Differential suppression of menstrual fluid prostaglandin F2a, prostaglandin E2, 6-keto prostaglandin F1a and thromboxane B2 by suprofen in women with primary dysmenorrhea.

Eleven women with primary dysmenorrhea completed a randomized, double-blind, placebo-controlled, three-way cross-over study comparing 200 and 400mg suprofen. Menstrual fluid volume did not change. Mean+/-S.E.M. menstrual fluid PGF2a was significantly suppressed from 18.9+/-1.9 microg (placebo) to 10.9+/-1.7 and 9.3+/-2.1 microg with 200 and 400 mg suprofen, respectively (p=<0.005). PGE2 dropped from 7.8+/-0.9 to 4.6+/-0.8 and 4.6+/-1.1 microg (p=<0.05) and TxB2 from 17.5+/-4.3 to 7.5+/-2.9 and 3.6+/-1.3 microg (p=<0.01), respectively. 6-Keto PGF1a was significantly suppressed (2.7+/-0.4 to 1.9+/-0.5 microg, p=<0.025) with only 400 mg suprofen. Six subjects rated placebo poor and five fair to very good. In contrast, nine rated suprofen excellent to fair while two rated poor. Thus, suprofen was clinically effective but the differential suppression of prostanoids favors 200mg which spares 6-keto PGF1a.

Non-steroidal anti-inflammatory drug and endotoxin induced uveitis.

Suprofen eye drop was instilled into one eye of 10 pigmented rabbits and then anterior uveitis was induced by intraperitoneal injection of endotoxin of Shigella flexneri serotype 1A to evaluate the effects of non-steroidal anti-inflammatory drug on endotoxin induced uveitis. The pupillary diameters were measured, and aqueous cell and flare gradings were recorded in 20 eyes of 10 rabbits for one week at an interval of 12 hours for the first 24 hours and then every 24 hours for a week. A difference between the treated and control groups were investigated. All the above parameters showed greatest changes at 12 or 24 hours after injection and became normal by one week. The two groups demonstrated statistically significant difference at 12 hours, day 1 and day 2 as for pupillary diameter, at day 1 and day 2 as for cell and at 12 hours and day 1 as for flare. Thus, it can be concluded that prostaglandins play a role in miosis, in the appearance of inflammatory cells and flare in endotoxin induced uveitis and the topical administration of non-steroidal anti-inflammatory drug can alleviate signs of anterior uveitis. Specific relationship between leukotriene B4 and aqueous cell was not demonstrated.

Antagonists and inhibitors of lipid mediators in experimental inflammation of the cornea.

In experimental immunogenic keratitis, provoked in rabbits by intracorneal injection of 20 microliters of human serum albumin (HSA), various anti-inflammatory agents were studied in their effects on corneal edema, neovascularisation and leukocyte infiltration. Prophylactic treatment with a corticosteroid completely prevented the occurrence of keratitis. Nonsteroidal anti-inflammatory drugs such as a cyclooxygenase inhibitor partly prevented neovascularisation and corneal edema, a lipoxygenase inhibitor, a leukotriene antagonist or platelet-activating factor (PAF)-antagonist BN 52021 partially prevented mainly leukocyte infiltration. Prophylactic topical treatment with the poly-unsaturated fatty acids eicosapentaenoic acid and columbinic acid or a dietary supplement with fish oil showed less symptoms of keratitis in all respects.

Non-steroidal anti-inflammatory drug and endotoxin induced uveitis

Suprofen eye drop was instilled into one eye of 10 pigmented rabbits and then anterior uveitis was induced by intraperitoneal injection of endotoxin of Shigella flexneri serotype 1A to evaluate the effects of non-steroidal anti-inflammatory drug on endotoxin induced uveitis. The pupillary diameters were measured, and aqueous cell and flare gradings were recorded in 20 eyes of 10 rabbits for one week at an interval of 12 hours for the first 24 hours and then every 24 hours for a week. A difference between the treated and control groups were investigated. All the above parameters showed greatest changes at 12 or 24 hours after injection and became normal by one week. The two groups demonstrated statistically significant difference at 12 hours, day 1 and day 2 as for pupillary diameter, at day 1 and day 2 as for cell and at 12 hours and day 1 as for flare. Thus, it can be concluded that prostaglandins play a role in miosis, in the appearance of inflammatory cells and flare in endotoxin induced uveitis and the topical administration of non-steroidal anti-inflammatory drug can alleviate signs of anterior uveitis. Specific relationship between leukotriene B4 and aqueous cell was not demonstrated.

Suprofen: its usefulness in the control of pain following surgical removal of impacted wisdom tooth.

The results of the present investigation have shown the usefulness of suprofen in the control of pain following surgical removal of impacted wisdom tooth. The regime of 200 mg. q.d.s. orally, was shown to be satisfactory in the control of postoperative pain. Pain was rapidly controlled by the 1st hour after ingestion and subsequently maintained at a low profile until is was completely abolished by the 8th hour of the postoperative period.

