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Journal of Veterinary Science Nov 2023Antibiotic beads are used to treat local bacterial infections by delivering high drug concentrations to infected tissue.
BACKGROUND
Antibiotic beads are used to treat local bacterial infections by delivering high drug concentrations to infected tissue.
OBJECTIVES
This study examined the elution characteristics of metronidazole from metronidazole-calcium sulfate (MCa) and metronidazole-calcium-potassium sulfate (MCaK) beads over 20 days and the antibacterial efficacy of the beads after storage.
METHODS
The MCa and MCaK beads were prepared by mixing 250 mg of metronidazole and 10 g of calcium sulfate hemihydrate with water and a 3% potassium sulfate solution, respectively. The beads were placed in phosphate-buffered saline for the elution study. The metronidazole eluents were determined using high-performance liquid chromatography. The microstructures were examined by scanning electron microscopy (SEM), and the antimicrobial activity was evaluated by a microbioassay.
RESULTS
For the 20-day study, the total amount of metronidazole released was greater in the MCa beads than in the MCaK beads by 6.61 ± 0.48 mg (89.11% ± 3.04%) and 4.65 ± 0.36 mg (73.11% ± 4.38%), respectively. The amounts of eluted drugs from the MCa and MCaK beads were higher than the minimum inhibitory concentration at 0.5 µg/mL against anaerobic bacteria at both 20 days and 14 days. SEM showed that calcium crystals on the outer surface had dissolved after elution, and thinner calcium crystals were prominent in the MCaK beads. The MCa and MCaK beads exhibited antibacterial activity after setting, followed by storage at room temperature or 4°C for 21 days.
CONCLUSIONS
The MCa beads could release more drug than the MCaK beads, but all eluted metronidazole amounts were effective in controlling bacterial infections. Both metronidazole beads could be stored at ambient temperature or in a refrigerator.
Topics: Animals; Metronidazole; Calcium Sulfate; Calcium; Anti-Bacterial Agents; Bacterial Infections
PubMed: 37904636
DOI: 10.4142/jvs.23166 -
Antimicrobial Agents and Chemotherapy Jan 2024The intestinal parasites and are major causes of morbidity and mortality associated with diarrheal diseases. Metronidazole is the most common drug used to treat...
The intestinal parasites and are major causes of morbidity and mortality associated with diarrheal diseases. Metronidazole is the most common drug used to treat giardiasis and amebiasis. Despite its efficacy, treatment failures in giardiasis occur in up to 5%-40% of cases. Potential resistance of to metronidazole is an increasing concern. Therefore, it is critical to search for more effective drugs to treat giardiasis and amebiasis. We identified antigiardial and antiamebic activities of the rediscovered nitroimidazole compound, fexinidazole, and its sulfone and sulfoxide metabolites. Fexinidazole is equally active against and trophozoites, and both metabolites were 3- to 18-fold more active than the parent drug. Fexinidazole and its metabolites were also active against a metronidazole-resistant strain of . and cell extracts exhibited decreased residual nitroreductase activity when metabolites were used as substrates, indicating nitroreductase may be central to the mechanism of action of fexinidazole. In a cell invasion model, fexinidazole and its metabolites significantly reduced the invasiveness of trophozoites through basement membrane matrix. A q.d. oral dose of fexinidazole and its metabolites at 10 mg/kg for 3 days reduced infection significantly in mice compared to control. The newly discovered antigiardial and antiamebic activities of fexinidazole, combined with its FDA-approval and inclusion in the WHO Model List of Essential Medicines for the treatment of human African trypanosomiasis, offer decreased risk and a shortened development timeline toward clinical use of fexinidazole for treatment of giardiasis or amebiasis.
Topics: Mice; Animals; Humans; Giardiasis; Metronidazole; Nitroimidazoles; Amebiasis; Giardia lamblia; Entamoeba histolytica; Nitroreductases
PubMed: 38063401
DOI: 10.1128/aac.00731-23 -
Canadian Family Physician Medecin de... Aug 2002
Topics: Administration, Oral; Administration, Topical; Adult; Anti-Bacterial Agents; Bacterial Infections; Female; Gardnerella vaginalis; Humans; Metronidazole; Pregnancy; Pregnancy Complications, Infectious; Sexually Transmitted Diseases; Vaginosis, Bacterial
PubMed: 12228952
DOI: No ID Found -
The British Journal of Venereal Diseases Sep 1966
Topics: Female; Humans; Metronidazole; Pregnancy
PubMed: 5919867
DOI: 10.1136/sti.42.3.210 -
The Pediatric Infectious Disease Journal Sep 2020Metronidazole is frequently used off-label in infants with complicated intra-abdominal infections (cIAI) to provide coverage against anaerobic organisms, but its safety... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Metronidazole is frequently used off-label in infants with complicated intra-abdominal infections (cIAI) to provide coverage against anaerobic organisms, but its safety and efficacy in this indication are unknown.
