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At least 73 records · Page 4Linked to original sources
PubMed1983

Oral analgesic efficacy of suprofen compared to aspirin, aspirin plus codeine, and placebo in patients with postoperative dental pain.

The purpose of this study was to evaluate the analgesic efficacy and safety of single oral doses of suprofen 200 and 400 mg, compared with aspirin 650 plus codeine 60 mg, aspirin 650 mg, and placebo in the relief of moderate to severe pain resulting from the surgical removal of impacted third molars. 157 patients completed a randomized, double-blind, single-dose, stratified, parallel-groups trial, and were observed for at least 4 h. Based upon each of the summary efficacy measures, sum pain intensity difference (SPID), percent SPID, TOTPAR and a global evaluation, all four active treatments were approximately equally effective and all were statistically superior to placebo. In addition, suprofen at both dose levels was significantly more effective than placebo beginning at the 0.5-hour observation for mean pain intensity, whereas the two aspirin treatments were not superior to placebo until the 1-hour observation. Side effects were minimal; there was one in the suprofen 200 mg, three in the aspirin 650 mg, and one in the placebo treatment group. Thus, it appears that suprofen at 200 and 400 mg is a safe and effective oral analgesic for the relief of moderate or severe postoperative dental pain, and it is possible that compared to aspirin 650 mg and aspirin 650 mg plus codeine 60 mg, it has a more rapid onset of action.

Adolescent↗
PubMed1983

Multiple-dose comparison of suprofen, aspirin, and placebo in the treatment of musculoskeletal pain.

The effectiveness and safety of suprofen 200 mg, aspirin 650 mg, and placebo in the treatment of moderate to severe pain were compared in a 72-hour multiple-dose, double-blind, parallel, randomized study in 75 adults suffering from musculoskeletal pain. Suprofen was superior to aspirin and placebo for pain relief, total pain relief scores, pain severity, activity impairment, comparative evaluation of activity impairment, and comparative evaluation of pain and sleep, with differences achieving statistical significance for most parameters at the 24- to 72-hour evaluation points. 1 mild, transient side effect occurred in the suprofen group, 3 in the placebo group, and 4 of moderate intensity in the aspirin group. The effectiveness of multiple-dose treatment of musculoskeletal pain with suprofen 200 mg is superior to that of aspirin and placebo.

Adolescent↗
PubMed1988

Suprofen-induced uricosuria. A potential mechanism for acute nephropathy and flank pain.

Suprofen, a nonsteroidal anti-inflammatory drug, has been associated with the onset of acute flank pain, hematuria, and transient renal dysfunction after the ingestion of one or two doses, particularly in young males. Potential mechanisms of this nephropathy were evaluated in normal males following ingestion of suprofen (200 mg) on two occasions: the first with ad libitum fluid intake and the second during forced water diuresis. On the first study occasion, creatinine clearance, the fractional excretions of uric acid (FEUA) and sodium (FENa), the urinary concentration of undissociated uric acid, and the urinary excretions of prostaglandins and glomerular and tubular proteins were assessed. On the second occasion, inulin and PAH clearances and FEUA and FENa were determined. Within 90 min after suprofen administration, the FEUA increased from 8.8 +/- 2.6 to 35.5 +/- 9.6% (p less than 0.05). Urine became supersaturated for uric acid during ad libitum fluid intake. Glomerular filtration rate, renal plasma flow, and FENa decreased significantly, while prostaglandin and protein excretions did not change. The findings are consistent with acute uric acid nephropathy as a mechanism of suprofen-induced renal dysfunction.

Acute Disease↗
PubMed1986

Treatment of postoperative pain with suprofen injected by the intramuscular route.

The analgesic effect and the tolerability of alpha-methyl-4-(2-thienyl-carbonyl)phenylacetic acid (suprofen, Suprol) 200 mg/ml were compared with lysine acetylsalicylate 0.9 g/2.5 ml; the study included 60 subjects in severe to very severe pain following orthopedic surgery. The trial was performed in randomized single-blind fashion in patients who had given informed consent. The substances were injected into the upper out quadrant; maximally 4 intramuscular injections were given within 2 days. The test population was homogeneous with respect to the anamnestic data. The intensity of pain prior to treatment was comparable in both groups. Statistical analysis of the data revealed that suprofen was at the rating times (15 min to 4 h) significantly superior to the control groups. The investigator's and the patients' final appreciation indicated good to very good effect in 93% of the subjects on suprofen, and in 40 and 47%, respectively, of the patients in the control group. Here, too, suprofen was significantly superior to the reference Substance. Systemic and local tolerability of both drugs was very good. Adverse drug experience (heartburn) occurred in only 1 patient in the control group.

