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  • 1
    ISSN: 1432-1041
    Keywords: moclobemide (Ro 11-1163) ; MAO-inhibitor ; cardiocirculatory effects ; systolic time intervals ; depressive patients ; control subjects ; chronic treatment ; side effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The benzamide-derivative moclobemide (Ro 11-1163) is a new short-acting, reversible MAO-inhibitor, preferentially affecting Type A MAO, which is, being developed as an antidepressant agent. The effect of moclobemide on heart rate, blood pressure, electrocardiographic and systolic time intervals was assessed in eight healthy volunteers and seven depressive patients. The volunteers received single doses of 100 mg, 150 mg and placebo in radomized single-blind order. Seven patients received placebo and 100 mg as single doses and five patients were also given chronic treatment with individually assessed optimal therapeutic dose (100–400 mg). No change in blood pressure, heart rate, ECG or systolic time intervals was found. The compound was well tolerated. The findings suggest that moclobemide may be a safe MAO-inhibitor as far as sympathetic responsiveness and cardiovascular effects are concerned.
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  • 2
    ISSN: 1432-1041
    Keywords: Key words Tamsulosin ; Benign prostatic hyperplasia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Objective: This study was performed to estimate whether the pharmacokinetics and safety of tamsulosin, an α1A-adrenoceptor antagonist for the treatment of symptomatic benign prostatic hyperplasia (BPH), are influenced by impaired renal function. Methods: In an open-label study design, the plasma concentration profile of 0.4 mg tamsulosin p.o. was studied in age-matched groups of male subjects with normal (n = 10), moderately impaired (n = 10), and severely impaired (n = 8) renal function after single-dose administration and in steady state, i.e. after 21 days of multiple-dose administration. Results: The AUC of total, but not of unbound, tamsulosin was correlated to creatinine clearance and α1-acid glycoprotein plasma levels, and was found to be significantly higher in both groups of subjects with impaired renal function than in controls after single- and multiple-dose administration. However, the pharmacokinetics of total and unbound tamsulosin were comparable for both trial periods. Conclusions: Impaired renal function increases total tamsulosin plasma concentration by approximately 100% after single-dose administration and in steady state. Since active unbound drug levels are not affected, no dose modification is required in symptomatic BPH patients with renal impairment.
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  • 3
    ISSN: 1432-1041
    Keywords: tiapamil ; desmethyltiapamil ; pharmacokinetics ; cardiovascular effects ; cirrhotic patients ; plasma protein binding ; impaired hepatic elimination ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Tiapamil 70 mg was administered i.v. to 8 healthy male volunteers and 8 patients (7 males, 1 female) with biopsy proven hepatic cirrhosis. Two of the patients also received 600 mg p.o. Serial plasma and urine samples were collected and the parent drug in plasma and urine and desmethyl-tiapamil in urine were assayed by a specific HPLC method. The plasma and urine data for the parent drug after i.v. and p.o. dosing were simultaneously fitted to linear p.o. and i.v. two compartment models with exit from and input into the central compartment. Absorption was assumed to be a first order process. In the volunteers the mean pharmacokinetic parameters were: 101 l for the steady-state volume of distribution, 750 ml·min−1 for nonrenal clearance, 195 ml·min−1 for renal clearance and 1.7 h for the half-life of the terminal disposition phase. The urinary recoveries of the parent drug and desmethyltiapamil averaged 21.4 and 0.8% of the dose, respectively. In the patients the steady-state volume of distribution, the amount of unchanged drug in urine and the half-life of the terminal disposition phase were significantly increased (171 l, 29.0% of the dose, 3.5 h, respectively). Decreased plasma protein binding in the patients accounted for the larger steady-state volume of distribution. The nonrenal clearance of 519 ml·min−1, tended to be smaller in the patients than in the volunteers. Together with the increased urinary recovery of tiapamil in the patients this indicates a moderately impaired elimination capacity in the cirrhotics. The renal clearance was similar in the patients (213 ml·min−1) and the volunteers. The absolute oral bioavailability of tiapamil was 55 and 49% in 2 patients. No effects of tiapamil on heart rate or supine blood pressure were detected, either in volunteers or in patients. Negative dromotropic effects were found in 2 volunteers and 2 patients after i.v. dosing.
