Colonic absorption of human calcitonin in man.

1. Human calcitonin was administered into the distal colon and by intravenous infusion in eight healthy subjects in an open, fixed sequence, cross-over bioavailability study. 2.

Intravenous amine pressor tests in healthy volunteers. Within- and between subject variances and sex differences.

The pressor effect of intravenous tyramine (TYR) and noradrenaline (NA) has been evaluated, respectively, in 157 tests in 19 healthy unmedicated subjects, and in 202 tests in 24 similar subjects, all of whom took part in greater than or equal to 3 test sessions. The pressor dose (PD) that raised systolic blood pressure by 30 mm Hg (PD30) ranged from 2 to 8 mg for TYR, and from 3.5 to 17 micrograms.

Effect of the selective MAO-A inhibitors brofaromine, clorgyline and moclobemide on human platelet MAO-B activity.

MAO-B activity was compared in healthy volunteers following oral treatment with clinically effective doses of the selective MAO-A inhibitors brofaromine (100 mg q.d. for 14 days), moclobemide (150 mg t.

Effect of orally administered misoprostol and cimetidine on the steady state pharmacokinetics of diazepam and nordiazepam in human volunteers.

The effects of misoprostol and cimetidine on diazepam pharmacokinetics were evaluated in order to determine whether the kinetic variables for diazepam and nordiazepam alone differ with the repeated oral administration of misoprostol and cimetidine to healthy adult volunteers. The trial was conducted as an open crossover study in 12 normal subjects, divided into two groups with all subjects receiving both regimens. Total study duration was 5 weeks.

No effect of famotidine on cardiac performance by noninvasive hemodynamic measurements.

In a randomized, double-blind, placebo-controlled, two-way crossover study, 12 healthy volunteers were treated once daily for 1 week each with 40 mg famotidine or placebo. Stroke index, cardiac index, preejection period, left ventricular ejection time, and carotid and femoral blood flow were measured noninvasively with Doppler ultrasonography. No significant changes in these hemodynamic parameters were observed when differences between baseline and each time point after administration of famotidine were compared with corresponding differences after placebo.

Urinary excretion of CGS 5,649 and its conjugated glucuronide and sulfate in man.

Experiments in animals have indicated that CGS 5,649 B [6-(2-isopropylaminopropyl)-3-pyridinol fumarate] might enhance memory and learning processes and might be a valuable drug for treatment of impairment of vigilance and mental performance in the elderly. CGS 5,649 (I) is extensively metabolized. Therefore, we investigated the excretion of the drug and its conjugates (I-SULF,I-GLUC) into urine after oral administration of 1200 mg of the fumarate salt of I to one healthy male volunteer.

Effect of the new selective COMT inhibitor CGP 28014 A on the formation of 3-O-methyldopa (3OMD) in plasma of healthy subjects.

CGP 28014 A is a specific inhibitor of catechol-O-methyl transferase (COMT). The effect on COMT was assessed with the levodopa test in 5 unmedicated subjects and after pretreatment with 200-600 mg CGP 28014 p.o.

Tyramine kinetics and pressor sensitivity during monoamine oxidase inhibition by selegiline.

The effect of the monoamine oxidase inhibitor selegiline on tyramine metabolism and intravenous and oral tyramine pressor sensitivity was studied in healthy subjects. After oral doses of tyramine, which caused systolic blood pressure to increase by 30 mm Hg, we determined plasma concentrations of p-hydroxyphenylacetic acid (HPAA) and of conjugated and unconjugated tyramine. When 20 mg/day of selegiline was administered, the AUCspec of HPAA decreased from 86% to 64% and the AUCspec of conjugated tyramine increased from 13% to 35% of the sum of total tyramine and HPAA.

Monoamine oxidase inhibition by phenelzine and brofaromine in healthy volunteers.

The two monoamine oxidase (MAO) inhibitors phenelzine and brofaromine given for 2 to 3 weeks were compared in six volunteers. Blood pressure sensitivity to intravenous tyramine increased 2.6-fold during phenelzine (60 mg/day) and 4.

Tyramine potentiation during treatment with MAO inhibitors: brofaromine and moclobemide vs irreversible inhibitors.

Healthy ambulatory subjects were treated p.o. for 2 to 4 weeks with 6 different MAO inhibitors (MAOI).

Interaction of alcohol and transdermally administered scopolamine.

In a placebo-controlled, randomized, double-blind cross-over study in 12 healthy volunteers the effect of acute alcohol intake during treatment with transdermally administered scopolamine (TTS-scopolamine) was investigated. One group of six subjects reached maximal blood alcohol concentrations (BAC) of 80 mg/dL and another group of six subjects a BAC of 130 mg/dL. There was no significant potentiation of alcohol effects on critical flicker fusion frequency by TTS-scopolamine.

A new method for analysing the geometry and timecourse of epicardial potential spreading.

A 256 unipolar electrode matrix fixed at the surface of an isolated rabbit heart was connected to a PC system via an amplifying and analog/digital converting frontend computer. This system allows measurement of 256 electrodes within 100 microseconds with a sampling rate of 0.25 ms.

Practice effect of volunteers in repeated psychometric testing. How to handle this intervening variable in clinical pharmacology studies?

Performance in psychometric tests may show a practice effect with repeated testing. Ideally, a plateau of efficiency should be reached prior to first drug intake. In order to assess the period of familiarization in a multiple choice reaction task (MCRT) 17 healthy subjects practiced the test up to 36 times in the drug free run-in period of 2 trials.

Oral tyramine pressor test and the safety of monoamine oxidase inhibitor drugs: comparison of brofaromine and tranylcypromine in healthy subjects.

The pressor effect of orally administered tyramine (TYR) has been evaluated in 124 tests of 49 healthy unmedicated volunteers, in 99 tests of 29 subjects treated with the reversible selective monoamine oxidase (MAO) A inhibitor brofaromine (BROF), and in 73 tests of 12 subjects treated with tranylcypromine (TCP). In unmedicated subjects, pressor doses of TYR to raise systolic blood pressure (BP) by 30 mm Hg (PD30) ranged between 200 and 800 mg of TYR. There was no correlation of PD30 with sex, age, or weight.

High-performance liquid chromatographic determination of a new pyrazoloquinoline type benzodiazepine receptor antagonist and its hydroxy metabolite.

A rapid high-performance liquid chromatographic (HPLC) method for the determination of the novel benzodiazepine receptor antagonist 2-phenylpyrazolo[4,3-c]quinolin-3(5H)-one (CGS 8216) and its hydroxy metabolite is described. The method involves a solid-phase extraction with C18 disposable columns and quantification by HPLC with UV-detection. In plasma 20 ng/ml of the antagonist and 10 ng/ml of metabolite can be measured with a coefficient of variation of about 10%.

Effect of brofaromine and pargyline on human plasma melatonin concentrations.

1. Plasma melatonin was used to determine the influence of two monoamine oxidase inhibitor drugs in 11 normal subjects. 2.