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PubMed1976

Mechanism of action of a new anti-inflammatory agent, naproxen (II). Effects of naproxen on activities of mucopolysaccharase, acid protease and collagenolytic enzymes in inflamed tissues.

In order to elucidate the biochemical anti-inflammatory properties of naproxen, the effects of this compound on activities of mucopolysaccharase [beta-glucuronidase (beta-Gase) and lysozyme (LZ)], acid protease (APase) and collagenolytic enzyme (CL) in inflamed tissues were investigated by means of a proliferative inflammatory model in filter-paper-implanted rats. In the preventive test, naproxen strongly inhibited granuloma formation and exudate accumulation as did indomethacin and prednisolone. Although the inhibitory effects of naproxen on all these enzymes were quite evident, indomethacin failed to inhibit APase activity. Prednisolone did not significantly inhibit LZ and APase activities in granuloma. In the curative test, prednisolone caused a marked decrease in the weight of the granuloma already formed and in the volume of the exudate, but with naproxen and indomethacin there was only a slight decrease. Naproxen and indomethacin induced slight but significant inhibition of LZ and CL activities, while prednisolone showing a weak inhibition of CL activity only. From these results, it may be concluded that anti-inflammatory and anti-rheumatic effects of naproxen are partly attributable to its inhibitory actions on these lysosomal enzymes.

Adenosine Triphosphatases↗
PubMed1992

Efficacy and tolerability of enteric-coated naproxen in the treatment of osteoarthritis and rheumatoid arthritis: a double-blind comparison with standard naproxen followed by an open-label trial.

One hundred and twenty-three patients with osteoarthritis (n = 50) or rheumatoid arthritis (n = 73) were enrolled in a 6-week, double-blind, randomized, controlled, parallel trial comparing enteric-coated naproxen with standard naproxen. Ninety-eight patients subsequently entered a 20-week, open-label trial of enteric-coated naproxen. The study demonstrated that naproxen in both its standard formulation and its new enteric-coated formulation is a highly effective form of therapy for osteoarthritis and rheumatoid arthritis. The tolerability profiles of the two formulations were similar in terms of the types of complaints reported. It is concluded that enteric-coated naproxen is an efficacious and well-tolerated formulation for the treatment of osteoarthritis and rheumatoid arthritis.

Adult↗
PubMedDate not supplied

Stereoselective (S)- and (R)-naproxen glucuronosyl transferases of rat liver.

Stereoselective glucuronidation of naproxen, one of the 2-arylpropionic acids that are widely used as anti-inflammatory drugs, was investigated in chromatofocusing fractions of solubilized liver microsomes from 3-methylcholanthrene- (MC) and phenobarbital- (PB) treated rats. On chromatofocusing of solubilized microsomes of PB-treated rats, two naproxen glucuronosyltransferase (GT) fractions were separated. The fraction eluting at pH 8.7 preferentially conjugated (S)-naproxen (S/R ratio = 1.6) and the fraction eluting at pH 7.8 mostly conjugated (R)-naproxen (S/R ratio = 0.7). Chromatofocusing of solubilized microsomes from MC-treated rats also resulted in the separation of two naproxen GT fractions, eluting at pH 9.4 (S/R ratio 0.2) and at pH 8.7 (S/R ratio 0.8). These two fractions coincided with the elution of known MC-inducible GT activities assigned to a GT isozyme variously termed 4-nitrophenol GT or GT-I. Interestingly, kidney microsomes, known to contain a high constitutive expression of GT-I, preferentially glucuronidated (R)-naproxen (S/R ratio 0.2). The S/R ratio of 0.8, observed with the pI 8.7 fraction of MC-treated rat liver, may be explained by the presence of a mixture of naproxen GTs, consisting of (R)-naproxen GT (S/R ratio 0.2) and of (S)-naproxen GT (S/R ratio 1.6). The results suggest that naproxen is conjugated by at least 3 GT isozymes in rat liver; these have been operationally designated (S)-naproxen GTPB (S/R ratio 1.6), (R)-naproxen GTPB (S/R ratio 0.7), and (R)-naproxen GTMC (S/R ratio 0.2). The latter isozyme is probably identical to the previously characterized MC-inducible GT-I. Thus, (S)- and (R)-naproxen represent useful substrates to distinguish different GT isozymes.

Adult↗
PubMed1992

Determination of naproxen and its metabolite O-desmethylnaproxen with their acyl glucuronides in human plasma and urine by means of direct gradient high-performance liquid chromatography.

