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At least 253 records · Page 14Linked to original sources
PubMed1992

Metabolic effects of rectal administration of unmodified eel calcitonin in humans.

To evaluate the metabolic effects of unmodified eel calcitonin, nine normal subjects and eleven patients with Paget's disease of the bone entered the study. Eel calcitonin was administered via rectal mucosa at the dosage of 100 and 200 MRCU. Plasma calcium, plasma phosphate and plasma cAMP were measured at a baseline and after 10, 20, 30, 60, 90, 120, 180, 240 min. Rectal administration of 100 MRCU of eel calcitonin decreased plasma calcium and phosphate levels in normal subjects; the hypocalcaemic and hypophosphatemic effects were more marked and statistically significant in Paget's disease patients. Using 200 MRCU of eel calcitonin, statistically significant reductions in plasma calcium levels were observed in controls and in Paget's disease patients. Plasma phosphate decreased after rectal administration of the hormone, but not significantly. A slight but not significant increase in plasma cAMP was observed in normal subjects after the administration of 200 MRCU. These data demonstrate that eel calcitonin administered via rectal mucosa can exert some of the known biologic effects of the peptide.

Administration, Rectal↗
PubMed2006

The rectal administration of lignocaine gel and periprostatic lignocaine infiltration during transrectal ultrasound-guided prostate biopsy provides effective analgesia.

INTRODUCTION: Transrectal ultrasound guided prostate needle biopsy (TRUS) is the standard procedure to diagnose or exclude prostate cancer. This procedure can be associated with significant discomfort, both on insertion of the ultrasound probe as well as on taking the biopsy. We evaluated a new technique for pain relief during TRUS biopsy. PATIENTS AND METHODS: In Group 1 (n = 60), the biopsies were taken without any analgesia. In Group 2 (n = 60), 11 ml of Instillagel (2% lignocaine) was administered rectally prior to probe insertion and 5 ml of 1% lignocaine periprostatic injection was administered before taking the biopsy. The discomfort encountered during the procedure was graded by the patient on a scale ranging from no discomfort to mild, moderate and severe pain. RESULTS: In Group 2, there was a marked reduction in the pain experienced during the procedure. The Chi-squared test for trend showed a significant association between the rectal administration of local anaesthetic gel and reduction in pain on probe insertion (P = 0.0001). There was also a significant association between the use of periprostatic lignocaine injection and reduction in pain on taking the biopsy (P < 0.0001). CONCLUSIONS: The use of lignocaine gel prior to probe insertion and periprostatic infiltration of lignocaine before taking the needle biopsy significantly reduces the pain experienced by the patient during TRUS-guided prostate biopsy.

Administration, Rectal↗
PubMed1994

Rectal administration of nicomorphine in patients improves biological availability of morphine and its glucuronide conjugates.

The pharmacokinetics of 30 mg nicomorphine after rectal administration with a suppository are described in 8 patients under combined general and epidural anaesthesia. No nicomorphine or 6-mononicotinoylmorphine could be detected in the serum. Morphine appeared almost instantaneously with a lag-time of 8 min and had a final elimination half-life of 1.48 +/- 0.48 h. Morphine was metabolized to morphine-3-glucuronide and morphine-6-glucuronide. These glucuronide conjugates appeared after a lag-time of 12 min and the half-life of these two glucuronide conjugates was similar: about 2.8 h (P > 0.8). The glucuronide conjugate of 6-mononicotinoylmorphine was not detected. In the urine only morphine and its glucuronides were found. The renal clearance value for morphine was 162 ml.min-1 and for the glucuronides 81 ml.min-1. This study shows that administration of a suppository with 30 mg nicomorphine gives an excellent absolute bioavailability of morphine and its metabolites of 88%. The lipid-soluble prodrug nicomorphine is quickly absorbed and immediately hydrolysed to morphine.

Administration, Rectal↗
PubMed2001

[Rectal administration of misoprostol for delivery induced hemorrhage. Preliminary study].

OBJECTIVE: Assess the efficacy of one misoprostol tablet (Cytotec) in severe delivery-induced hemorrhage on uterine atony after failure of syntocinon. PATIENTS AND METHODS: A descriptive study was conducted at the Djibouti Army Hospital from September to December 2000. Five patients with severe delivery-induced hemorrhage due to uterine atony unresponsive to syntocinon were give a tablet of misoprostol by rectal administration. RESULTS: The hemorrhage ceased in less than 5 minutes in all patients. No immediate side effect was observed. DISCUSSION: These preliminary findings are encouraging and suggest that further investigations would be useful to assess the beneficial effect of misoprostol by rectal administration for patients with severe delivery-induced hemorrhage due to uterine atony. Case-control studies with a sufficient number of cases should be undertaken to determine the real efficacy of misoprostol in this indication.

