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At least 19 recordsLinked to original sources
PubMed1977

Studies on the absorption and disposition of meptazinol following rectal administration.

1 Rectal administration of the new analgesic drug, meptazinol, resulted in rapid absorption of the compound both in the monkey and in man. Peak plasma levels were observed within 0.5 h of dosing. 2 Absorption of the drug following rectal administration was extensive as shown by the recovery of 65-90% of the dose in the urine. 3 Despite substantial inter-individual variation in the observed maximum plasma concentrations of the drug, it was still evident that concentrations after rectal dosage were considerably higher than when the same dosage was given orally. 4 Elimination of the drug from plasma took place rapidly in an apparently mono-exponential manner in both species. The half-life of elimination in monkeys was 1.25 h and in man 2.0 h.

Adult↗
PubMed1976

Pharmacokinetics and relative bioavailability of vinylbital in man after oral and rectal administration.

A sensitive and specific method for the quantitative determination of 5-vinyl-5-(1-methylbutyl)-barbituric acid (vinylbital) in plasma was developed, by using gas chromatography with alkali flame ionization detection. The method is suitable for measuring vinylbital plasma levels in man after administration of therapeutic doses. The pharmacokinetics and relative bioavailability of vinylbital after oral and rectal administration were studied in man. Tablets (Bykonox) containing 150 mg vinylbital, were used for the oral experiments and suppositories (Suppoptanox, polyethylene glycol base) containing 200 mg vinylbital, were used for rectal administration. Six volunteers participated in a cross-over way in the study. Vinylbital plasma concentrations were determined at regular intervals after drug administration. Absorption and elimination of vinylbital appeared to occur according to a single first-order process and the plasma concentrations were fitted by computer according to the equation intrinsic to the one-compartment open model after oral or rectal administration. The lag time was shorter for the suppository than for the tablet, whereas the absorption rate was faster for the tablet (mean absorption half-life 0.24 h compared with 0.64 h for the suppository). The elimination half-life of vinylbital varied from 17.6 to 33.5 h, with a mean value of 23.5 h for oral administration and 23.8 h for rectal administration. The half-lives were not considerably different on the two occasions for the individual volunteers. The average bioavailability of vinylbital for the suppository, relative to the tablet, was approximately 93%. Three volunteers collected their urine during 3--4 days after administration of a tablet. Unchanged vinylbital was determined and approximately 1.6% of the administered dose was excreted as unchanged drug. Some preliminary experiments of repetive vinylbital administration showed that self-induction of metabolism did not occur.

Administration, Oral↗
PubMed2026

A clinical study on the efficacy of rectal administration of Tongfu Qinghua decoction combined with external application of Ruyi Jinhuang powder in treating acute pancreatitis.

BACKGROUND: Acute pancreatitis (AP) is a common acute abdominal disease with high mortality in moderate and severe cases. Integrated Chinese and Western medicine therapy has promising clinical application prospects. OBJECTIVES: This study investigated the efficacy and safety of Tongfu Qinghua decoction enema combined with Ruyi Jinhuang powder external application for AP and its therapeutic effects across different age groups. METHODS: A total of 100 AP patients from October 2023 to August 2025 were randomly divided into observation and control groups (50 cases each). The control group received conventional Western medicine and the observation group received additional combined Chinese medicine therapy. Outcomes including hospital stay, symptom relief, inflammatory and pancreatic injury markers, clinical efficacy and adverse reactions were compared, with subgroup analysis of patients aged 18-40, 41-60 and 61-75 years. RESULTS: The observation group had significantly shorter hospital stay, faster symptom relief and gastrointestinal recovery (P<0.05). Post-treatment inflammatory and pancreatic markers improved significantly and the total effective rate was higher (P<0.05), with no significant difference in adverse reactions (P>0.05). Benefits were consistent across all age subgroups, with younger patients recovering faster and elderly patients still achieving significant improvement. CONCLUSION: This combined therapy is effective and safe for AP patients aged 18-75 years, significantly improving clinical outcomes and worthy of clinical promotion.

Humans↗
PubMed1975

Plasma levels of diazepam after parenteral and rectal administration in children.

