An aim of the study was to assess the severity of the syndrome of nonspecific metabolic endogenous intoxication (EI) and characteristics of compensatory reaction of serum albumin (SA) in patients in the early restoration period (4-5 months) of ischemic stroke (II). We measured levels of middle-sized molecules (MSM) and malonic dialdehyde (MDA) and determined parameters of functional activity of SA in 30 patients (mean age 69±8 years) after the first II and in 17 age- and sex-matched healthy people. Neurological deficit and functional restoration of patients were assessed with the NIHSS and Barthel index. The increase of MSM and MDA concentrations was found in 98% and 88% patients, respectively, as compared to healthy people (p<0,01). These metabolic disturbances were associated with the formation of EI and caused functional-structural changes of SA molecules. The correlation between changes of effective concentrations of SA and MDA was characteristic of the group of patients with II. The increase of total SA concentration was found in 87% of cases compared to controls (p<0,01) that indicated the manifestation of compensatory reaction of SA in response to EI. The decrease of all SA parameters, including the total concentration, was noted in 13% of patients and was associated with the decompensatory reaction to SA. The rehabilitation of CNS dysfunctions was associated with the undamaged SA compensatory reaction. The functional-structural changes of SA molecules in patients in the restoration period of II may lead to the changes in drug disposition, i.e. pharmacokinetics and pharmacodynamics, thus reducing possibilities of rehabilitation therapy.