scholarly journals Intravenous Voriconazole after Toxic Oral Administration

2009 ◽  
Vol 54 (6) ◽  
pp. 2741-2742 ◽  
Author(s):  
J. W. C. Alffenaar ◽  
S. van Assen ◽  
J. G. R. de Monchy ◽  
D. R. A. Uges ◽  
J. G. W. Kosterink ◽  
...  
Keyword(s):  
Oral Administration ◽  
Invasive Aspergillosis ◽  
Liver Enzyme ◽  
Male Patient ◽  
Intravenous Administration ◽  
Portal Blood ◽  
Cutaneous Reaction ◽  
High Concentrations ◽  
Severe Cutaneous Reaction

ABSTRACT In a male patient with rhinocerebral invasive aspergillosis, prolonged high-dosage oral administration of voriconazole led to hepatotoxicity combined with a severe cutaneous reaction while intravenous administration in the same patient did not. High concentrations in the portal blood precipitate liver enzyme abnormalities, and therefore, oral administration of voriconazole may have a hepatotoxicity profile different from that of intravenous (i.v.) administration. Intravenously administered voriconazole might still be an option after oral-voriconazole-induced toxicity has resolved.

scholarly journals Effects of Diabetes Mellitus Induced by Alloxan on the Pharmacokinetics of Metformin in Rats: Restoration of Pharmacokinetic Parameters to the Control State by Insulin Treatment

2008 ◽  
Vol 11 (1) ◽  
pp. 88 ◽  
Author(s):  
Myung G. Lee ◽  
Young H Choi ◽  
Inchul Lee
Keyword(s):  
Diabetes Mellitus ◽  
Oral Administration ◽  
Protein Expression ◽  
Intravenous Administration ◽  
Insulin Treatment ◽  
Pharmacokinetic Parameters ◽  
Mrna Levels ◽  
Altered Pharmacokinetic ◽  
Intravenous And Oral Administration ◽  
Control State

To test the effect of insulin treatment on the pharmacokinetics of metformin in rats with diabetes mellitus induced by alloxan (DMIA rats). The following results were reported from other studies. Metformin was metabolized via hepatic CYP2C11, 2D1, and 3A1/2 in rats. In DMIA rats, the protein expression and mRNA levels of hepatic CYP2C11 and 3A1/2 decreased and increased, respectively. In rat model of diabetes mellitus induced by streptozotocin, the protein expression of hepatic CYP2D1 was not changed. The increase in hepatic CYP1A2, 2B1, and 2E1, and decrease in hepatic CYP2C11 in DMIA rats was returned to the controls by insulin treatment. METHODS. Metformin (100 mg/kg) was administered intravenously and orally to the control rats, DMIA rats, and DMIA rats with insulin treatment for 3 weeks (DMIA rats with insulin). RESULTS. After intravenous administration of metformin to the DMIA rats, the CLR and CLNR of the drug were significantly slower than the controls. After oral administration of metformin to the DMIA rats, the AUC of the drug was also significantly greater than the controls. After intravenous administration of metformin to the DMIA rats with insulin, the significantly slower CLNR of the drug in the DMIA rats was returned to the controls. The altered pharmacokinetic indices observed following intravenous and oral administration of metformin to DMIA rats returned to the control values in the DMIA rats with insulin. CONCLUSIONS. The significantly slower CLNR of metformin in the DMIA rats could be due to the decrease in hepatic CYP2C11 than the controls. The comparable CLNR of metformin between the DMIA rats with insulin and the control rats could be due to restoration of hepatic CYP enzyme changes in DMIA rats to the controls.

scholarly journals Detection of curcumin and its metabolites in hepatic tissue and portal blood of patients following oral administration

2004 ◽  
Vol 90 (5) ◽  
pp. 1011-1015 ◽  
Author(s):  
G Garcea ◽  
D J L Jones ◽  
R Singh ◽  
A R Dennison ◽  
P B Farmer ◽  
...  
Keyword(s):  
Oral Administration ◽  
Portal Blood ◽  
Hepatic Tissue

scholarly journals Physicochemical Effects of the Major Quassinoids in a Standardized Eurycoma longifolia Extract (Fr 2) on the Bioavailability and Pharmacokinetic Properties, and their Implications for Oral Antimalarial Activity

