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PubMed1988

Changes of portal systemic shunting after sclerotherapy and/or partial splenic embolization observed by thallium-201 per rectal administration.

Tl-201 per-rectal scintigraphy was performed before and after injection sclerotherapy of esophageal varices and/or partial splenic embolization in patients with esophageal varices to observe the changes of portal systemic shunting by these treatments. The changes in the heart-to-liver uptake ratio of Tl-201 after injection sclerotherapy ranged widely from a decrease to an increase with a mean change rate (mean of the absolute value of change rate) and one standard deviation of 19.0 +/- 19.9%. By partial splenic embolization the heart-to-liver uptake ratio was decreased significantly with the mean change rate and one standard deviation of 26.2 +/- 17.4% (P less than .05). This noninvasive and simple method seems to be useful in evaluating pathophysiological changes of portal systemic shunting observed from inferior mesenteric vein blood flow after treatments of portal circulation system.

Administration, Rectal↗

PubMed1998

Studies of drug delivery systems for a therapeutic agent used in osteoporosis. I. Pharmacodynamics (hypocalcemic effect) of elcatonin in rabbits following rectal administration of hollow-type suppositories containing elcatonin.

In this study, we developed a new hollow-type suppository containing elcatonin ((Asu1,7)-eel calcitonin, ECT), a synthetic derivative of eel calcitonin, which produces hypocalcemia, as a pharmaceutical preparation for self administration, to be used instead of parenteral injections for patients with osteoporosis. The absorption of ECT from the rectal mucous membrane was evaluated by observation of the decrease in serum calcium (Ca) concentrations following rectal administration in rabbits. ECT was efficiently absorbed from the rectum and effectively decreased serum Ca concentrations. The data of the area under the percent decrease in serum Ca concentration (deltaCa%)-time curve (deltaCa%-AUC), assumed to be an index of the pharmacodynamics (pharmacological effect) of ECT, indicated that similar hypocalcemic effects were obtained following rectal and intravenous administrations of ECT. In regard to the effect of coadministration of other compounds on rectal absorption of ECT, no significant difference in the deltaCa%-AUC between rectal ECT administration with or without nafamostat mesilate (a protease inhibitor) was observed. However, the coadministration of ECT with cytochalasin B or monensin (endocytosis inhibitors) significantly decreased the deltaCa%-AUC, indicating that rectal ECT absorption is probably inhibited by endocytosis inhibitors. On the other hand, it was found that sodium decanoate, a medium-chain fatty acid (sodium salt), significantly enhanced the rectal absorption of ECT. We conclude that this ECT hollow-type suppository offers promise as a new method for the administration of ECT.

Absorption↗

PubMed1975

Plasma levels of diazepam after parenteral and rectal administration in children.

Plasma levels of diazepam and N-desmethyldiazepam were investigated in 19 children by a gas chromatographic method permitting the use of capillary sample. Intravenous administration was studied in 3 children and the plasma level curves showed a rapid decline during the first hour. Absorption and elimination after rectal administration of a solution in 16 children were similar to those after intramuscular administration. Diazepam given by suppository to 5 children gave much lower plasma levels and delayed time to peak levels. Recurrence of seizures in 2 children indicated that the anticonvulsants plasma level was of the order of 150 to 200 mug/liter. No significant side effects were observed. Thus rectal administration of a solution of diazepam is a practical method to arrest convulsions in children.

Child↗

PubMed1982

Metabolism and excretion of the quaternary ammonium compound thiazinamium methylsulfate (Multergan) in man. II. Oral and rectal administration.

In this study it is shown that biotransformation of thiazinamium, when given orally, does not differ qualitatively from the pattern found after parenteral administration. However, quantitatively both the metabolism and excretion patterns are considerably different from those after intravenous injection. The renal clearance accounted for 256 +/- 136 ml.min-1 (mean +/- SD). This value is higher than glomerular filtration, which may be indicative of an active excretion process. Hepatic clearance (biotransformation and biliary excretion of unchanged cation) was 537 +/- 495 ml.min-1 (mean +/- SD). Hepatic clearance was found to correlate negatively with bioavailability. The ratio between unchanged drug and the only metabolite, the sulfoxide, in urine was about I:0.9. This is substantially different from that found after parenteral administration (ca. I:0.2), which may imply that a 'first-pass effect' occurs. It was estimated that ca. 50% of the absorbed amount was metabolized during the first liver passage. The fate of thiazinamium after rectal administration in Witepsol HI5 suppositories shows several similarities with that after oral administration. The ratio between unchanged drug and metabolite in urine in this case was ca. I:0.8, indicating that also after rectal administration a 'first-pass effect' occurs, now to a degree of ca. 35%.

