DESCRIPTION
Norfloxacin – A synthetic fluoroquinolone (fluoroquinolones) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA gyrase.Tinidazole – A nitroimidazole antitrichomonal agent effective against Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections.
CATEGORIES
Norfloxacin – Anti-Infective Agents,Quinolones.Tinidazole -Antiprotozoal Agents,Anti-Infective Agents.
CHEMICAL FORMULA
Norfloxacin – C16H18FN3O3,Tinidazole – C8H13N3O4S.
COMPOSITION
NORFLOXACIN 400 + TINIDAZOLE 600
INDICATION
Norfloxacin – For the treatment of urinary tract infection ,Tinidazole – For the treatment of trichomoniasis caused by T. vaginalis in both female and male patients. Also for the treatment of giardiasis caused by G. duodenalis in both adults and pediatric patients older than three years of age and for the treatment of intestinal amebiasis and amebic liver abscess caused by E. histolytica in both adults and pediatric patients older than three years of age.
PHARMACODYNAMICS
Norfloxacin – Norfloxacin is a quinolone/fluoroquinolone antibiotic. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Tinidazole – Tinidazole is a synthetic antiprotozoal agent. Tinidazole demonstrates activity both in vitro and in clinical infections against the following protozoa: Trichomonas vaginalis, Giardia duodenalis (also termed G. lamblia), and Entamoeba histolytica. Tinidazole does not appear to have activity against most strains of vaginal lactobacilli.
No Information
ABSORPTION
Norfloxacin – Rapid,Tinidazole – Rapidly and completely absorbed under fasting conditions. Administration with food results in a delay in Tmax of approximately 2 hours and a decline in Cmax of approximately 10% and an AUC of 901.6 ± 126.5 mcg hr/mL.
VOLUME DISTRIBUTION
Tinidazole – 50L.
METABOLISM
Norfloxacin – Via liver and kidney.Tinidazole – Hepatic, mainly via CYP3A4. Tinidazole, like metronidazole, is significantly metabolized in humans prior to excretion. Tinidazole is partly metabolized by oxidation, hydroxylation and conjugation. Tinidazole is the major drug-related constituent in plasma after human treatment, along with a small amount of the 2-hydroxymethyl metabolite.
ELIMINATION
Norfloxacin – Norfloxacin is eliminated through metabolism, biliary excretion, and renal excretion. Renal excretion occurs by both glomerular filtration and tubular secretion as evidenced by the high rate of renal clearance (approximately 275 mL/min). Tinidazole – Tinidazole crosses the placental barrier and is secreted in breast milk. Tinidazole is excreted by the liver and the kidneys. Tinidazole is excreted in the urine mainly as unchanged drug (approximately 20-25% of the administered dose). Approximately 12% of the drug is excreted in the feces.
HALF LIFE
Norfloxacin – 3-4 hours ,Tinidazole – Elimination half-life is 13.2 ± 1.4 hours. Plasma half-life is 12 to 14 hours.
TOXICITY
Tinidazole – There are no reported overdoses with tinidazole in humans. In acute studies with mice and rats, the LD 50 for mice was generally > 3,600 mg/kg for oral administration and was > 2,300 mg/kg for intraperitoneal administration. In rats, the LD 50 was > 2,000 mg/kg for both oral and intraperitoneal administration.
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Norfloxacin – Headache. Feeling dizzy. Rise slowly over a few minutes when sitting or lying down. Be careful climbing. Belly pain. Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. Loose stools (diarrhea). Yogurt or probiotics may help. You may get these products at health food stores or in some pharmacies. Tendons may rarely get irritated and tear. Unsafe allergic effects may rarely happen.Tinidazole – vaginal itching or discharge; nausea, vomiting, loss of appetite, indigestion; constipation, diarrhea, stomach cramps; feeling weak or tired; headache, dizziness; or. a metallic or bitter taste in your mouth;