Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “INDOMETHACIN”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 55 records · Page 3Linked to original sources
PubMed1990

Topical indomethacin in overuse injuries in athletes. A randomized double-blind study comparing Elmetacin with oral indomethacin and placebo.

In this double-blind trial in 70 athletes with superficial overuse injuries, the effect of topically and systemically administered indomethacin was compared with a placebo control. The treatment period was 2 weeks and blindness was secured by the double-dummy technique. The basic data of the patients showed no significant differences on entry to the study. The majority of cases were acute or subacute, the mean duration of symptoms being 7.4 weeks. The results showed a marked therapeutic effect after 3-7 days of treatment and statistically significant differences between the topical formulation and the placebo were reached in the parameters patients assessment of improvement and pain in connection with daily activity within the first week of treatment. However, during the second week the statistical significances were lost. Only in the topically treated patients local adverse reactions were observed. In the oral indomethacin group all reactions were systemic, GI- and CNS-complaints being predominant. The results on efficacy as well as adverse reactions favour the use of topical indomethacin in superficial overuse injuries in athletes.

Administration, Oral↗
PubMed1993

Preoperative indomethacin for pain relief after thoracotomy: comparison with postoperative indomethacin.

Indomethacin commenced before operation was compared with postoperative indomethacin administration for pain relief in patients after elective thoracic surgery. In addition to indomethacin, all patients received i.v. opioids titrated to their individual requirements. There was no significant difference between the two groups in quality of pain relief, in cumulative opioid requirement or in the incidence of adverse effects. The quality of pain relief compared well with previous similar studies using this technique.

Adult↗
PubMed1980

Indomethacin treatment in patent ductus arteriosus. A double-blind study utilizing indomethacin plasma levels.

23 premature infants were placed on a randomized double-blind study to evaluate the effectiveness of indomethacin in closing a patent ductus arteriosus. Infants received 0.2 mg/kg indomethacin or placebo by gavage. In the treatment group, 7 patients responded out of a total of 12, while in the placebo group, 2 responded out of a total of 11. Indomethacin plasma levels were obtained in 6 patients in the treatment group. Plasma levels showed marked variability in peak level (60-3,100 ng/ml), time to peak level (0.5-6 h) and t1/2 (1 to greater than 24 h).

Clinical Trials as Topic↗
PubMedDate not supplied

[Indomethacin kinetics in synovia and plasma following administration of indomethacin Gits 7/85 in patients with chronic polyarthritis].

Patients suffering from rheumatoid arthritis received a single dose of the new therapeutic system of indomethacin (Gits 7/85). Samples of plasma and synovial fluid were taken after 1, 2, 4, 6, 8, 10, 12, and 24 h. Concentration peaks could not be observed. After 2-3 h plasma levels were achieved which remained constant over the investigational period. Indomethacin concentrations in synovial fluid were seen with some delay. All synovial fluid levels after single application were lower than the plasma concentrations. The kinetics of elimination showed no difference between the two compartments. The above findings confirm the expectations regarding the new therapeutic system of indomethacin (Gits 7/85), i.e., the maintenance of a nearly constant plasma and synovia level for at least 10 h. The avoidance of peaks is seen as an additional advantage.

Arthritis, Rheumatoid↗
PubMedDate not supplied

Augmentation of luteinizing hormone action by prostaglandin E2 in the prevention of antispermatogenic effect of indomethacin. Indomethacin & spermatogenesis.

Administration of indomethacin exhibited antigonadal action by inhibiting the Leydig cells, sex-accessories and spermatocyte-spermatid conversion process. Administration of PGE2 or PGF2 alpha had no effect on Leydig cell nuclear volume or accessory organ weights, but PGE2 had a restorative effect on the efficiency of meiosis, although at a statistical non-significant level. Administration of LH to indomethacin treated rats restored the accessories fully with a non-significant effect on the yield of step-7 spermatids from meiosis. Simultaneous administration of indomethacin, LH and PGE2 (but not PGF2 alpha) restored both sex-accessories and spermatid number to the level of vehicle injected controls.

Animals↗
PubMed1995

Ulcerogenicity and effect on inhibition of prostaglandin generation of indometacin farnesil, a prodrug of indomethacin, in rat gastric mucosa: comparison with indomethacin or loxoprofen.