Administration, Oral↗

PubMed2004

Ketamine and midazolam for invasive procedures in children with malignancy: a comparison of routes of intravenous, oral, and rectal administration.

We investigated the efficacy of a combination of ketamine and midazolam, comparing intravenous, oral, and rectal administrations for invasive procedures in children with malignancy. Seventy-three children under 5 years of age, who were scheduled for invasive procedure, were assigned to one of three groups: IV group (n = 25), ketamine 1 mg/kg and midazolam 0.05-0.1 mg/kg were given intravenously; PO group (n = 24), ketamine 3 mg/kg and midazolam 0.5 mg/kg were given orally; and PR group (n = 24), ketamine 3 mg/kg and midazolam 0.5 mg/kg given rectally. Vital signs including blood pressure, pulse rate, respiratory rate, and oxygen saturation were monitored, and patients were observed for side-effects. Optimal sedation (drowsy and asleep) was provided in 78 per cent of all patients and no statistical difference was observed among the three groups. No severe complications were observed in all groups. Recovery time from sedation was significantly longer in the intravenous group (>120 min in two patients). Hallucination was noted in three (12 per cent) patients given intravenous medication, but not in those given oral or rectal medications. It is concluded that intravenous, oral, and rectal midazolam/ketamine are equally effective for invasive procedures in children with malignancy. The use of intravenous ketamine/midazolam may produce prolonged sedation and psychedelic effects in children. These adverse effects may alter the child's comfort and parental satisfaction.

Administration, Oral↗

PubMed1989

Distributions of tegafur in tissues of gastric adenocarcinoma patients: tissue uptakes and concentrations in plasma after oral and rectal administrations.

Fifty-one gastric adenocarcinoma patients were divided into two groups, according to the route of administration of the anticancer drug. One group was given FT-207 (tegafur, an enteric coated granule) orally and the other group, FT-207 in the form of a suppository. Blood and tissue concentrations of the drug were examined after a three-day administration of 750 mg at 09.00 and 21.00 hours. There were no significant differences between the two groups with respect to the concentrations of FT-207 and its metabolite 5-FU in the tissues. Levels of 5-FU in the excised tumor averaged 0.256 and 0.160 micrograms/g, in oral and rectal administrations, respectively, and levels in normal lymph nodes averaged 0.174 and 0.179 micrograms/g, respectively. The difference in 5-FU levels between normal and tumor tissues was statistically significant (P less than 0.05).

Adenocarcinoma↗

PubMed1995

Rectal administration of iodide and propylthiouracil in the treatment of thyroid storm.

We administered potassium iodide and propylthiouracil per rectum, in conjunction with intravenous dexamethasone and propranolol, for emergent treatment of a patient in thyroid storm with small bowel obstruction. Shortly after initiation of this treatment, the patient successfully underwent two emergent surgical procedures for resection of an intestinal volvulus with advanced peritonitis. Serum levels of iodide and propylthiouracil showed substantial absorption of these drugs via the rectal route. Measurement of 24-h urinary-free iodide indicated that the bioavailability of potassium iodide delivered by retention enema was at least 40%. Parenteral iodide preparations have been unavailable in the past, and continue to be difficult to obtain emergently. Rectal administration of inorganic iodide is an effective, readily available and less expensive alternative to parenteral sodium iodide for patients in thyroid storm with upper gastrointestinal tract dysfunction.

Administration, Rectal↗

PubMed1990

Design of a polyvinyl alcohol hydrogen containing phospholipid as controlled-release vehicle for rectal administration of (+/-)-propranolol HCl.

Polyvinyl alcohol hydrogels which contained phospholipid, egg yolk lecithin or hydrogenated soya lecithin were designed as a transrectal delivery system for propranolol hydrochloride. The hydrogel preparations containing phospholipid were prepared by a low-temperature crystallization method. The release profile of propranolol from hydrogel preparations containing phospholipid complied with Fickian diffusion (Higuchi model). The release of propranolol from the hydrogel preparation decreased with higher contents of phospholipid (approximately 2% w/w). In rats plasma concentrations of propranolol after rectal administration of hydrogel preparations containing phospholipid (1 and 2% w/w) were prolonged compared with those of rats receiving preparations without phospholipid.

Administration, Rectal↗

PubMed2006

Severe hypokalemia caused by oral and rectal administration of bentonite in a pediatric patient.

