Skip to main content
SpringerLink
Log in

Proquazone

A Review of its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Efficacy in Rheumatic Diseases and Pain States

  • Drug Evaluation
  • Published:
Drugs Aims and scope Submit manuscript

Summary

Synopsis

Proquazone 1 is a non-steroidal anti-inflammatory agent (NSAID) which, unlike most other NSAIDs, does not have a free acid group in its structure. It is advocated for use in rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, musculoskeletal disorders, acute inflammatory conditions and acute pain states such as dysmenorrhoea, postoperative pain and headache.

Published data in small groups of patients indicate that proquazone 300 to 900 mg/day in 3 divided doses is a possible alternative to aspirin, ibuprofen, indomethacin, and naproxen in rheumatoid arthritis, and to indomethacin and ibuprofen in ankylosing spondylitis. Similarly, proquazone 300 to 900 mg/day is as effective as aspirin, diclofenac, ibuprofen, indomethacin and naproxen in patients with osteoarthritis. Preliminary studies have confirmed the efficacy of proquazone in acute inflammatory disorders, and shown that it provides useful analgesic relief in acute pain states such as dysmenorrhoea, headache and after minor surgery. Evidence from small groups of patients with rheumatoid arthritis treated for a year or more suggests that proquazone may inhibit or arrest progression of bone erosions. However, these encouraging findings clearly need confirmation in a larger number of patients studied under well-controlled conditions.

The overall impression from clinical trials to date is that proquazone at dosages of ⩾ 900 mg/day produces a high incidence of gastrointestinal symptoms such as diarrhoea (in approximately 30% of patients). However, these effects were usually of mild to moderate severity and transient in nature and in most comparative studies the overall tolerability of proquazone was assessed as being comparable to that of other NSAIDs tested. Similarly, withdrawal from therapy due to side effects was no greater with proquazone than with other NSAIDs evaluated. Initial experience with lower dosages of proquazone (300 to 450 mg/day) suggest that efficacy is maintained and tolerability markedly improved.

Thus, at present, proquazone would seem to be as effective as other NSAIDs used in the management of rheumatoid arthritis and osteoarthritis. However, further studies are needed to fully evaluate the efficacy and tolerability of this agent, especially at the lower daily dosages currently recommended, and to clarify whether it does have significant ‘disease modifying’ potential.

Pharmacodynamic Properties

Proquazone is a non-steroidal anti-inflammatory drug (NSAID) which possesses analgesic and antipyretic properties. It has been shown to suppress inflammation in various animal models of acute and chronic disease. In carrageenin-induced paw oedema and adjuvant-induced arthritis, it appears to be equipotent with diclofenac but less active than indomethacin. In animal and human models of pain, proquazone has generally been at least as active as indomethacin and other NSAIDs in tests designed to detect ‘non-narcotic-type’ analgesia. Indeed, in man, proquazone 600mg as a single dose was found to be a superior analgesic to phenylbutazone 400mg, naproxen 500mg and diclofenac 100mg and marginally better than indomethacin 100mg. In vitro and in vivo, proquazone is a potent inhibitor of prostaglandin synthesis, comparable in activity to indomethacin and diclofenac and superior to naproxen. It also inhibits collagen-, arachidonic acid- and ADP-induced platelet aggregation.

Preliminary results in patients with rheumatoid arthritis suggest that proquazone 600 to 900 mg/day may increase the synovial fluid concentrations of complement components (C3 and C4) and decrease the concentration of immunoglobulins IgG, IgM and IgA, which are indicative of an immunological mechanism. However, in various animal models, proquazone (like indomethacin and phenylbutazone) did not influence cell-mediated or humoral immune mechanisms. Animal studies generally demonstrated that proquazone had a lower ulcerogenic potential than other NSAIDs, although in a study involving healthy volunteers proquazone 600 and 900 mg/day and aspirin 3600 mg/day produced a similar extent of faecal blood loss.