METHODS
In the Antibiotic Safety in Infants with Complicated Intra-Abdominal Infections open-label multicenter trial infants ≥34 weeks gestation at birth and <121 days postnatal age with cIAIs were administered metronidazole as part of multimodal therapy. Metronidazole safety was evaluated by reporting of adverse events (AEs) and safety events of special interest. Cure from disease was determined by blood cultures and a clinical cure score >4. A blinded adjudication committee reviewed all safety events of special interest.
RESULTS
Fifty-five infants were included, median gestational age was 36 weeks (range: 34-41) and postnatal age was 7 days (0-63). The most common additional antibiotics received included gentamicin, piperacillin-tazobactam, ampicillin and vancomycin. Only one AE, a candidal rash, was identified to be potentially caused by metronidazole administration. One infant died of cardiopulmonary failure, which was deemed unrelated to metronidazole. The most common events of special interest included feeding intolerance in 18 (33%) infants, and exploratory laparotomy in 10 (18%) requiring intestinal anastomosis in 7 (13%) infants. There was 1 (2%) intestinal stricture. Fifty-three infants (96%) achieved overall therapeutic success, 54 (98%) were alive through 30 days post-study therapy, and 54 (98%) had 30-day clinical cure score >4.
CONCLUSIONS
In a cohort of late pre-term and term infants with cIAIs, combination antibiotic therapy that included metronidazole was safe, and therapeutic success was high.
Topics: Anti-Bacterial Agents; Cohort Studies; Drug Therapy, Combination; Drug-Related Side Effects and Adverse Reactions; Female; Gestational Age; Humans; Infant; Infant, Newborn; Intraabdominal Infections; Male; Metronidazole; United States
PubMed: 32453198
DOI: 10.1097/INF.0000000000002698 -
British Journal of Clinical Pharmacology Nov 1995Metronidazole pharmacokinetics were studied in patients with different degrees of liver cirrhosis, classified according to the Child-Pugh algorithm (A, B or C, as liver... (Clinical Trial)
Clinical Trial Comparative Study
Metronidazole pharmacokinetics were studied in patients with different degrees of liver cirrhosis, classified according to the Child-Pugh algorithm (A, B or C, as liver disease severity increases) and in schistosomic patients. Metronidazole (500 mg) was administered i.v. as a slow infusion over 20 min, and blood samples were collected at set intervals after the end of the infusion. The plasma concentrations of metronidazole and its main metabolite hydroxy-metronidazole were quantified by reversed-phase h.p.l.c. with u.v. detection. The metronidazole and hydroxy-metronidazole areas under the curve from 0 to 24 h (AUC0,24h), the metronidazole terminal elimination half-life (t1/2), the total clearance (CL), the metronidazole volume of distribution (V) values and the hydroxy-metronidazole/metronidazole concentration ratios as a function of time were calculated for each group. Comparison of the metronidazole AUC0,24h, t1/2 and CL values revealed that metronidazole metabolism is progressively impaired as the severity of liver disease increases. There were no variations in these parameters between the schistosomic and Child-Pugh A groups. In addition, there were no differences in the V and hydroxy-metronidazole AUC0,24h among the various groups studied. However, metronidazole metabolism was delayed in patients with hepatic disease, as illustrated by the hydroxy-metronidazole/metronidazole ratio 10 min after the end of metronidazole infusion. These results indicate that the clinical assessment of liver disease is paralleled by an impairment of metronidazole metabolism. Of the studied variables, we propose the hydroxy-metronidazole/metronidazole ratio 10 min after metronidazole infusion as a suitable and practical index for liver function evaluation.
Topics: Adult; Biotransformation; Female; Half-Life; Humans; Liver Cirrhosis; Liver Function Tests; Male; Metronidazole; Middle Aged; Schistosomiasis mansoni
PubMed: 8703652
DOI: 10.1111/j.1365-2125.1995.tb05792.x -
Expert Review of Anti-infective Therapy Aug 2022Single-dose 2-g oral secnidazole (SEC), newly approved by the U.S. Food and Drug administration (FDA) for treatment of trichomoniasis, is a potent 5-nitroimidazole with...
INTRODUCTION
Single-dose 2-g oral secnidazole (SEC), newly approved by the U.S. Food and Drug administration (FDA) for treatment of trichomoniasis, is a potent 5-nitroimidazole with selective toxicity against various micro-organisms. It has been used internationally to treat trichomoniasis, bacterial vaginosis, and other infections for decades. Trichomoniasis is the most common non-viral sexually transmitted infection worldwide and is associated with significant morbidity. In comparison to the only other FDA-approved treatments for trichomoniasis in the United States - metronidazole and tinidazole - SEC has favorable pharmacokinetics, including a longer half-life and a lower minimal lethal concentration.
