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At least 811 records · Page 45Linked to original sources
PubMed1977

Metabolic effects of salbutamol: comparison of aerosol and intravenous administration.

The effects of intravenous salbutamol (4 mug/kg) were compared with those of aerosol salbutamol (200 mug) in 10 asthmatic patients in a double-blind placebo-controlled study. Both methods of administration produced equal bronchodilatation. Intravenous salbutamol caused significant increases in plasma insulin and glucose levels and a fall in serum potassium concentration in addition to tachycardia and tremor, whereas aerosol salbutamol produced only a small transient increase in the plasma glucose level. The initially raised non-esterified fatty acid levels decreased significantly after aerosol and placebo but not after intravenous salbutamol.

Adult↗
PubMed2004

Tissue and intrahepatic distribution and subcellular localization of a mannosylated lipoplex after intravenous administration in mice.

We have previously reported that, unlike a lipoplex and mannosylated (Man) lipoplex underwent gene transfer to liver nonparenchymal cells (NPC) that possess mannose receptors after intravenous administration in mice. In this study, the tissue, intrahepatic distribution, and subcellular localization of the lipoplex after intravenous administration were investigated. DC-Chol liposome was selected as a cationic liposomes. After administration of lipoplex and Man lipoplex, the high gene expression was observed in the lung and liver, respectively. After administration of [32P]Man lipoplex, about 80% of [32P]plasmid DNA (pDNA) was accumulated in the liver. As for the intrahepatic distribution, the NPC/parenchymal cells (PC) ratio of [32P]Man lipoplex was 9.64, whereas the NPC/PC ratio of [32P]lipoplex was 1.93. The radioactivity in the cytosolic fraction of liver homogenate of [111In]Man lipoplex was two-fold higher than that of [111In]lipoplex, indicating that Man liposomes facilitate the release of pDNA into the cytosolic space. However, a rapid sorting of the radioactivity from endosomes to lysosomes was observed with the [111In]Man lipoplex. Also, amplification of pDNA by PCR suggested that the Man lipoplex is more rapidly degraded within the intracellular vesicles than the lipoplex. These results suggested that modulation of its intracellular sorting could improve the transfection efficiency of Man lipoplex.

Animals↗
PubMed1995

Vancomycin levels in the vitreous cavity after intravenous administration.

PURPOSE: We studied the effects of inflammation, repeated antibiotic doses, and the surgical status of the eye on penetration of vancomycin hydrochloride into the rabbit vitreous cavity after intravenous administration. METHODS: We studied three anatomic states (phakic, aphakic, and aphakic, vitrectomy-treated eyes) subdividing each into inflamed and noninflamed groups. Intravenous vancomycin hydrochloride (15 mg/kg of body weight) was administered every 12 hours for 48 hours. Eyes were harvested for the assay of vitreous cavity antibiotic levels at various intervals from one to 49 hours. We determined concentrations and calculated mean values and S.E.M. RESULTS: Therapeutic levels were not established in the vitreous cavity at any time period in the two phakic groups. At 25 hours, the inflamed aphakic eyes had concentrations of 5.05 +/- 1.9 micrograms/ml and the control noninflamed aphakic eyes 4.5 +/- 1.23 micrograms/ml; slight increases were found by 49 hours. Concentrations tested in the aphakic, vitrectomy-treated eyes at two, 13, 25, and 49 hours demonstrated progressive increases both in the inflamed eyes (5.4 +/- 2.4 micrograms/ml, 9.64 +/- 4.25 micrograms/ml, 9.2 +/- 3.96 micrograms/ml, 10.34 +/- 4.49 micrograms/ml) and noninflamed eyes (3.52 +/- 2.1 micrograms/ml, 5.4 +/- 1.96 micrograms/ml, 6.8 +/- 2.53 micrograms/ml, 8.7 +/- 5.44 micrograms/ml). CONCLUSIONS: Vitreous vancomycin concentrations in aphakic and aphakic, vitrectomy-treated eyes after intravenous administration exceed the minimal inhibitory concentrations for the usual gram-positive pathogens that create endophthalmitis, suggesting a role for intravenous vancomycin in the treatment of bacterial endophthalmitis.