Pharmacokinetic Properties

Proquazone 100 to 900mg orally is rapidly absorbed from the gastrointestinal tract, peak plasma concentrations being attained in about 1.5 hours. Food appears to markedly increase the bioavailability of proquazone as estimated by area under the plasma concentration-time curve (AUG). Following intravenous administration of proquazone 75 or 122mg to healthy subjects the mean apparent volume of distribution was 10.8L while the volume of distribution at steady-state was 39.5L. Proquazone is extensively bound to plasma protein (> 98%).

After oral administration, proquazone is subject to extensive first-pass metabolism — between 80 and 95% of a single dose is metabolised during its first passage through the liver. Hydroxylation of the parent molecule to m-hydroxyproquazone (existing mainly in the conjugated form) seems to be the major metabolic pathway. A number of other metabolites have also been identified in man. Further research is necessary to evaluate the anti-inflammatory and analgesic activity of the metabolites. Proquazone and its metabolites are removed from the body by a combination of urinary (46 to 51%) and biliary (30 to 43%) excretion and the majority is eliminated within the first 24 hours. The total body clearance of proquazone is about 40 L/h while renal clearance is only about 0.004 L/h, highlighting the importance of hepatic extraction in the elimination of proquazone. The elimination half-life of proquazone is usually between 0.6 and 1.3 hours whereas that of its major metabolite, m-hydroxyproquazone, is much longer (6.7 to 13.4 hours).

In patients with hydrarthrosis of the knee, the synovial fluid concentrations of proquazone and its metabolites steadily increased over the first 3 hours and were still high after 4 to 7 hours. In another study, the pharmacokinetic properties of proquazone were found to be similar in children with juvenile rheumatoid arthritis to those in healthy subjects.

Therapeutic Trials

Proquazone 300 to 1200 mg/day produced clinically significant relief from pain, improved grip strength and reduced the number of affected joints in placebo-controlled trials in patients with rheumatoid arthritis. In other comparative studies, proquazone 300 to 900 mg/day was usually shown to be as efficacious as NSAIDs such as aspirin, diclofenac, ibuprofen, indomethacin and naproxen in patients with rheumatoid arthritis. Preliminary results from long term trials (⩾ 12 months) have demonstrated that proquazone 600 to 900 mg/day maintains its efficacy and may arrest the progression of bone erosions, although this encouraging finding needs to be confirmed in well-controlled trials in larger numbers of patients.

Short term studies in patients with osteoarthritis usually involved only small groups of patients, and have shown that proquazone 300 to 900 mg/day was of comparable efficacy as indomethacin 75 to 150 mg/day, aspirin 1200 to 3600 mg/day, diclofenac 75 to 150 mg/day and ibuprofen 1200 mg/day and tended to be more effective than naproxen 500 mg/day. Preliminary dose-ranging studies in patients with osteoarthritis showed that lower daily dosages of proquazone (300 to 500mg) did not result in reduced efficacy but were associated with only half the incidence of side effects compared with proquazone 900 mg/day (13.3% vs 27.1%, respectively).

Proquazone 900 mg/day was as effective as indomethacin 75 mg/day and ibuprofen 1200 mg/day in patients with ankylosing spondylitis. For treating the pain, swelling and redness associated with acute gouty arthritis, proquazone 900 mg/day was comparable to indomethacin 150 mg/day and superior to phenylbutazone 600 mg/day. In addition to conservative therapy, proquazone 600 to 1500 mg/day was as effective as naproxen 500 to 750 mg/day, diclofenac 50 to 125 mg/day, indomethacin 150 mg/day and ibuprofen 800 to 1600 mg/day in patients suffering from low back pain and sciatica. In these studies proquazone produced analgesic relief more quickly than naproxen and indomethacin, and elicited an overall better global assessment than diclofenac. Proquazone 900 to 1200 mg/day and oxyphenbutazone 300 to 400 mg/day both produced marked improvement in 70 to 80% of patients with acute traumatic injury.

The analgesic activity of proquazone in patients with pain associated with dysmenorrhoea, minor surgery or headaches was demonstrated to be significantly superior to that of placebo, oxyphenbutazone and aspirin, and equivalent to that produced by indomethacin.

