Penicillin

Natural

Antistaphyloccol

Extended spectrum

Antipseudomonal

Monobactams

Cephalosporins

1st-4th generation

Vancomycin

MOA

Inhibit the transpeptidase enzyme that assists with cross linking of peptidoglycan chains

Resistance

By production of beta-lactamase that cleaves the beta-lactam ring to inactivate the

metabolite

Alteration in penicillin-binding proteins

Decrease penetrability of the cell wall

Side effects: type I hypersensitivity reaction

Penicillin G (IM) and V (oral, because acid stable)

Renally excreted add probenecid to increase blood levels

Crosses blood brain barrier with inflammation

Spectrum of activity

Gram positive

Non resistant staph and strep, anthrax

With aminoglycoside for enterococcus

Gram-negative: Neisseria meningtidis

Anaerobes: Clostridium (not B fragilis)

Spirochetes: Treponema

Methicillin (IV), nafcillin (IV), oxacillin (IV),

Dicloxacillin (PO)

Resistant to breakdown by beta-lactamase

Spectrum of activity

Beta-lactamase producing staph

Not effective against gram negative organisms

MRSA treat with vancomycin

Side effects

Methicillin: interstitial nephritis (not used clinically).

Ampicllin (PO,IV), amoxicillin (PO)

Spectrum of activity Covers strep

Have some gram negative coverage

H. flu

E. coli

Listeria monocytogenes

Proteus mirabillis

Salmonella

Neisseria

Beta lactam inhibitors: extend the spectrum of activity Clavulanate

Plus amoxicillin is Augmentin

Sulbactam

Plus ampicillin is Unasyn

Side effects: Ampicillin: diarrhea, pseudomembranous

colitis

Ampicillin rash: infectious mono

Carbenicillin (PO), ticarcillin (IV), piperacillin (IV)

Spectrum of activity Cover pseudomonas and some aerobic and anaerobic

gram negative rods E.coli, Proteus, Enterobacter, Citrobacter, Serratia, Klebsiella

Side effects

GI disturbances

Prolonged bleeding time (platelet dysfunction)

Beta-lactamase inhibitors: addition adds staph staph coverage

Clavulanate Plus ticarcillin is Timentin

Tazobactam Plus piperacillin is Zosyn

Aztreonam (IV)

Spectrum of activity Active against gram-negative rods, including

pseudomonas

No activity against gram-positive rods or anaerobes

Side effects While is a beta-lactam, it is not

contraindicated in patients allergic to penicillin or cephalosporins

Cefazolin (Ancef) (IV), cephalexin (Keflex) (PO), Cephaslothin (Keflin) (IV), cefadroxil (Duricef) (PO),

Spectrum of activity Oral cavity anaerobes except B.fragilis Cover some gram-negatives (used in UTI) E.coli

Cover S. pneumoniae and H. flu but not as well as later generations Avoid in treating URI

Cover staph, not MRSA Used in surgical prophylaxis

Side effects:

Diarrhea

Hypersensitivity reactions

Fever

Increased liver function tests (uncommon)

Neutropenia, thrombocytopenia (uncommon)

Respiratory and PID

Cefaclor (Ceclor) (PO), Loracarbef (Lorabid) (PO),

Cefoxitin (Mefoxin) (IV), Cefuroxime (Zinacef, IV),

Ceftin (PO), cefotetan (Cefotan, IV), cefprozil

(Cefzil, PO)

Spectrum of activity

Increased activity against S. pneumonia, H.flu (cefuroxime is the best for URI/sinusitis)

Active against anaerobic infection including B. fragilis, (cefoxitin, cefotetan)

Use in PID

Spectrum of activity (continued)

Covers same gram-negatives as first generation plus h.flu, enterobacter, klebsiella, proteus, Neisseria species

Side effects same as first generation

Pneumonia, CNS

Ceftriaxone (Rocephin, IV),

cefixime(Suprax, PO), ceftizoxime

(Cefizox, IV), ceftazidime (fortax),

cefpodoxime (Vantin, PO),

Spectrum of activity

Against s. pneumo and h.flu

Good penetration of CNS (meningitis)

Spectrum of activity continued

Used to treat N. gonorrhoeae

Cover pseudomonas (ceftazidime, cefepime)

Poor activity against s.aureus

Side effects

Same as first and second generation

Increased risk of enterococcal superinfection

Cefepime(Maxipime IV)

Spectrum of activity

Must be methicillin susceptible staph and strep

Gram negative bacilli including pseudomonas

Side effects

Same as other groups

Going from first generation to fourth,

gram positive coverage lost, gram

negative gained

Do not cover MRSA or enterococcus

Avoid alcohol

May have disulfiram-like reaction

May cause bleeding disorders

Imipenem plus cilastatin(IV), meropenem (IV) Cilastatin inhibits breakdown of imipenem in the

kidney

Spectrum of activity Broad spectrum gram positive, gram negative,

anerobes Covers 90% of clinically important bacteria

Meropenem has high activity against pseudomonas

Side effects Can cause seizures

Action

Inhibits bacterial cell wall synthesis; binds of portion of cell wall precursors

Bactericidal against most bacteria (except enterococcus)

Spectrum of activity

S. aureus (including MRSA), s.epidermidis, strep, corynebacterium diphtheriae,

clostridium

Spectrum of activity continued

Use in endocarditis, osteomyelitis, necrotizing fasciitis

Pseudomembranous colitis (oral vancomycin)

