-
CIPRO
- most potent FQ against GM- bacteria
- limited activity vs strep and anareobes
- UTI=GM- =cipro but resistance with monotherapy
- BID dosing t1/2=5 hours
- first broad spec
-
LEVOfloxacin
- GM+ anaerobe
- upper respieratory tract
- active vs pen presistant and macrolide resistant strep pneumo and pseudomonasaeruginosa
- 5x more soluble than oflox
-
MOXIfloxacin
- gm + anaerobe
- upper respiratory tract
- improved activity vs strep pneumoniae
- resaonable anaerobic activity
- mainly metbaolized by conjugation
- NO URINARY EXCRETION
- longest t/12
- dont need to adjust in renal failure
- watch interaction with antiarrhythmics
- active for MDRTB
-
norfloxacin
- first FQ
- low bioavailability
-
ofloxacin
- racemate has 1/2 the activity of LEVOfloxacin
- opthlamic available
- IV/PO
- generic available
-
DOXYcycline
- DOC chlamydia trachomatis (7d) borellia, anaplasma, ehrlichia and rickettsia
- bronchitis,
- CAP--not atypicals
- broad spec gm + gm - atypical organisms tick borne pathogens
- take on an empty stomach avoid vitamins do not lay down x30 minutes
-
TIGEcycline
- very broad spec MRSA and VRE and nosocimial enterobacteriaciae
- IV only
- NAUSEA 40%
- photosensitivity
-
MINOcycline
- metabolized
- somewhat more lipophilic at physiological pH reaches higher concentrations in tears and saliva --useful for meningococcal carrier state
-
GENTAmicin
- not for pseudomonas auerginosa (76%R) okay for serratia (93%)
- good for gram negative
- mixture of drugs
- inactivated by 2' adenylation and acetylation at the 2'6'and 3' positions
-
TOBRAmycin
- good for pseudomonas aerginosa (95%) not for serratia(79%)
- good for gram - infections
- less renal dysfunction
- inactivated by 2' adenylation and acetylation at the 2'6'and 3' positions
-
amikacin
- synthetic AG analog
- used for infections resistant to other AG
- not good for pseudomonas
- exellent gm -
- only inactivated by 6'acetylation and is resistant to other inactiviating enzymes
-
ORDER OF MOST TOXIC TO LEAST TOXIC nephrotoxic AG
neomycin>gentamicin=amkikacin= netilmicin>tobramycin>streptomycin
-
ORDER OF MOST TOXIC TO LEAST TOXIC ototoxic AG
streptomycin =kanamyin > amikcacin=gentamicin = tobramycin>netlimycin
-
amphotericin B
- combines with cytoplasmic membran sterols
- broad specturm of ctivity versus a variety of funagl pathogens TOXIC
- first line for cryptococcus neoformans, histoplasma capsulatim blastomyces
- highest concentrations in liver > spleen = kidneys> lungs>heart = muscles>bone
- LOW RENAL not UTI
- adverese effects--RENAL TOXICITY, binds renal sterols, GI problems, hypokalemia, phlebitis, thrombophlebitis at injection site
- give APAP 500 mg 30 min prior to to prevent rigors
-
fungizone
amphotericin B, toxicity effects, 0.5mg/kg/dose
-
abelcet
amphotericin B lipid complex,
-
ambisome
more effective less toxic than fungizone, $$$$$
-
flucytosine
- candida albicans--UTIs
- cryptococcal meningitis first line
- if fail azoles
- PO
- well distrubited reaches joints, CSF levels high
- 80-90% renally eliminated
-
fluconazole
- water soluble triazole, PO and IV
- tx thrush, candida albicans esophagitis cryptococcus
- paritally effective for inital teatment of cryptococcal meningitis in AIDS to prevent candida infections
- achieve adequate CFS concentrations preferred for meningitis
- adjust in renal failure
- best tolerated
-
ketoconazole
- broad spec not as efective as amb for serious systemic fungal injfections
- highly protein bound ery lipophilic go to fat, liver kidney and skin
- primarily metabolized--excreted in bile
-
itraconazole
- broad spec
- expanded spec including ASPERGILLUS
- primary indications--blastomycosis pumonary and extrapulmonary and histoplasmosis DOC sporotrix schenkii, toenail infections $$
- hepatic metabolized--almost entirely, active metabolite hydroxyitraconazole
- Take with food
- highly protein bound
-
voriconazole
- second generation triazole enhanced activity vs flucoanzole resistnat C Krusei and grabrata IV and PO
- GOLD STANDARD FOR ASPERGILLUS
- ideal po to IV switch
- LARGE volume of distribution
- almost completley metabolized--saturable, CYP2C19 drug interactions!!
- VISUAL DISTURBANCES
-
posaconazole
- ORAL PROPHYLAXIS FOR ASPERGILLOSIS
- auc 4 x higher when given with fatty meal vs fatty state
- large volume of distrubution
- PROLONG QTC interval
-
drug interactions with AZOLES?
- AZOLES=INHIBITORS!!DRUGS HAVE INCREASED LEVEL!! therefore you will need to redraw levels of cyclosproin, HIV protease inhibitors tacrolimus (keto) phenytoin, warfarin (fluc)-- rifampin decreaesd auc of fluc 25%
- itraconazole---tacrolimus, cyclosporin, warfarin
- VORICONAZOLE--antiregctuoin drug, rifabutin increased 331% 3A4 substrate!!
- posaconazole--inhibits rifabutin but induces metabolism of rifampin.
-
caspofungin
echinocandin--aspergillus not first line , long half life and large volume of distrubution. load dose
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