Side Effects

In comparative studies proquazone 900 mg/day appeared to be of similar overall tolerability as indomethacin 150 mg/day, aspirin 1200 to 3600 mg/day and diclofenac 125 to 150 mg/day, but less well tolerated than ibuprofen 1200 mg/day and naproxen 500 mg/day. Reducing the daily dosage of proquazone to 300 to 500 mg/day in patients with rheumatoid arthritis or osteoarthritis resulted in a lower incidence of side effects without significantly altering the efficacy. Gastrointestinal symptoms, especially diarrhoea, occurred frequently with proquazone (diarrhoea in about 30% of patients usually treated with proquazone 900 mg/day); however, the symptoms were usually mild to moderate in severity and infrequently required discontinuation of therapy.

Dosage and Administration

Proquazone dosage should be adjusted to suit individual requirements. The recommended adult dosage is 300 to 450 mg/day orally or rectally in 2 or 3 divided doses. This can be increased to 900 mg/day if necessary and, in acute disease, a daily dosage of 1200mg may be administered for a maximum of 7 days. Proquazone is contraindicated in patients with active peptic ulceration or allergy to other NSAIDs. It should be used with caution in patients with a history of gastrointestinal disease, renal insufficiency or hepatic disease.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  • Akinci E, Olgun P. Eklem ici ve eklem disi romatizma olgularinda Biarison uygulamasi. Fizikt. Rehab. Dergisi 8: 81–94, 1985

    Google Scholar 

  • Allan R, Bleicher M. Biarison in the treatment of degenerative joint diseases: comparison with indomethacin and placebo. Journal of International Medical Research 5: 253–264, 1977

    PubMed  CAS  Google Scholar 

  • Arai M, Sato Y, Abe S, Ikeda M, Takakura K, et al. A study with proquazone in surgical operation. Shindan-to-Shinyaku 14: 2801–2805, 1977

    Google Scholar 

  • Bach GL. Proquazone (Biarison) treatment in rheumatoid arthritis. Egyptian Rheumatologist 2(Suppl. 1): 55–59, 1980

    Google Scholar 

  • Bach GL, Fotiades P. Treatment of rheumatoid arthritis with Biarison: results of a double-blind comparison with placebo. Medizinische Klinik 73: 1517–1522, 1978

    PubMed  CAS  Google Scholar 

  • Bach Andersen R, Halskov O. A double-blind clinical comparison of proquazone and naproxen in the treatment of patients with symptoms of lumbar nerve root compression syndrome. Scandinavian Journal of Rheumatology 7(Suppl. 21): 18–20, 1978

    Google Scholar 

  • Bachman F. Klinische Erfahrungen mit dem neuen Antirheumatikum RU 43-715 (Proquazon) bei rheumatoider Arthritis. Therapiewoche 28: 6552–6558, 1978

    Google Scholar 

  • Beck W. Ambulante Behandlung der Hüft- und Kniegelenksarthrose mit dem neuen nichtsteroidalen Antirheumatikum Biarison (Proquazon). Medizinische Welt 30: 751–753, 1979

    PubMed  CAS  Google Scholar 

  • Blau SP. A cooperative double-blind evaluation of efficacy, safety and tolerance of proquazone as compared with aspirin in patients with rheumatoid arthritis. Abstract no. 328 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Blechman W. Double-blind one year evaluation of the efficacy and safety of three dosage strengths of proquazone in rheumatoid arthritis patients. Abstract no. 329 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Bleicher M, Allan R, Craps L. Proquazone: a new approach in the treatment of gouty arthritis. Abstract no. 330 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Borel JF, Feurer C. A model for assessing effects of drugs on granulocyte migration in-vivo. In Willoughby et al. (Eds) Perspectives in inflammation: future trends and developments, pp. 69–74, MTP Press Ltd, Lancaster, 1977

    Google Scholar 

  • Borel JF, Feurer C. In-vivo effects of anti-inflammatory and other drugs on granulocyte emigration in the rabbit skin collection chamber. Journal of Pathology 124: 85–93, 1978

    Article  PubMed  CAS  Google Scholar 

  • Bragstad A. A comparative double-blind trial with proquazone and naproxen in the treatment of rheumatoid arthritis. Scandinavian Journal of Rheumatology 7(Suppl. 21): 33–35, 1978

