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Results for “Indoprofen”

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At least 19 recordsLinked to original sources

PubMed2003

DNA photosensitization by indoprofen - is DNA damage photoinduced by indoprofen or by its photoproducts?

The in vitro photosensitizing activity of indoprofen, a non-steroidal anti-inflammatory drug, toward DNA has been studied by gel sequencing experiments using (32)P-end labelled synthetic oligonucleotides in phosphate buffered solution. Upon irradiation at [small lambda] > 320 nm, piperidine-sensitive lesions were induced in single- and double-stranded DNA, exclusively at the position of guanine bases. In single-stranded DNA, all G sites were modified. This pattern of photooxidative damage without isotopic effect in deuterium oxide, is characteristic of a Type I mechanism involving electron transfer from the base to the excited drug. In duplex DNA, a Type I process was also observed since selective DNA breakage occurred with high selectivity at 5[prime or minute]-G of a 5[prime or minute]-GG-3[prime or minute]sequence. When the oligonucleotide displays TT sites, an energy transfer process becomes predominant, giving rise to the formation of thymine dimers as evidenced by using T4 endonuclease V. Moreover, the methyl ester of indoprofen has been synthesized in order to study the influence of the indoprofen photochemical properties in DNA photosensitization. The poor efficiency of this compound shows that the drug itself is not directly implicated in DNA photodamage and seems to imply the involvement of indoprofen photoproducts.

Animals↗

PubMed1985

Indoprofen, a non-steroidal anti-inflammatory analgesic which does not depress respiration in normal man. A study comparing indoprofen with morphine.

The respiratory effects of intravenous indoprofen 400 mg, a highly effective non-steroidal anti-inflammatory analgesic, were compared with those of morphine 10 mg in 10 healthy volunteers. Morphine exhibited its characteristic adverse respiratory depressant properties, Indoprofen, in contrast, did not influence the subjects' breathing pattern.

Adolescent↗

PubMed1989

[Binding of racemic indoprofen and its enantiomers to human serum albumin].

Binding of Racemic Indoprofen and its Enantiomers to Human Serum Albumin. The binding to 2% and 4% human serum albumin (HSA) of (+/-)-indoprofen, (-)-indoprofen, and (+)-indoprofen was examined applying a modified ultrafiltration process. The binding properties to HSA were characterized by determining the unbound portions of the drug (a), the overall binding constants (K1), the free reaction energy (delta F degrees), the apparent binding constants (k*), and slope (m). The following results were obtained: 1. Racemic indoprofen and its enantiomers show a high affinity to human serum albumin (a = 1-2%). 2. At higher HSA concentrations the free portion (a) diminishes. 3. The affinity to HSA is reduced in the order of levo-indoprofen racemic indoprofen, and dex-indoprofen.

Humans↗

PubMed1986

The effects of indoprofen vs paracetamol on swelling, pain and other events after surgery.

The capability of indoprofen compared to paracetamol in reducing swelling, pain and other events of an acute inflammatory reaction was tested in a double-blind crossover study with bilateral oral surgery. Identical surgical procedures were performed on two separate occasions in 24 patients. After one operation they received tablets of indoprofen, after the other, paracetamol. A double-placebo method was used, as dosage regimens for the two treatments were different. Medication started 3 h after surgery and continued for 3 days. Almost identical swelling was measured after both treatments indicating that indoprofen has the same anti-inflammatory activity as previously found with paracetamol, which reduces swelling with about 30% compared to placebo. The pain and preference assessments were significantly in favor of indoprofen. Subjective bleeding scores were significantly increased with indoprofen. However, bleeding was minimal, and the occurrence of hematoma/ecchymosis was not increased with indoprofen. The results indicate that indoprofen is capable of reducing an acute, post-operative inflammatory reaction. For this purpose, it appears to be more efficient than other non-steroid anti-inflammatory drugs like ibuprofen, oxyphenbutazone, indomethacin and naproxen.

Acetaminophen↗

PubMed1985

Comparison of a narcotic (oxicone) and a non-narcotic anti-inflammatory analgesic (indoprofen) in the treatment of renal colic.

Intravenous indoprofen (400 mg), a cyclooxygenase inhibitor, was compared with intramuscular oxicodone hydrochloride (= oxicone 10 mg), a narcotic analgesic agent, in regard to efficacy and side effects in the treatment of renal colic. Oxicone was combined with papaverine (20 mg). Patients were randomized to either treatment, and the drugs were given in double-dummy fashion, i.e. one injection of active drug plus one placebo injection. Pain intensity before and after treatment was registered by the patient (visual analog scale) and by a nurse, who also registered side effects. Oxicone was given to 46 patients and indoprofen to 48. The groups did not differ in body weight, age, sex distribution, or pretreatment intensity of pain. More patients required additional treatment in the oxicone than in the indoprofen group (19 v. 10). At 2-5 min after injection, pain reduction was greater with indoprofen, and more patients in this group had pain relief after 3-5 hours. Side effects were less frequent with indoprofen than with oxicone (1 v. 20 patients), in particular from the central nervous system. This difference probably was related to indoprofen's slow and poor penetration of the blood-brain barrier. The study affirmed that non-narcotic cyclooxygenase inhibitors can replace narcotic analgesics for acute pain alleviation in renal colic. Indoprofen seems to be a useful alternative, with low risk of central nervous side effects.

