Inhibits Cell Wall Synthesis Penicillins (bactericidal: blocks cross linking via competitive inhibition of the transpeptidase enzyme)

Class/Mechanism Penicillin Drugs Penicillin G Aqueous penicillin G Procaine penicillin G Benzathine penicillin G Penicillin Ampicillin Amo#icillin Indications (**Drug of Choice) Strep. pyogenes ( rp.!)!! Step. agalactiae ( rp.")** C. perfringens("acilli)** Above $ % Gram&negative: #. faecalis!! #. Coli!! Toxicity "ypersensitivity reaction "emolytic anemia

Aminopenicillins

Above

Penicillinase-resistantpenicillins

'ethicillin (afcillin )#acillin *lo#acillin +iclo#acillin *arbenicillin -icarcillin Piperacillin

Above $ Above $ P*(ase& ,nterstitial nephritis producingStaph. aureus

Antipseudomonal penicillins

!$o%e & 'seudomonas aeruginosa**

Above

Cephalosporins (bactericidal: inhibits bacterial cell .all synthesis via competitive inhibition of the transpeptidase enzyme) 1st generation *efazolin *ephale#in Staph. aureus** Allergic reaction Staph. epidermidis** *oombs&positive anemia /ome Gram&negatives: (01) #. Coli (le$siella

2nd generation

*efo#itin *efaclor *efuro#ime *eftria#one *efota#ime *eftazidime *efepime (4th generation) ancomycin

Above $ % Gram&negative Above $ % Gram&negative 'seudomonas

Allergic 2eaction 3-)" +isulfiram reaction Allergic 2eaction 3-)" +isulfiram reaction

3rd generation

Other Cell Wall Inhibitors Vancomycin (bactericidal: disrupts peptioglycan cross&linkage) '2/A!! P*(5*eph allegies!! S. aureus S. epidermidis 2ed man syndrome (ephroto#icity )toto#icity

eta-lactamase Inhibitors (bactericidal: blocking cross linking) Carbapenems

*lavulanic Acid /ulbactam -azobactam ,mipenem ($ cilastatin) 'eropenem +oripenem 3rtapenem Aztreonam

S aureus** S epidermis** #.Coli** (le$siella** Broadest activity of any antibiotic (e#cept '2/A6 'ycoplasma) Gram&negative rods Aerobes "ospital&acquired infections -opical Gram&negative infections -opical Gram&positive infections

"ypersensitivity 2eaction "emolytic anemia

A!treonam

Polymy"ins acitracin

Polymy#in B Polymy#in 3 Bacitracin

Protein Synthesis Inhibition

Aminoglycosides (bactericidal: irreversible binding to 07/)

Gentamicin (eomycin Amikacin -obramycin /treptomycin

Aerobic Gram&negatives (ephroto#icity #ntero$acteriaceae )toto#icity 'seudomonas

$etracyclines -etracycline (bacteriostatic: blocks t2(A) +o#ycycline 'inocycline +emeclocycline

)ic*ettsia Mycoplasma Spirochetes (8yme9s disease)

"epatoto#icity -ooth discoloration ,mpaired gro.th Avoid in children : ;< years of age

Anti-%#S ribosomal subunit &acrolides (bacteriostatic: reversibly binds =7/) Overview Bacteria Chloramphenicol (bacteriostatic) 'incosamide (bacteriostatic: inhibits peptidyl transferase by interfering .ith amino acyl& t2(A comple#) 'ine!olid (variable) Streptogramins 3rythromycin Azithromycin *larithromycin *hloramphenicol Streptococcus *oumadin ,nteraction +. influen,ae (cytochrome P4=7) Mycoplamsa pneumonia