    Article  Google Scholar 

  • Brewer EJ, Giannini EH, Baum J, Fink CW, Hanson V, et al. Proquazone (Biarsan®) in the treatment of juvenile rheumatoid arthritis. Journal of Rheumatology 9: 135–139, 1982

    PubMed  CAS  Google Scholar 

  • Broil H, Tausch G. Proquazone in the treatment of gout and rheumatoid arthritis. International Journal of Tissue Reactions 1: 137–141, 1979

    Google Scholar 

  • Brune K, Gubler H, Schweitzer A. Autoradiographic methods for the evaluation of ulcerogenic effects of anti-inflammatory drugs. Pharmacology and Therapeutics 5: 199–207, 1979

    Article  CAS  Google Scholar 

  • Capetola RJ, Shriver DA, Rosenthale ME. Suprofen, a new peripheral analgesic. Journal of Pharmacology and Experimental Therapeutics 214: 16–23, 1980

    PubMed  CAS  Google Scholar 

  • Cohen A, Garber H. Gastrointestinal microbleeding: a comparison of proquazone, aspirin, and placebo in adult male volunteers. Clinical Pharmacology and Therapeutics 23: 111, 1978

    Google Scholar 

  • De Moor M, Ooghe R. Etude clinique concernant un nouvel antirhumatismal: proquazone. Ars Medica 9: 1106–1110, 1980

    Google Scholar 

  • Del Vallado PF, Paulino TJ, Gigon BJ. Estudio comparativo, doble ciego, de la accion anti-inflammatoria y de la tolerancia de RU 43 715 y de fenilbutazone en pacientes con artritis gotosa aguda. Abstract presented at the 9th European Congress of Rheumatology, Wiesbaden, 1979

  • DiSerio FJ, Friedman AP, Pamo J, Singer JM. Proquazone for tension headache — a multicenter trial. Headache 25: 127–133, 1985a

    Article  PubMed  CAS  Google Scholar 

  • DiSerio FJ, Singer JM, Friedman AP, Pamo J. An evaluation of proquazone in the acute treatment of migraine headache. Cephalalgia 5(Suppl. 3): 146–147, 1985b

    Google Scholar 

  • Dittrich W. Behandlung degenerativer Gelenkerkrankungen mit einem neuen nichtsteroidalen Antirheumatikum. Therapiewoche 29: 7539–7544, 1979

    Google Scholar 

  • El-Badawy SA. Biarison® 600mg versus Biarison® 900mg and indomethacin 150mg daily in osteoarthritis of the knee-joint. Egyptian Rheumatologist 2(Suppl. 1): 41–46, 1980

    Google Scholar 

  • El Hadidi T, El Ghobary A, El Nagdy L, Sami M. “Studies on proquazone”: a double-blind study comparing proquazone with indomethacin in patients with rheumatoid arthritis. Egyptian Rheumatologist 2(Suppl. 1): 25–27, 1980

    Google Scholar 

  • Forbes JA, White RW, White EH, Hughes MK. An evaluation of the analgesic efficacy of proquazone and aspirin in postoperative dental pain. Journal of Clinical Pharmacology 20: 465–474, 1980

    PubMed  CAS  Google Scholar 

  • Fries JF, McShane D, Calin A, Young D. Evaluation of the effects of Biarison (proquazone) on bone erosions in rheumatoid arthritis. 15th International Congress of Rheumatology, pp. 90–100, Paris, 21–27 Jun, 1981

  • Gabka J. Vergleichende klinisch-experimentalle Untersuchungen zur Frage der analgetischen Wirksamkeit von Biarison®. Therapiewoche 29: 3903–3908, 1979

    Google Scholar 

  • Ghimicescu R. Wirkung und Verträuglichkeit von Biarison® (Proquazon) bei chronischer Polyarthritis. Münchener Medizinische Wochenschrift 120: 190–194, 1978a

