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PubMed2002

Pharmacokinetics and pharmacodynamics of human chorionic gonadotropin (hCG) after rectal administration of hollow-type suppositories containing hCG.

To determine the effectiveness of human chorionic gonadotropin (hCG) administered rectally, we studied the pharmacokinetics and pharmacodynamics of hCG using a hollow-type suppository. HCG was not detected in plasma when only hCG was administered rectally, even at a higher dose (4,000 IU/kg body weight) than intravenous injection, because of its low bioavailability due to high molecular weight or degradation by proteolytic activity. To enhance the rectal absorption of hCG, the effectiveness of its coadministration with alpha-cyclodextrin (alpha-CyD), an absorption-enhancing agent, was investigated in male rabbits. HCG was detected in plasma following coadministration of hCG and alpha-CyD (10 mg/kg body weight) into the rectum. The plasma hCG concentration increased with increasing dose of alpha-CyD. The AUC(0-48) observed after coadministration of hCG and alpha-CyD at 30 mg/kg body weight was approximately four times higher than that of hCG and alpha-CyD at 10mg/kg body weight. HCG at a high concentration induced a rapid increase in the plasma testosterone concentration (74.2 +/- 3.4 ng/ml) 2 h after intravenous administration. However, the testosterone concentration 24 h after intravenous administration decreased to the physiological level (approximately 20 ng/ml) which had been observed before such administration. On the other hand, the maximum level of testosterone concentration (40.0 +/- 12.6 ng/ml) was observed 24 h after rectal administration of hCG (400 IU/kg body weight) in combination with alpha-CyD (30 mg/kg body weight). Moreover, the plasma testosterone concentration (31.0 +/- 11.4 ng/ml) obtained 72 h after rectal administration tended to be maintained at a higher level than that (14.4 +/- 0.9ng/ml) observed before the administration. These results suggest that the hollow-type suppository as a rectal delivery system of hCG is promising as a new mode of hCG therapy.

Administration, Rectal↗

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↗

PubMed1992

Infants and young children metabolise codeine to morphine. A study after single and repeated rectal administration.

1. Codeine was administered rectally to thirteen infants and young children undergoing elective surgery. Nine infants (6-10 months old) received a 4 mg suppository and four children (3-4 years old) an 8 mg suppository. Codeine and its metabolite morphine were measured in plasma by GC/MS. 2. The mean concentrations of codeine at 3, 4 and 5 h after administration were 240, 163 and 123 nmol l-1 in the younger and 309, 251 and 169 nmol l-1 in the older patients. The corresponding concentrations of morphine were 8.3, 7.4 and 4.5 nmol l-1 and 6.8, 5.5 and 2.8 nmol l-1 respectively. One patient in each age group had no detectable amounts of morphine. 3. In the four children, the rectal dose was repeated 6-hourly for four doses. The plasma concentrations of codeine and morphine following the fifth dose were similar to those after the first dose. The mean AUC(0,5 h) of morphine was 1.6% that of codeine. 4. In the infants the mean plasma half-lives of codeine and morphine were 2.6 and 2.5 h. The two infants with the lowest body weights had the longest half-lives. 5. The mean morphine/codeine concentration ratio was 4.3% in the infants and 1.6% in the children, suggesting impaired glucuronidation of morphine in the former group. The hourly concentration ratios were almost identical following the first and fifth dose in the children. 6. We conclude that at the age of 6 months infants are capable of O-demethylating codeine to morphine.

Biotransformation↗

PubMed1983

Rectal administration of metronidazole in severely ill patients.

Ten severely ill patients with life threatening sepsis received metronidazole as suppositories and blood concentrations of the drug were measured twice daily over five days. Therapeutic blood concentrations of metronidazole were maintained at all times in all patients. Rectal administration of metronidazole is accepted as effective prophylaxis against infection associated with surgery and as treatment of established infection. This study shows that in gravely ill patients metronidazole administered as suppositories gives perfectly adequate therapeutic serum concentrations of the drug, but that to achieve these concentrations rapidly the first suppository should be given with an intravenous loading dose.

Adolescent↗

PubMedDate not supplied

Serum concentration and drug effect after intravenous and rectal administration of diazepam.

