ANTIMICROBIAL AGENTS

Lo is E B renneman, M SN , ANP , FN P, C

Table 1 - PENICILLINS

Natural penicillins - not resistant to beta-lactamase

pen icillin G Po tass ium (Pfizerpen , Pen tids) - P O, IM , IV

pen icillin G So dium : IM, IV
ben zathine G p enicillin (Bicillin) - IM
benzathine penicillin G benzathine and penicillin G procaine (Bicillin CR) IM
penicillin G procaine (W ycillin, Pfizerpen AS) IM, IV
penicillin V Potassium (Pen Vee K, V-Cillin, Veetids, Pen-V) - PO

Beta-lactamase stable penicillins - resistant to beta-lactamase

cloxacillin (Cloxapen ) - PO ; dicloxacillin (Dynapen) - PO

nafcillin (Unipen, Nafcil) - IV, ox acillin (Prosta phlin) - IV

Beta-lactamase stable combination penicillins - additive inactivates beta-lactamase

amoxicillin-clavulanate (Augmentin), ampicillin-sulbactam (Unasyn),

ticarcillin-clavulanate (Timentin), piperacillin-tazobactam (Zosyn)

Aminopenicillins (effective against gram positive and gram negative)

am oxicillin (Am oxil, Polymox ) - PO , am oxicillin/cla vulanate (Augm entin) - PO

am picillin (Om nipen, Principen) - PO, IV , am picillin/sulbactam (Unasyn) - PO , IV
bacampicillin (Spectrobid) - PO

Antipseudom onal penicillins

ticarcillin diso dium (Ticar) - IV, ticarcillin/clavulanate (T imentin) - IV

m ezlocillin (M ezlin) - IV, piperacillin (Pipracil) - IV
piperacillin tazobac tam (Zosyn) - IV , azlocillin (Azlin) - IV

most commonly used agents within a given class are underlined

Co m m ents : Beta-lactam ase sus cep tibility limits m ost agen ts for use in skin-sk in structure s. A
few agents are stable and accordingly indicated. Anaerobic coverage is highly variable.
Am inopenicillins and antipseudomonal agents have reasonably good coverage. Penicillin-allergy
is fairly comm on sometimes causing anaphylaxis. Agents are otherwise non-toxic and can be
used in pregnancy

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Table 2 - CARBAPENEMS - beta-lactam ase stab le

imipenem plus c ilastatin (P rim axin) - IV

meropenem (Merrem)

Table 3 - MACROLIDES - effective against typical and atypical organisms

1 st generation - unre liable co vera ge a gainst H influenzae

erythromycin (E-Mycin, Eryc, E.E.S., Ery-Tab, EryPed)

dirithromycin (Dynabac)

2 nd generation - reliable c overage aga inst H. influenzae

clarithrom ycin (Biaxin)

azithromycin (Zithroma x)

Good coverage S. au reus (MSSA) and s trepto coc cal sp., M c ata rrhalis, chlamydia sp,
m ycoplasm a sp , legionella sp.

Som e coverage: anaerob es (incon sistent)

No coverage ente rococc i or S epiderm idis, gm - rods.

CLINICAL INDICATION AND COMMENTS: Drug of c hoice for bronchitis. Use 2

nd
gen (H. influenzae) for
bronchitis in smok er or any sinusitis, otitis, AECB. Azithrom ycin used to cover ST D chlam ydia
and non -specific u rethritis. Goo d choice for dental prophylaxis and treatm ent of streptococcal
pharyngitis in penicillin-allergic. Good skin and skin structure coverage. Not subject to beta-
lactam ase. Low incidence of alle rgic re action . Overall safe and non-toxic. Can be used in
pregnancy (except estolate formulation). These agents are widely used in primary care although
2 nd generation has tended to replace erythromycin in many settings due to improved coverage
aga inst H. influenzae and much improved tolerance. Erythromycin tends to be poorly tolerated
resulted in significant GI distress. Certain form ulations (PCE , E-m ycin, Eryc, Ped iazole) tend to
be better tolerated. Causes significant phlebitis with IV administration and very poorly tolerated
via that route.

