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Penicillin SOA

Indxns DOC
SOA:s.pyogenes,peptostreptococci,streptococci,treponema pallidum
*note: inactivates AMG, separate IV PCNs from concurrent adm
DOC
pharyngitis (strep throat)
rheumatic fever
dental px/infxn
bicillin LA (pcn G benazthine) for syphilis
Penicillinase-resistant PCNs
SOA/DOC: MSSA
*No dose adj for renal impairment (all other PCNs need to be dose adj)
oxacillin unique: hepatotoxicity
nafcillin: neutropenia
PO forms: dicloxacillin,cloxacillin take on empty stomach
Aminopenicillins
SOA: strep pneum, enterococci, listeria, H. infl,M. catarralis
ampicillin=DOC enterococi & listeria
Amoxicillin: 500mg PO q8 or 875 bid
40-90mg/kg/d for AOM (1st line agent)
h. pylori
2gm dental px
Beta-lactam combination agents
SOA: staph, strep, enterococcus, HNPEK, B. frag
Zosyn/Timentin: (+) pseudomonas
Unasyn: DOC for animal/human bites
(also better enterococcal activity)
Timentin: high sodium load and weaker enterococcus and pseudomans vs zosyn


BQ Focus: Augmentin (amoxicillin/clavulanate)
indxn: acute bacterial sinusitis, AOM, animal/human bite wounds,LRI by susceptible organisms (strep pneumo)
*additonal coverage of beta-lactamase producing M.catarr,H. influen
general dosing: child>40kg and adults: PO 250-500 q8h OR 875mg q12h
Tabs: 250, 500, 875mg
do not use 875mg tabs in Crcl <30
Chewable/Susp: 200, 400: BID
Susp: 125, 250: TID
XR: 1000mg: 2 tabs BID; not for <16yo, CI in Crcl <30
Carbapenems
gram pos/neg,pseudomonas, anerobes
*Primaxin: dose dep sz, Q6-8H
*Merrem: longer half life, less sz potential
*Doribax: Q8H, SJS, more potent against pseudomonas in vitro vs imipenem
*Invanz: qday, no activity against pseudomonas, acinetobacter, less active against gram-positive
DOC: ESBL producing GNRs such as E.coli, klebsiella
*used for multiple drug resistant gram negative infxns
*cross sensitivity w/PCN is ~50%
Aztreonam
monobactam
SOA: AEROBIC GRAM (-) including pseudomonas ONLY
indxn: Rescue drug for AMG nephrotoxicity
Macrolides
indxn: CAP, PCN-allergic pts AOM, when TCN are CI (pregnant, children)
suprress RNA dep protein synth
lipophilic, inc concentration in MAC,PMNs, greater resp tract conc vs serum
Not well penetrated to CSF
Erythromycin salts
SOA: MSSA, strep,mycoplasma, chlamydia, M. catarr leginoella,bordetella pertussis
*Not H.influenza, enterococci
Clinical use:
gastroparesis: 250mg EES or 500mg base QID
*DOC for legionaire's, whooping cough,mycoplasma pneumoniae
-AOM w/sulfisoxazole-->which provides coverage for H.infl
-PCN-allergic for strep, syphilis, gonorrhea
(except neurosyphilis MUST desensitive for PCN)
400mg EES = 250mg base or stearate
Major ADR: N/V
ery-base/stearate: dec abs w/food
EES: inc abs w/food (take after meal)
Max daily dose: 4gm
ototoxicity w/OD, arrhythmia
*Potent cyp 3A4 inhibitor
Biaxin
clarithromycin
SOA: staph, strep,M.catarr (+) H.influ, H.pylori, MAC
Clinical uses: CAP,MAC px/tx, pharyngitis, sinusitis,
Prevpac ( biaxin 500mg bid, w/amox 1gmbid, prevacid 30mg qd)
CI in pregnancy
Available PO only: 250-500mg bid, 1000mg XL qd w/food
*Less potent CYP3A4, caution DDIs with HIV meds
Renal adjust
Metallic taste
Zithromax
azithromycin
SOA: gram pos, atypicals, M.catarr, H. influe
(+) STDs (N.gonorrhea, chlamydia, ureaplasma)
Z-pak: 500mg x1, 250mg qd x 4d
Tri-pak: 500mg qd x 3d
Z-max: 2gm/60ml ER susp single dose for gonorrhea (redose w/in 1 hr if vomit)- take on empty stomach;poorly tolerated-->prefer Roceph, doxy?
