Barium infiltration of the rectal wall.
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Barium Sulfate↗
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Results for “Rectal Absorption”
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Absorption of some cephalosporins by rectal route in rabbits.
In order to obtain an effective alternative to parenteral administration of several cephalosporins, experiments were carried out in rabbits by rectal route. The suppositories of cefotaxime (CTX), ceftazidime (CAZ) and cefoxitin (CFX) in association with surface active sodium lauryl sulfate (SLS), release the antibiotic for absorption. Based on the positive results of the comparative plasmatic levels, this dosage appears to be applicable to humans too.
Administration, Rectal↗
First-pass elimination of lidocaine in the rabbit after peroral and rectal route of administration.
Lidocaine shows pronounced first-pass metabolism upon peroral administration in man (about 30 per cent peroral bioavailability). Since the rectal bioavailability is about 65 per cent in man it is assumed that some drug is directly absorbed into systemic circulation by-passing the liver. In rats peroral bioavailability is about 8 per cent whereas rectal bioavailability is about 100 per cent. This indicates that the rat is not a suitable model to study rectal lidocaine dosage forms. The purpose of this study was to investigate lidocaine disposition and bioavailability in rabbits after peroral and rectal administration. The peroral bioavailability in rabbits was found to be about 6 per cent and the rectal bioavailability is about 33 per cent. The results indicate that the rabbit is a suitable model for the study of systemic absorption of rectal lidocaine dosage forms.
Administration, Oral↗
Biopharmaceutical evaluation of carprofen following single intravenous, oral, and rectal doses in dogs.
Absorption and disposition characteristics of carprofen were compared in the dog after intravenous, oral, and rectal administrations. Rectal formulations included an aqueous solution and a suppository. Single doses of 100 mg carprofen were given in a cross-over design and plasma concentrations of unchanged drug were determined by HPLC. Plasma concentration-time profiles could be adequately described after intravenous and extravascular administrations by tri-and biexponential functions, respectively. After intravenous applications the basic disposition parameters could be determined: mean (+/- S.D.) elimination half-life was about 11.7 (+/- 3.1) h; volume of distribution ranged from 0.12 to 0.22 l kg-1 and total plasma clearance was about 0.017 +/- 0.003 l h kg-1. After oral dosing, carprofen was rapidly absorbed (time of maximum concentration: 0.83 +/- 0.61 h) and comparison with the intravenous solution indicated complete bioavailability. After rectal administration, the rate of absorption evaluated through tmax and calculation of mean absorption times was always slower than after oral dosing. Relative bioavailabilities of the drug from the suppository were about 20 per cent lower than from rectal solutions. No significant difference in rates of absorption of carprofen from rectal solution and suppository was seen; this allowed the conclusion that drug release from the semi-solid dosage form was not the rate-limiting step in carprofen absorption from the suppository. From the present study, it is concluded that rectal administration of carprofen offers an alternative to the oral route of drug intake.
Administration, Oral↗
Pharmacokinetics and pharmacodynamics of the nitroimidazole antimicrobials.