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  • 4
    ISSN: 1432-1041
    Keywords: liposomes ; sodium fluorescin ; pharmacokinetics ; clinical studies ; drug delivery ; normals
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The in vivo kinetics and organ uptake of multilamellar liposomes have been studied in healthy volunteers. Sodium fluorescein-containing liposomes composed of equimolar amounts of egg phosphatidylocholine and cholesterol were injected into a peripheral vein in 4 healthy subjects. Blood samples collected from the femoral artery, hepatic vein and pulmonary artery, were analysed for liposomal dye content. The results, showing involvement of the reticuloendothelial system (RES) in the removal of liposomes, confirmed those previously obtained with radiolabelled preparations. Use of an innocuous liposomal marker (sodium fluorescein) and conventional vascular catheterization techniques, as employed here, may provide a reliable and clinically acceptable approach to establishing disease-induced changes in the kinetics of uptake of drug-containing liposomes by the RES, and thus help in the design of protocols for effective treatment.
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  • 5
    ISSN: 1432-1041
    Keywords: Tenoxicam ; Warfarin ; drug interaction ; pharmacokinetics ; anticoagulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of tenoxicam on plasma warfarin concentrations and on its anticoagulant effect has been studied in healthy volunteers. Tenoxicam did not alter the plasma warfarin concentration versus time profile. Treatment with it for 14 days had no effect on the average dose of warfarin required to maintain the prothrombin time within a specified range. The coumarin dose index, an indicator of warfarin sensitivity, remained unchanged during tenoxicam administration. The results demonstrate the lack of a clinically relevant effect of tenoxicam on warfarin-induced anticoagulation.
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  • 6
    ISSN: 1432-0428
    Keywords: Trestatin ; Ro 9-0154 ; Type2 diabetes ; α-amylase inhibitor ; starch digestion ; starch meal ; blood glucose ; plasma insulin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Trestatin (Ro 9-0154), a new specific α-amylase inhibitor of microbial origin, was tested in six normal subjects and seven Type 2 (non-insulin-dependent) diabetic patients. In normal subjects the maximal increases in blood glucose following a 115-g starch meal were 2.19±0.57 mmol/l (mean±SEM) with placebo, but 1.32±0.39 mmol/l with 10 mg, 1.06±0.26 mmol/l with 20 mg, 0.43±0.07 mmol/l with 50 mg (p〈0.05) and 0.26±0.14 mmol/l with 100 mg (p〈0.05) Trestatin. The corresponding increases in plasma insulin were 116.5±19.6mU/l; 74.8±17.5 mU/l; 50.7±8.3 mU/l; 28.7±6.9 mU/l (p〈0.05) and 16.5±3.2 mU/l (p〈0.05). In the diabetic patients the maximal increases in blood glucose following a 50-g starch meal were 6.09±0.02 mmol/l with placebo, but 3.17±0.59 mmol/ (p〈0.05) with 10 mg and 1.69±0.41 mmol/l (p〈0.05) with 30 mg Trestatin. The corresponding insulin increases were: 58.8±12.7 mU/l, 31.5±9.7mU/l (p〈0.05) and 23.4±4.8 mU/l (p〈0.05). Trestatin fully retained this pharmacological activity during treatment for 4 weeks in the diabetic patients. Trestatin did not influence glucose and insulin profiles after oral glucose and sucrose. These results are consistent with a specific inhibition of α-amylase in man.