AREAS COVERED
This work summarizes the chemistry and pharmacology of SEC and reviews the evidence on its efficacy, tolerability, and safety for the treatment of trichomoniasis.
EXPERT OPINION
SEC is an efficacious, well tolerated, and safe treatment for patients aged ≥12 years with trichomoniasis. Single-dose administration makes it a favorable treatment option, especially in cases where adherence to multi-dose treatment regimens may be low.
Topics: Adolescent; Adult; Female; Humans; Metronidazole; Nitroimidazoles; Trichomonas Infections; Trichomonas Vaginitis; Trichomonas vaginalis; United States; Vaginosis, Bacterial
PubMed: 35642509
DOI: 10.1080/14787210.2022.2080656 -
Neurology India 2020
Topics: Anti-Infective Agents; Brain Diseases; Humans; Magnetic Resonance Imaging; Metronidazole
PubMed: 32415040
DOI: 10.4103/0028-3886.284372 -
BMC Women's Health May 2023Bacterial vaginosis is a common and distressing condition for women. Short-term antibiotic treatment is usually clinically effective, but recurrence is common. We... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Bacterial vaginosis is a common and distressing condition for women. Short-term antibiotic treatment is usually clinically effective, but recurrence is common. We assessed the effectiveness of intravaginal lactic acid gel versus oral metronidazole for treating recurrent bacterial vaginosis.
METHODS
We undertook an open-label, multicentre, parallel group, randomised controlled trial in nineteen UK sexual health clinics and a university health centre. Women aged ≥ 16 years, with current bacterial vaginosis symptoms and a preceding history of bacterial vaginosis, were randomised in a 1:1 ratio using a web-based minimisation algorithm, to 400 mg twice daily oral metronidazole tablets or 5 ml once daily intravaginal lactic acid gel, for 7 days. Masking of participants was not possible. The primary outcome was participant-reported resolution of symptoms within 2 weeks. Secondary outcomes included time to first recurrence of symptoms, number of recurrences and repeat treatments over 6 months and side effects.
RESULTS
Five hundred and eighteen participants were randomised before the trial was advised to stop recruiting by the Data Monitoring Committee. Primary outcome data were available for 79% (204/259) allocated to metronidazole and 79% (205/259) allocated to lactic acid gel. Resolution of bacterial vaginosis symptoms within 2 weeks was reported in 70% (143/204) receiving metronidazole versus 47% (97/205) receiving lactic acid gel (adjusted risk difference -23·2%; 95% confidence interval -32.3 to -14·0%). In those participants who had initial resolution and for whom 6 month data were available, 51 of 72 (71%) women in the metronidazole group and 32 of 46 women (70%) in the lactic acid gel group had recurrence of symptoms, with median times to first recurrence of 92 and 126 days, respectively. Reported side effects were more common following metronidazole than lactic acid gel (nausea 32% vs. 8%; taste changes 18% vs. 1%; diarrhoea 20% vs. 6%, respectively).
CONCLUSIONS
Metronidazole was more effective than lactic acid gel for short-term resolution of bacterial vaginosis symptoms, but recurrence is common following both treatments. Lactic acid gel was associated with fewer reported side effects.
TRIAL REGISTRATION
ISRCTN14161293 , prospectively registered on 18 September 2017.
Topics: Humans; Female; Male; Metronidazole; Vaginosis, Bacterial; Drug-Related Side Effects and Adverse Reactions; Ambulatory Care Facilities; Lactic Acid
PubMed: 37161454
DOI: 10.1186/s12905-023-02303-5 -
The Indian Journal of Medical Research Feb 2006Amoebiasis caused by Entamoeba histolytica, is a major public health problem in developing countries. Morphologically similar E. dispar is non pathogenic. Because of the... (Review)
Review
Amoebiasis caused by Entamoeba histolytica, is a major public health problem in developing countries. Morphologically similar E. dispar is non pathogenic. Because of the redefinition of E. histolytica and E. dispar, and the limited number of antiamoebic drugs available, a new approach to treat such individuals is necessary. The cost of treating asymptomatic individuals is highly exorbitant and not justifiable. The indiscriminate use of antiamoebic drugs can result in increased minimum inhibitory concentration (MIC) values against Entamoeba species, and treatment failure may emerge as an important public health problem. Development of new antiamoebic drugs is still in infancy and vaccine development appears to be distant dream. In future, the development of drug resistance may seriously affect the control of disease. This review discusses the factors involved in drug resistance mechanisms developed by the parasite.
Topics: Animals; Antiprotozoal Agents; Drug Resistance, Multiple; Entamoeba histolytica; Entamoebiasis; Humans; Metronidazole
PubMed: 16575108
DOI: No ID Found