Animals↗
PubMed1992

Pharmacokinetics of teicoplanin upon multiple-dose intravenous administration of 3, 12, and 30 milligrams per kilogram of body weight to healthy male volunteers.

Teicoplanin pharmacokinetics were evaluated after multiple-dose intravenous administration to healthy male volunteers by using a randomized, double-blind, parallel design. Doses of 3, 12, or 30 mg of teicoplanin per kg of body weight were administered every 24 h for 14 days as 60-min constant-rate intravenous infusions. Blood and urine samples were collected over 21 days and analyzed by a microbiological assay. Twenty-three subjects were included in the pharmacokinetic analysis. The median pharmacokinetic parameters upon multiple-dose intravenous administration of 3, 12, and 30 mg/kg included steady-state volumes of distribution of 0.94, 0.77, and 0.68 liter/kg; total clearances of 11.9, 12.0, and 13.2 ml/h/kg; and terminal disposition half-lives of 143, 166, and 96 h, respectively. Renal clearance accounted for approximately 95% of total clearance. No dose-related differences existed for teicoplanin total or renal clearance. The steady-state volume of distribution decreased significantly with increasing doses. As a result of the decrease in the volume of distribution, the terminal disposition half-life at 30 mg/kg was significantly decreased. However, the decreases in the volume of distribution and terminal disposition half-life are of limited clinical importance, since steady-state trough concentrations in serum increase in proportion to dose. Combined results of all multiple-dose studies with similar durations of sample collection indicate no dose-related differences for any pharmacokinetic parameters from 3 to 12 mg/kg. As observed in the present study, no dose-related differences exist for teicoplanin total and renal clearances from 3 to 30 mg/kg. However, at 30 mg/kg, a significant decrease in the steady-state volume of distribution is observed. As a consequence of the reduction in the volume of distribution at 30 mg/kg with no change in clearance, the terminal disposition half-life is decreased.

Adult↗
PubMed1978

Plasma timolol levels after oral and intravenous administration.

The plasma kinetics of timolol administered orally and intravenously to 5 male subjects were examined. Bioavailability was reduced by 25% when the drug was taken orally. Mean plasma half-life after oral dosing was 4.86 h, and after intravenous administration it was 4.56 h; the difference was not significant. The volume of distribution was 3.5 1/k. It is suggested that timolol is little affected by the 'first pass effect', even though there is marked interindividual variation in availability and peak plasma level.

Administration, Oral↗
PubMed1983

Distribution of gold in rat blood after intravenous administration of auranofin, gold sodium thiomalate and aurothioglucose to rats.

Serum, blood and cell-associated gold were determined at various time periods after intravenous administration of 1 mg Au/kg of auranofin (AF), gold sodium thiomalate (GSTM) and aurothioglucose (GTG). AF gold exhibited an early phase of decay with high levels of cell-association; whereas, after 72 h cell-associated gold was not detectable. In contrast, GSTM and GTG serum gold values were generally higher than blood values since cell-associated gold rarely occurred. These observations suggest that, in contrast to GSTM and GTG, intravenous administration of AF results in a dynamic equilibrium of gold between the cellular and serum compartments of blood.

Animals↗
PubMed1992

Pharmacokinetics of glycyrrhizin after intravenous administration to rats.

A simple high-performance liquid chromatographic method was developed to study the pharmacokinetics of glycyrrhizin in the rat after bolus intravenous administration at a dose of 20, 50, or 100 mg/kg. The decline in the concentration of glycyrrhizin in plasma was generally biexponential at each dose, but the terminal disposition became much slower as the dose was increased. A greater-than-proportional increase in the glycyrrhizin concentration in plasma was observed with an increase in the dose, a result suggesting a dose-dependent glycyrrhizin disposition. The disposition of drug in plasma at each dose fitted well to a two-compartment pharmacokinetic model. The apparent total body clearance decreased significantly with increases in the dose. On the other hand, the apparent distribution volume after intravenous administration was unaffected by the dose. The results indicate that the pharmacokinetics of glycyrrhizin is nonlinear.

