Evaluation of samarium-153 and holmium-166-EDTMP in the normal baboon model.

Bone-seeking radiopharmaceuticals such as ethylenediaminetetramethylene phosphonate (EDTMP) complexes of samarium-153 and holmium-166 are receiving considerable attention for therapeutic treatment of bone metastases. In this study, using the baboon experimental model, multicompartmental analysis revealed that with regard to pharmacokinetics, biodistribution, and skeletal localisation, 166Ho-EDTMP was significantly inferior to 153Sm-EDTMP and 99mTc-MDP. A more suitable 166Ho-bone-seeking agent should thus be sought for closer similarity to 153Sm-EDTMP to exploit fully the therapeutic potential of its shorter half-life and more energetic beta radiation.

Blood platelet kinetics in normal subjects modelled by compartmental analysis.

The purpose of this study was to describe the function of platelets throughout their life span by expressing their in vivo distribution and kinetic behaviour in mathematical terms by using multicompartmental analysis. The distribution of indium-111 labelled platelets in five normal subjects was imaged and quantified with a scintillation camera image processing system. Serial blood samples were also obtained. The data were modelled using the SAAM (Simulation Analysis and Modelling) compartmental computer program. Five models were entertained to evaluate the role of platelets that were either functional or injured during collection and their interaction with the liver, spleen and vascular endothelium. Models were evaluated by comparing F values calculated from the least squares estimate obtained from each model. The Dornhorst function was used to describe the sequestration of platelets in the compartmental model. Results indicated that the data could not be satisfactorily simulated when compartments were included that simulated only functional and sequestered platelets (model 1). It was necessary to include compartments that simulated the kinetics of collection-injured platelets in the liver (model 2) and spleen (model 3). The model that simulated the interaction with the vascular endothelium (model 5) showed a visual but not significant improvement in the fitting of the observed data compared to model 3. The mean organ uptake and range indicated in parentheses were calculated at equilibrium. There were 20% (15%-27%) of the injected platelets in the spleen, 10% (8%-11%) in the liver and 70% (64%-75%) in the circulation.(ABSTRACT TRUNCATED AT 250 WORDS)

Comparison of oxine and tropolone methods for labeling human platelets with indium-111.

The effect of the chelates oxine and tropolone, used to label platelets, on the kinetics of indium-111-(111In) labeled platelets was studied in twelve normal human subjects. Autologous platelets were labeled either in saline with 111In-oxine or in plasma with 111In-tropolone. Mean platelet lifespan was estimated by fitting the disappearance curve of platelets from the circulation to the multiple hit and other mathematical models. The in vivo distribution of platelets was quantitatively imaged with a scintillation camera. The in vivo recovery of 111In-oxine and 111In-tropolone did not differ, and the mean platelet lifespan was also similar (111In-oxine: 230 +/- 29 hr; 111In-tropolone: 226 +/- 13 hr). At equilibrium (90 min after reinjection of labeled platelets) and at the end of platelet lifespan, 111In-oxine and 111In-tropolone radioactivities in the spleen and liver were similar. These results demonstrate that the results of kinetics measured with 111In-oxine or 111In-tropolone do not differ significantly.

Investigation into the effect of Fenoterol on mucociliary clearance in patients with chronic bronchitis.

We investigated the effect of Fenoterol, a selective beta 2 adrenoceptor stimulant, on mucociliary clearance in 12 patients with chronic bronchitis. Mucociliary clearance was measured with a scintillation camera after inhalation of a 99mTc labelled aerosol. Fenoterol was administered one h after acquisition commenced and imaging was maintained for a further two h. Three regions of interest (ROI) were selected over each lung to generate time activity curves. Corrections for decay, alveolar deposition (using 24 h image), cough and movement of activity through each ROI were carried out. An exponential function was fitted to the clearance curves to determine clearance rates. The increase in percentage clearance after Fenoterol administration for the left and right whole lung ROI was 35% and 36% per h respectively (P = 0.006 and 0.020). Fenoterol enhances cilial clearance in chronic bronchitis patients.

The effects of nisoldipine on left ventricular filling rate in patients with ischemic heart disease measured with radionuclide gated blood pool scintigraphy.

Nisoldipine is a newly developed calcium channel blocker with outstanding vasodilatory properties especially with regard to the coronary arteries. Thus it may find wide-spread application as a therapeutic agent in various ischemic heart disease syndromes. The purpose of this study was to evaluate the effect of nisoldipine on the diastolic function of the left ventricle (LV) in the clinical situation. A patient group on nisoldipine treatment was compared to a control group. In the nisoldipine group a maximum decrease of 17 mmHg in the mean systolic blood pressure with an increase in the mean peak ejection rate (0.78 EDV/s) and peak filling rate (0.52 EDV/s) were observed. Mean LV ejection fraction increased by 6.4% and the time to peak filling rate decreased by 36.5 ms. After eight weeks of treatment the acute effects of nisoldipine were similar to the previous study. Nisoldipine therefore tends to improve both the diastolic and systolic function of the left ventricle.