Indometacin farnesil was compared with indomethacin and loxoprofen in rats to ascertain whether it caused less gastric mucosal damage than the two older drugs. Damage was evaluated in terms of the size of ulcers that formed after oral administration and the changes in concentrations of prostaglandins E2 and I2 in the mucosa. Indometacin farnesil caused less damage than indomethacin and tended to cause less damage than loxoprofen. Indometacin farnesil was less potent than indomethacin in inhibiting prostaglandin generation by gastric mucosa. This property of indometacin farnesil may contribute to the low ulcerogenicity of this compound.

Animals↗
PubMed1981

Sustained release indomethacin: a double blind comparison with indomethacin suppositories.

A double-blind crossover comparison of sustained release indomethacin capsules and indomethacin suppositories showed no efficacy advantage to either preparation. In other respects the two preparations were found to be comparable. More patients preferred the convenience of the oral route of medication when given the choice after the study was concluded.

Administration, Oral↗
PubMedDate not supplied

Polymorphism of indomethacin. Part II. Identification and rapid determination of polymorphic forms of indomethacin by IR spectrometry.

A procedure is described, which make it possible to determine the content of individual polymorphic forms of indomethacin in their mixture by IR spectrometry. IR spectra recorded in the range of 1600--1800 cm-1 have been used in the determinations. The method is especially useful for analytical control of the technological process of preparing the most pharmacologically active-gemma-form of indomethacin.

Indomethacin↗
PubMed1985

Unsaturated 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholines (unsaturated platelet-activating factor): aggregation of human platelets after incubation with indomethacin, creatinephosphate/creatinephosphokinase, xylocain and hirudine, and serotonin release after incubation with indomethacin.

Unsaturated platelet-activating factor (PAF) aggregates thrombocytes of healthy female volunteers and releases within 1 min up to 30.95% of the platelet serotonin. Indomethacin does not inhibit the aggregation but reduces the release of serotonin induced by unsaturated PAF in citrated platelet-rich plasma (PRP). Creatinephosphate combined with creatinephosphokinase (CP/CPK) inhibits the second phase, whereas xylocain inhibits the first and second phase of aggregation induced by unsaturated PAF. Hirudine shows no influence on the aggregation induced by unsaturated PAF.

Blood Platelets↗
PubMed1980

The degenerative effect on rabbit implantation sites by indomethacin. I. Timing of indomethacin action, possible effect on uterine proteins and the effect of replacement doses of PGF2 alpha.

To determine the effective time of indomethacin (Id) action in disrupting early pregnancy, groups of rabbits were treated at various stages after mating with Id and/or replacement doses of PGF2 alpha. Effect of Id on the secretion of uterine proteins was also investigated. The highest rate of embryonic death occurred when Id was injected twice daily during days 5-7 of pregnancy, and days 5-6 appear to be the most critical. Persisting levels of Id during this critical stage is required to induce the antifertility effect. The results also indicate that the adverse effect of Id is not mediated through an effect on uterine proteins, and is mainly due to the inhibition of PG's synthesis. PG's are apparently required for normal implantation and early development.

Animals↗
PubMed2002

Lipid peroxidation induced by indomethacin with horseradish peroxidase and hydrogen peroxide: involvement of indomethacin radicals.

Some of the side-effects of using indomethacin (IM) involve damage to the gastric mucosa and liver mitochondria. On the other hand, neutrophils infiltrate inflammatory sites to damage the tissues through the generation of reactive oxygen species by myeloperoxidase. The stomach and intestine have large amounts of peroxidase. These findings suggest that peroxidases are involved in tissue damage induced by IM. To clarify the basis for the tissue damage induced by IM in the presence of horseradish peroxidase (HRP) and H2O2 (HRP-H2O2), lipid peroxidation was investigated. When IM was incubated with liver microsomes in the presence of HRP-H2O2 and ADP-Fe3+, lipid peroxidation was time-dependent. Catalase and desferrioxamine almost completely inhibited lipid peroxidation, indicating that H2O2 and iron are necessary for lipid peroxidation. Of interest, superoxide dismutase strongly inhibited lipid peroxidation, and it also inhibited the formation of bathophenanthroline-Fe2+, indicating that reduction of the ferric ion was due to superoxide (O2-). ESR signals of IM radicals were detected during the interaction of IM with HRP-H2O2. However, the IM radical by itself did not reduce the ferric ion. These results suggest that O2- may be generated during the interaction of IM radicals with H2O2. Ferryl species, which are formed during the reduction of iron by O2-, probably are involved in lipid peroxidation.

Animals↗
PubMed2001

Inactivation of creatine kinase during the interaction of indomethacin with horseradish peroxidase and hydrogen peroxide: involvement of indomethacin radicals.

