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pirazolac (pirazolac)

✓ Approved

Mediolanum Farmaceutici Spa · Small Molecule · Small Molecule

What is pirazolac?

pirazolac is a small molecule developed by Mediolanum Farmaceutici Spa. It is approved for therapeutic indications via unknown.

Drug Profile

Brand Namespirazolac
CompanyMediolanum Farmaceutici Spa
Drug ClassSmall Molecule
RouteUnknown
StatusApproved
Sources: ClinicalTrials.gov, Mediolanum Farmaceutici Spa

Therapeutic Indications

pirazolac is developed for 3 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Musculoskeletal and connective tissue disordersArthritisPreclinical
Musculoskeletal and connective tissue disordersMusculoskeletal painPreclinical
Musculoskeletal and connective tissue disordersRheumatoid arthritisPreclinical

Related Research Articles

PubMedDrugs under experimental and clinical research1990-01-01

Effect of pirazolac on prostanoid synthesis by human gastric mucosa in vitro.

Tavares I A IA, Bennett A A

Pirazolac concentration-relatedly inhibited the accumulation of prostanoids in incubates of human gastric mucosa, but this inhibition was less than that by indomethacin and other commonly used non-steroidal anti-inflammatory drugs. This difference may explain the claim that pirazolac is less damaging to the stomach.

PMID 2115830
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PubMedDrugs under experimental and clinical research1990-01-01

Multicentre double-blind study of the efficacy, safety and tolerance of pirazolac compared with sulindac in patients with rheumatoid arthritis.

Numo R R

Of the 160 patients (80 pirazolac/80 sulindac) who entered the study through 14 investigators, three-quarters completed a 12-weeks therapy and three-fifths completed the entire 24-weeks therapy. In the pirazolac group 15% of the patients and in the sulindac group 11% dropped out from the study due to adverse clinical experience. The drop-out rates due to unsatisfactory therapeutic response were respectively 15% and 16% in the pirazolac and the sulindac groups. Both treatment groups showed significant improvement from baseline for all parameters except for the erythrocyte sedimentation rate at weeks 4, 8, 12 and 16 for the sulindac group and weeks 4 and 8 for the pirazolac group. The two treatment groups were comparable as to effectiveness; however, the improvement rates in 36 out of 41 efficacy measurements based on the definition of clinically relevant changes in relation to baseline were estimated to be superior for the group under pirazolac therapy. The rate of improvement for the American Rheumatism Association functional class at the end of the study was 23% in the pirazolac group and 9% in the sulindac group (p less than 0.05). Of the patients in the pirazolac and sulindac groups, 45% and 44% respectively reported no adverse effects at all throughout the whole 24-weeks study. The rates of patients reporting at least one adverse reaction in a body system were not different between the two groups. An exception was the body as a whole where ten patients (12.5%) in the sulindac group and only two (2.5%) in the pirazolac group reported adverse reactions (p = 0.03). No differences occurred between the two treatment groups with regards to intensity, causality or the number of occurrences of adverse clinical experiences. One death in the sulindac treatment group was reported during the study. In both treatment groups, alterations in laboratory tests were minor or negligible or associated with abnormal pre-treatment values and, generally speaking, without any clinical relevance. There were some patients, who had increases from baseline in alkaline phosphate in both treatment groups. However, these were usually transient, occasionally complemented by a slight increase of serum glutamic oxaloacetic acid transaminase.

PMID 2198156
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PubMedDrugs under experimental and clinical research1990-01-01

Neutrophil functional and arachidonic acid metabolic correlates and clinical disease activity in pirazolac-treated rheumatoid arthritis patients.

Turner R A RA, Johnson J A JA, Turner S R SR, McGee M M et al.

Neutrophils from 20 medication-free rheumatoid arthritis patients were chemotactically hyporesponsive to 2 x 10(-8) M formyl-methionyl-leucyl-phenylalanine (f-MLP) as compared to 20 normal controls. They were relatively high producers of 5-hydroxyeicosatetraenoic acid (5-HETE) and low producers of leukotriene C4 (LTC4). Neutrophils from 10 patients treated with pirazolac (4-(4-chlorophenyl)-1-(4-fluorophenyl)-5-pyrazole acetic acid) showed increased chemotactic responsiveness concomitantly with normalization of 5-HETE and LTC4 production and a decrease in the clinical parameters of disease activity. Clinically attainable (30-60 micrograms/ml) in-vitro doses of pirazolac further depressed the chemotactic responsiveness of normal neutrophils treated with 10(-5)M f-MLP. Effects on endothelial gating of migrating neutrophil populations may explain this apparent contradiction between in-vivo and in-vitro actions of pirazolac on neutrophil chemotaxis.

PMID 2115831
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PubMedDrugs under experimental and clinical research1990-01-01

A 12-week double-blind study of the efficacy, safety and tolerance of pirazolac b.i.d. compared with indomethacin t.i.d. in patients with ankylosing spondylitis.

Carcassi C C, La Nasa G G, Perpignano G G

A 12-week trial was carried out to compare the efficacy of pirazolac (300-600 mg b.i.d.) with that of indomethacin (25-50 mg t.i.d.) in patients with ankylosing spondylitis. A total of 119 patients completed the treatment period, with 32 drop-outs. Both therapies showed significant improvements in clinical symptoms.

PMID 2198157
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PubMedDrugs under experimental and clinical research1990-01-01

The pharmacokinetics of pirazolac in human subjects.

Täuber U U

Pirazolac (PAA) is a new non-steroidal anti-inflammatory drug (NSAID) belonging to the subgroup of heterocyclic acetic acids. PAA is rapidly and completely absorbed and bioavailable at all dose levels tested. Plasma level curves after oral administration of capsule-shaped tablets were no different from those after administration of a crystalline suspension. The drug is highly (greater than 99%) bound to plasma albumins and penetrates easily into the synovial fluid. Plasma levels obey first-order pharmacokinetics over the whole therapeutic dose range. PAA is entirely conjugated with glucuronic acid before leaving the body, mainly in the urine. It has an intermediate elimination half-life of 17 h which does not depend on age or sex. Under twice-daily administration, fairly constant plasma levels are achieved, thus avoiding the high fluctuation observed with short half-life NSAIDs like indomethacin or diclofenac, and also avoiding the excessive accumulation observed with long half-life NSAIDs like pyrazolones and oxicams. This pharmacokinetic property makes pirazolac highly appropriate for long-term therapy of rheumatic diseases.

PMID 2376240
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PubMedEuropean journal of drug metabolism and pharmacokinetics1988-07-01

Pharmacokinetics of pirazolac, a new anti-inflammatory drug, in human volunteers. III. Steady state plasma levels.

Täuber U U, Beiersdorff R O RO, Matthes H H

Seven male, young subjects received twice daily 300 mg of pirazolac (PAA) for one week and twice daily 600 mg PAA for a further week as tablet. Plasma levels of PAA were monitored every day just before dosing and up to 72 hours after the last dose using a specific HPLC-method. During the first week of treatment trough steady state levels of Cssmin = 24 +/- 8 micrograms/ml were reached at day 4. After changing of dose regimen to twice daily 600 mg a new steady was established four days later with Cssmin = 62 +/- 15 micrograms/ml. PAA in the plasma was highly (99.2 +/- 0.8%) bound to plasma proteins. Time course of the decay of PAA levels in the plasma after the last dose was similar to that after a single administration.

PMID 3240767
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