Adult↗

PubMed1985

Pharmacokinetics of indoprofen in elderly patients following repeated oral administration.

Twenty patients suffering from osteoarthritis or rheumatoid arthritis, aged between 60 and 85 years, received 200 mg indoprofen tablets thrice daily for 4-7 days. Following the last dose, plasma samples were drawn and analysed for indoprofen. The mean peak plasma concentration of 25.5 +/- 7.06 micrograms/ml indoprofen was reached after 1.25 +/- 0.71 h. The total area under the curve was calculated as 207.2 +/- 108.7 micrograms X h/ml. Indoprofen was eliminated with a mean elimination half-life of t1/2 beta = 8.29 +/- 2.93 h compared with 5.5 +/- 0.64 h in young subjects. In elderly patients receiving indoprofen, terminal plasma half-lives and area under the plasma level time curves corrected for body weight were moderately increased compared with young subjects whereas no significant differences were found for Vd beta. During the dosage interval indoprofen levels were appreciably higher in elderly patients than in healthy volunteers due to higher nadir values and slower elimination half-lives, whereas only minor differences could be detected for peak plasma levels. The differences observed between young healthy volunteers and elderly patients may be explained by the reduction of renal function with increasing age, since creatinine clearance was 30-40% lower than normal values. The dose schedule for elderly patients over 60 years of age should therefore be adjusted to 200 mg indoprofen twice daily. A further reduction of the total daily dose should be considered for patients suffering from renal diseases associated with reduced creatinine clearance.

Administration, Oral↗

PubMed1980

Kinetic interaction of glipizide and indoprofen in healthy volunteers.

There is accumulating evidence that salicylate and glipizide may exert a clinically relevant interaction. Therefore, it was of interest to examine the possible interactions of glipizide and antirheumatics of non-salicylate character, e.g., phenyl propionic acid derivatives. The present report deals with the possible interaction between glipizide and indoprofen, a novel and potent antirheumatic agent. The subjects studied were 6 healthy volunteers, who took indoprofen 200 mg t.i.d. for 7 days and a single 5 mg dose of glipizide before and during indoprofen medication. Series of blood samples were obtained for measurements of indoprofen, glipizide, and glucose concentrations in blood. In addition, urine concentrations of indoprofen were determined. The concentrations of glipizide and indoprofen were measured by high-pressure liquid chromatography, and that of glucose ezymatically. The results indicate that chronic indoprofen administration may reduce glipizide concentrations in plasma, but this reduction need not lead to a major influence on the blood glucose response to glipizide.

Adult↗

PubMed1981

Three trials of indoprofen.

Three trials have been used to document various properties of indoprofen. As a simple analgesic, indoprofen (200 mg) was superior to placebo and at least as effective as aspirin (700 mg). As an anti-inflammatory, indoprofen (200 mg four times daily) was superior to both ibuprofen (300 mg four times daily) and placebo. With regular administration, the effect of indoprofen reached a plateau within 24 hours of the start of treatment. Long term administration confirmed the safety of indoprofen and the overall incidence of side effects was similar to that associated with ibuprofen therapy. Equal numbers of patients were withdrawn from the indoprofen and ibuprofen groups but the reasons for withdrawal were different. Patients were withdrawn from the ibuprofen group because of lack of effect and from the indoprofen group because of gastric side effects.

Anti-Inflammatory Agents↗

PubMed1981

Interaction of glipizide and indoprofen.

The possible kinetic and dynamic interactions of indoprofen and glipizide were investigated in 6 healthy volunteers, taking indoprofen 200 mg t.i.d. for 7 days and a single dose of glipizide 5 mg before and during indoprofen medication. Series of blood samples were obtained for measurements of indoprofen, glipizide and glucose concentrations in blood. In addition urine concentrations of indoprofen were determined. The concentrations of indoprofen and glipizide were examined by HPLC and that of glucose enzymatically. Results suggest that indoprofen may reduce glipizide concentrations in plasma, but this does not seem to influence the blood glucose response to glipizide.

Administration, Oral↗

PubMed1978

The effect of indoprofen on phenylquinone-writhing and prostaglandin synthesis.