Creatine kinase (CK) was used as a marker molecule to examine the side effect of damage to tissues by indomethacin (IM), an effective drug to treat rheumatoid arthritis and gout, with horseradish peroxidase and hydrogen peroxide (HRP-H2O2). IM inactivated CK during its interaction with HRP-H2O2. Under aerobic conditions, inactivation of CK significantly decreased. CK in rat heart homogenate was also inactivated by IM with HRP-H2O2. When IM was incubated with HRP-H2O2, the maximum absorption of IM at 280 nm rapidly decreased and a new peak at 410 nm occurred with isosbestic points at 260 and 312 nm. In contrast, under anaerobic conditions, the spectral change of IM was almost absent, indicating IM was oxidized to the yellow substance by HRP-H2O2. Adding catalase strongly inhibited the production of yellow substance. Sodium azide also blocked the formation of yellow substance and the inactivation of CK. Electron spin resonance signals of IM carbon-centered radical were detected using 2-methyl-2-nitrosopropane during the interaction of IM with HRP-H2O2 under anaerobic conditions. Oxygen was consumed during the interaction of IM with HRP-H2O2. These results suggest that IM carbon-centered radicals may rapidly react with O2 to generate the peroxyl radicals. Sulfhydryl groups and tryptophane residues of CK decreased during the interaction of IM with HRP-H2O2. Other sulfhydryl enzymes, including alcohol dehydrogenase and glyceraldehyde-3-phosphate dehydrogenase, were also readily inactivated during the interaction with HRP-H2O2. Sulfhydryl enzymes seem to be very sensitive to IM activated by HRP-H2O2.

Alcohol Dehydrogenase↗
PubMed2001

Indomethacin-loaded methoxy poly(ethylene glycol)/ poly(epsilon-caprolactone) diblock copolymeric nanosphere: pharmacokinetic characteristics of indomethacin in the normal Sprague-Dawley rats.

We prepared the drug-loaded polymeric nanospheres composed of the methoxy poly(ethylene glycol) (MePEG) and poly(epsilon-caprolactone) (PCL) that showed a narrow size distribution and average diameter of less than 200 nm. We could obtain the nanosphere having a relatively high drug-loading efficiency of about 42% when the feed weight ratio of indomethacin (IMC) to polymer was 1:1. To investigate the IMC pharmacokinetics in the IMC-loaded MePEG/PCL nanosphere (DMEP70) using the rats as animal model, we analyzed the IMC concentration in plasma with HPLC after i.v. bolus administered at a dose of 10 mg/kg in free IMC (control) and IMC-loaded MePEG/PCL nanosphere (DMEP70) groups via tail vein. Pharmacokinetics parameters (mean +/- s.d.) such as the mean residence time (MRT, h), the steady-state volume of distribution (Vdss, l), the terminal half-time (t 1/2, h) and the plasma clearance (CL, l/h) of IMC in each groups (control vs. DMEP70) were determined; MRT (16.97 +/- 4.83 vs. 28.69 +/- 11.28, p < 0.01); Vdss (14.26 +/- 4.86 vs. 20.37 +/- 12.04, p < 0.05); t 1/2 (15.12 +/- 4.77 vs. 23.1 +/- 8.24, p < 0.01); CL (0.84 +/- 0.27 vs. 0.71 +/- 0.41). From these results, we could concluded that MEP70 has a significant potential for sustained release and the enhancement of circulation time of loaded drug by prolonging terminal half-life, increasing MRT and Vdss of IMC. Therefore, The MePEG/PCL block copolymeric nanosphere system is being considered as promising biodegradable and biocompatible drug carrier vehicles for parentral use and may be useful as sustained release injectable delivery systems for hydrophobic drugs.

Animals↗
PubMed2000

Enhanced absorption of indomethacin after oral or rectal administration of a self-emulsifying system containing indomethacin to rats.