Naproxen is metabolized in humans by O-demethylation, and by acyl glucuronidation to the 1-O-glucuronide. Naproxen, its metabolite and the conjugates can be measured directly by gradient high-performance liquid chromatographic analysis without enzymic deglucuronidation. The glucuronide conjugates were isolated by preparative chromatography from human urine samples. Mild acidic hydrolysis of one urinary conjugate resulted in naproxen. This conjugate was also formed by alkaline isomerization of isolated naproxen acyl glucuronide, indicating that the structure of this urinary conjugate must have been naproxen isoglucuronide (4-O-glucuronide). Mild acidic hydrolysis of another urinary conjugate resulted in O-desmethylnaproxen. This conjugate was also formed by alkaline isomerisation of isolated O-desmethylnaproxen acyl glucuronide, indicating that the structure of this urinary conjugate must have been O-desmethylnaproxen isoglucuronide (4-O-glucuronide). Calibriation curves were constructed by enzymic deconjugation of samples containing different concentrations of isolated naproxen acyl glucuronide, O-desmethylnaproxen acyl glucuronide, and the isoglucuronides of naproxen and O-desmethylnaproxen by mild acidic hydrolysis. The limit of quantitation of naproxen in plasma is 1.5 microgram/ml. The limits of quantitation in urine are: naproxen, O-desmethylnaproxen, naproxen acyl glucuronide and O-desmethylnaproxen acyl glucuronide, 1 microgram/ml; the isoglucuronide of naproxen and O-desmethylnaproxen, 1.5 microgram/ml. A pharmacokinetic profile of naproxen is shown, and some preliminary pharmacokinetic parameters of naproxen obtained from two human volunteers are given.

Acylation↗
PubMed1992

Long-term effect of naproxen on cancellous bone in ovariectomized rats.

Previous work shows that at 42 d post-ovariectomy (OX) in aged rats, naproxen, a nonsteriodal anti-inflammatory drug (NSAID) prevents cancellous bone loss. The purpose of this study was to evaluate the effects of naproxen on cancellous bone of aged OX and sham-OX rats, at 90 days post-OX. Six-month-old Sprague-Dawley retired breeder female rats underwent either sham-OX (n = 49) or OX (n = 65). Sham-OX rats were randomized into five groups and OX rats into six groups. The first five groups of both were given ad lib access to water containing 0, 4, 10, 25, or 62.5 mg/l of naproxen sodium. The sixth group of OX rats was given water containing 156.25 mg naproxen sodium/l. After ninety days, the rats were killed following in vivo dual calcein labeling. Terminal serum naproxen was measured by HPLC. In the proximal tibial metaphysis, trabecular bone volume, trabecular thickness, trabecular number, mineralizing surface (double label), osteoclast surface, and bone formation rate were measured. Sham-OX and OX rats were compared by t-test of means. Kruskal-Wallis tests and, as necessary, Dunnett's t-tests, were applied separately to the groups of Sham-OX and OX rats. Dose-related serum levels of naproxen up to 9.4 mcg/ml were achieved in the 156.25 mg/ml group. OX rats had significantly lower bone volume, trabecular thickness, and trabecular number than Sham-OX groups (p less than .001). OX rats had significantly higher mineralizing surface, formation rate, and osteoclast surface than sham-OX rats (p less than .001). No differences related to naproxen treatment existed in sham-OX rats. Naproxen treatment producing a serum level of 9.4 mcg/ml reduced bone volume in OX rats consuming water with 156.25 mg/l (p less than .05). At 90 days post-OX, naproxen, at serum levels of 9.4 mcg/ml or less, did not diminish estrogen-depletion cancellous bone loss in rats. Naproxen lacks lasting ability to halt estrogen-depletion bone loss in aged OX rats.

Animals↗
PubMed1979

Naproxen up to date: a review of its pharmacological properties and therapeutic efficacy and use in rheumatic diseases and pain states.

Naproxen is a propionic acid derivative with analgesic and anti-inflammatory activity which has been widely used in the treatment of rheumatic diseases. Naproxen has been well studied in rheumatoid arthritis and is as effective as aspirin but better tolerated, thus enabling more patients to continue with treatment. For this reason some clinicians now prefer to try propionic acid derivatives, such as naproxen, before aspirin in arthritic patients. In comparative studies with other non-steroidal anti-inflammatory drugs, such as indomethacin, ibuprofen, fenoprofen and others, all drugs were usually of similar overall efficacy although naproxen was sometimes preferred: but as with other non-steroidal anti-inflammatory agents, not all patients will respond to naproxen and in such cases other agents should also be tried until the most satisfactory drug is found for each patient. Naproxen is also effective in degenerative joint diseases of the hip and knee, although further well designed studies are needed to more clearly define its relative place compared with newer drugs such as diclofenac or diflunisal. Results of other comparative studies have shown that naproxen is a suitable alternative to phenylbutazone or indomethacin in ankylosing spondylitis and to aspirin in juvenile rheumatoid arthritis. Naproxen appears to be effective in reducing pain and swelling in acute gout and is an effective analgesic in patients with pain following surgery or trauma and in pain of dysmenorrhoea. Naproxen has generally been better tolerated than aspirin or indomethacin at the dosages used. Because of its relatively long plasma half-life, naproxen can with convenieice be given twice daily, and there is some evidence that once daily dosage is as effective in rheumatoid arthritis.