Administration, Rectal↗
PubMed1996

Rectal administration of paracetamol: a comparison of a solution and suppositories in adult volunteers.

The pharmacokinetics and tolerability of two dosage forms for rectal administration of paracetamol were compared. A fatty suppository was compared with a solution of 60 mg/ml paracetamol. Both dosage forms were given as 1000 mg doses to 10 healthy adult volunteers. The solution produced peak plasma concentrations significantly faster (t (max)) than did the suppository. The peak concentration (C(max)) and the area under the curve (AUC(6)) were also significantly greater. The pharmacokinetic characteristics of the solution were superior to those of the suppository. No difference in irritation score was identified and no discomfort was reported.

Acetaminophen↗
PubMed1999

Preoperative detection of occult enterovesical fistulas in patients with Crohn's disease: efficacy of oral or rectal administration of indocyanine green solution.

OBJECTIVES: Nonhazardous enteral administration of indocyanine green solution was performed to detect enterovesical occult microfistulas in patients with Crohn's disease before the fistulas had become readily apparent. METHODS: A total of 12 patients with Crohn's disease who were suspected from their clinical manifestations of having enterovesical fistulas underwent study. For detection of the fistulas after oral or rectal administration of the indocyanine green solution, urine was collected and examined using a colorimeter to check for contamination with indocyanine green. The effectiveness of the indocyanine green test and conventional x-ray study was compared. RESULTS: The indocyanine green test was positive after either oral or rectal administration in 11 of the 12 patients, providing a rate of accurate diagnosis of 92 percent (11/12 patients). In contrast, the rate of accurate diagnosis using the x-ray study was only 17 percent (2/12 patients). Furthermore, in eight patients with occult fistulas, accurate diagnosis could be made in none using the x-ray study, whereas all showed positive results with use of the indocyanine green test. CONCLUSIONS: The ability to diagnose obscure fistulas using the indocyanine green test was 92 percent. This indocyanine green test was highly diagnostic, whereas conventional examinations are often complicated and much less diagnostic.

Administration, Oral↗
PubMed1994

Maternal plasma progesterone levels fall after rectal administration of estriol.

Maternal plasma unconjugated estriol (E3), progesterone (P), and estradiol (E2) levels were measured at 30-min intervals for 6 h after the rectal administration of a 100-mg E3 or placebo suppository to 28 pregnant women at term. Mean plasma unconjugated E3 levels showed a sustained rise approximately 50% above baseline levels 2 h after rectal E3 administration (P < 0.003). There was a simultaneous sustained fall of approximately 20% in mean plasma P levels (P < 0.05); the fall in mean P levels was greatest in the women who delivered within 48 h of E3 suppository administration (P < 0.05). There was no change in mean plasma E2 levels. This study demonstrates that a significant rapid increase in maternal circulating E3 levels can be obtained by the rectal administration of E3, and that this increase in maternal E3 levels is associated with a decrease in circulating P levels.

Adult↗
PubMed1994

Pharmacokinetics of clonidine after rectal administration in children.

BACKGROUND: alpha 2 Agonists have been shown to produce desirable effects when used as premedication or as an adjunct to general anesthesia in adult patients. Several of these beneficial effects (e.g., reduced anesthetic requirements and analgesia without respiratory depression) would be of great benefit in pediatric anesthesia. Information regarding the use of alpha 2 agonists in children is largely lacking. The aim of this study was to investigate the pharmacokinetics of clonidine after rectal administration in children. METHODS: Ten ASA physical status 1 pediatric patients (age 14-48 months, weight 10-20 kg) received 2.5 micrograms.kg-1 of clonidine by the rectal route. Blood samples were taken during a 24-h period after the administration. Plasma levels of clonidine were analyzed by radioimmunoassay and subjected to a computer-aided curve-fitting program (PC Nonlin). To estimate the bioavailability of clonidine the results from the current study were compared with data from a previous study in which the same dose of clonidine was given to a similar patient population by the intravenous route. RESULTS: Maximum plasma concentration was 0.77 ng.ml-1 (0.62-0.88), time to maximum plasma concentration 51 min (29-70), terminal half-life 12.5 h (8.7-19.5), and bioavailability 95% (73-119) (medians [95% confidence interval]). Plasma concentrations within the adult clinically effective range (0.2-2.0 ng.ml-1) were obtained within 10 min of administration. CONCLUSIONS: Rectal administration of 2.5 micrograms.kg-1 of clonidine in children, approximately 20 min before induction of anesthesia, achieves plasma concentrations within the range known to be clinically effective in adults.

