COMPARATIVE PHARMACOKINETICS AND EFFECT ON THE HEMODYNAMICS OF ORIGINAL AND GENERIC NEBIVOLOL IN HEALTHY VOLUNTEERS

Beta-blockers are an important part of modern pharmacotherapy in cardiology. The introduction of generics into clinical practice requires clear evidence of bioequivalence to the original drug.Aim. To study the pharmacokinetics and effect on hemodynamic parameters of the original and a generic nebivolol in healthy volunteers in the fasting state. Material and methods. 18 healthy volunteers were included into the randomized open study on cross-balanced design. They received single dose (5 mg) of two compared preparations of nebivolol under fasting condition. The concentration of unchanged nebivolol in blood plasma was determined by gas chromatography-tandem mass spectrometry. Calculation of pharmacokinetic parameters and assessment of the hemodynamic were performed.Results. The concentrations of nebivolol after the original and generic drugs intake did not differ significantly in any time point (AUC0-∞ 41.09±46.82 vs 47.16±66.58 ng•hr/mL and T1/2 30.84±10.78 vs 29.59±12.08 hours, respectively). Blood pressure reduction was slightly more pronounced when taking generic nebivolol, while the reduction in heart rate at 2 and 4 hours – after original nebivolol intake.Conclusion. A comparative pharmacokinetic study of the genetic nebivolol showed its bioequivalence to the original drug. The effect on hemodynamic parameters with single dose (5 mg) of generic and original nebivolol in healthy volunteers was comparable

Myocarditis mimicking acute coronary syndrome - the role of cardiac magnetic resonance imaging in the diagnosis

Myocarditis is an inflammatory disease of myocardium with a wide range of clinical presentations. Myocarditis may mimic acute coronary syndrome (ACS) and adequate differential diagnosis is not possible by conventional tests. Cardiac magnetic resonance (CMR) has emerged as a leading imaging modality in the diagnosis of myocarditis in such patients. Here, we report three cases of myocarditis mimicking ACS with normal coronary arteries. CMR was used for confirming the diagnosis of myocarditis in all three patients presented here

Long-range intramolecular S -> N acyl migration: a study of the formation of native peptide analogues via 13-, 15-, and 16-membered cyclic transition states

The intramolecular long-range S -> N acyl migration via 13-, 15-, and 16-membered cyclic transition states to form native tetra- and pentapeptide analogues was studied on S-acylcysteine peptides containing beta- or gamma-amino acids. The pH-dependency study of the acyl migration via a 15-membered cyclic transition state indicated that the reaction is favored at a pH range from 7.0 to 7.6. Experimental observations are supported by structural and computational investigations