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Biomedical subjects

K O Haustein

Publications and source records attributed to K O Haustein.

At least 73 records · Page 4Linked to original sources
PubMed1983

[Hepatic clearance of aminopyrine in the evaluation of liver function in hormonal contraception].

The function of microsomal destructing medicaments enzyme systems of the liver cell under hormonal contraception was objectified with the help of the aminopyrine test. After the oral administration of 9 mg dimethylaminoantipyrine (DMAAP) per kg body-weight together with 111 kBq 14C-DMAAP the elimination of 14CO2 was measured on the basis of the decrease of the radioactivity in the expiration air (respiration test). The plasma levels of DMAAP and its metabolites were measured, too. The two measurements lasted 5 hours. In contrast to a control group consisting of 8 women with healthy liver who were not ovulostatically treated (half-value time 14CO2-DMAAP 2.9 +/- 0.8 h, plasma 2.2 +/- 0.5 h) in 20 test women with healthy liver under ovulation inhibitors the elimination of 14CO2-DMAAP with 4.7 +/- 1.6 was clearly (alpha less than 0.01), the plasma elimination with 3.0 +/- 0.8 h was slightly retarded (alpha less than 0.05). In 19 patients with histologically ascertained chronic hepatopathies of above all insignificant degree of severity (13 degenerative lesions of liver parenchyma, 3 fatty livers stage I or II, 1 chronic active hepatitis each, chronic persisting hepatitis and cirrhosis) under hormonal contraception a half-value time of the 14CO2 elimination (alpha less than 0.001) prolonged to 5.0 +/- 1.5 h and a prolongation of the plasma elimination to 3.8 +/- (alpha less than 0.05). In 9 women in double examinations the 14CO2 elimination of the DMAAP after discontinuation of the application of ovulation inhibitors was compared with the values obtained under hormonal contraception and a regression of the retarded excretion in the expiration air (4.2 +/- 2.3 less than 5.1 +/- 1.2 h) and plasma (2.6 +/- 0.7 less than 3.4 +/- 1.7) was proved.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1983

On the pharmacokinetics of pengitoxin and its cardioactive derivative 16-acetyl-gitoxin.

The pharmacokinetics of pengitoxin has been studied in 28 healthy subjects after intravenous and oral administration. The mean plasma concentration 24 h after 0.5 mg i.v. was 5.2 ng X ml-1. Following an open two-compartment model a mean elimination half-life of 60.5 h (24.9 to 103.5 h) and a mean volume of distribution (Vdarea) of 66.91 (31.8 to 109.61) were calculated. Absorption calculated by comparison of the AUC0-infinity-values amounted to 99%. Within 4 days, 16.7% (11.7 to 21.1%) or 27.8% (18.4 to 33.7%) (0.5 mg i.v. or 1.2 mg p.o.) was excreted in urine. After pengitoxin 0.5 mg i.v. total body clearance and renal clearance were 13.3 ml X min-1 (7.0 to 18.6 ml X min-1) and 3.0 ml X min-1 (1.9 to 3.9 ml X min-1) respectively. The elimination half-life of pengitoxin is longer than that of digoxin and distinctly shorter than that of digitoxin, whilst its distribution volume and clearance are closer to those of digitoxin than of digoxin.

Acetyldigoxins↗
PubMed1982

Digitalis.

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Animals↗
PubMed1982

The determination of aminopyrin elimination for control of the metabolic capacity of the liver in man.

The kinetics of plasma and breath elimination of aminopyrine after 14C-aminopyrine given orally were studied using an open one-compartment model and first order rates of elimination. The study comprised eight healthy volunteers and two groups with histologically verified chronic liver diseases (cirrhosis, n = 12, and chronic aggressive hepatitis, n = 12). Elimination rates from plasma and breath were significantly reduced in the group with cirrhosis, but only so in chronic aggressive hepatitis when they were expressed relative to each other. Monomethylaminopyrine was eliminated more rapidly compared to aminopyrine, and the rate of formaldehyde formation was positively correlated to the excretion rate of CO2 (r = 0.53, P less than 0.002). No correlation was found with clinical or other laboratory data in the groups of liver diseases studied. The test is a quantitative indicator of the drug metabolizing mixed function oxidases of the endoplasmatic reticulum of the liver, and may reflect the degree of damage to this system in chronic liver disease.

Adult↗
PubMed1981

Interindividual differences in the pharmacokinetics of digitoxin and digoxin during long-term treatment.