2011 ◽  
Vol 6 (3) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Bin-Seng Low ◽  
Chin-Hoe Teh ◽  
Kah-Hay Yuen ◽  
Kit-Lam Chan
Keyword(s):  
Oral Administration ◽  
Intravenous Administration ◽  
Antimalarial Activity ◽  
Elimination Rate ◽  
Rat Plasma ◽  
Chemical Degradation ◽  
Absolute Bioavailability ◽  
Phytochemical Analysis ◽  
Eurycoma Longifolia ◽  
Pharmacokinetic Properties

A simple validated LC-UV method for the phytochemical analysis of four bioactive quassinoids, 13α(21)-epoxyeurycomanone (EP), eurycomanone (EN), 13α,21-dihydroeurycomanone (ED) and eurycomanol (EL) in rat plasma following oral (200 mg/kg) and intravenous administration (10 mg/kg) of a standardized extract Fr 2 of Eurycoma longifolia Jack was developed for pharmacokinetic and bioavailability studies. The extract Fr 2 contained 4.0%, 18.5%, 0.7% and 9.5% of EP, EN, ED and EL, respectively. Following intravenous administration, EP displayed a relatively longer biological half-life (t½ = 0.75 ± 0.25 h) due primarily to its lower elimination rate constant (ke) of 0.84 ± 0.26 h−1) when compared with the t½ of 0.35 ± 0.04 h and ke of 2.14 ± 0.27 h−1, respectively of EN. Following oral administration, EP showed a higher Cmax of 1.61± 0.41 μg/mL over that of EN (Cmax = 0.53 ± 0.10 μg/mL). The absolute bioavailability of EP was 9.5-fold higher than that of EN, not because of chemical degradation since both quassinoids were stable at the simulated gastric pH of 1. Instead, the higher log Kow value of EP (-0.43) contributed to greater membrane permeability over that of EN (log Kow = −1.46) at pH 1. In contrast, EL, being in higher concentration in the extract than EP, was not detected in the plasma after oral administration because of substantial degradation by the gastric juices after 2 h. Similarly, ED, being unstable at the acidic pH and together with its low concentration in Fr 2, was not detectable in the rat plasma. In conclusion, upon oral administration of the bioactive standardized extract Fr 2, EP and EN may be the only quassinoids contributing to the overall antimalarial activity; this is worthy of further investigation.

The Absorption of Glycine and Glycine Oligopeptides by the Rat

1970 ◽  
Vol 39 (6) ◽  
pp. 811-821 ◽  
Author(s):  
T. J. Peters ◽  
M. T. MacMahon
Keyword(s):  
Brush Border ◽  
Portal Blood ◽  
Similar Concentration ◽  
Mesenteric Lymph ◽  
Dual Localization ◽  
Portal Plasma ◽  
High Concentrations ◽  
Arterial Plasma

1. Samples of portal venous and femoral arterial plasma and mesenteric lymph were collected from unanaesthetized rats before and during the intra-duodenal infusion of high concentrations (100 mmol/l) of glycine or glycine oligopeptides (up to and including tetraglycine). 2. There was a marked increase in the concentration of free glycine, and a small amount of diglycine was detected in all the fluids when the peptides were infused but not during the infusion of free glycine. No other glycine oligopeptides were detected. 3. Mesenteric lymph contained a similar concentration of glycine and diglycine to that found in portal blood, suggesting that the mesenteric lymph is a dialysate of portal plasma. 4. The results are interpreted as supporting a dual localization of peptidases within the enterocyte; glycine oligopeptides are hydrolysed to diglycine and free glycine at the brush border and the diglycine is hydrolysed within the cytoplasm.

