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NR565 Week 5 Study Outline

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Many questions are written to assess your clinical application of the material from the textbook, in real-world scenarios. Chapter 24: Drugs used in treating infectious diseases (p. 692-760) SEE DRUG CHART BELOW Know the following for each drug class (penicillins, cephalosporins, fluoroquinolones, lincosamides, macrolides, sulfonamides, trimethoprim, nitrofurantoin, lipoglycopeptides): • • Spectrum of coverage for various organisms • • Pharmacodynamics • • Pharmacokinetics • • Pharmacotherapeutics • • Clinical indications & dosing • • ADRs • • Monitoring • • Patient education Antimicrobial resistance Treatment of Group A and Group B beta streptococci Cross sensitivity with cephalosporins anaerobes and gram negative (MSSA, strep, H.flu, E.coli, Klebsiella, Neisseria meningitides); amoxicillin, ampicillin; combined with betalactamase inhib Pcnase-resistant – (pcnase staph, strep, MSSA); not effective against MRSA; cloxacillin, dicloxacillin, methicillin, nafcillin, oxacillin Antipseudomonal – gramneg bacilli (pseudo aeruginosa, enterbacter, morganella); piperacillin, ticarcillin binding, well distributed, inflammation enhance distribution, crosses placenta/breast milk Metabolism – minimal metab except for nafcillin/oxacill in Excretion – primarily unchanged in urine, caution in renal insufficiency (increase half life) infectio - Seizures ability - Decreas oral contrap ves effectiv - Interstit nephriti * Severe, type I allergic reaction to cephalospori carbapenems, o beta-lactamase inhibitors may contraindicate u penicillins. Cephalosporins – 1st Generation (Cephalexin) & 2nd Generation (Cefuroxime) 3rd Generation (ceftriaxone) & 4th Generation (cefepime) 1st – narrow spectrum 5th – broad spectrum Bactericidal Increase in gram neg up the generations and decreases in gram pos. Treat surgical prophylaxis, resp tract infx, strep pharyngitis/sinusi tis, CAP, skin, soft tissues, bones/joints, UTI (2nd line for kids), STI First  gram pos and limited gram neg; doesn’t enter CSF, staph aureus, strep, pna/resp infx (cephalexin, cefazolin) Second  gram + and H. flu, more potent, broader spectrum, gonorrhea, resp infx (cefaclor (CAP), cefziroxine) Third  some gram + and -, not active against MRSA, effective against pseudomonas, less freq dosing, crosses BBB with inflammation Absorption  oral, GI tract, rate of absorption delayed by food, IM – absorbed by muscle Distribution  widely distributed to most tissue, variation in protein binding, penetration CSF varies by generation Metabolism  hepatic metabolism – insignificant Excretion  In pregnancy d/t increase fluid  shorter half life, lower serum levels and larger Vd Lactation  safe Pediatrics  in neonates immature renal fx causes increased half life and accumulation; kids – varies by drug - GI distuban (C.diff) - Alterati blood clotting - Combin with alc (disulfir rxn – flushing dizzines n/v, coa problem - Nephrot ty - Superin n - Renal/h c dysfun extends halflife - Anaphy rxn to p don’t gi cephalo acid; Metabolism – metabolized in liver, erythromycin, heavily metabolized by CYP3A4 Excretion – excreted in feces and urine, caution with clarithromycin increased renal excretion halved Pregnancy - Erythromyci n: cat B - Clarithromy cin: cat C - Azithromyci n: cat B Lactation - Safe Pediatrics - Safe over age 6 months - Rash, fe eosinop - Metab. Interacti esp with erythro - Prolong QT syndrom maligna arrthym Interactions - Colchic - Warfari - Digoxin increase effect Lincosamides (clindamycin - Cleocin) Bacteriostatic in usual doses; suppresses protein synthesis – binds to 50S subunit of the bacterial ribosome First line tx in MRSA, primarily gram +, some anaerobic pathogens Absorption – good oral absorption Distribution – highly protein bound Metabolism – metabolized in liver Excretion – excreted in bile and urine Cautions - Asthma - Severe allergies - Severe renal/liver impairment Pregnancy - Category B - Okay for 3rd trimester Lactation - Present in breast milk – weigh risk/benefit Pediatrics - Severe infx only - GI symp - Dizzine vertigo, - C.diff ( serious Quinolones (Levofloxacin, Ciprofloxacin, Moxifloxacin) Bactericidal for DNA gyrase (needed to synthesize bacterial DNA) Broad spectrum; extensive gram -; later generations increased activity against gram +; only moxifloxacin has activity against anaerobic bacteria; PO and IV formulations; resistance already occurring from inappropriate use Absorption – well absorbed after PO admin, IV and oral  similar serum concentration Distribution – widely distributed; high tissue, urinary prostate, sinus and lung penetration; variable protein binding; moderately Cautions - Renal dysfunction: can cause increase half-life with majority of drug excreted unchanged in urine - CrCl 50mL/min: adjust dosage - Cautious in patients - GI - CNS - Phototo - Skin - Superin n - Muscul etal - Renal - Diabetic - Serious effect: dysrhyt

