The pharmacokinetics of artemisinin after administration of two different suppositories to healthy Vietnamese subjects.
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Eight healthy Vietnamese male subjects received 400 mg artemisinin formulated into fatty suppositories (FS), and six different subjects received 500 mg of artemisinin formulated in polyethylene glycol suppositories (PEGS). Plasma concentrations were measured by high-performance liquid chromatography with electrochemical detection; concentration versus time curves were analyzed with nonparametric methods. No statistically significant differences were found between the two formulations. The maximum concentration (Cmax) was 100 +/- 102 microg/L (mean +/- SD, range = 24-330) microg/L (FS), the pharmacokinetic lag time (Tlag) was 1.3 +/- 1.0 hr (range = 0-3) (FS), and the time of the maximum concentration (Tmax) was 7.1 +/- 2.1 hr (range = 3-10) hr (FS). Because artemisinin is not available for intravenous dosage, absolute bioavailability cannot be assessed. However, compared with a previous study on oral artemisinin in healthy Vietnamese subjects, bioavailability relative to oral administration was estimated to be approximately 30%. We conclude that therapeutic blood concentrations of artemisinin can be reached after rectal dosage. The dose after rectal administration should probably be higher than after oral administration; doubling or tripling the oral dose might be necessary, which would imply a rectal dose of at least 20 mg/kg of body weight given twice a day. (+info)
Efficacy of promethazine suppositories dispensed to outpatient surgical patients.
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Postoperative nausea and vomiting frequently complicate outpatient anesthesia and surgery. The duration of treatment for this complication must occasionally extend beyond discharge from the hospital. In this study, we evaluated the commonly used anti-emetic promethazine for its efficacy in the post-discharge period. Adult outpatient surgical patients who had excessive postoperative nausea and vomiting in the recovery room, or who were at risk for postoperative nausea and vomiting following discharge were given two promethazine suppositories (25 mg) for home use. All patients were contacted by our recovery room nurses on the first business day after their surgery and questioned as to their use of the suppositories and, if used, their efficacy. We found that 55 percent of patients given promethazine suppositories for home use had nausea and vomiting in the post-discharge period. Of the patients given promethazine, 89 percent used the suppositories. All of these patients reported improvement in their symptoms following use of the suppositories. None reported adverse effects from the promethazine suppositories. In conclusion, we found promethazine suppositories to be an inexpensive and efficacious treatment for nausea and vomiting in adult outpatient surgical patients following discharge from the hospital. Side-effects were minimal, and our patients voiced no complaints about this mode of therapy. We recommend this therapy for treatment of nausea and vomiting after hospital discharge following adult outpatient surgery. (+info)
Rectal paracetamol has a significant morphine-sparing effect after hysterectomy.
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We have evaluated the morphine-sparing effect of rectal paracetamol during the first 24 h after abdominal hysterectomy in a placebo-controlled, double-blind study. We studied 72 patients receiving patient-controlled analgesia (PCA) with i.v. morphine after a standardized anaesthetic, allocated randomly to receive rectal paracetamol 1.3 g, diclofenac 50 mg or placebo, after wound closure and at 8 and 16 h. Suppositories were blinded by the hospital pharmacy. Study violations excluded data from seven patients. Patient data, morphine doses during anaesthesia and recovery, and sedation and nausea scores were comparable. Mean morphine consumption during PCA was 35.0 (SD 20.4) mg, 32.7 (27.4) mg and 54.9 (28.3) mg in the paracetamol (n = 24), diclofenac (n = 20) and placebo (n = 21) groups, respectively (P < 0.05). Morphine sparing during PCA for paracetamol and diclofenac (36% vs 40% over 24 h) was significant from 4 h. Global scores of average pain over 24 h were lower after diclofenac compared with paracetamol (P < 0.01) and placebo (P = 0.08). We conclude that rectal paracetamol was an efficacious adjuvant analgesic after regular dosing. (+info)
Improving the view in the rectal clinic: a randomised control trial.