In a randomized crossover study on sedation in outpatient oral surgery, the relation between the serum profile and the drug effect profile for intravenously (i.v.) and rectally administered diazepam was studied. Both sedation methods were found to be equally efficient at a mean dose of 0.25 mg/kg (range, 0.14-0.45) for i.v. administration, and 0.53 mg/kg (range, 0.50-0.58) for rectal administration. Both the serum concentration and the effect reached their mean peaks at the same time; however, this was 15 min later after rectal sedation than after i.v. sedation. Intravenous administration yielded a significantly higher serum concentration of diazepam at the clinical endpoint than did rectal administration, but the mean effect levels at the clinical endpoint were equal for both sedation methods. No linear correlation between log-serum concentration and the patient's estimation of effect was found.

Administration, Rectal↗

PubMed1994

Conscious sedation by rectal administration of midazolam or midazolam plus ketamine as alternatives to general anesthesia for dental treatment of uncooperative children.

The trial included 24 children (aged 2-7 yr) referred for dental treatment under general anesthesia, since conventional behavioral management methods had failed to achieve treatment acceptance. As an alternative, they received, on two separate occasions with "identical" dental treatment, conscious sedation by rectal administration of either midazolam (0.3 mg/kg body weight (bwt)) or midazolam (0.3 mg/kg bwt) plus ketamine (1.0 mg/kg bwt). This allowed a double-blind, crossover design. The aims were to assess conscious sedation, combined with local anesthesia, as an alternative to general anesthesia, and further to evaluate the effects obtained by addition of a low dose of ketamine to rectally administered midazolam. The feasibility of dental treatment was rated as excellent or good for 16 of the 24 children when premedicated with midazolam, and for 18 of the 24 children when ketamine was added to midazolam. At least some treatment could be given to all children. Verbal contact was maintained with all children throughout both treatment sessions. The children were significantly less anxious when they arrived for the second session. Amnesia and drowsiness were significantly increased when ketamine was added to midazolam. The combination also tended to be more efficient in relief of anxiety and prevention of pain, but there were large variations in the children's responses to the drugs. Midazolam significantly reduced the blood oxygen level, but not with ketamine added. For most children, both regimens proved to be appropriate as alternatives to general anesthesia.(ABSTRACT TRUNCATED AT 250 WORDS)

Anesthesia, Dental↗

PubMed1989

[Midazolam for premedication of infants. A comparison of the effect between oral and rectal administration].

Midazolam (M) has been successfully used in oral and rectal premedication of children of one to six years of age. The following study was designed to investigate the efficacy of both methods when used as premedication "on demand". 60 children (1-6 years) were randomly assigned to 0.3 mg/kg bw M orally and 0.5 mg/kg bw M rectally. Psychological, behavioural and physiological parameters were measured at special time intervals and special stressful events (separation from the mother or father, induction of anaesthesia). Rectally premedicated children were found to be better prepared concerning psychological and behavioural parameters. This can be due to the dosage as well as the faster absorption of M. In the postoperative period orally premedicated children experienced significantly more nausea and vomiting. This might be due to the preparation with saccharin, peppermint oil and ethanol. - In "premedication on demand" rectal Midazolam must be preferred to orally administered Midazolam in the preparation mentioned above.

Administration, Oral↗

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↗

PubMed1985

[Clinical study on concentration of FT-207 and 5-FU in serum, lymph nodes and tissues after rectal administration of FT-207 suppositories for malignant diseases of the liver, biliary tract and pancreas].

In order to study the antitumor effect of FT-207 in a solid tumor, it is necessary to determine the concentration of 5-FU and FT-207 in a tissue. This has only been done so far for gastric cancer and colon cancer, but these has been practically no research carried out regarding cancers of the liver, biliary tract and pancreas. A study was therefore made of lymph nodes and tissues after rectal administration of FT-207 suppositories to 12 patients with cancers of the liver, biliary tract and pancreas. These included 7 cases of pancreatic cancer, 2 cases of gall bladder cancer with infiltration to the liver, and 3 cases of hepatoma. In serum, the concentration of 5-FU reached 0.018 +/- 0.006 micrograms/ml at one hour after administration, 0.019 +/- 0.004 micrograms/ml at three hours after administration, and 0.023 +/- 0.008 micrograms/ml at six hours after administration. These concentrations would be expected to maintain a clinically sufficient dose. The concentration of 5-FU in metastatic lymph nodes was high compared with normal lymph nodes (p less than 0.05), its concentration in liver tumors was high while compared with normal liver tissues (p less than 0.05).

