ANTI-BACTERIAL AGENTS
Drug
I. -Lactams
A. Penicillin
PenG (benzylpenicillin)
PenV
(Phenoxymethylpenicillin)
Oxacillin
Cloxacillin (oral)
Ampicillin inj.
Amoxicillin oral
Piperacillin inj.
(Antipseudomonal pen.)
Anti--lactamases
Amox + clavulanic acid oral
Ampi + sulbactam IV
Piperacillin + tazobactam IV
B. Cephalosporins
1st Generation cefazolin IV;
cefalexin, cefadroxil oral
2nd Gen
Cefuroxime
Cephamycin (cefoxitin)
Use
DOC: GPC (S. pyogenes & pen sensitive S. pneumonia,
staph), GPB (anthracis & diptheria), GNC
(menigococcus and gonococcus), GNB (bubonic
plague, Vincents infection by Spirilum minus),
Spirochetes (treponema like syphilis yaws, leptospira
and bacilli in bubonic plague and spirilum minus),
anaerobes (cocci, fusobac, actino, clostridium in
tetanus and gas gangrene, bacteroides except fragilis)
PenG sens bact in respi (strep tonsillitis/pharyngitis),
skin, subQ
Penicillinase Staph infxns, not active vs enterococci,
anaerobes, gram negative cocci & bacilli
Retain antibac of Pen and improve against G(-), IV in
enterococci, Listeria, Gonorrhea, H. influenza, E. coli,
Proteus, shigella, salmonella
same w/ ampicillin but None in Shigella, Tx typhoid
fever, anti-H.pylori with PPI and bismuth subcitrate for
ulcers, chemoprophylaxis in bacterial endocarditis in
dental surgery
Ampicillin spectrum plus vs Pseudo, B. fragilis, Kleb.,
more active than ticarcillin
Ureidopenicillin acylureido deriv. of ampicillin
UTI, otitis media, sinusitis, bite wounds
Complicated intraab/pelvic infxns, polymicrobial RTI
Immunocompromised pxs, nosocomial pneumonia w/
resistance
None active against enterococcus, listeria, MRSA
GPC, penicillinase Staph, strep; alt: for impetigo,
osteomyelitis, pharyngitis, skin/soft tx infxn, surgical
chemopylaxis (cefazolin), Pen allergic pxs
GPC = 1st, better GN, none w/ Pseudo
Haemo, enterobacteriaceae, -lactamase Neisseria ,
alt: for chr bronchitis, epiglotitis, otitis media, sinusitis,
pyelonephritis, orbital cellulitis, pneumonia, skin &
soft tx, bone, jt infxns
Enterobacteriaceae, anaerobes, B. Fragilis outside
CNS, mixed infections in peritonitis liver & pelvic inf.,
surgical chemoprophy in colorectal & appendectomy
MOA
binds with PBP selective
inhibition of transpeptidase
reaction no synthesis of
mucopeptide (murein,
peptidoglycan)
inactivation of inhibitor of
autolytic enzymes
(autolysins, murein
hydrolases cell wall lysis
(bactericidal)
PBP-1, PBP-3, 6-amino-
penicillanic acid (-lactam +
5-membered thiazolidine
ring)
inhibitors of -lactamases
Same as -lactams
Notes PRC
Cidal, time-dependent antimicrobial
Limitations: Deactivated by -lactamases,
unstable in acid gastric contents, limited
spectrum,rapid renal excr, hps, poor BBB
penetration
Short acting: PenG aqueous(crystalline) Na
K salt- for severe life threatening infxns
Repository Forms: IM: Procaine PenG
(sustain serum levels for 12-24h,high pen R)
Benzathine PenG (low but sustained levels
1-3wks, 1o & 2o prevention of RF & syphilis)
Penicillinase susceptible analogue of
PenG
Limitations: poor bioav, qid on empty
stomach, narrow spectrum
Penicillinase resistant, isoxazolyl grp
Expanded spectrum (penicillinase sensi),
Aminopenicillins
In combi with aminoglycoside/
fluoroquinolone for pseudo inf. outside
urinary tract to prevent resistance
Co-amoxiclav, 7:1 if BID, 4:1 if TID
Sultamicillin- oral, prodrug
Activity vs Pseud&S.fecalis not enhanced by
fixed dose combo w/ B-lactamase inhibitor
7-aminocephalosporanic acid (betalactam
ring fused with 6-membered
dihydrothiazine ring), cephamycins
Drug interactions: Disulfiram-like rxn after
alcohol ingestion w/ ceph w/ MTT side