Animals↗
PubMed1975

[Long-term therapy of progressive chronic polyarthritis with naproxen].

The efficacy of d-2-(6'-methoxy-2'-naphthyl)-propionic acid (naproxen) in the treatment of patients with rheumatoid arthritis as well as its good tolerance has been established in double-blind studies which have been conducted in 34 centers in the U.S.A. Since the value of a new antirheumatic drug can only be assessed after years of clinical experience, provision was made in the protocols of the double-blind studies that the patients completing the controlled studies could continue naproxen treatment. Our experience is based on 603 patients, of whom 337 came from controlled, and 266 from previous open studies. The longest treatment with naproxen lasted four years. 16% of the patients discontinued therapy because of a exacerbation of their symptoms, and 8% because of side-effects, the latter being described in detail. Follow-up examinations of the patients were performed 4841 times at bi-monthly intervals. The statistical analysis of the objective disease symptoms showed a significant decrease of the rheumatic manifestations. In order to exclude the possibility of a long-term placebo effect, and as a proof of continuing efficacy, 73 patients received double-blind placebo instead of naproxen (placebo pulse) for two weeks, whereas the others continued on naproxen. Statistical analysis of the objective symptoms during the two treatment phases of the study showed naproxen significantly superior to placebo in all disease manifestations. Symptoms of those patients receiving placebo aggravated rapidly. They improved again after naproxen was resumed. The situation was reverse in those patients who received placebo during the second phase of the study. Side-effects were observed 13 times under placebo, but only two times under naproxen. The integration of a 2-week-placebo-pulse during long-term naproxen therapy of patients with rheumatoid arthritis is a sensitive method to prove the continuing therapeutic efficacy of this drug.

Arthritis, Rheumatoid↗
PubMed1975

Naproxen and aspirin in rheumatoid arthritis: a multicenter double-blind crossover comparison study.

One hundred nineteen adults with active definite or classical rheumatoid arthritis were studied in a multicenter double-blind crossover study of naproxen (500 mg/day) and aspirin (3.6 Gm/day). Each drug was given in sequence for a six-week study period. Patients already receiving corticosteriod and/or gold therapy were maintained at constant dose throughout the study, but analgesics and other nonsteroidal antiinflammatory agents were discontinued at baseline. Objective and subjective evaluations by both investigator and patient were carried out at two-week intervals. No significant difference in global evaluation of efficacy or individual measures of efficacy was observed between aspirin and naproxen therapy, although physicians' global evaluation tended to favor naproxen. Sedimentation rate was lower on aspirin (naproxen 43.1 mm/hr; aspirin 38.7 mm/hr; P=0.02). Naproxen, 250 mg twice daily, was significantly better tolerated than aspirin, 900 mg four times daily. Mild, moderate, and severe side effects were less frequent with naproxen. The incidence of heartburn was significantly lower on naproxen, and significantly fewer patients terminated their six-week study period on naproxen than on aspirin. There were no significant deviations from baseline values in hematocrit, white cell or differential counts, or in tests of renal and hepatic function during the course of the study.

Anti-Inflammatory Agents↗
PubMed1975

Ankylosing spondylitis: open long-term and double-blind crossover studies with naproxen.

Participation in open and double-blind crossover studies in rheumatoid arthritis confirmed that naproxen improved pain and stiffness. This observation suggested that naproxen might be effective in ankylosing spondylitis. The initial trial was open, but at six months, a double-blind crossover "placebo pulse" was superimposed on the open trial. Thirty-six patients entered the trial taking a daily dose of 500 mg naproxen. At the end of the first month, 35 assessed naproxen as being equally effective to, or better than, previous therapy. The first ten patients to complete six months on naproxen took part in a placebo pulse study comprising two consecutive four-week periods, in one of which each patient took 500 mg naproxen, in the other, identical placebo capsules, the order being randomized. Eight patients correctly identified the placebo capsules (P=0.02). During the 16 months of trial, six patients have withdrawn, two being in remission and four for lack of efficacy. The remaining 30 patients have completed six months and 22 have completed at least 12 months on naproxen. At the end of six months pain was less (P=0.02), morning stiffness had decreased (P less than 0.01), and immobility stiffness had improved (P less than 0.01). These patients are impressed by the improvement in pain and stiffness and have little disability. All continue full-time employment and have been able to increase their leisure activities without discomfort. No persistent side effects were observed, and naproxen appears to be a useful drug in the treatment of anklyosing spondylitis.

