利伐沙班片可以长期吃吗
(Rivaroxaban) is a new anticoagulant drug that is rapidly absorbed after oral administration and has an average half-life of 7 to 13 hours. It has the advantages of high bioavailability, stable anticoagulant effect, high selectivity, and obvious therapeutic effect. Patients can benefit greatly from taking this drug consistently. Under normal circumstances, as long as there are no obvious contraindications and the instructions are strictly followed or the doctor's advice is followed, patients with indications can use rivaroxaban tablets for a long time.
Studies have shown that rivaroxaban inhibits the activity of factor xa in a dose-dependent manner. The strongest inhibition occurs 1 to 4 hours after administration. When a single dose of 5 to 80 mg is taken, the maximum inhibition rate is 20% to 61%. After multiple doses per day, there is no significant difference in the maximum inhibition of factor xa activity. Rivaroxaban prolongs the prothrombin time (PT) and activated partial thromboplastin time (APTT) in a dose-dependent manner, and the degree of inhibition of factor Xa activity is closely related to the plasma concentration of rivaroxaban.
A dose escalation study on the pharmacokinetics and pharmacodynamics of 48 healthy elderly volunteers (60-76 years old) showed that a single dose of rivaroxaban within 40 mg has predictable pharmacokinetic and pharmacodynamic characteristics and reaches the maximum pharmacokinetic and pharmacodynamic effects. At this time, the anticoagulant effect is optimal. In this age range, the half-life of rivaroxaban is 11-13 hours.
Another randomized, single-blind, placebo-controlled, parallel-group trial tested 34 subjects in a single oral dose of 10 After mg of rivaroxaban, the effects of age and gender on the pharmacokinetics and pharmacodynamic parameters of rivaroxaban were studied. The results showed that gender had no effect on the pharmacokinetics and pharmacodynamic parameters. Compared with the young group (18-45 years old) in the elderly group (over 75 years old), the pharmacokinetic parameter Auc value increased by 41%, while Cmax did not change significantly. The pharmacodynamic parameter xa factor inhibition rate was enhanced, and PT was prolonged, but at 24 It can return to close to baseline levels within hours, so the changes in pharmacokinetic and pharmacodynamic parameters in the elderly group are not clinically significant, and there is no need to adjust the dose (i.e. Xarelto) during clinical use.
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