Примери за използване на Ara-g на Английски и техните преводи на Български
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Nelarabine and ara-G are partially eliminated by the kidneys.
Nelarabine is a pro-drug of the deoxyguanosine analogue ara-G.
Gender has no effect on nelarabine or ara-G plasma pharmacokinetics.
Age has no effect on the pharmacokinetics of nelarabine or ara-G.
The apparent clearance of ara-G(Ci/F) is comparable between the two groups 9.5 l/h/m.
Ara-G is excreted by the kidney to a greater extent(20 to 30% of the administered nelarabine dose).
The effect of race on nelarabine and ara-G pharmacokinetics has not been specifically studied.
Renal clearance averaged 9.0 l/ h/ m2(151%) for nelarabine and2.6 l/ h/ m2(83%) for ara-G in 21 adult patients.
Nelarabine and ara-G are not substantially bound to human plasma proteins(less than 25%) in vitro.
Decreased renal function, which is more common in the elderly,may reduce ara-G clearance(see section 4.2).
Mean plasma ara-G Cmax and AUCinf values were 115 µM(16%) and 571 µM. h(30%), respectively.
The principal route of metabolism for nelarabine is O-demethylation by adenosine deaminase to form ara-G, which undergoes hydrolysis to form guanine.
Mean plasma ara-G Cmax and AUCinf values were 60.1 µM(17%) and 212 µM.h(18%), respectively.
In a pharmacokinetic/ pharmacodynamic cross study analysis, race had no apparent effect on nelarabine, ara-G, or intracellular ara-GTP pharmacokinetics.
Nelarabine and ara-G are rapidly eliminated from plasma with a half-life of approximately 30 minutes and 3 hours, respectively.
In 28 adult patients, 24 hours after nelarabine infusion on day 1,mean urinary excretion of nelarabine and ara-G was 5.3% and 23.2% of the administered dose, respectively.
The pharmacokinetics of nelarabine and ara-G have not been specifically studied in renally impaired or haemodialysed patients.
Combined Phase 1 pharmacokinetic data at nelarabine doses of 104 to 2,900 mg/ m2 indicate that the clearance(Cl) andVss values for nelarabine and ara-G are comparable between the two groups.
Further data with respect to nelarabine and ara-G pharmacokinetics in the paediatric population are provided in other subsections.
Plasma ara-G Cmax values generally occurred at the end of the nelarabine infusion and were generally higher than nelarabine Cmax values, suggesting rapid and extensive conversion of nelarabine to ara-G. .
In a cross-study analysis using data fromfour Phase I studies, the pharmacokinetics of nelarabine and ara-G were characterized in patients aged less than 18 years and adult patients with refractory leukaemia or lymphoma.
Nelarabine and ara-G are extensively distributed throughout the body based on combined Phase I pharmacokinetic data at nelarabine doses of 104 to 2,900 mg/m2.
No accumulation of nelarabine or ara-G was observed in plasma after nelarabine administration on either a daily or a day 1, 3, 5 schedule.
Nelarabine and ara-G did not significantly inhibit the activities of the major hepatic cytochrome P450(CYP) isoenzymes CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 in vitro.
The mean apparent clearance(Cl/ F) of ara-G was about 7% lower in patients with mild renal impairment than in patients with normal renal function(see section 4.2).
Nelarabine and ara-G are not substantially bound to human plasma proteins(less than 25%) in vitro, and binding is independent of nelarabine or ara-G concentrations up to 600 µM.
The apparent clearance of ara-G(Cl/ F) is comparable between the two groups[9.5 l/ h/ m2(35%) in adult patients and 10.8 l/ h/ m2(36%) in paediatric patients] on day 1.
Nelarabine and ara-G did not significantly inhibit the activities of the major hepatic cytochrome P450(CYP) isoenzymes CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 in vitro.