Non-steroidal anti-inflammatory drugs as the first step in cancer pain therapy: double-blind, within-patient study comparing nine drugs.

The efficacy and tolerability of acetylsalicylic acid, paracetamol, diclofenac, ibuprofen, indomethacin, pirprofen, sulindac, naproxen and suprofen were compared in the treatment of cancer pain. In a double-blind, within-patient randomized study, each drug was given for 1 week to eight patients and for another week to a further eight patients. A total of 65 patients were effectively treated; only 48 completed week 1 and 41 completed week 2. Naproxen, diclofenac and indomethacin were highly effective in pain relief (tested by means of a 100 mm visual analogue scale) and were relatively well tolerated. It is concluded that these non-steroidal anti-inflammatory drugs can be considered as first choice in the treatment of cancer pain.

[The radioprotective action of suprofen]. / Radiozashchitnoe deistvie suprofena.

Suprofen is a new non-steroidal anti-inflammatory drug administered intragastrically 90 min before roentgen irradiation in a dose of 20 mg/kg and then daily for 10 days in a dose of 10 mg/kg exerts the radioprotective effect evaluated according to a 30-day survival rate and an average life expectancy of the deceased animals as well as according to a decrease of postirradiation leukopenia incidence. A single administration of suprofen following roentgen irradiation exerts no radioprotective effect. Suprofen was found to enhance the radioprotective action of cysteamine.

Suprofen treatment of contact lens-associated giant papillary conjunctivitis.

This multicenter study of patients with contact lens-associated giant papillary conjunctivitis (GPC) was a randomized, double-masked comparison of a 1.0% suprofen solution versus the suprofen vehicle solution (placebo). Patients were given two drops of medication four times daily for up to 28 days and were clinically examined on days 0, 2, 7, 14, 21, and 28. The physicians' clinical judgments of the patients' responses to therapy significantly favored suprofen over placebo at day 21 (P = 0.02), while strongly favoring suprofen at day 14 (P = 0.057) and at day 28 (P = 0.067). The patients' opinions of their response to therapy significantly favored suprofen on day 14 (P = 0.03); a trend for suprofen was evident on day 28 (P = 0.1). Treatment with suprofen led to a greater overall reduction in ocular signs and symptoms than with placebo. Strong trends approaching statistically significant levels were found for reductions in the principal ocular sign, papillae, at day 28 (P = 0.068) and in mucus strands at days 14 and 28 (P = 0.09), which also favored suprofen.

A clinical trial in oral surgery of the analgesic efficacy of a suprofen/codeine combination.

Suprofen as well as codeine have been shown to be effective analgesics. In this study, a 200-mg suprofen/60-mg codeine dose is scored for analgesic efficacy and safety compared to suprofen (200 mg), codeine (60 mg), and placebo. One hundred sixty-five healthy, adult patients were asked to rate degree of pain experienced over a six-hour period after medication. The combination treatment was found to offer maximum pain relief. Dentists should be aware that flank pain and renal function abnormalities have been reported in postmarketing surveillance.

Comparación de la eficacia analgésica entre suprofén y diclofenac sódico, ambos por vía intramuscular, en pacientes con dolor dental agudo / Comparison of analgesic efficacy of suprofen and sodium dichlofenac, both by intramuscular way, in acute toothache

Mediante un estudio simple ciego se valoró la potencia analgésica y tolerancia de 400 mg de suprofén y 75 mg de diclofenac sódico, administrado por vía intramuscular a cuarenta pacientes con dolor dental agudo. Suprofén fue estadísticamente superior las primeras cuatro a seis horas observación, en los parámetros de disminución de la intensidad y alivio al dolor, corroborándose esta situación con la valoración global realizada por investigador y paciente, donde se ve un 95% de resultados buenos/excelentes. Se concluyó que suprofén es un medicamento seguro y eficaz en pacientes con dolor dental agudo

Suprofen versus paracetamol after oral surgery.

A randomized double-blind trial was performed to evaluate efficacy and tolerability of suprofen 200 mg (Suprocil) in comparison to paracetamol 500 mg after surgical extraction of a wisdom tooth. The study lasted 4 days per patient at the longest. Pain intensity and pain relief were evaluated by the patients using a visual analog scale. A total of 59 patients took part in the study; of these, 30 were on suprofen and 29 on paracetamol. The 30-min pain relief with paracetamol was superior to that obtained with suprofen. Roughly, the 90-min pain relief scores were somewhat higher for suprofen than for paracetamol. However, none of the differences were statistically significant. No significant difference was seen between the 2 treatment groups with respect to the frequency of the number of capsules taken per day. Broadly, the efficacy was good or excellent in 18 patients in each group. With suprofen, there were 8 moderate results and 4 insufficient ones. With paracetamol, 6 results were moderate and 5 insufficient or worse. No significant differences between the 2 treatments was seen. Tolerability was rated good by all but 1 patient in each treatment group; with suprofen, 1 result was moderate, while with paracetamol, 1 result was poor. Adverse reactions occurred in 3 patients on suprofen and in 2 patients on paracetamol, though these reactions could not be related to the use of the drug itself.

