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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 catalaseperoxidase). It binds to InhA (an enoylacyl carrier protein NAD red!ctase).

InhA is involved in mycolic acidsythesis and hence inhibits cell "allsynthesis.

#!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%eGlossitisGI dist!rbance

Aller%ic rxnN reversed by pyridoxine

(*&+ ho!rs) lon% or short is

%enetically determined (ethnic)Activity of hepatic&N&acetyltransferase 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!nitof 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%eGI dist!rbanceAller%y

(7&1 ho!rs8 deacylation) ,xcreted

in bile and enterohepaticcirc!lation

ral

Dr!% interaction/'012ther dr!% activity("arfarin6 prednisone6contraception6

methadone)

Ethambutol(bacteriostatic) Inhibits arabin o%alactan

sythesis (cell "all). Th is "ea-ens the"all and enhances lipophillic dr!%s li-e4ifampin

9n-no"n T!berc!losis

#AKansasii

ptic ne!ritis

vis!al ac!ityred %reen visionaller%ic rxnexacerbate %o!t6 b!t less than

pyra:inamide

(0 ho!rs) !nchan%ed

-idney

oral

0%ra*inamide(bactericidal) 9n-no"nydroly:ed into its active form6

pyra:inoic acid. Tho!%ht to tar%et fattyacid synthase I6 "hich converts%lycolipid to mycolic acid. ence6 thecell "all is affected

$oss of pyra:in amidase action6"hich activates pyra:inamide.

'enetrates the macropha%elysosome beca!se it operates best

at lo" pT!berc!losis

$iver dama%eGI dist!rbance

,xacerbates %o!t more thanethamb!tol

Kidney ral

Streptom%cinInhibits bacterial protein synthesis by

bindin% to ribosomes

'oint m!tation in ribosome 'oor diff!sion across plasma

membrane. ence6 it only affectsextracell!lar t!berc!losis.

;estib!lar f!nctionearin% loss

Aller%ic rxn4ash4enal dama%e

(+ ho!rs) 9nchan%ed

Kidney

I#

Riabutin(bactericidal) Inhibits initiation of

transcription by bindin% to the s!b!nitof bacterial 4NA polymerase

#!tation of 4NA polymerase

res!ltin% in affinity or permeability

Atypical mycobacteri!m that

affects I; &*2 days in anephric pt.8not removed by hemodialysis.

I;

If %iven rapidly6ca!ses fl!shin%(histamine release).

C%loserine)inhibits cell +all

s%nthesis/

Inhibits ala "acemase (prevents $&ala

D&ala) andDala Dala 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!sion6coma)7. 'eripheral ne!ritis.

+. $iver dama%e.0. olate 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 cellmembrane..

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 2 initiationcomplex to form b!t inhibits it frommovin% alon% m4NA. 7. prevents

peptide elon%ation (prevents bindin% of

aminoacyl t4NA) +. disr!pts bacterialcell membrane*selectivity= %s only in bacteria

*. #!tation in *7 protein in +2

s!b!nit7. '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) Oototo2icit% (deafness).7. Nephroto2icit%"+. M%oneural bloc:ade

rare0. 4ash5fever post parenteraladministration.

No metabolism.

,xcretion by %lomer!lar filtration.

T J 7 hrs. ("5 renal dx F a%e)

adH!st dose.elective acc!m!lation in 'T of-idney6 endo F perilymph of haircells.

$imited F slo" oral

absorption.#!st be %iven

parenteral (I;) inC#.Acc. in ple!ral6

pericardial6 synovialfl!ids F fet!s.

$ittle

penetration.

*

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!apsone

'ABA a%onist. ence6 folic acid

biosynthesis is bloc-ed. 'rod!ction ofmethionine6 serine6 p!rines6 and N formlmet 4NA are inhibited

C'ABA,n:yme m!tation

$eprae 4ash

emolytic anemiaGI dist!rbance$iver dama%e

'eripheral ne!ropathy

,limiated in free form and

%l!c!ronideKidney

ral

Cloa*imine

Binds to DNA and inhibits templatef!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 derivativeIt has anti&inflammatory and imm!no&mod!latin% effects

Ne" ,rethema

Nodos!m lepros!m$eprae

Terato%en

'eripheral ne!ropathyedationonstipation

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 membraneand ma-es a pore that allo"s ionic fl!xand cell lysis

4are 9sef!l a%ainst all f!n%i6 b!t !selimited to systemic'ro%ressive infections

$ife threatenin% infectionAsper%ill!s

Ac!te febrile rxn !poninf!sion4enal dama%e

A:otemiaypo-alemiaThrombophlebitisAnorexia

M2 protein bo!nd lo" I; No

N%statin

(polyene)

Binds to er%osterol of the cell membraneand ma-es a pore that allo"s ionic fl!xand cell lysis

4are !perficial mycosis#ostly candida

Aller%ic rxnGI dist!rbance

Topical No

;luc%tosine

(pyrimidine)

Deaminated by cytosine deaminase to 1

fl!oro!racil and anaboli:ed into an!cleotide6 1&d9#' or 1&9T'. Then!cleotide binds to thymidilatesynthetase and deprives the cell of

thymidilic acid6 an essential DNAcomponent. 1 &9T' incorporates into4NA and disr!pts n!cleic acid and

protein synthesis.