    Google Scholar 

  • Ghimicescu R. Erfahrungen mit dem neuen Antiphlogistikum Biarison bei der Behandlung der Knie- und Hüftgelenksarthrosen. Medizinische Welt 29: 1768–1771, 1978b

    PubMed  CAS  Google Scholar 

  • Gonzalez-Pares EN, De LaCruz S. Double-blind one year evaluation of the efficacy and safety of proquazone (Sall 43-715) in rheumatoid arthritis patients receiving concomitant antiinflammatory medication. Abstract no. 337 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Grieder A, Vuille R, Baggiolini M. Effects of anti-inflammatory compounds on the RNA synthesis of macrophages activated in vitro. Basic Applied Histochemistry 24: 332, 1980

    Google Scholar 

  • Gubler HU, Baggiolini M. Pharmacological properties of proquazone. Scandinavian Journal of Rheumatology 7(Suppl. 21): 8–11, 1978

    Article  Google Scholar 

  • Gueguen Y. Summary of clinical trials with Biarison. Egyptian Rheumatologist 2(Suppl. 1): 13–24, 1980

    Google Scholar 

  • Gueguen Y. Fresh cases of rheumatoid arthritis: one year study, Briarison versus indomethacine. 15th International Congress of Rheumatology, pp. 59–67, Paris, Jun 21–27, 1981

  • Habashy A. Assessment of the analgesic and anti-inflammatory effects of proquazone and oxyphenbutazone in post-operative wounds, by a double-blind study. Egyptian Rheumatologist 2(Suppl. 1): 47–53, 1980

    Google Scholar 

  • Halskov O, Bach Andersen R. A double-blind clinical comparison of Biarison and naproxen in treatment of patients with symptoms of lumbar nerve root compression syndrome. 9th European Congress Rheumatology, Wiesbaden, 2–8 Sep, 1979. Abstract no. D12, p.245, 1980

  • Hamawi A. A double-blind trial of proquazone and indomethacin in acute low back pain with radiation. Egyptian Rheumatologist 2(Suppl. 1): 29–33, 1980

    Google Scholar 

  • Hardtmann GE, Huegi B, Koletar G, Kroin S, Ott H. Synthesis and antiinflammatory activity of some 1-alkyl-4-phenylpyrido [2,3-d]pyrimidin-2(1H)-ones. Journal of Medicinal Chemistry 17: 636–639, 1974

    Article  PubMed  CAS  Google Scholar 

  • Hinderling PH, Roos A. Pharmacokinetics of the antirheumatic proquazone in healthy humans. Journal of Pharmaceutical Sciences 73: 332–340, 1984

    Article  PubMed  CAS  Google Scholar 

  • Holmes IB. A comparison of the effect of proquazone, a new nonsteroidal antiinflammatory compound, and acetylsalicylic acid on blood platelet function in vitro and in vivo. Archives Internationales de Pharmacodynamie et de Thérapie 228: 136–152, 1977

    PubMed  CAS  Google Scholar 

  • Houlihan WJ, Cook G, Van Bochoven R, Perrine J, Takesue EI, et al. Antiinflammatory properties of 8-aryl-5-isopropyl-2H-l, 3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones. Journal of Medicinal Chemistry 25: 1110–1113, 1982

    Article  PubMed  CAS  Google Scholar 

  • Kangasaho M, Vapaatalo H. Flumizole, nictindole and proquazone — potent antiaggregatory agents. Abstract no. 1919 presented at the 8th International Congress of Pharmacology, Tokyo, 19–24 Jul, 1981

  • Kantor TG. A double-blind evaluation of the efficacy and safety of proquazone (SaH 43-715) compared to aspirin in patients with osteoarthritis. Abstract no. 341 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Karakaya M. A double-blind comparison of a new anti-inflammatory substance, proquazone, with indomethacin and placebo in osteoarthritis of the knee joint. Current Therapeutic Research 22: 127–133, 1977

    Google Scholar 

  • Klockars M. Does proquazon interfere with the immunodiffusion assay of immunoglobulins or directly affect the structure of immunoglobulins. Abstract no. 44. Scandinavian Journal of Rheumatology Suppl. 33: 21, 1980