Adult↗
PubMed1986

Double-blind placebo-controlled study of the efficacy and tolerability of suprofen suppositories in patients with osteoarthritic pain.

In a placebo-controlled double-blind trial analgesic effectiveness and tolerability of alpha-methyl-4-(2-thienyl-carbonyl)phenylacetic acid (suprofen, Suprol) 300 mg suppositories were evaluated for 45 informed patients suffering from chronic pain due to osteoarthritis; the subjects were treated rectally, t.i.d., for 10 days. Suprofen proved to be statistically significantly superior to placebo in all the variables considered for evaluation of the analgesic effect, i.e., pain intensity and relief scores, sum of pain intensity differences (SPID), total pain relief (TOTPAR), global assessments by investigator and patient. In particular, the efficacy of suprofen was judged by the physician good or very good in 86.3% of the patients. Similar frequencies of rectal side-effects were observed in both treatment groups, with slightly but not significantly higher incidence in the group treated with suprofen. Haematologic and clinical chemistry laboratory tests showed no statistically significant alterations due to the treatment.

Adult↗
PubMed1986

Open clinical study with suprofen drops in the treatment of postoperative and posttraumatic pain.

Analgesic effect and tolerability of alpha-methyl-4-(2-thienyl-carbonyl)phenylacetic acid (suprofen, Suprol) drops were tested in an open study including 51 informed outpatients with moderate to severe postoperative and posttraumatic pain. Suprofen drops were administered for 7 days, at doses of 33 drops (= 200 mg of suprofen) t.i.d. or q.i.d. The pain intensity was recorded prior to the treatment and after 2, 4 and 7 days; pain relief was assessed on days 2, 4 and 7. Effectiveness and tolerability were by the investigator and by the patients globally evaluated upon completion of the trial. The intensity of pain dropped within the 7-day treatment period from initially severe pain to mild. Pain relief was seen in 92% of the subjects after day 2, in 98% after day 4, and in 100% after day 7 of treatment. Investigator's and patients' final evaluation of the therapeutic effect indicated good analgesic activity in 86% of the population, and very good analgesic effect in 84%. Moderate effect was seen in 12 and 14%, respectively. The tolerability of suprofen drops was by investigator and patients considered good to very good in 82% of the cases, moderate in 16%, and poor in 1 case.

Adult↗
PubMed1983

Double-blind study of suprofen vs naproxen in the treatment of osteoarthritic pain.

In a 2-week double-blind study involving 79 patients with mainly osteoarthritis of the hip and knee, Suprofen and Naproxen were compared for efficacy and tolerability in the treatment of the symptoms of the disease. The drugs were administered on a b.i.d. schedule: 800 mg of Suprofen or 750 mg of Naproxen. Nocturnal pain, pain at rest, pain on motion and tenderness were evaluated at baseline and at days 7 and 14. Results showed that patients in both groups were significantly improved in all parameters. Between the groups no statistically significant differences were found. Thus, Suprofen was as effective in pain relief as Naproxen. One patient in the Suprofen group and two patients in the Naproxen group experienced mild gastrointestinal symptoms. Overall tolerability was very good.

Aged↗
PubMed1975

Effects of suprofen, an inhibitor of prostaglandin biosynthesis, on platelet function, plasma coagulation and fibrinolysis II. In vivo experiments.

Suprofen, an inhibitor of prostaglandin biosynthesis, was found to affect certain aspects of platelet function after in vivo administration in various species. In guinea-pigs, platelet aggregation induced by collagen and Thrombofax, and secondary A.D.P. aggregation were reduced in a dose-dependent way by suprofen (single oral administration) from 0.08 mg/kg on. In dogs, the effect of a single oral dose of 2.5 mg/kg of suprofen on collagen-induced aggregation started 30 min after administration, lasted for at least 8 h and had disappeared after 24 h. Plasma coagulation parameters were not affected by the compound in this species. In rats, suprofen prolonged tail bleeding times, but did not modify fibrinolysis, platelet adhesion to glass beads or plasma coagulation. Sub-chronic administration of comparatively high doses of the compound resulted in potentiation of the anti-coagulant effect of warfarin in this species.

Adenosine Diphosphate↗
PubMed1976

Inhibition by suprofen and other non-narcotic analgesic drugs of the effects of prostaglandin precursor on isolated tissues and platelets.

