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Biomedical subjects

P Pavek

Publications and source records attributed to P Pavek.

18 recordsLinked to original sources

Stereoselective pharmacokinetics of flobufen in rats.

Stereoselectivity of the pharmacokinetics of the nonsteroidal anti-inflammatory drug flobufen, 4-(2', 4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid, was studied in male Wistar rats after intravenous administration. Pharmacokinetic parameters and chiral inversion of flobufen enantiomers were studied after a bolus injection of the racemate and individual enantiomers (5 mg/kg). Determinations of the enantiomers in rat plasma were performed using chiral HPLC (terguride column). After i.v. administration of flobufen racemate, plasma levels of R-enantiomer decreased more rapidly. The S-/R-enantiomer ratio of AUCs after rac-flobufen was 13.3. The total plasma clearance value of S-flobufen was more than 10-fold lower than R-flobufen. The other pharmacokinetic parameters of the enantiomers were also significantly different. While only traces of R-enantiomer (less than 1%) were detected in rat plasma after S-flobufen administration, considerable conversion to the S-enantiomer was found after injection of R-flobufen (R-enantiomer AUC/S-enantiomer AUC = 0.52). The results indicate substantial stereoselectivity in the disposition of flobufen enantiomers in the rat, which is, at least in part, attributed to chiral bioconversion.

Animals↗

[Echocardiographic and hemodynamic studies on the influence of verapamil in hypertrophic obstructive cardiomyopathy (author's transl)].

15 patients with obstructive hypertrophic cardiomyopathy were studied by m-mode echocardiography and 9 of them also by left heart catheterism before and after 10 mg Verpamil. The following results were obtained: 1. The systolic anterior movement (SAM) of the mitral valve was reduced (p less than 0.005), 2. the enddiastolic and endsystolic diameter were increased (p less than 0.02 and 0.05 respectively), 3. the EF-slope remained unchanged. 4. The left ventricular systolic pressure was reduced (p less than 0.025) and the gradient diminished from an average value of 58 to 34 mmHg (p less than 0.02), 5. heart rate and left ventricular enddiastolic pressure remained constant. The results of this acute study suggest a beneficial effect of Verpamil in patients with hypertrophic obstructive cardiomyopathy.

Blood Pressure↗

[Preliminary hemodynamic studies on the activity of meproscillarin (author's transl)].

In 10 patients with arterial hypertension and left heart failure the hemodynamic effect of 14-hydroxy-3-beta-[4-O-methyl-alpha-L-rhamnopyranosyl)oxy]-14beta-bufa-4,20,22-trienolide (Ky 18, meproscillarin, Clift) was compared with placebo in a double-blind study. 15 min after oral administration of meproscillarin there was an increase of cardiac output and stroke volume by up to 25%. Heart rate, arterial blood pressure and left ventricular filling pressure remained unchanged.

Aged↗

[Exercise echocardiography in coronary heart disease (author's transl)].

23 patients with coronary heart disease (11 with angiographically normal and 12 with depressed left ventricular function) were studied by m-mode echocardiography before and after handgrip. The following results were obtained: 1. There were statistical significant differences in enddiastolic volume, ejection fraction, and circumferential fiber shortening between the two groups. 2. Isometric exercise (handgrip) did not alter left ventricular dimensions or contractility, if mean values were calculated in both groups. 3. The majority of patients with compromised left ventricular function at rest, however, responded to handgrip by increasing their enddiastolic volume, apparently using the diastolic volume reserves. Ejection fraction and circumferential fiber shortening remained constant. 4. The majority of patients with angiographically normal left ventricular function at rest, on the contrary, displayed augmented contractility under handgrip. Only 4 out of 11 patients with proximally located, high-degree lesions and inadequate collaterals responed to isometric exercise with a reduction of ejection fraction and circumferential fiber shortening.

Angiocardiography↗

[The serum triglycerides and their role as a coronary risk factor (author's transl)].

291 patients with various types of hyperlipoproteinemia and 216 persons with normal serum lipid levels were examined for the frequency of angina pectoris and myocardial infarction. As a risk factor of myocardial infarction, Fredrickson's Type IIb was ranking on top, followed by simultaneous elevation of serum cholesterol and serum triglycerides regardless of the lipid-electrophoretic tappern, followed by Fredrickson's Type IV and finally by isolated hypercholesterolemia and Fredrickson's Type IIa. For angina pectoris, the order was slightly different: the highest risk factor was the simultaneous elevation of serum cholesterol and serum triglycerides, followed by hyperlipoproteinemia Type IV, hyperlipoproteinemia Type IIb, and finally by isolated hypercholesterolemia. The risk of both myocardial infarction and angina pectoris caused by isolated hypertriglycerolemia was not statistically significant, the same observation was made for the risk of angina pectoris in hyperlipoproteinemia Tye IIa. The present results confirm that an elevation of the serum triglycerides plays a minor role as a coronary risk factor in comparison to hypercholesterolemia.

Angina Pectoris↗

[Cardiac pacing in tachycardiac arrhythmias].

Cardiac pacing may be useful in the management of supraventricular and ventricular tachycardias. Prophylactically, recurrent ectopic tachycardias may be prevented by atrial or ventricular pacing for a sustained period at a rate faster than the spontaneous rate, but slower than the rate of the tachycardia being suppressed. Moreover, the pacemaker permits the dosage of antiarrhythmic agents to be increased until the recurrent arrhythmias are completely controlled. Therapeutically, supraventricular tachycardias may be terminated by (1) overdrive suppression, (2) delivery of a single stimulus or two serial stimuli or repetitive stimulation at a rate slower than the tachycardia (competitive stimulation) and (3) orthorhythmic stimulation. Today, implantable units exist. Advantages and disadvantages as well as risks of pacing in patients with tachycardias, are discussed.

Electric Stimulation↗

[Mitral valve function during frequency stimulation in coronary disease. Echocardiographic and hemodynamic comparative studies].

In 3 controls and 10 patients with coronary heart disease (CHD) and angina pectoris (AP) left ventricular enddiastolic pressure (LVEDP) and pulmonary artery diastolic pressure (PADP) are measured at rest (R) and during right atrial pacing with stepwise increments in heart rate. The values were compared to the simultaneously recorded DE-slope and EF-slope of the mitral valve echocardiogram. The following results could be obtained: 1. In the control group PADP increased sharply at a rate of aobut 120/min, while LVEDP further decreased. This "physiological dysfunction" of the mitral valve could not be detected by echocardiography. 2. In patients with CHD and AP both pressures rose concomitantly with the onset of the angina; moreover, the EF-slope showed a significant reduction. 3. This decrease of the EF-slope is due to an increment of LVEDP during angina and may be used as a diastolic tool, if the exercise electrocardiogram is negative. 4. LVEDP and EF-slope are correlated weil in most patients with CHD. However, there was a lack of correlation between the reduction of the EF-slope and left ventricular function.

Arteriosclerosis↗