Animals↗
PubMed1997

The role of intravenous administration of dextran 70 in enteric bacterial translocation after partial hepatectomy in rats.

The aim of this study was to assess the effect of intravenous dextran on bacterial translocation and intestinal vascular endothelial and epithelial barrier function after experimental partial hepatectomy. We determined systemic arterial pressure, enteric bacterial growth (proximal and distal small intestine and colon) and bacterial translocation (BT) to mesenteric lymph nodes (MLN), liver, lungs, spleen, kidneys and blood, as well as intestinal vascular endothelial and epithelial barrier permeability, after sham operation or partial hepatectomy (50% and 90%) with preoperative intravenous administration of saline, albumin or dextran 70. Subtotal hepatectomy induced a significant decrease in arterial pressure and an increase in the number of Escherichia coli in the distal small intestine. BT was not observed in sham-operated animals or in rats with 50% hepatectomy administered dextran. The number of positive cultures of enteric bacteria was significantly increased after hepatectomy, whereas dextran treatment decreased the number of animals with BT. Increased permeability of the intestinal vascular endothelial and epithelial barriers was noted in hepatectomized animals, while dextran prevented hepatectomy-induced vascular endothelial barrier injury. Enteric bacterial translocation occurred following partial hepatectomy in the rat, associated with bacterial overgrowth in the distal small intestine. Intravenous administration of dextran 70 prevented bacterial overgrowth and translocation, at least in part, by maintaining gut vascular endothelial barrier integrity

Animals↗
PubMed1994

Pharmacokinetics of a novel retinoid AGN 190168 and its metabolite AGN 190299 after intravenous administration of AGN 190168 to rats.

The pharmacokinetics of AGN 190168, a novel synthetic retinoid, and its major metabolite, AGN 190299, in rat blood after intravenous administration was investigated. Approximately 4.4 mg kg-1 (high dose) or 0.49 mg kg-1 (low dose) of AGN 190168 was administered to rats via the femoral vein. Blood was collected from the femoral artery at various time points during an 8 h period. Blood concentrations of AGN 190168 and AGN 190299 were determined by a specific and sensitive high-pressure liquid chromatographic (HPLC) method. AGN 190168 was rapidly metabolized in rats. The only detectable drug-related species in the blood was AGN 190299. Therefore, only pharmacokinetics of AGN 190299 were calculated. Elimination of AGN 190299 appeared to be non-linear after administration of the high dose, and linear after administration of the low dose. The maximum elimination rate (Vmax) and the concentration at half of the Vmax (km), as estimated by a Michaelis-Menten one-compartment model, were 7.58 +/- 2.42 micrograms min-1 (mean +/- SD) and 6.10 +/- 1.58 micrograms mL-1, respectively. The value of the area under the blood concentration time curve (AUC) was 9.54 +/- 1.68 micrograms h mL-1 after administration of the high dose and 0.594 +/- 0.095 micrograms h mL-1 after administration of the low dose. The clearance value was 7.79 +/- 1.20 mL min-1 kg-1 after the high dose, statistically significantly different from that after the low dose (p < 0.05), 14.0 +/- 2.2 mL min-1 kg-1. The terminal half-life (t1/2) was 1.25 +/- 0.74 h for the high-dose group and 0.95 +/- 0.16 h for the low-dose group. Study results demonstrate rapid systemic metabolism of AGN 190168 to AGN 190299, non-linear pharmacokinetics of AGN 190299 after the 4.4 mg kg-1 dose, and the lack of difference in disposition profiles between sexes after intravenous administration of AGN 190168 to rats.

Animals↗
PubMed1988

Inhibitors of sterol synthesis. Metabolism of 5 alpha-cholest-8(14)-en-3 beta-ol-15-one after intravenous administration to bile duct-cannulated rats.

