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The effectiveness of antihypertensive treatment remains at a low level despite of numerous antihypertensives. Nitric oxide (NO) plays an important role in the pathogenesis of arterial hypertension (AH). It is synthesized from L-arginine in the presence of endothelial NO-synthase but the practical use of the above mentioned amino acid in the treatment of AH remains uncertain. In this study a total of 80 adult patients (men and women in equivalent amounts) with AH II stage were recruited. The whole group of patients was divided into 2 subgroups according to the prescribed antihypertensive pharmacotherapy: 1st subgroup (n=40) used Valsartan 0.08 g per os once a day in the morning + Amlodipinum 0.005 g per os once a day in the evening; 2nd subgroup (n=40) in addition to the above mentioned medicines used L-arginine 1.0 g three times a day before meal. To estimate the efficacy of treatment and its metabolic effects were evaluated the following parameters: systolic and diastolic blood pressure, glucose, total cholesterol, high- and low- density lipoproteins, triglycerides. The period of clinical observation was 30 days. All patients had different neurological complaints, such as: anxiety, headache, loss of concentration, insomnia, dizziness, fatigue. At the end of clinical observation their quantity and expressiveness decreased, especially in the 2nd group. One patient even required lower dose of L-arginine (2.0 g/day) because of the significant daytime sleepiness. After the correction of pharmacotherapy this complaint disappeared. In 5 patients the use of L-arginine before meal caused gastrointestinal disorders, such as nausea, flatulence and epigastric discomfort. That is why they began to use this medicine during or after meal. Such change in the treatment didn’t reduce the effectiveness of L-arginine. In 30 days the levels of systolic and diastolic blood pressure decreased, especially in the 2nd group of comparison (p<0.05). The effectiveness of antihypertensive therapy in the 1st group was 78%, the optimal levels of blood pressure were achieved after 12-14 days of treatment. Patients of the 2nd group achieved stable levels of blood pressure in 10-12 days, but in 10 patients the dose of Amlodipin was reduced to 0.0025 mg/day because of the threat of hypotension. In this study had not found any effects of L-arginine on levels of glucose, total cholesterol, high- and low- density lipoproteins, triglycerides (p>0.05). Absence of significant effect of L-arginine on the levels of blood glucose and lipids allows to use it in patients with different risk factors or comorbid pathology.