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  • 7
    ISSN: 1433-8580
    Keywords: Erythrocytes ; Vitamin B12 ; Drug carrier ; Carrier erythrocytes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Resealed erythrocyte ghosts (carrier erythrocytes) are potential in vivo carriers for exogenous enzymes or drugs, but data on carrier erythrocyte survival and clearance rate in humans are not available. We have measured the in vitro efflux of vitamin B12 encapsulated in human red cell by hypo-osmotic dialysis, as a preliminary for its use as a marker for in vivo human studies. Vitamin B12 was encapsulated into erythrocytes at a relative incorporation efficiency of 60%. In vitro hemolysis of carrier erythrocytes was minimal over 40 h, but vitamin B12 was rapidly lost from the cells, effluxt/2 was 5 h, presumably by diffusion through the intact cell membrane. Vitamin B12 (Vit B12) may, nevertheless, be a suitable marker for short-term human studies on carrier erythrocyte splanchnic clearance.
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  • 8
    ISSN: 1433-8580
    Keywords: Erythrocytes ; Carrier erythrocytes ; Heparin ; Drug carrier ; Pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Encapsulation of heparin into resealed carrier erythrocytes may be useful in the prevention of thromboembolism because heparin may be released locally during retraction of fresh thrombi. Heparin encapsulation in human and canine erythrocytes was achieved by hypo-osmotic dialysis with 44% and 36% encapsulation, respectively. Encapsulated heparin did not leak from carrier erythrocytes in vitro. In vivo survival of heparin-loaded carrier erythrocytes in dogs was biphasic: After an initial phase of cell loss the carrier cells survived in circulation with a half-life of 28 h. The present results seem to warrant clinical studies with heparin-loaded carrier erythrocytes.
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  • 9
    ISSN: 1398-9995
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Allergen extracts for skin prick testing (SPT) are available from several manufacturers. Although these solutions are specified according to well-defined internal company standards, there is no generally accepted overall standardization. To assess the comparability of skin prick test solutions of various manufacturers, we compared extracts of nine different allergens from four companies by SPT in 29 children sensitive to one or more of the allergens, in a double blind fashion. RAST (Pharmacia) and EAST (Kallestad) were determined in simultaneous blood samples. Allergen extracts were also examined by rocket immunoelectrophoresis for their content of major allergens. Skin reactions, assessed by mean diameter of wheals, to identical allegen extracts varied significantly between the four vendors (P〈0.05-0.001). Correlation between RAST and EAST was good for all allergens except birch pollen and mugwort. Content of the major allergen in corresponding extracts varied significantly between the different companies (〈1%-2000%). These data underline the need for international reference extracts as intracompany standardization of test solutions alone is not enough to yield general reproducibility of skin prick test results.
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  • 10
    ISSN: 1365-2222
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Background Several studies have demonstrated that mucosal administration of soluble antigens can prevent the onset or reduce the severity of certain autoimmune diseases or allergies. Few studies exist showing the efficacy of mucosal tolerance for therapy of such diseases.Objective The aim of the present study was to modulate an allergic immune response by intranasal antigen administration in an already sensitized organism.Methods A murine model of allergic asthma to birch pollen (BP) and its major allergen Bet v 1 was utilized. Sensitized mice were intranasally treated with recombinant (r)Bet v 1 in different concentrations and at different intervals. On the day the mice were killed, blood and bronchoalveolar lavage fluids were taken and immediate type I skin tests were performed. T cell proliferation and cytokine production (interleukin (IL)-5, interferon (IFN)-γ) were measured in spleen and lung cell cultures.Results Mucosal treatment with rBet v 1 (3 × 50 µg in 4 day intervals) led to a reduction of type I skin reactions, suppressed immunoglobulin (Ig)G1/IgE antibody levels and markedly decreased IL-5 and IFN-γ production in vitro in spleen and lung cell cultures. Moreover, lung inflammation (i.e. eosinophilia and IL-5 levels in bronchoalveolar lavage fluids) was significantly suppressed by the treatment.Conclusion Our results demonstrate that intranasal treatment with rBet v 1 reduced systemic allergic immune responses as well as airway inflammation in BP-sensitized mice. We therefore suggest that mucosal tolerance induction with recombinant allergens could be a promising concept for the therapy of allergic diseases.
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