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NR565 Week 5 Study Outline

Many questions are written to assess your clinical application of the material from the textbook, in real-world
scenarios.

Chapter 24: Drugs used in treating infectious diseases (p. 692-760) SEE DRUG CHART BELOW

Know the following for each drug class (penicillins, cephalosporins, fluoroquinolones, lincosamides, macrolides,
sulfonamides, trimethoprim, nitrofurantoin, lipoglycopeptides):

• • Spectrum of coverage for various organisms

• • Pharmacodynamics

• • Pharmacokinetics

• • Pharmacotherapeutics

• • Clinical indications & dosing

• • ADRs

• • Monitoring

• • Patient education

Antimicrobial resistance
Treatment of Group A and Group B beta

streptococci Cross sensitivity with cephalosporins




Category Bacteriocidal or What do they Pharmacokineti Pregnancy Adverse
Bacteriostatic Treat? cs Category? Safe in
(Indications) pediatrics?
Safe in Lactation?
Penicillins Bacteriocidal; Pcn - Treat Absorption – - Catergory B - Hyp
(PCN and Amoxicillin) inhibits synthesis aerobic and gram from GI tract, - Safe in y
of bacterial cell positive. Red depends on lactation - Sup
wall Book recommends agent, ph of - Safe in nn
Used in tx bact. URI, penicillin for stomach/intesti pediatrics - GI
pharyngitis strep, otitis Group ne, presence of - Does not distu
media, sinusitis, pna, STI, A beta streptococci food; high cross BBB s
wound infx & for Group doses can cause unless - Ras
B beta streptococci GI inflammatio (ma
due to low upset/diarrhea n lar)
resistance - Cha
Distribution – rena
Aminopcn – treat varies in func
gram posivite protein n

, anaerobes and binding, well infe
gram negative distributed, - Seiz
(MSSA, strep, inflammation abili
H.flu, E.coli, enhance - Dec
Klebsiella, distribution, oral
Neisseria crosses cont
meningitides); placenta/breast ves
amoxicillin, milk effe
ampicillin; - Inte
combined with Metabolism – neph
betalactamase minimal metab i
inhib except for
nafcillin/oxacill * Severe, ty
Pcnase-resistant – in allergic reac
(pcnase staph, to cephalosp
strep, MSSA); not Excretion – carbapenem
effective against primarily beta-lactama
MRSA; cloxacillin, unchanged in inhibitors m
dicloxacillin, urine, caution contraindica
methicillin, in renal penicillins.
nafcillin, oxacillin insufficiency
(increase half
Antipseudomonal – life)
gramneg bacilli
(pseudo
aeruginosa,
enterbacter,
morganella);
piperacillin,
ticarcillin
Cephalosporins – 1st Bactericidal First  gram pos Absorption  In pregnancy d/t - GI
Generation and limited gram oral, GI tract, increase fluid  distu
(Cephalexin) & Increase in gram neg; doesn’t enter rate of shorter half life, (C.d
2nd Generation neg up the CSF, staph aureus, absorption lower serum levels - Alte
(Cefuroxime) generations and strep, pna/resp infx delayed by and larger Vd bloo
3rd Generation decreases in gram (cephalexin, food, IM – clott
cefazolin) Lactation  safe
(ceftriaxone) & pos. absorbed by g
4th Generation muscle Pediatrics  in - Com
Treat surgical Second  gram +
(cefepime) neonates immature with
and H. flu, more
prophylaxis, resp potent, broader Distribution  renal fx causes (disu
1st – narrow spectrum tract infx, strep spectrum, widely increased half life rxn
5th – broad spectrum pharyngitis/sinusi distributed to and accumulation; flush
gonorrhea, resp
tis, CAP, skin, most tissue, kids – varies by dizz
infx (cefaclor
soft tissues, variation in drug n/v,
(CAP),
bones/joints, UTI cefziroxine) protein prob
(2nd line for kids), binding, m
STI Third  some penetration - Nep
gram + and -, not CSF varies by ty
active against generation - Sup
MRSA, effective nn
against Metabolism  - Ren
pseudomonas, less hepatic c dy
metabolism – exte
freq dosing,
insignificant half
crosses BBB with
inflammation - Ana
Excretion 
y rx
p d
gi
ceph