Metronidazole, the prototype nitroimidazole antimicrobial, was originally introduced to treat Trichomonas vaginalis, but is now used for the treatment of anaerobic and protozoal infections. The nitroimidazoles are bactericidal through toxic metabolites which cause DNA strand breakage. Resistance, both clinical and microbiological, has been described only rarely. Metronidazole given orally is absorbed almost completely, with bioavailability > 90% for tablets; absorption is unaffected by infection. Rectal and intravaginal absorption are 67 to 82%, and 20 to 56%, of the dose, respectively. Metronidazole is distributed widely and has low protein binding (< 20%). The volume of distribution at steady state in adults is 0.51 to 1.1 L/kg. Metronidazole reaches 60 to 100% of plasma concentrations in most tissues studied, including the central nervous system, but does not reach high concentrations in placental tissue. Metronidazole is extensively metabolised by the liver to 5 metabolites. The hydroxy metabolite has biological activity of 30 to 65% and a longer elimination half-life than the parent compound. The majority of metronidazole and its metabolites are excreted in urine and faeces, with less than 12% excreted unchanged in urine. The pharmacokinetics of metronidazole are unaffected by acute or chronic renal failure, haemodialysis, continuous ambulatory peritoneal dialysis, age, pregnancy or enteric disease. Renal dysfunction reduces the elimination of metronidazole metabolites; however, no toxicity has been documented and dosage alterations are unnecessary. Liver disease leads to a decreased clearance of metronidazole and dosage reduction is recommended. Recent pharmacodynamic studies of metronidazole have demonstrated activity for 12 to 24 hours after administration of metronidazole 1 g. The post-antibiotic effect of metronidazole extends beyond 3 hours after the concentration falls below the minimum inhibitory concentration (MIC). The concentration-dependent bactericidal activity, prolonged half-life and sustained activity in plasma support the clinical evaluation of higher doses of metronidazole given less frequently. Metronidazole-containing regimens for Helicobacter pylori in combination with proton pump inhibitors demonstrate higher success rates than antimicrobial regimens alone. The pharmacokinetics of metronidazole in gastric fluid appear contradictory to these results, since omeprazole reduces peak drug concentration and area under the concentration-time curve for metronidazole and its hydroxy metabolite; however, concentrations remain above the MIC. Other members of this class include tinidazole, ornidazole and secnidazole. They are also well absorbed and distributed after oral administration. Their only distinguishing features are prolonged half-lives compared with metronidazole. The choice of nitroimidazole may be influenced by the longer administration intervals possible with other members of this class; however, metronidazole remains the predominant antimicrobial for anaerobic and protozoal infections.
Adult↗
Pharmacokinetic implications for the clinical use of atropine, scopolamine and glycopyrrolate.
Several specific and sensitive new methods for determining atropine and its metabolites in biological fluids have increased the possibility to characterise the pharmacokinetic properties of this antimuscarinic agent. Following i.v. injection, atropine disappears very quickly from the circulation, resembling its fast onset of action. Age, but not sex, appears to have a clear effect on its kinetics, explaining at least partly the higher sensitivity of very young and very old patients to this anticholinergic agent. Following i.m. or oral atropine administration, typical anticholinergic effects coincide quite well with the absorption rate of the drug, indicating that the premedication should be given about 1 and 2 h before induction of anaesthesia. A sufficient absorption after rectal administration offers an alternative treatment, especially in children. Differing from its placental transfer, atropine has a delayed and incomplete lumbar cerebrospinal fluid penetration, indicating a fundamental difference between these two biological membranes. Oropharyngeally administered atropine has a very variable absorption, but inhaled or intratracheally given drug has produced interesting new results, e.g. pulmonary atropine administration appears to have clinical significance in special situations, such as cardiac arrest and organophosphate poisoning (military personnel). Depending on the method used, different data on the metabolism and excretion for atropine have been reported and therefore further studies are needed in this respect. The pharmacokinetics of scopolamine and glycopyrrolate and their relation to clinical response are poorly understood.
Aging↗
Soft drugs. 18. Oral and rectal delivery of loteprednol etabonate, a novel soft corticosteroid, in rats--for safer treatment of gastrointestinal inflammation.
PURPOSE: As a safe anti-inflammatory corticosteroid, the utility of loteprednol etabonate (LE) for the treatment of gastrointestinal inflammation, via oral and rectal administration, was investigated in rats. METHODS: In vivo, LE solution and suspension were orally administered (20 mg/kg), and various LE preparations (solution, suspension & suppository) were applied in rectal loops (0.2 mg per loop). In vitro, various GI tissues were used to study the stability and partition of LE. RESULTS: After oral administration of LE solution, LE reached the upper GI tract effectively, but not the colon, due to absorption and/or decomposition. In suspension, LE reached most of the GI tract (except rectum) in 8 hr and showed little absorption. After rectal applications, LE remained intact in the rectal loop for more than five hours with a slow rate of disappearance, however, LE distributed in the rectal membrane to some extent. The concentrations of LE and its inactive metabolites in plasma after both oral and rectal administrations were lower than the detection limit (0.1 microgram/ml) at anytime during the experiments. In vitro, LE in solution was stable in stomach, but not in cecum, due to the hydrolysis by the cecal resident micro flora. In solution, LE distributed into the mucosal membranes efficiently (about 2.5-4.0 micrograms/g tissue). CONCLUSIONS: The results suggest that LE can be orally or rectally delivered in the GI tract for the topical treatment of the inflammatory bowel disease.
