[Study on the pharmaceutical preparations for rectal administration].
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Humans↗
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Comparative studies on absorption patterns of the drug after intrarectal administration of 5-FU emulsion and 5-FU solution.
Intrarectal administration of 5-fluorouracil (5-FU) emulsion was compared experimentally with that of 5-FU solution as to the degree of absorption and tissue distribution. For the 5-FU levels in the rectal wall, the levels in the emulsion group remained at high levels during the 6 hour period after administration while the levels in the solution group decreased rapidly. For the 5-FU levels in the lymph nodes, those in the emulsion group were significantly higher (more than four times) and remained at relatively high levels for a longer period than those in the solution group. In the thoracic lymph, 5-FU levels in the emulsion group remained more than two times higher throughout the experimental period. The results suggest tha preoperative intrarectal administration of 5-FU emulsion may be effective as an adjunct to surgery for rectal cancer with lymph node metastasis, because of the long duration of high concentration resulting in the rectal lymphatics and rectal wall.
Animals↗
High-dose rectal and oral acetaminophen in postoperative patients--serum and saliva concentrations.
BACKGROUND: The primary purpose of the study was to examine the absorption of acetaminophen by measuring serum and saliva concentrations produced by a standard postoperative acetaminophen dosing regimen and secondary to examine the correlation between saliva and serum concentrations of acetaminophen after rectal and oral dosing. METHODS: Twenty-four women, aged 18-60 years, scheduled for minor gynaecological laparoscopic surgery were studied. Patients received acetaminophen 2000 mg suppositories after surgery and oral doses of 1000 mg at 4 and 8 h postoperatively. Alfentanil was available via patient-controlled analgesia. Saliva and blood samples were collected postoperatively. RESULTS: At 1, 2, 3, and 4 h after rectal dosing the saliva concentrations (mean+/-SD) were 15.2+/-5.9 micromol/l, 33.7+/-12.5 micromol/l, 45.5+/-19.1 micromol/l, and 55.4+/-23.1 micromol/l, respectively. The serum concentrations at 2 and 4 h were 31.0+/-11.2 micromol/l and 54.8+/-23.8 micromol/l, respectively. Additional oral dosing resulted in saliva concentrations at 5, 8, and 9 h of 99.7+/-49.5 micromol/l, 106.9+/-31.7 micromol/l, and 139.3+/-55.4 micromol/l, respectively, with coincident serum concentrations of 100.1 +/- 50.2 micromol/l, 105.6+/-29.0 micromol/l, and 141.2+/-52.1 micromol/l. After rectal dosing the linear regression resulted in r2=0.96, P<0.001 and saliva/ serum-ratio=0.99. After additional oral dosing the outcome of linear regression was: r2=0.90, P<0.001 and saliva/serum-ratio= 1.00. CONCLUSION: The slow and ongoing absorption process resulting in no maximum concentration within 4 h after administration of 2000 mg acetaminophen suppositories makes this rectal regimen therapeutically irrational for treatment of postoperative pain. The significant ratio and linear correlation between saliva and serum concentrations of acetaminophen suggests that saliva could be used instead of blood to monitor acetaminophen administration in patients.
Absorption↗
A high-pressure liquid chromatographic method for measuring mitotane [1,1-(o,p'-Dichlorodiphenyl)-2,2-dichloroethane] and its metabolite 1,1-(o,p'-Dichlorodiphenyl)-2,2-dichloroethene in plasma.
The adrenolytic agent mitotane [o,p'-DDD or 1,1-(o,p'-dichlorodiphenyl)-2, 2-dichloroethane] has been employed in the nonsurgical treatment of patients with adrenal carcinoma for several decades. Its use is hampered by serious side effects, which may be limited by analytically guided dose modifications in the individual patient. Mitotane analyses have previously been undertaken by gas chromatography with electron capture detection. A sensitive high-pressure liquid chromatographic method for measuring mitotane in plasma is described. After protein precipitation with 1.5 vol of acetone, mitotane and its metabolite 1,1-(o,p'-dichlorodiphenyl)-2,2-dichloroethene (o,p'-DDE) are resolved by isocratic elution from a C18 reversed-phase support and quantified by ultraviolet detection at 230 nm. Recoveries of mitotane and o,p'-DDE after deproteinization were quantitative. Within-run and between-day coefficients of variation were < 4% over the entire therapeutic range. The limit of detection was 0.25 mumol/L and the standard curve was linear in the 1-100 mumol/L range. The method has been evaluated using samples obtained from an adolescent girl who had metastatic adrenocortical carcinoma. Data from this single patient may suggest that systemic absorption of mitotane is adequate, and toxicity possibly decreased, when mitotane is administered by the rectal route.
