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PubMed1987

Plasma concentrations of 3-keto-desogestrel after oral administration of desogestrel and intravenous administration of 3-keto-desogestrel.

The plasma concentrations of 3-keto-desogestrel have been measured by radioimmunoassay in a crossover study in nine healthy female volunteers given oral desogestrel (150 micrograms) and ethinyloestradiol (30 micrograms) and intravenous (i.v.) 3-keto-desogestrel (150 micrograms) and ethinyloestradiol (30 micrograms). Bioavailability ranged between 40.0 and 113% with a mean value ( +/- SD) of 76.1 +/- 22.5%. Only 3 subjects had a bioavailability of less than 70%. There was no significant difference in the elimination half life of 3-keto-desogestrel which was 12.6 +/- 4.1h following i.v. administration and 11.9 +/- 4.1h after oral administration of desogestrel.

Administration, Oral↗
PubMed1987

[Studies on the metabolic fate of isepamicin sulfate (HAPA-B). IV. Intramuscular, intravenous and drip intravenous administration of HAPA-B in dogs].

The plasma concentration and urinary excretion of isepamicin sulfate (HAPA-B) were studied following intramuscular, intravenous and drip intravenous administrations of 6.25, 25 and 100 mg/kg in dogs. Maximum plasma concentrations (Cmax) of HAPA-B after intramuscular, intravenous and drip intravenous administration depended on dosage levels. Biological half-lives (T1/2) and areas under plasma concentration-time curves (AUC) for the three different routes of administration were similar to each other. The peak plasma concentration of HAPA-B achieved with intramuscular administration was similar to that with a 1-hour drip intravenous administration at a dose level of 6.25 or 25 mg/kg. On the other hand, at a dose level of 100 mg/kg, the Cmax following intramuscular administration was similar to that following 2-hour drip intravenous administration. It was, therefore, presumed that the plasma concentration curves which are similar to that of intramuscular administration can be obtained by regulating the infusion time. The observed Cmax value for drip intravenous administration was a little higher than the theoretical Cmax value for drip intravenous administration calculated from parameters for intramuscular administration. Simulation curves obtained for extended infusion times agreed more closely with observed curves than curves simulated for shorter infusion periods. These investigations showed that plasma concentration curves for any dosage levels can be estimated from parameters calculated from experimental data obtained using intramuscular or drip intravenous administration. HAPA-B was rapidly excreted into the urine after administration through any of these 3 routes and 71 approximately 89% of the dose was excreted into the unrine in 24 hours at all dosage levels. Bioautograms of thin-layer chromatographs of the 0 approximately 6 hours urine after intramuscular administration showed single bands with a similar Rf value to that of the standard HAPA-B. No significant differences in plasma concentration and urinary excretion between HAPA-B and amikacin were observed upon intramuscular or intravenous administration of 25 mg/kg.

Aminoglycosides↗
PubMed1996

Pharmacokinetics of the new thyrotropin releasing hormone analogue montirelin hydrate. 1st communication: plasma concentrations, metabolism and excretion after a single intravenous administration to rats, dogs and monkeys.

The plasma concentrations, metabolism and excretion were studied in rats, dogs and monkeys after a single intravenous administration of 14C-montirelin hydrate (CAS 90243-66-6, 14C-NS-3). 1. The plasma concentration of radioactivity and the area under curve (AUC0-infinity) increased with the dose after intravenous administration of 0.25, 1 and 4 mg/kg to male rats. 2. Until 4 h after intravenous administration of 0.25 mg/kg, the plasma concentration of radioactivity decreased with half-lives of 0.512, 0.771 and 0.786 h in male rats, dogs and monkeys, respectively. The plasma concentration of radioactivity in rats increased 6-10 h after administration, suggesting enterohepatic circulation. 3. The plasma concentration of NS-3 in various animal species decreased biphasically after intravenous administration. The elimination half-lives, t1/2 beta, in rats, dogs and monkeys were 0.324, 0.679 and 0.682 h, respectively, and the steady state volumes of distribution, Vdss, were 0.248, 0.319 and 0.306 l/kg, respectively. 4. The binding of NS-3 to serum protein was less than 3% in rats, dogs, monkeys and humans. 5. Within 48 h after intravenous administration of 1 mg/kg to male rats, the excretion of radioactivity in urine, feces and expired air was 67.3, 15.0 and 14.8% of the dose, respectively (total 97.1%). The biliary excretion of radioactivity was 26.6% within 24 h after dosing. 6. No sex-related difference was found in plasma concentration of radioactivity or the excretion of radioactivity in urine, feces and expired air after intravenous administration of 1 mg/kg to male and female rats. 7. In male dogs, the excretion of radioactivity in urine and feces was 92.3 and 5.6% of the dose, respectively, during 72 h after intravenous administration of 0.25 mg/kg (total 97.9%). 8. In male monkeys, the excretion of radioactivity in urine and feces was 91.7 and 2.9% of the dose, respectively, during 72 h after intravenous administration of 0.25 mg/kg (total 94.6%). 9. The urinary excretion of NS-3 and its main metabolite CNK-6004 (deamidation product) during 24 h after intravenous administration was 31.4 and 25.3% of the dose in male rats, 45.4 and 30.1% in male dogs, and 20.2 and 48.0% in male monkeys, respectively. The biliary excretion of NS-3 and CNK-6004 in male rats was 1.1 and 17.4%, respectively, during 24 h after administration. 10. The radioactivity in the bile collected from donor rats that had received 14C-NS-3 was easily absorbed from the intestinal tract of recipient rats after intraduodenal administration of the donor's bile.

