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  • 1
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and toxicology of sparsomycin in beagle dogs (1987)
    Springer
    Cancer chemotherapy and pharmacology 20 (1987), S. 115-124 
    Details
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Sparsomycin is a cytotoxic drug exhibiting a broad spectrum of in vitro activity against murine tumors and many tumor cell lines. It also appears to be a potent stimulator of the antitumor activity of cisplatin against L1210 leukemia in vivo. However, because of its toxicity, the antitumor activity of sparsomycin on murine tumors in vivo has been disappointing. The purpose of our study was to investigate the pharmacokinetics of this drug as well as the possible mechanisms that produce sparsomycin toxicity. Tests on beagle dogs revealed that about 60% of the drug is eliminated by metabolic clearance, while 40% is eliminated by the kidneys. After a single bolus injection of 0.1 mg/kg sparsomycin without narcosis, sparsomycin was eliminated with a tβ1/2 of 0.6–0.7 h, the AUC being 0.32–0.38 mg·h·1-1, and the volume of distribution (Vd) 0.26 l/kg. In addition to being subject to glomerular filtration, sparsomycin is probably also actively excreted and actively reabsorbed by the renal tubuli. Sparsomycin itself may inhibit its active tubular excretion, thus resulting in a decrease in the drug's renal clearance and its accumulation in the plasma. Sparsomycin appeared to be toxic primarily in the liver, disturbing its function and the synthesis of plasma proteins. Two out of five dogs developed hemorrhagic diathesis due to hypofibrinogenemia and deficiency of other blood-coagulation factors. Sparsomycin was not toxic to the bone marrow.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00253964
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  • 2
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of Anthracyclines in Dogs: Evidence for Structure-Related Body Distribution and Reduction to Their Hydroxy Metabolites (1984)
    Springer
    Pharmaceutical research 1 (1984), S. 33-38 
    Details
    ISSN: 1573-904X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetic disposition of the anthracyclines, adriamycin (doxorubicin), daunorubicin, 4′-epi-adriamycin, carminomycin, and 4-demethoxy-daunorubicin, and the formation of their reduced C13 hydroxy metabolites were studied in dogs. The presence of a C14hydroxy group (adriamycin and 4′epi-adriamycin) drastically reduces the appearance of the C13 hydroxy metabolites in plasma. Substitution of the C4-H with C4-OH and C4-OCH3, in this rank order, decreases the area under the plasma concentration-time curves of the parent compounds and their C13 hydroxy metabolites.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016378609450
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  • 3
    Electronic Resource
    Electronic Resource
    Comparison of the effects and disposition kinetics of articaine and lidocaine in 20 patients undergoing intravenous regional anaesthesia during day case surgery. (1998)
    Springer
    Pharmacy world & science 20 (1998), S. 88-92 
    Details
    ISSN: 1573-739X
    Keywords: Articaine ; Lidocaine ; Intravenous regional analgesia ; Elimination kinetics ; Disposition
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The aim of this investigation was to assess the effects and dispostion kinetics of the local anaesthetic drugs (±)articaine and lidocaine during intravenous regional anaesthesia (IVRA). The mean onset time of surgical analgesia of articaine was 2.5±1.1 min and that of lidocaine 11.2 ± 5.1 min (p = 0.0006). None of the patients exhibited objective symptoms of toxicity, either local or systemic, during injection of articaine or lidocaine, nor were there any subjective complaints. No changes in blood pressure, heart rate or oxygen saturation were observed with these local anesthetics at any time during the procedure, nor after deflation of the tourniquet. After releasing the tourniquet, articaine appears in the blood and is rapidly eliminated with a t1/2a of 5±3 min and a t1/2β of 59±39 min due to hydrolysis. Lidocaine is rapidly and biexponentially eliminated with similar half‐lives of t1/2a of 4±2 min and a t1/2β of 79±31 min. Total body clearance of articaine (8.9±3.5 L/min) is ten times greater than that of lidocaine (0.9±0.4 L/min; p = 0.0005). We concluded that both (±)articaine and lidocaine are suitable and safe agents for IVRA with rapid onset of good surgical anaesthesia. Articaine is a racemic mixture, which is nowadays considered as less favourable. After releasing the tourniquet, articaine is eliminated with a t1/2β of 60 min and lidocaine with a t1/2β of 80 min. Quicker onset and shorter elimination time favours (±)articaine over lidocaine for IVRA in day case settings so that patients treated with articaine will be ‘drug free’ more quickly than those who receive lidocaine. Faster elimination and more rapid onset are important advantages for articaine in IVRA for day‐case procedures.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1008622018161