scholarly journals Metabolic Profile, Bioavailability and Toxicokinetics of Zearalenone-14-Glucoside in Rats after Oral and Intravenous Administration by Liquid Chromatography High-Resolution Mass Spectrometry and Tandem Mass Spectrometry

2019 ◽  
Vol 20 (21) ◽  
pp. 5473 ◽  
Author(s):  
Feifei Sun ◽  
Haiguang Tan ◽  
Yanshen Li ◽  
Marthe De Boevre ◽  
Sarah De Saeger ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Liquid Chromatography ◽  
High Resolution ◽  
Oral Administration ◽  
Intravenous Administration ◽  
Metabolic Profile ◽  
Glucuronic Acid ◽  
High Resolution Mass Spectrometry ◽  
Tandem Mass ◽  
Resolution Mass

Zearalenone-14-glucoside (ZEN-14G), a key modified mycotoxin, has attracted a great deal of attention due to the possible conversion to its free form of zearalenone (ZEN) exerting toxicity. In this study, the toxicokinetics of ZEN-14G were investigated in rats after oral and intravenous administration. The plasma concentrations of ZEN-14G and its major five metabolites were quantified using a validated liquid chromatography tandem mass spectrometry (LC-MS/MS) method. The data were analyzed via non-compartmental analysis using software WinNonlin 6.3. The results indicated that ZEN-14G was rapidly hydrolyzed into ZEN in vivo. In addition, the major parameters of ZEN-14G following intravenous administration were: area under the plasma concentration–time curve (AUC), 1.80 h·ng/mL; the apparent volume of distribution (VZ), 7.25 L/kg; and total body clearance (CL), 5.02 mL/h/kg, respectively. After oral administration, the typical parameters were: AUC, 0.16 h·ng/mL; VZ, 6.24 mL/kg; and CL, 4.50 mL/h/kg, respectively. The absolute oral bioavailability of ZEN-14G in rats was about 9%, since low levels of ZEN-14G were detected in plasma, which might be attributed to its extensive metabolism. Therefore, liquid chromatography high-resolution mass spectrometry (LC-HRMS) was adopted to clarify the metabolic profile of ZEN-14G in rats’ plasma. As a result, eight metabolites were identified in which ZEN-14-glucuronic acid (ZEN-14GlcA) had a large yield from the first time-point and continued accumulating after oral administration, indicating that ZEN-14-glucuronic acid could serve a potential biomarker of ZEN-14G. The obtained outcomes would prompt the accurate safety evaluation of ZEN-14G.

Valganciclovir Is Safe and Effective as Pre-Emptive Treatment for CMV Infection in Allogeneic Hematopoietic Stem Cell Transplantation.

Blood ◽  
2006 ◽  
Vol 108 (11) ◽  
pp. 5300-5300
Author(s):  
Rocco Pastano ◽  
Federica Gigli ◽  
Giovanna Andreola ◽  
Liliana Calabrese ◽  
Fedro Peccatori ◽  
...  
Keyword(s):  
Stem Cell ◽  
Oral Administration ◽  
Intravenous Administration ◽  
Oral Treatment ◽  
Drug Formulation ◽  
Haematopoietic Stem Cell ◽  
Cell Transplant ◽  
Cmv Infection ◽  
Intravenous Ganciclovir ◽  
Hematopoietic Stem

Abstract RATIONALE OF STUDY: Despite significant advances in prevention and therapy, cytomegalovirus (CMV) infection still represents an important cause of morbidity and mortality in patients undergoing allogeneic haematopoietic stem cell transplant (HSCT). The standard pre-emptive treatment is based on intravenous administration of Ganciclovir (GCV). Valganciclovir (VGC), the pro-drug formulation of GCV is characterised by an excellent bio availability, making this drug suitable for oral administration. PATIENTS: Since March 2003 all patients treated with reduced (27 patients) or fully ablative (3 patients) conditioning regimens followed by sibling HSCT, were monitored with bi-weekly CMV/PCR and pp65/assays. Overall 15 episodes of CMV positivity were detected in seven patients. Patients resulted positive (3 cells pp65+ or 1000/100000 PCR +) started oral treatment with VGC 900 mg bid, for the first fourteen days, followed by 900 mg q.d. up to at least seven days after assays normalization. The median duration of therapy was 21 days (range 10–21 days). No significant toxicity was observed. All patients had a normalization of CMV/PCR and pp65/assays within fourteen days, with a response rate (RR) of 100%. In two patients the oral VGC therapy was changed to the intravenous administration of Foscavir, because of concomitant neutropenia and acute GvHD. CONCLUSION: Pre-emptive treatment of CMV infection with VGC is safe, feasible and effective. Furthermore, the oral administration of this drug in an outpatient setting, reduces significantly the costs compared with a therapy that needs hospitalization as intravenous Ganciclovir.

