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At least 631 records · Page 35Linked to original sources
PubMed1999

Effect of preoperative paracetamol on gastric volumes and pH in children.

The effect preoperative paracetamol elixir has on gastric contents is unknown. Children presenting for elective adenotonsillectomy were randomized to receive either paracetamol elixir (40 mg x kg(-1)) 90 min before surgery or paracetamol suppositories (40 mg x kg(-1)) intraoperatively. Following induction of anaesthesia a 16 Fr multiple-oriface orogastric tube was passed into the stomach and measure taken of the residual gastric volume and pH. The children had a mean age of 8.5 years (SD 3.2) with a weight of 35 kg (SD 16.5). Children given elixir (n=41) had a mean residual gastric volume of 0.083 ml x kg(-1) (95% CI; 0.006, 1.24) and a pH of 1.83 (95% CI; 0.75, 4.49), while those given suppositories (n=40) had a mean residual gastric volume of 0.083 ml x kg(-1)(95% CI; 0.008, 0.9) and a pH of 2.07 (95% CI; 0.84, 5.12). There was no significant difference between these two groups. Paracetamol elixir is rapidly absorbed in the gastrointestinal system of children and preoperative administration has no effect on gastric contents. Given paracetamol's slow equilibration rate constant from the central to the effect compartment, children may be given this medication preoperatively for routine surgical procedures.

Absorption↗
PubMed2000

Effects of alosetron on gastrointestinal transit time and rectal sensation in patients with irritable bowel syndrome.

BACKGROUND: Alosetron, a 5-HT3-receptor antagonist, relieves abdominal pain and improves bowel function in non-constipated, female patients with irritable bowel syndrome. 5-HT3 antagonists delay colonic transit, increase colonic compliance, and increase small intestinal water absorption. AIM: To evaluate the effects of alosetron on gastrointestinal and colonic transit, rectal compliance and rectal sensation in irritable bowel syndrome. METHODS: A double-blind, placebo-controlled, two-dose study of alosetron was performed in 25 non-constipated irritable bowel syndrome patients, with paired studies before and after 4 weeks of treatment with placebo (n=5), 1 mg alosetron (n=10) or 4 mg (n=10) alosetron b.d. Gastrointestinal and colonic transit were measured by scintigraphy. Rectal compliance and sensation were assessed by rectal balloon distention with a barostat. RESULTS: There was a trend (P=0.06) for 1 mg alosetron to increase rectal compliance (median pressure at half maximum volume 11 mmHg after alosetron vs. 15.6 mmHg before alosetron). The 1 mg b.d. alosetron dose non-significantly retarded proximal colonic transit. Alosetron and placebo reduced sensory scores relative to baseline values; none of the changes induced by alosetron was significant relative to placebo. CONCLUSIONS: Alosetron had no significant effect on gastrointestinal transit or rectal sensory and motor mechanisms in non-constipated irritable bowel syndrome patients in this study. Alosetron's effects on colonic sensorimotor function and central sensory mechanisms deserve further evaluation.

Adult↗
PubMedDate not supplied

[Peri-rectal infectious cellulitis with septicemia of anal origin. Suppository on trial].

Rectal route with local or general effects, is an interesting possibility of treatment. Easy use and rapid absorption are two major advantages. But this therapeutic modality is not riskless. We report a case of septicemia with peri-rectal cellulitis which was generated by two ano-rectal ulcerations after using Trophires suppositories. The infection was favoured by local application of cortisone. Our original observation, with ano-rectal ulcerations and short use of suppository, confirms the idea of short-term treatment stopped in case of unwanted symptom.

Adult↗
PubMed1984

Relationship between rectal mucosal prostaglandin production and water and electrolyte transport in ulcerative colitis.