Administration, Oral↗
Butyrate absorption and lactate secretion in ulcerative colitis.
PURPOSE: Fecal electrolytes and organic anion concentrations are altered in ulcerative colitis, presumably reflecting changes in colon epithelial transport. Information of mucosal absorption of butyrate in active ulcerative proctosigmoiditis is not available. METHODS: Dialysis bags containing 70 mmol/liter of butyrate in an isotonic electrolyte solution were placed in the rectum for 30 minutes. Net absorption or secretion rates of butyrate, lactate, and electrolytes were determined in the rectum of 12 patients with active ulcerative colitis (UC) and in 10 patients with quiescent UC and then compared with 10 healthy controls. RESULTS: Net flux rates demonstrated a considerable absorption of butyrate in patients with active inflammation of 7.5 +/- 0.4 mumol/cm2/h and quiescent colitis of 6.6 +/- 0.4 mumol/cm2/h, equal to absorption in healthy controls of 6.3 +/- 0.5 mumol/cm2/h, P = 0.12. Despite normal butyrate absorption, sodium absorption was compromised in active ulcerative colitis (11.5 +/- 1.4 mumol/cm2/h) compared with quiescent (15.4 +/- 1.0 mumol/cm2/h) and controls (18.7 +/- 0.8 mumol/cm2/h) (P = 0.0006). Mucosal secretion of L-lactate was minimal in both healthy controls and quiescent UC but significantly increased in patients with proctosigmoiditis (0.2 +/- 0.1 mumol/cm2/h, 0.2 +/- 0.1 mumol/cm2/h vs. 0.9 +/- 0.2 mumol/cm2/h; P = 0.0001). Appearance of D-lactate was negligible in all three groups. CONCLUSIONS: This study demonstrates that rectal butyrate absorption is normal in UC, and it follows that butyrate supplied in enemas can be expected to be absorbed. The inflamed colonic mucosa secretes L-lactate, and the increased fecal lactate concentrations can be explained by mucosal origin of lactate.
Adult↗
Suicide attempt by means of aspirin enema.
OBJECTIVE: To report a suicide attempt with an aspirin enema. CASE SUMMARY: A patient presented to the emergency room after self-administering, in enema form, approximately 700 aspirin tablets dissolved in water. Over the next 12 hours the patient became progressively acidemic with eventual cardiac arrest and subsequent chronic hypoxic encephalopathy. DISCUSSION: This patient's poor outcome was the result of retained aspirin products in the rectal vault combined with the failure to recognize the delayed absorption properties of rectally administered aspirin. CONCLUSIONS: In rectal aspirin overdoses, aspirin absorption from the rectum may occur over a long period of time. It is important to remove as much aspirin from the rectum as possible and to closely monitor these patients so that appropriate therapy may be started quickly. Activated charcoal given both in enema and oral form may help decrease aspirin absorption. Hemodialysis should be available and performed without delay should the patient require it.
Administration, Rectal↗
Review of the rectal use of opioids.
The rectal route for the administration of opioid analgesics is often forgotten by physicians seeking alternatives to the oral route. This article reviews the physiology of rectal drug absorption and such data as exists on the different opioids that have been administered by this route. Conventional fatty-based suppositories have a place in the management of chronic pain but the variability in dissolution and drug absorption limit their usefulness. Recently, sustained release vehicles have become available that offer the prospect of the attainment of steady analgesic drug concentrations with once or twice daily dosing. Early studies with the morphine hydrogel suppository suggest that it may be capable of fulfilling this prospect. Their inherent safety, as dose-dumping is impossible, will make them suitable for use in the home.