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BACKGROUND: Rigid sigmoidoscopy forms an integral part of the out-patient assessment of patients with colorectal symptoms. However, the value of this of this examination is often diminished by faecal loading of the rectum. This trial aimed to determine the ability of a single self-administered glycerine suppository to clear the rectum in preparation for rigid sigmoidoscopy, and considered patient acceptability of this practice. METHODS: Consecutive patients were randomly allocated to receive suppository or no suppository prior to out-patient rigid sigmoidoscopy. Assessment was made of patient compliance, the effectiveness of rectal examination, and the depth to which the sigmoidoscope was inserted. RESULTS: 131 patients were randomised into suppository (n = 66) or control groups (n = 65). The number of patients deemed to have good views of the rectum (> 75% of rectal mucosa seen) was significantly greater in suppository than control groups (79% versus 26.2%, P < 0.05 Chi square test), whilst that of poor examinations (< 50% of rectal mucosa seen) was significantly greater in control than suppository groups (44.6% versus 4%, P < 0.05). The depth of insertion of the sigmoidoscope was significantly greater in those receiving suppositories (54.5% versus 21.5% undergoing evaluation to 18 cm or more, P < 0.05). Compliance amongst those who received suppositories was high with only 3 of 53 (4.5%) patients in the suppository group evaluated by questionnaire reporting difficulty or concerns over their use. CONCLUSION: Self-administered suppositories are acceptable to patients and significantly improve the efficiency of outpatient rigid sigmoidoscopy. Their usage should become routine. (+info)
Pharmacokinetics of rectal paracetamol after repeated dosing in children.
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Twenty-three children (aged between 9 weeks and 11 yr) were given paracetamol suppositories 25 mg kg-1 every 6 h (maximum 5 days) after major surgery and serum and saliva concentrations were measured. There was a good correlation (r = 0.91, P < 0.05) between saliva and serum concentrations. A one-compartment linear model with first-order elimination and absorption and lag-time was fitted to the data (ADAPT II). At steady state, the mean (SD) concentration was 15.2 (6.8) mg litre-1. Mean (SD) time to reach 90% of the steady state concentration was 11.4 (8.6) h. Body weight, age and body surface area were well correlated (P < 0.05) with clearance and apparent volume of distribution. There was no evidence of accumulation leading to supratherapeutic concentrations during this dosing schedule for a mean of approximately 2-3 days. (+info)
An unexpected benefit of pre-emptive rectal analgesic administration: the "key" to postoperative analgesia.
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Analgesic and anti-inflammatory drugs are frequently administered intraoperatively by the rectal route to provide pre-emptive postoperative analgesia. We report the case of an inmate of a federal penitentiary who underwent orthopedic surgery in a public hospital. After induction of general anesthesia, indomethacin and acetaminophen were administered rectally. This led to the incidental discovery of a handcuff key hidden in the rectum and, thereby, the prevention of a planned escape. A review of data regarding escapes by prisoners from public hospitals is provided, as well as a description of cases of patients presenting with foreign rectal objects. A number of benefits have been described for the use of pre-emptive analgesia. This is the first reported description of an incidental benefit: the prevention of a planned escape by a prison inmate. (+info)
The suppository form of antibiotic administration: pharmacokinetics and clinical application.
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The rectal route of antibiotic administration might be used effectively when other routes of administration are inadequate or unsuitable. With the use of various adjuvants, the rectal route can provide satisfactory pharmacokinetics and acceptable local tolerance. Experiments in animals have demonstrated the influence of the pharmaceutical formulation of suppositories on the rectal absorption and systemic distribution of beta-lactams and aminoglycosides. In healthy volunteers and in children under treatment, similar adjuvants--mainly glyceride mixtures or non-ionic surface agents--have increased the rectal absorption of aminopenicillins, cephalosporins and macrolides. Other antibiotics, including metronidazole and cotrimoxazole, have been investigated in respect of their potential rectal administration. (+info)
Response of the human cardia sphincter to circulating prostaglandins F2ALPHA and E2 and to antiinflammatory drugs.
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The effects on intraluminal pressure in the oesophagus, the cardiac sphincter, and the gastric fundus of intravenous prostaglandin F2alpha, E2, And of rectal indomethacin were studies in 41 subjects. Intravenous infusion of prostaglandin F2alpha (0-05 to 0-8 mug kg-minus1) produced marked, dose-related and sustained elevation of cardiac sphincter pressure without significantly affecting oesophageal peristalsis or gastric fundal motility. Sphincteric relaxation during swallowing was prolonged. Plasma gastrin levels were unchanged. Intravenous infusion of PGE2 (0-08 mug kg-minus1 min-minus) inhibited sphincter contractions to serial bolus intravenous injections of pentagastrin (0-1 or 0-2 mug kg-minus 1). Rectal indomethacin (200 mg) resulted in a riseof cardiac sphincter pressure, suggesting that endogenous synthesis of an inhibitory (E-type) prostaglandin was suppressed. The results indicate that prostaglandin E2 may be concerned in the regulation of cardiac sphincter tone in man, whilst prostaglandin F2alpha may be useful in the treatment of gastrooesphageal reflux. (+info)