+ influen,ae Aplastic Anemia Bacterial 'eningitis Gray Baby /yndrome 0ram Posti1e Cocci Brain absces Staphylococcus "acteroides fragilis /taph? aureus *lindamycin Pseudomembranous '//A colitis S aureus '2/A "ypersensitivity Coagulase-negati%e Staph . Strep /taph? epidermis 2eaction 3#cellent Bone /taph saprophyticus /trep pneumoniae 2esistant Gram& /trep pyogenes (Group A) /trep agalacticae (Group B) positives /trep viridans >uinupristin 23 /trep Bovis (Group +) +alfopristin GA/ and /? aureus skin 2nterococci 3? faecalis (Group + strep) infections 0ram Positi1e acilli ()A Synthesis Inhibitors 8inezolid Streptococcus Penetration

Spore *luoro+uinolones *orming Bacillus anthracis Bacillus cereus (bactericidal: inhibit +(A gyrase enzyme6 inhibiting +(A synthesis) *lostridium tetani (alidi#ic acid Steptococcus Phototo#icity *lostridium botulinum 1st generation Mycoplasma Achilles tendon rupture *lostridium perfringens !ero$ic ram & *lostridium ,mpaired fracture difficile healing )on-Spore *orming *orynebacterium diphtheriae 8isteriaas monocytogenes 2nd generation *iproflo#acin As Above above (orflo#acin $'seudomonas 0ram )egati1e Cocci 3no#acin )eisseria (eisseria meningitidis )flo#acin (eisseria gonorrhoeae 8evoflo#acin 3rd generation ,th generation 0ram )egati1e asacilli As above $ Gram& above positives 3scherichia coli /almonella typhi As above $ Gram& as above /almonella enteridis positives $ anaerobes /higella dysenteriae Other ()A Inhibitors Clebsiella pneumoniae /erratia/eizures 'etronidazole (@lagyl) Anaerobics Proteus*rebelar dysfunction *ampylobacter DeDuni 3-)" disulfram ibrio cholerae reaction ibrio parahaemolyticus5vulnificus -)A Synthesis Inhibitors "elicobacter pylori aeruginosa 2ifampin Staphylococcus Pseudomonas Body fluid discoloration Bacteroides fragilis (.ith ,(") "epato#icity Myco$acterium (-B) Gatiflo#acin 2nterics 'o#iflo#acin Gemiflo#acin "aemophilus influenzae "aemophilius ducreyi &ycolic Acids Synthesis Inhibitors Bordatella pertussis 3oonotic bacilli -B ,soniazidz 8atent -B *olic acid Synthesis Inhibitors Eersinia enterocolitica Eersinia pestis Brucella @rancisella tularensis Pasteurella multocida -hrombocytopenia Bartonella henselae Avoid in third trimester of pregnancy Gardnerella vaginalis -espiratory bacilli

&etronida!ole (bacteridical: metabolic biproducts disrupt +(A)

-i.ampin (bactericidal: inhibits 2(A transcription by inhibiting 2(A polymerase) Isonia!id

$rimethoprim/Sul.onamide -rimethoprim5/ulfame B-, organisms s tho#azole (/'A) 'roteus (bacteriostatic: inhibition .ith /ulfiso#azole #ntero$acter Other PABA) /ulfadiazine Other acteria Pyrimethamine Pyrimethamine 'alaria &ycobacteria T. gondii 'ycobacterium tuberculosis 'ycobacterium leprae ')--/ Spirochetes Borrelia burgdorferi

8eptospira interrogans -reponema pallidum Chlamydiaceae *hlamydia trachomatis *hlamydophila 2ickettsia 3hrlichia 'ycoplasma pneumoniae Breaplasma urealyticum Actinomyces israelii (ocardia

&ycoplasmataceae *ungus-li4e acteria

Antibiotic Resistance Mechanisms

Bacteria develop ability to hydrolyze these drugs using lactamase

o o o

confers resistance to penicillin e.g. E. coli, Staph epidermidis, Pseudomonas aeruginosa, Klebsiella pneumoniae add lactamase inhibitor e.g. clavulanic acid in amoxicillin clavulanate !"ugmentin#