chain; toxic renal damage potentiated by
concurrent use of aminoglycoside,
probenecid, rapid acting diuretic ; drugs for
hemostasis (heparin, anticoags) increase
hemorrhage risk w/ Moxalactam & others
w/ MTT side chain
PK
60% pr. binding, Acid labile, low
bioav., poor oral, distributed in
all tx & fluids, penetrate
inflamed BBB, kidneys (10% GF,
90% TS) Parenteral, t1/2 0.5 h
Good oral w/o food, 60% pr
binding, acid stable
B Low oral, 90-94% pr binding
Low oral, 95-98% pr binding,
acid stable
Low oral, 18-22% pr binding
High oral B, 17% pr binding, acid
stable
Acid labile, 16-48% pr binding
Oral, 20-30% pr binding
Oral, 28-38% pr binding
16-48% pr binding
B Renal except cefixime &
ceftriaxone (renal and hepatic)
No CSF, Cefalexin & Cefadroxil-
90% absorbed orally, low pr
binding, Cefazolin-80% pr bound
Poor CSF
NOT for meningitis
Cefuroxime axetil (oral)-
prodrug, 52% absorbed, 50% pr
bound; Cefuroxime IV- the only
2nd gen ceph w/c cross BBB but
NOT sufficient for Tx
Most active vs. Anaerobes (B.
fragilis), 65-99% pr bound
others
all beta-lactams in high conc. cause seizures
CI: hps coz all Pen have cross-allergenecity,
bleeding abn for extended spec pen like
antipseudomonal(BT, PT)
ADR:
Frequent: allergy, maculopapular rash (ampicillin
& amoxicillin), diarrhea (esp w/ ampicillin & co-
amoxiclav), nausea & vomiting w/ co-amoxiclav in
children
Occasional: hemolytic anemia, neutropenia,
pseudomembranous colitis, plt dysfxn (high dose
carbenicillin, ticarcillin, azlocillin, piperacillin,
nafcillin, methilcillin), cholestatic hepatitis (co-
amoxiclav)
Rare: muscle irritability & seizures (in px w/ renal
impairment), hyperkalemia & arrhythmia (w/ IV
penG given rapidly), agranulocytosis & hepatic
renal damage with semisythetic penicillins,
bleeding diathesis, Henoch-Schonlein purpura
(ampicillin), disorientation, hallucinations,
agitation, neurologic rxns like Hoignes syndrome
(w/ high dose of procain penicillin G)
Drug interactions:
High dose cabenicillin/ticarcillin inactivates
aminoglycosides; Ampicillin decrease effects of
oral contraceptives; Amoxicillin after MMR
vaccine cause erythema multiforme; increase
methotrexate toxicity; B lactams +
aminoglycosides = synergism; Probenecid
increase half life of penicillin; Static agents (ex.
Tetracycline) reduce effectiveness of B-lactams
Antagonism
intrinsic activity, potent irrev inhibitor of
Ambler Class A B-lactamases (plasma encoded
TEM B-lactamase), NOT good inhibitor of Class C
(chrom encoded B-lactamase)
ADR:
Frequent: thrombophlebitis w/ IV use, serum
sickness like rxn w/ Cefaclor, diarrhea w/
Cefoperazone
Occasional: allergy, GI disturbance,
hypothrombinemia, hemorrhage w/ Ceph w/
MTT side chain ex. Cefamandole&
cefoperazone ,plt dysfxn, coagulopathy, Vit K dep
CF def w/ Moxalactam, rash&arthritis w/ Cefaclor
in children, bile sludging & pseudocholelithiasis
w/ Ceftriaxone
Rare: hemolytic anemia, hepatic dysfxn, blood
dyscrasias, renal damage, acute interstitial
nephritis & convulsions w/ Cephalotin
 Even better GN, resistance to GN-lactamase,
3rd Gen
reach bactericidal conc. in CSF except cefoperazone
GN-lactamase producers, penicillin resistant
Cefotaxime, Ceftriaxone (IV)
pneumococci, LIMITED anti-pseudo activity
single dose Tx of uncomplicated gonorrhea, NOT active
Cefixime (oral)
vs S. aureus & pseudomonas
Best vs Pseudo (antipseudomonal) & indole (+)
Ceftazidime Proteus, empiric treatment of febrile neutropenic pxs
combi w/ antipseudomonal aminoglycosides
GP, enterobacteriaceae, Pseudo, severe inf. Like
4th Gen Cefepime sepsis, pneumonia, meningitis, severe mix g(+) and
g(-), empiric monotherapy in febrile neutropenic pxs.
