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Biomedical subjects

J Kanto

Publications and source records attributed to J Kanto.

At least 181 records · Page 10Linked to original sources
PubMed1980

The pharmacokinetics of dihydroergotamine in the beagle dog after a single intravenous injection and after a continuous intravenous infusion.

The pharmacokinetics of dihydroergotamine (DHE) was studied in 6 beagles after a single 2.0 mg intravenous dose and after a continuous intravenous infusion (dose 2.0 mg, infusion time 51 min.=2.8-3.5 micrograms/min./kg). The concentrations of DHE in the plasma during 6 hours were determined by a radioimmunoassay. The mean alpha-phase T1/2 was 0.92 min. and 5.93 min., the mean beta-phase T1/2 was 104.42 min. and 115.79 min., and the mean plasma clearance value 202.88 ml/min. and 234.79 ml/min. after a single intravenous injection a continuous infusion administration, respectively. Similarly, the Vdc - values were 0.121/kg and significantly from each other. The simulated concentrations of DHE in the peripheral compartment increased rapidly explaining its fast effect on the vasculature in clinical use.

Animals↗
PubMed1980

Plasma and tissue concentrations of methylergometrine (methylergonovine) in the rabbit.

The concentrations of methylergometrine (M) (methylergonovine) in the plasma, uterus, liver, and kidneys of the rabbit were determined by a radioimmunoassay after a single 0.2 mg/kg intravenous injection and the drug response was studied in the uterus in situ. M disappeared quickly from the plasma with a mean distribution phase half-life of 0.91 min. According to the fast uterine tissue uptake of M the drug response in this effector organ began quickly. The stimulated concentrations in the peripheral compartment of the two-compartment open model can be useful in the understanding of the rapid drug effect, but they do not describe the real situation in any particular tissue.

Animals↗
PubMed1980

A comparative study on the clinical effects of flunitrazepam and lorazepam.

The clinical effects of flunitrazepam and lorazepam as oral premedicants were tested in a double-blind study in 81 gynaecological patients. Flunitrazepam showed a higher sedative effect (p < 0.05), but in regard to other parameters tested, no significant differences were found (sleep, apprehension, excitement, dizziness, emetic effect, headache, increase or decrease in systolic blood pressure, increase in pulse rate, venipuncture). In 9 per cent of the patients treated with lorazepam, a prominent muscular relaxation with slurred speech was observed, but in none of the cases treated with flunitrazepam. Our results support the earlier claims of flunitrazepam's relatively specific sedative property, but on the whole the difference in the clinical effects of these benzodiazepine derivatives is not marked.

Adult↗
PubMed1980

A comparative study of the clinical effects of pentobarbital and diazepam given orally as preoperative medication.

The clinical effects of pentobarbital, 100 mg, and diazepam, 10 mg, given orally as preoperative medications before dental surgery were tested in a double-blind study in 50 adult patients. The concnetrations of pentobarbital and diazepam (plus its three active metabolites) in plasma, measured by gas chromatography, were correlated with their clinical effects as assessed both subjectively and objectively (sedation, apprehension, excitement, dizziness, pre- and post-operative emetic effect, increase or decrease in systolic blood pressure, pulse rate, and ease of venipuncture). No significant difference in the effects of these two agents was observed, nor was there any obvious relationship between the concentration in plasma and clinical effect.

Adult↗
PubMed1980

Transcutaneous nerve stimulation for pain relief during labour: a controlled study.

Transcutaneous nerve stimulation (TNS) was applied to 100 parturients with a view of decreasing pain during labour. A control group of 100 parturients was randomly selected. Two hours after delivery the mothers and their midwives independently completed questionnaires regarding the pain which was subjectively quantified, during the different stages of labour. The distribution of age and parity of the mothers, the duration of labour, and Apgar score of the neonates at one minute were comparable in the two groups. The desire for and administration of analgesic agents was equal in each group. Significantly more mothers in the TNS group reported that labour had been moderately or intensively painful compared to the control group during cervical dilatation from 1--7 cm. After this degree of dilation the subjective judgement regarding pain were the same in both groups. The expectation of pain during labour, as well as the experience of pain compared to expectation, was similar in both groups. Thirty-one of the mothers in the TNS group considered the pain relieving affect of the TNS good and 55 considered it moderate. Thirty-two of the mothers in the TNS group wanted a more efficient analgesic method for the next labour.

