Fluoroquinolones for Students PDF

FLUOROQUINOLONES By Dr. T.S. SUBASHINI M.Sc., Ph.D., D.Acu., Lecturer, Dept. of Pharmacology, SRM DENTAL COLLEGE, RAMAPURAM  CLASSIFICATION I.QUINOLONES Excellent activity on gram negative bacteria ONLY NALIDIXIC ACID II. FLUOROQUINOLONES 1. Least activi...

FLUOROQUINOLONES By Dr. T.S. SUBASHINI M.Sc., Ph.D., D.Acu., Lecturer, Dept. of Pharmacology, SRM DENTAL COLLEGE, RAMAPURAM  CLASSIFICATION I.QUINOLONES Excellent activity on gram negative bacteria ONLY NALIDIXIC ACID II. FLUOROQUINOLONES 1. Least activity on gram negative and gram positive bacteria. NORFLOXACIN 2. Excellent activity on gram negative and moderate activity on gram positive bacteria. CIPROFLOXACIN PEFLOXACIN LEVOFLOXACIN LOMEFLOXACIN** OFLOXACIN SPARFLOXACIN** PAZUFLOXACIN BALOFLOXACIN 3. Excellent activity on gram negative and gram positive bacteria, including anaerobic gram negative rods. MOXIFLOXACIN, GEMIFLOXACIN, PRULIFLOXACIN, GATIFLOXACIN**, DELAFLOXACIN - NEW Mechanism of action of Quinolones Bactericidal Quinolones block bacterial DNA synthesis by inhibiting topoisomerase II (DNA gyrase) and topoisomerase IV. MECHANISM OF RESISTANCE Chromosomal mutation Reduced permeability Increased efflux  Antimicrobial spectrum of Quinolones Gram – negative bacteria Escherichia coli, Salmonella typhi, Shigella, Enterobacter, Campylobacter jejuni Vibrio cholerae Neisseria gonorrhoeae Neisseria meningitidis Pseudomonas aeruginosa Moraxella catarrhalis Brucella Klebsiella pneumoniae Haemophilus influenzae, ducreyi Legionella Proteus Yersinia enterocolitica Serratia  Antimicrobial spectrum of Quinolones Gram - positive bacteria Streptococci Staphylococci Enterococci Pneumococci Anaerobes Bacteroides fragilis Mycoplasma Mycoplasma pneumaniae Chlamydia Chlamydia pneumoniae, trachomatis Rickettsiae  FLUOROQUINOLONES ADVERSE DRUG REACTIONS Gastrointestinal tract Central nervous system Skin Tendon & Cartilage CVS Blood Glucose Disturbance Drug Interactions CONTRAINDICATION Pregnancy, lactation, Paediatric age  CIPROFLOXACIN THERAPEUTIC USES DENTAL USES OTHER USES Genitourinary tract Gastrointestinal tract Respiratory tract ENT Typhoid Bone, soft tissues, gynaecological and wound infections Tuberculosis Gram negative septicaemias Meningitis Prophylaxis Conjunctivitis STD: Gonorrhoea, Chancroid. NORFLOXACIN Genitourinary tract infections Bacterial diarrhea PEFLOXACIN Meningeal infections Genitourinary tract infections Gastrointestinal infections Systemic infections Typhoid Gram positive cocci & Listeria - less effective. Dose reduction in liver disease & not in renal insufficiency. OFLOXACIN SIMILAR TO CIPROFLOXACIN Also in LEPROSY Less interaction with theophylline LEVOFLOXACIN SIMILAR TO CIPROFLOXACIN Better activity – Strep. Pneumonia. High oral bioavailability Single dose No drug interaction Primary Indication: Community acquired pneumonia Exacerbation of chronic bronchitis LOMEFLOXACIN SIMILAR TO CIPROFLOXACIN More active – gram negative, Chlamydia. Single dose No interaction with theophylline. SPARFLOXACIN More active against gram positive bacteria – Strept.pneumoniae, Staphylococcus, Enterococcus; Bacteroides fragilis, mycobacteria. Main Indication: Pneumonia, Chronic bronchitis, Sinusitis, Tuberculosis, MAC –AIDS patients, Leprosy, Chlamydial infections. Single dose Phototoxic reaction Prolongation of QTc interval  GATIFLOXACIN Excellent activity against –Strept.pneumoniae, some anerobes, atypical respiratory pathogens including Chlamydia pneumoniae, M.tuberculosis. Primary Indication: Community acquired pneumonia Exacerbation of chronic bronchitis & other RTIs. Adverse Reactions: Tachycardia Prolongation of QTc interval Phototoxicity CNS effects Swelling over face Torsades de pointes Changes in blood glucose levels. Discontinued in U.S.A & U.K. MOXIFLOXACIN Excellent activity against –Strept.pneumoniae, Beta lactam/Macrolide resistant gram positive bacteria. Primary Indication Pneumonia Bronchitis Otitis Media Sinusitis ROUTES OF ADMINISTRATION Nalidixic acid - oral Ciprofloxacin - Oral IV infusion Eye - Drops, Ointment Ear - Drops Norfloxacin Oral Eye - Drops ROUTES OF ADMINISTRATION Levofloxacin Oral IV infusion Eye - Drops Ear - Drops Ofloxacin Oral IV infusion Eye - Drops Ear - Drops ROUTES OF ADMINISTRATION Pefloxacin Oral IV infusion Eye - Drops Lomefloxacin Oral Eye - Drops Ear - Drops ROUTES OF ADMINISTRATION Sparfloxacin - Oral Moxifloxacin Oral IV infusion Eye - Drops Gemifloxacin - oral Gatifloxacin - oral, IV infusion. Eye -drops