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PubMed1988

[Per rectal administration of antibiotics. Clinical use of ampicillin in respiratory tract infection in children].

As one of our clinical studies on per rectal administration of antibiotics, children who suffered respiratory tract infection (RTI) were administered with ampicillin (ABPC) through this route. Our conclusions drawn from this study are as follows: 1. One hundred and eighty strains of aerobic bacteria which were isolated by us in 1984-1985 were tested for the sensitivity to ABPC using plate-disk method. MIC's of ABPC for all the strains of Streptococcus pyogenes were lower than 0.024 micrograms/ml. MIC's for all the strains of Streptococcus haemolyticus were 0.05-0.20 microgram/ml. MIC's for 88% of the strains tested of Haemophilus influenzae were 0.10-0.78 microgram/ml. 2. Bacterial flora in the respiratory tract of 97 cases of children, who suffered RTI, were cultured. Almost half of them were Gram-positive cocci, the rest belonged to Gram-negative groups. This indicates that broad-spectrum antibiotics should be chosen first even before the diagnosis of causative organisms is established. 3. Soon after a per rectal administration of ABPC to children, high blood concentrations of the drug were observed by paper-disk method. 4. Eleven cases, which included 2 cases of pneumonia, of 15 children who suffered RTI and were given this antibiotic were greatly improved within 3-10 days. No serious side effects were observed. 5. Our brief study reported here indicates that ABPC administration by rectal route is safe and useful for the clinical treatment of RTI of children.

Age Factors↗

PubMed1986

Pharmaceutical evaluation of hollow type suppositories. IV. Improvement of bioavailability of propranolol in rabbits after rectal administration.

Three kinds of suppositories were constructed with oleaginous base material (Witepsol H-15): a conventional type suppository containing propranolol (PPL) hydrochloride mixed with a base material (I), a hollow type suppository containing PPL in a form of aqueous solution (PPL was dissolved in isotonic NaCl solution) in its cavity (II), a hollow type suppository containing PPL as powder (hydrochloride salt) in its cavity (III). Bioavailability was estimated after rectal administration of each suppository in rabbits and compared with oral administration. The peak plasma PPL concentration (Cmax) and the area under the plasma concentration-time curve (AUC) were lower with I than with II or III. The Cmax and the AUC measured after rectal administration of III were significantly higher than those in the case of oral administration. By using III, the highest values of the mean Cmax (795 +/- 160 ng/ml) and of the mean AUC (459 +/- 21 h X ng/ml) were obtained. It was found that systemic availability was increased by rectal administration of PPL hollow type suppositories. These data on bioavailability suggested that PPL was absorbed more efficiently with the hollow type suppository than with the conventional one. PPL was released faster from II and III than from I. It was concluded that the hollow type suppository was a suitable device for absorption of PPL into the rectum.

Administration, Rectal↗

PubMed1996

Pharmacokinetics of propylene glycol after rectal administration.

Propylene glycol is an excipient of various pharmaceutical preparations. The pharmacokinetics after rectal administration are studied, followed by a consideration on local and systemic side-effects for a solution of paracetamol in a mixture of propylene glycol and water. After administration of 8.64 g propylene glycol to 10 adults and 173 mg/kg body weight to 4 children, peak concentrations (Cmax) of 199 mg/l and 171 mg/l respectively were reached (tmax) after 1.5 hr and 1.0 hr. The average terminal half-lives (t1/2) in adults and children were respectively 2.8 hr and 2.6 hr, total body clearance (CI/F) 0.20 l/hr*kg and 0.21 l/h*kg and apparent volume of distribution (VD/F) 0.79 l/kg and 0.77 l/kg.

Administration, Rectal↗

PubMed2004

Severe hyperphosphatemia and hypocalcemia following the rectal administration of a phosphate-containing Fleet pediatric enema.