1gm single dose for chlamydia
CAP: 500mg IV/PO qd x 7-10d
1200mg qwk for MAC px
* little to no CYP inhibition
Erythromycin, Clarithromycin
DDIs
CYP 3A4 inhibitors
inc serum lvls: CBZ, VPA, PHT, theophylline, cyclosporine, tacrolimus,RTV, warfarin, statins
Caution: QTc prolongation (ery,clar)
FQs
MOA: DNA gyrase inh, bactericidal
ALL FQ DDI: multivalent cations d/t chelation -->dec cmax by 60%
BBW: Tendonitis/rupture (inc risk in >60yo, concurrent steroid, transplant pt), avoid in children/adolescent <18 yo
Preg Cat C
ADR: nvd, rash, photosensitivity, seizure/cns stim, qtc prolongation (most w/moxi (levo))
Norfloxacin (Noroxin)
UTI, gonorrhea,spont bact peritonitis px, no indxn for RTI (no systemic!), no providencia coverage
SOA: gram - aerobes (urine)
1st gen
Ciprofloxacin (Cipro)
SOA: excellent gram neg incl pseudomonas, poor gram pos act, min atypical legionella
*Cipro best pseudomonas act
Dosing: Q12H
250-750mg PO q12
200-400mg IV q12
500mg XR qd x 3d for UTI
1000mg XR qd x 7-14d for compl UTI
2nd gen
Most DDIs: theophylline, warfarin, dig
potent CYP1A2inh, weak 3A4 inh, pgp sub
Ofloxacin (Floxin)
most active against chlamydia.
also tx gonorrhea, UTI
2nd gen
Levofloxacin (Levaquin)
SOA: gram neg, gram pos (better s.pneumo act vs cipro), excellent atypical activity (chlamydia, mycoplasma spp)
*PNA, UTI
Dosing: 250, 500m 750mg PO/IV qday
3rd gen
Moxifloxacin (Avelox)
Dosing: 400mg PO/IV qday
*Only non-renal FQ, no need to renal dose adjust
*also some anaerobic act, but less potent against pseudomonas
3rd gen
Worst QTc prolongation risk, rare hepatic injury
CI w/geodon
Gemifloxacin (Factive)
CAP, ABECB
better gram pos, good for pcn/cipro resistant strep pneumo
*Rash 2.8%
Risk/higher incidence in women <40yo, treatment duration (7d 9%, 14 d 23%)
Gatifloxacin (Zymaxid) 0.5%
bacterial conjunctivitis
day 1: 1gtt q2hr while awake (max 8x/d)
day 2-7: 1gtt 2-4x/d while awake
3rd gen
Aminoglycosides
MOA: ionic interaction w/ cell surface, energy dep uptake, binds to 30s ribosome/inh protein synthesis
*SOA: Gram neg incl pseudomonas, acinetobacter, mycobacteria
Synergy only for gram pos: mssa, staph epi, enterococcus
ADRs: nephrotoxcity (8-26% onset ~day 5; higher risk w/concurrent nephrotoxic: vanco, ampho, foscarnet, radiocontraset), ototoxicity, neuromuscular block (rare/CI in myasthenia gravis)
(high renal cortex, inner ear penetration)
Urine conc exceed peak plasma lvls 25-100x w/in 1hr of drug admin, and ext PAE
*DDI: physically incompatible w/PCNs
Gentamicin
Tobramycin
Gent=1st line AMG for gram neg infections
Both Dosing: 1 7mg/kg
*3-5mg/kg traditional
*5-7mg/kg HDQD
peak: 5-10 mcg/ml and tr<2
Synergy: pk 3-4mcg/ml; tr <1

TOBI used for CF,more active against pseudomonas vs gent
Amikacin
MAC, TB (non-fda approved indxns)
Dosing: 7.5-15mg/kg
Pk: 20-30mcg/ml tr <10 (8)
Neomycin
Indxns: gut sterilization to prep for GI sx, adjunct to tx hepatic encephalopathy (ammonium detoxicant), tx of diarrhea d/t e. coli
amg for oral, topical use
Vancomycin
SOA: all gram positives, MRSA/MRSE, coag-neg staph DOC
Clinical use: PCN/ceph allergic pt w/gram pos infxn
Oral vanco: 2nd line agent for c.diff mild-mod
dosing: 125-500mg PO QID x 7-10d
Used together w/AMG for endocarditis
SEs: nephrotoxicity, ototoxcity, neutropenia
Tr: 10-20mcg/ml
BQ: red man syndrome d/t his release, rapid infusion cause hypotension
Tetracycline
SOA: propionibacterium acne, listeria, protozoa, tick borne (rikettsia,borrelia), h. pylori, chlamydia
Dosing: 250-500mg Q6H
PO only
Limited strep
No MSSA/RA!!
