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pharmacology antibacterials
exam 1
28
Medical
Professional
09/28/2008

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Term
carbapenems
Definition
gram+, gram-, aerobic, anaerobic

good against serious sepsis caused by pseudomonas

i.v.

always with cilistatin (inhibits dehydropeptidases in renal)

penicillin allergies also allergic to carbapenems
Term
monobactams
Definition
beta lactam resistant

gram negative aerobic

good vs. enterobacteria and resistant bacteria like pseudomonas (pneumonia, osteomyelitis, endocarditis, sepsis)

penicillin alleric patients are ok
Term
beta lactamase inhibitors
Definition
clavulanic acid, sulbactam, tazobactam

hospital acquired pneumonias
anaerobic
pseudomonas

augmentin (clav + amox)
timentin (clav + ticarcillin)
Term
vancomycin
Definition
only gram+

includes CNS coverage (meningitis)

nephrotoxic and orotoxic at high doses

not absorbed orally, for cdif pseudomembrane colitis administer vanco orally
Term
bacitracin
Definition
gram+

nephrotoxic if absorbed systemically (mostly topical use)
Term
cycloserine
Definition
broad spectrum including coliforms and mycobacteria

mainly used in drug resistant tb as 2nd line drug

alanine racemase / d-alanyl-d-alanine ligase

CNS coverage, absorbed orally, acid labile

rare resistance (enzyme modification)
Term
tetracycline
Definition
30s aminoacyl-tRNA

CNS and placenta (NEVER GIVE TO PREGNANT/NURSING or YOUNG KIDS)

Ca++ chelation (localized in bone and teeth, teeth staining, bone deformity in developing children)

efflux pumps or ribosomal protection proteins

tigecycline (bad vs. pseudomonas and proteus)
Term
aminoglycosides
Definition
gran negatives and staph, mycobacterium tb

30s non enzymatic site that alters codon:anticodon recognition

killed by phosphorylation, adenylation, acetylation
Term
aminocyclitols
Definition
gonorrhea

30s
Term
chloramphenical
Definition
very toxic so use carefully:
1. severe rickettsia infections in children and pregnant women (can't use tetracycline)
2. severe bacterial meningitis in patients who have severe allergies to penicillin and cephalosporin

50s, peptidyl transferase

gray baby syndrome (not use in newborns because can't metabolize - aplastic anemia)

acetyl transferases inactivate the drug
Term
clindamycin
Definition
gram+ cocci, gram- anaerobics

associated cdif colitis

50s

gram+ if allergic to penicillins and ceph

anaerobes of female genital tract and those that penetrate abdomen

cross placenta but not CNS

resistance via methylation of 50s ribosomes and adenylation of methyl OH groups
Term
erythromycin
Definition
50s, translocation and initiation complex formation

gram+ except enterococci, yes some gram-

cross placenta, not CNS
Term
ketolide
Definition
related to macrolide

50s
Term
streptogramin
Definition
50s, inhibit initiation complex, translocation


cp34a inhibits p450
gram+

VRE
skin /structure infections
nosocomial pneomonia
Term
linezolid (oxazolidinone)
Definition
gram+

VRE, VRSA

50s to inhibit formation of 70s initiation complex
Term
pleuromutilins
Definition
50s, prevents tRNA binding and inhibits peptidyl transferase

gel, skin / topical

VRSA, strep pyogenes
Term
quinolones
Definition
mostly gram-, some gram+

hospital acquired pseudomonas

diarrhea caused by enterics

gram- facultative intracelular like legionella, brucella, salmonella typhi, atypical mycobacteria

dna gyrase

nausea, dizziness, headache, insomnia, siezures when combined with nsaids

orally administered, widely distributed but not CNS

nalidixic acid structure
Term
rifampin
Definition
tb and leprosy as first line drug

prophylactially for N. meningitidis

inhibits RNA synthesis by binding to dna dependent rna polymerase

naphthalene

orally absorbed, widely distributed including CNA

occasional liver damage and wll enhave degradation of oral contraceptives by inducing p450

resistance arises from chomosomal mutation of rna polymerase gene
Term
rifampin
Definition
tb and leprosy as first line drug

prophylactially for N. meningitidis

inhibits RNA synthesis by binding to dna dependent rna polymerase

naphthalene

orally absorbed, widely distributed including CNA

occasional liver damage and wll enhave degradation of oral contraceptives by inducing p450

resistance arises from chomosomal mutation of rna polymerase gene
Term
polypeptides
Definition
gram- aerobic

interact with membrane phospholipids acting as "cationic detergent"

nephro and neuro toxic if systemic, limit use to superficial skin lesions
Term
daptomycin
Definition
MRSA, VRE

depolarizes membranes of gram+

insert into bac cyto in calcium dependent fashion

adverse effects: skeletal muscle elevations in serum CPK (monitor muscle status!)

intravenous infusion every 24 hrs. for 1-2 weeks
Term
isoniazid
Definition
mycobacteria (first line for tb)

perhaps via inhibition of mycolic acid synthesis

administer in combo with other tb antibiotics to avoid resistance (ie. streptomycin, ethambutol, clofazimine)
Term
ethambutol
Definition
first line drug for active tb

only d isomer is active

optic neuritis possible side effect
Term
clofazime
Definition
good against leprosy

half life up to 8 weeks

side effects: skin discoloration, urine/sweat/tears turn red
Term
bactrim
Definition
gram+ and gram- aerobics only

uncomplicated UTI, prostatitis, urethritis caused by (susceptible) enterics

AIDS: pneumocystis carinii peumonia, nocardia in lungs

orally

all tissues including CNS

side effects = folate deficiency patients is dangerous, avoid use in final trimester of pregnancy or will increase fetal bilirubin leading to kernicterus
Term
sulfones
Definition
similar to sulfonamide

side effects include metabolite induced hemolytic anemia
Term
penicillins
Definition
gram+

widespread but not CNS

anaphylactic shock, broad spectrum may change intestinal flora

penG penV poor gram-

aminopen improved gram-

antipseudomonal (aeruginosa) = tic, car, pipe, mez

penicillinase resistance = clox, meth, naf, ox
Term
cephalosporins and cephamycins
Definition
first gen: ro-lex zol
gram+, surgical prophylaxis for skin infxn

second gen: fox te
- improved gram-, haemophilus influenza, amp/amox resistance

third gen: tri tax fix taz
broader gram-, antipseudomonal
excellent CSF penetration (meningitis caused by pneumococci, meningicoci, H. influenza)

fourth gen: cefepime
extended spectrum and incread beta lactamase stability
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