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Rectal Administration (rectal + administration)
Selected AbstractsRectal Absorption of Lamotrigine Compressed TabletsEPILEPSIA, Issue 7 2000Angela K. Birnbaum Summary: Purpose: Interruption of oral drug administration poses a significant clinical problem for antiepileptic drugs that have no parenteral formulation. If a drug is absorbed rectally, rectal administration can be a useful alternative when the oral route of administration is not possible. The purpose of this study was to compare the single-dose pharmacokinetics of la-motrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers. Methods: A single LTG compressed tablet (100 mg) was administered orally and rectally to 12 volunteers in this single-dose, two-period, crossover study with a 2-week washout between doses. For rectal administration, tablets were crushed and suspended in 10 mL of water. Plasma samples were collected from 0 to 120 hr after each dose and analyzed for LTG by an HPLC method developed for this investigation. Results: LTG plasma concentrations were lower after rectal administration versus oral administration. The average area under the curve was 28.90 ± 9.5 ,g/mL/hr after rectal administration and 51.71 ± 19.2 ,g/mL/hr after oral administration. The average maximum LTG concentration was 0.53 ± 0.14 ,g/mL after rectal administration and 1.45 ± 0.35 ,g/mL after oral administration. The relative bioavailability for LTG compressed tablets was 0.63 ± 0.33 for rectal administration. There were no drug-related rashes or serious side effects. Conclusions: LTG suspension prepared from LTG compressed tablets is absorbed rectally, although not to the same extent or rate as when given orally. [source] Febrile Seizures: Treatment and PrognosisEPILEPSIA, Issue 1 2000Finn Ursin Knudsen Summary: Recent epidemiologic data indicate that the vast majority of children with febrile seizures have a normal long-term outcome. A precise knowledge of the short- and long-term outcome with or without treatment, and short- and long-term side effects is an important prerequisite for assessing the various treatment strategies. We focus on the impact of short-term or prophylactic treatment on the short- and long-term outcome of various types of febrile seizures. There is universal agreement that daily prophylaxis with antiepileptic agents should never be used routinely in simple febrile seizures, but only in highly selected cases, if at all. Intermittent diazepam (DZP) prophylaxis at times of fever may or may not reduce the recurrence rate, but it does not appear to improve the long-term outcome as compared with short-term seizure control. The treatment may be used to reduce the recurrence rate for a small arbitrarily defined group with multiple simple febrile seizures, complex febrile seizures, especially focal, prolonged or both, febrile status, and when parental anxiety is severe. However, there is no evidence that treatment of simple febrile seizures can prevent the rare cases of later epilepsy, and many children with complex febrile seizures have a benign long-term outcome, even without treatment. Many prefer a "wait and see" policy. An attractive alternative is to treat new febrile seizures with rectal DZP in solution at seizure onset, given by the parents at home to prevent febrile status. Newer, less well documented short-term strategies include nasal, oral, or rectal administration of other benzodiazepines. Short-term seizure control of febrile status and careful parental counseling are the two most important targets of treatment. [source] Rebamipide enema therapy as a treatment for patients with active distal ulcerative colitisJOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY, Issue 2 2007Ryuichi Furuta Background:, The clinical efficacy of corticosteroids in the treatment of ulcerative colitis (UC) is well-established. However, prolonged usage of these drugs can result in serious complications. Rebamipide {2-(4-chlorobenzoylamino)-3[2-(1H)-quinolinon-4-yl] propionic acid}, a cytoprotective agent, has been reported to have anti-inflammatory activity and to repair mucosal injury in animal colitis models. The aim of the present study was to assess the clinical efficacy and safety of a novel Rebamipide enema therapy in UC patients. Methods:, Twenty patients with the active distal type of UC in whom corticosteroid treatment had been unsuccessful were treated with rectal administration of Rebamipide twice a day for 3 weeks, during which corticosteroid dosage was kept constant. The efficacy of treatment was assessed from clinical symptoms and endoscopic findings. The anti-inflammatory effect of Rebamipide was also examined by monitoring changes in the intensity of histological inflammation and levels of cytokine activity in the rectal mucosa. Results:, At 3 weeks after the initiation of Rebamipide enema therapy, 11 patients (55%) achieved clinical remission. Sixteen (80%) were colonoscopically judged to be responders, with decreased levels of interleukin (IL)-1, but not of IL-8, and an increased ratio of IL-1 receptor antagonist/IL-1, in organ cultures of mucosal tissues. The change in the number of infiltrating neutrophils was not significantly correlated with the clinical response to this therapy. No side-effects were noted in any patients. Conclusion:, Rebamipide enema therapy proved to be safe and useful in corticosteroid-refractory patients with the active distal type of UC. [source] MR colonography for the assessment of colonic anastomosesJOURNAL OF MAGNETIC RESONANCE IMAGING, Issue 1 2006Waleed Ajaj MD Abstract Purpose To assess colonic anastomoses