Multiple resistant GN (esp Meropenem), DOC
enterobacters & infxn by ESBL producing GN, mixed
C. Carbapenem infect of Staph, GNB and anaerobes, monotherapy for
intraabd, febrile neutropenic px & Pseudomonas (in
combo w/ antipseudo aminoglycoside to prevent R)
Broadest spectrum (GP&GN), better vs GP compared
1. Imipenem to Meropene, cidal except to E. faecium, MRSA, C.
difficile, Burkhoderia, Stenotrophomonas maltophilia
Better vs GN, CSF levels potentially therapeutic, combo
2. Meropenem IV
w/ antipseudomonal aminoglycoside
IM and IV, OD, less active than 2 above vs
3. Ertapenem
Pseudomonas & acinetobacter
GN aerobes (substi for aminoglycosides), allergy to
D. Monobactams Aztreonam pen or cepha, mixed infections, spectrum like AMG,
combi with clindamycin, vanco, metroni
II. Aminoglycosides AMG cidal vs. GN aerobes & S. aureus, conc dep.
Streptomycin TB, mycobac, Strep viridans w/ PenG (ex. SBE)
UTI with GNB, combo w/ pen or ceph: empiric therapy
Gentamicin for serious infxn (neonatal sepsis etc), mixed infxn
(peritonitis), Pseudo, Prot, Kleb, acute cholangitis
Netilmicin Same as gentamicin, but more resistant to inactivation
Amikacin by enzymes (adenylating)
aminocyclitol, Bacteriostatic, alt: Tx gonococci in px
Spectinomycin
who are allergic to pen
III. Chloramphenicol DOC: severe H. influenza, susceptible S. typhi,
Bacteroides (meningitis, brain abscess), alt: for PenG
allergy in pneumococcal and meningococcal
meningitis, rickettsia in pxs w/ tetracycline hps,
pregnant, brucellosis, glanders, plague, intraocular inf
Static except in H. influenza, N, meningitides,
Same as -lactams,
PBP-2, 1b
Same as -lactams, binds
PBP-3, cidal
Bind 30s ribosomes inhibit
CHON synthesis
Reversibly binds to 50s
prevent AA transfer inhibit
peptidyl transferase inh.
CHON synthesis
betalactam ring attached to 5-membered
ring, sub of carbon for sulfur and unsat. In
5-membered ring
Induces -lactamases
Not absorbed orally, penetrate all tx & CSF
when inflamed, 75% excr unchanged
not degraded by dehydropeptidase
-lactamase resistant, not induce chrom
mediated B-lactamase (unlike ceph &
imipenem) not crossreact w/ pen&ceph,
synergy w/ AMG, levels w/ probenecid
impaired if w/ hypoxemia and acidemia
DI: nephrotox (ceph, AMB, furosemide),
ototox (ethacrynate/bumetamide), NMJ
(curare and MgSO4), inactivated by
carbenicillin and ticarcillin
lithium tox
Prodrugs needs hydrolysis: Succinate ester
(IV), Palmitate ester (oral) for pediatrics
DI: inhibit drug metab, anticoag w/
dicoumarol, hypoglycemia with
sulfonylureas, inc. phenytoin tox, w/
phenobarb/toin & rifampicin; disulfiram like
Good CSF
Ceftriaxone-qd, 90% bound,
DOC for gonorrhea;MDR S. typhi
50% absorbed, 65% bound, T1/2
is 3h
Most active 3rd gen ceph vs P.
