Efficacy of pharmacokinetic interactions between piperonyl butoxide and albendazole against gastrointestinal nematodiasis in goats

2015 ◽  
Vol 90 (5) ◽  
pp. 624-629 ◽  
Author(s):  
N.K. Kumbhakar ◽  
P.K. Sanyal ◽  
D. Rawte ◽  
D. Kumar ◽  
A.E. Kerketta ◽  
...  
Keyword(s):  
Body Weight ◽  
Half Life ◽  
Maximum Concentration ◽  
Piperonyl Butoxide ◽  
Time Curve ◽  
Concentration Time ◽  
Elimination Half ◽  
Concentration Maximum ◽  
Faecal Egg Count ◽  
Minimum Residence Time

AbstractTo test the hypothesis that modulation of hepatic microsomal sulphoxidation and sulphonation by the cytochrome P450 inhibitor piperonyl butoxide could increase bioavailability of albendazole, the present study was undertaken to understand the pharmacokinetics of albendazole in goats at a dose of 7.5 mg kg− 1 body weight with and without co-administration with piperonyl butoxide at 63.0 mg kg− 1 body weight. Plasma albendazole sulphoxide metabolite, the anthelmintically active moiety, reached its maximum concentration of 0.322 ± 0.045 μg ml− 1 and 0.384 ± 0.013 μg ml− 1 at 18 h and 24 h after administration of albendazole alone and co-administration of albendazole with piperonyl butoxide, respectively. Analysis of the data revealed statistically increased albendazole sulphoxide levels at 24 (P <  0.001), 30 (P <  0.001) and 36 h (P <  0.01) after administration of albendazole with piperonyl butoxide, with statistically increased levels of albendazole sulphone at 24, 30 and 48 h after administration. No significance difference (P > 0.05) in values of maximum concentration (normal and calculated) could be observed between groups of goats. However, values of time to reach the concentration maximum (normal and calculated), area under the concentration–time curve (0–∞ and calculated), minimum residence time, distribution half-life, elimination half-life and total area under the first movement of plasma drug concentration–time curve were significantly higher (P <  0.05) in plasma levels of albendazole sulphoxide in goats following single oral co-administration of albendazole with piperonyl butoxide. The faecal egg count reduction and lower 95% confidence limit for the group treated with albendazole alone were 97 and 68%, while for co-administration of albendazole and piperonyl butoxide the values were 99 and 97%, respectively. The ED50 for egg hatch was 0.196, indicating suspected resistance to benzimidazole anthelmintics. The drug combination proved efficacious against an albendazole-resistant nematode parasite population in goats.

Diet-induced modulation of pharmacokinetics of albendazole in Sahiwal cattle

2015 ◽  
Vol 90 (5) ◽  
pp. 555-560 ◽  
Author(s):  
P.K. Sanyal ◽  
D. Rawte ◽  
A.E. Kerketta ◽  
N.K. Kumbhakar ◽  
D. Kumar ◽  
...  
Keyword(s):  
Half Life ◽  
Maximum Concentration ◽  
Active Metabolite ◽  
Time Curve ◽  
Active Moiety ◽  
Concentration Time ◽  
Elimination Half ◽  
Green Fodder ◽  
Pre Treatment ◽  
Diet Type

AbstractThe influence of diet type and pre-treatment fasting on the kinetic disposition of albendazole was evaluated in Sahiwal heifers following oral and intra-ruminal administration of the drug. The anthelmintically active moiety albendazole sulphoxide appeared early and was eliminated early in cattle offered green fodder, with decreased maximum concentration (Cmax) and area under concentration–time curve (AUC) when the drug was administered both through oral and intra-ruminal routes. Further, the elimination half-life (t½β) revealed significantly increased values for albendazole sulphoxide in cattle administered albendazole through the intra-ruminal route. An increased AUC and t½β is reflective of increased bioavailability of albendazole in animals offered dry fodder. Increased values (P <  0.05) of Cmax, time to Cmax (Tmax), AUC and t½β for albendazole sulphoxide occurred in cattle with a pre-treatment 24-h fast, resulting in its increased bioavailability. Extrapolation of data of the active metabolite albendazole sulphoxide levels in terms of drug–parasite contact revealed increased exposure of parasites to the drug in cattle administered albendazole through the intra-ruminal route and with 24-h pre-treatment fasting.

scholarly journals Interaction between Grapefruit Juice and Praziquantel in Humans