BACKGROUND: Toxicity secondary to rectally administered hypertonic phosphate solution in patients with normal renal function is rarely reported in the literature. We report a case of electrolyte disturbance and seizure secondary to the rectal administration of 2 Fleet pediatric enemas. CASE REPORT: A 4-year-old white female with spinal muscular atrophy and chronic constipation was brought to the emergency department with complaints of lethargy and difficulty breathing following the administration of 2 Fleet pediatric enemas. In the emergency department, physical examination was significant for a depressed level of consciousness and shallow respirations. A basic metabolic profile was significant for a calcium of 3.3 mg/dL, phosphate of 23 mg/dL, and sodium of 153 mEq/L. Arterial blood gases revealed a pH of 7.24, Pco2 of 38 mm Hg, Po2 of 220 mm Hg. Electrocardiogram revealed a prolonged QT interval of 340 milliseconds with a corrected QT interval of 498 milliseconds. Sixteen hours postexposure, she experienced a generalized seizure unresponsive to multiple doses of lorazepam and responsive only to 100 mg of intravenous calcium chloride. Two days after presentation, the patient experienced complete resolution of symptoms. CONCLUSION: Osmotically acting hypertonic phosphate enemas can result in severe toxicity if retained. This is true even in patients without predisposing risk factors.

Acidosis↗

PubMed1997

Plasma concentrations after rectal administration of acetaminophen in preterm neonates.

Acetaminophen is frequently administered to infants and children for its antipyretic and analgesic properties. Oral administration is the route of choice in daily practice. In some circumstances this is impractical. Rectal administration of acetaminophen is an alternative route. This study measures plasma concentrations following rectal administration of acetaminophen 20 mg.kg-1 (10% Infants' Tylenol Drops, McNeil Consumer Product Co., diluted with an equal volume of sterile water) in five preterm neonates. Serial arterial blood samples were obtained at 0, 15, 30, 60, 120, and 240 min. Pharmacokinetic parameters were (mean +/- SD): Cmax (maximum plasma concentration) of 8.38 +/- 3.92 micrograms.ml-1 and Tmax (time to reach maximum plasma concentration) of 78.0 +/- 40.2 min. Our results show that 20 mg.kg-1 of acetaminophen rectally results in low plasma levels in preterm neonates.

Acetaminophen↗

PubMed1995

Immunosuppressive effect induced by intraperitoneal and rectal administration of boar seminal immunosuppressive factor.

The immunosuppressive component was isolated from boar seminal vesicle secretion and administered i.p. or rectally to male mice. By means of the immunofluorescent method, the seminal immunosuppressive component was found on the membranes of 50-70% of white blood cells of treated mice the first day after i.p. and the third day after rectal administration. The immunosuppressive component was observed on the membranes of 10-20% of white cells even at the 17th day after treatment. Intraperitoneal or rectal administration of the immunosuppressive component led to a decrease in the white cell concentration in blood of treated mice. These findings indicate that rectal deposition of semen may compromise some aspects of the immune system and may be an important cofactor in the development of viral or bacterial infections among homosexual men.

Absorption↗

PubMed2001

Pediatric imaging: sedation with an injection formulation modified for rectal administration.

PURPOSE: To determine if rectal sedation with thiopental sodium produced for intravenous administration provides safe and effective sedation for children undergoing diagnostic imaging. MATERIALS AND METHODS: Five hundred twenty-five consecutive children (mean age, 2.7 years +/- 2.2 [SD]) underwent magnetic resonance imaging (n = 425), computed tomography (n = 89), and nuclear medicine (n = 11) examinations after rectal administration of thiopental sodium injection solution. The solution was prepared from thiopental sodium powder mixed with sterile water to create a concentration of 100 mg/mL. The dose ranged from 25 to 40 mg per kilogram of body weight, with a total dose limit of 1.5 g. The percentages of successful sedations and adverse reactions were evaluated on the basis of data collected at the time of the sedation. RESULTS: Sedation was successful in 504 (96%) children. Ten (2%) children experienced desaturation, but only three of the 10 experienced sedation failure. All cases of desaturation were treated successfully with head repositioning, administration of supplemental oxygen, or both. No children experienced vomiting, acute rectal irritation, paradoxical hyperactivity, or prolonged sedation. CONCLUSION: Thiopental sodium sedation for pediatric imaging, with use of a rectal solution prepared from thiopental sodium preparation for intravenous injection, is safe and effective.

Administration, Rectal↗

PubMed1981

On the pharmacokinetics of domperidone in animals and man. IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration.

