Antibacterial Pharmacology
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Subject: microbiology
54 terms | 155 facts
USMLE Step 1: Microbiology
Antibacterial Parmacology
!ifampin is
propyla"is for#
$nfection: meningococcal infection %cil&ren'
(ral penicillin is
propyla"is for#
$nfection: cil& )it prior reumatic fe*er+ must ta,e &aily
-ancomycin .o"icity: neproto"icity+ ototo"icity+ tromboplebitis+ se*ere
/using )en infusion too rapi&
clinical use: M!SA+ 01 2i3
resistance: if bacteria mutates 425ala 25ala4 to 425ala 25lac4
mecanism: bin&s 25ala 25ala part of cell )all precursors to
inibit pepti&oglycan formation
Ami,acin 0lass: aminoglycosi&e
clinical use: gram negati*e ro&s
mecanism: inibits 67S at te formation of te initiation
comple"
resistance: bacterial transferase →
acetylates8posporylates8a&enylates te &rug
to"icity: neproto"icity+ inibits 9M:+ ototo"icity+ teratogenicity
.obramycin 0lass: aminoglycosi&e
clinical use: gram negati*e ro&s
mecanism: inibits 67S at te formation of te initiation
comple"
resistance: bacterial transferase →
acetylates8posporylates8a&enylates te &rug
to"icity: neproto"icity+ inibits 9M:+ ototo"icity+ teratogenicity
0efepime Mecanism: inibits cell )all syntesis
clinical use: serious infections )it resistance+ inclu&ing
pseu&monas+ gram negati*e+ an& gram positi*es %broa&5
spectrum'
to"icity: allergic reaction+ *it ; &e<ciency+ neproto"icity
class: 4t5generation cepalosporin
0lorampenicol .o"icity: aplastic anemia+ gray baby syn&rome
clinical use: =n& line for meningitis secon&ary to >1 $n/uen?ae+
91 Meningiti&is+ S1 Pneumoniae
mecanism: bloc,s protein cain elongation by inibiting
pepti&yl transferase at te 57S subunit
resistance: acetyltransferase pro&uce& by bacteria pre*ents
bin&ing of &rug to ribosomes
2o"ycycline 0lass: tetracycline
to"icity: teet &iscoloration+ potosensiti*ity+ acilles ten&on
rupture+ interference )it bone8ten&on gro)t
clinical use: !MS@+ mycoplasma+ clamy&ia
mecanism: bin&s 67S an& pre*ents attacment to aminoacyl5
t!9A
resistance: bacterial transport pumps &ecrease upta,e or
increase eAu" of te &rug
5@lo"acin+ eno"acin+
nali&i"ic aci&
Mecanism: inibit topoisomerase $$ %29A gyrase' an& $-
clinical use: U.$s+ pyelonepritis+ pseu&omonas
to"icity: acilles ten&on rupture especially in pts B C7+ organ
transplant recipients+ an& pts ta,ing corticosteroi&s+
contrain&icate& in pregnancy+ periperal neuropaty+ ten&initis
an& cartilage &amage in cil&ren+ prolongation of D. inter*al
resistance: eAu" pumps+ mutate& topoisomerase $$ %29A
gyrase'
class: /uoroEuinolone
M1 a*ium5
intracellulare
Propyla"is: a?itromycin %024 F 57'
treatment: a?itromycin+ rifampin+ etambutol+ streptomycin
.icarcillin+ piperacillin .o"icity: allergic reaction
class: anti5pseu&omonal penicillin
clinical use: pseuo&omonas %combine )it cla*ulanic aci& or
ta?obactam'
mecanism: bloc,s pepti&oglycan cross5lin,ing+ acti*ates
autolytic en?ymes+ bin&s transpepti&ases
.riple terapy for >1
pylori
2rugs: amo"icillin+ PP$+ claritromycin
Ampicillin+ amo"icillin .o"icity: allergy+ pseu&omembranous colitis %01 2iGcile'
resistance: beta5lactamases
clinical use: >1 Pylori+ >1 $n/uen?ae+ E1 0oli+ Listeria+ Proteus+
Salmonella+ Sigella
mecanism: bloc,s pepti&oglycan cross5lin,ing+ acti*ates
autolytic en?ymes+ bin&s transpepti&ases
Penicillin !esistance: beta5lactamases
clinical use: gram positi*es+ 91 Meningi&itis+ sypilis
to"icity: allergic reaction+ emolytic anemia %rare'
mecanism: bloc,s pepti&oglycan cross5lin,ing+ acti*ates
autolytic en?ymes+ bin&s transpepti&ases
9eomycin 0lass: aminoglycosi&e
clinical use: gram negati*e ro&s
mecanism: inibits 67S at te formation of te initiation