Anti-Inflammatory Agents↗
PubMed1992

Naproxen premedication reduces postoperative tubal ligation pain.

This study evaluated the effectiveness of naproxen sodium oral premedication in reducing postoperative pain, analgesic requirements and day surgery length of stay in patients undergoing outpatient laparoscopic tubal ligations. We undertook a randomized, double-blind clinical trial on ASA I and ASA II patients undergoing outpatient laparoscopic tubal ligations. The treatment group received two capsules containing naproxen sodium, 275 mg each, and the control group received two identical capsules containing placebo. Postoperative visual analogue pain scores, analgesic requirements, side-effects and length of day surgery stay were studied. Forty-four patients completed the study with 21 patients in the naproxen group and 23 in the placebo group. There was a statistically significant difference between groups in terms of pain score (naproxen group 0.9 +/- 0.2 vs placebo group 3.5 +/- 0.6); patients requiring postoperative opioids (naproxen group 0% vs placebo group 34.8%); and time spent in the day surgery unit (naproxen group 168 +/- 13 min vs placebo group 188 +/- 15 min). There was no difference in the incidence of nausea and vomiting. Only one person developed a side-effect from the naproxen sodium which was minor gastric discomfort. This study shows that naproxen decreased the postoperative tubal ligation pain with less subsequent postoperative analgesic requirements, less time to street fitness and no increase in analgesic side-effects. We recommend the use of this premedication in outpatient laparoscopic tubal ligations.

Administration, Oral↗
PubMed1977

Naproxen, aspirin, and codeine in postpartum uterine pain.

The analgesic efficacy of oral naproxen and its sodium salt was compared with that of aspirin and codeine in two separate trials involving 140 and 90 patients, respectively, with postpartum uterine pain in a single-dose, parallel, stratified, randomized, placebo-controlled, double-blind design. With 300 or 600 mg naproxen and with 275 mg naproxen sodium, significant analgesia, measured subjectively by pain intensity differences (PID), was prolonged at least 7 or 8 hr; onset tended to be delayed 2 hr or more. With 650 mg aspirin analgesia began within 1 hr and continued until the fifth hour, while with 60 mg codeine responses were indistinguishable from placebo responses throughout the 8-hr time course. Although time-effect patterns with naproxen sodium and aspirin were different, summed analgesic effects (SPID) showed equal efficacy and superiority over placebo (p less than 0.005). With each of the 2 doses of naproxen, SPID separation from placebo was comparable to that above (p less than 0.02 and 0.005, respectively), but analgesic dose response, though measurable, was not significant. Side effects were not significant with any of the treatments. It appears that naproxen and naproxen sodium are analgesics with efficacy equal to aspirin and may prove to be rational substitutes for currently available analgesics in some painful states in which longer pain relief would be desireable.

Adolescent↗
PubMed1979

The effects of ibuprofen, indomethacin, aspirin, naproxen, and placebo on the gastric mucosa of normal volunteers: a gastroscopic and photographic study.

The effects of various nonsteroidal antiinflammatory drugs on the gastric mucosa were endoscopically evaluated in 40 normal volunteers. Eight groups, each containing five subjects were designed: aspirin (3600 mg/d); placebo; ibuprofen (1600 mg/d); ibuprofen (2400 mg/d); indomethacin (100 mg/d); indomethacin (150 mg/d); naproxen (500 mg/d); and naproxen (750 mg/d). All volunteers took medication for seven days and gastroscopy was carried out on day one and day eight. All findings were documented by photography. Severe gastric mucosal injury occurred with aspirin (P less than 0.05), both doses of indomethacin, and the higher dose of naproxen. Lesser changes were seen with the lower dose of naproxen, both doses of ibuprofen and placebo. The higher doses of ibuprofen, indomethacin, and naproxen caused a greater degree of gastric mucosal injury, but statistical significance was achieved only with naproxen (P less than 0.01). Subjective gastrointestinal complaints generally correlated with endoscopic pathology; however, nine volunteers had evidence of severe injury to the gastric mucosa with no symptomatology. This was confined to the patients on indomethacin, naproxen, and ibuprofen. Aspirin patients all had some degree of symptomatology but to a lesser degree than expected in view of the endoscopic findings.