Animals↗
PubMed1991

[Spinal myoclonus secondary to the intravenous administration of iodine contrast media].

We describe a patient with a longstanding paraplegia who developed spinal myoclonus on 3 different occasions spanning one year, once after an enhanced CT scan and twice after excretory urographies, one of which was also followed by a generalized tonic-clonic seizure. To our knowledge only one case of spinal myoclonus secondary to the administration of intravenous contrast material in a patient with a spinal arteriovenous malformation has yet been reported. Taken together, the findings in these cases suggest that spinal myoclonus following intravenous iodine administration is indicative of an underlying spinal cord lesion.

Adult↗
PubMed2001

Fludarabine pharmacokinetics after subcutaneous and intravenous administration in patients with lupus nephritis.

STUDY OBJECTIVE: To compare the pharmacokinetics of subcutaneous and intravenous fludarabine in patients with lupus nephritis. DESIGN: Open-label, randomized, crossover trial conducted with a phase I-II trial. SETTING: Government research hospital. PATIENTS: Five patients with lupus nephritis. INTERVENTION: Fludarabine 30 mg/m2/day was administered either subcutaneously or as a 0.5-hour intravenous infusion for 3 consecutive days. All patients received oral cyclophosphamide 0.5 g/m2 on the first day of each cycle. MEASUREMENTS AND MAIN RESULTS: Plasma samples were collected before and 0.5, 1, 1.5, 2, 4, 8, and 24 hours after the first dose. Urine was collected at 6-hour intervals for 24 hours. Plasma and urine were analyzed for fluoro-arabinofuranosyladenine (F-ara-A), fludarabine's main metabolite, using high-performance liquid chromatography. Compartmental techniques were used to determine the pharmacokinetics of F-ara-A; a linear two-compartment model best described them. Comparison of the pharmacokinetics between subcutaneous and intravenous administration was done by using a Wilcoxon signed rank test. No significant differences were found between subcutaneous and intravenous administration in median (interquartile range) maximum concentrations of 0.51 (0.38-0.56) and 0.75 (0.52-0.91) mg/L, respectively, or in fitted area under the concentration-time curves from 0-24 hours of 4.65 (4.17-4.98) and 4.55 (3.5-4.94) mg x hour/L, respectively. Bioavailability of F-ara-A after subcutaneous dosing was approximately 105% of the bioavailability after intravenous administration. Differences in renal clearance and percentage of dose excreted in urine for subcutaneous and intravenous administration were nonsignificant. No injection site reactions were seen with subcutaneous dosing. CONCLUSION: Subcutaneous and intravenous administration of fludarabine appear to have similar pharmacokinetics in patients with lupus nephritis. Subcutaneous injection may offer a convenient alternative to intravenous administration.

Adult↗
PubMed1986

A study of IgE in immunoglobulin preparations for intravenous administration. I. IgE in intravenous IgG.

We have studied the IgE content of different lots of commercial intravenous IgG preparations used in our day hospital as replacement therapy for patients with agammaglobulinemia. Two enzymatic methods were used: Phadezym and FAST. The average amounts of IgE detected in Endobulin and Sandoglobulin lots were very high with respect to serum values in the general population. In some lots we found low titers of specific IgE (RAST class 1) to house dust mite, rye grass and cow's milk. We also found in most preparations the presence of IgG anti-IgE which are usually present in sera from atopic patients. Despite a low post-infusion increase of serum IgE and the absence of sensitization or adverse reactions observed, a careful selection of donors with normal IgE levels may need to be recommended to manufacturers in the future.

Agammaglobulinemia↗
PubMed1987

[Studies on the metabolic fate of isepamicin sulfate (HAPA-B). III. Intramuscular, intravenous and drip intravenous administration of HAPA-B in rabbits].