Biliary Tract Neoplasms↗

PubMed1995

[Research on rectal administration of bark of official Magnolia].

Fluorescence assay was applied to the determination of magnolol in rabbit blood, and the best way to administer the bark of official magnolia per rectal was established by orthogonal test. Then the two routes of administration were compared by AUC of magnolol and per rectal was found better than P.O. In addition, the modified isolated rectum-bag method was applied successfully to the research on rectal administration of bark of official magnolia.

Administration, Rectal↗

PubMed1984

Rectal administration of insulin.

According to recent statistics for the time span 1951-1970, the mortality ratio of diabetics to non-diabetics was 335% (46). For those diabetics who were younger than 15 years when entering the study, the mortality ratio was 1127%, with a mean life expectancy of another 32 years, as compared to 59 years for non-diabetics. Among the major causes of disablement and early death are ischemic heart disease, retinopathy, nephropathy, peripheral vascular disease and neuropathy. In spite of newer, more potent and highly purified insulins, development of human insulin, change of once-daily injection to twice-daily insulin therapy (47), and the introduction of portable insulin infusion pumps, diabetes is still a high-risk disease, far from being controlled. Considering that the present mode of insulin administration is by the subcutaneous route by which the insulin is presented to the body in a nonphysiological manner, because the insulin is peripherally administered to the systemic circulation instead of portally, new therapeutic ways for insulin administration are worth study. During the past years, considerable interest has arisen in the rectal route of administration. Based on a physiological-kinetic model presented in this paper, utilization of the first-pass effect inherent to the rectal anatomy offers a physiological insulin input via the rectal route of administration. A review on the present state of rectal insulin administration is given, and experimental data from our laboratories are presented. The usefulness of sorption promoters on rectal insulin absorption is discussed. The "effectiveness" of rectal insulin preparations is suggested to be evaluated by four criteria: the pharmacological availability via the area under the % glucose reduction-time profile, the maximum glucose concentration reduction, Cmax, the time to reach the maximum reduction, tmax, and the mean residence time for glucose reduction, MRT.

Animals↗

PubMed2004

Rectal administration of Escherichia coli O157:H7: novel model for colonization of ruminants.

Escherichia coli O157:H7 causes hemorrhagic colitis and life-threatening complications. Because healthy cattle are reservoirs for the bacterium, ruminant infection models have applications in analyzing the relationship between cattle and this human pathogen and in testing interventions to reduce or prevent bovine colonization with this bacterium. Current approaches often do not reliably mimic natural, long-term bovine colonization with E. coli O157:H7 in older calves and adult animals (ages that enter our food chain). Based on the recent identification of the bovine rectoanal junction mucosa as a site of E. coli O157:H7 colonization, we developed a novel rectal swab administration colonization model. We compared this method with oral dosing and direct contact transmission (Trojan) methods. E. coli O157:H7 carriage status was determined by fecal or rectoanal mucosa swab culture. High ( approximately 10(10) CFU) and low ( approximately 10(7) CFU) oral doses of E. coli O157:H7 in sheep and cattle resulted in variable infection with the bacterium. Some animals became colonized with the bacteria and remained culture positive for several weeks, and some animals did not become colonized and rapidly cleared the bacteria in a few days. Pen mates of E. coli O157:H7 culture-positive Trojan cattle had a low infection rate and variable colonization status. However, rectal swab administration of E. coli O157:H7 to cattle resulted in consistent long-term colonization in all animals. The surprising ease with which long-term infections resulted from a single application of bacteria to the rectoanal mucosa also strongly supported this location as a site of E. coli O157:H7 colonization in cattle.

Administration, Rectal↗

PubMed1992

Chronopharmacological study of valproic acid in mice: comparison of oral and rectal administration.