Absorption↗
The structural barrier of absorptive mucosae: site difference of the permeability of fluorescein isothiocyanate-labelled dextran in rabbits.
The permeability of fluorescein isothiocyanate-labelled dextran (FD, M.W. 4400-71,200) across nasal, buccal, duodenal, jejunal, ileal, colonic, and rectal mucosae excised from rabbits has been measured to estimate the structural barrier of absorptive mucosae using Ussing-type diffusion chambers. The permeability coefficient of FD in all these mucosae decreased with increasing molecular weight. The rank order of FD permeability did not always correlate with the electrical resistance of the mucosae. Among components of the small intestine (duodenum, jejunum, ileum) and the large intestine (colon, rectum), however, the rank order of FD permeability corresponded to the magnitude of the electrical resistance in each instance; the upper colonic mucosa showed the highest permeability, especially in FD of low molecular weight, and permeability of the rectal mucosa was lowest except for the duodenal mucosa. The nasal mucosa showed the lowest electrical resistance and the highest permeability of those studied, suggesting that it has a leaky structural barrier.
Animals↗
Scintigraphic imaging and absorption of a 5-aminosalicylic acid enema in patients with ileorectal anastomosis.
UNLABELLED: Ileorectal anastomosis (IRA) is a possible surgical treatment for hyperacute and drug-unresponsive forms of ulcerative colitis (UC). UC relapses in the rectal remnant usually are prevented by chronic administration of 5-aminosalicylic acid (5-ASA) in topical formulations. The relationships between intestinal absorption and pattern of luminal spread of 5-ASA enemas are still unknown in patients with IRA. We correlated the absorption of a 5-ASA enema with its spread in the distal bowel of patients with IRA as assessed by 99mTc radioenema imaging. METHODS: Eight patients with UC in remission and previous IRA received a therapeutic 50-mL 5-ASA enema labeled with 99mTc-sulfer colloid. Absorbed 5-ASA and its major metabolite, acetyl 5-ASA, were measured in plasma, and dynamic images of radiolabeled enema were obtained for 6 h. The retrograde ileal spread (RIS) was determined and expressed as percentage of total enema radioactivity. Plasma levels of 5-ASA and acetyl 5-ASA were measured in six healthy volunteers after administration of the same enema volume with no radiolabeling. RESULTS: The mean 5-ASA plasma level was 0.70 microg/mL (range 0.37-0.95 microg/mL) in patients and 0.96 microg/mL (range 0.78-1.16 microg/mL) in healthy volunteers (P = not significant), and the mean acetyl 5-ASA plasma levels were 0.89 microg/mL (range 0.44-1.19 microg/mL) and 0.84 microg/mL (range 0.51-1.02 microg/mL), respectively (P = not significant). Radioenema imaging allows RIS assessment of patients with IRA. The mean value was 8.5% (range 2%-19.3%) of administered radioactivity, which correlated significantly with the total absorption of 5-ASA in the IRA group (P = 0.033, linear correlation test). Rectal wall contractions recognized by dynamic radioenema imaging were defined as a common cause of RIS episodes. CONCLUSION: In IRA patients, 5-ASA plasma levels were similar to those in healthy volunteers after administration in enema. Only part of a 50-mL 5-ASA enema reaches the ileum, and radiolabeled imaging shows the degree and number of these RIS episodes. The absorption of 5-ASA can increase in patients compared with healthy volunteers, in the presence of either occasional but significant ileal spread associated with postural factors and abdominal wall contraction or multiple moderate episodes of radioenema backdiffusion related to rectal wall motility.
Adult↗
Pharmacokinetic and pharmacodynamic aspects of artelinic acid in rodents.