We have used in vivo rectal dialysis to test the hypothesis that the diarrhoea of patients with active ulcerative colitis (UC) is due to inhibition of large intestinal salt and water absorption by enhanced local mucosal prostaglandin (PG) synthesis. In 28 patients with untreated UC, increased rectal mucosal PGE2 release varied inversely with sodium transport and directly with potassium transport; higher PGE2 release was also associated with lower (i.e. less negative) potential difference (PD). Disease activity assessed sigmoidoscopically was positively related to PGE2 release, potassium transport and lower PD. Similar relationships were found in 33 patients treated with sulphasalazine and/or corticosteroids and in 9 patients studied serially when on unaltered conventional, or no treatment. In contrast, when 10 patients with UC were given the PG synthesis inhibitor, flurbiprofen, a significant fall in PGE2 release was associated with deteriorations in mucosal PD and transport of sodium and potassium. Increased PG production is therefore unlikely to be a major determinant of the abnormalities of electrolyte transport found in UC. The correlations between mucosal PGE2 release and electrolyte transport were probably due to the relationship of these variables with some other consequence of tissue damage.

Adrenal Cortex Hormones↗
PubMed1999

Recent trends in drug delivery systems: intranasal drug delivery.

Nasal route of drug delivery is commonly known for treatment of local ailments like-cold, cough, rhinitis etc. Recently, efforts have been made to deliver various drugs, specially peptides and proteins, through nasal route for systemic use; utilizing the principles and concepts of rate controlled drug delivery and various polymers and absorption promoters. Considering the large number of problems associated with oral, parenteral, rectal and other routes of drug administration and gradual increase in interest of pharmaceutical scientists towards exploring the possibilities of intranasal delivery of various drugs, this article aims at giving an insight into nasal cavity, consideration of factors affecting and strategies to improve drug absorption through nasal route, pharmaceutical dosage forms and delivery systems with examples of some peptides for intra nasal delivery, its advantages and limitations.

Administration, Intranasal↗
PubMed1994

Endocrine and mucous differentiation by a cloned human rectal adenocarcinoma cell line (HRA-19) in vitro: inhibition by TGF-beta 1.

Colorectal epithelium is composed of absorptive, mucous and endocrine cells, all of which are considered to arise from a common stem cell located in the crypt base. However, the factors controlling the commitment to differentiate are poorly understood. This is partly due to the lack of in vitro model systems for the study of differentiation in colorectal epithelium. The HRA-19 cell line, established from a human rectal adenocarcinoma, has been shown to have multipotential characteristics with cloned HRA-19 cells able to differentiate into absorptive, mucous and endocrine cells when grown as xenografts. The lack of such differentiated cells in HRA-19 monolayers in vitro suggests that differentiation is controlled by extracellular matrix, stromal cells and/or soluble factors. Such observations show that differentiation in HRA-19 cells can be controlled by extrinsic factors and therefore provide a model system for studying control of differentiation in colorectal epithelium. Unfortunately, the restriction of differentiation to xenografts of the cell line limits the degree to which this differentiation can be manipulated. In this study, the possibility that HRA-19 cells could be induced to differentiate in vitro under appropriate conditions has been investigated. Endocrine and mucous cells were identified by immunocytochemistry with differentiation-related antibodies and histology of monolayers. Preconfluent HRA-19 cells grown in 10% foetal calf serum formed a well polarised monolayer with apical tight junctions and sparse microvilli, but cells with mucous or endocrine phenotypes were only very occasionally observed. However, endocrine and mucous cells could reproducibly be demonstrated in postconfluent monolayers grown in 1% foetal calf serum.(ABSTRACT TRUNCATED AT 250 WORDS)

Adenocarcinoma↗
PubMed1991

[Erythromycin pharmacokinetics in children after rectal and oral administration].

Pharmacokinetics of erythromycin base was studied clinically in children not older than 14 years treated with new children dosage forms of the antibiotic i. e. 0.1 and 0.25 g enteric coated tablets and 0.06 and 0.125 g suppositories. It was noted that the new dosage forms were characterized by higher availability which was 2.5-3 times higher than that after using the erythromycin base tablets without the coating. Systematic increasing of erythromycin availability after the use of the rectal suppositories was observed with increasing of the children age. Absolute absorption in newborns, sucklings and children over 1 year amounted to 28, 36 and 54 per cent respectively.

Administration, Oral↗
PubMed2001

Trans-rectal ultrasonography (TRUS) with lipiodol injection for localization of the prostatic apex before radiotherapy planning.