, (ceftriaxone, excreted by - Prob
omnicef (CAM) kidney  i
conc
Fourth  broad n of
spectrum of - Loo
activity, good diur
for c
organisms that incr
developed risk
resistance to earlier neph
generation y
cephalos, strep,
staph, doesn’t
penetrate CSF
(cefepime,
maxipime)
Glycopeptides Bacteriocidal Inhibits cell wall Absorption – Pregnancy Side effect
(Vancomycin – gram positive synthesis and poor absorption - Category B - Irrit
narrow spectrum disrupts from GI tract, (oral) tissu
(Vancocin)) membrance barrier IV rapidly - Category C an
(telavancin (Vibativ)- used to function; affects absorbed; (parenteral) bloo
tx HAP or CAP when vanc RNA synthesis vanc:52-56% - Must do intim
fails) protein bound; pregnancy - Red
Vanc: C.diff, and telavancin: test prior to synd
staph enterocolitis 90% protein telavancin (fac
bound use tors
Telavancin: Lactation min
complicated skin Distribution – - Excreted in infu
infections widely breast milk Adverse Eff
distributed; Pediatrics - Nep
penetrates CSF - Hospitalized - Tran
patients otot
Metabolism – only with - Hyp
primarily given serious e vit
IV; bypasses illness - Phle
first pass i
inje
Excretion –
oral vanc
(feces); Iv vanc
(renally via
glomerular
filtration);
telavancin
(primarily
urine)
Macrolides Bactericidal or Inhibits gram + Absorption – Cautions - GI u
(Erythromycin, bacteriostatic and few gram - well absorbed - Prolongs (esp
Clarithromycin, depending on in duodenum QT eryt
Azithromycin, dirithromycin, concentration; - Liver )
telithromycin) reversibly binds Distribution – impairment - Sev
to 50S ribosome distribute - Clarithromy expl
unit, preventing readily to body cin: wate
protein synthesis tissues, enters - CrCl diar
of bacteria; CSF when <30ml/min - Acu
alkaline – meninges are requires chol
inactivated by inflamed dosage to be hepa

, acid; halved - Rash
Metabolism – Pregnancy eosi
metabolized in - Erythromyci - Met
liver, n: cat B Inte
erythromycin, - Clarithromy esp
heavily cin: cat C eryt
metabolized by - Azithromyci - Prol
CYP3A4 n: cat B QT
Lactation synd
Excretion – - Safe mali
excreted in Pediatrics arrth
feces and urine, - Safe over
caution with age 6 Interactions
clarithromycin months - Colc
increased renal - War
excretion
- Digo
incr
effe

Lincosamides Bacteriostatic in First line tx in Absorption – Cautions - GI s
(clindamycin - Cleocin) usual doses; MRSA, primarily good oral - Asthma - Dizz
suppresses gram +, some absorption - Severe vert
protein synthesis anaerobic allergies - C.di
– binds to 50S pathogens Distribution – - Severe serio
subunit of the highly protein renal/liver
bacterial bound impairment
ribosome Pregnancy
Metabolism – - Category B
metabolized in - Okay for 3rd
liver trimester
Lactation
Excretion – - Present in
excreted in bile breast milk
and urine – weigh
risk/benefit
Pediatrics
- Severe infx
only
Quinolones Bactericidal for Broad spectrum; Absorption – Cautions - GI
(Levofloxacin, DNA gyrase extensive gram -; well absorbed - Renal - CNS
Ciprofloxacin, Moxifloxacin) (needed to later generations after PO admin, dysfunction: - Pho
synthesize increased activity IV and oral  can cause - Skin
bacterial DNA) against gram +; similar serum increase - Sup
only moxifloxacin concentration half-life nn
has activity against with - Mus
anaerobic bacteria; Distribution – majority of l eta
PO and IV widely drug - Ren
formulations; distributed; excreted - Diab
resistance already high tissue, unchanged - Seri
occurring from urinary in urine s
inappropriate use prostate, sinus - CrCl effe
and lung <50mL/min: dysr
penetration; adjust t
variable protein dosage
binding; - Cautious in
moderately patients

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