Patients suffering from congestive heart failure received maintenance doses of digitoxin (N = 10) or digoxin (N = 8). The plasma glycoside concentration was determined, and after a single dose of 3H-digitoxin or 3H-digoxin, the decline and excretion of radioactivity were measured over a period of 7 (digitoxin) and 3 days (digoxin). Plasma radioactivity declined with a T1/2 beta between 77 and 234 h (mean 138 h) in the case of digitoxin and with a T1/2 beta between 9.2 and 38.6 h (mean 23.5 h) for digoxin. A close correlation between T1/2 beta and excreted radioactivity and T1/2 beta and total plasma level was found for digitoxin. In 4 patients TLC of urine showed that interindividual variations in digitoxin elimination could possibly be attributed to variation in metabolism, resulting in the production of different metabolites. Predicted digitoxin plasma levels agreed well with measured values. The maintenance dose could be calculated from the total body clearance (VCl) and a presumed plasma glycoside level. The recommended technique facilitates dosage calculations in patients treated with digitoxin.

Adult↗
PubMed1981

On the pharmacokinetics of talinolol, a new beta 1-receptor blocking agent.

In six female and male patients taking the specific beta 1-receptor blocking agent talinolol in daily maintenance doses between 100 and 300 mg, the plasma elimination half-life (t1/2) and the amount of excreted radioactivity via urine was evaluated after intake of a single dose of 14C-talinolol (0.88 MBq per 100 mg talinolol), and in the case of one patient with biliary fistula after intravenous injection (1.06 MBq per 10 mg talinolol). In this patient the bile concentration and elimination of radioactivity via bile was studied additionally. In the urine of three healthy volunteers, talinolol metabolites were isolated by TLC. In the six patients, 14C-talinolol was eliminated with a plasma t1/2 of 2.4 and 2.5 h, and a t1/2 of 4.6 via bile. The excretion of radioactivity amounted to 51.19% (intravenous injection), 23.9% (oral intake) in urine, and 7.49% in bile. In a urine fraction of one volunteer m-OH-talinolol was identified besides talinolol. The results indicate a remarkably high hepatic first-pass effect after oral administration of talinolol.

Adrenergic beta-Antagonists↗
PubMed1981

On the plasma protein binding of 16-acetyl-gitoxin.

The plasma protein binding of 16-acetyl-gitoxin (16-AG) was estimated in comparison with that of digoxin by the use of equilibrium dialysis, ultracentrifugation, and gel filtration techniques. Depending on temperature, the binding of 16-AG reached values between 81 and 90%. Calculations of the reaction enthalpy and entropy show that hydrophobic interaction results. The corresponding values of digoxin amount to 13 and 15%.

Acetyldigoxins↗
PubMed1981

[Quantitative thin-layer chromatographic estimation of aminophenazone (I.N.N.), 4-methylaminophenazone and 4-aminophenazone in plasma (author's transl)].

A TLC method for measurement of aminophenazone (1) and of its degradation products 4-methylaminophenazone (2) and 4-aminophenazone (3) in plasma was described. After chloroform extraction amd separation on Silufol plates the substances were stained by ferric chloride/potassium hexacyanotoferrate(III) and the area of the spots was measured. Concentrations from 1 to 25 micrograms 1, 2 and 3 per ml plasma could be estimated.

Aminopyrine↗
PubMed1980

[Interaction of digoxin and quinidine].

Plasma digoxin level and digoxin excretion were studied in 5 pat. suffering from cardiovascular diseases who had to be digitalized because of acute states of congestive heart failure. One of the patients took quinidine simultaneously. In the "quinidine" patient digoxin level was elevated to the 2--2.5 fold, as compared with "control" patients. Digoxin excretion of the "quinidine" patient was slightly increased. Following the results, a reduction in digoxin dosage to half of the dose is recommended.

Adolescent↗
PubMed1980

Studies on cardioactive steroids. IV. Influence of nitrate ester formation on cardiac and extracardiac activity.

The effects of 19 nitrate esters of genins and glycosides on the isolated guinea pig atrium and ileum were studied. The positive inotropic effect of glycoside nitrates correlated with the contracting effect on the ileum. Genin nitrates with weak cardiac activity were found to exert smooth muscle relaxing effects. Compared to genin nitrates, glyceryl trinitrate had a weaker relaxing effect on the ileum. On the coronary strip it had a stronger effect than delta 14-anhydrodigitoxigenin-3 beta-mononitrate, the most effective smooth muscle relaxing genin nitrate.

Animals↗
PubMed1980

Studies on cardioactive steroids. V. Structure-activity relationships of derivatives of 16 alpha-gitoxin.