Minocycline
SOA: strep(no enterococci), staph, atypicals, tick borne, gram neg
Clinical use:
CA-MRSA, SSTI, Acne
Dosing 100mg q12h
* Lupus
*dizziness/itransient vestibular toxicity
Doxycycline
(Vibramycin)
Periostat
Oracea
SOA: same as mino + covers enterococci,not c.diff
CA-MRSA/PNA, acne, STDs (syphilis, uncompl gonorrhea, chlamydial): 100mg PO/IVq12h
malaria px 100mg daily 1-2 d prior to travel, then continue daily x 4 wks after leave area
periodontitis: 20mg PO bid
rosacea: 40mg qd
* reflux esophagitis (upright 30min)
Better in renal imp vs TCN
(no renal adjustment)
Demeclocycline
SIADH (unlabeled use)
900-1200mg/d
tetracylcine class DDIs,
contraindications, precautions
DDI: divalent cations; separate dose from milk/antacids/iron by >2hrs (dec absorp 50%),
oral contraceptives (use back-up), bile acid seq (cholestyramine,coletipol)
Photosensitivity: more common in TCN
Preg cat D: affect skeletal/bone growth of fetus
Tooth discoloration: CI in children </= 8 yrs old
ADR: hepatotoxicity > risk in those w/pre-exisiting imp
Renal imp caution: ARF, azotemia dose adjust (EXCEPTION DOXY b/c elim via hepatobiliary)
Other DDIs: anticonvulsants, warfain potentiation

*Vertigo/lupus: minocycline
Tygacil
tigecycline
SOA: broad-spect inclu anaerobe and atypical but NO COVER pseudomonas!
clinical use: MRSA/MRSE, VRE
* not for sepsis
*tooth discoloration (der of minocycline)
Bactrim (400mg/80mg(
Bactrim DS (800/160)
Septra DS
Sulfatrim (oral susp)
sulfamethoxazole/Trimethoprim
general oral: 1-2 DS (800/160) tab Q12-24h
IV: 8-20mg TMP/kg/day Q6-12h
Renal adjust: Crcl <30 by inc interval
UTI,PCP px/tx, CA-MRSA
IV dose based on TMP
*DOC for nocardia (GPR), unlabeled use opportunistic
SOA: PCP (DOC?), s. maltophilia (DOC), toxoplasma, MRSA, HPEKSS
No cover: enterococci, pseudomonas, or anaerobes
Preg cat C (avoid in 1st, last trimester--> kernicterus), SJS/TEN photosensitivity , report rash
Crystalluria (elim via tubular secretion), ADRs also include: Monitor: Scr, bun, hyperkalemia at high doses, hematologic (dose related)
Inform if HIV + (more skin rxns), G6PDef, liver or kidney dz
DDI:SMP: CYP 2C9 inh/substrate; TMP CYP 2C9 inh, substrate of 2c9, 3A4
sulfonylurea protein binding displacement, PHT/Fos dec clearance d/t inh met by TMP, MTX toxicity, warfarin (PB, dec vit K)
TMP: prostatic tissue concentration >2-3x plasma levels
Clindamycin
(Cleocin HCl/Pediatric/Phosphate)
SOA: strep, staph (incl MRSA) and anaerobes. NOT enterococci, no gram neg aerobes, no atypicals
But does covers: T. gondii, PCP, gardnerella vaginalis
Lots of off label use: PCP, toxoplasmosis
Alternative dental px for PCN-allergic pts, anaerobic infxns, CA-MRSA, endocarditis px, colorectal sx px
MLS phenotype
D test to check for inducible resistance
Biliary elimination/enterohepatic recirculation
SE: associated with C.diff, report severe diarrhea/DNU antidiarrheals
Flagyl
Flagyl 375
Flagyl ER
metronidazole
SOA: anaerobes; trichomonas vaginalis, giardia
DOC: c. diff mild-mod: 500mg q8h x 10-14d
Trich: 2gm single dose (can take 1 gm bid) or 250mg TID x 7d or 375mg bid x 7d
Bacterial vaginosis: 750mg ER PO QD x 7d; or 500mg bid regular release
