia
& hypo%lycemic action of s!lphonyl!reas and
antiplatelet action of aspirin
Central Eects
$ =ABAA receptor L a li%and %ated ion channel ((l
&
)
& conc ,t. effects of maHor inhibitory
ne!rotransmitter (GABA)
$ =lutamate responses (N#DA rec) are inhibited by
,t. ne!ronal excitability
& ,xcitation mediated by 9$HT8 serotonin rec
emetic response (na!sea5vomitin%)

Tolerence
& #etabolic ('harm -inetic) L ind!ction of metabolic en:
expression
& G!nctional ('harm Dyn) L red!ction of the (N) sensivity to
adaptive chan%es in ne!rons
& (ross&tolerance to other sedative&hypnotic dr!%s
& 'hysical dependance
0eripheral
& $iver/ hypo%lycemia F fat acc!m!lation (NAD depletion)6
liver dama%e6 '012 en:
& GI/ irritation6 scarin% of %!t absorption deficits
& ,ndocrine/ Gynecomastia6 testic!lar atrophy6 salt retention 7
to altered steroid met in cirrhotic liver
& (;/ TTN6 anemia6 #I
& Neoplasia/ ,t. not a * carcinogen, but coincidence of
carcinomas
Ner4ous s%s
& most common K 'eripheral ne!ropathies
& less often L thiamin def. Wernic:e$<orsa:o syn (ataxia6
conf!sion6 paralysis of ,.#) L tx "5 I; thiamine to prevent
brain dama%e
$ ;AS & terato%enic
Acute
& s!bstrate for '012 th!s competes "ith
other dr!%s
& if %iven a dr!% that is (N) dependant
and met. via '012 s!per&additive effect
Chronic
& ind!ces '012 en: L esp 0-9C @E?
accelerates dr!% met
& 7,* formation of toxic
metabolites of certain dr!%s
(acetaminophen) hepatotoxicity
Absorption
& rapidly and completely absorbed
A!H L cytosolic NAD dependant en:
& in liver and %!t (men O "omen)
& :ero order -inetics (max capacity K N&*2 %5h)
Microsomal ethanol o2idi*in& s%stem (#,.))
& '012 liver en: only -ic-s in at blood ,t. levels O
2.*I
& increases "ith chronic expos!re to ,t.
& responsible for development of metabolic tolerance
3es
Methanol
;is!al dysf!nction6 GI distress6 shortness of breath6 loss of
conscio!sness

Tx "ith ,t.5'omepi:ole L ,t. is the
preferred s!bstrate for AD and
competitively inhibits the ox of #e.
(an be metaboli:ed to formaldehyde acidosis6 retinal
dama%e6 blindness
Eth%lene &l%col
Antifree:e L acidosis F renal dama%e Tx "ith ,t.5Gomepi:ole #et .xalic acid
Naltre2one
.pioid anta%onist L red!ces cravin% via effects of
endo%eno!s opioid peptides
4ed!ces the re"ardin% effects of ,t.
(an ca!se severe "ithdra"al in an opioid dependant pat L do a
Narcan challen%e before prescription
!ia*epam
Clonidine
!isuliram
& Inhibits Aldehyde D
& concentration of Acetaldehyde if ,t. is ta-en
& Acetaldehyde b!ild!p ca!ses na!sea6 vomitin%6 liver
dama%e
& Eor-s via aversion
& !sef!l "ith "ell motivated alcoholics
;omepi*ole
Inhibits AD L !sed as an antidote for #e. or ,thylene
%lycol poisonin% L it prevents the formation of their toxic
metabolites
*2