The pharmacokinetics and bioavailability of domperidone, a novel gastrokinetic, were studied in healthy male subjects by comparing plasma concentrations and urinary excretion following intravenous, intramuscular, oral and rectal administration. Two oral dosage forms were studied: 10-mg tablets and a 10-mg/ml oral solution. The influence of a meal on the oral bioavailability and the dose-proportionality were also investigated. Plasma levels of intravenous domperidone could be described by a three-compartment model with a rapid distribution of 40% of the dose to a "shallow" peripheral compartment. The final elimination half-life was 7.5 hours. Peak plasma levels were reached within 30 minutes following intramuscular and oral administration and at 1-4 hours following rectal administration. Since domperidone showed an extensive first-pass elimination, AUC-values -a measure for the bioavailability- were considerably lower after oral than after parenteral administration. Equal oral and rectal doses gave a similar bioavailability. AUC-values increased proportionally with the dose over a 10-60 mg range. Cumulative urinary excretion of unchanged domperidone was proportional to corresponding AUC-values. The bioavailability was discussed in the light of the therapeutic results.

Administration, Oral↗

PubMed2005

Therapeutic effects of rectal administration of basic fibroblast growth factor on experimental murine colitis.

BACKGROUND & AIMS: Basic fibroblast growth factor (bFGF) is a promising therapeutic agent for various diseases. It remains unclear, however, whether bFGF is effective for the treatment of inflammatory bowel disease. The aim of this study was to examine the efficacy of bFGF on 2 experimental murine colitis models and to investigate its molecular mechanisms. METHODS: We evaluated the effects of human recombinant bFGF (hrbFGF) on mice with dextran sulfate sodium (DSS)-induced colitis and mice with trinitrobenzene sulfonic acid (TNBS)-induced colitis as well as normal mice. Body weight, survival rate, and histologic findings of the colonic tissues were examined. Gene expression of tumor necrosis factor (TNF)-alpha, cyclooxygenase (COX)-2, transforming growth factor (TGF)-beta, mucin 2 (MUC2), intestinal trefoil factor (ITF), and vascular endothelial growth factor (VEGF) in the colonic tissues was determined. The proliferation activity of hrbFGF on the colonic epithelium was evaluated by immunohistochemistry. RESULTS: Rectal administration of hrbFGF ameliorated DSS-induced colitis in a dose-dependent manner. Gene expression of TNF-alpha was significantly reduced in the colonic tissues of mice with DSS-induced colitis treated with hrbFGF, whereas MUC2 and ITF messenger RNA expression was up-regulated. Rectal administration of hrbFGF significantly improved the survival rate of mice with TNBS-induced colitis and partially ameliorated colitis. hrbFGF significantly increased the number of Ki-67-positive cells in the colonic epithelium of normal mice, and up-regulated the gene expression of COX-2, TGF-beta, MUC2, ITF, and VEGF in the colonic tissues. CONCLUSIONS: Rectal administration of bFGF might be a promising option for the treatment of inflammatory bowel disease.

Administration, Rectal↗

PubMedDate not supplied

Rectal administration of nifedipine: haemodynamic effects and pharmacokinetics in hypertensives.

The haemodynamic effects and pharmacokinetics of nifedipine suppositories, used mainly for hypertensive emergencies, were studied in 10 severely hypertensive patients. Following rectal administration, significant hypotensive effects occurred after 0.5 h and lasted until 7 h after administration. The mean (+/- SE) maximum decreases in systolic and diastolic blood pressures 1.5 h after administration were: systolic, 61.8 +/- 7.9 mmHg (P less than 0.001); and diastolic, 30.8 +/- 4.0 mmHg (P less than 0.001). No serious side-effects were reported and heart rate did not change significantly. Mean nifedipine concentration in the blood peaked at 52.4 ng/ml, 1 h after administration and, after 7 h, was still 14.3 ng/ml which is higher than the minimum plasma concentration required for hypotensive effects to occur. There was a close correlation between nifedipine concentration in the blood and hypotensive effects. These results indicate that rectal administration of nifedipine should be regarded as a useful alternative treatment in hypertensive emergencies.