PURPOSE: To evaluate reliability of Trans-rectal ultra-sonography (TRUS) guidance with lipiodol injection for prostate localization before radiotherapy planning. MATERIAL AND METHODS: From October 1997 to March 2000, 31 patients with prostatic adenocarcinoma and six patients with anastomotic recurrence after radical prostatectomy had TRUS-guided injection of lipiodol. Two milliliters of lipiodol were injected into each side of the prostate and 1 ml into both seminal vesicles with a 22 Gauge CHIBA needle and US probe guide before radiotherapy planning. We had established a contrast quality index (0 for no prostate enhancement to 5 for efficient pacification without any diffusion). On simulation films, we had performed anatomic measurements for comparison with other anatomic studies. RESULTS: For all 37 patients, TRUS-guided injection was well tolerated. Among 31 patients with the prostate in situ, three had no apex opacification and 15 had no vesicle enhancement or peri-vesicle space diffusion. However, in 19 patients there was good contrast quality with an index score of > or =3. The majority of patients had prostatic apex between 1.5 and 3.5 cm from ischial tuberosities ligne (27 from 28 evaluable for apex). Among 19 evaluable patients, 15 had seminal vesicles 2-4 cm above the top of pubis. For six patients with anastomotic recurrence after radical prostatectomy, lipiodol was precious aid to locate it. We had only one failure because of a precocious bladder absorption relating to a delay which is too long between rectal probe locating and portal films. CONCLUSION: TRUS injection of lipiodol is a simple, inexpensive, relatively safe technique for localization of prostatic apex, but not appropriate for seminal vesicles enhancement. This is also an interesting method to locate anastomotic recurrence.

Contrast Media↗
PubMed1994

Comparison of the pharmacokinetics of an ondansetron solution (8 mg) when administered intravenously, orally, to the colon, and to the rectum.

Ondansetron, an antagonist of the serotonin type 3 (5-HT3) receptor, is indicated for the treatment of chemotherapy-induced emesis. This study compares the pharmacokinetics, especially the bioavailability, of an ondansetron 8-mg solution when administered intravenously, orally, to the colon via nasogastric intubation, and to the rectum using a retention enema. Six healthy, male volunteers received ondansetron infused into the colon during the first treatment period. These subjects then received the remaining three treatments in random order, with a minimum 1-week washout period between treatments. Serial plasma samples were obtained for up to 24 hr after dosing in each treatment period. Absolute bioavailability after the oral dosing, colonic infusion, and rectal administration averaged 71 +/- 14, 74 +/- 26, and 58 +/- 18%, respectively. These values were not significantly different (P > 0.05). Values of Tmax and Cmax were also not significantly different among the nonparenteral routes. Mean absorption half-lives were 0.66, 1.1, and 0.75 hr after the oral, colonic, and rectal administrations, respectively. These results indicate that ondansetron is well absorbed in the intestinal segments studied including the upper small intestine, the colon, and the rectum and that sustained-release and suppository formulations of ondansetron are feasible.

Administration, Oral↗
PubMed1994

Calcium salts for treating hypocalcemia: carrier effects, acid-base balance, and oral versus rectal administration.

Oral Ca salt supplements are being used to combat hypocalcemia in dairy cows. The absorption of these Ca supplements is dependent on the salt and carrier used. In the studies presented, the magnitude of the rise in plasma Ca concentration following administration of the Ca preparation was used as an index of Ca absorption by the gastrointestinal tract. Calcium chloride preparations in a water-soluble carrier (propylene glycol) were absorbed more readily than Ca propionate in propylene glycol, but Ca propionate effected a more sustained increase in plasma Ca concentration. Vegetable oil preparations of these salts were poorly absorbed. Calcium chloride preparations induced a significant decrease in blood and urine pH. Calcium propionate salts did not alter acid-base balance. Rectal administration of Ca salts could raise plasma Ca concentration rapidly, but caused serious pathological lesions, precluding their use.

Acid-Base Equilibrium↗
PubMedDate not supplied

Clinical Pharmacokinetics of indomethacin.