Contractions caused by Slow Reacting Substance C(SRS-C) and by Arachidonic Acid hydroperoxide (AAP) in the guinea-pig ileum and by AAP in the rat fundus were studied in the presence of suprofen and of 3 reference compounds. The dose-related inhibitions were not due to antagonism of prostaglandins. Other agonists of gastrointestinal smooth muscle were not or only weakly antagonized. For the study of selective inhibition of AAP-induced contractions by non-narcotic analgesics, the rat fundus is the preferred preparation. In this model suprofen had an ED50 of 1.27 x 10(-7) M (0.033 mug/ml), being 1.5, 94 and 2, 020 times more potent than indomethacin, phenybutazone and acetylsalicylic acid, respectively. Suprofen also strongly inhibited malondialdehyde formation by guinea-pig platelets incubated with arachidonic acid. The reported effects point to inhibition by suprofen of prostaglandin biosynthesis. The antagonism of AAP-induced contractions in the rat fundus is a valuable test system for inhibitors of prostaglandin biosynthesis.

Analgesics↗
PubMed2000

Dynamic kinetic resolution of suprofen thioester via coupled trioctylamine and lipase catalysis.

A lipase-catalyzed enantioselective hydrolysis process under conditions of continuous in situ racemization of substrate with trioctylamine as the catalyst was developed for the production of (S)-suprofen from (R,S)-suprofen 2,2,2-trifluoroethyl thioester in isooctane. A detailed investigation of trioctylamine concentration on the enzyme activation and stability as well as the kinetic behaviors of the thioester in racemization and enzymatic reaction was conducted, in which good agreement between the experimental data and theoretical results was observed. A complete conversion of the racemate for the desired (S)-suprofen in 95% ee(P) was obtained. Moreover, the recovery of the acid product by extraction and reuse of the organic solution were reported.

Amines↗
PubMed2004

Process modeling of the lipase-catalyzed dynamic kinetic resolution of (R, S)-suprofen 2,2,2-trifluoroethyl thioester in a hollow-fiber membrane.

A Candida rugosa lipase immobilized on polypropylene powder was employed as the biocatalyst for the enantioselective hydrolysis of (R, S)-suprofen 2,2,2-trifluorothioester in cyclohexane, in which trioctylamine was added as the catalyst to perform in situ racemization of the remaining (R)-thioester. A hollow-fiber membrane was also integrated with the dynamic kinetic resolution process in order to continuously extract the desired (S)-suprofen into an aqueous solution containing NaOH. A kinetic model for the whole process (operating in batch and feed-batch modes) was developed, in which enzymatic hydrolysis and deactivation, lipase activation, racemization and non-enantioselective hydrolysis of the substrate by trioctylamine, and reactive extraction of (R)- and (S)-suprofen into the aqueous phase in the membrane were considered. Theoretical predictions from the model for the time-course variations of substrate and product concentrations in each phase were compared with experimental data.

Amines↗
PubMed1998

Swellable microparticles containing Suprofen: evaluation of in vitro release and photochemical behaviour.

Suprofen, an anti-inflammatory drug was incorporated in polymer networks based on biocompatible macromolecules, such as alpha,beta-polyasparthydrazide (PAHy) and alpha,beta-poly(N-hydroxyethyl)-DL-aspartamide (PHEA) crosslinked by glutaraldehyde or gamma-rays, respectively. Swelling tests carried out in aqueous media showed that pH value affects the swelling degree of the prepared hydrogels. In vitro release tests were performed in simulated gastrointestinal fluids (pH 1/6.8) using the pH variation method and in phosphate-buffered saline, pH 7.4. Experimental data indicated that Suprofen was released in a sustained way both from PAHy and PHEA microparticles. Further, incorporation of Suprofen in PAHy and PHEA networks provided a significant reduction of the drug photosensitizing activity, as evidenced by in vitro hemolysis tests.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1991

Effects of topical suprofen and flurbiprofen on the miosis produced by anterior chamber irrigation with cholinergic agonists.

Pretreatment with topical nonsteroidal anti-inflammatory drugs is common practice to maintain maximal pupil dilation for cataract surgery. Most surgeons also inject a cholinergic agent intracamerally for miosis after intraocular lens insertion. We evaluated the effects of topical suprofen and flurbiprofen on the miosis induced by anterior chamber irrigation with either acetylcholine or carbachol. One eye of 30 pigmented rabbits was dilated with cyclopentolate HCl and phenylephrine HCl. Three groups, each composed of ten eyes, received flurbiprofen, suprofen, or a control. In each group, five eyes received acetylcholine by anterior chamber irrigation and five received carbachol. Pupil diameters were measured with calipers before and five minutes after irrigation by an observer unaware of the treatment regimen. Irides irrigated with carbachol constricted less than those irrigated with acetylcholine (P = .016). In anterior chambers irrigated with carbachol, suprofen was associated with less miosis than either tears (P = .005) or flurbiprofen (P = .009); however, if the infusion was performed with acetylcholine, no differences between the three groups were noted (P = .44).

