Pharmacokinetic observations on piroxicam in young adult, middle‐aged and elderly patients.

Woolf, AD; Rogers, H. J.; Bradbrook, ID; Corless, D.

doi:10.1111/j.1365-2125.1983.tb02191.x

Cited by 46 publications

(13 citation statements)

References 9 publications

(12 reference statements)

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“…There is also little accumulation of ketoprofen (28%) upon repeated dosing of the controlled release formulation, in marked contrast to a 490% accumulation of piroxicam in a group consisting mainly of elderly patients (Woolf et al, 1983).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic profile of controlled release ketoprofen in elderly patients.

Dennis¹,

Pc²,

Crome³

et al. 1985

Brit J Clinical Pharma

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The pharmacokinetics of ketoprofen following the administration of the first and final dose of a controlled release formulation (200 mg ketoprofen) once daily for 10 days to nine elderly patients have been studied. Plasma ketoprofen concentrations were measured by h.p.l.c. The data were compared to previously reported studies in young male volunteers. Mean +/‐ s.d. peak plasma concentrations (5.6 +/‐ 1.75 micrograms ml‐1 and 6.3 +/‐ 2.7 micrograms ml‐1 on day 1 and day 10, respectively) were higher than those reported in young volunteers given similar treatment, but similar to those reported in young volunteers following 50 mg four times daily of conventionally formulated ketoprofen, and markedly lower than reported following a single 100 mg dose of ketoprofen. The half‐life for drug release (mean +/‐ s.d.) from the controlled release formulation (8.5 +/‐ 7.4 h) and accumulation upon repeated dosing (28%) were essentially the same as reported for young volunteers. The area under the plasma concentration‐time curve was about 65% greater than reported in young volunteers following administration of controlled release ketoprofen. This increase in exposure to ketoprofen is probably partly due to the lower volume of distribution in the elderly and partly due to a reduced renal excretion of the glucuronide metabolite of ketoprofen. It was concluded that controlled release ketoprofen may be administered in standard doses (200 mg once daily) to elderly patients whose elimination processes are not severely impaired (i.e. severe renal failure or hepatic disease).(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetic profile of controlled release ketoprofen in elderly patients.

Dennis¹,

Pc²,

Crome³

et al. 1985

Brit J Clinical Pharma

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“…Thus, it is not surprising that its apparent oral volume of distribution is only 0.10 to 0.20 L/kg (Darragh et al 1985;Kobayashi et al 1984;Richardson et al 1985Richardson et al , 1986Woolf et al 1983). Since piroxicam has not been administered to humans intravenously, volume of distribution was determined after oral administration, assuming complete absorption.…”

Section: Distributionmentioning

confidence: 92%

“…Plasma concentrations of piroxicam can be assessed by a large selection of HPLC methods (e.g. Richardson et al 1986;Twomey et al 1980;Woolf et al 1983). Similarly, there are several HPLC methods available for determination of other oxicams, e.g.…”

Section: Analytical Methods For Oxicam Nsaidsmentioning

confidence: 99%

“…Renal impairment does not appear to alter the pharmacokinetic profile of piroxicam (Darragh et al 1985;Dupont et al 1982;Woolf et al 1983). Interestingly, and in accordance with pharmacokinetic theory, the elimination of piroxicam, a low extraction drug, is enhanced in patients with endstage renal disease.…”

Section: Effect Of Age and Diseasementioning

confidence: 96%

“…The pharmacokinetic profile of piroxicam appears to be independent of age (Darragh et al 1985;Edwards et al 1985;Woolf et al 1983). Richardson et al (1985) have reported that elderly healthy women eliminate piroxicam at a slower rate than young healthy women.…”

Section: Effect Of Age and Diseasementioning

confidence: 96%

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Pharmacokinetics of Oxicam Nonsteroidal Anti-Inflammatory Agents