Administration, Rectal↗

PubMed1992

Rectal administration of perforated nifedipine capsules in acute severe hypertension in children.

Nine hypertensive children (mean age: 5.0 years (SD: 4.5), range: 10 months to 15 years) were administered nifedipine (capsule) rectally (0.2 to 0.5 mg/kg) when their blood pressures were over 170 mmHg systolic and/or over 110 mmhg diastolic, independent of their ages. The causes of hypertension were acute glomerulonephritis (n = 2), chronic glomerulonephritis (n = 2), renovascular hypertension (n = 4), and polycystic kidney (n = 1). Both systolic and diastolic blood pressures fell in all children after rectal administration of nifedipine, although the response of blood pressure was weak in one child with renovascular hypertension. Blood pressures were lowest at 30 to 60 minutes, and remained under 140 mmHg systolic and 80 mmHg diastolic at least for three hours. Side-effects were headache in one child, palpitations in two children, and facial flushing in three. All of these symptoms were mild, and no special treatment was required. These findings suggest that rectal administration of nifedipine may be effective and the most reliable way to treat young children with severe or urgent hypertension.

Acute Disease↗

PubMed1999

The rectal administration of lidocaine gel and tolerance of transrectal ultrasonography-guided biopsy of the prostate: a prospective randomized placebo-controlled study.

OBJECTIVE: To evaluate the effect of the rectal administration of lidocaine gel on the tolerance of systematic sextant transrectal ultrasonography (TRUS)-guided prostatic biopsies. PATIENTS AND METHODS: From January to September 1997, patients undergoing initial biopsy mapping of the prostate (with six systematic TRUS-guided transrectal biopsies) were randomized using a pre-established randomization list into two groups. In group 1, 15 mL of 2% lidocaine gel (Astra, Södertälje, Sweden) was administered intrarectally 15 min before the biopsies. In group 2 (placebo), 15 mL of trans-sonic hydrophilic gel (Rivadis Laboratory, Thouars, France) was administered transrectally under the same conditions. Patients were randomized and the gel administered by a nurse; neither the patients nor the urologists were aware of which product was administered. At the end of the procedure, patients were asked to score the severity of discomfort of the biopsies, using a self-administered rating scale. RESULTS: In all, 109 patients were included, in either group 1 (56 patients) or group 2 (53 patients). Slight pain or no pain was experienced by the vast majority of patients in both groups. Moderate to severe pain was experienced in 12.5% of patients in group 1 and 11.3% of patients in group 2. There was no difference in patient tolerance between the groups (P=0.39). Only minor complications occurred and complication rates were not significantly different between the groups. CONCLUSION: The rectal administration of lidocaine has no impact on the tolerance to prostatic biopsy.

Administration, Rectal↗

PubMed2001

Bioavailability of diazepam from aqueous-organic solution, submicron emulsion and solid lipid nanoparticles after rectal administration in rabbits.

The bioavailability of diazepam in rabbits after rectal administration of three formulations: organic-aqueous Relsed rectal solution (containing ethanol, benzyl alcohol and propylene glycol), submicron emulsion and solid lipid nanoparticles (SLN), was studied. Submicron emulsion contained MCT oil (20% w/w), egg lecithin and poloxamer; SLN were prepared with cetyl palmitate 10% w/v and non-ionic emulsifying agent, Plantacare. All formulations contained 4 mg/ml of diazepam and the dose administrated to rabbits was 2 mg/kg. In both submicron preparations nearly the same mean size of the dispersed particles (201-206 nm) and the fraction of the free drug in aqueous phase (0.9-1.5%) was determined. Besides very moderate prolongation of drug release, the submicron emulsion as a vehicle did not alter pharmacokinetics of diazepam when compared with the solution: the mean C(max) was 48.9+/-24.0 and 49.5+/-17.0 ng/ml, and area under the curve was 134.0+/-42.3 and 186.8+/-59.8 ng h/ml, for solution and emulsion, respectively. The low relative bioavailability, 47% compared to the solution, was observed after administration of SLN. Transmission electron microscopy pictures revealed that some of diazepam is present on the surface of the SLN and this fraction was immediately absorbed, while the diffusion of the drug in the solid core was not efficient enough to allow a complete release. It may be concluded that submicron emulsion may be a good choice of an ethanol-free drug formulation, but lipid matrix, which is solid at body temperature, is not advantageous system for diazepam rectal delivery, even if delivered as a submicron dispersion.