This study was performed to investigate the influence of the dosing route on chronopharmacological aspect of valproic acid (VPA) in mice, comparing the oral and rectal route. ICR male mice, housed under a standardized light-dark cycle (lights on from 0700 to 1900), were orally or rectally administered 400 mg/kg VPA each at the following scheduled time: 0900, 1300, 1700, 2100, 0100 and 0500. VPA concentrations in plasma and brain were determined by gas-liquid chromatography. There was a circadian rhythm in the electroshock seizure (ES) threshold 30 min after oral VPA administration, with the highest value at the midlight (1300) and the lowest at the middark (0100) (p < 0.01). A significant circadian rhythm was also found in plasma and brain VPA concentrations 30 min after oral administration (p < 0.01). This finding is related to the rhythm in the ES threshold. In contrast to oral administration, no circadian rhythm in the ES threshold, plasma and brain VPA concentrations was observed after rectal administration. These values after rectal dosing showed higher levels in comparison to those after oral dosing. Thus, the rectal route for VPA might have merit to eliminate the time-dependent changes in VPA pharmacologic action and kinetics. The timing of drug administration is an important factor that must be carefully controlled in drug pharmacokinetic and pharmacodynamic studies and must be considered in planning dosing routes.

Administration, Oral↗

PubMed1991

A comparative study of intravenous and rectal administration of propofol in piglets.

To compare the effectiveness of propofol given intravenously and rectally, ten piglets received propofol intravenously. On the next day, the same piglets and five other piglets were given suppositories containing propofol. Serial blood samples were collected for the analysis of propofol plasma concentration. The time course of the total plasma drug concentration was fitted into a bi-exponential function using a least square fitting regression computer programme. The volume of distribution was 2.5-2.8 l.kg-1, mean elimination half-life, 23.9 min and mean clearance 0.08 l.kg-1.min-1. The mean bioavailability by the rectal route was low. In contrast to the intravenously administered propofol, none of the piglets slept when given propofol rectally, reflecting the extremely low plasma propofol concentration. In veterinary medicine, propofol would seem to be clinically valuable for inducing intravenous anaesthesia, but would be ineffective when given rectally. The findings indicate that with the dosage forms used here, propofol would be clinically ineffective if given rectally to human infants and children.

Administration, Rectal↗

PubMed2001

Local and systemic immune responses to rectal administration of recombinant cholera toxin B subunit in humans.

The induction of immune responses to rectally administered recombinant cholera toxin B subunit (CTB) in humans was studied. Three immunizations induced high levels of CTB-specific antibody-secreting cells, particular of the immunoglobulin A isotype, in both rectum and peripheral blood. Antitoxin antibody responses in rectal secretions and serum were also found.

Administration, Rectal↗

PubMed1980

The pharmacokinetics and acceptability of benoxaprofen following rectal administration.

The bioavailability of a single 300 mg dose of benoxaprofen was compared after rectal and oral administration in 5 subjects. The total absorption rectally from a suppository was 83% of that achieved orally from a capsule. Six further subjects took a 300 mg benoxaprofen suppository twice daily for 12 d. Steady state plasma levels (mean level 94 microgram/ml) were reached at about 120 h, while the elimination half-life for benoxaprofen was approximately 38 h in this study. The suppositories were well tolerated. The plasma levels obtained compared very favorably with theoretically expected levels and levels obtained after comparable oral doses.

Absorption↗

PubMed1984

Absolute bioavailability of paracetamol after oral or rectal administration in healthy volunteers.

The absolute bioavailability of paracetamol (Tachipirina) administered in single doses orally and rectally was studied in nine healthy adult volunteers. The results of the rapid intravenous injection of 600 mg show that the kinetics of paracetamol can be represented by an open two-compartment model with introduction and elimination occurring in the central compartment. The oral administration shows an absolute bioavailability of 60-70% independent of the pharmaceutical form and gastric contents. The rectal administration shows a lower absolute bioavailability (of about 30-40%) substantially independent of dose in the range under consideration. The pharmaceutical form, food and the route of administration modify the plasma concentration-time curves of free paracetamol and of its main metabolites. A moderate inter-individual variation in the kinetics and the bioavailability was observed.

Acetaminophen↗

PubMedDate not supplied

Rectal administration of antiepileptic drugs in children.

This article reviews the current literature describing the use of rectally administered antiepileptic drugs. Individual antiepileptic drugs are discussed in regard to efficacy, toxicity, and rate of absorption. Absorption occurs through passive diffusion; therefore, solutions are absorbed most quickly. Paraldehyde, diazepam, secobarbital, and valproic acid are used when rapid effect for termination of prolonged or serial seizures is desired. Valproic acid, lorazepam, carbamazepine, and phenytoin all can be used for maintenance therapy.

Administration, Rectal↗