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Table 4 - CEPHALOSPORINS

1st generation cephalosporins:

PO: cefadroxil (Duricef), Cephalexin (Keflex), cephradine (Velosef) cefazolin

Parenteral: cefazolin (Ancef, Kefzol), cephapirin (Cefadyl)

2nd generation cephalosporins:

PO: cefuroxime axetil (Ceftin), cefaclor (Ceclor), cefprozil (Cefzil), loracarbef (Lorabid)
Parenteral: cefamandole (Mandol), cefotetan (Cefotan), cefuroxime (Zinacef)

3rd generation cephalosporins

PO: cefixime (Suprax), cefpodoxime proxetil (Vantin), ceftibuten (Cedax), cefdinir

(Omnicef), cefditoren (Spectrocef)

Parenteral: cefoperazone (Cefobid), cefotaxime (Claforan), ceftazidime (Fortaz)

Tazicef, Tazidime), Ceftizoxime (Cefizox), ceftriaxone (Rocephin), moxalactam
(Moxam)

4th generation cephalosporins: Cefepime (Maxipime), cefpirome (HR810)

COVERAGE AND CLINICAL USAGE

1ST gen best for gram positives (except enterococci) with some gram negative coverage (M.
Catarrhalis, E. coli, P. mirabilis, K. pneumoniae) - Good beta-lactamase resistance - Used
extensively with skin and skin structure infections

2ND gen increases coverage of gm negatives but some gm positive is lost; no enterococci -
overall broad spectrum - widely used in variety of infections

3RD gen: excellent gm negative coverage; limited gram positive esp against S aureus but
streptococcal sp. Is still good. Widely used for surgical prophylaxis; used empirically with
aminoglycoside for gm negative meningitis and for fever unknown origin.

4th gen: good gram positive and broad array of gm negative incl P aeruginosa

CLINICAL INDICATIONS AND COMMENTS:

Much less beta-lactamase resistance as compared to penicillins. First and second generation
have bro ader spectrum . Can be used in re spiratory tract infectio ns, sinusitis, o titis, sk in and sk in
structures (1 st gen is best choice). An alternative in UTI where other agents are not an option
Cross reactivity (8%) with penicillin allergy. Overall non-toxic; can be used in pregnancy. Can
substitute for penicillin in allergic patient e.g. strep pharyngitis . Inconsistent to poor for
anaerobes. Some 4 th generation have pseudomonal coverage; 1st-3rd generation have no
coverag e.

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Table 5 - TETRACYCLINES - effective against typical and atypical organisms
tetracycline (Sumycin, Achromycin)
doxyc ycline (D oryx, V ibram ycin)
m inocyc line (M inocin )
demecolcine (Declomycin)
meclocycline (Meclan)
oxytetracycline (Terramycin)

underline d indicate s th e m ost co m m only used agents; others agents rarely

used

Minocycline is ex trem ely active aga inst M RS A an d M RS E an d us ed s ucc ess fully with
staphylococcal infections. Doxycycline active against some strains VRE; regular
tetrac ycline is poorly ac tive against S. pneumoniae howeve r doxycycline is active
aga inst S. pneumoniae including penicillin-resistant strains

TRADITIONAL USES FOR DOXYCYCLINE

M. pneumoniae, Psittac osis, Q fe ver, C. trachom atis , G. inguinale, Bruc ella, T. pallidum,
rickettsia, Bo rrelia re currentis , Tularem ia, Anthrax , Leptosp irosis, Yersinia pestis,
Ac tino myc es isra elii, Nocardia

NEW USES FOR DOXYCYCLINE (1990s)