The efficacy of artelinic acid and artemisinin, orally administered at 10 and 50 mg kg-1 day-1, was compared in Plasmodium berghei infected mice. Subsequently, the pharmacokinetics of artelinic acid after intravenous, intramuscular, oral and rectal administration of a 20 mg kg-1 aqueous solution to rabbits were studied in a four-way randomized cross-over experiment. After intravenous administration, artelinic acid concentrations in blood plasma were high (C0: 76 +/- 15 mg L-1), and the drug was rapidly eliminated from the central compartment, showing linear elimination kinetics with an elimination half-life of 15 +/- 3 min. A large inter-subject variation appeared in the absorption rate and the extent of absorption (2-92%) over the 120 min interval after intramuscular administration. Also, a large inter-subject variation in individual rectal bioavailability (17-100%) was shown, which was dependent on the site of absorption in the rectum. The estimated oral bioavailability was low (4.6 +/- 1.7%), probably due to a high first-pass effect and possible decomposition in the acidic gastric environment.
Absorption↗
Pentobarbital absorption from capsules and suppositories in humans.
Serum pentobarbital levels following administration of the sodium salt as a 100-mg capsule orally and as two 120-mg suppository formulations (A and B) rectally were measured. From these data and previously determined kinetic constants after intravenous administration, the absorption rates and bioavailability of pentobarbital from each dosage form were determined. All three dosage forms were 100% absorbed. Peak serum pentobarbital levels occurred at 1, 4, and 10 hr for the capsule, Suppository A, and Suppository B, respectively. In vitro studies agreed with the serum data in that Suppository A released drug in an in vitro aqueous pH 1.4 system at a much greater rate that Suppository B. The capsule and Suppository A both appeared to be absorbed by simple first-order processes; however, Suppository B had a complex absorption pattern, which was modeled using sequential zero-order and first-order absorption.
Administration, Oral↗
Pharmacokinetics of indomethacin.
Plasma concentrations of indomethacin have been studied in 5 healthy volunteers after single and multiple doses (25 mg intravenously [iv], 25, 50, and 100 mg orally, 100 mg rectally, and 25 mg three times daily [tid]. In 8 other normal subjects and in 5 patients a 50-mg oral dose of indomethacin was given and the indomethacin concentration was followed from 8 to 32 hr after dosing. All analyses were carried out using a new mass fragmentographic method. After oral and rectal doses the plasma decay of indomethacin was biphasic, and the data were interpreted according to a 2-compartment open model. The half-life of the beta-phase varied between 2.6 and 11.2 hr. The volume of distribution ranged from 0.34 to 1.57 L/kg and the plasma clearance from 0.044 to 0.109 L/kg/hr. There was no evidence of dose-dependent elimination. Indomethacin was rapidly and well absorbed after oral dosing with peak plasma concentrations within 2 hr. Comparison with the area under the curve (AUC) after iv dosing indicated complete bioavailability. The AUC after rectal dosing indicated complete bioavailability, but the rate of absorption was slower than after oral administration. Indomethacin, 25 mg three times daily, was also given for 9 days to the same normal subjects; equilibrium concentrations obtained did not differ significantly (p greater than 0.1) from those predicted from single-dose data in the 5 subjects.
Administration, Oral↗
Iodine toxicity: an unusual cause of cardiovascular collapse during anesthesia in an infant with Hirschsprung's disease.
This report describes a case of acute life-threatening iodine toxicity in an infant with Hirschsprung's disease caused by rectal irrigation with povidone-iodine. A hypothesis regarding absorption and recommendations for povidone-iodine usage for bowel preparation are presented.
Anesthesia, General↗
Nonenteral routes of administration for psychiatric medications. A literature review.
In the treatment of psychiatric patients with complicating medical illness, clinicians may encounter patients who cannot take oral medications. This review will acquaint the practicing clinical psychiatrist with psychotropic medications available by nonenteral routes of administration. A computerized MEDLINE search was conducted of the literature 1981 to 1997. All articles citing nonenteral routes of psychotropic medication administration were reviewed. The results are summarized according to drug class and specific routes of administration (intravenous, intramuscular, sublingual, rectal). Psychotropic medications now available by these alternative routes are also listed in table form. The majority of the information available comes from small case series or case reports. Intravenous and intramuscular routes of administration of psychotropics are the most common. In addition, certain psychotropics are available by less common routes, such as sublingual or rectal administration. Consideration of alterations in pharmacokinetics, including poorer absorption and slower metabolism, are discussed. Clinicians may need to consider these novel routes of medication administration when dealing with patients unable to take oral medications.