2002 ◽  
Vol 46 (5) ◽  
pp. 1614-1616 ◽  
Author(s):  
Nelly Castro ◽  
Helgi Jung ◽  
Roberto Medina ◽  
Dinora González-Esquivel ◽  
Mario Lopez ◽  
...  
Keyword(s):  
Water Treatment ◽  
Oral Dose ◽  
Single Oral Dose ◽  
Half Life ◽  
Maximum Concentration ◽  
Grapefruit Juice ◽  
Time Curve ◽  
Elimination Half Life ◽  
Concentration Time ◽  
Elimination Half

ABSTRACT After a single oral dose of praziquantel with 250 ml of grapefruit juice, the area under the concentration-time curve and the maximum concentration in plasma of praziquantel (C max) were significantly increased (C max for water treatment, 637.71 ± 128.5 ng/ml; and C max for grapefruit juice treatment, 1,037.65 ± 305.7 ng/ml, P < 0.05). No statistically significant differences were found in the time to maximum concentration of drug in plasma or elimination half-life.

scholarly journals Safety, toleration, and pharmacokinetics of intravenous azithromycin.

1996 ◽  
Vol 40 (11) ◽  
pp. 2577-2581 ◽  
Author(s):  
D R Luke ◽  
G Foulds ◽  
S F Cohen ◽  
B Levy
Keyword(s):  
Half Life ◽  
Active Drug ◽  
Slow Release ◽  
Volume Of Distribution ◽  
Pharmacokinetic Parameters ◽  
Time Curve ◽  
Concentration Time ◽  
Elimination Half ◽  
The Mean ◽  
Male Subjects

To date, the clinical pharmacology of large intravenous doses of azithromycin has not been described. In the present study, single 2-h intravenous infusions of 1, 2, and 4 g of azithromycin were administered to three parallel groups (in each group, six received active drug and two received placebo) of healthy male subjects. Toleration (assessed by scores of subject-administered visual analog scale tests spanning 0 [good] to 10 [poor]), safety, pharmacokinetics, and serum motilin levels were monitored for up to 240 h after the start of each intravenous infusion. Mean nausea scores of 0.0, 0.0, 1.0, and 0.5 and abdominal cramping scores of 0.0, 0.0, 0.4, and 0.4 for 12-h periods after doses of 0, 1, 2, and 4 g of azithromycin, respectively, suggested that azithromycin was well tolerated. Because of the standardized 1-mg/ml infusates, all subjects in the 4-g dosing group complained of an urgent need to urinate. There were no consistent trends in endogenous motilin levels throughout the study. The maximum concentration of azithromycin in serum (10 micrograms/ml after a 4-g dose) and the area under the concentration-time curve (82 micrograms.h/ml after a 4-g dose) were dose related. The mean pharmacokinetic parameters were an elimination half-life of 69 h, total systemic clearance of 10 ml/min/kg, and a volume of distribution at steady state of 33.3 liters/kg. The pharmacokinetic results suggest that the long half-life of azithromycin is due to extensive uptake and slow release of the drug from tissues rather than an inability to clear the drug. Single intravenous doses of up to 4 g of azithromycin in healthy subjects are generally well tolerated, and quantifiable concentrations may persist in serum for 10 days or more.

scholarly journals Effect of Calcium Carbonate on Bioavailability of Orally Administered Gemifloxacin

2003 ◽  
Vol 47 (7) ◽  
pp. 2158-2160 ◽  
Author(s):  
M. W. Pletz ◽  
P. Petzold ◽  
A. Allen ◽  
O. Burkhardt ◽  
H. Lode
Keyword(s):  
Calcium Carbonate ◽  
Oral Bioavailability ◽  
Half Life ◽  
Maximum Concentration ◽  
Time Curve ◽  
Concentration Time

ABSTRACT We investigated the effect of calcium carbonate on the oral bioavailability of gemifloxacin. Gemifloxacin was administered alone, 2 h before, simultaneously, or 2 h after calcium carbonate in 16 volunteers. Data for 320 mg of gemifloxacin alone were as follows: maximum concentration of drug in serum (C max),13 μg/ml; half-life, 7.33 h; and area under the concentration-time curve from 0 h to infinity (AUC∞), 6.79 μg · h/ml. Only simultaneous coadministration of calcium carbonate reduced C max (−17%) and AUC∞ (−21%) significantly.

scholarly journals ABT-773: Pharmacokinetics and Interactions with Ranitidine and Sucralfate

2003 ◽  
Vol 47 (3) ◽  
pp. 1129-1131 ◽  
Author(s):  
M. W. Pletz ◽  
V. Preechachatchaval ◽  
J. Bulitta ◽  
M. Allewelt ◽  
O. Burkhardt ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Half Life ◽  
Maximum Concentration ◽  
Time Curve ◽  
Concentration Time ◽  
Plasma Concentration Time Curve