anaerobic infxns: oral,IV: 500 q6-8h NTE 4gm/d
Giardia: 500mg bid x 5-7d
PUD (h.pylori) in combination
Colorectal sx px: IV
CI: 1 st trimester of pregnancy
Peripheral neuropathy w/long term
Metallic taste
SE/counseling:
1. disulfiram rxn (no etoh during and for 3d after finish)
2. darkens urine
3. GI upset transient
Nitrofurantoin
(Macrobid, Furadantin, Macrodantin)
SOA: gram pos: S. saprophyticus/aureus, E. faecalis and all UTI gram neg except pseudomonas, proteus
Rate of absorption differs w/r/t micro vs macrocrystal (macro more slower rate so better tolerated)
Take w/food (severe GI upset: most potent nausea), HA, sedation
Dicoloration of urine
CI: CrCl <60ml/hr (abs <40)
DDI: probenecid dec clearance of NTF and inc levles
*Pulmonary fibrosis w/chronic prolonged use
Zyvox
linezolid 600mg PO/IV q12h
SOA: VRE, MRSA, other gram positives
SEs: dec PLTs, anemia, peripheral neuropathy
CI: Concurrent or w/in 2 wks of MAO inhibitor,uncontrolled htn, tyramine food
Cubicin
lipopeptide, ca dep insertion of tail into cell memb--> rapid depolarization--> efflux of K/destroys ion conc of membrane--> cell death
daptomycin
Dosing: 4-6mg/kg IV daily in NS (not compatible w/D5W)
Renal <30: Q48H
SE: myopathy (monitor CPK)
Clinical use: VRE unreponsive/intolerant to Zyvox, synercid, CSSTI
NOT indicated for PNA (inactivated by lung surfactants)
FDA approved only for: CSSTI and bacteremia
No CYP interactions
Concentration dep killing/cidal, PAE: 6hrs
Synercid
inh protein synth (seq binding on 50s ribosome)
dalfo alters conformation incr afficity for quinu--> tertiary complex
quinupristin/dalfopristin
SOA: VRE (no faecalis act), MRSA, bacteremia, SSTI
Dosing: 7.5mg/kg IV q8H
No renal adj
NOT active against e. FAECALIS (better VRE act vs. zyvox)
SE: venous irritation (phlebitis), arthralgia, myalgia, hyperbili
DDI: CYP3A4 inh (weak)
Synergy w/ vanco : combo for recalcitrant infxns
Mepron
atovaquone
Tx PCP: 750mg bid w/food x 21 d
Px PCP: 1500mg qday w/food
MOA: inhibits electron transport in mitochondria resulting in inh of key metabolisc enzymes resp for synth of nucleic acids, ATP
Antiprotozoal
Chloramphenicol
Bacteroides, H,infl, Neisseria meningitidis,VRE, salmonella, rickettsia

IV only 50-100mg/kg/d Q6H; max 4gm/d
Aplastic anemia
gray baby syndrome
Pentamidine
Miscellaneous/antiprotozoal
Tx/Px of PCP
inhalation, IM,IV
less used d/t association w/: Pancreatitis
Type I DM
Xifaxan
rifaximin
indxn: travelers' diarrhea caused by noninvasive e.coli; reduction in the risk of overt hepatic encephalopathy recurrence
rifampin like drug, inhibitis bact RNA synth by bind to bacterial DNA-sep RNA polymerase
NS only IV stability
Amp, unasyn, oxacillin, primaxin, meropenem, erythromycin, daptomycin,
capsofungin
D5W only IV stability
Amphotericin, synercid, bactrim, rifampin
Protect From Light
Amphotericin, Cipro, doxy, bactrim, flagyl, linezolid, rifampin
Short-term stability
Bactrim,primaxin,meropenem, rifampin
Potentiates INR
Bactrim, macrolides (except zithro), cipro, flagyl, tigecycline
Decreases effect of oral contraceptives
Tetracyclines, PCNs, Bactrim, Flagyl, Rifampin, griseofulvin
