Bile and serum levels of tinidazole after a single oral dose.

Hunt, P. S.; Davidson, A J; Alden, J; Cheng, S

doi:10.1111/j.1365-2125.1982.tb01363.x

Cited by 11 publications

(3 citation statements)

References 5 publications

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“…Tinidazole displays extensive tissue distribution with a V d in healthy volunteers of 0.64 to 0.67 L/ kg after single or multiple intravenous doses (Chaikin et al 1982). Highest concentrations are found in the bile where they rise slowly and then approximate serum concentrations 12h after administration (Hunt et al 1982). Similar concentrations can also be found in saliva, with a mean saliva: plasma ratio of 0.9 (Wood et al 1982).…”

Section: Clinical Pharmacokinetics 0/ Concentrations Decline By Firstmentioning

confidence: 91%

Clinical Pharmacokinetics of Metronidazole and Other Nitroimidazole Anti-Infectives

Lau

Lam

Piscitelli

et al. 1992

Clinical Pharmacokinetics

184

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Metronidazole was first introduced for the treatment of trichomoniasis. Its therapeutic use has subsequently been expanded to include amoebiasis, giardiasis and, more recently, anaerobic infections. Most of the early pharmacokinetic studies employed nonspecific assays such as microbiological and chemical assays. These assays were not able to differentiate the parent drug from the metabolites or other interfering substances. Pharmacokinetic data obtained through the use of specific chromatographic techniques provide the basis for this review of recent pharmacokinetic findings concerning metronidazole and other nitroimidazole antibiotics. When given intravenously or orally at usual recommended doses, metronidazole attains concentrations well above the minimum inhibitory concentrations for most susceptible micro-organisms. The drug has an oral bioavailability approaching 100%. Rectal and vaginal administration results in a smaller amount of drug absorption and lower serum concentrations. Metronidazole has limited plasma protein binding but can attain very favourable tissue distribution, including into the central nervous system. The drug is extensively metabolised by the liver to form 2 primary oxidative metabolites: the hydroxy and acetic acid metabolites. The kidney is responsible for the elimination of only a small amount of the parent drug; however, normal excretion of the 2 metabolites is dependent on the integrity of kidney function. The metabolism of metronidazole was found to vary among patient groups. Preterm and term infants have lower total body clearance (CL) and prolonged elimination half-lives. However, children older than 4 years old were observed to have pharmacokinetic parameters similar to those in adults. Reduced CL was also observed in children who are malnourished. Elderly patients have reduced renal excretion of both the parent drug and hydroxy metabolite. Pharmacokinetic parameters in pregnant patients were not significantly different from those in nonpregnant women; however, the drug is distributed into breastmilk and the infant will be exposed to the drug through the nursing mother. Patients undergoing gastrointestinal surgery or having enteric diseases and those who are hospitalised or critically ill also have altered pharmacokinetics. Metabolism of the drug is reduced in patients with liver dysfunction, giving delayed production of metabolites. In contrast, renal failure has little effect on the elimination of the parent drug, but affects the excretion of the metabolites more significantly. Haemodialysis was found to remove a substantial amount of the metronidazole while the effect of peritoneal dialysis was more limited. Energy and protein deficient diets as well as occupational exposure to gasoline did not alter metronidazole pharmacokinetics. However, the effect of alcohol consumption on metronidazole CL requires further study.(ABSTRACT TRUNCATED AT 400 WORDS)

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Section: Clinical Pharmacokinetics 0/ Concentrations Decline By Firstmentioning

confidence: 91%

Clinical Pharmacokinetics of Metronidazole and Other Nitroimidazole Anti-Infectives

Lau

Lam

Piscitelli

et al. 1992

Clinical Pharmacokinetics

184

View full text Add to dashboard Cite

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“…Renal clearance was about 8% of total body clearance, whereas in healthy subjects renal clearance was approximately 25% of body clearance, but this decrease in renal clearance in renal failure was not sufficient to modify plasma tinidazole elimination. It was thought possible that most of the drug (either unchanged or metabolized) was eliminated through the liver and the bile (Hunt et al, 1982) into the gastrointestinal tract, especially in renal failure, during which there would be an increase in hepatic blood flow (1.1 I/min in normal to 1.7 I/min in terminal renal failure).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of tinidazole in chronic renal failure and in patients on haemodialysis.

Flouvat¹,

Imbert²,

Dubois³

et al. 1983

Brit J Clinical Pharma

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The pharmacokinetics of tinidazole after infusion (800 mg in 15 min) were studied in 12 patients with chronic renal failure (RI) and in five patients undergoing regular dialysis treatment (RD). Tinidazole elimination plasma half‐life was 15.09 +/‐ 0.68 h (mean +/‐ s.e. mean) (RI) and 12.9 +/‐ 1.0 h after dialysis (RD), but there was a significant decrease in half‐life during dialysis (4.25 +/‐ 0.43 h) P less than 0.001). The apparent volume of distribution (0.64 +/‐ 0.03 l/kg) was equal to extra and intracellular water volume and tinidazole was little bound to plasma protein (8%). There was a slight sex difference in apparent volume of distribution between male patients (0.70 +/‐ 0.09 l/kg) and female patients (0.59 +/‐ 0.10 l/kg) (P = 0.07), but as body clearance decreases in the same order, there was no modification of plasma half‐life. In renal failure, pharmacokinetics of tinidazole were not disturbed because no correlation between half‐life, body clearance and creatinine clearance occurred; urine elimination was about 7% of administered dose. Plasma clearance during dialysis was 49.9 +/‐ 3.2 ml/min and about 43% of the available drug was eliminated during the 6 h dialysis procedure. These results suggest that an additional half‐dose infusion should be given after the end of dialysis in patients undergoing regular dialysis treatment.

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“…The drug resin complex is absolutely tasteless with no after taste, and at the same time, its bioavailability is not affected. AZT is orally absorbed drug used in the treatment or prevents certain bacterial infections, most often those causing middle ear infections, throat, pneumonia, typhoid, bronchitis and sinusitis 3 . Being highly bitter drug AZT posses a challenge particularly in the formulation of a pediatric dosage form.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Taste Masked Suspension of Azithromycin Dihydrate

Shet¹,

Vaidya²,

Hiranandani³

2013

JCPR

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The article describes strategy for masking the intensely bitter taste of Azithromycin Dihydrate (AZT) by using complexation with Kyron T-134. The resinates prepared with drug-Kyron T-134 ratio (1:3) at pH 8, gave maximum drug loading. Suspension containing, resinate showed more than 90% invitro drug release within 45min. Prepared formulation showed good stability and retention of palatable taste. Thus, the "patient-friendly dosage form" of bitter drugs, especially for pediatric, geriatric, bedridden, and non cooperative patients, can be successfully formulated using this technology.

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Bile and serum levels of tinidazole after a single oral dose.

Cited by 11 publications

References 5 publications

Clinical Pharmacokinetics of Metronidazole and Other Nitroimidazole Anti-Infectives

Clinical Pharmacokinetics of Metronidazole and Other Nitroimidazole Anti-Infectives

Pharmacokinetics of tinidazole in chronic renal failure and in patients on haemodialysis.

Formulation and Evaluation of Taste Masked Suspension of Azithromycin Dihydrate

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