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Am J Health Syst Pharm. 1995 Nov 1;52(21):2423-6.
Compatibility and activity of aldesleukin (recombinant interleukin-2) in presence of selected drugs during simulated Y-site administration: evaluation of three methods.

Alex S, Gupta SL, Minor JR, Turcovski-Corrales S, Gallelli JF, Taub D, Piscitelli SC.

Asco Health Care, Inc., Columbia, MD, USA.

The compatibility and biological activity of aldesleukin (a form of recombinant interleukin-2) in the presence of selected i.v. drugs during simulated Y-site administration was studied. Five milliliters of aldesleukin 33,800 IU/mL in 5% dextrose injection was mixed in glass test tubes with 5 mL of each of 19 i.v. drugs prepared at concentrations used in routine clinical practice. The compatibility of the combinations was assessed by visual examination and spectrophotometry at 0, 0.5, 1, and 2 hours after preparation, and bioassays were conducted to determine the activity of aldesleukin in the combinations. Lorazepam was the only drug visually incompatible with aldesleukin. All the secondary drugs were spectrophotometrically compatible with aldesleukin. However, the bioassays showed that the following drugs reduced the activity of aldesleukin: ganciclovir sodium, lorazepam, pentamidine isethionate, prochlorperazine edisylate, and promethazine hydrochloride. Thus, aldesleukin became less biologically active when combined with four drugs for which visual examination suggested compatibility and when combined with five drugs for which spectrophotometry indicated compatibility. Aldesleukin 33,800 IU/mL in 5% dextrose injection lost significant biological activity in the presence of prochlorperazine edisylate, promethazine hydrochloride, lorazepam, ganciclovir sodium, and pentamidine isethionate during simulated Y-site administration. Visual assessment and spectrophotometry may not be valid methods for assessing possible changes in the biological activity of aldesleukin when combined with other agents.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8564607&dopt=Abstract




J Pharm Biomed Anal. 1995 Aug;13(9):1161-6.
A liquid chromatographic method for the determination of promethazine enantiomers in human urine and serum using solid-phase extraction and fluorescence detection.

Ponder GW, Stewart JT.

Department of Medicinal Chemistry, College of Pharmacy, University of Georgia, Athens 30602, USA.

A LC method was developed for the concurrent assay of R(+) and S(-) promethazine from human urine and serum. The method involves the use of solid-phase extraction for sample clean-up. Chromatographic resolution of the enantiomers was performed under isocratic conditions using a mobile phase of hexane-1,2-dichlorethane-absolute ethanol-trifluoroacetic acid (400:150:100:1, v/v/v/v) at a flow rate of 1 ml min-1 on a brush-type column KK-CARNU. The enantiomers were detected by fluorescence using an excitation wavelength of 250 nm and a 280 nm emission cutoff filter. Chlorpromazine was used as the internal standard for urine analysis. Standard addition was used for promethazine analysis from serum. Drug to internal standard ratios were linear from 0.25 to 10 micrograms ml-1 in urine. Serum levels were linear from 2 to 10 ng ml-1.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8573643&dopt=Abstract




Psychopharmacology (Berl). 1995 Oct;121(3):347-56.
The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis.

Fiorella D, Rabin RA, Winter JC.

Department of Pharmacology and Toxicology, School of Medicine and Biomedical Sciences, State University of New York at Buffalo, USA.

Investigations conducted over the past 3 decades have demonstrated that serotonergic receptors, specifically the 5-HT2A and 5-HT2C subtypes, play an important role in the behavioral effects of hallucinogenic compounds. The present study was designed to determine the respective significance of these two receptors in the stimulus effects of LSD and (-)DOM in the rat. Specifically, the interactions of a series of serotonergic antagonists (risperidone, pirenpirone, metergoline, ketanserin, loxapine, LY53857, pizotyline, spiperone, cyprohepatadine, mesulergine, promethazine, and thioridazine) with the LSD stimulus and the (-)DOM stimulus in LSD-trained subjects was defined. From these data, IC50 values were determined for the inhibition of the LSD-appropriate responding elicited by either 0.1 mg/kg LSD (15-min pretreatment time) or 0.4 mg/kg (-)DOM (75-min pretreatment). In addition, the affinities of these antagonists for 5-HT2A and 5-HT2C receptors were determined in radioligand competition studies, 5-HT2A affinity correlated significantly with IC50 values for the blockade of the LSD (r = +0.75, P < 0.05) and (-)DOM (r = +0.95, P < 0.001) stimuli in the LSD trained subjects. 5-HT2C affinity did not correlate significantly with either series of IC50 values. These data indicate that (1) the stimulus effects of LSD, and (2) the substitution of (-)DOM for the LSD stimulus are mediated by agonist activity at 5-HT2A receptors.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8584617&dopt=Abstract













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