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Biomedical subjects

J Lund

Publications and source records attributed to J Lund.

At least 199 records · Page 11Linked to original sources

Paroxetine: pharmacokinetics, tolerance and depletion of blood 5-HT in man.

The tolerance of paroxetine (FG 7051), as well as its pharmacokinetics and reduction of 5-HT in blood, has been investigated in man. Three normal, healthy volunteers were administered the single doses 10, 25, 50, and 75 mg orally, and three volunteers received 10, 25, and 50 mg per day for seven or fourteen days. No toxic effect on blood, kidney, liver, heart or general condition was found by chemical and physical examinations. The pharmacokinetic studies revealed a dose dependent systemic availability, a rather slow elimination (t1-z2 = approximately 16 hrs), a good fit to one compartment open model, and an almost complete metabolism of the substance. 25 mg paroxetine per day gave a maximal reduction of 5-HT in the blood within 2--3 weeks (to approximately 0.03 microgram/ml). The 5-HT levels returned to the basic levels during a three to four weeks drug-free period.

Administration, Oral↗

Determination of (+)-(3R), (4S)-3-[(4methoxyphenoxy)methyl]-1-methyl-4-phenylpiperidine hydrochloride (FG 4963) in biological fluids using competition for adsorption to glass.

A procedure has been developed for the gas chromatographic determination of a structurally new 5HT-uptake inhibitor with antidepressant properties (FG 4963) in plasma and urine. The method involves an extraction from alkaline solution with n-pentane, and a quantitative determination by gas chromatography using an internal standard and a nitrogen-sensitive detector. The binding of FG 4963 to glass during storage and evaporation necessitates the addition of a structurally similar compound to the vials used for collection of the blood and urine, in order to compete for the binding sites of the glass. The method is suitable for pharmacokinetic and clinical studies, the sensitivity being ca. 5 ng/ml in plasma and 1 ng/ml in urine and the precision being 10-15% for concentrations greater than 10 ng/ml.

Adsorption↗

Antidepressant evaluation and the pharmacological actions of FG4963 in depressive patients.

FG4963 a phenylpiperidine derivative and potent 5-HT reuptake inhibitor at neuronal sites was investigated in a group of 10 depressive patients, and its effect was compared with that of amitryptyline in a group of 10 depressive patients treated with amitriptyline. FG4963 was found to be significantly inferior as an antidepressant compared to amitryptyline over a 6-week period. FG4963 did not appear to be anticholinergic as judged by its lack of effect on salivary flow. Its effect (in the dosage used) on the tyramine dose--pressor response and NA dose--pressor response tests were less than those of amitryptyline.

Amitriptyline↗

Metabolism of vitamin D3-3H in human subjects: distribution in blood, bile, feces, and urine.

Vitamin D(3)-(3)H has been administered intravenously to seven normal subjects, three patients with biliary fistulas, and four patients with cirrhosis. Plasma D(3)-(3)H half-times normally ranged from 20 to 30 hours. in vivo evidence that a metabolic transformation of vitamin D occurs was obtained, and a polar biologically active vitamin D metabolite was isolated from plasma. Urinary radioactivity averaged 2.4% of the administered dose for the 48-hour period after infusion, and all the excreted radioactivity represented chemically altered metabolites of vitamin D. The metabolites in urine were mainly water-soluble, with 26% in conjugated form. From 3 to 6% of the injected radioactivity was excreted in the bile of subjects with T-tube drainage and 5% in the feces of patients having no T-tube. The pattern of fecal and biliary radioactivity suggested that the passage of vitamin D and its metabolites from bile into the intestine represents an essential stage for the fecal excretion of vitamin D metabolites in man. Abnormally slow plasma disappearance of vitamin D(3)-(3)H in patients with cirrhosis was associated with a significant decrease in the quantity and rate of glucuronide metabolite excretion in the urine.

Adult↗