The metabolism of 5 alpha-cholest-8(14)-en-3 beta-ol-15-one has been studied after intravenous administration to bile duct-cannulated rats. Very rapid and substantial conversion of the 15-ketosterol to polar biliary metabolites was observed in both male and female rats. For example, upon intravenous injection of [4-14C]5 alpha-cholest-8(14)-en-3 beta-ol-15-one to male bile duct-cannulated rats, approximately 86% of the administered 14C was recovered in bile in the first 38 h. Of the total amount of 14C recovered in bile in 38 h, approximately 50% was excreted in bile in the first 70 min and approximately 90% was excreted within 8 h after the injection of the 15-ketosterol. A substantial fraction of the polar biliary metabolites was shown to undergo enterohepatic circulation. Of the radioactivity derived from the labeled 15-ketosterol which was not recovered in bile or other excreta at 48 h after the intravenous administration of the 15-ketosterol, most (approximately 79%) was recovered in the form of cholesterol and cholesteryl esters of blood and the various tissues. The very substantial and rapid biliary excretion of polar metabolites of the 15-ketosterol (or of cholesterol derived from the 15-ketosterol), coupled with inhibition of the intestinal absorption of cholesterol by the 15-ketosterol, may contribute to the overall hypocholesterolemic action of the 15-ketosterol which has been observed in rodents and in nonhuman primates by providing a metabolic pathway(s) wherein a substantial fraction of the absorbed 15-ketosterol is rapidly removed from the body by biliary excretion in the form of polar metabolites.

Animals↗
PubMed1982

Pharmacokinetic study of PAF-acether. Preliminary results after the intravenous administration of a 3H-labelled product to the rabbit.

3H-PAF-acether was rapidly distributed and deacetylated to 3H-lyso-PAF-acether after its intravenous administration to the rabbit. Within 30 min, an equilibrium was established between PAF-acether (10%) and lyso-PAF-acether (90%). A pharmacokinetic study and a preliminary metabolic evaluation were carried out in three rabbits, after the intravenous administration of 3H-labelled PAF-acether (40 Ci/mM, CEA, Saclay, France). This work required the development of a method for the separation of the unchanged product from its potential plasma metabolites, particularly from lysoPAF which appears to be the only early degradation product.

Animals↗
PubMed2005

Biodistribution characteristics of all-trans retinoic acid incorporated in liposomes and polymeric micelles following intravenous administration.

The aim of this study was to investigate the biodistribution characteristics of all-trans retinoic acid (ATRA) incorporated in liposomes and polymeric micelles following intravenous administration. [3H] ATRA were incorporated in distearoylphosphatidylcholine (DSPC)/cholesterol (6:4) liposomes. Two types of block copolymers, poly (ethylene glycol)-b-poly-(aspartic acid) derivatives with benzyl (Bz-75) groups, were synthesized to prepare the polymeric micelles for [(3)H]ATRA incorporation. ATRA were dissolved in mouse serum to analyze their inherent distribution. After intravenous administration, the blood concentration of [3H] ATRA in liposomes and polymeric micelles (Bz-75) was higher than that of inherent [3H]ATRA, suggesting that liposomes and polymeric micelles (Bz-75) control the distribution of ATRA. Pharmacokinetic analysis demonstrated that [3H]ATRA incorporated in polymeric micelles (Bz-75) exhibit the largest AUC(blood) and lowest hepatic clearance of ATRA, suggesting that polymeric micelles (Bz-75) are an effective ATRA carrier system for acute promyelocytic leukemia (APL) therapy. These results have potential implications for the design of ATRA carriers for APL patients.

Animals↗
PubMed2002

Phenytoin toxicity with mandibular tremor secondary to intravenous administration.

The parenteral form of phenytoin is the most commonly used antiepileptic agent during the perioperative period in neurosurgery clinics. We report observations in a 52-year-old male patient with hypoalbuminemia and phenytoin intoxicity following 1 day preoperative administration and a 7-day postoperative intravenous administration of the drug with no modification of the oral dose. This report emphasizes the need for careful surveillance of phenytoin-induced toxicity during parenteral therapy, especially in debilitated patients.

Anticonvulsants↗
PubMed1977

Measurement of cerebral blood flow following intravenous administration of pentoxifyline ('Trentral').