Drug Administration Routes↗
Equine lymphocytic-plasmacytic enterocolitis: a retrospective study of 14 cases.
Lymphocytic-plasmacytic enteritis (LPE) is a morphological diagnosis given to a type of infiltrative intestinal disease classified within the complex of idiopathic inflammatory bowel disease (IBD). The purpose of this retrospective study was to describe the details of breed, age and sex, clinical and clinicopathological findings and outcome of horses diagnosed with LPE. Data were reported from 14 horses that had a histopathological diagnosis of LPE; the median age was 12 years, and there was no breed or sex predilection. Common clinical signs were weight loss (100%), diarrhoea (50%) and lethargy (50%). Hypoproteinaemia and hypoalbuminaemia were present in 6/13 (46%) and 9/12 (75%) horses, respectively. Results of the oral glucose tolerance tests or D-xylose absorption tests were abnormal in 9/12 (75%) horses and rectal mucosal biopsies were abnormal in 3/7 (43%) horses. Corticosteroid treatment was used unsuccessfully in 4 horses. All horses were subjected to euthanasia and LPE was diagnosed at necropsy. Diffuse thickening of the small intestine was apparent grossly in 10/13 (77%) horses examined. LPE is an uncommon equine intestinal disease that is difficult to diagnose antemortem and has a poor prognosis.
Adrenal Cortex Hormones↗
Pharmacokinetics of oxicam nonsteroidal anti-inflammatory agents.
Oxicam nonsteroidal anti-inflammatory drugs (NSAIDs) are a group of structurally closely related substances with anti-inflammatory, analgesic and antipyretic activities. They have a weakly acidic character and are extensively bound to plasma proteins. Piroxicam, the most widely used oxicam, is well absorbed after oral administration. Peak plasma concentrations (Cmax) of the drug are reached within 2 to 4 hours. Piroxicam has a small volume of distribution and a low plasma clearance. It undergoes hepatic metabolism and only 5 to 10% is excreted unchanged in urine. The elimination half-life varies between 30 and 70 hours. Age of the patient and renal or hepatic dysfunction do not seem to have any major effect on the pharmacokinetics of piroxicam. The drug reduces the renal excretion of lithium to a clinically significant extent, but the clinical significance of piroxicam-aspirin (acetylsalicylic-acid) and piroxicam-acenocoumarol interaction has not been established. Ampiroxicam, droxicam and pivoxicam are prodrugs of piroxicam that have been synthesised to reduce piroxicam-related gastrointestinal irritation. All prodrugs are well absorbed, but Cmax values are reached later than those following administration of piroxicam. Tenoxicam is used in the management of rheumatic and inflammatory diseases. Mean Cmax values are achieved 2 hours postdose. Food reduces the rate but not the extent of absorption. The oral bioavailability of tenoxicam is 100% and rectal bioavailability is 80%. Like piroxicam, tenoxicam has a low volume of distribution and low plasma clearance. It is eliminated through hepatic metabolism. The mean elimination half-life is 60 to 75 hours. The pharmacokinetics of tenoxicam are independent of patient age, or concurrent liver or renal diseases. High doses of aspirin have been shown to increase the elimination of tenoxicam, but this has little clinical significance. Isoxicam was in widespread clinical use until its worldwide marketing was suspended because of fatal skin reactions. Isoxicam is completely absorbed, but Cmax values are not reached until 10 hours postdose. It has a low plasma clearance, approximately 5 ml/min (0.3 L/h), and low volume of distribution. The mean elimination half-life is 30 hours and does not appear to be affected by the age of the patient. Isoxicam potentiated the anticoagulant effect of warfarin, necessitating a 20% dosage reduction. Lornoxicam differs from other oxicam NSAIDs because it has a short elimination half-life of 3 to 4 hours. On the basis of limited data, some individuals seem to eliminate lornoxicam very slowly, suggesting the presence of polymorphic metabolism. The pharmacokinetics of cinnoxicam and sudoxicam have not been studied thoroughly.(ABSTRACT TRUNCATED AT 400 WORDS)
Aging↗
[The effect of ion pair formation on the pharmacokinetics of drugs. 2. The effect of hexylsalicylic acid on the pharmacokinetics of quinine].
