Radioimmunoassay of Buprenorphine with Iodine Label: Analysis of Buprenorphine and Metabolites in Human Plasma

Abstract

SUMMARY.Quantitative analysis of potent opiate drugs in plasma by radioimmunoassay is potentially inaccurate because of the occurence of cross-reacting metabolites. This paper describes the chemical synthesis of buprenorphine-3-0-glucuronide, a metabolite of buprenorphine, and an extraction procedure coupled with radioimmunoassay which allows the sensitive and specific measurement of buprenorphine using an iodinated buprenorphine derivative. The measurement of extracted and unextracted samples using two different antisera allowed investigation of the metabolism of buprenorphine. In four patients who had taken sublingual buprenorphine for at least one month, N-dealkyl buprenorphine was present in similar concentrations to those of buprenorphine, while buprenorphine-3-0-glucuronide was present if} two to three times those concentrations.Buprenorphine (Fig.

The pharmacokinetics and physiological effects of buprenorphine infusion in premature neonates.

“…Samples were analysed for buprenorphine using a radioimmunoassay (r.i.a.) based on the method of Hand et al [10]. The …”

Stability of morphine and buprenorphine in whole blood

“…A recent report on morphine conjugate stability showed that morphine glucuronides are stable for a few days [8] and controversial data exist concerning the stability of morphine in urine samples [9,10]. Buprenorphine is a recently marketed opiate and most of the published work relates either to the pharmacokinetics [11,12] or analysis [13][14][15][16]. No data are available regarding its stability in blood, but some reports have evaluated the stability of other drugs in biological fluids stored for 1 year at various temperatures [17,18].…”

Characterization of the discriminative stimulus effects of buprenorphine in pigeons

“…The long duration of the discriminative stimulus effects of buprenorphine is not fully understood and might be due to a number of factors, including a long elimination half-life (6-8 h) (Hand et al 1990;Amani et al 1997) as compared to morphine (1.4 h) (Hain et al 1999); in humans, the plasma concentrations of major metabolites of buprenorphine (nor-buprenorphine and buprenorphine-3-O-glucuronide) are sometimes greater than concentrations of the parent compound (Hand et al 1986). Other data indicate that dispositional factors might be important for the long duration of action of buprenorphine.…”