A self-emulsifying system (SES), a mixture of an oil and a surfactant which forms an oil-in-water emulsion, is expected to improve the in vitro drug dissolution and enhance the in vivo drug absorption. In this study, a poorly water-soluble drug, indomethacin (IDM) was incorporated into the SES to increase bioavailability. The SES with 30% of Tween 85 and 70% of ethyl oleate, EO (w/w) was selected as an optimized formulation (high drug loading, low surfactant concentration, and small particle size). After an oral administration of the SES containing IDM and IDM suspension, (IDM was suspended in methyl cellulose), 22.5 mg/kg as IDM, to rats, the area under the plasma concentration-time curve from time zero to the last measured time in plasma, 12 h (AUC(0-12 h)) was significantly greater (57% increase) in the SES, suggesting that oral absorption of IDM increased significantly by the SES. After a rectal administration of gelatin hollow type suppositories, filled with the SES containing IDM and IDM powder physically mixed with the SES, 22. 5 mg/kg, to rats, the AUC(0-12 h) also increased significantly (41% increase) by the SES, suggesting that rectal absorption of IDM also increased significantly by the SES.

Administration, Oral↗
PubMed2006

Quantitative measurement of indomethacin crystallinity in indomethacin-silica gel binary system using differential scanning calorimetry and X-ray powder diffractometry.

Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRPD) methods were developed for the quantitative analysis of the crystallinity of indomethacin (IMC) in IMC and silica gel (SG) binary system. The DSC calibration curve exhibited better linearity than that of XRPD. No phase transformation occurred in the IMC-SG mixtures during DSC measurement. The major sources of error in DSC measurements were inhomogeneous mixing and sampling. Analyzing the amount of IMC in the mixtures using high-performance liquid chromatography (HPLC) could reduce the sampling error. DSC demonstrated greater sensitivity and had less variation in measurement than XRPD in quantifying crystalline IMC in the IMC-SG binary system.

Calibration↗
PubMed2002

Effects of particle size, helium gas pressure and microparticle dose on the plasma concentration of indomethacin after bombardment of indomethacin-loaded poly-L-lactic acid microspheres using a Helios gun system.

We investigated the effects of the particle size of indomethacin-loaded poly-L-lactic acid microspheres (IDM-loaded PLA MS), the helium pressure used to accelerate the particles, and the bombardment dose of PLA MS on the plasma concentration of IDM after bombarding with IDM-loaded PLA MS of different particle size ranges, 20-38, 44-53 and 75-100 microm, the abdomen of hairless rats using the Helios gene gun system (Helios gun system). Using larger particles and a higher helium pressure, produced an increase in the plasma IDM concentration and the area under the plasma concentration-time curve (AUC) and resultant F (relative bioavailability with respect to intracutaneous injection) of IDM increased by an amount depending on the particle size and helium pressure. Although a reduction in the bombardment dose led to a decrease in C(max) and AUC, F increased on decreasing the bombardment dose. In addition, a more efficient F was obtained after bombarding with IDM-loaded PLA MS of 75-100 microm in diameter at each low dose in different sites of the abdomen compared with that after bolus bombardment with a high dose (dose equivalent). These results suggest that the bombardment injection of drug-loaded microspheres by the Helios gun system is a very useful tool for delivering a variety of drugs in powder form into the skin and systemic circulation.

Air Pressure↗
PubMed2004

An evidence-based approach to predicting low IQ in very preterm infants from the neurological examination: outcome data from the indomethacin Indomethacin Intraventricular Hemorrhage Prevention Trial.

We evaluated whether the degree of cerebral palsy (CP) at age 3 in very preterm children is predictive of full-scale intelligence quotient (FSIQ) <70 at age 8 by calculating likelihood ratios (LRs) for findings on the neurologic examination. Data from the follow-up phase of the Indomethacin Intraventricular Hemorrhage Prevention Trial, which includes periodic neurologic examination and neuropsychometric testing, were used. Information was available on 366 of 440 (83%) children with birth weight of 600 to 1250 g who survived. Neurologic examination at age 3 was grouped by presence and type of CP, and the Weschler Intelligence Scale for Children-Third Edition FSIQ at age 8 was grouped dichotomously (<70 or > or =70). CP was identified in 35 of 366 3-year-olds (9.5%). An FSIQ <70 was identified in 47 of 366 children at 8 years old (12.8%). FSIQ <70 occurred in 14 of 17 children with tri- or quadriplegia (82%), 8 of 18 children with di- or hemiplegia (44%), and 25 of 331 children without CP (7.5%). Useful LRs were calculated for tri- or quadriplegia (30), di- or hemiplegia (5.7), and children without CP (0.55). These LRs have greater impact on posttest odds for FSIQ <70 than those for birth weight <1000 g, history of bronchopulmonary dysplasia, and Stanford-Binet Intelligence Score <70 at age 3. We conclude that the neurologic examination at 3 years old predicts FSIQ <70 at age 8 with LRs that allow evidence-based parental counseling and intervention planning.

Cerebral Palsy↗