ACTIVE METABOLITE AFFECTS THE KINETICS OF LORCAINIDE

InPharma ◽  
1983 ◽  
Vol 377 (1) ◽  
pp. 10-10
Keyword(s):  
Active Metabolite ◽  
Kinetics Of

scholarly journals Tissue Accumulation Kinetics of Ciclesonide‐active Metabolite and Budesonide in Mice

2013 ◽  
Vol 112 (6) ◽  
pp. 401-411 ◽  
Author(s):  
Ulla Mårs ◽  
Roland d'Argy ◽  
Karin Hallbeck ◽  
Anna Miller‐Larsson ◽  
Staffan Edsbäcker
Keyword(s):  
Active Metabolite ◽  
Tissue Accumulation ◽  
Accumulation Kinetics ◽  
Kinetics Of

[1H,15N] N.M.R. Kinetic Studies of Reactions of cis- and trans-[PtCl2(15NH3)(c-C6H1115NH2)] with Guanosine 5'-Monophosphate

1999 ◽  
Vol 52 (3) ◽  
pp. 173 ◽  
Author(s):  
Sarah J. Barton ◽  
Kevin J. Barnham ◽  
Abraha Habtemariam ◽  
Urban Frey ◽  
Rodney E. Sue ◽  
...  
Keyword(s):  
Trans Isomer ◽  
Active Metabolite ◽  
Kinetic Studies ◽  
Trans Influence ◽  
Trans Complex ◽  
Kinetics Of Reaction ◽  
Cis And Trans ◽  
Kinetics Of ◽  
Cis Isomer ◽  
Amine Ligand

cis-[PtCl2(15NH3)(c-C6H11NH2)] is an active metabolite of the oral platinum(IV) anticancer drug cis,trans,cis-[PtCl2(CH3CO2)2(NH2)(c-C6H11NH2)]. Since it is likely that guanine bases on DNA are targets for this drug, we have analysed the kinetics of reaction of this platinum(II) metabolite with guanosine 5′-monophosphate (5′-GMP) at 310 K, pH 7, using [1H, 15N] n.m.r. methods. Reactions of the trans isomer are reported for comparison. The reactions proceed via aquated intermediates, and, for the cis isomer, the rates of aquation and substitution of H2O by 5′-GMP are 2-5 times faster trans to the amine ligand (c-C6H11NH2) compared to trans to NH3 for both the first and second steps. For the trans complex, the first aquation step is c. 3 times faster than for the cis complex, as expected from the higher trans influence of Cl¯, whereas the rate of the second aquation step (trans to N7 of 5′-GMP) is comparable to that trans to NH3. These findings have implications for the courses of reactions with DNA.

Steady-State Kinetics of Proguanil and Its Active Metabolite, Cycloguanil, in Man

Chemotherapy ◽  
1988 ◽  
Vol 34 (5) ◽  
pp. 385-392 ◽  
Author(s):  
M.D. Edstein ◽  
J.R. Veenendaal ◽  
H.V. Scott ◽  
K.H. Rieckmann
Keyword(s):  
Steady State ◽  
Active Metabolite ◽  
Steady State Kinetics ◽  
Kinetics Of

scholarly journals Bradykinin and des-Arg9-bradykinin metabolic pathways and kinetics of activation of human plasma

2001 ◽  
Vol 281 (1) ◽  
pp. H275-H283 ◽  
Author(s):  
Mélanie Cyr ◽  
Yves Lepage ◽  
Charles Blais ◽  
Nicole Gervais ◽  
Massimo Cugno ◽  
...  
Keyword(s):  
Metabolic Pathways ◽  
Active Metabolite ◽  
Ace Inhibitor ◽  
Healthy Individuals ◽  
High Molecular Weight Kininogen ◽  
Plasma Activation ◽  
Significant Difference ◽  
Inflammatory Processes ◽  
Aminopeptidase P ◽  
Kinetics Of

In the serum of 116 healthy individuals, exogenous bradykinin (BK) half-life (27 ± 10 s) was lower than that of des-Arg9-BK (643 ± 436 s) and was statistically different in men compared with women. The potentiating effect of an angiotensin-converting enzyme (ACE) inhibitor was, however, more extensive for BK (9.0-fold) than for des-Arg9-BK (2.2- fold). The activities of ACE, aminopeptidase P (APP), and kininase I were respectively 44 ± 12, 22 ± 9, and 62 ± 10 nmol · min−1· ml−1. A mathematical model ( y = ktαe−β t, t > 0), applied to the BK kinetically released from endogenous high-molecular-weight kininogen (HK) during plasma activation in the presence of an ACE inhibitor, revealed a significant difference in the rate of formation of BK between men and women. For des-Arg9-BK, the active metabolite of BK, the rate of degradation was higher in women compared with men, correlating significantly with serum APP activity ( r2= 0.6485, P < 0.001). In conclusion, these results constitute a basis for future pathophysiological studies of inflammatory processes where activation of the contact system of plasma and the kinins is involved.