No coverage against gram negative

organisms

Side effects

Red man syndrome

Histamine release

No problem if drug given slowly

Ototoxicity (can be permanent)

Nephrotoxicity (increased with other nephrotoxic drugs)

Chloramphenicol

Tetracycline

Macrolides

Aminoglycosides

Clindamycin

Linezolid

Bacteriostatic: binds to 50S ribosomal

subunit

Metabolized in the liver and enters CNS

Good choice for brain abscess

Spectrum of action

Kills most gram-positive, gram negative, and anaerobes

Effective against Rickettsial infections (RMSF)

Side effects

Bone marrow suppression/aplastic anemia

Gray baby syndrome

Due to inability to metabolize drug to inactive metabolites

Present with shock, abdominal distention, cyanosis

Decrease use due to severe side effects

Short vs. long acting Tetracycline: t1/2 6-12 hours

Doxycycline/minocycline t1/2 16-18 hours

MOA Bacteriostatic, bind to 30S ribosomal unit

Crosses the placenta and is in breast milk

Binds to calcium and antacids

Inhibits absorption of tetracycline

Renal excretion

Doxycycline eliminated non-renal, so safe in renal failure

Spectrum of activity

Cover gram positive and gram negative but not drug of choice due to increased resistance

Covers: Rickettisal infections

Spirochete infections (Lyme disease)

Mycoplasma pneumoneae

Chlamydial infection

Minocycline for acne

Side effects:

Hepatotoxicity

GI upset: diarrhea, nausea, vomiting

Phototoxic dermatitis

Discolored teeth/decreased bone growth (do not give to children

Erythromycin (e-mycin)

Clarithromycin (Biaxin)

Azithromycin (Zithromax)

MOA

Bacteriostatic, bind to 50S ribosomal subunit

Hepatic metabolism

Azithromycin concentrates in tissue and releases slowly over prolonged period (t1/2 72 hours)

Spectrum of activity Group A strep, strep pneumo, chlamydia,

mycoplasma, .flu, legionella

Mycobacterium avium can use azithromycin

Side effects: GI upset

Cholestatic hepatitis

Inhibits cytochrome P-45

Can lead to an increase in other drugs if metabolized by liver

Gentamycin, Tobramycin, amikacin, streptomycin

MOA Poor oral absorption

Eliminated by kidneys

Bactericidal; bind to 30S ribosomal subunit and inhibit bacterial protein synthesis

Antibiotic enters bacteria by oxygen dependent active transport

Not effective against anaerobes

Spectrum of action

Aerobic gram negative

Tobramycin more active against pseudomonas

Amikacin reserved for the most serious infections

Endocarditis due to enterococcus

Side effects:

Ototoxicity

Hearing loss (usually irreversible), tinnitus, vertigo, ataxia

Nephrotoxicity

Acute tubular necrosis

Monitor serum creatinine

PO, IV, topical

MOA Bacteriostatic, binds to 50S ribosomal subunit

to inhibit bacterial protein synthesis

Spectrum of action Gram positive and anaerobic bacteria

Anaerobes above the diaphragm

Will cover strep pyogenes

Alternative to pcn and ceph in allergic pt

Side effects: psedomembranous colitis

MOA

Inhibits protein synthesis, binds to 50S subunit

Spectrum of activity

MRSA, VRE, corynebacterium, listeria

Side effects:

GI upset, diarrhea, headache, rash, thrombocytopenia

Ciprofloxacin (cipro), ofloxacin (Floxin), norfloxacin (Noroxin), Levofloxacin (Levaquin), moxifloxacin (Avelox) MOA

Bactericidal; binds to bacterial enzyme DNA gyrase

Inhibits DNA replication and RNA transcription

Undergo hepatic biotransformation and are excreted unchanged in urine

Decreased oral absorption with ingestion of dairy and antacids

Spectrum of action Broad spectrum: aerobic gram positive and

gram negative bacteria

UTI: due to gram neg rods and pseudomonas

Prostatitis: good prostate penetration

Travelers diarrhea: shigeela, salmonella, E.coli, camplobacter

URI due to pneumococci, chlamydia, mycoplasma, h.flu, legionella

Some coverage of mycobacterium

Side effects:

N, headache, dizzy

Sensitivity to UV light

Due to damage to growing cartilage, contraindicated in children

Sulfonamides

Sulfacetaminde (Sulamyd): topical

Sulfadiazine (PO or topical)

Sulfamethoxazole (PO)

Folate reductase inhibitors

Trimethroprim (PO)

Trimethroprim-sulfamethoxazole (Bactrim)(PO, IV)

MOA

Decreased production of essential cofactors for the synthesis of DNA, RNA, and proteins through the blockage of tetrahydrofolic acid

production

Spectrum of action

Allergic skin rash, steven johnson syndrome

Kernicterus: displacement of billirubin which penetrates the CNS

Bactrim: N/V, GI upset, thrombocytopenia, leukopenia

Avoid during pregnancy; fetotoxic

MOA

Bacteriocidal, drug reduced to toxic agents that bind intracellular macromolecules

Metabolized in the liver

Spectrum of action

Active against nearly all anaerobic and microaerophilic bacteria including B. fragilis

Antiparasitic

Side effects:

Disulfiram reaction

Cacinogenic potential

Metalic taste

Macrobid or macrodantin (PO)

MOA: Causes damage to bacterial DNA

Rapidly excreted in urine

Spectrum of action Treat UTI due to E.coli, enterococcus,

S.saprophyticus

Side effects: N/V, hemolytic anemia, pulmonary and

hepatic toxicity