Abstract |
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.
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Authors | U Täuber |
Journal | Drugs under experimental and clinical research
(Drugs Exp Clin Res)
Vol. 16
Issue 1
Pg. 7-15
( 1990)
ISSN: 0378-6501 [Print] Switzerland |
PMID | 2376240
(Publication Type: Journal Article)
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Chemical References |
- Anti-Inflammatory Agents, Non-Steroidal
- Pyrazoles
- pirazolac
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Topics |
- Absorption
- Administration, Oral
- Adult
- Anti-Inflammatory Agents, Non-Steroidal
(administration & dosage, pharmacokinetics)
- Biological Availability
- Dose-Response Relationship, Drug
- Drug Administration Schedule
- Drug Interactions
- Female
- Humans
- Kidney Diseases
(metabolism)
- Male
- Middle Aged
- Pyrazoles
(administration & dosage, pharmacokinetics)
- Regression Analysis
- Synovial Fluid
(metabolism)
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