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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↗
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↗
PubMed1990

Improvement by adjuvants on the rectal bioavailability of non-absorbable drugs following administration of suppository.

The influence of suppository bases and adjuvants on the release rate of drugs and the absorption of non-absorbable drugs such as sulfanilic acid (SA) and sulfaguanidine (SG), was investigated following the rectal administration of suppositories. The suppository bases used were lipophilic bases such as Witepsol W 35, H 15, S 55, E 75 and hydrophilic base such as macrogol. SA was rapidly released from macrogol, W 35, H 15 and S 55, except E 75. On the other hand, SG was rapidly released from macrogol, whereas the release of SG from lipophilic bases was slow. Rectal absorption of SA and SG following administration of each drug alone in suppository form was slight. On the addition of diclofenac sodium (DF) as absorption promoter the blood levels of SA and SG released from all suppositories increased by about two to four fold compared with those suppositories containing only SA or SG, respectively. However, the absorption of SG still did not attain sufficient levels by the administration of DF only. The rectal absorption of SG was markedly increased by the release rate of the drug from the suppository. These results indicate that after administration of these suppositories the bioavailability of non-absorbable drugs was sufficiently improved by enhancing both the release rate from the suppositories and the rectal membrane permeability.

Adjuvants, Pharmaceutic↗
PubMed1988

Comparison of nasal, rectal, buccal, sublingual and intramuscular insulin efficacy and the effects of a bile salt absorption promoter.

The purpose of this investigation was to develop a method to quantitate insulin absorption, and to compare insulin absorption from various noninjection sites of administration. Log dose/effect curves were established for i.m. insulin in adult male rats. The effects measured were the maximum change in plasma glucose concentration and the cumulative percentage of change in plasma glucose concentrations from 0 to 4 hr. Both log dose/effect curves gave similar results when calculating the efficacy of other routes, relative to i.m. Nasal, buccal, sublingual and rectal absorption sites were isolated by ligation procedures or with physical barriers. Rectal insulin was more efficacious than nasal, buccal and sublingual insulin, when administered without an absorption-promoting adjuvant. However, the efficacy relative to i.m. insulin was low for each route, probably due to a combination of slow membrane permeation and metabolism at the absorption site. Administration in a solution containing 5% sodium glycocholate, an absorption-promoting adjuvant, increased insulin efficacy by each route. The rank order was nasal greater than rectal greater than buccal greater than sublingual, with nasal and rectal insulin being roughly half as efficacious as i.m. insulin. Orally administered insulin, at doses 5 times higher than administered by other routes, and with Na glycocholate, produced no hypoglycemic response.

Absorption↗
PubMed1991

Effect of low-molecular casein and gelatin on absorption of ibuprofen after oral and rectal administration.

Kneaded mixture of ibuprofen with low-molecular gelatin or casein (LM gelatin or LM casein) was prepared, and their in vitro dissolution, release from suppository base and in vivo absorption behaviours were examined. The dissolution rate of ibuprofen from the kneaded mixtures was markedly higher than that of the drug itself. The LM gelatin and LM casein also enhanced the release rate of ibuprofen from suppository base. After oral administration of the kneaded mixture with LM gelatin to beagle dogs, the initial serum concentration was higher than that of the drug alone. On the other hand, LM casein accelerated the absorption of ibuprofen from rectum. However, LM gelatin and LM casein did not affect the bioinversion of R(-)- to S(+)-ibuprofen.

Administration, Oral↗
PubMed1982

Enhanced rectal bioavailability of polypeptides using sodium 5-methoxysalicylate as an absorption promoter.

The absorption-promoting effect of sodium 5-methoxysalicylate was studied in the rat with respect to rectal delivery of pentagastrin and gastrin. Rectal bioavailability was quantitated by direct comparison of pharmacological effect with intravenous dose response. Coadministration of the absorption adjuvant greatly enhanced the rectal bioavailability of the model polypeptides. Sodium 5-methoxysalicylate, therefore, is representative of a new type of absorption promoter which appears to facilitate rectal absorption of polypeptide drug entities.