in patients after surgical treatment by means of MR colonography (MRC) in comparison with conventional colonoscopy (CC). Materials and Methods A total of 39 patients who had previously undergone colonic resection and end-to-end-anastomosis were included in the study. MRI was based on a dark-lumen approach. Contrast-enhanced T1-weighted (T1w) three-dimensional (3D) images were collected following the rectal administration of water for colonic distension. The MRC data were evaluated by two radiologists. The criteria employed to evaluate the anastomoses included bowel wall thickening and increased contrast uptake in this region. Furthermore, all other colonic segments were assessed for the presence of pathologies. Results In 23 and 20 patients the anastomosis was rated to be normal by MRC and CC, respectively. In three patients CC revealed a slight inflammation of the anastomosis that was missed by MRI. A moderate stenosis of the anastomosis without inflammation was detected by MRC in five patients, which was confirmed by CC. In the remaining 11 patients a relevant pathology of the anastomosis was diagnosed by both MRC and CC. Recurrent tumor was diagnosed in two patients with a history of colorectal carcinoma. In the other nine patients inflammation of the anastomosis was seen in seven with Crohn's disease (CD) and two with ulcerative colitis. MRC did not yield any false-positive findings, resulting in an overall sensitivity/specificity for the assessment of the anastomosis of 84%/100%. Conclusion MRC represents a promising alternative to CC for the assessment of colonic anastomoses in patients with previous colonic resection. J. Magn. Reson. Imaging 2006. © 2006 Wiley-Liss, Inc. [source] Small bowel hydro-MR imaging for optimized ileocecal distension in Crohn's disease: Should an additional rectal enema filling be performed?JOURNAL OF MAGNETIC RESONANCE IMAGING, Issue 1 2005Waleed Ajaj MD Abstract Purpose To assess the impact of an additional rectal enema filling in small bowel hydro-MRI in patients with Crohn's disease. Materials and Methods A total of 40 patients with known Crohn's disease were analyzed retrospectively: 20 patients only ingested an oral contrast agent (group A), the other 20 subjects obtained an additional rectal water enema (group B). For small bowel distension, a solution containing 0.2% locust bean gum (LBG) and 2.5% mannitol was used. In all patients, a breathhold contrast-enhanced T1w three-dimensional volumetric interpolated breathhold examination (VIBE) sequence was acquired. Comparative analysis was based on image quality and bowel distension as well as signal-to-noise ratio (SNR) measurements. MR findings were compared with those of conventional colonoscopy, as available (N = 25). Results The terminal ileum and rectum showed a significantly higher distension following the rectal administration of water. Furthermore, fewer artifacts were seen within group B. This resulted in a higher reader confidence for the diagnosis of bowel disease, not only in the colon, but also in the ileocecal region. Diagnostic accuracy in diagnosing inflammation of the terminal ileum was 100% in group B; in the nonenema group there were three false-negative diagnoses of terminal ileitis. Conclusion Our data show that the additional administration of a rectal enema is useful in small bowel MRI for the visualization of the terminal ileum. The additional time needed for the enema administration was minimal, and small and large bowel pathologies could be diagnosed with high accuracy. Thus, we suggest that a rectal enema in small bowel MR imaging be considered. J. Magn. Reson. Imaging 2005;22:92,100. © 2005 Wiley-Liss, Inc. [source] Population pharmacokinetics of pyrazinamide in elephantsJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 5 2005M. ZHU This study was undertaken to characterize the population pharmacokinetics (PK), therapeutic dose, and preferred route of administration for pyrazinamide (PZA) in elephants. Twenty-three African (Loxodonta africana) and Asian (Elephas maximus) elephants infected with or in contact with others culture positive for Mycobacterium tuberculosis were dosed under treatment conditions. PZA was dosed daily at 20,30 mg/kg via oral (fasting or nonfasting state) or rectal (enema or suppository) administration. Blood samples were collected 0,24 h postdose. Population PK was estimated using nonlinear mixed effect modeling. Drug absorption was rapid with Tmax at or before 2 h regardless of the method of drug administration. Cmax at a mean dose of 25.6 (±4.6) mg/kg was 19.6 (±9.5 ,g/mL) for PZA given orally under fasting conditions. Under nonfasting conditions at a mean dose of 26.1 ± 4.2 mg/kg, Cmax was 25% (4.87 ± 4.89 ,g/mL) and area under concentration curve (AUC) was 30% of the values observed under fasting conditions. Mean rectal dose of 32.6 ± 15.2 mg/kg yielded Cmax of 12.3 ± 6.3 ,g/mL, but comparable AUC to PZA administered orally while fasting. Both oral and rectal administration of PZA appeared to be acceptable and oral dosing is preferred because of the higher Cmax and lower inter-subject variability. A starting dose of 30 mg/kg is recommended with drug monitoring between 1 and 2 h postdose. Higher doses may be required if the achieved Cmax values are below the recommended 20,50 ,g/mL range. [source] Population pharmacokinetics of isoniazid in the treatment of Mycobacterium tuberculosis among Asian and African elephants (Elephas maximus and Loxodonta africana)JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 1 2005J. N. MASLOW We recently described the clinical presentation and treatment of 18 elephants from six