$oss of cytosine permease

9#' phophorlyase or cytosine deaminase

rytococc!s Neoformans

ome candidahromobastomycosis(dermitacio!s mold)

Intestinal conversion to

fl!oro!racil ca!ses bonemarro" toxicity6 le!-openia6thrombocytopeniaGI dist!rbance

9nchan%ed

Kidney

ral 3es

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Clotrima*ole

(imida:ole)

(!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 themembrane permeability and f!nction.

!perficial mycosis ,rythema

'r!ritisB!rnin%GI irritation

Topical

ral

Anti$;un&al A&ents' )continued/


Mechanism ResistanceAntibacterial

SpectrumSide Eects Metabolism

!istribution

Adm" # CNS

Micona*ole

(imida:ole)

(!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 themembrane permeability and f!nction

!perficial mycosis B!rnin%

Irritation

Topical

;lucona*ole

(tria:ole)

(!n%icidal) 4ed!ction of er%osterolsynthesis by inhibition of f!n%al '012.


ral and esopha%eal candidiasis!perficial mycosis ("idest of

a:oles)ryptococcal menin%itisDimorphic f!n%i

Q side effects than imida:oleNo interaction "ith liver

en:ymeGIypo-alemia

,demaypertension

9nchan%edKidney

ralI;

3es

Itracona*ole

(tria:ole)

(!n%icidal) 4ed!ction of er%osterolsynthesis by inhibition of f!n%al '012.


Dimorphic/ blastomycosis6histoplasma6 sporothrix#ost potent of tria:ole6 b!t

bioavailability Q "th rifampin

Asper%ill!sDermatophytosis

nchomycosis

Interat "ith some hepaticen:ymesGIypo-alemia

,demaypertension

$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 mycosisR* dermatophyte

nchomycosis

Irritation Topical

=riseoul4in

(%risan)

#ytotic inhibitorBinds to microt!b!les to bloc- assemblyand f!nction

!perficial mycosis GI dist!rbanceAller%ic rxn'hotosensitivityInd!ce '012. o"ever6 it

tar%ets -eratin cells andeffects are minimaleadache

$iver,xcreted in feces and !rine

ral

0entamidine

'ne!mocystic carinni pne!moniaBlastomycosis

Ato4a>uone

'ne!mocystic carinni pne!moniaBlastomycosis

+

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0

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Cell Wall Inhibitors'



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 theen: and inhibitin% it@/activates endo%eno!s a!tolytic en:ymemurein h%drolase "hich de%rades the cell

"all f!rther

Beta$lactamase

& hydroly:es the beta&lactambond& most common esp in Gpos& Gpos secrete o!tside cell "all

& Gne% -eep in periplasmicspace!ecreases perm to 0EN

& Gne% can chan%e the porin so

it dosent let ',N inAlterations in 0B0s!ch asalterin% the transpeptidases L ex

is #4A

Narro" pectr!m

& 'rimarily activea%ainst =pos

aerobesandanaerobes

o+ 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

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!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 GABAN effects

4,NA$ ral N ,,T

Norlo2acin

(fl!oroP!inolone)

Inhibit DNA Gyrase and Topoisomerase #!tation in Gyrase,ffl!x

Gram Ne%'oor tiss!e penetration

9TI only

Inhibit GABAN effects

4,NA$ ral N ,,T

Nitrourantoin

(!nrinaryantiseptic)

9n-no"n

DNAUxy%en free radicalU

lo" resistance

4are

Gram 'ost

e" Gram Ne%

Not 'se!domonas or 'rote!s

Bro"n 9rine

Na!sea and ;omitin%'!lmonary ibrosis

4,NA$ ral

Methenamine(!rinary

antiseptic)

Decomoses at p V1.1 to

4#A$D,3D,

4are #ost Bacteria

,xcept !rease splittin% bacteriaie. 'rote!s

Toxic to GI

Bladder irritation

4,NA$ ral

>

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;luoro>uinilones and Drinar% Antiseptics'

Amino&l%cosides'

Tetrac%clines'




!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!tation4arely active a%ainst Gram 'os

T'IA$ 4INT,TINA$ $4A

Too nephrotoxic forparenteral

Intestinal #alabsorption(not absorbed "ell)

eces T'IA$

4A$ for red!cin%intestinal flora

Streptom%cin

Inhibit +2 Decrease 9pta-e

,xtensive 4esistance4arely !sed b!t for TB

TB totoxicNephrotoxic;estib!lar

4,NA$ I;

Ami:acin

Inhibit +2 Decrease 9pta-e Gram Ne%yner%y "ith Beta $actams

'otent a%ainst 'se!domonas

totoxicNephrotoxic

;estib!lar

4,NA$ I;

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Miscellaneous Anti$Bacterial !ru&s'




!istribution

Adm" # CNS

Chloramphenicol

binds 12 and

inhibits peptidyltransferaseno

protein elon%ation

'lasmid ma-es AT

(cholrampenicolacetyl transferase)

acetylation

inactivation

Ne4er irst choice6

b!t !sed forsalmonella6 h. fl!

