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At least 19 recordsLinked to original sources
PubMed2005

[Dynamic release of tinidazole from the degradable PLLA-tinidazole blend gel].

OBJECTIVE: To determine the dynamic release of tinidazole from the degradable poly-lactic acid (PLLA)-tinidazole blend gel (a periodontal local drug delivery) by high-performance liquid chromatography (HPLC) in vitro and to observe the polylactic acid (as a vector of tinidazole) how to affect the release of tinidazole. METHODS: HPLC analysis was conducted. The operating conditions were C18-ODS-A column, water-methanol-acetic acid as mobile phase at a flow rate of 1.5 ml/min and a detection wavelength at 310 nm and a column temperature at 30 degrees C. RESULTS: The retention time of tinidazole was about 12 min. There was good linear relationship between the concentrations of tinidazole in blend gel and their peak areas in the ranges of 5 - 500 mg/L. The regression reaction was y = 0.836 + 8.452 2 x 10(-5) x (r = 0.998 6). RSD was 0.2%. Polylactic acid had no influence on the determination of tinidazole. The daily average release of tinidazole was 5.60%. The cumulative release of tinidazole was about 78.40% in 14 days. CONCLUSION: The in vitro drug release analysis is an useful method in evaluating the performance of local drug delivery system. HPLC analysis is a simple and accurate method with good reproducibility.

Chromatography, High Pressure Liquid↗
PubMed1996

High performance thin layer chromatographic analysis of hydrolyzed tinidazole solutions. II. Hydrolysis kinetics of tinidazole.

In a citrate-borate-phosphate buffer, 5 mM tinidazole solutions exhibited maximum stability stability around pH 4.0-5.0. The hydrolysis of tinidazole was mostly a first-order reaction. At pH 10.0 and 60-80 degrees C, tinidazole had an activation energy of 122 kJ mol-1 for hydrolysis. It was postulated that tinidazole decomposes by different mechanisms under basic and neutral/acidic conditions.

Antitrichomonal Agents↗
PubMed1983

Clinical trial of prophylaxis of wound sepsis in elective colorectal surgery. Cephamandole with tinidazole versus tinidazole alone.

A prospective randomized double-blind clinical trial was undertaken to determine whether prophylactic therapy with an antibiotic agent active against anaerobic bacteria needs to be supplemented by an antibiotic agent predominantly active against aerobic bacteria to minimize postoperative wound sepsis caused by enteric organisms in elective colorectal surgery. Two hundred and eleven patients were studied, of whom 100 received tinidazole and cephamandole, and 111 received tinidazole and a placebo. Wound infection occurred in 7% of the tinidazole/cephamandole group and in 9% of the tinidazole/placebo group (P greater than 0.7). After patients who required a second laparotomy, and those with staphylococcal wound infections were excluded, the wound infection rate in patients who received prophylaxis with combination chemotherapy was 2% compared with 9% in patients who received tinidazole alone (P = 0.03, Fisher's exact test). When patients with intra-abdominal sepsis were also excluded, the wound infection rate in the tinidazole group fell to 7%; in the combination therapy group, it remained at 2% (P = 0.08). There was a significant reduction in the mean wound infection rate in the combination chemotherapy group (P = 0.05, Fisher's exact test) when patients of the two surgeons who contributed two-thirds of the patients in the trial were excluded from analysis.

Cefamandole↗
PubMed1977

Bactericidal activity of tinidazole. An in vitro comparison of the effects of tinidazole and metronidazole against Bacteroides fragilis and other Anaerobic bacteria.

The new antiprotozoal agent, tinidazole, was found to be bactericidal against all 52 isolates of obligate anaerobic bacteria tested, 42 Bacteroides fragilis, 4 clostridia and 6 peptostreptococci. The minimum bactericidal concentrations of tinidazole for B. fragilis ranged from 0.25 to 4 mug/ml, and those of metronidazole from 0.25 to 8 mug/ml, i.e. several times lower than the serum concentrations achievable after oral administration. In most cases the MIC was identical with MBC or half of it. On the average, tinidazole was slightly more effective against B. fragilis than metronidazole. Although essentially the activities of the two drugs were positively correlated, there was a fourfold difference in their MBC for 10 of the 42 B. fragilis.