herds infected with TB. Treatment protocols and methods varied between herds to include both oral and rectal dosing using multiple drug doses and formulations. In this paper we present information regarding the pharmacokinetics (PK) of isoniazid (INH) in elephants and provide suggestions regarding initial treatment regimens. Forty-one elephants received INH daily by either oral or rectal administration with different formulations. Population PK analysis was performed using Non-linear Mixed Effect Modeling (NONMEM). Results of oral administration indicated that compared with premixed INH solution, the drug exposure was highest with a suspension prepared freshly with INH powder. When INH was concomitantly given as an admixture over food, Tmax was delayed and variability in drug absorption was significantly increased. Compared with oral administration, similar drug exposures were found when INH was dosed rectally. The data generated suggest that a starting dose of 7.5 mg/kg of INH is appropriate for initial TB treatment in elephants when premixed solution is administered directly into the oropharynx or rectal vault and 4 mg/kg are when INH is administered following immediate suspension from powdered form. [source] A Comparison of Salicylic Acid Levels in Normal Subjects after Rectal versus Oral DosingACADEMIC EMERGENCY MEDICINE, Issue 2 2009Roger Maalouf MD Abstract Objectives:, The common practice is to use 162 mg of aspirin orally in the emergency department (ED) for patients presenting with myocardial infarction. If the patient cannot take aspirin orally in the authors' facility, then 600 mg of aspirin is given rectally. However, no strong evidence exists as to whether the oral and rectal doses provide equivalent risk protection. The authors hypothesized that the salicylic acid levels for orally and rectally administered aspirin will not be similar, because of the different dosages used and the different routes of administration. Methods:, The study sample consisted of healthy, nonpregnant, adult volunteers without active illness, who did not take any medication regularly. Each subject served as his or her own control to account for any confounding factors. The study was conducted on 2 days, separated by a 1-week washout period. On the first day, 162 mg of oral aspirin was chewed and swallowed. Salicylic acid levels were obtained at baseline (i.e., before taking the aspirin) and then 30, 60, and 90 minutes after dosing. The 600-mg aspirin suppository was self-administered 1 week later with a sample for laboratory measures again drawn at baseline and then 30, 60, and 90 minutes after dosing. Results:, Twenty-four subjects completed the study. The rectal suppository provided significantly more salicylic acid into the blood than the oral tablets over 90 minutes (p < 0.001). No statistical difference was noted between oral and rectal administration from baseline to 30 minutes (p > 0.05). However, mean salicylic acid levels from the rectal suppository were statistically higher than from the oral tablets from 30 to 60 minutes (p < 0.001) and from 60 to 90 minutes (p = 0.002). More than 60% of the subjects had an increasing salicylic acid level response over time to the rectal suppository. The salicylic acid level response to the oral administration was more evenly divided between those subjects whose salicylic acid levels peaked quickly and then fell or held steady (33%), those whose salicylic acid levels increased over time (29%), and those whose salicylic acid levels were measureable only after 60 minutes (25%). Although not statistically significant, these differences in group distributions for the type of salicylic acid level response between oral and rectal doses suggested the possibility of a rectal advantage. Conclusions:, Whether the higher salicylic acid levels and faster absorption of the rectal aspirin translate into better clinical outcomes is unknown and cannot be concluded from our study. Previous evidence, however, has shown that 162 mg of aspirin chewed and swallowed provided lower mortality in patients presenting with myocardial infarction. Our results suggested the rectal administration of a 600-mg suppository provides sufficient levels of salicylic acid within 90 minutes to meet or exceed that of oral aspirin. [source] Oral versus rectal midazolam as a pre-anaesthetic sedative in children receiving dental treatment under general anaesthesiaACTA PAEDIATRICA, Issue 8 2002B Jensen Dental treatment in children who are too young or too apprehensive to cooperate is often performed under sedation. In Sweden, the tradition has been to administer sedatives rectally in small children, but oral liquid sedation is now increasingly used. Aim: To compare the sedative effects of oral and rectal administration of midazolam in children undergoing dental treatment under general anaesthesia and to assess acceptance of sedative administration, acceptance of application of the facemask, and amnesia. Methods: Fifty children aged 2,7 y were randomly allocated to receive either liquid oral or rectal sedation, with 25 children in each group. Results: The sedative effect of rectal administration was higher, but not statistically significantly, than that of oral administration (p= 0.07). No significant differences in acceptance of sedative administration, acceptance of mask application or amnesia were found between the groups. Conclusion: Both the oral and the rectal routes can in most cases be appropriate. However, the better sedative effect of rectal administration of midazolam makes it a more favourable route in pre-cooperative and non-compliant children. [source] | ||||||||||