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53 Cards in this Set

  • Front
  • Back
What class of drugs interfere with replication and transcription?
Quinolones
Fluorinated quinolones are more or less potent?
Are more potent
What is the ending for quinolones?
"-oxacin"
Name one second generation quinolone:
Ciprofloxacin
Name one third generation quinolone:
Levofloxacin
Ciprofloxacin is a second or third generation quinolone?
Second generation quinolone
Levofloxacin is a second or third generation quinolone?
Third generation quinolone
Quinolones are bacteriostatic or bacteriocidal?
Bacteriocidal
Quinolones inhibit what enzymes in the cell?
Topoisomerases
What enzymes change the topography of DNA?
Topoisomerases
What phenomenon during DNA replication, repair, and transcription is relieved by topoisomerase?
Supercoiling
Why are quinolones tolerated by humans?
1. Quinolones have greater affinity for bacterial topoisomerases
2. Bacteria are actively growing (more)
Quinolones have greater/lesser affinity for bacterial topoisomerases?
Greater affinity - basis for selective toxicity
The concept that quinolones are more targeted towards bacterial topoisomerases rather than human ones is what?
Selective toxicity
Topoisomerase IV is the target of quinolones in gram +/- bacteria?
Gram + bacteria
Topoisomerase II (DNA gyrase) is the target of quinolones in gram +/- bacteria?
Gram - bacteria
Topoisomerase IV or II is involved in decatenation?
Topoisomerase IV
Quinolones against gram +/- bacteria block decatenation?
Gram + bacteria
Topoisomerase IV or II is involved in relaxing DNA supercoiling (introducing negative supercoils)?
Topoisomerase II
Quinolones against gram +/- bacteria inhibits gyrase-mediated DNA supercoiling?
Gram - bacteria
Name two quinolones used to treat UTIs
Ciprofloxacin
Levofloxacin
Name two quinolones used to treat GI tract infections caused by gram - rods?
Ciprofloxacin
Levofloxacin
Neisseria gonorrhea treatment with ciprofloxacin is now replaced by what antibiotic?
Ceftriaxone
What quinolone is used to treat Bacillus anthracis?
Ciprofloxacin
What quinolone is used to treat community-acquired pneumonia?
Levofloxacin
What quinolone is used to treat streptococcus pneumoniae with high-level penicillin resistance?
Levofloxacin
Metals do what to quinolones?
Chelate quinolones - Don't take with antacids
What blocks adsorption of quinolones?
Metals - CI with metal containing antacids (Al and Mg)
Quinolones are/are not contraindicated in children, pregnant/nursing women?
Are contraindicated
Why are quinolones contraindicated in children and pregnant/nursing women?
Damages growing cartilage
Is it okay to give children with cystic fibrosis quinolones?
Yes, benefit may outweigh risk of cartilage damage
What is a main CNS side effect of quinolones?
Headache
What CV side effect can occur with quinolones?
QTc-interval prolongation
What can happen to muscle tendons with quinolone?
Tendinitis - tendon rupture possible
Can ciprofloxacin penetrate the CNS?
Yes it can penetrate the CNS
Norfloxacin does not have good penetration of tissues and body fluids like other quinolones, therefore it is limited to treatment of what condition?
UTIs
Sulfonamides, Trimethoprim, TMP/SMX are three drugs used to treat what condition?
UTI
Drugs used to treat UTI interfere with DNA replication and transcription. They also have what effect on enzymes?
Inhibit metabolism
What drug inhibits dihydropteroate synthase (DHPS)?
Sulfonamides
Is dihydropteroate synthase (DHPS) present in mammals?
No it is not
What drug inhibits dihydrofolate reductase?
Trimethoprim (TMP)
Is DHFR present in mammals? If yes, is it the same or different?
Yes, but different
What drug is similar to PABA?
Sulfonamides
What drug is dubbed "first antimicrobial drug?"
Sulfonamides
Name a sulfonamide:
Sulfamethoxazole
Sulfonamides bind reversibly/irreversibly inhibits DHPS?
Reversibly
Because sulfonamides bind DHPS reversibly, is it bacteriostatic or bacteriocidal?
Bacteriostatic
What is an important adverse reaction with sulfamethoxazole?
Hypersensitivity/allergic reaction (Sulfa allergy)
TMP and SMX together are bacteriostatic or bacteriocidal?
Bacteriocidal
Are adverse effects more or less pronounced the TMP-SMX?
More pronouced
What drug is used to treat recurrent UTI and acute recurrent chronic bronchitis?
TMP-SMX
Drug resistance to TMP or SMX is rapidly increasing?
TMP
Name two antifolates:
TMP
SMX