-
Expert Review of Anti-infective Therapy Jun 2007Tinidazole has been used for bacterial vaginosis (BV) outside the USA for almost four decades. Tinidazole has recently been resurrected and FDA approved for... (Review)
Review
Tinidazole has been used for bacterial vaginosis (BV) outside the USA for almost four decades. Tinidazole has recently been resurrected and FDA approved for trichomoniasis and BV in the USA and is being restudied as an alternative to metronidazole for BV. In vitro antimicrobial activity and pharmacokinetics studies indicate that when compared directly with metronidazole, tinidazole has minor but possibly relevant antimicrobial as well as pharmacokinetic advantages. Clinical comparisons have been infrequent, although the limited head-to-head studies indicate minimal therapeutic advantage with tinidazole. Perhaps the more relevant differences relate to the enhanced tolerance and reduced toxicity of tinidazole. Currently, studies are still ongoing directly comparing the clinical efficacy of metronidazole and tinidazole. These studies should establish the role of tinidazole in the treatment of BV; however, cure rates are unlikely to be significantly different.
Topics: Anti-Bacterial Agents; Female; Humans; Microbial Sensitivity Tests; Tinidazole; Vaginosis, Bacterial
PubMed: 17547500
DOI: 10.1586/14787210.5.3.343 -
Journal of AOAC International Mar 2023Tinidazole (TIN) has amoebicidal, giardicidal, antifungal, and antimicrobial activities. It is marketed in the form of tablets. Analytical methods to assess the quality... (Review)
Review
BACKGROUND
Tinidazole (TIN) has amoebicidal, giardicidal, antifungal, and antimicrobial activities. It is marketed in the form of tablets. Analytical methods to assess the quality of TIN-based products are essential for correct pharmacotherapy.
OBJECTIVE
The objective of this review is to show an overview of the existing analytical methods for evaluating TIN, according to the quality control (QC) analysis routine and green analytical chemistry (GAC).
RESULTS
Official compendia show a method for evaluating TIN in tablets by nonaqueous titration, which has limitations (materials on the mg scale using solvents considered not recommended and harmful). The literature shows some analytical methods for evaluating TIN, both physicochemical and microbiological. The most used physicochemical method is UV (41%), and second is HPLC (28%). Among the microbiological methods, agar diffusion and turbidimetric methods are equally divided. The most studied matrix is TIN tablets (73%), and the most used solvent is methanol.
CONCLUSIONS
The literature shows space for the development of analytical methods according to GAC for evaluating TIN, optimizing time, resources, and materials, reducing waste generation, and opting for less aggressive reagents, solvents, and diluents.
HIGHLIGHTS
This review shows the status of analytical methods, both physicochemical and microbiological, for the analysis of TIN in pharmaceutical matrix, in the context of routine analysis of the chemical-pharmaceutical industries and of GAC.
Topics: Antifungal Agents; Chromatography, High Pressure Liquid; Solvents; Tablets; Tinidazole
PubMed: 36355444
DOI: 10.1093/jaoacint/qsac142 -
Expert Opinion on Investigational Drugs May 2007Tinidazole has been used for vaginal infection worldwide but not in the US for > 40 years. Recently, tinidazole has been re-introduced and approved by the FDA for... (Review)
Review
Tinidazole has been used for vaginal infection worldwide but not in the US for > 40 years. Recently, tinidazole has been re-introduced and approved by the FDA for trichomoniasis and restudied as an alternative to metronidazole for bacterial vaginosis. In vitro antimicrobial activity and pharmacokinetics studies indicate that tinidazole has minor but possibly relevant antimicrobial as well as pharmacokinetic advantages when compared directly with metronidazole. Clinical comparison has been infrequent although the limited head-to-head studies indicate minimal therapeutic advantage with tinidazole. Perhaps the more relevant differences relate to the enhanced tolerance and reduced toxicity of tinidazole. Ongoing, as yet incomplete, studies directly comparing the clinical efficacy of metronidazole and tinidazole for bacterial vaginosis should clarify the status of tinidazole; however, cure rates are unlikely to be significantly different. Although uncommon, high-level trichomonal metronidazole resistance can be reliably cured by using tinidazole, which is an invaluable advantage.
Topics: Anti-Bacterial Agents; Antitrichomonal Agents; Drug Administration Schedule; Drug Interactions; Drug Resistance; Female; Humans; Metronidazole; Microbial Sensitivity Tests; Parasitic Sensitivity Tests; Tinidazole; Treatment Outcome; Trichomonas Vaginitis; Vaginosis, Bacterial
PubMed: 17461745
DOI: 10.1517/13543784.16.5.743 -
Clinical Therapeutics Dec 2005Tinidazole, a structural analogue of metrondazole, is an antiprotozoal agent that has been widely used in Europe and developing countries for >2 decades with established... (Review)
Review
BACKGROUND
Tinidazole, a structural analogue of metrondazole, is an antiprotozoal agent that has been widely used in Europe and developing countries for >2 decades with established efficacy and acceptable tolerability. It was recently approved by the US Food and Drug Administration for the treatment of trichomoniasis, giardiasis, amebiasis, and amebic liver abscess.