Bacteria↗
PubMed1978

[Clinical studies on the therapeutic effect of tinidazole ("Fasigyn") during treatment of urogenital trichomonas infections in women and men (with comparative laboratory studies on the effect of metronidazole and tinidazole)].

Tinidazole preparations are effective agents for the therapy of genitourinary trichomoniasis in women and men. The application of these drugs is very simple and, in particular, suitable as the application time is short and the occurrence of slight side effects shows a very low incidence. Unfortunately, these medicaments cannot be used during pregnancy and lactation. In addition, definite therapeutical recommendations are lacking and the published specific experiences in the therapy of obese persons with these drugs should be verified in future.

Adult↗
PubMed1976

Tinidazole: a review of its antiprotozoal activity and therapeutic efficacy.

Tinidazole, a synthetic imidazole derivative, has been used in the oral treatment of several protozoal infections - trichomoniasis, giardiasis and amoebiasis. Among the protozoal organisms inhibited by tinidazole are Trichomonas vaginalis, Trichomonas foetus, and Entamoeba histolytica. In vitro, tinidazole has been shown to possess antiprotozoal activity at least comparable to, and in some cases greater than, metronidazole. Tinidazole also has activity against some Gram-negative anaerobic bacilli, including Bacteroides spp. Following oral administration of a 2g dose, like metronidazole serum levels peak in about 2 hours but persist for longer. Any clinical significance of the longer plasma half-life (tinidazole 12.5h; metronidazole 7.3h) has yet to be demonstrated. Tinidazole is approximately 20% bound to plasma proteins. Only unchanged drug has been found in the plasma and urine of tinidazole-treated subjects, although metabolites have been detected in animal studies. A single 2g dose of tinidazole has been shown to be effective therapy in vaginal trichomoniasis and in urogenital trichomoniasis in males. Single-dose therapy in general offers advantages in regard to convenience, and in the treatment of a sexually transmissible disease such as trichomoniasis, single-dose therapy facilitates compliance of patient and sexual partner. In comparative studies, tinidazole, in both single-dose and traditional multiple-dose regimens, has been shown to be equivalent and often superior to other antitrichomonal agents, including metronidazole. In intestinal amoebiasis, tinidazole has been evaluated after both once-a-day and multiple daily dose regimens, with the former giving slightly better results. When both metronidazole and tinidazole were administered in multiple daily dose regimens, the two agents yielded similar cure rates; in one study fewer tinidazole-treated patients required a second course. Tinidazole has also been successful in some cases of amoebic liver abscess, but an advantage over metronidazole has not been demonstrated. Results in the treatment of giardiasis, especially with the single-dose regimen, are promising, and in one study, tinidazole proved effective in infections resistant to metronidazole. Even in large doses, tinidazole has been well tolerated, although rarely vomiting may occur and the patient may need to be re-treated with a multiple dose regimen.

Abnormalities, Drug-Induced↗
PubMed2005

Tinidazole: a nitroimidazole antiprotozoal agent.

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.

Antiprotozoal Agents↗
PubMed2003

Comparative study on the effects of ointments of tinidazole, hydrocortisone and clobetasol on animal models for inflammatory dermatitis in mice.