Kinetics of Methaemoglobin Production (2). Kinetics of the Cyanide Antidote p-Aminopropiophenone During Oral Administration

1986 ◽  
Vol 5 (5) ◽  
pp. 303-307 ◽  
Author(s):  
J.E. Bright ◽  
T.C. Marrs
Keyword(s):  
Regression Analysis ◽  
Kinetic Model ◽  
Active Metabolite ◽  
Least Squares Regression ◽  
Analysis Program ◽  
Linear Least Squares ◽  
Cyanide Antidote ◽  
First Pass ◽  
Kinetics Of ◽  
Simulation Package

The kinetics of methaemoglobin production by orally administered p-aminopropiophenone (PAPP) was studied by using a kinetic model previously developed to describe methaemoglobinaemia consequent on intravenous injection of PAPP. Both ISIS, a simulation package, and NONLIN, a non-linear least-squares regression analysis program, were used to analyse the data. Some modification of the model was necessary to describe oral profiles and 40-50% of the administered PAPP appeared to be being metabolized at first pass to a non-active metabolite.

Single-Dose Kinetics of an Enteric-Coated Formulation of Carbamazepine-10,11-epoxide, an Active Metabolite of Carbamazepine

1988 ◽  
Vol 10 (4) ◽  
pp. 386-389 ◽  
Author(s):  
Edoardo Spina ◽  
Torbjörn Tomson ◽  
Jan-Olof Svensson ◽  
DRJohann W. Faigle ◽  
Leif Bertilsson ◽  
...  
Keyword(s):  
Single Dose ◽  
Active Metabolite ◽  
Enteric Coated ◽  
Kinetics Of

Direct observations of radiation-enhanced transformations in glass

1983 ◽  
Vol 41 ◽  
pp. 354-355
Author(s):  
J. F. DeNatale ◽  
D. G. Howitt
Keyword(s):  
Glass Matrix ◽  
Diffusion Mechanism ◽  
Bubble Formation ◽  
Silicate Glasses ◽  
Phase Decomposition ◽  
Direct Observations ◽  
Thin Foils ◽  
Oxygen Bubble ◽  
Electron Energy Loss ◽  
Kinetics Of

The electron irradiation of silicate glasses containing metal cations produces various types of phase separation and decomposition which includes oxygen bubble formation at intermediate temperatures figure I. The kinetics of bubble formation are too rapid to be accounted for by oxygen diffusion but the behavior is consistent with a cation diffusion mechanism if the amount of oxygen in the bubble is not significantly different from that in the same volume of silicate glass. The formation of oxygen bubbles is often accompanied by precipitation of crystalline phases and/or amorphous phase decomposition in the regions between the bubbles and the detection of differences in oxygen concentration between the bubble and matrix by electron energy loss spectroscopy cannot be discerned (figure 2) even when the bubble occupies the majority of the foil depth.The oxygen bubbles are stable, even in the thin foils, months after irradiation and if van der Waals behavior of the interior gas is assumed an oxygen pressure of about 4000 atmospheres must be sustained for a 100 bubble if the surface tension with the glass matrix is to balance against it at intermediate temperatures.

Irradiation behavior of pyrolytic silicon carbide

1983 ◽  
Vol 41 ◽  
pp. 72-73
Author(s):  
R. J. Lauf
Keyword(s):  
Silicon Carbide ◽  
Fission Products ◽  
Thermodynamics And Kinetics ◽  
Neutron Fluences ◽  
Fuel Particles ◽  
Sic Coatings ◽  
Irradiation Behavior ◽  
Kinetics Of ◽  
Htgr Fuel

Fuel particles for the High-Temperature Gas-Cooled Reactor (HTGR) contain a layer of pyrolytic silicon carbide to act as a miniature pressure vessel and primary fission product barrier. Optimization of the SiC with respect to fuel performance involves four areas of study: (a) characterization of as-deposited SiC coatings; (b) thermodynamics and kinetics of chemical reactions between SiC and fission products; (c) irradiation behavior of SiC in the absence of fission products; and (d) combined effects of irradiation and fission products. This paper reports the behavior of SiC deposited on inert microspheres and irradiated to fast neutron fluences typical of HTGR fuel at end-of-life.

The Ordered Phase Formation in Ti-Al-Ga Alloys

1970 ◽  
Vol 28 ◽  
pp. 440-441
Author(s):  
Shiro Fujishiro ◽  
Harold L. Gegel
Keyword(s):  
Thermal Stability ◽  
High Temperature ◽  
Titanium Alloys ◽  
Growth Kinetics ◽  
Stoichiometric Composition ◽  
Good Potential ◽  
Alpha Titanium ◽  
Cold Rolled ◽  
Kinetics Of ◽  
Thermal Stability Of

Ordered-alpha titanium alloys having a DO19 type structure have good potential for high temperature (600°C) applications, due to the thermal stability of the ordered phase and the inherent resistance to recrystallization of these alloys. Five different Ti-Al-Ga alloys consisting of equal atomic percents of aluminum and gallium solute additions up to the stoichiometric composition, Ti3(Al, Ga), were used to study the growth kinetics of the ordered phase and the nature of its interface.The alloys were homogenized in the beta region in a vacuum of about 5×10-7 torr, furnace cooled; reheated in air to 50°C below the alpha transus for hot working. The alloys were subsequently acid cleaned, annealed in vacuo, and cold rolled to about. 050 inch prior to additional homogenization

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