BACKGROUND: Bentonite is a clay substance that has been used as a homeopathic cathartic. Oral ingestion of bentonite in large quantities has the potential to cause gastrointestinal obstruction and electrolyte abnormalities. We present a case of severe hypokalemia in a pediatric patient who received both oral and rectal administrations of bentonite. CASE: A 3-year-old girl presented with a chief complaint of vomiting, constipation, lethargy, and weakness over several days. On initial evaluation, the child was mildly dehydrated and had a serum potassium of 0.9 mmol/L. Electrocardiographic findings were also consistent with hypokalemia. Upon further questioning, the parents reported that they had been administering a home remedy, containing colloidal bentonite, both orally and rectally as treatment for persistent constipation. The child received intravenous antibiotics, a normal saline bolus, and multiple boluses of potassium chloride, resulting in eventual normalization of her electrolyte abnormalities. CONCLUSION: Ingestion of large quantities of clay substances, such as bentonite, can result in gastrointestinal binding of essential electrolytes and possible obstruction. Symptoms and laboratory values often resolve with replacement of electrolytes and cessation of bentonite intake. Although cases of oral ingestion of clay-like substances resulting in electrolyte abnormalities have been reported, there are no previously reported human cases of hypokalemia caused specifically by bentonite administration. This may be due to the unique rectal administration seen in this child, which has not previously been described.

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↗

PubMed2002

Pharmacokinetics of ketotifen fumarate after intravenous, intranasal, oral and rectal administration in rabbits.

The pharmacokinetics of ketotifen fumarate (KF) was examined after administration in rabbits through four different routes (intravenous, intranasal, oral and rectal). The time-course of the plasma concentration of KF after intravenous administration (1 mg/kg dose) fitted a two-compartment open model. KF was rapidly absorbed and showed a high plasma concentration within 0.33 h after intranasal administration. The absolute bioavailability of KF after intranasal administration was 66%. After oral administration at a dose of 1 mg/kg, the plasma concentration of KF was below the detection limit of HPLC analysis. Even at 5 mg/kg, the value of the area under the plasma concentration-time curve (AUC) after oral administration of KF was significantly lower than that after intranasal administration of 1 mg/kg. Oral bioavailability was only 8%. The very low bioavailability of KF after oral administration might be due to the first-pass effect in the liver. We also prepared suppositories containing KF (1 mg/kg) for rectal administration in rabbits. After rectal administration, KF was rapidly absorbed and its bioavailability was 34%. These results indicated that the intranasal route appears the most effective for administering KF, and that rectal administration may be superior to oral administration in terms of bioavailability.

Administration, Intranasal↗

PubMed2005

Formulation and evaluation of diazepam hydrogel for rectal administration.

Diazepam (DZP) has become a commonly used drug for treatment of acute repetitive epileptic seizures and febrile convulsions in children. Considering the advantages of rectal administration of DZP, the objective of our study was to formulate and evaluate rectal hydrogels containing DZP as a drug substance in combination with suitable co-solvents and preservatives. Prepared HPMC (hydroxypropyl methylcellulose) hydrogels containing different concentrations of DZP (2, 4 and 6 mg mL(-1)) manifested good quality in respect to physico-chemical parameters (pH value, drug content, ingredients content and viscosity), antimicrobial efficiency and microbiological quality. Under the proposed HPLC conditions, satisfactory separation of DZP and the preservatives used was achieved. In vitro release studies have shown that the total amount of DZP was released in a period of 3 h. Prepared formulations were stable for four months at 26 degrees C (ambient temperature characteristic of the 2nd climate zone).

Administration, Rectal↗

PubMed1983

Serum concentration of clonazepam after rectal administration.

The purpose of the present study was to evaluate the absorption of clonazepam administered rectally. 10 adult non-epileptics were given 0.02 mg clonazepam/kg body weight, and blood samples were drawn 0, 2, 5, 7, 10, 15, 30 and 60 min after administration. The concentrations were measured by gas-chromatography. To gain an impression of the serum concentration after intravenous administration, 2 persons were given 1 mg clonazepam and blood samples were drawn and analyzed in the same way as after rectal administration. Peak values occurred 10 to 30 min after rectal administration; the values were between 18 and 57 nmol/l. After intravenous administration, the values were very high within the first 10-15 min; hereafter the concentrations were about the same level as the peak values after rectal administration, indicating that clonazepam is well-absorbed after rectal administration and can be used in the treatment of status epilepticus, possibly in larger doses than those used in this study.

Adult↗

PubMed1995

[Rectal administration of anesthetic agents].