Adult↗
PubMed1980

The use of labetalol as a moderate hypotensive agent in otological operations--plasma concentrations after intravenous administration.

The usefulness of labetalol, a combined alpha and beta adrenoceptor antagonist, as a moderate hypotensive agent during combination anaesthesia in otological operations was studied. These preliminary results show that an intravenous dose of 2.0 mg/kg of body weight of labetalol causes a moderate decrease in blood pressure without a concomitant increase in heart rate or excessive hypotension. The half-life of the elimination phase of labetalol in plasma varied between 3.9 and 6.3 hours. A direct relationship between the intravenous dose of the drug (0.5, 1.0 and 2.0 mg/kg i.v.) and the increase in the AUC value was observed. No correlation was found between the decrease in either the systolic or diastolic blood pressure and the plasma level of labetalol. This new type of antagonist may possess advantages over other current hypotensive drugs, i.e lack of tachycardia and excessive hypotension.

Adult↗
PubMed1980

A comparative study on the clinical effects of rectal diazepam and pentobarbital on small children. Relationship between plasma level and effect.

In order to test the possible differences in the clinical effects between benzodiazepines and barbiturates, 5 mg of diazepam and 60 mg of pentobarbital were used in a double-blind study as rectal premedication in 75 small children before major surgery. There were no significant differences between the two groups in the six parameters tested (demeanour in the anaesthetic room, preoperative emetic effect, response to venepuncture, degree of salivary suppression, postoperative state in the recovery room, postoperative emetic effect). The concentrations of pentobarbital and diazepam (and its 3 active metabolites) in the plasma were determined by gas chromatography and correlated with the clinical effects. No significant correlation was found between the total active benzodiazepine concentrations and the clinical effects of rectal diazepam. In contrast to diazepam, a weak but significantly positive correlation between the plasma concentrations of pentobarbital and the total score was found. Similarly, the plasma level of pentobarbital and the response to venepuncture and the degree of salivary secretion were in correlation with each other. In the plasma concentrations of both pentobarbital and total benzodiazepines, a wide interindividual variation was observed, indicating irregular rectal drug absorption.

Child, Preschool↗
PubMed1979

Long-term nitrazepam treatment in psychiatric out-patients with insomnia.

Psychiatric patients (N = 26) were treated chronically (from 1 week to 12 years) with nitrazepam, because of insomnia. The patients gave their subjective estimations of the effects and side effects of nitrazepam. The concentrations of nitrazepam in the plasma were measured by 63Ni-EC-gas-liquid chromatography. The pharmacokinetics of nitrazepam were compared between the psychiatric patients and healthy volunteers (N = 11). The steady-state concentrations and the half-life of nitrazepam in the psychiatric patients were comparable to those of the healthy volunteers. The subjective hypnotic effect of nitrazepam was mostly good or satisfactory and remained unchanged during long-term treatment. Only a few, mild side effects were reported. Nitrazepam does not seem to cause enzyme induction with lowered plasma levels and may therefore be of special value in the treatment of chronic insomnia.

Adult↗
PubMed1979

Human pharmacokinetics of nitrazepam: effect of age and diseases.

Plasma concentrations of nitrazepam were measured by gas-liquid chromatography in: young healthy volunteers, in geriatric and psychiatric patients and in epileptic children. The disposition of nitrazepam was described in terms of a two-compartment open model. After a single oral dose of nitrazepam 5 mg the most prominent differences between the experimental groups were in the beta-phase half-life mean 29 h in the young volunteers and 40 h in geriatric patients , and in the apparent volume of distribution during the beta-phase of 2.4 vs 4.8 1/kg. Total plasma clearance and the average steady state concentration in both groups were equal. The plasma level rose at a rate proportional to the beta-phase half-life, and so, they were achieved more rapidly in the young than in the old subjects (3.5 vs 7.5 d). No change in steady-state level or in the half-life of nitrazepam were found during long term treatment, which indicates lack of enzyme induction or inhibition. In 95% of the epileptic children with a good to fair clinical response, the plasma concentration of nitrazepam was 40-180 ng/ml (mean 114 ng/ml). As all of the patients were on combined antiepileptic therapy, no attempt was made to correlate plasma level with therapeutic response.