Acetylcholine↗
PubMedDate not supplied

Mechanisms of drug photobinding to proteins: photobinding of suprofen to human serum albumin.

Photobinding of drugs to biomolecules constitutes an important early event in the onset of photoallergy. In the present work, UV irradiation of human serum albumin in the presence of either suprofen (SUP) or its major photoproduct, decarboxylated suprofen (DSUP), has been studied as a model system for drug-photosensitised protein binding. Both dark binding and binding in the presence of light were investigated since this will affect the mode, site and mechanism of drug interaction with the protein. In order to determine the binding features of SUP to albumin, competitive binding experiments were carried out using fluorescent probes specific for site I and II. Suprofen was found to selectively dark bind to site II on HSA. Photobinding of DSUP to HSA was more efficient than SUP. Parallel to this, the intrinsic tryptophan fluorescence of HSA decreased when the protein was previously irradiated in the presence of the photoactive compounds, again being DSUP more efficient compared with SUP. As fluorescence quenching involves electron transfer from the excited Trp to the ground state DSUP, it follows that the photoactive compound binding to HSA must be on (or in close proximity to) site I Trp(214) residue. It appears that photobinding of SUP is largely preceded by its photodecomposition to DSUP which, in turn, associates and photobinds to HSA.

Binding, Competitive↗
PubMed1994

Photodynamic lipid peroxidation by the photosensitizing nonsteroidal antiinflammatory drugs suprofen and tiaprofenic acid.

The photochemistry of the photosensitizing nonsteroidal antiinflammatory drugs tiaprofenic acid and suprofen involves the intermediacy of short-lived species (i.e. radicals). The data obtained in the present work strongly suggest that such intermediates may be responsible for the phototoxicity of 2-arylpropionic acids by inducing photodynamic lipid peroxidation at drug concentrations likely to be reached in the skin. This has been investigated using linoleic acid as a model lipid and determining the amount of hydroperoxides by measuring the spectrophotometric absorption at 233 nm, associated with the formation of dienic hydroperoxides. The major photoproducts of tiaprofenic acid and suprofen are derivatives bearing an ethyl side chain. Photoproducts of this type, due to the lack of polar moieties, are highly lipophilic and likely to accumulate in the lipid bilayer of cell membranes. Taking into account their ability to induce photodynamic lipid peroxidation and their marked photostability, it is conceivable that such photoproducts can participate in many catalytic cycles, playing a significant role in the mechanism of photosensitization by tiaprofenic acid and suprofen.

Animals↗
PubMed1983

Comparison of suprofen and ibuprofen in the treatment of pain secondary to osteoarthritis.

43 patients with osteoarthritis of the knee and/or hip(s) were treated with suprofen 800 mg/day or ibuprofen 1,600 mg/day for 14 days. Both drugs produced an improvement in subjective symptoms by day 7, although the most rapid analgesic effect was obtained with suprofen. Patients receiving suprofen experienced a significantly greater improvement in pain on motion at day 7 than did patients taking ibuprofen. Patients and investigators evaluated both drugs as having good to very good efficacy in the great majority (over 75%) of cases. Both drugs were well tolerated, with only a single drug withdrawal in the ibuprofen group.

Adolescent↗
PubMed1983

Long-term clinical evaluation of suprofen and aspirin in patients with osteoarthritis.

The safety and efficacy of suprofen 200 mg q.i.d. and aspirin 650 mg q.i.d. in the treatment of chronic pain due to osteoarthritis were compared in a double-blind, randomized, parallel group study over a 12-week period. Suprofen was comparable to aspirin in the relief of pain and improvement in activity impairment. Results of ocular examination, laboratory data, and vital signs examinations indicated no clinically significant changes for suprofen. No serious side effects were reported by either group.

Aspirin↗
PubMed1983

Clinical comparison of the analgesic efficacy of suprofen, diflunisal and placebo in the treatment of pain after meniscectomy.

Suprofen 200 mg and suprofen 400 mg were found to be as efficacious as diflunisal 750 mg in a single-dose, double-blind randomized study of 130 hospitalized patients with pain following meniscectomy. Pain intensity was measured using both an interval scale and a visual analogue scale. Pain indices derived from both scales as well as the physician's global evaluation were consistent in demonstrating that suprofen is an effective analgesic agent in the relief of moderate to severe pain following orthopedic surgery.

Adolescent↗