aeruginosa
Good CSF, more resistant to
chromosomal B-lactamase by
enterobacter
Not oral, inflamed BBB, renal Dec dose: elderly (renal dysfxn, cerebrovasc dxs)
exc, inactivated by renal (in ADR: Phlebitis, F, uritcaria, pruritus, N, V,
Prox tubule) dihydropeptidase I pseudomem colitis, seizures w/ imipenem
*10x more neurotox than Admin w/ Cilastatin (renal dehydropeptidase
benzylpenicillin; R to B- inhibitor) to prevent low urinary conc, IV q 6-8h,
C
lactamases but NOT to metallo- Seizure potential, potent inducer of Class C B-
B-lactamase lactamase (w/c can inactivate other B-lactams)
No seizure potential when admin w/ cilastatin
B Hepatobiliary
(imipinem higher affinity to GABA)
95% pr bound, excr renal &
B
biliary, IM prep has 1% lidocaine
Not oral, inflamed BBB, renal & Local rxn, rash, D, N, V, aminotransferase,
B
biliary, penetrates into all thrombocytopenia, pseudomem colitis
Relative renal toxicity:
neo>kana,amikacin, genta,
w/ edema/ ascitis.obesity base dose on ideal wt
netilmicin>tobra>streptomycin
Dosages for estimated clearance >/=80mL/min
Relative ototox: neo
Measure peak serum levels 2h after infusion,
(cochlear)>strep (vestibular)>
trough level just before next dose
kana (cochlear)>amika, genta,
tobra, netilmicin
8th (vestibular) nerve damage, paresthesia,
pruritus, renal damage, blood dyscrasias, NMJ
IM, not CSF, kidneys
D block (reversed by Neostigmine), SJS, optic
neutitis, hepatic necrosis, mocarditis etc.
IM, IV, topical, otic, ophtha, qd Vestibular damage, renal tox ( w/ qd dose),
dose, Not w/ heparin lock coz of auditory,NMJ blockade and apnea (reverse w/ Ca
ionic bind, excr unchangd by GF or Neostigmine), anaphylaxis, polyneuropathy
IM, IV, qd dose Less nephrotoxic
IM, IV, qd, Not w/ heparin
Neither oto/nephrotox, w/ benzylalcohol = fatal
IM gasping syndrome in infants; dec. urine output,
allergy, nausea, chills, fever, insomnia, dizziness
C Oral (75-100%, >bioav vs *attach polar grp (ester linkage) to inc solubility
chloramphenicol succinate), 25- CI: Hps, hematotox, preggy, neonates/breastfeed
50% pr bound, in CSF, bones, ADR: Anemia, gray baby, GI, allergy, aplastic,
inactivated by liver conj, 5-15% leukemia, peripheral neuropathy, pseudomem
via urine, 4% via bile; can colitis, hemolytic anemia (G6PD def.)
antagonize cidal axn of pen and

IV. Tetracyclines
(tetracycline HCLimpaired by
food, doxycyclin, nubicycline
both high oral abs, q12hrs)
V. Macrolides / Azalides (ACE)
Erythromycin (prototype)
Clarithomycin
Azithromycin
VI. Lincosamides
Linco/Clindamycin
VII. Glycopeptide
vancomycin (cidal)
VIII. Fluoroquinolones
Ciprofloxacin(prototype 2nd
gen.); DOC anthrax, greatest
anti pseudo activity in this grp
Ofloxacin 2nd gen.
Levofloxacin- 3rd gen, B. fragilis
NOT susceptible
Gatifloxacin
Norfloxacin
IX. Nitromidazoles
metronidazole (prototype)
bacteroides (cidal)
DOC: Chlamydia--Doxycyclin (urethritis, pelvic inflame
dxs, lymphogranuloma venereum, psittacosis),
rickettsia (RMSF, typhus), Lyme, lepto, brucella (in
combo w/ streptomycin), plague, cholera, tularemia
M.fortuitum (only doxycyclin), malaria (doxycycline),
Granuloma inguinale
Others: intestinal amebiasis, alt: actinomycosis, rat
bite, syphilis, tularemia, yersinia, Penicillinase gonocci,
Mycoplasma, acne (long term low dose), leprosy
(minocycline comb w/ rifampicin and ofloxacin);
adjuvant in amebiasis
DOC: diphtheria inf/carrier state, Mycoplasma
pneumo, Legionella, pertussis Tx&prophylaxis,
chancroid, gastroenteritis Campylo, Chylamidia
pneumo in preggy/kids
Px hps in pen: strep & pneumococcal, syphilis, RF
prophy, prevent bacty endocarditis after dental
procedure; acne; pre-op chemoprohy in elective
colorectal surg, alt drug for C trachomatis urethritis
Added effects vs Haemo, M. avium, M. leprae, T.
gondii, Anti-H.pylori
Broader spectrum but less active vs staph & strep
Never a 1st choice, Static vs GN aerobes & non CNS
anaerobes (ex. Intraab inf, combo w/ AMG or
aztreonam), alt: Pen and cephalosporin allergy (esp in
osteomyelitis & septic arthritis)
GPN, but GNB & mycobacty R
DOC: MRSA, GP
IV: Alt: unresponsive or S. viridians & enterococcal
endocarditis, pseudomembranous colitis, prosthetic
device inf. CSF shunt inf., serious nosocomial inf.