OBJECTIVE
This article reviews the pharmacologic and pharmacokinetic properties and clinical usefulness of tinidazole.
METHODS
Relevant information was identified through a search of MEDLINE (1966-August 2005), Iowa Drug Information Service (1966-August 2005), and International Pharmaceutical Abstracts (1970-August 2005) using the terms tinidazole, Fasigyn, and nitroimidazole.
RESULTS
In vitro, tinidazole exhibits activity against pathogenic protozoa (eg, Tricbomonas vaginalis, Entamoeba bistolytica, Giardia duodenalis), a wide range of clinically significant anaerobic bacteria (eg, Bacteroides fragilis, Clostridium difficile), and the microaerophilic bacterium Helicobacter pylori. In susceptible protozoal and bacterial cells, tinidazole is reduced to cytotoxic intermediates that covalently bind to DNA, causing irreversible damage. In human adults, tinidazole had a bioavailability of 100% and a V(d) of 50.7 L, was minimally bound to plasma protein (12%), had a plasma elimination t((1/2)) of 12.3 hours, and was eliminated primarily by hepatic metabolism (approximately 63%). Dose adjustment does not appear to be necessary on the basis of race, sex, or renal function. No data were found on the disposition of tinidazole in patients with hepatic insufficiency; therefore, use of tinidazole in patients with severe hepatic impairment (Child-Pugh class C) is not recommended. Clinical cure rates in patients with trichomoniasis, giardiasis, amebiasis, and amebic liver abscess were generally >90%. In comparative trials, tinidazole was as effective as metronidazole in the treatment of trichomoniasis and was significantly more effective than metronidazole in the treatment of giardiasis (P < 0.05) and amebiasis (P < 0.05). The most commonly reported (>1%) adverse effects included bitter taste, nausea, abdominal discomfort, anorexia, vomiting, and fatigue. The recommended dosage of tinidazole is a single dose of 2 g for trichomoniasis and giardiasis, and 2 g/d for 3 to 5 days for amebiasis.
CONCLUSIONS
Tinidazole appears to be a promising agent for the treatment of trichomoniasis, giardiasis, amebiasis, and amebic liver abscess. Clinical studies are needed to evaluate the use of tinidazole against anaerobic bacteria and H pylori.
Topics: Antiprotozoal Agents; Clinical Trials as Topic; Drug Interactions; Humans; Molecular Structure; Tinidazole
PubMed: 16507373
DOI: 10.1016/j.clinthera.2005.12.012 -
Infection 1983Tinidazole is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa. It is bactericidal at low concentrations and its spectrum covers most... (Review)
Review
Tinidazole is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa. It is bactericidal at low concentrations and its spectrum covers most anaerobic bacteria and some capnophilic microorganisms. Anaerobic bacteria known to be resistant to tinidazole include anaerobic streptococci, actinomyces and propionibacteria. Tinidazole is one of the most active antibacterial agents against Bacteroides fragilis which is one of the most resistant species of anaerobic bacteria. Only a few strains have been reported to be resistant. Tinidazole has been shown to be efficacious in protozoal infections such as trichomonal vaginitis, amoebiasis and giardiasis. Clinical studies have also shown that tinidazole is efficacious in the treatment of anaerobic infections including respiratory tract infections, intra-abdominal sepsis and obstetrical and gynecological infections. Since tinidazole has no activity against aerobic bacteria, it must be combined with other antibacterial agents in the treatment of mixed infections involving aerobic and anaerobic bacteria. Tinidazole has also been used successfully alone or in combination with other antimicrobial agents for prophylaxis in patients undergoing elective colonic and abdominal surgery, emergency appendectomy and gynecological surgery.