Action of a prostaglandin synthetase inhibitor on IUD associated uterine bleeding.

The Authors treated twenty-eight women using IUD, who suffered from increased menstrual blood loss and pelvic pain, with a prostaglandin synthetase inhibitor, Suprofen, in an attempt to reduce their symptomatology, in a double blind crossover study. The drug produced an important reduction of the menstrual blood loss and pains. These observations suggest that prostaglandins are involved in the etiology of excessive menstrual blood loss and pains, and that prostaglandin inhibitors may be useful for reducing these symptoms.

PIP: Suprofen (Suprol-Cilag S.p.A.), a prostaglandin synthetase inhibitor, was tested in a double-blind crossover design on 28 women whose IUDs caused them pain or increased menstrual bleeding. The subjects had worn either a Gravigard (18 women) or a Copper T (10) for 6 to 10 months. Each subject was observed for the first month, and took either placebo or Suprofen during the next menses, followed by the alternative for the third cycle. They took 20 mg Suprofen 4 times daily, at the first sign of bleeding and or pain, then 3 times daily thereafter, for the duration of symptoms or up to 7 days. Before treatment, 71% had severe bleeding, 18% had moderate bleeding and 11% had slightly increased bleeding. During Suprofen, 43% obtained a strong decrease in menstrual blood loss, 36% had a moderate decrease and 7% had a slight decrease. Placebo decreased bleeding moderately in 2. Pain was moderate to intense in 26 women and slight or none in 2 before treatment. With Suprofen, pain decreased moderately or greatly in 23 and slightly or not at all in 5 women. Placebo improved pain moderately in 1 subject. Reported side effects of the drug were stomach cramps in 1 and nausea and headaches in 2 women. In this study, when the subjects were categorized by degree of symptoms, the prostaglandin antagonist was more effective in those complaining of more severe bleeding and pain.

Effects of suprofen on renal function in patients with rheumatoid arthritis.

Suprofen is a new potent analgesic with antiinflammatory properties that appears to inhibit prostaglandin synthetase in a tissue-selective manner, having relatively little effect on the kidneys of experimental animals. The effects were studied of one week of treatment of rheumatoid arthritis patients with suprofen or ibuprofen on Na+ and K+ excretion, creatinine clearance, urinary enzymes that are markers for tubular damage, and urinary prostaglandins such as PGE2 and 6-keto PGF1 alpha (a stable metabolite of prostacyclin). Neither compound caused changes in renal function related to the week of treatment, but significant decreases in prostaglandins were observed: this change was fully reversible after discontinuation of the drug.

Flupirtine: the first Italian experience.

This paper reports the results of five single-dose short-term, controlled clinical trials conducted in Italy with the structurally new analgesic flupirtine. A total of 200 patients were enrolled in the trials. One hundred and two patients received flupirtine, 61 were treated with reference drugs (suprofen and paracetamol) and 37 were on placebo. Analgesic efficacy was evaluated in post-episiotomy pain (2 studies and 70 patients), post-traumatic pain (2 studies and 100 patients) and in 30 post-operative patients. Flupirtine was given as a single dose of 100 mg (one capsule) or as a single day's treatment (100 mg t.i.d.). For suprofen and paracetamol, oral doses of 200 mg and 500 mg respectively were used. A semi-quantitative four- or five-point scale or a linear analogue scale was used to determine the degree of pain. In post-episiotomy pain, the time required to achieve a reduction of 50% of the initial pain was also used. In post-operative pain, flupirtine induced a 69% reduction in the pain score 6 hours after administration, compared with 26% in the placebo group. In post-episiotomy pain and pain due to sport injury, flupirtine showed greater efficacy as judged by the number of patients reporting good and acceptable pain relief, and a faster onset of pain relief than suprofen (episiotomy) or paracetamol plus massage (sport injury). The adverse reaction, nausea, was complained of once only during treatment with flupirtine.

The analgesic efficacy of suprofen in periodontal and oral surgical pain.

Suprofen is a new, orally effective nonsteroidal antiinflammatory analgesic of the propionic acid chemical class. Three separate single-dose studies were performed to evaluate the efficacy of suprofen in acute pain associated with periodontal surgery and removal of impacted third molars. Study medications were: A--suprofen 200 mg, codeine 60 mg, propoxyphene HCl 65 mg, and placebo; B--suprofen 400 mg and 200 mg, aspirin 650 mg, and placebo; C--suprofen 400 mg and 200 mg, aspirin 650 mg with codeine 60 mg, aspirin 650 mg alone, and placebo. Analgesic and side effect data were collected over a 6-hour period after patients medicated for moderate to severe pain. All studies were randomized, double-blinded, and parallel-group in design. Suprofen was significantly more effective than codeine 60 mg, propoxyphene HCl 65 mg, and aspirin 650 mg. Suprofen 400 mg appeared to be clinically more effective than the aspirin-codeine combination and the difference was statistically significant for most of the analgesic variables. Of the 224 patients who received suprofen in the 3 studies, 16 reported drowsiness and 1 reported constipation.