To understand further the possible clinical effects of tinidazole ointment at relatively high concentration (2%) for atopic dermatitis (AD), we performed a comparative study with readily available topical corticosteroids, clobetasol propionate (0.005 or 0.05%) and hydrocorotisone butyrate (0.1%) (hereafter referred as clobetasol and hydrocortisone, respectively), on inflammatory dermatitis in mice. We also observed the effects of combined application of tinidazole with clobetasol (0.005%, one tenth of the clinical use) in comparison with tinidazole itself, clobetasol (0.05%) or hydrocortisone (0.1%) on the animal model. All ointments suppressed inflammatory dermatitis induced by trinitrochlorobenzen (TNCB) or oxazolone. The rank order of the potency to suppress the ear edema was clobetasol (0.05%), tinidazole (2%) with clobetasol (0.005%) > clobetasol (0.005%) > tinidazole (2%) in TNCB-induced dermatitis, and hydrocortisone (0.1%), clobetasol (0.05%) > tinidazole (2%), tinidazole with clobetasol (0.005%) > clobetasol (0.005%) in case of oxazolone-induced dermatitis. We confirmed that tinidazole (2%) suppresses immediate and late phase reactions in mice passively sensitized with anti-DNP IgE Mab. In addition, tinidazole (2%) was much more potent than hydrocortisone (0.1%) in suppressing the amount of scratching, presumably due to itching, in passively sensitized mice. These results indicate that the advantage of using ointments of tinidazole would be that it has stronger anti-itching effects than corticosteroids.

Adjuvants, Immunologic↗
PubMed2002

Design and in vitro evaluation of oral colon targeted drug delivery systems for tinidazole.

The aim of the present investigation is to develop colon targeted drag delivery sytems for tinidazole using guar gum as a carrier in the treatment of amoebiasis. Fast-disintegrating tinidazole core tablets were compression-coated with 55, 65 and 75% of guar gum. All the formulations were evaluated for the hardness, drug content uniformity, and subjected to in vitro drug release studies. The amount of tinidazole released from tablets at different time intervals was estimated by HPLC method. The compression-coated formulations released < 0.5% of tinidazole in the physiological environment of stomach and small intestine. When the dissolution study was continued in simulated colonic fluids, the compression coated tablet with 55% of guar gum coat released 99% of tinidazole after degradation by colonic bacteria at the end of 24 h of the dissolution study. The compression coated tablets with 65 and 75% of guar gum coat released about 67 and 20% of tinidazole, respectively in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that compression coated tinidazole tablets with either 55 or 65% of guar gum coat is most likely to provide targeting of tinidazole for local action in the colon owing to its minimal release of the drug in the first 5 h of physiological environment of stomach and small intestine. The tinidazole compression coated tablets showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40 degrees C/75% RH for 6 months.

Animals↗
PubMedDate not supplied

Pharmacokinetics of tinidazole in male and female subjects.

Tinidazole is a potent nitroimidazole compound active against, and used to treat, Trichomonas vaginalis infections in males and females. Speculation exists in the literature that observed differences in tinidazole plasma concentrations between males and females may be due to sex-mediated pharmacokinetic differences. To investigate this phenomenon, a study was designed to determine the pharmacokinetics of tinidazole in male and female subjects. Six male and six female volunteers were each administered a single 2-Gm oral dose of tinidazole. Plasma and urine samples, collected over a 72-hour period, were assayed by a sensitive and specific HPLC assay. Results demonstrate a significant correlation between tinidazole oral plasma clearance and body weight and apparent volume of distribution of tinidazole and body weight for male and female subjects, respectively. There were no apparent sex-mediated differences in weight-normalized pharmacokinetic parameters as documented by statistically equivalent mean oral plasma clearances (36.1 and 35.4 ml/kg/hour), apparent volumes of distribution (0.65 and 0.63 liter/kg), and elimination half-lives (12.3 and 12.3 hours, males and females, respectively). Mean area under the tinidazole plasma concentration-versus-time curve and mean peak plasma concentration of tinidazole were 1.3 times greater for females than for males, apparently due to the smaller mean body weight of females and consequently a 1.3 times greater administered dose to the females on a weight basis.

Adult↗
PubMedDate not supplied

Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of tinidazole in healthy human volunteers.