ABSTRACT We assessed the pharmacokinetics and interaction of ABT-773 in 12 volunteers receiving ABT-773 alone or concomitantly with ranitidine or sucralfate. Data for 150 mg of ABT-773 were as follows: the maximum concentration of the drug in plasma (C max) was 318 ng/ml, its half-life was 5.66 h, and its area under the plasma concentration-time curve from 0 h to ∞ (AUC0-∞) was 1,662 ng · h/ml. Coadministration of ranitidine, reduced the C max (−25.7%) and AUC0-∞ (−15.8%) significantly. Sucralfate had no impact on the bioavailability of ABT-773.

Dose Proportionality and Pharmacokinetics of Oral Transmucosal Fentanyl Citrate 

1998 ◽  
Vol 88 (2) ◽  
pp. 305-309 ◽  
Author(s):  
James B. Streisand ◽  
Michael A. Busch ◽  
Talmage D. Egan ◽  
Barbara Gaylord Smith ◽  
Mason Gay ◽  
...  
Keyword(s):  
Respiratory Rate ◽  
Half Life ◽  
Maximum Concentration ◽  
Area Under The Curve ◽  
Supplemental Oxygen ◽  
Fentanyl Citrate ◽  
Oral Transmucosal Fentanyl Citrate ◽  
Concentration Time ◽  
Elimination Half ◽  
Dose Proportional

Background The pharmacokinetics of a single dose (15 microg/kg) of oral transmucosal fentanyl citrate (OTFC) have been characterized. A range of doses may eventually be used in clinical practice. The goal of this study was to determine if the pharmacokinetics of OTFC are dose proportional for doses ranging from 200 to 1,600 microg. Methods Twelve healthy male volunteers were studied on four different occasions, receiving 200, 400, 800, and 1,600 microg OTFC in a double-blind, randomized protocol. Venous blood samples were collected at selected times during and after dosing for a 24-h period and assayed for fentanyl using a radioimmunoassay. Maximum concentration, time to maximum concentration, area under the curve, and elimination half-life were determined for each dose administered. In addition, respiratory rate, need for verbal prompting to breathe, and supplemental oxygen requirements were noted. Results Mean fentanyl concentration time curves were similarly shaped with increasing doses. Both peak concentrations and area under the curve increased linearly with an increase in dose, whereas time to reach peak serum concentrations did not vary significantly between doses. Except for the 200-microg dose, the apparent elimination half-life remained relatively constant (358-386 min). The incidence of low respiratory rate, supplemental oxygen requirement, and number of breathing prompts significantly increased with increasing doses. Conclusions Oral transmucosal fentanyl citrate exhibits dose-proportional pharmacokinetics over the dose range of 200-1,600 microg.

Pharmacokinetics and Inflammatory Fluid Penetration of Clinafloxacin

1998 ◽  
Vol 42 (2) ◽  
pp. 428-430 ◽  
Author(s):  
R. Wise ◽  
S. Jones ◽  
I. Das ◽  
J. M. Andrews
Keyword(s):  
Half Life ◽  
Maximum Concentration ◽  
Healthy Male ◽  
Elimination Half Life ◽  
Concentration Time ◽  
Healthy Male Volunteers ◽  
Elimination Half ◽  
The Mean ◽  
Fluid Penetration ◽  
Mean Time

ABSTRACT A single 200-mg dose of clinafloxacin was given orally to each of nine healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharidin-induced inflammatory fluid, and urine over the following 24 h (48 h in the case of urine). The mean maximum concentration in plasma was 1.34 μg/ml at a mean time of 1.8 h postdose. The mean maximum concentration in the inflammatory fluid was 1.3 μg/ml at 3.8 h postdose. The mean elimination half-life of clinafloxacin in plasma was 5.65 h. The overall penetration into the inflammatory fluid was 93.1%, as assessed by determining the ratio of area under the concentration-time curves. Recovery of clinafloxacin in urine was 58.8% by 24 h and 71.8% by 48 h postdose.

scholarly journals Pharmacokinetics and Inflammatory Fluid Penetration of Intravenous Daptomycin in Volunteers

2002 ◽  
Vol 46 (1) ◽  
pp. 31-33 ◽  
Author(s):  
R. Wise ◽  
T. Gee ◽  
J. M. Andrews ◽  
B. Dvorchik ◽  
G. Marshall
Keyword(s):  
Body Weight ◽  
Standard Deviation ◽  
Total Drug ◽  
Healthy Male ◽  
Urinary Recovery ◽  
Time Curve ◽  
Concentration Time ◽  
Elimination Half ◽  
The Mean ◽  
Fluid Penetration

