Floroquinolones lecture 際際滷Share
- 2. Contents Introduction Classification Pharmacokinetics &MOA Antimicrobial spectrum Clinicaluse Introduction (1ST Generation drug) Classification Pharmacokinetics Mechanism of Action Antimicrobial spectrum Clinical use Adverse reactions Contraindications Drug Interactions Brands available ADRs Contraindications Interactions &Brands
- 3. Introduction Member of a large group of broad-spectrum bacteriocidals. Contain a fluorine atom in their chemical structure Are effective against both Gram-negative and Gram-positive bacteria. Nalidixic acid is considered the first quinolone drug. Introduced in 1962 for treatment of urinary tract infections (UTIs) . Nalidixic acid was discovered by George Lesher and coworkers in a distillate during an attempt at chloroquine synthesis Classification Pharmacokinetics &MOA Antimicrobial spectrum Clinicaluse ADRs Contraindications Interactions &Brands
- 5. Contents Introduction Classification Pharmacokinetics & MOA Absorption: Well absorbed from GI tract. Distribution: Concentrates in renal tissue. Drug is highly protein-bound Metabolism: Metabolized to more active hydroxynalidixic acid Excretion: In patients with normal renal function, plasma half- life is 1 to 2 hours Pregnancy category: Pregnancy risk category B Inhibition of DNA gyrase results in relaxation of supercoiled DNA, promoting DNA strand breakage. Inhibition of topoisomerase IV impacts chromosomal stabilization during cell division, thus interfering with the separation of newly replicated DNA Antimicrobial spectrum Clinicaluse ADRs Contraindications Interactions &Brands MOA
- 7. Contents Introduction Classification Pharmacokinetics & MOA Antimicrobial spectrum Nalidixic acid is effective against gram negative bacteria such as E coli, Proteus mirabilis, Klebsiella species, Shigella species . Have no activity against Pseudomonas aeruginosa. Resistant Bacteria: Bifidobacteria, Lactobacillus, Pseudomonas and Staphylococcus are resistant.Clinicaluse ADRs Contraindications Interactions &Brands
- 8. Contents Introduction Classification Pharmacokinetics & MOA Antimicrobial spectrum Clinicaluse DOSE: Adults: 1 g orally for 7-14 days Up to 6 g daily have been used for severe urinary tract infection. Children older than age 3 months: 55 mg/kg orally for 7-14 days Complicated and uncomplicated urinary tract infections. Prostatitis. Bacterial gastroenteritis caused by E. coli, Proteus spp, Klebsiella spp, Shigella spp. ADRs Contraindications Interactions &Brands
- 9. Contents Introduction Classification Pharmacokinetics & MOA Antimicrobial spectrum ADRs Rash Itchy skin Blurred or double vision Changes in color vision Nausea Vomiting Diarrhea. Convulsions Photosensitivity reactions Contraindications Interactions &Brands
- 10. Contents Introduction Classification Pharmacokinetics & MOA Antimicrobial spectrum ADRs Contraindications Interactions &Brands These agents should be avoided in pregnancy and lactation Should not be given to arrhythmic patients. Caution in children: cartilage damage Epilepsy
- 11. Contents Introduction Classification Pharmacokinetics & MOA Antimicrobial spectrum ADRs Contraindications Interactions &Brands Antacids: Decreases absorption of antibiotic. Give nalidixic acid 2 hours before or 6 hours after antacids. Warfarin: Using nalidixic acid together with warfarin may cause to bleed more easily Drug -Interactions Brands available NEGRAM (Suspension, Tablet) by SEARLE Pakistan. NAXID SUSPENSION by STANLEY pharmaceuticals. Nogram by GLOBAL pharmaceuticals.
- 12. Reference: Lippincott illustrated Reviews: Pharmacology(Sixth Edition) Goodman and GiIman Pharmacology. Google search