    Google Scholar 

  • Kokino S. Akut lomber hemi diskal olgularinin medikal tedavisinde biarisonun yeri. Acta ortop. — traum. Turcica 19: 90–100, 1985

    Google Scholar 

  • Kupfrian G, Zöller A. Biarison bei Gon- und Coxarthrose: ergenbnisse eines Doppelblindvergleiches mit Indometacin. Zeitschrift für Allgemeinmedizin 55: 1891–1896, 1979

    PubMed  CAS  Google Scholar 

  • Lempiäuinen M, Mäukeläu A-L. Determination of proquazone and its m-hydroxy metabolite by high-performance liquid chromatography. Journal of Chromatography 341: 105–113, 1985

    Article  Google Scholar 

  • Lepistö PV. Long-term treatment of osteoarthritis of the hip with proquazone. Pharmatherapeutica 2: 110–113, 1978

    Google Scholar 

  • Mäukäuräuinen L, Ylikorkala O. Menstrual blood loss in dysmenorrhoea: effects of proquazone and indomethacin. British Journal of Obstetrics and Gynaecology 90: 570–572, 1983

    Article  Google Scholar 

  • Mertz DP. Wirkung und Verträuglichkeit von Proquazon bei Spondylitis ankylosans. Therapiewoche 31: 3274–3286, 1981

    Google Scholar 

  • Milne GM, Twomey TM. The analgesic properties of Piroxicam in animals and correlation with experimentally determined plasma levels. Agents and Actions 10: 31–37, 1980

    Article  PubMed  CAS  Google Scholar 

  • Mortier G, De Neve M. Effet et tolerance de trois posologies d’un nouvel antirhumatismal. Ars Medica 9: 911–916, 1980

    Google Scholar 

  • Naghma-e-Rehan. Proquazone (Biarison) in the treatment of osteo-arthritis. Clinical Trials Journal 18: 24–29, 1981

    Google Scholar 

  • Nissiläu M. Treatment of early seropositive rheumatoid arthritis: a comparison between gold and Biarison. Presented at the 15th International Congress of Rheumatology, Paris, 21–27 Jun, 1981

  • Nissiläu M, Kajander A. Proquazone (Biarison®) and indomethacin (Indocid®) in the treatment of ankylosing spondylitis. Scandinavian Journal of Rheumatology 7(Suppl. 21): 36–39, 1978

    Article  Google Scholar 

  • Ohnhaus EE. The effect of antacid and food on the absorption of proquazone (Biarison) in man. International Journal of Clinical Pharmacology, Therapy and Toxicology 18: 136–139, 1980

    CAS  Google Scholar 

  • Ohnhaus EE, Beveridge T. Mehtodischer Beitrag zur Messung der Plättchenaggregation unter kontrollierten Bedingungen. Schweizerische Medizinische Wochenschrift 106: 1365–1366, 1976

    PubMed  CAS  Google Scholar 

  • Ott H. 2(1H)-quinazolinones as novel non-acidic anti-inflammatory agents. Scandinavian Journal of Rheumatology 7(Suppl. 21): 5–7, 1978

    Article  Google Scholar 

  • Ott H, Meier J. The distribution of proquazone and three of its metabolites in serum and synovial fluid. Scandinavian Journal of Rheumatology 7(Suppl. 21): 12–14, 1978

    Google Scholar 

  • Oyemade GAA. A double-blind comparison of proquazone (Biarison®) with indomethacin in patients with musculo-skeletal diseases. Current Therapeutic Research 29: 785–789, 1981

    Google Scholar 

  • Puranen J, Rönty H. A new anti-inflammatory drug, proquazone, and ibuprofen in the treatment of degenerative joint disease of the knee (gonarthrosis). Scandinavian Journal of Rheumatology 7(Suppl. 21): 21–24, 1978

    Google Scholar 

  • Radi I. Low dose of Biarison in osteoarthritis. Presented at the 15th International Congress of Rheumatology, Paris, 21–27 Jun, 1981