P. multocida, H. pylori, Mycobacterium marinum, VRE, plasmodium falciparum m alaria,

c. p neum onia, Ba cillary angiomato sis, Vibrio vulnificus, Aeromonas, Plesiomonas,
Eh rlichiosis, Legionella, Lym e disease. A lso denta l plaque prophylaxis

NEW USES FOR MINOCYCLINE - Methicillin-R esistant-Staphylococcus aureus (MRSA)

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Table 6 - SULFONAMIDES

Bro ad spe ctru m- system ic

Trimethoprim-Sulfamethoxazole - (Bactrim) -SMP-TMX

Topical skin esp burns

Silver sulfadiazine (Silvadene cream) -
Mafenide acetate (Sulfamylon cream) - rarely used (metabolic acidosis)

Urinary tract age nts

Sulfisoxazole (Gantrisin, Azo-Gantrisin)
Su lfam eth oxazo le (G antan ol, A zo-Gantan ol)

Op hthalm ic agents
Sulfacetamide sodium (Bleph-10, Cetamide, Blephamide, Sulamyd)

V ag in al cre am s
Sulfathiazole (Sultrin vaginal cream an d tablets, Triple Sulfa) - vaginal therapy
Sulfanilamide (AVC, Vaginal Sulfa, Vagitrol) - vaginal cream

Inflamm atory bow el disease ag ents

Sulfasalazine (Azulfidine) * - sulfonamide plus salicylate

* mesalamine (Pentasa, Canasa) a salicylate with no sulfa moiety is more commonly

used since benefit for IBD derives from antiinflammatory effect of salicylate; sulfa moiety
is irrelevant. Underline are most commonly used agents; others rarely used

TRADITIONAL USES (1970s)

- Traditional use : UT I, pros tatitis, epididym itis, OM , shige llosis, P. C arinii pneumonia
- Good activity against variety of comm unity-acquired organisms
H influenzae, M catarrhalis, E coli, P mirabilis, K. Pneumoniae, enterotoxigenic E.
Co li, Shigella species and Y enterocolitica. Listeria and PCP

Little or no activity: P. aeruginosa - Anaerobic bacteria including Ba cte roides fragilis

NEWER USES

- Good activity against many strains of S aureus and some strains of MRSA
- Newer nosocomial pathogens: Stenotrophomonas m altophilia and Burkholderia cepacia.
- Penetrates CSF: alternative therapy for Listeria meningitis in pcn-allergic patient
- Im m uno com prom ised patien t:
- PCP prophylaxis - C NS to xoplasm osis
- Diarrhea from Isos pora belli and Cyclospo ra.
- W egner’s granulomatosis - TMP -SMX results in fewer relapses

© 2002 Lois E. Brenneman, MSN, CS, ANP, FNP

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Table 8 - AMINOGLYCOSIDES - high toxicity - systemically only for serious infections - IV

amikacin (Amikin)
tobramycin (Tobrex, Tobrex ophthalmic)
gentamycin (Garamycin, Garamycin ophthalmic )
netilmicin (Netromycin)
neomycin (Mycifradin, Neosporin) - now used only topically due to toxicity

Covers
Gram negative rods (enterobacteriaceae), S. aureus (MSSA), S. faecalis,
L. monocytogenes
No coverage: streptococcus sp, neisseria sp, atypicals, anaerobes

Table 9 - URINARY TRACT ANTIBIOTICS - used exc lusively for UT I - no systemic absorption

nitrofurantoin (Macrobid, Mac rodantin) - UTI - E. coli, S. saprophyticus only

fosfom ycin (Monurol) - UTI - E. c oli, S saprophyticu s, E . fac ialis, not for pseudo
methenam ine (Mandelamine, Hiprex, Urised) - liberates formalin in bladder

Trimethoprim-sulfamethoxazole (Bactrim) and fluoroquinolones are more commonly used for