The ability of indoprofen or sodium indoprofen to inhibit phenylquinone-writhing and renal prostaglandin synthesis was determined in mice following a single oral dose of either drug. Male mice (4/group) were treated with 1.5 mg/kg indoprofen or sodium indoprofen. Inhibition of phenylquinone-writhing was determined at 2, 4, 8, 16 and 32 hr post treatment. Animals were sacrificed and blood collected for determination of plasma indoprofen concentration. Kidneys were removed and prepared for determination of renal prostaglandin synthesis by an in vitro technique. Phenylquinone-writhing was significantly depressed by both preparations at 2 and 4 hr post treatment. Sodium indoprofen also significantly depressed writhing at 8 hr post treatment. Renal prostaglandin synthesis, like phenylquinone-writhing, was significantly depressed at 2 and 4 hr after drug treatment. Plasma indoprofen concentration was correlated with both inhibition of phenylquinone-wrighing and inhibition of renal prostaglandin synthesis. When writhes were plotted versus prostaglandin synthesis, a positive correlation was observed suggesting a temporal relationship between inhibition of phenylquinone-writhing and inhibition of renal prostaglandin synthesis.

Analgesics↗

PubMedDate not supplied

A study of the analgesic potency of indoprofen and pentazocine in postoperative pain.

The relative potency of intravenous indoprofen and intramuscular pentazocine in postoperative pain was evaluated. Indoprofen was administered in 200- and 400-mg single doses and pentazocine was given in 15- and 30-mg doses. Pain was assessed at different time intervals, and additional medication consumption was recorded, as well as side effects and overall evaluations. An analysis of peak pain intensity difference (PID) has shown a significant dose-effect relationship for both drugs and a potency ratio of 1:7 between indoprofen and pentazocine (mg to mg). Based on the frequency of patients requiring remedication and those reporting total pain relief in at least one instance, the potency ratio of indoprofen:pentazocine was 1:13 and 1:10, respectively. The mean peak PID of the pooled data for both doses of each drug was significantly greater for indoprofen. Intravenous indoprofen 400 mg was ranked the most effective overall.

Humans↗

PubMed1980

Intravenous indoprofen for prompt relief of acute gout: a regimen-finding study.

The results of an open exploratory trial with different regimens of indoprofen in patients with acute gouty arthritis are described. Two main daily regimens were assessed: (a) indoprofen 200 mg as an intravenous bolus, followed by slow infusion of 100 mg/hour for about 4 hours (24 attacks treated in twenty-three patients); and (b) indoprofen 400 mg as an intravenous bolus (13 attacks treated in twelve patients). In both regimens intravenous indoprofen was supplemented with 400-600 mg daily of indoprofen by mouth. The patient's response, as judged by pain, tenderness, local heat, redness, range of motion and joint circumference, was dramatic in both series, with no significant difference between them at any time of observation. Substantial improvement was apparent for subjective variables already within 2 hours after the beginning of treatment, and a complete resolution was obtained in 35 of 37 attacks within 48 hours. A mild adverse reaction was recorded in one patient for each group (dizziness and gastric pain, respectively). Intravenous indoprofen appears to afford an extremely rapid relief of acute gout; of the two regimens assessed, the second should be preferred in that it seems to be at least equally effective but less troublesome for the patients.

Acute Disease↗

PubMed1984

Pharmacokinetics of the enantiomers of indoprofen in man.

Indoprofen, a non-steroidal analgesic and antiinflammatory drug whose activity and safety in man have been established in a large number of studies, has an asymmetric carbon atom and can therefore occur as either the (+) or the (-) enantiomer. As it has been shown that its pharmacological effects are almost entirely due to the (+) isomer (d-indoprofen), some pharmacokinetic properties of the latter have been studied in man in comparison with the racemic mixture given by oral administration, d-indoprofen is cleared from plasma and excreted in urine (as unchanged plus conjugated drug) at a slower rate than l-indoprofen. Moreover, no stereospecific inversion of d-indoprofen to the inactive enantiomer occurs after either single or repeated (one week) administration. The pharmacokinetic behaviour of d-indoprofen in the human organism appears to be the same after administration of the racemic form or of the dextro-enantiomer, when the latter is given at half the dose.

Administration, Oral↗

PubMedDate not supplied

The in vitro metabolic inversion of R(-) to S(+) indoprofen.

The paper reports a study on the metabolic inversion of indoprofen (2-[4-(2-isoindolinyl-1-one)-phenyl]-propionic acid) following incubation of the drug with liver microsomes from non-induced and phenobarbital-induced rats. The enantiomeric composition of the drug was determined after different incubation times of the racemate and the individual isomers. The S(+)/R(-) ratio was evaluated by densitometry following HPTLC separation of the R(+)-1-phenylethylamides. After incubation of the racemate and the individual isomers, no detectable amounts of indoprofen catabolites were extracted from the acidified incubation mixture. An appreciable enrichment in the S(+) enantiomer was observed after incubation of both racemate and R(-)-indoprofen; the S(+)/R(-) ratio reached a maximum after 1 h. Values were higher in the case of induction. After incubation of S(+)-indoprofen, a small but statistically significant decrease of the S(+)/R(-) ratio was observed. The increase of the S(+)-isomer concentration observed following incubation of R(-)-indoprofen can be ascribed to metabolic inversion by phenobarbital-inducible liver enzymes.