Administration, Rectal↗
PubMed1991

Pharmacokinetic study of etodolac after rectal administration; "in vitro" release kinetics.

The present study describes the pharmacokinetic behaviour of a new dosage form of etodolac not available in the Spanish market: suppositories. Rectal administration was chosen as an alternative for the oral route. The dose used was 200 mg. The pharmacokinetic parameters of the drug are estimated by means of two possible methods i.e., model-independent and model-dependent. The results obtained are compared and discussed. At the same time, an "in vitro" study of the release kinetics of etodolac from the suppository was performed using a continuous flow system without fluid recirculation or accumulating reservoir. The dissolution media used were buffered aqueous solutions at pH 6.5 and 7.4. The results obtained show that the release of the drug from the supposity could be a limiting factor for its absorption.

Administration, Rectal↗
PubMed1984

First pass conjugation of phenol following rectal administration in rats.

The systemic availability of phenol following rectal administration to rats has been compared to intraduodenal and intravenous administration via the hepatic portal and jugular veins. Phenol blood concentration-time curves after the rectal route of dosing indicate that first pass conjugation by the intestinal mucosa and liver is drastically reduced when compared to the other routes of administration.

Animals↗
PubMed1996

Rectal administration of morphine in children. Pharmacokinetic evaluation after a single-dose.

BACKGROUND: There is limited knowledge about the pharmacokinetics of morphine and its metabolites after rectal administration in children. In this study the pharmacokinetics of two different rectal formulations of morphine were examined and compared with intravenous morphine. METHODS: Children undergoing elective surgery received rectal morphine 0.2 mg/kg before start of surgery. Ten children (mean age 14 months) received morphine rectally in a hydrogel formulation and another 10 children (mean age 16 months) received morphine rectally in a parenteral formulation. For comparison, 6 children (mean age 21 months) were given the same dose intravenously. The plasma concentrations of morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) were measured by HPLC over 6 h after drug administration. RESULTS: The mean rectal bioavailability of morphine was 35% (range 18-59) after hydrogel administration and 27% (range 6-93) after the solution. Mean values of Cmax were 76 nmol/l (25-129) and 56 nmol/1 (15-140), respectively. The results showed that morphine gel had a significantly higher bioavailability (P < 0.02) than the solution. The ratios of plasma (M3G + M6G) to morphine were higher after rectal administration (mean 7.5-8.7) than after i.v. injection (mean 5.3), indicating the presence of first-pass metabolism using the rectal route. CONCLUSIONS: The rectal morphine hydrogel has pharmacokinetic properties which makes it a useful formulation for premedication and pain alleviation in paediatric patients.

Administration, Rectal↗
PubMed1985

The influence of body weight on plasma concentration of atropine after rectal administration in children.

To avoid an unpleasant injection, the rectal administration of drugs to children is often to be preferred. Very little has been published on plasma concentrations of atropine given rectally. To determine whether body weight has any influence on the plasma concentrations of atropine, 18 children weighing 7.5-55.0 kg were given 0.02 mg atropine sulphate per kg rectally, and the plasma levels of atropine were determined. The mean peak plasma concentration of atropine was 1.17 ng/ml and it was reached after 33 min. In the group of smaller children (b.w. less than 15 kg) the peak plasma concentration was (0.83 ng/ml) lower than that observed in older children (1.26-1.36 ng/ml), but this difference was not statistically significant. Plasma concentrations in the group of smaller children declined significantly faster than in the other weight groups.

Adolescent↗
PubMed1994

Acetic acid intoxication by rectal administration.

The enhanced toxicity of acid instilled directly into the rectum, without benefit of dilution and neutralization in the upper intestine, is evident in a case of acetic acid intoxication by accidental rectal administration of 50 mL of 9% acetic acid to a 5-year-old boy. The complications included necrosis of the colon, acute renal failure, acute liver dysfunction, disseminated intravascular coagulopathy (DIC) and sepsis.