Using 99mTc cerebral scintigraphy and a gamma camera/computer system, the pattern of cerebral blood flow in 5 brain areas was monitored in 30 geriatric patients with cerebrovascular insufficiency. Readings were compared on a within-patient basis for the following treatments: initial control (I), intravenous administration of 10 ml physiological saline solution (II), and intravenous administration of 10 ml (200 mg) pentoxifylline (III). By comparsion with treatment I and II, pentoxifylline produced significant increases in cerebral blood flow. It is suggested that this increase in perfusion is possibly due to an improvement in the flow properties of blood.

Aged↗
PubMed1993

[Effects of intravenous administration of nasaruplase, a plasminogen pro-activator, on left ventricular function and systemic hemodynamics in a canine model of acute myocardial infarction].

The thrombolytic effects and changes in left ventricular function after intravenous administration of nasaruplase were examined in a canine thrombus model of acute myocardial infarction. When 8 U/kg/min of nasaruplase was intravenously administered after 30 min of coronary arterial occlusion, coronary recanalization was achieved in 78.6% (11/14) of the animals with little change in plasma fibrinogen concentration. There was no further decrease in cardiac output, left ventricular ejection fraction or regional wall motion immediately after reperfusion, compared with 30 min after coronary arterial occlusion. However, all these parameters returned to pre-occlusion levels one week after reperfusion. Nasaruplase markedly reduced infarct size as well as cardiac hypertrophy following coronary arterial occlusion, demonstrating suppression of the development of ischemic myocardial damage. These results indicate that coronary thrombolytic therapy with intravenous administration of nasaruplase is useful for the treatment of acute myocardial infarction.

Animals↗
PubMedDate not supplied

Cardiorespiratory inhibitory reflex induced by intravenous administration of acetaldehyde in rats.

In urethane anesthetized rats, intravenous administration of a bolus of acetaldehyde (diluted 50 times its volume in Ringer Locke solution) induced after a latency of about 1 second, a triple reflex response characterized by transient bradycardia, hypotension and apnea. Intensity of both bradycardia (r = -0.78) and hypotension (r = -0.74) were dose dependent (p less than 0.001). The triple response was blocked by vagotomy. Atropine and hexamethonium blocked bradycardia and hypotension and pretreatment of rats with reserpine (0.5 mg/100 g b.wt., IP) did not change the magnitude of the reflex response. The bolus effect was discarded by injecting the same volume of Ringer Locke solution in control test experiments. Administration of acetaldehyde directly into the left ventricle induced neither bradycardia nor hypotension, thus discarding a Bezold-Jarish reflex response. Administration of acetaldehyde directly into the right ventricle induced an increase in reflex bradycardia, hypotension and apnea with a shorter latency as compared to the intravenous route. The results suggest that the response induced by acetaldehyde is mediated by a reflex increase in vagal tone and probably is initiated in pulmonary vagal afferent fibers associated with the pulmonary J receptors.

Acetaldehyde↗
PubMed2001

Pharmacokinetic properties of a novel tissue-type plasminogen activator pamiteplase after single intravenous administration to rats, dogs, and monkeys.

The pharmacokinetics of pamiteplase and recombinant tissue-type plasminogen activator (rt-PA) in rats, dogs, and monkeys were examined using a newly developed enzyme-linked immunosorbent assay (ELISA). Plasma concentrations after intravenous administration of pamiteplase to rats declined in a triphasic manner. Plasma concentrations after intravenous administration of pamiteplase to dogs or monkeys declined in a biphasic manner. The area under the plasma concentration-time curve from zero to infinity (AUC(0-->infinity)) in rats and dogs increased with increasing dose. The half-life and mean residence time of pamiteplase in rats, dogs, and monkeys were shown to be longer than those of rt-PA. Total clearance (CL(total)) of pamiteplase was only 7-16% that of rt-PAs, suggesting that concentrations of pamiteplase in plasma were higher and more continuous than those of rt-PA in these experimental animals. The data suggest that a bolus administration of pamiteplase shows the same thrombolytic activity as continuous infusion of rt-PA in experimentally induced thrombosis in rats and dogs. The pharmacokinetic parameters distribution volume at the steady state and CL(total) calculated by immunoreactive concentration after administration of pamiteplase to rats, dogs, and monkeys show high correlation with body weights (r(2)=.7728 and .9039).

Animals↗