The potency of 17 derivatives of 16 alpha-gitoxin was tested in the isolated atrium and heart of the guinea pig and the contractility-increasing activity of the 16 alpha-gitoxin 16 alpha-acetate was compared with that of 16 alpha-gitoxin in the anesthetized dog. The potency of 16 alpha-gitoxin was increased by the substitution of 16 alpha-OH for 16 alpha-methyl ether, 16 alpha-acetate and 16 alpha-nitrate. Substitution of the 16 alpha-acetyl group for substituents with a higher molar volume diminished this enhanced potency. Variation in the digitoxose moiety caused an increase or decrease in potency depending on the position and number of the substituted OH groups. In spite of changes in 16 alpha-OH, the low influence on rhythmicity persisted, as was found in experiments in the dog.

Acetyldigoxins↗
PubMed1980

Problems of rapid digitalization in severe congestive heart failure.

The pharmacodynamic effects (changes of systolic time intervals, STI, reaction of pulmonary arterial pressure) of digitoxin were studied in 7 patients with severe congestive heart failure in comparison with the corresponding plasma level. STI indicated glycoside-dependent changes, i.e. shortening of LVETc and QS2c and normalization of prolonged PEPc, while ICT shortening was less observed. In 2 patients with cor pulmonale a pulmonary oedema occurred accompanied with prolonged LVETc. During the early period of glycoside-dependent recompensation no significant correlation between STI shortening and glycoside plasma level was observed. Because of the retarded normalization of the haemodynamics of the pulmonary circulation and because of possible side-effects, rapid digitalization has to be reconsidered.

Adult↗
PubMed1980

Problems of an optimum digitalis therapy.

In 25 digitalized patients with ischaemic heart disease who had survived a myocardial infarction for 2 to 4 weeks, the systolic time intervals (STI) and changes of glycoside plasma level were measured before and up to 5 hrs after oral intake of a maintenance dose of digitoxin (n = 18) or of digoxin (n = 7). Between the changes of STI and the increase in digitoxon and digoxin plasma level no significant correlations were found. Therefore it is concluded that neither shortening of STI during the test period nor PEP/LVET are reliable criteria of individualizing and optimizing the therapy with cardioactive glycosides.

Adult↗
PubMed1979

[Dangers of rapid digitalization].

On the patients with moderate and severe heart insufficiency haemodynamic, clinical and electrocardiographic examinations were carried out. After the application of digitoxin at the beginning in the majority of cases no favourable effects on clinical and haemodynamic findings could be proved. In 2 patients with cor pulmonale even a drastic deterioration with increase of the pulmonary pressure and formation of a pulmonary oedema developed. The temporary analysis of the systole and the estimation of the glycoside level did not give any reliable references. The recompensation began only after 2-3 days. In 5 out of 10 patients in whom the cardiac rhythm was continuously controlled by means of a tape storage device, after the application of digoxin ventricular extrasystoles appeared. Also in these cases increased as well as subtherapeutic digoxin-plasma levels were present. In 2 patients with hypertrophic obstructive cardiomyopathy the infundibular gradients were considerably increased by strophantin. The causes of the different reaction patters are to be sought in disease-specific peculiarities, in the degree of severity of the heart insufficiency, in the speed of the flooding of glycoside and several extracardiac factors.

Adult↗
PubMed1979

On the cardiac efficacy of helveticosol-3',4'-di-nitrate, a new glycoside.

The cardiac and extracardiac effects of a new glycoside, helveticosol-3',4'-di-nitrate (HdN), were compared with those of helveticosol (H) and helveticosol-3',4'-di-propionate (HdP) in isolated guinea-pig heart preparations, in volunteers and dogs. In the atrium and heart, HdN produces positive inotropic effects at the same concentrations as H and at 10 times lower concentrations than HdP. In the heart, the difference between equieffective concentrations of HdN and HdP is smaller, but this is true only for the concentration required to produce the maximum inotropic effect. In the anaesthetized dog equieffective cardiac effects are obtained after oral admiinistration of the glycosides in the ratio 1 : 2 : 0.5 (HdN : HdP : H). After administration of HdN and HdP at equal ratios, no significant differences were observed between the toxic effects in conscious dogs or in the extent of shortening of STI in volunteers. Replacement of the hydrophobic subsituent propionate for the more hydrophilic nitrate residue causes slight changes in cardiac efficiency.

Animals↗
PubMed1978

Investigation into the species-specific deacylation of penta-acetyl-gitoxin.

Penta-acetyl-gitoxin (PAG) shows species-specific deacylation to 16-acetyl-gitoxin (16 AG; I and III) or gitoxin (II and IV) by homogenates of liver and intestinal mucosa of man (I), rabbit (II), guinea-pig (III) and rat (IV), whereas it is degraded into tri- and tetra-acetates by homogenates of guinea-pig myocardium as well as by human blood and serum. The identity of the principal and chloroform-extractable metabolities in human urine after PAG administration with 16-AG has been demonstrated by mass spectrometry.

Acetyldigoxins↗