Animals↗
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↗
PubMed1992

Glycine absorption from irrigation fluid during endoscopic resection of rectal tumours.

A significant rise in plasma glycine concentration was observed in nine elderly patients undergoing endoscopic transanal resection of rectal tumours using glycine solution for irrigation. Despite the obvious absorption of glycine, plasma sodium concentration and osmolality were not significantly altered, except in a patient whose rectal wall was perforated. In this case plasma sodium and osmolality fell, and the patient developed hyperammonaemia. Potentially adverse metabolic consequences may occur when there are surgical complications, but in the absence of such problems the absorption of glycine appears to cause little effect.

Aged↗
PubMed1979

Absorption of diazepam in man following rectal and parenteral administration.

Serum concentrations of diazepam and N-desmethyldiazepam were measured in six adult patients following administration of 10 mg diazepam in solution by the rectal, intravenous, and intramuscular routes. Maximum serum concentrations of 121--200 ng/ml were recorded from 10 to 20 min. after the rectal instillation, whereas following intramuscular injection the levels rose slowly and irregularly, reaching a maximum (62--186 ng/ml) in 1 to 24 hours. The bioavailability of diazepam given by rectal instillation was found to be 50 +/- 17 per cent (mean +/- S. D.) as compared with the intravenous administration. The possible reasons for the low bioavailability are discussed. It is concluded that administration by rectal tube provides a useful alternative to the tablets (and intramuscular injections) when a rapid onset of effect of the drug is wanted, and when intravenous administration is not applicable or practical.

Absorption↗
PubMedDate not supplied

Pharmacology of bile acids and their derivatives: absorption promoters and therapeutic agents.

The role of bile acids in pharmacotherapy is reviewed in this article. The therapeutic use of bile has been recognized since ancient times. Previously bile acids were the standard treatment for gallstones where chenodeoxycholic acid and ursodeoxycholic acid were effective in promoting the dissolution of cholesterol gallstones. Today their therapeutic role looks set to expand enormously. Bile acids as absorption promoters have the potential to aid intestinal, buccal, transdermal, ocular, nasal, rectal and pulmonary absorption of various drugs at concentrations that are non-toxic. Keto derivatives of cholic acid, such as 3a,7a,dihydroxy-12-keto-5alpha-cholic acid (sodium salt and methyl ester) are potential modifiers of blood-brain barrier transport and have been shown to promote quinine uptake, enhance the analgesic effect of morphine and prolong the sleeping time induced by pentobarbital. They have also been shown to be hypoglycaemic. Bile acids as therapeutic agents have the potential to produce beneficial effects in sexually transmitted diseases, primary biliary cirrhosis, primary sclerosing cholangitis, gallstones, digestive tract diseases, cystic fibrosis, cancer and diabetes.

Animals↗
PubMed2001

Delivery systems for acute migraine medications.

OBJECTIVE: To discuss advantages and disadvantages of various routes of administration and delivery systems for acute migraine medications, and to assist family physicians in optimizing treatment for individual patients. QUALITY OF EVIDENCE: A MEDLINE search from January 1966 to October 2000 and a Current Contents search for the year 1999 to October 2000 were conducted. Randomized controlled trials were selected, when available. Also included are guidelines (Canadian), non-blinded trials, systematic reviews, and population-based studies. MAIN MESSAGE: Selecting an appropriate way to deliver medication is important in acute migraine therapy. The parenteral route has advantages, such as rapid onset, greater efficacy, and the possibility of use during nausea and vomiting. Disadvantages include local site discomfort, inconvenience, and patients' dislike of needles. Most patients prefer oral therapy, but gastric stasis and nausea and vomiting during a migraine attack might limit its use. The intranasal route usually provides fairly rapid onset, but side effects, such as disturbances in taste, can occur. The rectal route is another option, but absorption is sometimes erratic, rectal irritation can occur, and few migraine medications are available in rectal formulation. CONCLUSION: Selection of appropriate medications and suitable delivery systems for individual patients, based on the characteristics of their attacks (e.g., severity, speed of progression to severe intensity, degree of associated symptoms), ease of administration, and patient preference, will optimize therapy for acute migraine attacks.

Acute Disease↗