Plasma levels of diazepam and N-desmethyldiazepam were investigated in 19 children by a gas chromatographic method permitting the use of capillary sample. Intravenous administration was studied in 3 children and the plasma level curves showed a rapid decline during the first hour. Absorption and elimination after rectal administration of a solution in 16 children were similar to those after intramuscular administration. Diazepam given by suppository to 5 children gave much lower plasma levels and delayed time to peak levels. Recurrence of seizures in 2 children indicated that the anticonvulsants plasma level was of the order of 150 to 200 mug/liter. No significant side effects were observed. Thus rectal administration of a solution of diazepam is a practical method to arrest convulsions in children.

Child↗
PubMed1975

Absorption of 3H-benzocaine from ointments following rectal administration in rats.

Total radioactivity in the blood of rats for 5 hr following rectal administration of 3H-benzocaine in oleaginous, absorption, emulsion (water-in-oil and oil-in water), and water-soluble ointment vehicles was measured. The release was greatest from the water-soluble vehicle and followed the same relative order as seen in an earlier in vitro experiment. No intact benzocaine was found in the blood using radiochromatography. In vitro hydrolysis of benzocaine by rat blood did not occur as determined with the techniques of this experiment.

Administration, Topical↗
PubMed1979

First-pass effect after rectal administration of thiazinamium methylsulfate.

The absorption and metabolism of the quaternary ammonium compound thiazinamium methylsulfate were studied in humans using plasma concentration data and urinary excretion measurements. After giving a dose of 150 mg in suppositories, the relative bioavailability was 5.8 +/- 3.2 (SD) % of the dose, comparable to the values obtained following oral administration. The degree of first-pass effect observed after rectal administration was comparable with that after oral administration.

Aged↗
PubMed1977

Plasma-diazepam in infants after rectal administration in solution and by suppository.

Twenty infants aged 1-2 years who had previously had one attack of febrile convulsions were randomly given a single dose of diazepam rectally, either as a solution (0.7 mg/kg) or by suppository (5 mg). Plasma-diazepam levels were determined repeatedly during the first hour using gas chromatography. Rectal administration of diazepam in solution resulted in anticonvulsant plasma values within 4 +/- 1 min. Similar plasma levels were obtained only after 20-30 min in the group treated with suppositories. Diazepam in solution given rectally may therefore be useful in the acute treatment of febrile convulsions, while treatment by suppository would seem to be of little value in this respect. Moreover, diazepam in solution given rectally seems suitable for use at home in case of recurrent febrile convulsions. This treatment, however, cannot be recommended until the anticonvulsant effect and side-effects have been elucidated further.

Child, Preschool↗
PubMed1979

Rectal administration of diazepam in solution in the acute treatment of convulsions in infants and children.

In a prospective study 44 children, aged 6 months to 5 years, admitted to hospital with febrile convulsions or epilepsy, were treated with diazepam in solution administered rectally during 59 generalised attacks. Rectal administration of diazepam was effective in the acute treatment of convulsions in 80% of cases. In 10% the treatment failed, whereas diazepam administered intravenously had prompt effect; another 10% of the convulsions wer resistant to diazepam, irrespective of the route of administration. The therapeutic effect was significantly correlated with the duration of convulsions before treatment started. Early treatment (convulsions less than or equal to 15 minutes) had effect in 96%, and late treatment (convulsions greater than 15 minutes) in 57% of cases. A total of 317 children admitted with febrile convulsions were treated prophylactically with diazepam administered rectally whenever the temperature was greater than or equal to 38.5 degrees C. No case of significant respiratory depression or other serious side effects was observed. The rapid and reliable anticonvulsant effect of diazepam given rectally and the very few side effects makes this treatment a valuable alternative to IV administration in childhood.

Acute Disease↗
PubMed1979

Plasma theophylline level and effect on lung function after oral and rectal administration of aminophylline.