Oral: antibiotic induced pseudomembranous colitis
In vitro activity: less active in GPAerobes than GNA
Not for anaerobes, Alt: Mtb, MAC
MSSA, severe UTI (pyelonephritis), GI infxn (ex. MDR
Salmonella), STD (gonococcus), -lactam resistant
osteomyelitis/septcimea, meningococci carrier
eradication & prophylaxis
only for UTI & acute bacty invasive diarrhea shigellosis
GN, protozoals, cidal for anaerobes (ex. fragilis &
clostridia)
Anti-protozoal: T. vaginalis, amebiasis, giardiasis
Inh pr synthesis by binding
w/ 30s (or 50s) & inh binding
of incoming charged
aminosyl tRNA into acceptor
site on mRNA-ribosome
complex (prevent addition of
aa to peptide), alter
cytoplasmic membrane,
static
macocyclic lactone ring with
14-16 atoms where
deoxysugars are attached;
time dep.
MOA: Static, Inhibit RNA-
dependent CHON syn at
chain elongation, bind 50s
block transpeptidation and
aminoacyl translocation
Reversibly binds 50s
prevent peptidation inh.
CHON syn.
Binds D-alanine-D-alanine
block glycopep polymer,
Cidal inh.
Transglycosylase prevent
elong. of peptido and x-link
(time dep) x cell wall
Synthetic fluorinated
analogue of nalidixic acid; all
are GABA inhibitors account
for CNS tox.
MOT: Inhibit DNA gyrase
(topoisomera II,IV) inh
DNA synthesis
Nitro grp Reduced
intracellularly interact w/
DNA loss of helical DNA
syndrome w/ alc.
DI: nephrotox (methoxyflurane), tetra
effects (antacids, iron, ZnSO4, bismuth
subsalicylate) dec. doxy effects (chelators,
barbi, CBZ, phenytoin), effects
(contraceptives, digoxin), Li tox, lactic
acidosis w/ phenformin, antag with pen
CYP1A2 & CYP3A3/4 inhibitors and dec.
hepatic metabolism of other drugs
DI: effect & toxicity of theophyllines, oral
anticoags, digoxin, CBZ, cyclosporine, ergot,
arrhythmia / Torsades de pointes when
given w/ astemizole, amiodarone,
haloperidol and terfenadine (Erythro &
clarithromycin inc. QT interval)
Base: enteric coated to prevent gastric acid
destruction, Stearate: better abs&bioav,
Esters: < acid labile vs 2 above, Estolate:
higher plasma level ut only 20-30% active,
causes cholestatic jaundice, Ethyl
succinate : >rapid hydrolysis vs estolate
Not preggy, w/ active metab: 14-
hydroxyclarithromycin eliminated via urine
15-member lactone ring by addition of
methylated nitrogen into the lactone ring,
hence doesnt inhibit CYP450 so no DI
static/cidal (depends on conc, infxn site,
org), time dep
DI: NMJ block (w/ curareform drugs),
lincomycin w/ Kaolin pectin
DI: nephrotox (AMG, ceph), ototox
(AMG), digoxin, synergistic with
streptomycin and gentamicin against
enterococci
DI: tox (theophylline), conc (caffeine &
warfarin via interfering w/ hepatic metab),
abs (antacids); prolong QT (inc risk if
hypoK, hypoMg, Ia & IIIa antiarrhymic drug,
macrolides, anti hpn, CNS drugs)
DI: tox (warfarin, phenytoin, lithium,
cimetidine), disulfiram-like rxn (avoid
alcohol on & until 48h after), organic brain
AMG coz static
CI: hps, preggy, kids under 8, renal failure except
doxycycline; ADR: freq: GI, bone growth retard,
permanent pigmentation, teeth hypoplasia;occ:
malabsoprtion, enterocolitis, photosensitivity
Oral, variable abs w/ food,
(demeclocycline), azotemia (except doxy), liver
divalent cations, antacids; not
D damage (IV in preg & px w/ renal dxs), esophageal
CNS, bound to bones & teeth,
ulcer, vestibular tox &hyperpigment
liver, spleen; excr in bile & urine
(minocycline); rare: allergy, bld dyscrasia, inc