Indomethacin (1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid) is an anit-in-flammatory antipyretic drug commonly used for symptomatic relief of pain and stiffness in rheumatic diseases. Following oral administration the absorption of the drug is rapid and complete, but with important inter-and intraindividual variations. In general, peak plasma concentrations of 2 to 3 microgram/ml are achieved with 1 to 2 hours, but concomitant ingestion of food reduces and delays the peak concentrations without reducing the amount absorbed. Rectal administration is associated with earlier but lower peak plasma concentrations, incomplete absorption form suppositories, and offers no clinical advantages when compared with equivalent oral dosage. In plasma at 90% of indomethacin is bound to albumin at therapeutic plasma concentrations. Indomethacin is distributed into the synovial fluid, is excreted in human breast milk and crosses the placenta in significant amounts. It is metabolised to O-desmethylindomethacin, N-deschlorobenzoylindomethacin and O-desmethy-N-deschlorobenzoylindomethacin, which are devoid of anti-inflammatory activity and are present in significant amount in the plasma. About 60% of an oral dose is excreted in the urine predominantly in glucuronidated form, while about 40% is excreted in the faeces after biliary secretion. A large amount of the dose undergoes biliary recycling. The biotransformation is independent of the route of administration. A 2-compartment open model with correction for biliary recycling can be used to describe the disposition of indomethacin. The drug has a biological half-life of about 5 to 10 hours and a plasma clearance of 1 to 2.5ml/kg/min. In premature infants the half-life of indomethacin is inversely correlated with gestational age and is significantly prolonged as compared with adults. Renal failure does not affect the serum concentrations of indomethacin. Probenecid results in increased plasma concentrations of indomethacin with enhanced pain relief without increasing the incidence of side effects. There seem to be no significant pharmacokinetic interactions between indomethacin and aspirin or warfarin. To date it has not been possible to identify a relationship between the clinical effects and plasma concentration of indomethacin.

Acute Kidney Injury↗
PubMed1995

Rectal methadone in cancer patients with pain. A preliminary clinical and pharmacokinetic study.

BACKGROUND: Cancer pain can be treated in most cases with oral analgesics. However, during their clinical history, 53% to 70% of patients will need alternative routes of opioid administration. The rectal administration of opioids is a simple alternative route for many patients. There are no data in the literature regarding the pharmacodynamics and pharmacokinetics of rectal methadone. PATIENTS AND METHODS: We evaluated the analgesia, tolerability and absorption profile of methadone hydrochloride in six opioid-naive cancer patients with pain. A blood sample was collected before administration of a single dose of drug (10 mg) and then again after fixed times. At these fixed times the patients were asked about pain, nausea and drowsiness by means of a visual analogue scale of 0-100 mm (VAS). RESULTS: Pain relief was statistically significant as early as 30 minutes and up to eight hours after methadone administration. None of the patients reported significant side effects. The pharmacokinetics of rectal methadone showed rapid and extensive distribution phases followed by a slow elimination phase. CONCLUSIONS: Rectal methadone can be considered an effective analgesic therapy for patients with cancer pain for whom oral and/or parenteral opioids are not indicated or available.

Administration, Rectal↗
PubMed1988

Chloroquine absorption in children from polyethylene glycol base suppositories.

Chloroquine phosphate (CP) has been formulated in a suppository base consisting of polyethylene glycol, PEG 1000 and PEG 6000 (7:3) with 0.5% polysorbate 80 included as an absorption promoter. Peak chloroquine blood levels in children (mean body weight 10 kg, age 21 months) were 0.67 +/- 0.08 micrograms/ml (after 200 mg CP) and 1.06 +/- 0.23 micrograms/ml (after 300 mg CP) following rectal administration of the suppositories. Prior to drug administration, the base level chloroquine was 0.30 +/- 0.02 micrograms/ml. Elimination half lives calculated from the rapid phase of log concentration-time curves were 3.3 h (after 200 mg CP) and 2.7 h (after 300 mg CP), respectively. Based on literature evidence the blood levels obtained with the 300 mg CP suppositories would be therapeutic in the management of malaria and rheumatoid disease.

Absorption↗
PubMed1984

Serum concentration patterns of an LHRH agonist, gonadotrophins and sex steroids after subcutaneous, vaginal, rectal and nasal administration of the agonist to pregnant rats.