Administration, Rectal↗

PubMed2002

Long-term rectal administration of high-dose sustained-release morphine tablets.

Two proprietary sustained-release morphine tablets for oral administration are available in the USA, and the authors have found that rectal administration of these provide excellent analgesia although their use by this route is not approved by the United States Food and Drug Administration. An illustrative case in a 72-year-old patient with prostate cancer is reported.

Administration, Rectal↗

PubMed1992

Case report: renal excretion of gastrografin following rectal administration.

Renal excretion of water soluble iodinated contrast media following oral administration has often been described but no reports describing renal excretion following rectal administration of such contrast have previously been described. We describe a case of renal excretion of diatrizoate methylglucamine (Gastrografin, Schering) following a diagnostic 'gastrografin enema' in a woman with caecal carcinoma.

Administration, Rectal↗

PubMed1988

Comparative plasma concentration profiles after i.v., i.m. and rectal administration of pethidine in children.

Plasma concentration-time curves of pethidine and norpethidine were studied in 25 children allocated after operation to three groups to receive pethidine 1 mg kg-1 i.v., i.m. or rectally. Peak concentrations occurred after 5 +/- 1, 10 +/- 2, and 60 +/- 10 min, respectively, while the maximum concentrations amounted to 2800 +/- 462, 1609 +/- 367 and 531 +/- 179 nmol litre-1, respectively. The area under the curve (0-240 min) was similarly reduced in the group with rectal administration (P less than 0.05). Compared with the i.v. data, approximately 40% systemic availability occurred after rectal application, although considerable individual variation was noted. In one child very high plasma concentrations were observed after rectal administration, possibly as a result of redistribution/recirculation phenomena. The average results are similar to those obtained when other opioids are given rectally.

Administration, Rectal↗

PubMed1999

Bioavailability of racemic ketoprofen in healthy horses following rectal administration.

Ketoprofen (KTP) is a chiral non-steroidal anti-inflammatory drug (NSAID) of the propionic acid class, approved by the FDA for the allevation of pain associated with musculoskeletal disorders in horses. The present study was designed to examine the bioavailability of ketoprofen enantiomers after rectal administration of the racemate to healthy horses. One gram of racemic ketoprofen was injected intravenously and administered rectally as a fat based suppository in a cross-over design study (n = 4). Blood samples were analysed for KTP enantiomers using HPLC. After IV administration, the S(+) enantiomer concentrations in plasma were higher than the R(-) enantiomer concentrations and the AUC(0-12 h) for the S(+) enantiomer was significantly higher than for the R(-) enantiomer. Following rectal administration C(max) and AUC(0-12 h) were significantly higher for the S(+) than for the R(-) enantiomer. Bioavailability after rectal administration was low. Since there was no significant difference in bioavailability between the two enantiomers, it is assumed that no pre-systemic inversion from R(-) to S(+) occurred after rectal administration of racemic KTP to horses.

Administration, Rectal↗

PubMedDate not supplied

Rectal administration of propylthiouracil in suppository form in patients with thyrotoxicosis and critical illness: case report and review of literature.

OBJECTIVE: To report the successful management of thyrotoxicosis in a seriously ill 47-year-old man with a perforated gastric ulcer in whom oral intake was contraindicated. METHODS: Our patient was treated with 400 mg of propylthiouracil (PTU) every 6 hours in the form of specially prepared suppositories for rectal administration, together with intravenously infused esmolol. RESULTS: We were able to demonstrate substantial absorption of PTU administered by means of rectal suppositories. Serum levels of PTU were maintained within the high therapeutic range for 5 days until the patient was able to tolerate orally administered therapy. The patient improved clinically during this treatment. CONCLUSION: This case strongly supports the rectal administration of PTU in suppository form as an appropriate alternative route in any patient with thyrotoxicosis, including the critically ill patient, when oral administration is not possible.

Administration, Rectal↗