Twelve patients with partly reversible, chronic airway obstruction, according to a double blind randomized cross-over design, received on three consecutive days oral aminophylline 500 mg, a 500 mg aminophylline suppository and a placebo. The effects on ventilatory function were studied and the plasma concentration of theophylline was measured. After rectal administration, the plasma concentration of theophylline rose to 5 to 10 microgram/ml, and after oral ingestion the plasma level in most patients exceeded 10 microgram/ml. Administration of the aminophylline suppository resulted in moderate improvement in ventilatory function, and although the improvement was less pronounced than after oral administration, the use of a suppository in the treatment of patients with chronic obstructive lung disease should not be rejected.

Administration, Oral↗
PubMed1979

A multicentre pilot study of parenteral and rectal administration of domperidone in the treatment of severe vomiting in children.

A small scale pilot study among 41 children with severe vomiting, showed that a single administration of domperidone either intravenously, intramuscularly or rectally, effectively controlled the symptom within 3 hours in 36 (88%) patients. The excellent results together with the safety of this new drug indicate its potential value in these patients.

Adolescent↗
PubMed1978

Rectal administration of sodium valproate in status epilepticus.

Six patients suffering from status epilepticus were refractory to parenteral treatment with either diazepam, amobarbital or both, and were given sodium valproate 200 to 800 mg every 6 hours. The drug was administered rectally as 200 mg lipid-based suppositories, thereby avoiding impaired absorption, which occurs in the presence of paralytic ileus. Plasma levels of sodium valproate in all patients reached the therapeutic range within 36 hours of starting therapy. Seizures were totally controlled in five patients and a 75 percent reduction was noted in the sixth. In two patients, the route of administration was changed from rectal to an equivalent oral dose with continuing control of seizures and minimal change in plasma levels, suggesting that bioavailability is similar for the two forms of the drug. The rectal route of administration was effective in achieving systemic absorption of sodium valproate in the treatment of status epilepticus.

Adolescent↗
PubMedDate not supplied

Rectal administration of 13N-ammonia in cirrhosis of the liver.

13N-ammonia, applied rectally, after absorption and transportation visualises the liver. After release of 13N-aminoacids and 13N-urea by the liver, 13N-activity can be measured over other organs. In patients with porta-systemic shunts, 13N-ammonia will appear in the systemic circulation as well. In 16 controls and 26 patients with cirrhosis, activities were measured for 20 minutes over liver, spleen, heart, lungs and forearm. In all subjects, the liver was visualised within a minute, in some patients with cirrhosis faintly, however. Release by the liver of 13N-ammonia metabolites started within a few minutes. Liver/heart activity ratios proved to be more discriminating between the control- and the cirrhosis group than liver/lung and liver/spleen ratios. In the control group, the 20 minutes' liver/heart ratio was most suitable for determining the normal range. The lower normal level was found to be 2.25. Fourteen of the 26 patients with cirrhosis had a normal, 12 an abnormally low 20 minutes' liver/heart ratio.

Adult↗
PubMed1975

Plasma concentrations of diazepam and its metabolites after peroral, intramuscular, and rectal administration. Correlation between plasma concentration and sedatory effect of diazepam.

Plasma levels of diazepam, N-demethyldiazepam and free oxazepam were measured gaschromatographically in ten healthy volunteers after 5 mg of diazepam perorally, intramuscularly and rectally (with three different kinds of suppositories). The best absorption of diazepam was found after peroral administration. After an intramuscular injection a delayed absorption with low plasma concentrations of diazepam was found. The basal component of a diazepam suppository seems to have a great effect on the rectal absorption of diazepam. Two of the three different kinds of diazepam suppositories caused higher plasma diazepam concentrations than the intramuscular injection of the drug. There were no great differences in the amount of the metabolites of diazepam after different kinds of administration. The subjective sedatory effect of diazepam lasted approximately as long as the fast distribution of diazepam from plasma took place. A very highly significant correlation between plasma concentration and subjective sedatory effect of diazepam after a single dose was found.

Administration, Oral↗
PubMed1976

Results of the rectal administration of ketoprofen in fifty-two patients.

The results of a clinical study of ketoprofen suppositories suggest that the drug is effective when given in this way. It is suggested that, in the treatment of inflammatory rheumatic disorders, advantage should be taken of the longer duration of action of ketoprofen suppositories to prescribe their administration early in the morning and before retiring. Local intolerance occurred in only 4 of 52 patients.

Adult↗