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3.19 Antibiotics I
by Dr. Hobden
53
Pharmacology
Professional
03/19/2012

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Term
Which aspects of modern medicine are made practical by antimicrobials?
Definition
cancer chemotherapy, gut surgery
Term
Asian fish, shrimp, and shellfish test repeatedly positive for...
Definition
nitrofuran, malachite green, flouroquinolones
Term
What is NDM-1?
Definition
new delhi metallo-lactimase 1 found in E coli and klebsiella pneumonia; confers resistance to antibiotics
Term
Name the beta lactam drugs.
Definition
penicllins, cephalosporins, carbapenems
Term
Name the nonbeta lactam antibiotics that are inhibitors of cell wall synthesis?
Definition
cecloserine, vancomycin, bacitracin
Term
Which antimicrobials work by disrupting cell membranes?
Definition
polymyxin, polyenes
Term
What antibiotics are reversible inhibitors of protein synthesis (bacteristatic)?
Definition
chloramphenicol, tetracyclines, macrolides (erythromycin), clindamycin, linezolid
Term
What antibiotics are irreversible inhibitors or protein synthesis?
Definition
the bacteriocidal aminoglycosides
Term
____ concentrations are what determine susceptibility of resistance to drug.
Definition
achievable serum concentrations
Term
What are some pharmacokinetic considerations that must be taken into account when treating an infection?
Definition
location of infection (some antibiotics may or may not reach therapeutic concentrations in certain bodily fluids), and the degree to which antibiotic binds serum proteins (excessive binding can affect passive diffusion from serum to tissue)
Term
Sulfonamides are analogues of...
Definition
PABA
Term
What is the MOA of sulfonamides?
Definition
competitive inhibitors of dihydropteroate synthase--needed for folic acid synthesis
Term
Are sulfonamides bactericidal?
Definition
they are in the urine
Term
What is the mech of resistance for sulfonamides?
Definition
altered affinity of enzyme for drug, decreased permeability or active efflux, new pathway of folic acid syntehsis
Term
Are sulfonamides easily absorbed from teh GI tract?
Definition
yes
Term
What is the distribution pattern of sulfonamides in the body?
Definition
binds variably to serum albumin, wide tissue distribution, including trans-placentally
Term
What is the metabolism and excretion of sulfonamides?
Definition
variably inactivated in liver by acetylation and then excreted in urine
Term
At what pH are sulfonamides at risk for precipitating out of the urine?
Definition
acidic
Term
Name some rapidly abosrbed and eliminated sulfonamides.
Definition
sulfisoxazole, sulfamethoxazole, sulfadiazine
Term
What is bactrim?
Definition
sulfamethoxazole combined with trimethoprim
Term
What is bactrim?
Definition
sulfamethoxazole combined with trimethoprim
Term
What are the pharmacokinetics of rapidly absorbed and eliminated sulfonamides?
Definition
binds extensively to plasma proteins and are highly concentrated in the urine (cidal)
Term
Name a poorly absorbed sulfonamide.
Definition
sulfasalazine
Term
What is sulfasalazine used for?
Definition
poorly absorbed in the GI tract so used to treat ulcerative colitis and irritable bowel syndrome
Term
How is sulfasalazine metabolized?
Definition
by gut flora into 2 compounds: 1 toxic, 1 therapeutic (5-aminosalicylate)
Term
Which sulfonamide has good penetration int he eye?
Definition
sulfacetamide
Term
Which sulfonamide is used for prevention and treatment of burn wound infections?
Definition
silver sulfadiazine; mafenide is used for prevention of burn wound infections
Term
Name a long acting sulfonamide.
Definition
sulfadoxine
Term
What is the half life of sulfadoxine?
Definition
days
Term
What is the use of sulfadoxine?
Definition
combined with pyrimethamine to treat malaria
Term
What are the therapuetic uses of sulfonamides?
Definition
urinary tract infections, nocardiosis, toxoplasmosis (avoid using in pregnant women)
Term
How do you prevent sulfonamides from forming crystals?
Definition
alkalize urine or increae hydration
Term
What are the toxicities of sulfonamides?
Definition
acute hemolytic anemia due to glucose-6-phosphate dehydrogenase deficiency, agranulocytosis, aplastic anemia, hypersensitivity reactions, nausea, anorexia, vomiting, kernicterus
Term
What are the different types of hypersensitivity reactions associated with sulfonamides?
Definition
skin and mucous membrane manifestations, serum sickness, focal or diffuse necrosis of the liver
Term
What are the very common side effects of sulfonamides?
Definition
nausea, anorexia, vomiting
Term
In what patient populations are sulfa drugs contraindicated?
Definition
those with G-6PD deficiency or pregnant or lactating women
Term
Why should sulfa drugs enver be given to a pregnant or lactating woman?
Definition
causes displacemnt of bilirubin from plasma albumin to brain resulting in encphalopathy
Term
Sulfonamides cause potentiation of which drugs
Definition
oral coagulants, sulfonylureas, and hydrantoin anticonvulsants
Term
What compounds are all quinolones dervied from?
Definition
naladixic acid
Term
What is the MOA of quinolones?
Definition
targets DNA gyrase (G-) and topoisomerase IV (G+)
Term
What causes resistance against quinolones?
Definition
resistance due to efflux and mutations in targets
Term
What are the first generation flouroquinolones?
Definition
nalidixic acid, cinoxacin, oxolinic acid
Term
What arethe second generation flouroquinolones?
Definition
ciprofloxacin, enoxacin, lomefloxacin, ofloxacin
Term
What are the favorable pharmacological attributes of quinolones?
Definition
quickly absorbed from GI, even with a full stomach, excellent bioavailability in a wide range of tissues and body fluids (including inside cells)
Term
How are quinolones excreted?
Definition
mostly by the kidneys; exceptions are perfloxacin and moxifloxacin which are metabolized by the liver
Term
Which quinolones are excreted in breast milk?
Definition
ciprofloxacin, ofloxacin, perfloxaci
Term
What are the therapeutic uses of quinolones?
Definition
UTIs, prostatitis, STDs (chalmydia, chancroid), GI and abdominal (travelers diarrhea, shigellosis, typhoid fever), respiratory tract (all work well against atypicals, new agents for strep pneumo); bone/joint/soft tissue, ideal for osteomyelitis, good against polymicrobial infections like diabetic foot ulcers, cipro for anthrax and tularemia, in combo for mycobacterium
Term
Quinolones are good for chronic osteomyelitis but resistance is developing in....
Definition
S. aureus, Paeuroginosa, and S. marcesens
Term
What are the GI side effects of quinolones?
Definition
nausea, vomiting, abdominal discomfort, diarrhea and antibiotic associated colitis
Term
What are the CNS side effects of quinolones?
Definition
mild headache and dizziness, hallucinations, delirium, and seizures
Term
What are the risks of giving quinolones to children?
Definition
arthropathy
Term
T/F Quinolones can cause arrhythmias.
Definition
true
Term
What toxic side effects do quinolones have on the blood?
Definition
leukopenia and eosinophilia
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