Effect of Barbiturate on Central Pain: Difference Between Intravenous Administration and Oral Administration

1998 ◽  
Vol 14 (1) ◽  
pp. 86-88 ◽  
Author(s):  
Tetsuo Koyama ◽  
Yukio Arakawa ◽  
Masahiko Shibata ◽  
Takashi Mashimo ◽  
Ikuto Yoshiya
Keyword(s):  
Oral Administration ◽  
Intravenous Administration ◽  
Central Pain

scholarly journals Principles and rationale of infusion therapy in tuberculosis

2020 ◽  
pp. 239-240
Author(s):  
T.I. Petrenko
Keyword(s):  
Drug Resistance ◽  
Treatment Group ◽  
Oral Administration ◽  
Intravenous Administration ◽  
Vena Cava ◽  
Medical Community ◽  
Infusion Therapy ◽  
Intravenous Therapy ◽  
Pulmonary Tb ◽  
Number Of Patients

Background. In 2018 7 million new cases of tuberculosis (TB) were registered, which is more than in previous years. Undoubtedly, TB is one of the most important threats to the public health globally. In developing countries, where there are no new TB drugs (TBD) and modern medical services, this threat is even more serious. Intravenous administration is an option to optimize the existing drug regimens, as it is accompanied by increased bioavailability. Objective. To substantiate the rationality of infusion therapy in TB. Materials and methods. Analysis of literature data on this topic; own study involving 106 patients with newly diagnosed infiltrative and disseminated pulmonary TB with bacterial excretion. Results and discussion. The medical community is concerned not only about the increase in the TB incidence, but also about the increase in the number of drug resistance (DR) cases. Improper treatment is one of the causes of DR. In case of oral administration absorption disorders of the drug are possible in people with digestive system diseases, in addition, part of the drug is metabolized by passing through the liver. In contrast, intravenous drugs enter the superior vena cava system, right ventricle, and pulmonary arteries. In a number of patients’ subgroups, it is not possible to achieve a sufficient concentration of drugs in serum when taken orally for various reasons. In particular, these reasons include host organism factors (features of drug metabolism (fast acetylators are more likely to have DR than slow ones), malabsorption, drug clearance, inability of the drug to reach lung tissue) and mycobacteria factors (biofilm formation, drug resistance due to efflux pumps, metabolic status of the bacterium – division phase or sleep phase). These factors are considered to be the consequences of continuous oral administration of TBD. Achieving a high concentration of TBD in the source of infection due to intravenous administration allows to overcome the DR of mycobacteria. In the own study, oral (n=33) and intravenous (n=73) modes of TBD administration were compared. The groups were identical in age, sex, and TB stage. In the intravenous treatment group there was a significantly higher proportion of complete closure of the decay cavities (90.5 % vs. 60.4 % in the oral treatment group; p=0.04), as well as the significantly lower number of toxic reactions (14.3 % vs. 57.9 %; p=0.001) and poor tolerability of treatment (31 % vs. 57.9 %; p=0.04). On the background of intravenous therapy less fluoroquinolone DR was observed. Conclusions. 1. Intravenous therapy in patients with pulmonary TB is more effective than standard in terms of closure of the decay cavities. 2. Intravenous therapy is accompanied by significantly less toxicity and better tolerability. 3. Intravenous TB therapy is less likely to provoke the development of DR.

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