Administration, Rectal↗
Influence of feeding different amounts of first colostrum on metabolic, endocrine, and health status and on growth performance in neonatal calves.
Colostrum intake is important for health and postnatal development of neonatal calves. We studied the effects of enhanced first colostrum feeding on growth, health status, and metabolic and endocrine traits in calves during their 1st wk of life. Calves of group CL (GrCL; n = 7) were fed colostrum of milkings 1 to 6 twice daily during the first 3 d of life, followed by milk replacer (MR) up to d 7. Calves of group CH (GrCH; n = 7) were fed colostrum of the first milking during the first 3 d and then colostrum (of the first milking) twice daily, which on d 4, 5, 6, and 7 was diluted with 25, 50, 75, and 75 parts of MR, respectively. Pre- and postprandial blood samples were taken on d 1, 2, 3, and 7 for the determination of various metabolic and endocrine traits, and on d 5 intestinal absorption capacity was measured using the xylose absorption test. Rectal temperatures and fecal scores were higher (P < .05) in GrCH than in GrCL. Plasma concentrations of total protein and albumin were higher (P < .05) on d 7, IgG on d 2 and 3, and urea on d 2, 3, and 7 in GrCH than in GrCL. Plasma concentrations of triglycerides were higher (P < .05) on d 2 and of phospholipids and cholesterol were higher (P < .01) on d 7 in GrCH than in GrCL. Plasma insulin and glucagon concentrations were higher (P < .05) in GrCH than in GrCL, whereas prolactin and growth hormone concentrations were higher (P < .05) in GrCL than in GrCH. Enhanced colostrum intake had no effects on xylose absorption on d 5. Higher plasma protein, urea, and lipid concentrations in GrCH partly mirrored higher protein and fat intake but additionally pointed to higher protein synthesis and lipid turnover.
Animal Feed↗
Pharmacokinetics of the anti-inflammatory drug ximoprofen in healthy subjects and in disease states.
The pharmacokinetics of ximoprofen, a potent new non-steroidal anti-inflammatory agent, has been investigated in normal healthy subjects and in patients with hepatic or renal disease. After intravenous infusion of 22.8 mg to healthy subjects, plasma ximoprofen concentrations declined in a polyexponential manner with a terminal phase half-life of 1.9 h. The systemic clearance of ximoprofen was 115 ml.min-1 and the volumes of distribution were 18.01 Vz and 13.81 Vss. Ximoprofen was 80-90% bound to plasma proteins. The systemic availabilities (f) of orally and rectally administered doses of 30 mg of ximoprofen were 98% and 56% respectively and, in the case of the rectal dose, absorption appeared to be prolonged leading to "flip-flop" kinetics. After single oral doses of 30 mg of ximoprofen to patients with hepatic disease, half-life (2.2 h), peak plasma concentrations (1.55 micrograms.ml-1 cf 1.04 micrograms.ml-1 in healthy subjects) and areas under the curve (6.12 micrograms.h.ml-1 cf 3.54 micrograms.h.ml-1 in healthy subjects) were significantly different from those in healthy subjects. After single oral doses of 30 mg of ximoprofen to patients with renal disease, pharmacokinetic parameters of half-life (4.0 h), mean residence time (6.0 h) and area under the curve (9.2 micrograms.h.ml-1) were significantly different from those in healthy subjects. There were no significant differences in pharmacokinetic parameters between patients having differing degrees of renal disease. These data nevertheless suggest that accumulation of ximoprofen in hepatic or renal disease would be of slight or negligible clinical relevance and that no alteration of the dose regimen (up to 15 mg twice daily) may be required when ximoprofen is administered in these disease states.
