SEARCH
You are in browse mode. You must login to use MEMORY

   Log in to start

level: Level 1 of QUIONOLONES

Questions and Answers List

level questions: Level 1 of QUIONOLONES

QuestionAnswer
Fluoroquinolones Therapeutic Uses1 Respiratory Tract Infection. (Levo, Spar, Ofloxacin) 2 Typhoid (Cipro, Ofloxacin) 3 Furunculosis 4 Tuberculosis 5 Osteomyelitis (Ciprofloxacin) 6 UTI (Norfloxacin 4-6 weeks) 7 Conjunctivitis 8 Bacillary Dysentery (Nor, Cipro, Trallver's-cotrimoxaz) 9 Otitis Media 10 Leprosy 11 STD. Except Syphilis 2nd line -> (Cipro, Oflo, Gatifloxacin) 12 Meningitis (2nd line Drugs)
Synthetic antibacterial agents that are highly effective in the tx of many types of infectious diseases. They are used against a variety of gram negative as well as positive pathogensQUINOLONES
Synthetic antibacterial patterned after NALIDIXIC ACID, a napthyridine derivatived introduced for the tx of UTI in 1963.1-Ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carboxylic acid
Isosteric heterocyclic groupingsa. Quinolones (Norfloxacin, Ciprofloxacin, Lomefloxacin) b. Napthyridines (nalidixic acid, enoxacin) c. Cinnolines (cinoxacin)
tx for serious systemic infections all members of the group have 6-fluoro substituent in common, and cyclic basic amine moiety at C-7 First manmade antibioticsFluoroquinolones
SAR OF QUINOLONES 1 Study shows that __ moiety is essential for antibacterial activity 2 The __ must be annulated with aromatic ring 3 Isosteric replacements of __ for carbon atoms at positions __ leads to retention of antibacterial activity 4 Introduction of substituents at position __ greatly reduces or abolishes activity But substitutions at position __ at annulated ring produce good effects 5) __ group at position C5 increases activity 6) __ substitution at position 6 significantly enhance activity 7) __ substitution at position 1 is essential for activity1) 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid 2 Pyridone system 3 Nitrogen, 2,5,6 and 8 4) 2, 5,6,7 and 8 5) Amino 6) Fluorine 7) Alkyl substitution
MOA of Quinolones 1 In gram negative 2 In gram positive1 Inhibition of DNA Gyrase 2 Inhibition of Topoisomerase IV
MOA of Fluoroquinolones 1 In gram negative 2 In gram positive1 Decrease permeability 2 Efflux pump, Mutation of enzymes
1 From chloroquine in 1939 to __ in 1962 2 Synthesis intermediate found to display antibacterial activity1 Nalidixic acid 2) 7-chloroquinoline
1 Limited usefulness as a drug - Narrow antibacterial spectrum (Enterobacteriaceae) - Short half life (1.5HR) - High protein binding 90% 2 Modify naphthyridone into quinolone __, Shows reduced protein binding 3 Shows weak but broad Gram negative activity 4 Shows Longer Half Life1 Nalidixic Acid 2 Oxolinic acid 3 Flumequine 4 Pipemidic acid
1 Broader gram negative activity Less protein binding 50% Longer half life (3-4 h) 2 Tricyclic compound, Flumequine but morpholine ring 3 From ofloxacin: Cyclopropyl to increase potency1 Norfloxacin 2 Ofloxacin 3 Ciprofloxacin
1 Piperazine 2 Cyclopropyl 3 Methyl 4 Morpholine1 Norfloxacin 2 Ciprofloxacin 3 Pefloxacin 4 Ofloxacin
1 Active form of ofloxacin 2 Pure (-) isomer1 (-) S isomer 2 Levofloxacin
1) 1-Ethyl-1,4-dihydro-4-oxo[1,3]dioxo[4,5g]cinnoline-3-carboxylic acid 2) 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid 3) 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperainyl)-1,8-naphthyridine-3-carboxylic acid 4) 1-cyclopropyl0-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid)1 Cinoxacin (Cinibac) 2 Norfloxacin (Noroxin) 3 Enoxacin (Penetrex) 4 Ciprofloxacin (Cipro)
1) 9-fluoro-2,3-dihydro-3-methyl-10(4-methyl-1-piperaziny l)-7-oxo-7H-pyrido[1,2,3-de]-1,4,-benzoxacine-6-carboxylic acid 2) 1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperaziny l)-4-oxo-quinolinecarboxylic acid 3) (cis)-5-amino-1-cyclopropyl-7-(3,5-dimethyl)-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-quinolinecarboxylic acid1 Ofloxacin (Floxin) 2 Lomefloxacin (Maxaquin) 3 Sparfloxacin
1 Fluoroquinolone Uses1 Opthalmic infections, 2 Respiratory Infections, 3 Infections of bones, joints & soft tissues, 4 GI & Abdominal infections, 5 Prostatitis (UTI &STD )
Fluoroquinolone 1 Routes 2 Mechanism 3 Adverse Effects1 ORAL, IV 2 Inhibits DNA Gyrase and Topoisomerase IV Bactericidal 3 Tendon rupture, Category C pregnancy, Seizures, Dizziness, Confusion, Photosensitivity
Fluoroquinolones: For Sexually Transmitted Diseases 1 A single dose of a fluoroquinolone such as __ or __ is effective treatment for sensitive strains of __ 2 But increasing resistance to fluoroquinolones has made __ the first-line agent1 ofloxacin, ciprofloxacin, N.gonorrhoeae 2 Ceftriaxone
Fluoroquinolones: Bone, Joint, and Soft Tissue Infections 1 Fluoroquinolones in combination with an agent with antianaerobic activity are a reasonable choice for __ 2 Fluoroquinolones have been used for the treatment of chronic __1 Diabetic Foot Infections 2 Osteomyelitis
Current Use of Fluoroquinolones 1 Wide range of Infections. Pneumonias, bone infections, diarrhea, Skin infections and urinary tract infections. Not good for methicillin resistant Staphylococcus Aureus. 2 Better for UTI. Effective against Gram-negative (including pseudomonas aeruginosa) and Gram-positive UTIs and prostatitis, but not systemic infections. 3 UTIs an bronchitis caused by Haemophilus influenzae or Moraxella catarrhalis. __ Is not effective against pseudomonal bacteremia __ Is recommended for STDs 4 Overcomes the problems with S. pneumoniae acute bacterial sinusitis; mild to moderate community acquired pneumonia1 Ciprofloxacin 2 Norfloxacin 3 Lomefloxacin, Enoxacin 4 Moxifloxacin
Fluoroquinolones Therapeutic Uses1 Respiratory Tract Infection. (Levo, Spar, Ofloxacin) 2 Typhoid (Cipro, Ofloxacin) 3 Furunculosis 4 Tuberculosis 5 Osteomyelitis (Ciprofloxacin) 6 UTI (Norfloxacin 4-6 weeks) 7 Conjunctivitis 8 Bacillary Dysentery (Nor, Cipro, Trallver's-cotrimoxaz) 9 Otitis Media 10 Leprosy 11 STD. Except Syphilis 2nd line -> (Cipro, Oflo, Gatifloxacin) 12 Meningitis (2nd line Drugs)