The aim of the present investigation was to determine the in vivo availability of guar gum-based colon-targeted tablets of tinidazole in comparison with immediate release tablets of tinidazole in human volunteers. Six healthy volunteers participated in the study, and a cross-over design was used. The plasma concentration of tinidazole was estimated by HPLC. The pharmacokinetic parameters were calculated from the plasma concentration of tinidazole versus time data. The immediate release tablets of tinidazole produced a peak plasma concentration (Cmax of 3239 +/- 428 ng/ml) at 1.04 +/- 0.32 hr (Tmax), whereas colon-targeted tablets produced peak plasma concentration (Cmax of 2158 +/- 78 ng/ml) at 14.9 +/- 1.6 hr. The delayed Tmax, decreased Cmax, and Ka, and unaltered bioavailability and elimination half-life of tinidazole from guar gum-based colon-targeted tinidazole tablets, in comparison with the immediate tablets, indicated that the drug was not released in the stomach and small intestine but delivered to the colon. Slow absorption of the drug from the less absorptive colon might result in the availability of the drug for local action in the colon. The guar gum-based colon-targeted tablets of tinidazole may be useful in providing an effective and safe therapy of intestinal amoebiasis.

Adult↗
PubMed1996

Concentrations of tinidazole in gingival crevicular fluid and plasma in dogs after multiple dose administration.

Tinidazole 15 mg/kg was administered to eight Beagle dogs with gingivitis or periodontitis twice daily for 3 days. Tinidazole concentrations in blood and gingival crevicular fluid (GCF) were measured 1, 3, 6 and 9 h after the morning dose each day. The concentration of tinidazole was determined by high performance liquid chromatography (HPLC). The mean concentration of tinidazole in GCF for each dog ranged from 6.05 to 9.32 micrograms/mL at different time points after the first dose, and on the first day the highest concentration was observed 6 h after the drug administration. Tinidazole concentrations were 34 +/- 4%-72 +/- 9% (mean +/- SEM) of simultaneous plasma concentration. At steady-state, on the third treatment day, the mean tinidazole concentrations in GCF ranged from 6.68 to 13.1 micrograms/mL, i.e. 44 +/- 6%-75 +/- 25% of the corresponding concentrations in plasma. Tinidazole concentration in GCF exceeded the MIC values for putative path-ogenic periodontal bacteria and it is concluded that, when indicated, tinidazole could be used for chemotherapy of periodontitis in dogs.

Administration, Oral↗
PubMed1978

Aspects of the pharmacology and pharmacokinetics of nitroimidazoles with special reference to tinidazole.

Tinidazole has been reported to be highly effective against trichomoniasis, giardiasis and amoebiasis. In vitro, tinidazole is more active against trichomonads than metronidazole and possesses antiprotozoal activity at least comparable to metronidazole against Entamoeba histolytica, Tinidazole gives higher serum levels in animals following oral administration than metronidazole and is well distributed in organs and tissues. When tinidazole or metronidazole is given to healthy volunteers at a dose of 2g orally, the serum level of tinidazole at 48h is considerably higher than that of metronidazole. At 72h tinidazole is still present but metronidazole is not. These pharmacokinetic differences result from the longer half-life of tinidazole. These findings suggest that tinidazole might prove to be more useful than metronidazole in the treatment of protozoal infections when given in once daily oral doses of 2g.

Animals↗
PubMedDate not supplied

Tinidazole--microbiology, pharmacology and efficacy in anaerobic infections.

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.

Anaerobiosis↗
PubMed2005

Rifabutin based triple therapy for eradication of H. pylori primary and secondary resistant to tinidazole and clarithromycin.

