(1) Background: This study was planned to assess the concentration of antihypertensive drugs (AHD) in the blood serum in patients with controlled and uncontrolled arterial hypertension (AH). (2) Methods: We assessed 46 patients with AH. Based on the results of 24 h blood pressure monitoring (ABPM), the patients were randomized into two groups. The first group consisted of the patients with controlled AH; the second group consisted of the patients with uncontrolled AH. Venous blood was taken in both groups of patients in the morning before and 2 h after taking drugs to assess the concentration of lisinopril, amlodipine, valsartan, and indapamide. (3) Results. The first group included 27 patients, and the second group 19 patients. In patients with uncontrolled AH, the median concentrations of lisinopril, indapamide, amlodipine, and valsartan before and after taking the drugs did not differ from patients who reached the target BP values. (p > 0.05). In some patients with uncontrolled and controlled (shown for the first time) AH the concentration of AHD was below the limit of quantitative determination. (4) Conclusions. The obtained results indicate that the pharmacokinetics of AHD, apparently, does not play a significant role in the development of ineffectiveness of the ongoing therapy for AH. Therapeutic drug monitoring can be used to test adherence to the treatment.
INTRODUCTION: Metoprolol is a selective β1-adrenoblocker without intrinsic sympathomimetic activity. The effectiveness of metoprolol has been proven in numerous clinical studies in the treatment of arterial hypertension, stable angina, myocardial infarction, chronic heart failure. To improve the efficiency and safety of the therapy, it is advisable to carry out therapeutic drug monitoring of metoprolol, which requires a sensitive method for its quantitative determination. AIM: To develop, validate and test a method for the determination of metoprolol in human plasma using high performance liquid chromatography (HPLC) with tandem mass spectrometric detection (MS/MS). MATERIALS AND METHODS: The work was performed on Ultimate 3000 TSQ Fortis HPLC-MS/MS (Thermo Fisher, USA). For sample preparation, acetonitrile was used with fexofenadine hydrochloride at a concentration of 10 ng/ml as an internal standard, which was added to plasma samples in 3:1 ratio. The volume of the injected sample was 5 μl. Separation was performed on UCT Selectra C18 4.6 mm × 100 mm, 3 um, 100 A column with a similar pre-column at 35°C, in gradient elution mode in proportion of 0.1% formic acid solution/acetonitrile: 0 min — 80%/20%, 0.1 min — 45%/55%, 5 min — 10%/90%, 10 min — 80%/20%, at flow rate of 300 µl/min. Detection was performed in positive electrospray ionization mode, electrospray voltage 4000 V, sheath gas 50 arb, auxiliary gas 10 arb, purge gas 1 arb, evaporator temperature 350°C, ion transport tube temperature 300°C, using the multiple reaction monitoring mode (MRM) at argon flow rate 2 mTorr, 268 m/z → 115.5 m/z, Collision Energy 18 V, Tube lens 95 V, 268 m/z → 191 m/z, Collision Energy 17 V, Tube lens 95 V. The blood plasma of healthy volunteers served as matrix. RESULTS: The analytical range of the technique was 2–1000 ng/ml. The developed technique was tested on a patient with arterial hypertension. During the analysis, an equilibrium concentration of metoprolol of 12.0 ng/ml was detected in the patient's blood plasma (previously, the patient took metoprolol tartrate at a dose of 12.5 mg twice a day for a week), and in 2 hours after taking the drug — 31.0 ng/ml. CONCLUSION: A method for the quantitative determination of metoprolol in human blood plasma using HPLC-MS/MS has been developed, validated and tested.
INTRODUCTION: Despite the recently established evidence-based and systemic approach to treatment for arterial hypertension (AH), not in all cases its control can be achieved. AIM: To conduct a comparative analysis of the concentration of antihypertensive drugs (AHTDs) in blood serum of patients with controlled and uncontrolled AH. MATERIALS AND METHODS: Fifty six patients were included. Inclusion criteria: age 18 years, signing of informed consent, established diagnosis of AH, regular intake of any two of study antihypertensive drugs (lisinopril, amlodipine, valsartan) and also of indapamide at stable doses, for women adequate contraception. According to the results of daily monitoring of the arterial pressure (AP), patients were divided into two groups: the first group controlled hypertension (AP 140/90 mmHg; n = 39), the second uncontrolled hypertension (AP 140/90 mmHg; n = 17). The mean age of patients in the first group was 65.03 10.80 years, in the second 63.50 8.31 (p = 0.576). In the first group, women prevailed (64.1% vs. 35.3%, p = 0.047) and the mean body mass index was lower (26.30 1.38 kg/m2 vs. 32.20 4.15 kg/m2, p = 0.02). In patients of both groups, venous blood was taken in fasting condition in the morning and 2 hours after intake of AHTDs to assess their concentration by high-performance liquid chromatography. The analytical range for lisinopril, indapamide, amlodipine was 5500 ng/ml, for valsartan 1010,000 ng/ml. RESULTS: In the first group, equilibrium concentration of lisinopril was 2.67 times higher (p = 0.053), and concentration of indapamide in 2 hours after intake was 1.83 times higher (р = 0,084); when normalized to the dose, the differences were leveled out (p 0.05). Concentrations of amlodipine and valsartan did not differ between the groups both before and 2 hours after intake (p 0.05). In 3 of 39 (7.7%) patients with controlled hypertension and in one of 17 patients (5.9%, p = 1.0) with uncontrolled hypertension, AHTDs were detected in blood serum, which were not administered to them. CONCLUSIONS: Results of the pilot part of the study (n = 56) demonstrated the absence of difference between the mean concentrations of the study AHTDs in the blood serum of patients with controlled and uncontrolled AH, and in some cases the presence of traces of AHTDs not administered by the doctor.
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