Adolescent↗
PubMed1979

Flunitrazepam versus placebo premedication for minor surgery.

The clinical effects of oral flunitrazepam (2 mg on the night before operation followed by 2 mg on the morning of operation) and placebo as premedicants were tested in a double-blind study in 81 gynaecological patients. The separate or total concentrations of flunitrazepam and its demethylated metabolite in plasma (measured by gas chromatography) were correlated with the clinical effects of flunitrapam premedication, assessed both sugjectively and objectively. In most parameters tested (sleep on the night before operation, sedation, apprehension, headache, pulse rate), there was a positive, significant difference between the flunitrazepam group (n = 44) and the placebo group (n = 37). No significant difference was found between the two groups in emetic effect, excitement, systolic blood pressure increase, and vene-puncture, but the patients receiving flunitrazepam felt significantly more dizziness. The temperature of the left forefinger before, during and after the anaesthesia did not vary significantly between the two groups. There was no correlation between the plasma concentration of flunitrazepam and its demethylated metabolite (separate or total concentrations) and any of the parameters tested before induction of anaesthesia. Flunitrazepam is a new oral premedicant with prominent sedative and anxiolytic actions. When the drug is given as a sedative on the night before operation, followed by a second dose on the morning of operation, the beneficial effects last for at least 8 hours after the second dose.

Adult↗
PubMed1979

A comparative study on the clinical effects of oxazepam and diazepam: Relationship between plasma level and effect.

The clinical effects of oxazepam and diazepam as oral premedicants were tested in a double-blind study of 60 children and 50 adults. The gas chromatographically measured concentrations of the active unconjugated forms of oxazepam and diazepam in the plasma were correlated to their clinical effects, as assessed both subjectively and objectively (sleep, sedation, apprehension, excitement, dizziness, emetic effect, headache, increase or decrease in systolic blood pressure, increase in pulse rate, venepuncture). No significant difference in the effects of these two benzodiazepine derivatives were observed, nor was there any obvious relationship between the plasma concentration and clinical effect.

Adult↗
PubMed1979

Erythromycin levels in serum during treatment with erythromycin stearate and base.

The serum concentrations of erythromycin during treatment with erythromycin stearate and erythromycin base were compared in a randomised cross-over study with 21 hospital patients. No statistically significant differences between the brands were found in the serum erythromycin levels at any time or in the areas under the serum level-time curve.

Administration, Oral↗
PubMed1979

Labetalol as a hypotensive agent in otological operations.

The usefulness of labetalol, a new combined alpha and beta adrenoceptor antagonist as a hypotensive agent in otological operations was studied in 18 otherwise healthy patients. After a single 1.0 mg/kg i.v. dose the maximum decrease in systolic (18%) and diastolic (8%) blood pressure occured between 5 to 15 minutes (mean 11 min), and the pretreatment blood pressure values were reached in 15 to 55 min (mean 26 min). Similarly, after a single 2.0 mg/kg i.v. dose the maximum blood pressure decrease (32%/20%) was observed in 5 to 40 minutes (mean 23.5 min) lasting 30 to 95 minutes (mean 60.1 min). Generally, a moderate decrease in blood pressure without a concomitant increase in heart rate or excessive hypotension was found.

Adrenergic alpha-Antagonists↗
PubMed1979

Absorption of sustained-release and plain papaverine in man.

The concentrations of papaverine in the plasma of healthy volunteers were determined by a GLC-method both after single and repeated oral doses of plain and sustained-release drug formulation. In both experiments the AUC-value after the sustained-release drug form was significantly lower than after the plain papaverine and no maintenance of plasma levels for 12 hours after the sustained-release drug form was observed. Our work demonstrates that the systemic availability or papaverine can be markedly affected by product formulation.

Adult↗