Acetates↗
PubMed1985

Evaluation of portal circulation in rats by rectal administration of 201Tl followed by intrasplenic injection of 51Cr-labeled microspheres.

The heart-to-liver (H/L) uptake ratio in rats was determined 8 min after the rectal administration of 201Tl. Apart from normal controls, three groups of rats were examined; these were composed of animals with induced (1) acute hepatic damage, (2) liver cirrhosis, and (3) partial portal-vein ligation. After the rectal administration of 201Tl, 51Cr-labeled microspheres were injected into the spleen. The radioactivity of the removed liver, lungs, and heart was determined in a gamma-well scintillation counter, and the radioactivity of 201Tl and the 51Cr-labeled microspheres was separately calculated using simultaneous equations derived from the results of a preliminary experiment. The H/L ratios (201Tl) in the normal controls and the animals with acute hepatic damage were not significantly different; however, there was a positive correlation (P less than 0.01) between the H/L ratio and the shunt index (51Cr microspheres) in three groups, i.e., normal controls, liver cirrhosis, and partial portal-vein ligation.

Animals↗
PubMed1997

Mechanism of absorption enhancement in humans after rectal administration of ampicillin in suppositories containing sodium caprate.

PURPOSE: The medium chain fatty acid sodium caprate (C10) is approved as an absorption enhancer but its mechanism of action has not been studied in humans. The aim of this study was to investigate the mechanism of action of C10 in human subjects after rectal administration. METHODS: Twelve healthy human subjects were randomised to receive ampicillin suppositories with (AM-C10) or without (AM) C10. Serum and urine samples were collected and analysed for ampicillin by HPLC. Rectal biopsies were taken before and 25 min (approximate time of maximum serum concentration, Cmax, for ampicillin) and 185 min (during the final part of the elimination phase) after rectal administration of the suppositories. The osmolality of the rectal fluid was also measured. RESULTS: AM-C10 administration increased Cmax, area under the serum concentration-time curve (AUC) and urinary recovery of ampicillin 2.6-, 2.3- and 1.8-fold, respectively, compared to AM. Histological examination of the biopsies showed that AM-C10 exposure resulted in reversible mucosal damage that occurred at the same time as the Cmax for ampicillin while AM prolonged mucosal damage. A reversible increase in rectal fluid osmolality was observed with both treatments. CONCLUSIONS: AM-C10-enhanced absorption of ampicillin coincides with non-specific damage to the rectal mucosa. C10 itself as well as the suppository base and the hyperosmolality of the rectal fluid contributed to this effect. However, the histological damage was reversible with AM-C10, suggesting that C10 also has a protective effect on the rectal mucosa.

Adult↗
PubMedDate not supplied

Pharmacokinetics of heptacaine, a novel potent local anaesthetic agent, after rectal administration to rats.

The pharmacokinetics of heptacaine, N-(2-(2-heptyloxyphenylcarbamoyloxy)ethyl)-piperidinium chloride, a new long-acting potent carbanilate type local anaesthetic, proposed for local anaesthesia in complex treatment of hemorrhoids, was studied following its rectal administration to rats in the form of cocoa butter suppositories. The heptacaine plasma concentration, 0.0083% of dose/ml, peaked at 90 min post administration and the maximum rate of its bioavailability, 0.19% of dose/min, assessed by deconvolution, occurred 38 min post administration. The plasma elimination half-life of heptacaine was 133 min and its biological availability of 52% was comparable to other agents of the class.

Administration, Rectal↗
PubMed1988

Changes of portal systemic shunting after sclerotherapy and/or partial splenic embolization observed by Tl-201 per-rectal administration.

Tl-201 per-rectal scintigraphy was performed before and after injection sclerotherapy of esophageal varices and/or partial splenic embolization in patients with esophageal varices to observe the changes of portal systemic shunting by these treatments. The changes in the heart-to-liver uptake ratio of Tl-201 after injection sclerotherapy ranged widely from a decrease to an increase with the mean change rate (mean of the absolute value of change rate) +/- 1 SD of 19.0% +/- 19.9%. By partial splenic embolization the heart-to-live uptake ratio was decreased significantly with the mean change rate +/- 1 SD of 26.2% +/- 17.4% (P less than 0.05). This noninvasive and simple method seems to be useful in evaluating pathophysiological changes of portal systemic shunting observed from inferior mesenteric vein blood flow after treatments of portal circulation system.

Administration, Rectal↗