  • Radi I, Ott H, Vischer T, Gueguen Y. Proquazone in the treatment of acute low back pain and sciatica. Abstract no. 348 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Rainsford KD. Comparison of the gastric ulcerogenic activity of new non-steroid anti-inflammatory drugs in stressed rats. British Journal of Pharmacology 73: 226P, 1981

    Google Scholar 

  • Roos A, Hinderling PH. Protein binding and erythrocyte partitioning of the antirheumatic proquazone. Journal of Pharmaceutical Sciences 70: 252–257, 1981

    Article  PubMed  CAS  Google Scholar 

  • Rozos J, Tsachalos P, Sfikakis P. Proquazone and naproxen in the treatment of osteoarthritis. Abstract no. 350 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Ruotsi A, Skrifvars B. A long-term double-blind comparative study on proquazone (Biarison®) and ibuprofen in rheumatoid arthritis. Scandinavian Journal of Rheumatology 7(Suppl. 21): 28–32, 1978

    Article  Google Scholar 

  • Ruotsi A, Vainio U. Treatment of acute gouty arthritis with proquazone and indomethacin. Scandinavian Journal of Rheumatology Suppl. 21: 15–17, 1978

    Article  Google Scholar 

  • Schattenkirchner M, Fryda-Kaurimsky Z. A controlled trial with proquazone in the treatment of rheumatoid arthritis. Current Therapeutic Research 24: 905–911, 1978

    Google Scholar 

  • Schweitzer A, Brune K. Salicylic acid and proquazone: the differences in absorption and biodistribution explain their different profile of side-effects. In Willoughby et al. (Eds) Perspectives in inflammation, pp. 353–360, MTP Press Ltd, Lancaster (UK), 1977

    Chapter  Google Scholar 

  • Serry MM. Proquazone (‘Biarison’) in osteoarthritis of the knee: a double-blind, dose comparison trial. Pharmatherapeutica 2: 323–329, 1980

    PubMed  CAS  Google Scholar 

  • Sfikakis P, Tsachalos P. Zur Behandlung der Kniegelenkarthrose mit Proquazon. Therapeutische Umschau 34: 730–734, 1977

    PubMed  CAS  Google Scholar 

  • Silvola J, Kangasaho M, Tokola O, Vapaatalo H. Effects of nonsteroidal anti-inflammatory drugs on rat gastric mucosal phosphodiesterase activity. Agents and Actions 12: 516–520, 1982

    Article  PubMed  CAS  Google Scholar 

  • Simson J, Double-blind eight week evaluation and comparison of efficacy and safety of proquazone (SaH 43-715), indomethacin and placebo in patients with rheumatoid arthritis. Abstract no. 352 presented at the 14th International Congress of Rheumatology, San Francisco, 26 Jun–1 Jul, 1977

  • Singer F, Graber J, Wemer-Breitenecker L, Nirnberger G. Assessment of the efficacy of proquazone (Biarison®) compared with that of indomethacin in the treatment of gonarthrosis. Clinical Trials Journal 19: 368–376, 1982

    Google Scholar 

  • Skrifvars B. Influence of proquazone (Biarison®) on the levels of complement components (C3 and C4) in synovial fluid and on IgM in serum in patients with active rheumatoid arthritis. Scandinavian Journal of Rheumatology 7(Suppl. 21): 40–42, 1978

    Article  Google Scholar 

  • Skrifvars B. Proquazone in long term treatment of patients with early rheumatoid arthritis. Presented at the 15th International Congress of Rheumatology, Paris, 21–27 Jun, 1981

  • Skrifvars B, Nissiläu M. Immunological effects of Biarison® in the treatment of rheumatoid arthritis and systemic lupus erythematosus. Scandinavian Journal of Rheumatology 9: 33–38, 1980

    PubMed  CAS  Google Scholar 

  • Sperling IL, Lepp BA. Proquazone (SaH 43-715), a controlled clinical trial with several doses of a new anti-arthritic compound. Abstract. International Congress Series 502: 1402, 1980

    Google Scholar 

  • Takesue EI, Perrine JW, Trapóld JH. The anti-inflammatory profile of proquazone. Archives Internationale de Pharmacodynamie et de Thérapie 221: 122–131, 1976