The influence of the hexylsalicylic acid (2) on the pharmacokinetic of the quinine (1), was studied using rabbits. It could be observed that after i.v. application the mean resistance time (MRT) of 1 was increased by means of ion-pair-formation with 2. But the AUC of 1 was not influenced. After rectal application of the combination 1/2 an acceleration of the 1 absorption could be pointed out. The kinetic parameters of 2 were not increased significantly if 1 was applicated simultaneously.
Administration, Rectal↗
The pharmacokinetics of oxprenolol following oral and rectal dosing--a comparison of delivery systems and routes of administration.
Plasma oxprenolol concentrations were measured in eight healthy volunteers who received equivalent oral doses of the drug in the form of an aqueous solution and a 10/170 oxprenolol Oros drug delivery system. Absorption from the lower gastrointestinal tract was assessed by measurement of plasma concentrations after rectal administration of the pre-equilibrated Oros systems. Because three of the first four volunteers suffered local irritation, however, the other four volunteers received Slow Trasicor 160 mg orally as a comparative preparation. The rate of in vivo absorption after oral administration of the Oros system closely mirrored its in vitro release rate. Drug availability from Oros was reduced, however, and was equivalent to 77% of that from the oral solution. Oxprenolol was well absorbed from the rectum while the system was present in this segment of the gut. The reduced systemic availability in three of the volunteers could be accounted for largely by drug loss when the system was expelled. Slow Trasicor produced higher peaks but lower 24 h plasma concentrations than the orally administered Oros system. As judged from the relative areas under the plasma concentration-time curve, however, the availability of the drug from the two dosage forms was comparable.
Administration, Oral↗
Absorption of ipsapirone along the human gastrointestinal tract.
Isapirone-HCl (5 mg) was administered orally, rectally and locally, by a remote control drug delivery device (HF-capsule) into different segments of the gastrointestinal tract, to four young healthy male adults. The relative systemic bioavailability of the drug from the colon and rectum was 2-3-fold greater than that from the upper gastrointestinal tract. This supports a rationale for a prolonged-release formulation.
Administration, Oral↗
[Nutrition physiologic studies of swine with ileorectal anastomoses. 1. Surgical method, biochemical and morphologic findings].
For the purpose of studying nutrient digestion and absorption in the small intestine, pigs were provided with ileo-rectal anastomoses. The anaesthetic and operation method is described. X-ray examinations do not show a significant backflow of digesta into the from colon cranially open towards the anastomosis as well as a totally intact sphincter ani. With the help of additional doses of highly digestible, N-free nutrients rich in energy (starch + saccharose), the operated animals achieved a growth development corresponding to that of intact control animals. For the assessment of the physiologic state of the animals, the concentrations in the serum of the total protein, of albumin, urea, glucose, calcium, inorganic phosphorus and creatinine as well as the activities of aspartate amino transferase and alkaline phosphatase were determined. These showed for the respective criteria changes conditioned by age and dependent on feed intake. The fixing of the anastomoses did not result in disturbances of nutritional or organic damages. Histologic studies of the mucosa of stomach, duodenum and jejunum did not show pathologic changes. The weight of stomach, duodenum and jejunum, determined in 2 live weight ranges, is identical for operated and intact animals in relation to the weight of the empty body of the animals. The weight of ileum, caecum and colon of the operated animals is significantly lower, due to inactivity atrophy. The tissue amount available for the intake of a volume unit (weight-volume index) is nearly identical for operated and intact animals in the duodenum and the jejunum. The index functionally increasing for intact animals from the jejunum to the ileum (stenosis due to temporary digesta congestion in the ileum) remained the same with anastomosis animals for 29 or 26 weeks resp. after the operation. As a result of the biochemical and morphological studies it was shown that animals with an ileo-rectal anastomosis are suitable for the determination of nutrient digestibility at the end of the ileum.
Alkaline Phosphatase↗
[Experimental research on absorption and hypoglycemic action of N1-sulfanilyl-N2-n-butyl urea and N-4-methyl-benzene sulfonyl-N1-butyl urea, rectal administration].
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Administration, Rectal↗