Are coagulation times biomarkers? Data from a phase I study of the oral thrombin inhibitor LB-30057 (CI-1028).

Ecarin clotting time and activated partial thromboplastin time are coagulation tests that meet the definition of a biomarker. Prolongation of these coagulation times closely correlated with blood concentrations of the oral thrombin inhibitor LB-30057 (CI-1028) during a phase 1 study. But this simply reflects their functioning as enzyme inhibition assays of drug concentration.

Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure.

Background: Arginine vasopressin may contribute to abnormalities in hemodynamics and fluid balance in heart failure through its actions on V(1A) (vascular and myocardial effects) and V(2) receptors (renal effects). Inhibiting the action of vasopressin may be beneficial in patients with heart failure.

Methods And Results: A total of 142 patients with symptomatic heart failure (New York Heart Association class III and IV) were randomized to double-blind, short-term treatment with conivaptan, a dual V(1a)/V(2) vasopressin receptor antagonist, at a single intravenous dose (10, 20, or 40 mg) or placebo.

Pharmacokinetics of butixocort 21-propionate, budesonide, and beclomethasone dipropionate in the rat after intratracheal, intravenous, and oral treatments.

The disposition of butixocort 21-propionate (JO 1222) in the rat after intratracheal treatment with a pulmonary aerosol was compared to that of budesonide (BUD) and beclomethasone dipropionate (BDP) using tritium-labeled aerosols. Each aerosol canister delivered 50 micrograms of 3H-labeled steroid through an intratracheal catheter directly into the lung. Rats were sacrificed at different times after treatment.

Effects of fedotozine on gastrointestinal motility in dogs: mechanism of action and related pharmacokinetics.

The effects of fedotozine, (+)-(1R)-1-phenyl-1-[(3,4,5-trimethoxy)benzyloxymethyl]-N,N-dim eth yl- n-propylamine, on motility of the antrum and small intestine were investigated in dog. In fasted dogs, following i.v.

Anaplastic small cell (oat cell) carcinoma of the tonsils: report of two cases.

Two cases of anaplastic small cell (oat cell) carcinoma of the tonsils are presented. In the first, cervical metastases preceded the manifestation of the primary tumour by 2 years. In case 2 the tonsillar carcinoma was accompanied by a bronchial tumour of the same histological type and by cervical and axillary metastases.

Isolation and identification of major metabolites of tixocortol pivalate in human urine.

The metabolism of tixocortol pivalate (PIVALONE), an anti-inflammatory steroid without systemic glucocorticoid effects, has been investigated in man. The analysis was conducted using urine samples collected from two volunteers who had received a 2-g oral dose of 14C-tixocortol pivalate as an oral suspension. Metabolites were purified and isolated from urine by normal phase HPLC, and structural identification was achieved by desorption chemical ionization/NH3 and electron impact/direct line introduction mass spectrometry.

[Familial hypocalciuric hypercalcemia. A new family].

A new example of familial hypocalciuric hypercalcaemia is reported. The family studied consists of 19 members over four generations. The first patient described in this study had already undergone a classical surgical operation for "primary hyperparathyroidism" before the correct diagnosis was established: that of a new syndrome described for the first time by Foley in 1972 and subsequently studied by Marx since 1977.

Comparative pharmacokinetic studies of tixocortol pivalate and cortisol in the rat.

Comparative pharmacokinetic studies of [14C]tixocortol pivalate ([14C]TP) and [14C]cortisol were carried out in rats. A 2.5 mg/kg i.

Bioavailability of Theodel, a new theophylline tablet, in humans.

The bioavailability of Theodel, a new scored tablet of theophylline, was investigated in eight healthy adult volunteers. Rate of absorption and AUC infinity were compared after single oral doses of Theodel (250 mg), of an aqueous solution (250 mg), and of two Theolair tablets (2 X 125 mg). Theophylline was rapidly absorbed from the Theodel tablet, with a t1/2abs of 0.

Plasma protein binding of the reversible type A MAO inhibitor cimoxatone (MD 780515).

Binding of a new selective reversible type A MAO inhibitor cimoxatone (MD 780515) to plasma proteins was studied in vitro by equilibrium dialysis. Binding to 580 microM human serum albumin (HSA) and to total plasma proteins was 93-96% and independent of cimoxatone concentration (0.15-207 microM).

Pharmacokinetics of theophylline: a dose-range study.

1 Pharmacokinetics of theophylline were investigated in a group of healthy adult volunteers (non smokers and on xanthine-free diet) following single oral administration of 125, 250, 375 and 500 mg doses as tablets (Theodel). 2 Absorption of theophylline was rapid and followed first-order kinetics. Plasma curves were fitted according to a one compartment open model.

Symptomatic hypopituitarism revealing a primary empty sella turcica.

A 64-year-old nulliparous woman presented with clinical signs of thyroid and adrenocortical insufficiency. Subsequent hormonal investigations demonstrated a failure of all anterior pituitary functions. Pneumotomo-encephalography revealed a large arachnoid herniation, leading to the diagnosis of primary empty sella turcica syndrome with secondary panhypopituitarism.

Absorption, distribution, elimination and metabolism of 14C-heptaminol hydrochloride in rat.

Absorption, distribution, excretion and metabolism studies with 14C-labelled 6-amino-2-methyl-2-heptanol hydrochloride (14C-heptaminol hydrochloride, Hept-amyl) were carried out in rat. After a 10 mg/kg p.o.