Adult↗
Are prostaglandins cytoprotective in the human large intestine? The effect of indomethacin on rectal mucosal function and prostaglandin E2 release in vivo.
To test the hypothesis that prostaglandins are cytoprotective in the human large intestine, we investigated the effect of withdrawal of treatment with indomethacin suppositories on bowel habit and on rectal mucosal electrolyte transport and prostaglandin production in 8 patients taking such treatment for rheumatological disorders. Discontinuation of indomethacin doubled rectal mucosal prostaglandin E2 release (p less than 0.05) measured by in vivo rectal dialysis. Although there was no significant overall change in stool frequency, stool consistency, rectal bleeding or sodium absorption (also assessed by rectal dialysis), sigmoidoscopic appearance (p = 0.05), rectal mucosal potential difference (p less than 0.05) and potassium transport (p = 0.01) each reverted towards normal on indomethacin withdrawal. These results accord with the theory that, as in the upper gastrointestinal tract, prostaglandins may play a role in the maintenance of rectal mucosal structure and function.
Adult↗
Salicylate absorption patterns: a comparison between rectal and oral administration.
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Administration, Oral↗
Pain relief after tonsillectomy in adults: intramuscular diclofenac and papaveretum compared.
A wide variety of surgical and pharmacological methods have been described in an attempt to reduce pain after tonsillectomy, with conflicting results. Opiates are still widely used, despite unwanted side-effects. Recently the non-steroidal anti-inflammatory drugs have been shown to be effective against a variety of post-operative pains. Diclofenac is effective in both children and adults in the relief of pain after tonsillectomy when administered rectally, but absorption is variable, and suppositories are not widely accepted in the UK. The present double-blind study compared a single intramuscular dose of diclofenac with papaveretum in adults undergoing tonsillectomy. Post-operatively, the patients who received diclofenac had less pain and started drinking significantly sooner than the control group. There were no undesirable side-effects. Intramuscular diclofenac is superior to papaveretum in the relief of pain in adults undergoing tonsillectomy.
Adolescent↗
Clinical pharmacology and therapeutic potential of artemisinin and its derivatives in the treatment of malaria.
Artemisinin and its derivatives are renowned for their potent antimalarial activity. They have found their way into clinical use in many areas where malaria is endemic. The in vitro concentration at which artemisinin can inhibit 50% of the growth of Plasmodium falciparum ranges from 3 to 30 micrograms/L. The fat-soluble derivatives artemether and arteether are approximately twice as active. The water-soluble dihydro-artemisinin and artesunate are 4 to 5 times more active in vitro. Artemisinin is available only for oral and rectal administration. Absorption is incomplete and elimination is fast, with and elimination half-life of 2 to 5 hours. Plasma concentrations after a single 500 mg oral dose most often exceed 200 micrograms/L. Artesunate and artemether can be considered as prodrugs. Biotransformation into the active metabolite dihydro-artemisinin occurs rapidly--almost immediately for artesunate. The reported elimination half-life of artesunate is less than 1 hour, and for artemether the figure is 3 to 11 hours. The pharmacokinetics of dihydro-artemisinin are not yet completely clear. Elimination is probably also rapid, with an elimination half-life of a few hours. Arteether, dissolved in oil for intramuscular administration, has a much longer elimination half-life of over 20 hours. The clinical efficacy of this group of drugs is characterised by an almost immediate onset and rapid reduction of parasitaemia, with complete clearance in most cases within 48 hours. Efficacy is high even in areas with multidrug-resistant parasite strains. To prevent recrudescence with monotherapy of these compounds, treatment needs to be extended beyond the disappearance of parasites. After 5 days of therapy the rate of recrudescence is approximately 10%. Alternatively, combination with other drugs can be used. Combination with mefloquine is recommended for areas with multidrug-resistant P. falciparum.
Antimalarials↗
[Absorption of vitamin B6 after rectal administration during pregnancy].
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Administration, Rectal↗
[Absorption of vitamin A by rectal administration].
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Administration, Rectal↗