intracranial pressure in infants, diabetes insipidus
(demeclocycline), blur vision, Fanconi-like synd
(outdated tetras), acute nephritis (minocycline)
No BBB, hepatobiliary
elimination
CI: hepatic impairment, hps to erythromycin
ADR: occ: Stomtitis,cholestatic jaundice, GI
irritation, rare: hps, pseudomem colitis,transient
deafness, inc QT interval (torsades de pointes),
ventricular tachy, aggravate M. gravis,
fatty acid R. & better absorbed
Motilin- activates duodenal & jejuna receptors to
B (Stearates & ester); Not in brain
initiate peristalsis. Erythromicin & esters (po,IV)
& CSF, excr bile, t1/2=1.5h
activates motilin receptors and cause
uncoordinated peristalsis with resultant A, N, V
C T1/2=6h, lesser GI SE
T1/2=68h, qd dosing shorter
B duration of therapy, > tx
penetration, <GI SE
Oral, CHON bind, No BBB, D, allergy, pseudomem colitis (C. difficile), toxic
B conc in bone & bile & urine, elim megacolon, blood dyscrasia, hypotension, impair
via hepatic metab liver fxn, esophageal ulcer
Freq: Thrombophlebitis, fever,chills, Occ: hearing
IV, not oral, inflamed BBB (need damage (CN8) if cont high dose >10d, allergy,
high dose coz low&erratic neuropenia, renal damage; rare: peripheral
C
penetration), 90% urine (beware neuropathy, red neck syndrome (flushing of
if w/ renal dysfxn), t1/2= 4-5h upper chest due to histamine release, prevent by
slow IV over 60-90mins) rash, hypotension
conc dep, cidal
Not for preggy & kids <18 -damage devl cartilage
Oral, ok pr bound, Vd CSF,
ADR: occ:N, V, Abd pain, D, dizzy, HA, tremor,
40% elim in urine (oral dose)
macular rash, candida infxn, inc eo, dec neutro,
70%(IV), 4 active metabolites
C inc hepatic enz activity, inc serum crea; rare:
Oral, poor CSF, t1/2=9h
Tendinopathy (Achilles tendinitis), CNS, hepatic
respi fluoroquinolone; Oral,
failure, hyper/hypoglycemia, Torsade de pointes
t1/2=7-8h
(least w/ Cipro!)
Oral, good CSF
B Enters abscesses w/ Little pr CI: hypersensitivity, 1st trimester
binding, liver metab, excr in N, HA, dry metallic taste, V, D, weakness,
urine & feces, NO mutagenic, insomnia, stomatitis,vertigo,paresthesia,phlebitis
 Anti-bacty: tetanus, anaerobe infxn, G. vaginalis, H. structure strand breakage syndrome (disulfiram), Metro effect w/ ,rash, dark urine, seizure, CNS, pancreatitis,
tumorigenic, teratogenic effect
pylori, antibiotic induced pseudomem colitis CHON synthesis & cidal phenobarbital ataxia, encephalopathy, leucopenia
DI: effect (sulfonylurease, anticoags, Not for topical or Streptococcal sore throat
TMP:SMX 1:5 useful becomes cidal like cotrimoxazole Oral, all tx& fluids, CSF, metab
phenytoin), antileukemic effect of CI: hps, preggy, lactation, infants <2mos, renal dxs
Systemic (mostly for cotrimoxazole): UTI, Nocardia, Interfere w/ folic acid liver, excretion urine
X. Sulfonamide Sulfas mercaptopurine, megaloblastic anemia (use only soluble sulfas or sulmonamide
Shigella, respi, Pneumocystis carinii, typhoid (alt to synthesis, Compete with Acetylated metabolites insoluble
(methotrexate), dec. effect & inc. mixtures),
chloram), orchitis prostatitis, chlamydia (alt to tetra, PABA DHF static in urine renal damage,
nephrotox (cyclosporines), inc. phenytoin Caution in G6PD def, renal/liver dysfxn
erythro), Toxoplasma (sulfadiazine+pyrimethamine), crystalluria
tox., MetHb (prilocaine/lidocaine cream) Inj vehicle contains benzyl OH & Na metabisulfite
