DESCRIPTION
Ciprofloxacin – A broad-spectrum antimicrobial carboxyfluoroquinoline. Tinidazole – A nitroimidazole antitrichomonal agent effective against Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections.
CATEGORIES
Ciprofloxacin – Anti-Infective Agents,Quinolones. Tinidazole – Antiprotozoal Agents,Anti-Infective Agents .
CHEMICAL FORMULA
Ciprofloxacin – C17H18FN3O3,Tinidazole -C8H13N3O4S .
COMPOSITION
Ciprofloxacin 500 mg + Tinidazole 600 mg
INDICATION
Ciprofloxacin – For the treatment of the following infections caused by susceptible organisms: urinary tract infections, acute uncomplicated cystitis, chronic bacterial prostatitis, lower respiratory tract infections, acute sinusitis, skin and skin structure infections, bone and joint infections, complicated intra-abdominal infections (used in combination with metronidazole), infectious diarrhea, typhoid fever (enteric fever), uncomplicated cervical and urethral gonorrhea, and inhalational anthrax (post-exposure). 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
Ciprofloxacin – Ciprofloxacin is a broad-spectrum antiinfective agent of the fluoroquinolone class. Ciprofloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. The
MECHANISM
of action of quinolones, including ciprofloxacin, is different from that of other antimicrobial agents such as beta-lactams, macrolides, tetracyclines, or aminoglycosides; therefore, organisms resistant to these drugs may be susceptible to ciprofloxacin. There is no known cross-resistance between ciprofloxacin and other classes of antimicrobials. 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.
MECHANISM
Ciprofloxacin – The bactericidal action of ciprofloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, strand supercoiling repair, and recombination. Tinidazole – Tinidazole is a prodrug and antiprotozoal agent. The nitro group of tinidazole is reduced in Trichomonas by a ferredoxin-mediated electron transport system. The free nitro radical generated as a result of this reduction is believed to be responsible for the antiprotozoal activity. It is suggested that the toxic free radicals covalently bind to DNA, causing DNA damage and leading to cell death. The
MECHANISM
by which tinidazole exhibits activity against Giardia and Entamoeba species is not known, though it is probably similar.
ABSORPTION
Ciprofloxacin – Rapidly and well absorbed from the gastrointestinal tract after oral administration. The absolute bioavailability is approximately 70% with no substantial loss by first pass metabolism. 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 – 50 L.
METABOLISM
Ciprofloxacin – Hepatic. Four metabolites have been identified in human urine which together account for approximately 15% of an oral dose. The metabolites have antimicrobial activity, but are less active than unchanged ciprofloxacin.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
Ciprofloxacin – Approximately 40 to 50% of an orally administered dose is excreted in the urine as unchanged drug. 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
Ciprofloxacin – 4 hours,Tinidazole – Elimination half-life is 13.2 ± 1.4 hours. Plasma half-life is 12 to 14 hours.
TOXICITY
Ciprofloxacin – The major adverse effect seen with use of is gastrointestinal irritation, common with many antibiotics. 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
Ciprofloxacin – 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 -Bitter taste,metallic taste.