    CAS  Google Scholar 

  • Tschirdewahn B. Behandlung vertebraler und vertebragener Syndrome mit Proquazon. Medizinische Weh 31: 1633–1635, 1980

    CAS  Google Scholar 

  • Tsurumi K, Kyuki K, Yasuda K, Fujimura H. Anti-inflammatory and analgesic activities of metabolites of l-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone (proquazone). Pharmacometrics 16: 125–129, 1978a

    CAS  Google Scholar 

  • Tsurumi K, Nakano M, Hasegawa J, Fujimura H. General pharmacological actions of l-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone (proquazone). Pharmacometrics 16: 115–123, 1978b

    CAS  Google Scholar 

  • Tsurumi K, Nakayama T, Togawa Y, Fujimura H. Anti-inflammatory, analgesic and antipyretic properties of 1-isopropyl-4-phenyl-7-methy1-2(1H)-quinazolinone (proquazone). Pharmacometrics 16: 99–113, 1978c

    CAS  Google Scholar 

  • Ulrych I. Zur Frage der Dosierung von nichtsteroidhaltigen neueren antiphlogistisch-analgetisch wirkenden Präuparaten. Praxis 68: 1292–1293, 1979

    PubMed  CAS  Google Scholar 

  • Vainio JT, Lepistö PV. A long-term comparison of proquazone and naproxen in the treatment of osteoarthritis of the hip. Scandinavian Journal of Rheumatology 7(Suppl. 21): 25–27, 1978

    Article  Google Scholar 

  • Velcovsky H-G, Bretzel RG, Michels H, Federlin K. Behandlung von Patienten mit rheumatoider Arthritis mit einem neuen nicht-steroidalen Antirheumatikum (RU 43-715). Therapiewoche 29: 7103–7117, 1979

    Google Scholar 

  • von Graffenried B, Hill RC, Nüesch E. Headache as a model for assessing mild analgesic drugs. Journal of Clinical Pharmacology 20: 131–144, 1980

    Google Scholar 

  • von Graffenried B, Nüesch E. Non-migrainous headache for the evaluation of oral analgesics. British Journal of Clinical Pharmacology 10 (Suppl.): 225S–231S, 1980

    Article  Google Scholar 

  • Weiler H, Mayer C, Frölich J, Pesker BM. Effect of proquazone and indomethacin on gastric prostaglandin synthesis in vitro and in vivo. Agents and Actions 15: 93–95, 1984

    Article  CAS  Google Scholar 

  • Zucker MB. Proquazone (Sandoz 43-715), an unusually potent inhibitor of the platelet release reaction of malondialdehyde formation. Proceedings of the Society for Experimental Biology and Medicine 156: 209–212, 1977

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. ADIS Drug Information Services, Centorian Drive, Private Bag, Mairangi Bay, Auckland 10, New Zealand

    Stephen P. Clissold & Rosemary Beresford

Authors
  1. Stephen P. Clissold
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Rosemary Beresford
    View author publications

    You can also search for this author in PubMed Google Scholar

Additional information

Various sections of the manuscript reviewed by: K. Brune, Lehrstuhl für Pharmakologie und Toxikologie, Der Universitäut Erlangen-Nürnberg, Erlangen, W. Germany; F.D. Hart, Harley Street, London, England; S.H. Roth, Arthritis Center, St Luke’s Hospital Medical Center, Phoenix, Arizona, USA; P.A. Simkin, Division of Rheumatology, Department of Medicine, University of Washington, Seattle, Washington, USA; B. Skrifvars, Department of Rheumatology, University Hospital, Umeå, Sweden; K. Tsurumi, Department of Pharmacology, Gifu University School of Medicine, Gifu, Japan; H. Yamamoto, Wakayama Medical College, Wakayama, Japan.

‘Biarsan’, ‘Biarison’ (Sandoz).

Rights and permissions

Reprints and permissions

About this article

Cite this article

Clissold, S.P., Beresford, R. Proquazone. Drugs 33, 478–502 (1987). https://doi.org/10.2165/00003495-198733050-00004

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-198733050-00004

Keywords

Search

Navigation