Absorption, distribution, metabolism and excretion of isepamicin sulfate (HAPA-B) were studied following intramuscular, intravenous and drip intravenous administration at doses of 6.25, 25 and 100 mg/kg to rabbits. Plasma concentrations of HAPA-B following intramuscular, intravenous and drip intravenous administration depended on dose levels. Biological half-lives (T1/2), body clearance (Clt) and areas under plasma concentration-time curves (AUC) for different routes of administration were similar in all 3 routes. A theoretical curve for drug concentrations vs. time was obtained using pharmacokinetic parameters calculated from drug concentrations in plasma following a 45-minute drip intravenous administration. From the curve, it was estimated that 60 to 90 minutes would be required to achieve a similar maximum drug concentration in plasma by drip intravenous administration to that obtained by intramuscular administration. Thus, drug concentration patterns obtained following intramuscular administration could be duplicated in drip intravenous administration by regulating the length of time for infusion. The concentration of HAPA-B in tissues obtained following a 15-minute drip intravenous administration reached maximum after 15 minutes at a level higher than that achieved by intramuscular administration, but an hour later, concentrations in tissues including the kidney decreased to similar levels obtained following intramuscular administration and patterns of concentration decrease for drip intravenous administration and intramuscular administration were quite similar to each other thereafter. The drug was rapidly excreted into the urine following any of the 3 routes, and urinary recoveries in 24 hours were 75 approximately 92% of dose amounts for all dose levels tested. Bioautograms on thin-layer chromatographs of 0 approximately 6 hours urine samples obtained following an intramuscular administration of the drug showed a single biologically active bands with similar Rf values to HAPA-B itself. No active metabolite of the drug was detected in the urine.

Aminoglycosides↗
PubMed1998

Pharmacokinetics of a chemoprotective agent, 2-(allylthio)pyrazine, after intravenous administration to rabbits.

The pharmacokinetics of 2-(allylthio)pyrazine (2-AP) were evaluated after intravenous administrations of the drug to rabbits. The reason for the multiple peaks in the plasma concentration of 2-AP after intravenous administration of the drug to rabbits were also investigated. After intravenous administration of 2-AP, 10, 20, and 50 mg/kg, to rabbits, the pharmacokinetic parameters of 2-AP, such as the total area under the plasma concentration-time curve from time 0 to 12 h (261, 672, and 1190 micrograms min/ml), the total body clearance (38.3, 42.0, 44.6 ml/min/kg), and the percentages of intravenous dose of 2-AP excreted in 24 h as unchanged drug (0.0306, 0.0252, and 0.0492%), were independent of the dose ranges studied. Since the amount of 2-AP excreted in 12-h bile as unchanged drug after intravenous administration of 2-AP, 20 mg/kg, was only 0.0241 +/- 0.00156%, and some of 2-AP excreted in gastrointestinal tract as unchanged drug was reabsorbed, the reason for the appearance of multiple peaks after intravenous administration of 2-AP could be at least partly due to gastrointestinal excretion of the drug.

Animals↗
PubMed1986

Effect of use-criteria for intravenous administration sets.

Numbers of intravenous administration sets used were studied in a 480-bed hospital before and after criteria for selecting sets were implemented. Criteria for use of eight common administration sets were developed by a committee of nurses and pharmacists. Hospital drug-use review was used as a pattern. Baseline data were collected for seven-day periods on each of five patient-care units; twice daily, one pharmacist recorded the numbers of sets used and determined their compliance with the criteria, which had been established but not disseminated to nurses or implemented. After nurses were instructed on use of the criteria, data were collected for a second seven-day period on each unit. Use of each set type as a percentage of all sets and compliant use of each type as a percentage of all compliant use were calculated. Annual hospitalwide cost savings were predicted from the observed changes in use and the hospital's costs in the six-month period before the study. Significant changes occurred in overall use and in use of individual set types. For each set type, use compliant with the criteria increased. Notable changes included decreased use of volumetric chambers (burettes) and increased relative use of Y maxidrip and Y minidrip sets. Annual savings of more than +20,000 were predicted. Criteria for selection of i.v. administration sets had an effect on set use at this hospital.

Anti-Bacterial Agents↗
PubMed1988

Experimental chloramphenicol intoxication in neonatal calves: intravenous administration.

Chloramphenicol was administered intravenously for eight to 17 days to five newborn calves at a daily dosage of 100 mg kg-1. Haemodynamic, haematological, blood chemistry, serum enzyme, urinalysis and clinical responses were evaluated. High levels of serum chloramphenicol were observed throughout the study although a marked increase in elimination rate was seen with increasing age. The most severe adverse effects were severe hypotension following rapid intravenous administration and severe gastrointestinal dysfunction with diarrhoea accompanying prolonged high dosage. There appeared to have been a haematological effect in one calf, but it was of minor significance compared with the other effects.

Animals↗
PubMed2005

Continuous versus intermittent intravenous administration of antibiotics: a meta-analysis of randomised controlled trials.