OBJECTIVES: To collect data in the current literature dealing with the diffusion, the reliability and the effectiveness of the rectal administration of anaesthetic drugs. To evaluate differences with parenteral administration. DATA SOURCES: Pharmacokinetics and clinical studies published in recent years in indexed journals. STUDY SELECTION: Based on the study methodology, drugs employed and pharmacokinetic parameters evaluated. DATA EXTRACTION: Factors involved in absorption of drugs from the rectal mucosa, clinical effect and pharmacokinetic data of the following drugs: diazepam, flunitrazepam, midazolam, ketamin and methohexital, then a brief evaluation of other drugs: thiopental, etomidate, morphine and chloral hydrate. DATA SYNTHESIS: The most widely used drugs are benzodiazepines: they are safe, easy to manage and highly effective; among them midazolam has the best kinetic and dynamic pattern. Ketamin is useful during painful diagnostic procedures; with the use of barbiturates there is a greater risk of respiratory depression and more caution must be employed. CONCLUSIONS: Wide intervariability of rate of absorption, achievement of plasma levels and clinical effect is a relevant drawback of this technique, such to make it not preferable to the parenteral route, when both are feasible. It deserves, anyway, more consideration, and maintains its validity for the preparation of the paediatric patient to general anaesthesia.

Administration, Rectal↗

PubMed1997

Midazolam for premedication in children: nasal vs. rectal administration.

The authors compared the acceptance and efficacy of rectal and nasal administration of midazolam (MDZ) for premedication. Ninety-five ASA I and II paediatric patients (8 months to 12 years) scheduled for elective surgery were randomly allocated to two groups. Group R received 0.3 mg kg-1 of rectal midazolam (in 5 mL saline). Group N received 0.2 mg kg-1 of nasal midazolam (5 mg ml-1). Both groups were divided in two subgroups according to age (group RA (< or = 6 years, n = 33), group RB (> 6 years, n = 18), group NA (< or = 6 years, n = 28), group NB (> 6 years, n = 16)). At the time of premedication, tolerance to the administration was confirmed. Twenty min after rectal or 10 min after nasal administration the quality of sedation was recorded. The nasal midazolam, in commonly used dosages, induced a sedation similar to that following rectal administration with a shorter delay of onset. Nasal administration was more often painful than rectal administration. Swallowing (nasal midazolam) and concerns about modesty (rectal midazolam) were more frequent in older children. Because of its poor tolerance, nasal premedication should be reversed for cases where there is no alternative. Rectal premedication should be avoided in older children.

Administration, Intranasal↗

PubMed1981

Bioavailability of phenobarbital by rectal administration.

Phenobarbital was administered to five patients, eight to 20 years of age, by four different administration routes: Intravenous, intramuscular, oral, and rectal. At each administration, extent of bioavailability, elimination rate constant, absorption rate constant, and volume of distribution of phenobarbital were calculated using a one-compartment open model. The results obtained suggest that rectal administration of phenobarbital is more reliable than intramuscular or oral administration of the drug for rapid treatment in children.

Adolescent↗

PubMed1999

The relative bioavailability of metoprolol following oral and rectal administration to volunteers and patients.

The pharmacokinetics, efficacy and safety of metoprolol tartrate 25 mg fatty suppositories were studied in 5 healthy volunteers and in 8 patients suffering from instable angina pectoris. Metoprolol 25 mg capsules were used as a control oral dosage form. Metoprolol showed a considerable rectal bioavailability (AUC, C max) and was absorbed quickly from the rectum (T max). In both groups rectal bioavailability was comparable. However, oral bioavailability was much lower in the volunteer group than in the patient group. Furthermore, ratios of metoprolol/alpha-OH-metoprolol concentrations in plasma and urine gave an indication for a partial avoidance of the first pass effect after rectal administration. Further research is necessary to define an exact rectal dosage of metoprolol. In all patients, a substantial drop in heart rate, systolic and diastolic blood pressure was seen after administration of the first suppository. Metoprolol suppositories appear to be an effective, safe and suitable alternative for patients who are in need for beta blocking medication and who are unable to take oral medication for a certain amount of time.

Administration, Oral↗

PubMed1995

Absorption enhancement of a hydrophilic model compound by verapamil after rectal administration to rats.

The use of verapamil as an absorption enhancer for the paracellular route in-vivo was studied using FITC-labelled dextran (molecular weight 4000) (FD-4) as a hydrophilic model compound for transport enhancement. The kinetics of FD-4 after intravenous doses of 1 or 10 mg could be described by a two-compartment model with a systemic clearance of approximately 2 mL min-1 and a terminal plasma half-life of approximately 36 min. Rectal administration to rats, performed as a rectal infusion of 10 mg FD-4 together with 7 mM verapamil, resulted in a 10-fold increase in the percentage of the dose absorbed over a 5-h period compared with the control and a 6-fold increase compared with a bolus administration, although the total amount absorbed remained relatively low (approx. 3% maximum). Large inter-animal variation in effect values were noted. The data indicate that although verapamil is able to enhance the absorption of hydrophilic compounds in-vivo, practical application of verapamil for this purpose doses not seem feasible.

Administration, Rectal↗