comple"
resistance: bacterial transferase →
acetylates8posporylates8a&enylates te &rug
to"icity: neproto"icity+ inibits 9M:+ ototo"icity+ teratogenicity
$mipenem8cilastatin+
meropenem
.o"icity: 09S to"icity
mecanism: H5lactams+ cilastatin inibits renal &ey&ropeptiase
$ to pre*ent neproto"icity
clinical use: last5resort )en oter &rugs a*e faile&1 Hroa&5
spectrum
class: carbapenem
Sulfameto"a?ole
%SMI'+ sul<so"a?ole+
sulfa&ia?ine
0lass: sulfonami&e
clinical use: U.$+ streptococcus+ M!SA+ E1 0oli+ >1 $n/uen?ae
to"icity: emolysis in JCP2 &e<ciency+ neproto"icity+ many
people a*e sulfa allergies+ ,ernicterus in babies
resistance: mo&i<e& bacterial &iy&ropteroate syntase+
increase PAHA syntesis %o*ercome competiti*e inibition'+
&ecrease& &rug upta,e
mecanism: competiti*e antagonist of PAHA → inibits
&iy&ropteroate syntetase →→ &ecrease& syntesis of .>@ →
&ecrease& 29A syntesis
0ipro/o"acin is
propyla"is for#
$nfection: meningococcal infection %a&ults'
Heta5lactamase
inibitors
0la*ulanic aci&+ sulbactam+ ta?obactam
!ifabutin 0linical use: .H treatment in >$-K patients %less P5457 in&uction'
Etambutol Mecanism: inibits arabinosyltransferase )ic bloc,s
carboy&rate polymeri?ation in te cell )all
to"icity: optic neuritis
clinical use: .H
0eftria"one+
cefota"ime+
cefta?i&ime
Mecanism: inibits cell )all syntesis
clinical use: gram negati*e infections+ ceftria"one &rug of coice
for 09S infections %meningitis' an& gonorrea+ cefta?i&ime for
pseu&omonas
to"icity: allergic reaction+ *it ; &e<ciency+ neproto"icity
class: 6r&5generation cepalosporin
Metroni&a?ole .o"icity: &isulfuram reaction )8 eto+ metallic taste
mecanism: free ra&icals tat &amage bacterial 29A
clinical use: Jiar&ia+ Entamoeba+ .ricomonas+ Jar&nerells
*aginalis+ Hacteroi&es+ 01 2iGcile+ >1 Pylori
Propyla"is Penicillin J is propyla"is for# $nfection: sypilis
ampicillin is propyla"is for# $nfection: maternal group H strep
>$- )8 024 F 177 propyla"is: .MP5SMI for P0P pneumonia an&
to"oplasmosis
M1 .uberculosis propyla"is: isonia?i& %$9>'
treatment: rifampin+ isonia?i& %$9>'
2emeclocycline 0lass: tetracycline
mecanism: A2> antagonist+ also bin&s 67S an& pre*ents
attacment to aminoacyl5trna
resistance: bacterial transport pumps &ecrease upta,e or
increase eAu" of te &rug
clinical use: S$A2>
to"icity: teet &iscoloration+ potosensiti*ity+ acilles ten&on
rupture+ interference )it bone8ten&on gro)t
Pyra?inami&e Mecanism: &ecreases intracellular p
to"icity: yperuricemia+ epatoto"ic
clinical use: .H
0efa?olin+ cepale"in Mecanism: inibits cell )all syntesis
clinical use: Proteus+ E1 0oli+ ;lebsiella+ S1 Aureus %prior to
surgery'
to"icity: allergic reaction+ *it ; &e<ciency+ neproto"icity
class: 1st5generation cepalosporin
.etracycline 0lass: tetracycline
to"icity: teet &iscoloration+ potosensiti*ity+ acilles ten&on
rupture+ interference )it bone8ten&on gro)t
clinical use: !MS@+ mycoplasma+ clamy&ia
mecanism: bin&s 67S an& pre*ents attacment to aminoacyl5
trna
resistance: bacterial transport pumps &ecrease upta,e or
increase eAu" of te &rug
!ifampin 0linical use: .H+ leprosy+ 91 Meningi&itis propyla"is in close
contacts+ >1 $n/uen?ae type H propyla"is in close contacts
to"icity: P5457 in&ucer+ re&8orange bo&y /ui&s
mecanism: inibits 29A5&epen&ent !9A polymerase
resistance: rapi& resistance if use& by itself
Erytromycin
ointment is
propyla"is for#
$nfection: optalmia neonatorum
.rimetoprim %.MP' 0linical use: combine to form .MP5SMI )ic is use& for utis+
P0P pneumoniae treatment an& propyla"is+ sigella+ salmonella
to"icity: megaloblastic anemia %secon&ary to .>@ inibition'
mecanism: inibits bacterial &iy&rofolate re&uctase %2>@!'