$enetic mutation of mec"

o o o

a bacterial gene encoding a penicillin binding protein. %e& PBP has reduced affinity for antibiotics confers resistance to methicillin, oxacillin, nafcillin e.g. '(S"

"ltered cell &all permeability

confers resistance to tetracyclines, )uinolones, trimethoprim and lactam antibiotics

*reation of biofilm barrier

provides an environment &here offending bacteria can multiply safe from the hoste immune system

"ctive efflux pumps

Salmonella Staph epidermidis

o o

confers resistance to erythromycin and tetracycline e.g. msr" gene in Staph

"ltered peptidoglycan subunit !altered + alanyl + alanine of %"',%"$ peptide#

o o

confers resistance to vancomycin e.g. vancomycin resistant enterococcus !-(E#

(ibosome alteration

erm gene confer inducible resistance to '.S !macrolide lincosamide streptogranin# agents via methylation of /0s r(%"

demonstrate using + zone test

Penicillins

for inducible clindamycin resistance in Staph and beta hemolytic Strep

'echanism

interfer &ith bacterial cell &all synthesis

Subclassification and tested examples

natural

penicillin $

penicillinase-resistant

methicillin !Staphcillin#

aminopenicillins

Cephalosporins

ampicillin !1mnipen, Polycillin#

1vervie&

bactericidal

'echanism

disrupts the synthesis of the peptidoglycan layer of bacterial cell &alls

does so through competitive inhibition on P*B !penicllin binding proteins# peptidoglycan layer is important for cell &all structural integrity.

same mechanicsm of action as beta lactam antibiotics !such as penicillins#

Subclassification and tested examples

first generation

cefazolin !"ncef, Kefzol#

second generation

cefaclor !*eclor#

third generation

cefriazone !(ocephin#

fourth generation

Fluoroquinolones

cefepime !'axipime#

'echanism

bloc2s +%" replication via inhibition of +%" gyrase

Side effects

o o

inhibit early fracture healing through toxic effects on chondrocytes increased rates of tendinitis, &ith special predilection for the "chilles tendon.

tenocytes in the "chilles tendon have exhibited degenerative changes &hen vie&ed microscopically after fluoro)uinolone administration. recent clinical studies have sho&n an increased relative ris2 of "chilles tendon rupture of 0.3.

Subclassification and tested examples

o o
Aminoglycosides

ciprofloxacin !*ipro# levofloxacin !.eva)uin#

'echanism

o o

bactericidal inhibition of bacterial protein synthesis

&or2 by binding to the 04s ribosome subunit, leading to the misreading of m(%". 5his misreading results in the synthesis of abnormal peptides that accumulate intracellularly and eventually lead to cell death. 5hese antibiotics arebactericidal.

Subclassification and tested examples

o
Vancomycin

gentamicin !$aramycin#

*overage

gram positive bacteria

'echanism

o o

bactericidal an inhibitor of cell &all synthesis

(esistance

o o

increasing emergence of vancomycin resistant enterococci has resulted in the development of guidelines for use by the !*+*# indications for vancomycin

Ri ampin

serious allergies to penicillins or beta lactam antimicrobials serious infections caused by susceptible organisms resistant to penicillins !'(S", '(SE# surgical prophylaxis for ma6or procedures involving implantation of prostheses in institutions &ith a high rate of '(S" or '(SE

!ine"olid

'ost effective against intracellular phagocytized Staphylococcus aureus in macrophages

.inezolid binds to the /0S portion of the 74S subunit and acts by preventing the formation of the initiation complex bet&een the the 04S and 74S subunits of the ribosome. #plenectomy

Splenectomy patients or patients &ith functional hyposplenism re)uire the follo&ing vaccines and,or antibiotics

o o o o o

Pneumococcal immunization 8aemophilus influenza type B vaccine 'eningococcal group * con6ugate vaccine 9nfluenza immunization .ifelong prophylactic antibiotics !oral phenoxymethylpenicillin or erythromycin#