Tenoxicam concentrations in synovium and joint cartilage in humans

Bannwarth, B; Netter, Patrick; Lapicque, Françoise; Mainard, Didier; Fener, P.; Gillet, Pierre; Gaucher, A

doi:10.1007/bf01980889

Cited by 16 publications

(5 citation statements)

References 8 publications

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“…26 Further, tenoxicam tends to be concentrated in the synovium rather than the cartilage. 27 While there may be some question as to whether or not all NSAID are safe for intra-articular injection we believe tenoxicam is safe. Despite this, for safety reasons we excluded patients with osteoarthritis.…”

Section: Discussionmentioning

confidence: 99%

Analgesia after day-case knee arthroscopy: double-blind study of intra-articular tenoxicam, intra-articular bupivacaine and placebo

Cook¹,

Tuckey²,

Nolan³

1997

British Journal of Anaesthesia

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Arthroscopy of the knee is performed regularly on a day-case basis. Intra-articular bupivacaine produces transient analgesia and reports of analgesia using intra-articular morphine have produced conflicting results. Non-steroidal anti-inflammatory drugs given systemically can provide effective analgesia for this procedure. In this study we attempted to determine if intra-articular tenoxicam provided useful analgesia after day-case arthroscopy. Sixty three ASA I-II patients were allocated randomly to one of three groups to receive 40 ml of a solution containing 0.9% saline (group Pla), 0.25% bupivacaine (group Bup) or tenoxicam 20 mg (group Ten). The injection was made into the knee joint at the end of surgery, 10 min before tourniquet deflation. Verbal rating and visual analogue pain scores (at rest and on knee flexion), use of analgesia, mobilization and disturbance by pain at home were recorded for the next 48 h. There were no differences between pain scores in any of the three groups when tested at rest or on movement. Less analgesia was used in the first 24 h by patients in the tenoxicam group but the difference in time to first analgesia was not statistically significant. Side effects and disturbance by pain were similar in all groups. The use of intra-articular tenoxicam 20 mg at the end of arthroscopy reduced oral analgesic requirements during the first day after operation but did not alter patients' perception of pain.

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Section: Discussionmentioning

confidence: 99%

Analgesia after day-case knee arthroscopy: double-blind study of intra-articular tenoxicam, intra-articular bupivacaine and placebo

Cook¹,

Tuckey²,

Nolan³

1997

British Journal of Anaesthesia

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“…Heizmann et al (1986) were able to codetermine tenoxicam and its 5' -hydroxy metabolite in plasma, and Dell et al (1984) estimated tenoxic am glucuronides in urine. Methods are also available for detection of the drug in synovial fluid (Bird et al 1985a;Corvetta et al 1991;Bannwarth et al 1991) and joint cartilage (Bannwarth et al 1991). …”

Section: Methods Of Analysismentioning

confidence: 98%

“…Table IX indicates, however, a higher steady-state distribution of the drug to synovial tissue (Bannwarth et al 1991) than to synovial fluid, which may have clinical significance. Tenoxicam seems to penetrate to a lesser extent into joint cartilage.…”

Section: Distribution To Other Fluids and Tissuesmentioning

confidence: 93%

Clinical Pharmacokinetics of Tenoxicam

Nilsen

1994

Clinical Pharmacokinetics

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Tenoxicam is a nonsteroidal anti-inflammatory drug (NSAID) in the oxicam group. It is completely absorbed by the oral route and is about 99% protein bound in human plasma. Intake of food delays absorption without affecting bioavailability. There is no evidence for enterohepatic recycling of the drug in humans. Peak plasma concentrations of 2.7 mg/L (range 2.3 to 3.0 mg/L) have been reported in different groups of fasted healthy volunteers 1.9 hours (1.0 to 5.0 hours) after a single oral dose of 20mg. A mean elimination half-life of 67 hours (49 to 81 hours) has been estimated. Tenoxicam demonstrates linear single-dose pharmacokinetics over doses of 10 to 100mg. Because of its low lipophilicity and high degree of ionisation in blood (approximately 99%), the drug is poorly distributed to body tissues and is slowly taken up by hepatic cells. A small apparent volume of distribution of 9.6L (7.5 to 11.5L), and low total plasma clearance of 0.106 L/h (0.079 to 0.142 L/h), have been reported in different groups of healthy volunteers after oral and intravenous administration. Peak concentrations of tenoxicam in synovial fluid are less than one-third of those in plasma and they appear later, 20 hours (10 to 34 hours) after an oral dose. A parallel decrease in synovial fluid and plasma concentrations with time for both total and unbound tenoxicam has been reported. In vivo pH differences between synovial fluid and plasma in patients with rheumatoid arthritis may indicate significantly lower concentrations of unbound ionised tenoxicam in synovial fluid than in plasma. Data on relative binding capacities for tenoxicam in plasma and synovial fluid, and between different groups of individuals, are not conclusive. The protein binding of tenoxicam is pH dependent. The drug is almost entirely eliminated by liver metabolism. The 2 main metabolites, the inactive 5'-hydroxy and 6-O-glucuronidated forms, are excreted in urine and bile, respectively. The existence of additional metabolites in human bile has been suggested. Urinary excretion of the 5'-hydroxy metabolite decreases with reduced renal function. The 5'-hydroxy metabolite is detected in plasma in concentrations 1 to 5% of the parent compound and its decline parallels that of the parent compound (formation-rate limitation). Urinary and faecal excretion of unchanged tenoxicam is less than 1% of the administered dose. No significant amounts of unchanged tenoxicam are excreted in bile. Tenoxicam shows nearly linear pharmacokinetics during multiple-dose administration.(ABSTRACT TRUNCATED AT 400 WORDS)

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“…Based on these early observations efforts have been devoted to exploit the ion exchange properties of the ECM to enhance drug accumulation in the cartilage tissue. Various positively charged organic molecules have been observed to distribute into cartilage 138–147. This includes (i) radiodiagnostic agents for joint imaging containing a N‐quaternary functional group,142, 143 (ii) N‐quaternary analogues of anti‐inflammatory oxicams,140, 144 and (iii) a derivative of the potential DMOAD doxycycline 147…”

Section: Drug Transport and Distribution Processes In A Synovial Envimentioning

confidence: 99%

Intra‐articular depot formulation principles: Role in the management of postoperative pain and arthritic disorders

Larsen

Østergaard

Larsen

et al. 2008

Journal of Pharmaceutical Sciences

257

212

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Tenoxicam concentrations in synovium and joint cartilage in humans

Cited by 16 publications

References 8 publications

Analgesia after day-case knee arthroscopy: double-blind study of intra-articular tenoxicam, intra-articular bupivacaine and placebo

Analgesia after day-case knee arthroscopy: double-blind study of intra-articular tenoxicam, intra-articular bupivacaine and placebo

Clinical Pharmacokinetics of Tenoxicam

Intra‐articular depot formulation principles: Role in the management of postoperative pain and arthritic disorders

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