Adult↗
PubMed1978

Naproxen in osteoarthrosis. Double-blind crossover trial.

In this double-blind crossover trial, naproxen (750 mg/day) was compared to placebo for the treatment of osteoarthrosis of the hip and knee. Patients were randomly assigned to treatment with either naproxen or placebo for 4 weeks and then to treatment with the alternate agent for a second 4-week period. 8 out of 9 objective and subjective measurements of drug efficacy clearly differentiated naproxen from placebo at highly significant levels (P = 0.0001 to 0.0004). Patient daily check lists of osteoarthrotic symptoms also showed a statistically significant difference between naproxen and placebo therapy. Both physicians and patients, when asked to give a 'final drug preference', showed a significant preference for naproxen over placebo. In general, the incidence of side effects was low and approximately the same for both naproxen and placebo. Laboratory assessments showed little difference between groups. The trial showed naproxen to be an effective and well tolerated drug for the treatment of osteoarthrosis of the hip and knee.

Activities of Daily Living↗
PubMed1991

The efficacy and tolerability of enteric and non-enteric coated naproxen tablets: a double-blind study in patients with osteoarthritis.

A double-blind, crossover study was undertaken to compare the efficacy and tolerability of a novel enteric coated 500 mg naproxen tablet with normal release 500 mg naproxen in patients with osteoarthritis. Eighty-eight patients were randomly allocated to receive enteric coated naproxen as a single daily dose of 2 tablets at night or 1 normal release naproxen tablet twice daily for a period of 3 weeks, followed by the alternative treatment for a further period of 3 weeks. The results of patient and doctor assessments showed that both treatments were increasingly efficacious, with a significant period effect found in the measures for pain on passive movement and duration of morning stiffness. No significant treatment differences were seen in any of the measures of efficacy and tolerability, although there were more withdrawals on normal release than on enteric coated naproxen (p = 0.07). It was concluded that enteric coated naproxen given as a single 1 g dose at night and normal release 500 mg naproxen given twice daily are equally efficacious and well tolerated.

Adult↗
PubMed1975

Clinical experience with naproxen in rheumatoid arthritis.

A total of 42 patients participated in three controlled clinical trials, each of different design, to demonstrate the efficacy and safety of naproxen in the treatment of rheumatodi arthritis. First, a double-blind comparison of aspirin and naproxen was made in 24 patients. As judged by objective and subjective measurements of disease activity, naproxen was at least as effective as aspirin and the incidence of severity of side effects were less with naproxen than with aspirin. Second, the safety and efficacy of naproxen administration was followed in 42 patients for up to two years. Third, the continued efficacy of naproxen during these two years was tested by interspersing a short period of double-blind placebo administration for some patients. The observations made in this clinical study suggest that naproxen is an effective and well-tolerated drug in the long-term treatment of rheumatoid arthritis.

Adult↗
PubMed1975

An open trial of naproxen in rheumatoid arthritis patients with significant esophageal, gastric, and duodenal lesions.

To confirm the reported lack of major gastrointestinal side effects of naproxen, we gave 58 patients with active rheumatoid arthritis and significant gastrointestinal disease therapeutic doses of naproxen while closely monitoring them for signs and symptoms of gastrointestinal dysfunction. All patients underwent upper gastrointestinal x-ray examinations at the start of the trail, and, when indicated, during the course of the study. Endoscopies were also performed when indicated. Forty patients had hiatus hernia and 35 had peptic ulcer (23 duodenal ulcer and 12 gastric ulcer). Twenty-six patients had a combination of hiatus hernia with either type of peptic ulcer. After 262 patient visits over a period of 52 weeks, 35 patients remained in the study, all having had more than six months of naproxen therapy in dosages ranging from 500 to 750 mg daily. In 33 of the 35, the response to naproxen had generally been good to excellent. Only seven patients dropped out of the trial because of complaints referable to side effects. There were no major related upper gastrointestinal side effects as monitored by continuing clinical evaluation, stool occult blood, comprehensive laboratory examination, and, where indicated, upper gastrointestinal x-ray studies. Approximately 70 per cent of the patients demonstrated efficacy on long-term naproxen therapy by subjective and objective parameters. Naproxen appears to be an efficacious and remarkably safe drug in the long-term therapy of rheumatoid arthritis, even in the presence of significant upper gastrointestinal symptomatology.

Anti-Inflammatory Agents↗