(menin%ial inf.) and

GN aerobes that

ca!se brain abscesses

4apid and complete

absorption6 especiallyto N6 inhibits p0126

ca!ses hepatic

ins!fficeintcy

,xcreted M2 as

non&toxic%l!c!ronide by

t!b!lar secretion6

*2 as parent

dr!%

phthalmic

sol!tion andointment

3es L !sed

for treatmentof 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

*. cornyinfections

7. chlamydial

infections

+. A pne!monia

Gram positives

(pneumococci strep

staphand corny)8

pne!monia frommycoandle&ionella

Abdominal crampin%6

increase stomach

motility6 cholestatic

hepatitis6 ototoxicity

Activity

enhanced at

al-aline p8

absorption

inhibited by

food8

concentrated in

liver andexcreted in bile

rally or

parentally

(I; as ,#

%l!ceptate

or ,#

lactobionate

)

No

Clarithrom%cin Binds $*1 proteinof 12 and bloc-s

translocation from

the A site to the '

site

'lasmid/


permeability6

hydrolysis by

esterases

hromosomal/

alternation of 12s

protein at ,#&

bindin% site

ombo therapy for

AID6 #A (myco

avium)6strepand

mycoand 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-stranslocation from

the A site to the '

site

'lasmid/

methylation6 decreasepermeability6

hydrolysis by

esterases

hromosomal/

alternation of 12s

protein at ,#&

bindin% site

ombo therapy for

AID6 #A strep6mycoand le&ionella

pne!monia6

chlamydia

GI6 reversible hearin%

loss "hen !sed to treat#A

No inhibition o p-9

nce daily

dosin%( no dru&$dru&

interactions

orally No

Tetrac%cline

Inhibit +2 at A& ite Decrease 9pta-eIncrease ,$9W

#!tation +2

Gram 'osGram Ne%

GIBROWN TEETH

!perinfection

4ed!ce bioavail. f ral

ontraceptives

a ion6 antacids and foodInhibit absorption

4A$

!o2%c%cline

Inhibit +2 at A& ite Decrease 9pta-eIncrease ,$9W#!tation +2

Gram 'osGram Ne%

GI

4ed!ce bioavail. f ralontraceptives


#ore $ipid sol!ble

$o" renal clearance

4A$

Minoc%cline

Inhibit +2 at A& ite Decrease 9pta-eIncrease ,$9W

#!tation +2

Gram 'osGram Ne%

GI

Vestibular

4ed!ce bioavail. f ral

ontraceptives


#ore $ipid sol!ble$o" renal clearance

Retained in lipids and CNS

4A$

X

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Clindam%cin

)CM/

Binds $*1 protein

of 12 and bloc-s

translocation from

the A site to the '

site

'lasmid/


permeability6

hydrolysis by

esterases

hromosomal/

alternation of 12s

protein at ,#&

bindin% site

Anaerobic infections

(b. fra&ilis) staph

andstrep

'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

ine*olid

Binds 7+ of 12

and prevents

formation off!nctional 2

4are/ m!tation of

bindin% site

ast resort

treatment for

vancomycin&resistantenterococcus staph

andstrep (%ram

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Alcohol and Related !ru&s'


Acute 0h%sical

Eects#MechChronic Eects

!ru&

InteractionsMetabolism CNS

Ethanol

Beha4ioral

& edation6 inhibition loss6 impaired H!d%ment6 sl!rredspeech6 ataxia

12&X2 m%5d$ drivin% impairment

*72&*>2 m%5d$ dr!n-enness O122 m%5d$ death0eripheral Eects

& cardiac fcn6 relaxes vasc!lar (and !terine) smoothm!scle vasodilation6 hypothermia& hypo%lycemic action of s!lphonyl!reas and antiplatelet action of aspirin

Central Eects

$ =ABAAreceptorL a li%and %ated ion channel (l&)

& conc ,t effects of maHor inhibitoryne!rotransmitter (GABA)

$ =lutamateresponses (N#DA rec) are inhibited by

,tne!ronal excitability& ,xcitation mediated by 9$HT8 serotonin recemetic response (na!sea5vomitin%)

Tolerence

& #etabolic ('harm -inetic) L ind!ction of metabolic en:expression& !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 %!tabsorption 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 ofcarcinomas

Ner4ous s%s

& most common 'eripheral ne!ropathies

& less often L thiamin def. Wernic:e$

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