Olkkola

Brunetto

Mattila

1994

Clinical Pharmacokinetics

110

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Oxicam nonsteroidal anti-inflammatory drugs (NSAIDs) are a group of structurally closely related substances with anti-inflammatory, analgesic and antipyretic activities. They have a weakly acidic character and are extensively bound to plasma proteins. Piroxicam, the most widely used oxicam, is well absorbed after oral administration. Peak plasma concentrations (Cmax) of the drug are reached within 2 to 4 hours. Piroxicam has a small volume of distribution and a low plasma clearance. It undergoes hepatic metabolism and only 5 to 10% is excreted unchanged in urine. The elimination half-life varies between 30 and 70 hours. Age of the patient and renal or hepatic dysfunction do not seem to have any major effect on the pharmacokinetics of piroxicam. The drug reduces the renal excretion of lithium to a clinically significant extent, but the clinical significance of piroxicam-aspirin (acetylsalicylic-acid) and piroxicam-acenocoumarol interaction has not been established. Ampiroxicam, droxicam and pivoxicam are prodrugs of piroxicam that have been synthesised to reduce piroxicam-related gastrointestinal irritation. All prodrugs are well absorbed, but Cmax values are reached later than those following administration of piroxicam. Tenoxicam is used in the management of rheumatic and inflammatory diseases. Mean Cmax values are achieved 2 hours postdose. Food reduces the rate but not the extent of absorption. The oral bioavailability of tenoxicam is 100% and rectal bioavailability is 80%. Like piroxicam, tenoxicam has a low volume of distribution and low plasma clearance. It is eliminated through hepatic metabolism. The mean elimination half-life is 60 to 75 hours. The pharmacokinetics of tenoxicam are independent of patient age, or concurrent liver or renal diseases. High doses of aspirin have been shown to increase the elimination of tenoxicam, but this has little clinical significance. Isoxicam was in widespread clinical use until its worldwide marketing was suspended because of fatal skin reactions. Isoxicam is completely absorbed, but Cmax values are not reached until 10 hours postdose. It has a low plasma clearance, approximately 5 ml/min (0.3 L/h), and low volume of distribution. The mean elimination half-life is 30 hours and does not appear to be affected by the age of the patient. Isoxicam potentiated the anticoagulant effect of warfarin, necessitating a 20% dosage reduction. Lornoxicam differs from other oxicam NSAIDs because it has a short elimination half-life of 3 to 4 hours. On the basis of limited data, some individuals seem to eliminate lornoxicam very slowly, suggesting the presence of polymorphic metabolism. The pharmacokinetics of cinnoxicam and sudoxicam have not been studied thoroughly.(ABSTRACT TRUNCATED AT 400 WORDS)

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Effects of dose and sex on the pharmacokinetics of piroxicam in the rat

Roskos

Boudinot

1990

Biopharm & Drug Disp

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The effects of dose and sex on the pharmacokinetics of piroxicam were studied in the rat. Piroxicam was administered intravenously at doses of 0.50 and 5.0 mg kg-1 to male and female rats. Plasma drug concentrations were determined by a highly sensitive high-performance liquid chromatographic technique. Non-compartmental pharmacokinetic parameters were calculated by area/moment analysis. A prolonged terminal half-life averaging 13.3 h in male rats and 40.8 h in female rats was observed. Dose had no effect on the disposition of piroxicam. The sex of the rat, however, had a marked effect on piroxicam pharmacokinetics, with mean total clearance differing three-fold from 0.0184 l h-1 kg-1 in male rats to 0.00622 l h-1 kg-1 in female rats. The free fraction of piroxicam in serum was greater in male rats than in female rats owing to a higher association constant for piroxicam binding to female rat serum proteins. Free piroxicam clearance differed approximately two-fold with mean values of 0.764 l h-1 kg-1 and 0.418 l h-1 kg-1 in male and female rats, respectively. Thus, protein binding partially explained the sex-dependent disposition of piroxicam. However, sex-dependent metabolism of the drug also appears to be a major determinant of sex-related differences in piroxicam pharmacokinetics. Steady-state volume of distribution was unaffected by sex. Half-life and mean residence time were three-fold greater in female rats owing to the three-fold lower clearance value compared to male rats.

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Pharmacokinetic observations on piroxicam in young adult, middle‐aged and elderly patients.

Cited by 46 publications

References 9 publications

Pharmacokinetic profile of controlled release ketoprofen in elderly patients.

Pharmacokinetic profile of controlled release ketoprofen in elderly patients.

Pharmacokinetics of Oxicam Nonsteroidal Anti-Inflammatory Agents

Effects of dose and sex on the pharmacokinetics of piroxicam in the rat

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