Animals↗

PubMed1979

Indoprofen versus ibuprofen in osteoarthrosis: a short-term, double-blind, crossover trial.

A double-blind, crossover, short-term clinical trial was carried out in osteoarthrosis to compare the activity of two non-steroidal anti-inflammatory drugs. Twenty-four patients were given orally, in sequence, 600 mg indoprofen daily and 1200 mg ibuprofen daily, or vice-versa, for 1 week with no interval between treatment periods. Pain, quality of sleep, and overall effectiveness were recorded at the end of each week by inviting patients to express a score on a simple rating scale. Finally, patients were asked to express a preference for one treatment or the other. Significant improvement was observed in all parameters following treatment with both drugs. The distribution of score differences between indoprofen and ibuprofen was in favour of the former in all measurements; statistical analysis, however, demonstrated a significant superiority of indoprofen only for pain elicited by passive motion. The patients' preferences were also in favour of indoprofen, though not attaining statistical significance. Indoprofen was well tolerated, and no side-effects were observed. While on treatment with ibuprofen, 1 patient had to be withdrawn from the study because of gastric intolerance and 2 further patients had transient skin rashes.

Adult↗

PubMed1980

A double-blind, crossover comparison between indoprofen and aspirin in rheumatoid arthritis.

Twenty in-patients with rheumatoid arthritis took part in a double-blind, crossover clinical trial to compare the effectiveness and tolerance of 400 mg indoprofen with 1000 mg aspirin each given 3-times a day for 1 week, with an interval of 2 days during which patients received an indistinguishable placebo. At the start and at the end of each treatment period several subjective and objective indices were measured. Both indoprofen and aspirin to remable improvement in patient conditions, with no significant differences between drugs in overall pain, number of swollen joints, grip strength and functional index. Indoprofen, however, was significantly superior to aspirin with regard to the number of painful joints (p < 0.01), duration of morning stiffness (p < 0.05) and articular index (p < 0.05). Moreover, both patients' and investigators' opinion of overall response favoured indoprofen. Small but significant decreases were recorded in ertythrocyte sedimentation rate and seromucoid levels in both treatment periods. Adverse reactions, mainly as gastric pyrosis and/or gastralgia, occurred in 6 patients while on aspirin, in 2 while on indoprofen, and in a further 2 while on both drugs. No statistically significant changes were observed in safety laboratory tests.

Adult↗

PubMed1985

Analgesic treatment in acute myocardial infarction: a comparison between indoprofen and morphine by a double-blind randomized pilot study.

On the basis of the results of an earlier study, showing that i.v. indoprofen induced no clinically significant changes in hemodynamic parameters of patients with acute myocardial infarction (AMI), a double-blind randomized trial was carried out in 40 AMI patients to evaluate the analgesic activity of 400 mg i.v. indoprofen in comparison with 10 mg i.m. morphine hydrochloride. Pain severity was recorded before and at several intervals within 24 h after drug administration. The average analgesic response was prompt and progressive up to the 6th hour in both treatment groups, with no significant difference between drugs in various pain descriptors. However, the proportion of responding patients in indoprofen group was greater than in morphine group at all observation times, indicating a significant difference (p less than 0.05) in favor of indoprofen. In view of its good tolerability, i.v. indoprofen is worth considering in early AMI as an alternative to morphine in those patients in whom non-opiate analgesia might be preferable.

Adult↗

PubMed1983

Effect of i.v. indoprofen on cancer pain and serum prolactin and growth hormone levels--a controlled pharmacologic study vs i. m. morphine and placebo.

Single doses of indoprofen (400 mg, i.v.), morphine hydrochloride (10 mg, i.m.), and placebo were given to 12 women with moderate to severe tumor pain, mainly due to bone involvement, according to a Latin square design. Analgesic response, along with serum prolactin (PRL) and growth hormone (GH) levels, were measured after each treatment under double-blind conditions. Indoprofen and morphine were not significantly different as regards pain relief, but both were significantly more effective than placebo. Unlike morphine, however, indoprofen did not raise PRL. GH levels did not change following any treatment. In a second study indoprofen (400 mg, i.v., three times daily for 7 days) did not modify the PRL response to thyrotropin-releasing hormone nor serum GH levels. On the basis of the above findings it is suggested that indoprofen may be a safe alternative to opiates for relief of moderate to severe pain in women with breast tumors suspected of being prolactin-dependent.

Adult↗