Intermittent intravenous administration of antibiotics is the first-line approach in the management of severe infections worldwide. However, the potential benefits of alternate modes of administration of antibiotics, including continuous intravenous infusion, deserve further evaluation. We did a meta-analysis of randomised controlled trials comparing continuous intravenous infusion with intermittent intravenous administration of the same antibiotic regimen. Nine randomised controlled trials studying beta-lactams, aminoglycosides, and vancomycin were included. Clinical failure was lower, although without statistical significance, in patients receiving continuous infusion of antibiotics (pooled OR 0.73, 95% CI 0.53-1.01); the difference was statistically significant in a subset of randomised controlled trials that used the same total daily antibiotic dose for both intervention arms (0.70, 0.50-0.98, fixed and random effects models). Regarding mortality and nephrotoxicity, no differences were found (mortality 0.89, 0.48-1.64; nephrotoxicity 0.91, 0.56-1.47). In conclusion, the data suggest that the administration of the same total antibiotic dose by continuous intravenous infusion may be more efficient, with regard to clinical effectiveness, compared with the intermittent mode. In an era of gradually increasing resistance among most pathogens, the potential advantages of continuous intravenous administration of antibiotics on several clinical outcomes should be further investigated.

Aminoglycosides↗
PubMed1981

Intravenous administration sets--an overview.

Intravenous administration sets continue to become more sophisticated in response to advances in medical therapy. A number of design options are available to meet specialized needs. It behooves the pharmacist to become familiar with them in order to insure that sets compatible with and optimal for their intended application are selected in his or her institution. Doing so will fully execute his or her increasing responsibilities in I.V. therapy.

Infusions, Parenteral↗
PubMed1983

Continuous intravenous administration of drugs.

Continuous intravenous administration of drugs may be a problem in clinical practice; for several reasons patients do not always receive the dose of drug intended for them. Problems of parenteral fluid composition are related to the solvent, dilution and drug interactions. Physical factors influencing drug stability are light and adsorption onto perfusion sets. Examples are reported for each problem. A practical solution, based on personal experimentation, is proposed for diazepam and nitroglycerin administration.

Adsorption↗
PubMed1983

[Pharmacokinetic studies on micronomicin in rats. Comparison of intramuscular and drip intravenous administration models].

Absorption, tissue distribution and excretion of micronomicin (MCR) were studied in rats after intramuscular or 30 minutes drip intravenous administration (10 mg/kg). Serum levels of MCR were measured by bioassay, enzyme immunoassay and high pressure liquid chromatography. The pharmacokinetic studies of MCR after intramuscular or drip intravenous administration were carried out using one-compartment open model or two-compartment open model, respectively. Among 3 assay methods, similar pharmacokinetic parameters of MCR were obtained. In the simulation of serum levels of MCR, the differences between the measured and calculated serum levels after intramuscular or drip intravenous administration were less than 19% of the former levels. After intramuscular or drip intravenous administration of MCR, similar changes of the organ (kidneys, lungs, spleen and liver) levels were observed. Urinary recovery rates of MCR amounted to 82.3% or 91.6% by 24 hours after intramuscular or drip intravenous administration, respectively. After intramuscular or drip intravenous administration of MCR, no metabolites were found in urine of rats.

Aminoglycosides↗
PubMed2004

Timing of intravenous administration set changes: a systematic review.

OBJECTIVE: To determine the optimal time interval for the routine replacement of intravenous administration sets when crystalloids or parenteral nutrition are administered via a central or peripheral catheter in an acute care setting. DESIGN: Systematic review of all randomized or systematically allocated controlled trials addressing the frequency of replacing intravenous administration sets. METHODS: The Cochrane Controlled Trials Register (June 2001) and the Ovid databases (Medline, CINAHL, and CancerLit-July 2001) were searched. Bibliographies, relevant conference proceedings, and any product information were also checked for references. RESULTS: Eighteen studies were selected for review. The 12 included studies were separated into 3 intravenous administration set change comparisons: 24 hours versus 48 hours or more; 48 hours versus 72 hours or more; and 72 hours versus 96 hours or more. There was good evidence that changing intravenous administration sets every 72 hours or more does not increase the risk of infusate-related bloodstream infection (BSI) in patients with central or peripheral catheters and a fair level of evidence that it does not increase the risk of catheter-related BSI. There were insufficient data regarding the incidence of BSI among patients receiving parenteral nutrition, particularly lipid-containing parenteral nutrition. CONCLUSIONS: It appears that intravenous administration sets containing crystalloids can be changed in patients with central or peripheral catheters every 72 hours or more without increasing the risk of BSI. However, it is not possible to conclude that intravenous administration sets containing parenteral nutrition, particularly lipid-containing parenteral nutrition, can be changed at this interval.

Bacteremia↗