A highly potent LHRH agonist, des-Gly10-[D-Leu6]-LHRH-ethylamide (TAP-144), was administered by subcutaneous, vaginal, rectal and nasal routes to pregnant rats on Day 10. After subcutaneous administration, almost all the TAP-144 was rapidly absorbed and eliminated. After vaginal administration, the fraction of the dose that reached the systemic circulation, the F value, was very high but the rate of absorption was very low; consequently there was a low peak level and persistence of serum level. After rectal administration, the F value was very low and the rate of absorption was lower than that by the subcutaneous route; consequently the terminal phase half-life was between those of the subcutaneous and vaginal routes. After nasal administration, the F value was also very low but the rate of absorption was enormously high and there was a rapid decrease in serum concentration. The pregnancy-terminating effectiveness of the peptide by these routes of administration was not proportional to the transient high concentrations of the peptide but attributable to its persistence in the serum. Serum LH and FSH concentrations after TAP-144 administration showed similar patterns with the different routes but the peak concentration of LH after vaginal administration was higher than that after other routes. Serum levels of progesterone and oestradiol-17 beta showed small peaks within 2 h after TAP-144 was administered by any route and fluctuated thereafter but the level dropped only in the rats given a dose of TAP-144 that was 100% effective in terminating pregnancy.

Administration, Intranasal↗
PubMed1986

Endocrine differentiation by a human rectal adenocarcinoma cell line (HRA-19).

Colorectal epithelium is composed of a variety of cell types, including absorptive, mucous and endocrine cells. All of these cell types are thought to arise from stem cells located at the base of the crypt. However, the factors which control these differentiation pathways are poorly understood. In attempts to establish differentiated in vitro systems, one approach has been to grow primary human colorectal adenocarcinomas as cell lines. Some of these cell lines retain a sufficient number of the differentiated features of their tissue of origin to make them useful experimental systems for studying differentiation. This study describes the characterisation of such a cell line, the HRA-19 line. HRA-19 cells were derived from a primary human rectal adenocarcinoma. The cells grew as monolayers in vitro on tissue-culture plastic and remained pleomorphic even after 150 passages in vitro. Some colonies of cells expressed alkaline phosphatase activity, an enzyme normally expressed in vivo by absorptive cells of the upper crypt and surface epithelium. No evidence of differentiation into goblet or endocrine cells was obtained in monolayer cultures of HRA-19 cells. Xenografts of this cell line contained cells with the ultrastructural characteristics of absorptive and endocrine cells. These endocrine cells exhibited Grimelius silver staining, displayed formaldehyde-induced fluorescence and contained many basally located, electron-dense granules. When grown as monolayers, clones of this cell line retained the heterogeneity with respect to morphology and alkaline phosphatase expression of the parent cell line. It is proposed that this cell line is derived from malignant progenitor cells which retain the ability to differentiate.(ABSTRACT TRUNCATED AT 250 WORDS)

Adenocarcinoma↗
PubMed1999

Evaluation of colonic absorbability of drugs in dogs using a novel colon-targeted delivery capsule (CTDC).

A series of dog studies were performed to examine the in vitro/in vivo relationship of drug release behavior of the newly developed colon-targeted delivery capsule (CTDC). The four kinds of CTDCs containing theophylline, each of which has a different in vitro dissolution lag time, were orally administered to four beagle dogs under fasted condition, and the onset times of drug absorption were compared. The CTDC with longer in vitro lag time had a later onset of drug absorption. It was also found that the time difference between the gastric emptying and the onset of drug absorption was almost equal to the in vitro dissolution lag time of the capsule, suggesting a similar performance of CTDC in the gastrointestinal tract. From the comparison to the absorption behavior of the colon arrival marker, i.e. sulfasalazine, it was proved that the CTDC with the lag time of 3 h can deliver the drug directly to the colon. This result implied that the CTDC can be used as a non-invasive means for assessing the regional absorbability of drugs in the gastrointestinal tract. To evaluate the absorbability of drugs in the colon, three model drugs, theophylline (THEO), acetaminophen (ACET), and phenylpropanolamine hydrochloride (PPA) were directly delivered to the colons of beagle dogs using the CTDC with the lag time of about 3 h. The obtained relative bioavailabilities to the solution form were as high as 94.2%, 71.0%, and 91.5% for THEO, ACET and PPA, respectively, suggesting that the colonic absorbability of those drugs is essentially good.

Absorption↗