UTI

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Table 10 - CLINDAMYCIN and VANCOMYCIN

van com ycin (Vanc ocin) - IV (PO on ly for C diffic ile) - tox ic

Indication: S. aureus (MRS A), C. difficile (pseudomem branous colitis)

Covers : gram pos itive (strep sp , staph sp incl MRS A, en teroc occ i sp, L
monocytogenes), some anaerobes: clostridia sp (incl C. difficile) and actinomyces
No coverage: gm negatives, non-clostridia anaerobes

clindamycin (Cleocin) - toxic - indicated for only serious gm + infections - PO and IV

Indication: respiratory, skin, soft-tissue, septicemia, intraabdominal, female pelvic or

gen ital, bone /joint.
Coverage: streptococcus sp and S. aureus (MSSA), some gram positive
anaerobes (not clostridium).
No coverage: enterococci, S epididymis, gram negatives rods (enterobacteriaceae )

TRADITIONAL USES CLINDAMYCIN (since 1960s)

- Serious anaerobic infections

- Intra-abdom inal infections (covers B . fragilis and other anaero bes) *
- Anaerobic pulmonary infections
- Pelvic infections *
- Bacterial vaginosis (used topically)
- Does not penetrate CN S th us not us ed for m eningitis
- Anaerobic lung infections
- Diabetic foot, polymicrobial osteomyelitis, infected decubitus *

* Requires combo with agent for gram negative coverage usually quinolone

NEWER USES OF CLINDAMYCIN

Diabetic foot infections *, S aureus, infected sacral decubitus ulcers *, PCP, cerebral
toxoplasmosis, Babesiosis, Staphylococcal intravenous or prosthetic device
infections)

* Requires combo with agent active against aerobic gm-negative bacilli

Babesiosis: clindamycin in combo with quinine is drug of choice

PCP; clindamycin in combo with pyrimetham ine is alternative for cerebral
tox oplasm osis
S. aureus osteomyelitis: highest bone-to-serum ratio
Fo llowed by va ncom ycin, nafcillin, tobram ycin, ce fazolin , ce phalothin

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Table 11 - NEW ANTIBIOTIC AGENTS

linezolid (Zyvo x) - first of new class - PO and IV

Indication: vancomycin resistant E. faecalis (VREF), skin /sk in structu res, pneum onia
(nosoco m ial, com m unity acquired)
Coverage: Stap h sp (incl M RS A), Strep s p, En teroc occ i sp, L m ono cytogene s,
No coverage: gm negatives, inconsistent for anaerobes

quinu pristin-dalfopristin (Syn ercid) - tox ic with po tential for adverse intera ctions - IV
Indications: serious life-threatening infections with VREF bacteremia, Complicated skin-
skin structure infections with S aureus (MSSA), S pyogenes
Coverage: Strep sp., Staph sp, (MRSA), E. Faecium, L monocytogenes, some
anaerobes, s om e atypic als
No coverage: most gm negatives

Table 12 - MISCELLANEOUS ANTIBIOTICS

M etronidaz ole (Flagyl, M etroG el) - anaerobes, parasites

TRADITIONAL USES (1950s)

- Anaerobic and some protozoa; similar to second generation of tetracyclines

- Attains therapeutic levels in all tissues including brain and csf
- Effective for serious anaerobic infections including brain abscesses

TRADITIONAL INDICATIONS:

Ba cte rial vaginosis, trichom onas, giardiasis, am ebiasis

Effective for polymicrobial infections when agent to cover gm neg bacillus and gm
positive cocci eg levofloxacin (also good for oral polymicrobial infections)

NEWER USES

Drug of choice for pseudom em branous colitis

Vancomycin often used in seriously ill patient
Useful vs H pylori in combo regimen with bismuth, omeprazole and tetracycline
Useful in Crohn’s disease -> healing of perianal disease
Topically helpful fo r rosacea and also bacterial va ginosis

Rifam pin (Rifad in) - N. meningitis prop hylaxis or ca rrier, M. tuberculin

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