ABSTRACT The lipopeptide antimicrobial daptomycin was administered intravenously at a dose of 4 mg/kg of body weight to seven healthy male volunteers. The concentrations of daptomycin in plasma, cantharidin-induced inflammatory fluid, and urine were measured by a microbiological assay. The mean ± standard deviation peak concentrations in plasma and inflammatory fluid were 77.5 ± 8.3 and 27.6 ± 9.5 μg/ml, respectively; the mean terminal elimination half-lives were 7.74 and 13.2 h, respectively. The overall penetration of total drug into the inflammatory fluid (measured by ratio of the area under the concentration-time curve from 0 to 24 h for inflammatory fluid compared with that for plasma) was 68.4%. The mean urinary recovery over 24 h was 59.7%.

Pharmacokinetics and penetration into inflammatory fluid of trovafloxacin (CP-99,219).

1996 ◽  
Vol 40 (1) ◽  
pp. 47-49 ◽  
Author(s):  
R Wise ◽  
D Mortiboy ◽  
J Child ◽  
J M Andrews
Keyword(s):  
Oral Dose ◽  
Half Life ◽  
Maximum Concentration ◽  
Healthy Male ◽  
Elimination Half Life ◽  
Concentration Time ◽  
Elimination Half ◽  
The Mean ◽  
Systemic Infections ◽  
Mean Time

A single 200-mg oral dose of trovafloxacin (CP-99,219) was given to each of eight healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharides-induced inflammatory fluid, and urine over the subsequent 36 h. The mean maximum concentration observed in plasma was 2.9 micrograms/ml at a mean time of 0.75 h postdose. The mean maximum concentration observed in inflammatory fluid was 1.2 micrograms/ml at 4.0 h postdose. The mean elimination half-life in plasma was 7.8 h. The overall penetration into inflammatory fluid was 64%, as assessed by determining the ratio of the area under the concentration-time curves. Recovery of the dose in urine within the first 36 h postdose was 5.0% of the administered dose. Our results indicate that trovafloxacin, at a dosage of 200 mg once or twice daily, should be adequate for the treatment of systemic infections caused by most common bacterial pathogens.

scholarly journals Pharmacokinetics of Ethambutol under Fasting Conditions, with Food, and with Antacids

1999 ◽  
Vol 43 (3) ◽  
pp. 568-572 ◽  
Author(s):  
Charles A. Peloquin ◽  
Amy E. Bulpitt ◽  
George S. Jaresko ◽  
Roger W. Jelliffe ◽  
James M. Childs ◽  
...  
Keyword(s):  
Maximum Concentration ◽  
Pharmacokinetic Model ◽  
Mass Spectrometry Data ◽  
Gas Chromatography Mass Spectrometry ◽  
High Fat ◽  
Time Curve ◽  
First Order ◽  
Concentration Time ◽  
Males And Females ◽  
Fat Meal

ABSTRACT Ethambutol (EMB) is the most frequent “fourth drug” used for the empiric treatment of Mycobacterium tuberculosis and a frequently used drug for infections caused by Mycobacterium avium complex. The pharmacokinetics of EMB in serum were studied with 14 healthy males and females in a randomized, four-period crossover study. Subjects ingested single doses of EMB of 25 mg/kg of body weight under fasting conditions twice, with a high-fat meal, and with aluminum-magnesium antacid. Serum was collected for 48 h and assayed by gas chromatography-mass spectrometry. Data were analyzed by noncompartmental methods and by a two-compartment pharmacokinetic model with zero-order absorption and first-order elimination. Both fasting conditions produced similar results: a mean (± standard deviation) EMB maximum concentration of drug in serum (C max) of 4.5 ± 1.0 μg/ml, time to maximum concentration of drug in serum (T max) of 2.5 ± 0.9 h, and area under the concentration-time curve from 0 h to infinity (AUC0–∞) of 28.9 ± 4.7 μg · h/ml. In the presence of antacids, subjects had a mean C maxof 3.3 ± 0.5 μg/ml, T max of 2.9 ± 1.2 h, and AUC0–∞ of 27.5 ± 5.9 μg · h/ml. In the presence of the Food and Drug Administration high-fat meal, subjects had a mean C max of 3.8 ± 0.8 μg/ml, T max of 3.2 ± 1.3 h, and AUC0–∞ of 29.6 ± 4.7 μg · h/ml. These reductions in C max, delays inT max, and modest reductions in AUC0–∞ can be avoided by giving EMB on an empty stomach whenever possible.

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