BACKGROUND: Rifabutin has been empirically used in Helicobacter pylori infections resistant to triple therapy. There are no data on primary and secondary resistance to rifabutin and its use in specific cases. AIM: To analyse the susceptibility and resistance to rifabutin in H. pylori-positive patients with or without previous H. pylori therapy and to test the efficacy of rifabutin in H. pylori resistant to clarithromycin and tinidazole. METHODS: Four hundred and twenty H. pylori-positive patients without previous exposure to triple therapy and 104 patients who had already received one course of triple therapy underwent upper endoscopy for dyspeptic symptoms and H. pylori susceptibility test. Amoxicillin, clarithromycin, tinidazole and rifabutin were evaluated for resistance and susceptibility. Forty patients with primary resistance to both clarithromycin and tinidazole and with susceptibility to amoxicillin and rifabutin, and 65 patients with secondary resistance and susceptibility to the same antibiotics were identified. All these patients received a 10-day triple therapy with pantoprazole amoxicillin and rifabutin. Treatment success was evaluated by the 13C-Urea Breath test. RESULTS: In naive patients 23% of strains were resistant to clarythromycin, 35% to tinidazole, 9% to both antibiotics, and none was resistant to rifabutin In patients already treated the percentages of resistant strains were 76, 64.4, 62.5 and 1%, respectively. With rifabutin based triple therapy eradication rates were (Per Protocol and Intention-to-Treat analysis) 100 and 87.5% in primary resistance to clarithromycin and tinidazole and 82.2 and 78.5% in secondary resistance. CONCLUSION: H. pylori primary and secondary resistances to clarithromycin and tinidazole are high in our geographic area, while resistance to rifabutin is rare. Rifabutin-based triple therapy, can be successfully used in primary and secondary resistance to clarithromycin and tinidazole according to the in vitro susceptibility test.

Adult↗
PubMed2006

Voltammetric sensor for tinidazole based on poly(carmine) film-modified electrode and its application.

A poly(carmine) film-modified glassy carbon electrode (GCE) was fabricated and the electrochemical behavior of tinidazole at the modified electrode was investigated by electrochemical methods. A well-defined reduction peak was observed at 0.61 V and was applied for the determination of tinidazole. Compared with that at a bare GCE, the reduction peak potential of tinidazole shifted negatively and the reduction peak current increased significantly. The influences of some parameters on the reduction of tinidazole were also examined. Based on the experimental data, a possible mechanism was proposed for the electrochemical reaction of tinidazole at the modified electrode. It was found that the reduction peak current was proportional to the concentration of tinidazole in the range from 1.0 x 10(-7) to 5.0 x 10(-5)mol L(-1). The detection limit was about 1.0 x 10(-8)mol L(-1) after accumulation 90 s at a constant potential of 0.0 V. The proposed method was applied to determine tinidazole in drugs and the result was satisfied.

Antitrichomonal Agents↗
PubMed1991

Single-dose concentrations of tinidazole in gingival crevicular fluid, serum, and gingival tissue in adults with periodontitis.

Previous studies have shown that metronidazole is effective in the treatment of subgingival microflora associated with destructive periodontitis. The aim of this study was to determine whether tinidazole, a close analogue of metronidazole, would reach sufficient concentrations in serum, gingival crevicular fluid, and gingival tissue, to inhibit putative periodontopathic bacteria. Ten adult patients with moderate to advanced periodontitis took a single 2-g dose of tinidazole orally. Samples were assayed by high-performance liquid chromatography. The concentrations of tinidazole in serum and GCF were in a similar range (3.2-46.5 micrograms/mL). Tinidazole was not detected in the GCF in three of the patients. The drug was found in gingival tissue obtained at two h (0.17 +/- 0.14 micrograms/mg) and six h (0.15 +/- 0.18 micrograms/mg) after oral administration. The mean concentration of tinidazole in serum at 24 h (13 +/- 3.0 micrograms/mL) is greater than the minimum inhibitory concentration for anaerobic bacteria as reported by others. The present data suggest that a single 2-g oral dose of tinidazole may lead to the presence of potentially bactericidal levels of tinidazole for up to 24 h in the periodontal pockets of some patients with periodontitis.

Administration, Oral↗