Minocycline 0lass: tetracycline
to"icity: teet &iscoloration+ potosensiti*ity+ acilles ten&on
rupture+ interference )it bone8ten&on gro)t
clinical use: !MS@+ mycoplasma+ clamy&ia
mecanism: bin&s 67S an& pre*ents attacment to aminoacyl5
trna
resistance: bacterial transport pumps &ecrease upta,e or
increase eAu" of te &rug
Penicillin is
propyla"is for#
$nfection: en&ocar&itis )it upcoming surgical8&ental proce&ures
0lin&amycin .o"icity: 01 2iGcile %pseu&omembranous colitis'
mecanism: bloc,s transpepti&ation at 57S subunit
clinical use: anaerobic infections in te upper an& lo)er
respiratory tracts
Streptomycin 0lass: aminoglycosi&e
clinical use: gram negati*e ro&s
mecanism: inibits 67S at te formation of te initiation
comple"
resistance: bacterial transferase →
acetylates8posporylates8a&enylates te &rug
to"icity: neproto"icity+ inibits 9M:+ ototo"icity+ teratogenicity
A?treonam 0linical use: gram negati*e ro&s1 @or penicillin5allergic patients
mecanism: inibits pepti&oglycan "5lin,e& by bin&ing pbp6
class: monobactam
to"icity: Lgi upset
-ancomycin is &rug of
coice for#
$nfection: M!SA
0efa?olin is
propyla"is for#
$nfection: postsurgical S1 Aureus inf"n
.MP5SMI is
propyla"is for#
$nfection: recurrent utis
0efo"itin+ cefaclor+
cefuro"ime
Mecanism: inibits cell )all syntesis
to"icity: allergic reaction+ *it ; &e<ciency+ neproto"icity
class: =n&5generation cepalosporin
clinical use: >1 $n/uen?ae+ Enterobacter+ 9eisseria+ Proteus+ E1
0oli+ ;lebsiella+ Serratia
Jentamicin 0lass: aminoglycosi&e
clinical use: gram negati*e ro&s
mecanism: inibits 67S at te formation of te initiation
comple"
resistance: bacterial transferase →
acetylates8posporylates8a&enylates te &rug
to"icity: neproto"icity+ inibits 9M:+ ototo"icity+ teratogenicity
>$- )8 024 F =77 Propyla"is: .MP5SMI for P0P pneumonia
("acillin+ nafcillin+
&iclo"acillin
0lass: anti5stap penicillins
mecanism: bloc,s pepti&oglycan cross5lin,ing+ acti*ates
autolytic en?ymes+ bin&s transpepti&ases1 $s beta5lactamase
resistant1
to"icity: allergic reaction+ interstitial nepritis
clinical use: s1 Aureus
A?itromycin+
claritromycin+
erytromycin
0lass: macroli&es
to"icity: &iarrea+ nausea+ ab&ominal pain+ colestatic epatitis
%rare'+ prolonge& D. → torsa&es %*ery rare'
clinical use: atypical pneumonia+ clamy&ia+ streptococcal
infections %=n& line'
mecanism: bin&s =6S portion of 57S subunit → inibits
translocation &uring protein syntesis
resistance: metylate =6S subunit
Line?oli& is &rug of
coice for#
$nfection: -!E
Mat are te
tetracyclines#
2rugs: tetracycline+ &o"ycycline+ &emeclocycline+ minocycline
$sonia?i& %$9>' Mecanism: con*erte& by bacterial ,atg to acti*e form an&
&ecreases mycolic aci& syntesis
clinical use: .H propyla"is an& treatment
to"icity: neuroto"icity %pre*ent )8 *it HC'+ epatoto"icity+ SLE
Mat are te
/uoroEuinolones#
2rugs: cipro/o"acin+ nor/o"acin+ le*o/o"acin+ o/o"acin+
spar/o"acin+ mo"i/o"acin+ gati/o"acin+ eno"acin+ nali&i"ic aci&
0eftria"one is
propyla"is for#
$nfection: gonorrea
Mat are te
aminoglycosi&es#
2rugs: gentamicin+ neomycin+ ami,acin+ tobramycin+
streptomycin
M1 leprae .reatment: &apsone+ rifampin+ K85 clofa?imine %if lepromatous'
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