Topics: Anaerobiosis; Animals; Bacteria; Bacterial Infections; Cellulitis; Colon; Digestive System; Enterocolitis, Pseudomembranous; Eukaryota; Female; Genital Diseases, Female; Humans; Kinetics; Nitroimidazoles; Peritonitis; Postoperative Complications; Premedication; Protozoan Infections; Respiratory Tract Infections; Sepsis; Tinidazole; Tissue Distribution
PubMed: 6341253
DOI: 10.1007/BF01651361 -
The Medical Letter on Drugs and... Sep 2007
Comparative Study Review
Topics: Administration, Oral; Female; Humans; Tinidazole; Vaginosis, Bacterial
PubMed: 17848905
DOI: No ID Found -
Drugs Aug 1982Tinidazole, like the structurally-related drug metronidazole, was initially introduced for treating protozoal infections. However, both these nitroimidazole compounds... (Review)
Review
Tinidazole, like the structurally-related drug metronidazole, was initially introduced for treating protozoal infections. However, both these nitroimidazole compounds are also active in vitro against most clinically important obligate anaerobes. Most of the clinical experience with tinidazole to date has involved prophylactic use to prevent postoperative anaerobic infection. Prospective placebo-controlled studies demonstrated that a single dose of tinidazole administered orally prior to elective colorectal surgery significantly reduced postoperative infection. Similarly, when given intravenously prior to appendectomy, tinidazole reduced the incidence of postoperative infection in some subgroups of patients. Although results of non-blinded studies with prophylactic tinidazole were encouraging when used in women undergoing gynaecological surgery (mainly hysterectomy), results from double-blind placebo-controlled studies in this situation have been somewhat equivocal. Thus, although the overall weight of evidence suggests that the drug is effective in this area of use, further study is needed to clarify its role in preventing anaerobic infection following gynaecological surgery compared with other antibiotics which can also be used for this purpose. Relatively few studies have been conducted with tinidazole in the treatment of established anaerobic infections, and this is an area needing further investigation. The drug is well tolerated when administered orally or intravenously.
Topics: Anaerobiosis; Animals; Bacteria; Bacterial Infections; Humans; Kinetics; Nitroimidazoles; Postoperative Complications; Tinidazole
PubMed: 6749473
DOI: 10.2165/00003495-198224020-00001 -
Sexually Transmitted Diseases Oct 2023
Topics: Humans; Female; Tinidazole; Metronidazole; Trichomonas Infections; Nitroimidazoles; Trichomonas Vaginitis
PubMed: 37432997
DOI: 10.1097/OLQ.0000000000001850 -
Expert Review of Anti-infective Therapy Oct 2004Tinidazole (Fasigyn, Pfizer Ltd), like metronidazole - to which it is structurally related - was initially introduced for treating protozoal infections. However, both of... (Review)
Review
Tinidazole (Fasigyn, Pfizer Ltd), like metronidazole - to which it is structurally related - was initially introduced for treating protozoal infections. However, both of these nitroimidazole compounds are active against most clinically important obligate anaerobes. In the last few years, the discovery of Heliobacter pylori and of its susceptibility to nitroimidazoles focused new attention on these drugs. Tinidazole, as a part of this class of drugs, shares the characteristics and indications of other nitroimidazoles. However, it has a number of desirable features that could potentially make it very successful: a better pharmacokinetic and pharmacodynamic profile, a better safety and tolerability spectrum, and a preserved activity against some bacteria that are resistant to metronidazole.
Topics: Amebiasis; Animals; Anti-Bacterial Agents; Antibiotic Prophylaxis; Antitrichomonal Agents; Clinical Trials as Topic; Drug Resistance; Eukaryota; Female; Giardiasis; Helicobacter Infections; Helicobacter pylori; Humans; Metronidazole; Tinidazole; Trichomonas Vaginitis; Vaginosis, Bacterial
PubMed: 15482233
DOI: 10.1586/14789072.2.5.695 -
Revista Espanola de Quimioterapia :... Jun 2009Tinidazole is a 5-nitroimidazole active in vitro against a wide variety of anaerobic bacteria and protozoa. Tinidazole is an effective treatment against anaerobic... (Review)
Review
Tinidazole is a 5-nitroimidazole active in vitro against a wide variety of anaerobic bacteria and protozoa. Tinidazole is an effective treatment against anaerobic microorganisms based on its pharmacokinetic characteristics (C(max) 51 microg/ml, t(1/2) 12.5 h) and its excellent in vitro activity. Its long half-life allows once a day regimens. Tinidazole is as effective as metronidazole in the treatment of infections caused by T. vaginalis, giardiasis and amebiasis and bacterial vaginosis, malaria, odontogenic infections, anaerobic bacterial infections (pelvic inflammatory disease, diabetic foot), surgical prophylaxis (abdominal and hysterectomy) and Helicobacter pylori eradication. Tinidazole was recently approved by the Food and Drug Administration (FDA) for the treatment of infections caused by Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia.
Topics: Anaerobiosis; Animals; Anti-Bacterial Agents; Antibiotic Prophylaxis; Antiprotozoal Agents; Bacteria, Anaerobic; Clinical Trials as Topic; Entamoebiasis; Eukaryota; Female; Giardiasis; Helicobacter Infections; Humans; Male; Periodontitis; Postoperative Complications; Tinidazole; Trichomonas Infections; Vaginosis, Bacterial
PubMed: 19544102
DOI: No ID Found