Quinolones, Folic Acid antagonists and urinary antiseptics Flashcards
Name the 6 Fluoroquinolones
ciprofloxacin levofloxacin moxifloxacin nalidixic acid norfloxacin ofloxacin
What infection is fluoroquinolone closely tied to
CDAD
Fluoroquinolone antibiotics targets ______, primarily in gram-_____ bacteria and ______________ in gram_____ bacteria to inhibit DNA __________
DNA gyrase, negative, topoisomerase IV, positive, replication
Ingestion of fluoroquinolone with calcium or other divalent cations can ______ absorption
reduce
Fluoroquinolone should be taken on a full/empty stomach
empty
clearance of fluoroquinolone
renal
levels of fluoroquinolone are high in….
bones, urine, kidney, prostatic tissue and lungs
Moxifloxacin is mainly metabolised by
liver
Cipro is most active against gram-___ strains and ____________
neg, enteric coliform
Cipro is active against penicillin, cephalosporin and amino glycoside-resistant strains
yes
Cipro is highly active against _____ and is commonly used in ___________ patients
P. aeruginosa, cystic fibrosis
Cipro is used in what type of infections?
skin, bone, joint
Name 5 indications for cipro
cystic fibrosis travellers diarrhoea (e.coli) food poisoning (enterobacteriaceae and campylobacter jejune) typhoid fever (salmonella typhi) UTI prostatitis
Is cipro the first line agent for simple UTI?
No
3rd gen fluoroquiinolones like levy and maxi have better coverage agains gram _____ organisms especially _________ and ________
positive, S.pneumoniae, atypical pathogens
3rd gen fluoroquinolone are useful against ________ infections
respiratory
common ADR of fluoroquinolone
nausea, vomiting, diarrhoea, phototoxicity
Serious ADR of fluoroquinolone
tendinitis or tondon rupture
prolong QTc interval (3rd gen) –> not in patients predisposed to arrhythmias or taking other medications cause QT
peripheral neuropathy
Fluoroquinolone in children?
no <18 yo
Fluoroquinolone in preggo and breastfeeding
no
Fluoroquinolone contraindication
myasthenia graves
co administration of a sulfonamide and trimethoprim introduces sequential blocks in the biosynthetic pathway for _______ –> synergistic effect –> bacteri____ effect
tetrahydrofolate, cidal
sulphonamides are competitive inhibitors of ___________
dihydropteroate synthase
Bacteriostasis induced by sulphonamides is counteracted by ____ competitively
PABA
Name the 2 intermediate acting sulfonamides
sulfamethoxazole
sulfadiazine
sulfonamides administration
oral (except sulfasalazine)
sulfonamides CSF?
yes even in the absence of inflammation
sulfonamides metabolism
acetylated and conjugated primarily in the liver. Acetylated product can precipitate at neutral or acidic pH and cause crystalluria –>damage kidneys
sulfonamides clinicsal indications
combined with trimethoprim for pneumocystis carinii
combined with pyrimethamine for drug resistant malaria
IBS
infected burns (topically)
resp infections (eg with Nocardia)
ADR of sulfonamides
Crystalluria
hypersensitivity with sulfa allergy
hematopoietic disturbances
kernicterus in newborns if mom takes in late preggo
sulfonamides preggo?
avoided in newborns and infants less than 2months of age and pregnant women at term
Trimethoprim is a potent inhibitor of __________
bacterial dihydrofolate reductase
Trimethoprim leads to a decreased availability of tetrahydrofolate cofactors required for ___, ______ and ______ synthesis
purine, pyrimidine and AA
Trimethoprim may be used alone in the treatment of __ and ________________
UTI and bacterial prostatitis
modes of resistance in Trimethoprim
resistance in gram nag bacteria
presence of altered dihydrofolate reductase –> lower affinity for trimethoprim
efflux pumps and decreased perm to the drug