Tamiflu
Influenza A & B, H1N1 influenza
Tx: 75mg bid x 5d
Px: 75mg qd x 10d
MOA: neuaminidase inhibitor
Start w/in 2 days of sx
Oral suspension >1 yo
Px not recommended for <3mo old
<12months: 3mg/kg/dose once daily
Relenza
zanamivir
influenza A & B, H1N1
Tx: 10mg inhalation BID
Px: 10mg inh qd
Caution: asthma, COPD
Cytovene IV
ganciclovir
PO form used for CMV px in transplant and HIV pts
SE: neutropenia
formulations: PO, IV, intravitreal implant, gel
Valcyte
valganciclovir
10-fold higher BA vs oral ganciclovir and similar BA vs IV ganciclovir
CMV retitinitis: 900mg bid x 21 days
PX of CMV s/p transplant: 900mg qd w/in 10d of transplant; continue until 100days (heart/kidney) or 200 days (kidney) post transplant
PO, oral soln
Boxed warning: Ganciclovir: Potential teratogen and cause aspermatogenesis -->contraception during and 30 days after, males barrier during and 90 days after
MOA: rapidly converted to ganciclovir in body, phosphorylated, then inh viral DNA synthesis
Vistide
cidofovir
indxn: Only for CMV retinitis in AIDs
CI: Scr >1.5
BBW: dose dep nephrotoxicity, renal failure,proteinuria,neutropenia,possibly carcinogenic and teratogenic, may cause hypospermia
*Adm must be accompanied by oral probenecid and hydration w/ IV normal saline
-Use in pt w/or at risk for myelosuprresion
But monitor for neutropenia
MOA: cidofovir disphosphate active metabolite; suppresses CMV repl by sel inh of viral DNA synth, incorporation of cidofovir into growing vDNA chain reduces rate of vDNA synth
Foscarnet
CMV retinitis in AIDs
Acyclovir-resistant HSV
IV: ~40-80mg/kg/dose Q8-12h
induction, maintenance
SE: renal failure, seizure d/t electrolyte imbalance, myelosuppression,
*Renal adjust
Peripheral vein adm: final concentration must not exceed 12mg/ml
Zovirax
acyclovir
Tx genital HSV:oral: 1st episode 200mg 5x/d x 10d or 400mg tid x 7-1-d
Recurrent: 200mg x 5x/d x 5d or 400mg tid x 5d or 800mg bid x 5d, or 800mg tid x 2d
Px: 400mg bid
*Herpes zoster: 800mg 5x/d x 7-10d
*Varicella-zoster (chickenpox): >40kg: 800 mg/dose QID x 5d
IV: HSV initial episode/severe: 5mg/kg/dose Q8H x 5-7d follow w/oral tx to complete at least 10days tx

Zoster: immuncompromised: 10mg/kg/dose Q8H x 10d
Famvir
famciclovir
~120-500mg PO BID
zoster, HSV,cold sores
*renal dose adjust for CrCl 40-60
converted to penciclovir (prodrug) in intestine and liver,phosphorylated, competes w/deoxyguanosine triphosphate to inh HSV polymerase
*neutropenia
Valtrex
valacyclovir
genital herpes: 1st episode 1gm bid x 10d
recurrent: 500mg bid x 3d
Zoster: 1gm TID x 7d
higher bioavailability vs acyclovir
Converted to acyclovir through 1st pass effect
Hepatitis B tx
lamivudine (Epivir/HBV)
adefovir (Hespera) NTRTI: renal toxicity
Telbivudine (Tyzeka) NRTI : myopathy
Tenofovir (Viread) NTRTI: renal tox, BMD
entecavir (Baraclude) NRTI: lactic acidosis, hepatomegaly w/steatosis w/ nucleoside analogs
-other BBW: severe, acute excarbation of hep b may occur upon d/c of antihepatitis b tx.
Hep C tx
Ribavirin + Pegylated IFN
ribavirin: hemolytic anemia
CI: in renal impairment

Inhaled ribavirin: used for RSV