Falciparum (sulfadoxine+pyrimethamine/sulfalene+
Trimethoprim Inhibit DHF reductase w/ metabolites
pyrimethamin), dermatitis herpetiformis (sulfapyridine
Local: ulcerative colitis & ileitis (oral sulfasalazine), eye ADR:Rash, N, V, hemolysis in G6PD, megalo-
infxn (sulfacetamide Na ophthalmic ointment), Sequential inhibition of Concentration attained in blood & tissue Tablet, suspensin, cream, blastic anemia, granulo/thrombocytopenia,
Cotrimoxazole C
prevent colonization in burns (prefer: Ag sulfdiazine) folate pathway Cidal (SMX+TMP) is 20:1 eyedrops pseudomem colitis, kernicterus, SJS, CNS, renal
problems, ataxia, pancreatitis, hepatotox, fever
1. Short/Intermediate Axn --- sulfisoxazole (soluble), sulfadiazine (highly active, low solubility & pr binding, high bld & CSF levels), Sulfamethizole (soluble, rapid elim,
Rapid absorption & excretion
for UTI), Sulfamethoxazole (<sol, >bld levels, slower enteric absorption, liver metab & renal excr, combo w/ trimethoprim co-trimoxazole)
Rapid abs, slow exc, pr binding
2. Long Axn--- sulfadoxine (t1/2=7-9days), sufalenes (sulfametopyrazine), both used in combo w/ pyrimethamine
extensive tubular reabsoprtion
3. Lumina--- sulfsalazine (absorbed in its parent form as sulfapyridine, only for ulcerative colitis & regional enteritis), Sulfguanadine, Sulfasuxidine, Sulfathalidine Poor GI abs
4. Topical--- sulfacetamide Na (optha ointment), Silver sulfadiazine (sulfa acts as vehicle for Ag release that exert antibact effect in burn cases, lesser SE vs mafenide); Metabolic acidosis due to carbonic anhydrase
Mafenide acetate (topical tx for burns but >SE) inhibition (Mafenide acetate)
Irreversible binds 50s
XI. Miscellaneous
complex to form stable
1. Streptogramins
Cidal vs GP expt E. faecium, MRSA, multiple drug quinupristin-ribosome- IV, no CNS nor placenta, taken
macrolactone belong to
resistant GP dalfopristin 3o complx up by macrophages, liver metab, ADR: Infusion pain,arthralgia-myalgia syndrome,
macrolide-linco-streptogramin DI: cyclosporine blood conc.
Prevent resistance reserved for serious, life- CHON syn t1/2 1.5h but prolong PAE (upto rash, jaundice
Quinupristin threatening systemic infection w/ no alt therapy Inhibits chain elongation 10h)
Interfere w/ peptidyl
Dalfopristin
transferase
substrate for chromosomally
encoded multidrug efflux
effective against tetracycline resistant strains pump pf Proteus and Pseudo
poor oral, should be IV, good tx
For skin inf; intraabdominal inf., multidrug resistant intrinsic resistance to all
semisynthetic der. of minocycline; broad & intracellular penetration, wide
2. Glycylcycline - tigecycline nosocomial inf. (MRSA , extended spectrum tetra and tigecycline
spectrum VD, elim via biliary, very low
betalactamase producing GN, acinetobacter, VRSA, Not a substrate for efflux
conc in urine
enterococci, GP and GN anaerobes) pump expressing organisms
(GN, staph) & ribosomal
protection CHONs by GP
Hematologic (thrombocytopenia most common,
Cidal to Strep, static to other GP, vanco-resistant neutropenia) MAO inhibitor, serotonin syndrome
Rapid oral,metab in liver, excr
3. Oxazolidinones - Linezolid E.faecium, multiple drug resistant GP, nosocomial Inhibit early CHON syn DI: HPN (tyramine rich foods) C (fever, agitation, tremor, mental status changes),
urine, tablet, suspensin IV
pneumonia & skin infxn risk of severe hpn if with tyramine rich food,
pseudoephedrine, phenylproplanolamine