RESUMO
INTRODUCTION: Ainuovirine/lamivudine/tenofovir is a novel antiretroviral therapy regimen used to treat human immunodeficiency virus-1 (HIV-1) infection. This study aimed to compare the pharmacokinetics of ainuovirine/lamivudine/tenofovir in HIV-1-infected patients aged ≥ 65 (elderly patients) and ≤ 40 years (young patients). METHODS: This prospective, open-label, parallel controlled clinical study included 15 young and 15 elderly patients. Blood (1 mL) was collected 30 min before dosing and at 0.5, 1, 1.5, 2, 3, 4, 8, 12, 16, and 24 h after dosing, to measure the plasma concentrations of ainuovirine/lamivudine/tenofovir. Safety was assessed by monitoring the adverse events, physical examinations, and clinical laboratory tests. RESULTS: Plasma concentrations of each ainuovirine/lamivudine/tenofovir component reached peak levels 1-4 h after dosing and gradually decreased during the remaining observation period. Compared with the young group, ainuovirine had significantly higher T1/2Ke, AUC0-24, and AUC0-inf (all P < 0.05) in the elderly group, whereas Ke (P = 0.002) was significantly lower. However, the Cmax and Tmax of ainuovirine did not differ significantly. Lamivudine and tenofovir also had a significantly higher Cmax (p = 0.004 and p = 0.008, respectively) and AUC0-inf (P = 0.014 and P = 0.006, respectively) in the elderly group, whereas there was no significant difference in Tmax, Ke, and T1/2Ke. Ainuovirine/lamivudine/tenofovir was well tolerated in both the young and elderly groups. CONCLUSION: This study suggests that the ainuovirine/lamivudine/tenofovir regimen might be an effective and safe treatment regimen for HIV-1-infected patients aged ≥ 65 years and ≤ 40 years. Further studies are needed to confirm these results and develop optimal dosing regimens for elderly HIV-1-infected patients.
RESUMO
Acute gastric mucosal lesions (AGM lesions) is a general term applied to conditions characterized by the acute development of mucosal lesions in the form of erythema, mucosal hemorrhage, erosions and ulcerations in the mucosa of the stomach and duodenum. Although the pathopphysiological events leading to the formation of these lesions remain unknown, we do know that they are after preceded by one of many situations. It has become traditional to use the term stress ulcer to describe AGM lesions proceded by a major stress such as that of an operation or of severe thermal burns or hemorrhagic shock. The silent clinical manifestation of acute gastric mucosal lesions, regardless of their cause, is bleeding. AGM lesions were experimentally produced by brain injury and administration of steroid. This experimental study was conducted in order to study the so called AGM lesions, especially on production and pathology of them. This experimental animals, normal adult rate, were divided into 4 groups the first group of brain injury, the second group of brain injury and administration of steroid, the third group of administration of steroid only, and the fourth group of normal control with administration of normal saline and normal rats. The frequency of AGM lesions was studied in relation to each experimental group, experimental period and grade of lesions. The AGM lesions were divided into 3 grades depending on the macroscopic and microscopic findings. 1. AGM lesions were observed in 34 out of 63 all experimental animals except for control group of animal. Majority of the lesions were found in the glandular portion of the stomach. 2. In the brain injured group, the lesions that was erythematous and superficial mucosal erosion were found in 3 out of 21(14.3%), which were observed only in experimental period of 3-5 days. 3. In the group with brain injury and steroid administration, the lesions were found in 16 out of 21 animals(76.2%) among them grade 1 was in 2 out of 16, grade 2 in 10 and grade 3 in 4, which observed in the period of 2-7 days. 4. In the group with administration of steroid, the lesions were found in 15 out of 21 animals(71.4%), among them grade 1 was 2 out of 15, grade 2 in 11 and grade 3 in 2, which started to be observed form 2nd day through out the experimental period. 5. No lesions were investigated in the control group. No correlation between the variety of brain injury and production of AGM lesion was studied.