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  • 4
    Electronic Resource
    Electronic Resource
    Influence of protein binding and severity of illness on renal elimination of four cephalosporin drugs in intensive-care patients (1987)
    Springer
    Pharmacy world & science 9 (1987), S. 98-103 
    Details
    ISSN: 1573-739X
    Keywords: Cefoxitin ; Ceftazidime ; Ceftriaxone ; Cefuroxime ; Chromatography, high pressure liquid ; Kidney diseases ; Pharmacokinetics ; Protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A pharmacokinetic study after a single dose of ceftriaxone, cefoxitin, cefuroxime and ceftazidime was performed to investigate the influence of protein binding and severity of disease on the renal elimination. In intensive-care patients drug-protein binding was substantially less compared to that in volunteers and patients with less complicated diseases. This did not result in increased elimination but, due to increased apparent volumes of distribution, prolonged half-life times were observed. Consequently, in patients with complicated disease states a dosage regimen should be based on pharmacokinetic studies performed in a similar patient group.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01960743
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of the antitumor antibiotic n-pentyl-sparsomycin in beagle dogs (1990)
    Springer
    Investigational new drugs 8 (1990), S. 25-32 
    Details
    ISSN: 1573-0646
    Keywords: sparsomycin ; n-pentyl-sparsomycin ; pharmacokinetics ; beagle dogs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary N-pentyl-sparsomycin (PSm) is a lipophilic analogue of sparsomycin (Sm), which is a well known inhibitor of protein synthesis. This compound was selected for preclinical pharmacokinetic studies because of its high in vitro and in vivo antitumor activity. In this study in which the drug was evaluated in beagle dogs under anaesthesia, the drug concentrations in plasma, urine and bile samples were determined using high performance liquid chromatography (HPLC). Plasma protein binding was approximately 54%. The mean t1/2 β was 0.2 hours (12 minutes) and t1/2 τ was 0.75 ± 0.1 hours (45 ± 6 minutes). During continuous infusions up to 5.25 hours, the steady state was reached in 3 out of 6 experiments, suggesting that in some cases the real t1/2 τ was longer than measured. PSm was actively reabsorbed from the renal tubuli. This process was saturable at the higher doses. Tubular reabsorption played only a minor role in pharmacokinetics as most of the drug (67%) was eliminated by the non-renal clearance. The non-renal clearance was saturable at higher doses of PSm and was the reason for non-linearity of pharmacokinetics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00216921
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  • 6
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and Anticonvulsant Activity of Three Monoesteric Prodrugs of Valproic Acid (1991)
    Springer
    Pharmaceutical research 8 (1991), S. 750-753 
    Details
    ISSN: 1573-904X
    Keywords: valproic acid ; esteric prodrugs ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of valproic acid (VPA) were compared in dogs with those of the prodrugs ethyl valproate (E-VPA), trichloroethyl valproate (T-VPA), and valproyl valproate (V-VPA). Valproic acid, E-VPA, T-VPA, and V-VPA were administered intravenously and orally to six dogs at equimolar doses. The three VPA prodrugs were rapidly converted to VPA. The biotransformation was complete in the case of E-VPA and T-VPA but was only partial in the case of V-VPA. Because of the rapid conversion to the parent drug, after administration of the prodrugs, VPA plasma levels did not yield a sustained-release profile. Further, the anticonvulsant activity of prodrugs was compared in mice to that of VPA and valpromide (VPD). The anticonvulsant activity of E-VPA, T-VPA, and V-VPA was less than that of VPA.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015854118110
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  • 7
    Electronic Resource
    Electronic Resource
    Analysis of N4-trideuteroacetylsulphamerazine and its metabolites sulphamerazine and N4-acetylsulphamerazine in man by means of high-performance liquid chromatography and mass spectrometry (1983)
    Chichester : Wiley-Blackwell
    Biological Mass Spectrometry 10 (1983), S. 114-119 
    Details
    ISSN: 0306-042X
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The synthesis, high-performance liquid chromatographic and mass spectrometric analysis of N4-trideuteroacetylsulphamerazine is described. N4-trideuteroacetylsulphamerazine in man is deacetylated into sulphamerazine, which in turn is acetylated again into N4-acetylsulphamerazine. The existence of a deacetylationacetylation equilibrium in man has been demonstrated.
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/bms.1200100303
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