PubMed Health⌕ Search

Biomedical subjects

H Allonen

Publications and source records attributed to H Allonen.

64 records · Page 4Linked to original sources

Methylergometrine: comparison of plasma concentrations and clinical response of two brands.

There were no significant differences between the two brands of methylergometrine (methylergonovine), Methergin and Myomergin, in the radioimmunologically measured serum concentrations nor in the AUC after an oral 0.250 mg dose determined on the third or sixth postpartum day during a continuous treatment with methylergometrine 0.125 mg t.i.d., nor were there significant differences in the clinical response to this oxytocic drug. Peak serum concentrations were obtained at 3 hours (Methergin 6.3 nmol/1 and Myomergin 6.0 nmol/1), indicating a delayed gastrointestinal absorption in postpartum females in comparison with healthy male volunteers [6]. Spontaneous complaints of side-effects were rare and mild.

Adult↗

Bioavailability and effect of food on the gastrointestinal absorption of two erythromycin derivatives.

The concentrations of erythromycin in the serum were comparable after a single 500 mg oral dose of two brands of erythromycin stearate (Resibion and Erythrocin) in six healthy fasting volunteers. There was no significant difference in their pharmacokinetics. Over a period of 24 hours, 4 and 5% of the 500 mg dose of each preparations was excreted in the urine. Analysis of serum erythromycin concentration data were performed according to a one-compartment open model. The short half-life in the serum (1.43-1.78 hours), small portion of the dose excreted in the urine (4-5%), and the low renal clearance value (0.43-0.51 ml/min/kg) indicate that the majority of erythromycin is extensively cleared by extrarenal mechanisms. In addition, serum concentrations of erythromycin were measured during continuous treatment (250 mg base every 6th hour) with erythromycin stearate (Resibion) or enteric-coated erythromycin base (Etromycin) in ten healthy volunteers, in both fasting and non-fasting conditions. Again in the fasting state the serum levels were comparable and those from both the stearate and base were markedly reduced by food.

Administration, Oral↗

Estimation of pharmacokinetic parameters of digoxin from serum, saliva and urine.

The pharmacokinetics of digoxin was studied in 14 healthy volunteers using concentrations measured radioimmunologically in the serum, saliva and urine. The subjects were given 0.75 mg of digoxin intravenously. Serum and saliva were obtained over a 72 hr period and urinary excretion rates over 6 or 7 days. Binding of digoxin to serum proteins was determined by ultracentrifugalization. A linear correlation between the serum and saliva concentrations was found. Salivary levels were equal to the unbound fraction in the serum. The half-lives of distribution did not differ between the serum and saliva. An erroneously short half-life of elimination was found in the serum, but in the saliva and urine it was found to be in the range previously reported. Salivary level measurements may be useful in pharmacokinetic studies and may have important clinical implications.

Adolescent↗

Excretion of methylergometrine (methylergonovine) into the human breast milk.

Methylergometrine concentrations in the maternal plasma and breast milk were determined by a radioimmunoassay during continuous treatment with 0.125 mg of methylergometrine 3 times daily. On the fifth postpartum day at 8:00 a.m. the patients (n=8) took 2 tablets of Myomergin (0.250 mg of methylergometrine) orally, and the levels in the plasma and milk were determined at 1 and 8 hr after the drug administration. Measurable amounts of the drug were found only in 5 out of 16 milk samples. It was concluded that this oxytocic drug does not appear in the breast milk in quantities sufficient to affect the infant. No cumulation in the plasma or in the breast milk was found.

Adult↗

Passage of digoxin into cerebrospinal fluid in man.

The passage of digoxin into the cerebrospinal fluid (CSF) was studied in 8 infants on maintenance therapy with digoxin, 11 adult patients on long-term digoxin therapy, and 15 patients, previously non-digitalized, who were given 0.5 mg digoxin orally 1 hr to 12 hrs prior to lumbar puncture. Digoxin in the serum and CSF was determined by radioimmunoassay. In the infants a mean serum concentration of 1.5 ng/ml (range 0.7-2.3 ng/ml) was found, and a simultaneous mean CSF concentration of 0.5 ng/ml (range 0.3-1.1 ng/ml). In the adults on long-term therapy, the corresponding figures were 1.1 ng/ml (range 0.5-2.2 ng/ml) and 0.3 ng/ml (range 0-0.6 ng/ml). Among the 15 patients given a single oral dose of digoxin, detectable CSF concentrations (0.2-0.3 ng/ml) were found in five, 1-12 hrs after the administration of the drug. In three paediatric patients with hydrocephalus (3 months-5 years) digoxin therapy was started as an attempt to decrease CSF production. In these patients, the production of CSF was reduced by 17, 25 and 30%, respectively.

Aged↗

The effect of phenytoin on the tissue concentrations of digoxin in the rat.

Rats treated chronically with digoxin were treated with two different dose levels of phenytoin, either as a single dose or chronically. Digoxin concentrations were measured by radioimmunoassay in the serum, urine, heart, muscle, liver, and the kidney. Chronic treatment with the high dose of phenytoin significantly increased the digoxin levels in the serum and tissues and decreased the renal clearance of digoxin. The low dose of phenytoin significantly reduced the serum and tissue levels of digoxin and increased the renal clearance. Single doses of phenytoin had a tendency to cause similar changes. Levels of digoxin were altered during the phenytoin treatment. In contrast to man, digoxin is extensively metabolized in the rat. Enzyme induction in connection with low phenytoin dosage and inhibition by high dosage is the suggested mechanism. It can be speculated that the tissue distribution and excretion of digoxin are altered.

Animals↗

Inotropic action and myocardial uptake of digoxin and betamethyldigoxin in isolated guinea pig atria.

The chronotropic and inotropic effects as well as the tissue levels of digoxin and methyldigoxin were studied in isolated guinea pig atria. Higher concentrations of methyldigoxin than of digoxin were required to cause arrhythmias. The inotropic potencies of the two glycosides did not differ from each another in equimolar concentrations in the organ bath. The increase in contractility correlated with the level of the glycoside in the organ bath and in the tissue. Digoxin was more effectively taken up by the heart tissue than methyldigoxin. Thus, when the tissue levels of the glycosides were the same, the contractility was greater after methyldigoxin than after digoxin.

Animals↗

Plasma concentrations of methylergometrine after intravenous and intramuscular administration.

The concentrations of methylergometrine (M) in the plasma were determined by a new radioimmunoassay after a single intravenous and intramuscular administration of two brands. Methergin (Sandoz Pharmaceuticals, Inc, East Hanover, NJ, USA) and Myomergin (Leiras Pharmaceuticals, Turku, Finland). No significant differences between the two brands were found. After the intravenous injection, M distributed quickly from the plasma to the tissues, and according to the elimination phase half-life M has no cumulative properties. After the intramuscular injection, M was absorbed quickly with peak plasma concentrations at one-half hour.

Abortion, Induced↗