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Background: Opioids inhibit motility and secretion of the gut and have been used for antidiarrheal treatment for centuries. However, the underlying mechanisms of opium tincture are not evident., Aim: To investigate the effects of opium tincture on gastrointestinal motility, intestinal volumes, and water content of different gut segments assessed by magnetic resonance imaging (MRI)., Methods: Twenty healthy volunteers were included in a randomized, placebo-controlled, crossover study of 9 days of treatment with 30 drops of opium tincture per day. MRI was performed on day 1 (before treatment) and day 9 (during treatment). Measurements included assessments of gastric volume, gastric emptying, gastric motility, small bowel volume, small bowel water content, small bowel motility, colon volume, colon water content, and whole gut transit., Key Results: Opium tincture delayed gastric emptying by a mean difference of 5.6 min [95% CI: 1.8-9.4], p = 0.004, and increased postprandial gastric meal volume (17-21%, p = 0.02). Small bowel endpoints did not change. Opium tincture delayed whole gut transit time (p = 0.027) and increased ascending colon volume by 59 mL [95% CI: 15-103], p = 0.004, and transverse colon volume by 48 mL [95% CI: 4-92], p = 0.027. T1-relaxation time of the descending colon chyme was decreased during opium treatment, indicating dryer feces (difference: -173 ms [95% CI: -336 -11], p = 0.03)., Conclusion and Inferences: Opium tincture induced changes in the stomach and colon in healthy volunteers. An improved understanding of how opioids affect gut functions may lead to a better understanding and optimized management of diarrhea., (© 2024 The Author(s). Neurogastroenterology & Motility published by John Wiley & Sons Ltd.)

Polypharmacy of elderly oncology patients and fragmented medication management are well-known risk factors for drug-drug interactions (DDIs). These interactions can occur among antineoplastic, ongoing chronic treatment(s) and chemotherapy-associated treatments, like antiemetics. Clinically relevant interactions based on enzyme- or transporter-inhibition phenomena of active drugs can increase the frequency of their DDIs. We describe a strongly suspected elderly cancer patient's DDI between aprepitant and opium powder in the context of an irinotecan-based regimen manifested by nightmares and visual hallucinations. We discuss this DDI's hypothetical pharmacological mechanisms and management., (© 2018 The British Pharmacological Society.)

Objective: The primary outcome of this study was to evaluate the effect of adding sufentanil to hyperbaric bupivacaine on duration of sensory blockade of spinal anesthesia in chronic opioid users in comparison with non-addicts., Methods: Sixty patients scheduled for orthopedic surgery under spinal anesthesia were allocated into four groups: group 1 (no history of opium use who received intrathecal hyperbaric bupivacaine along with 1mL saline as placebo); group 2 (no history of opium use who received intrathecal bupivacaine along with 1mL sufentanil [5μg]); group 3 (positive history of opium use who received intrathecal bupivacaine along with 1mL saline as placebo) and group 4 (positive history of opium use who received intrathecal bupivacaine along with 1mL sufentanil [5μg]). The onset time and duration of sensory and motor blockade were measured., Results: The duration of sensory blockade in group 3 was 120±23.1min which was significantly less than other groups (G1=148±28.7, G2=144±26.4, G4=139±24.7, p=0.007). The duration of motor blockade in group 3 was 145±30.0min which was significantly less than other groups (G1=164±36.0, G2=174±26.8, G4=174±24.9, p=0.03)., Conclusions: Addition of 5μg intrathecal sufentanil to hyperbaric bupivacaine in chronic opioid users lengthened the sensory and motor duration of blockade to be equivalent to blockade measured in non-addicts., (Copyright © 2015 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.)

We aimed to investigate the effect of perioperative analgesia with nonselective cyclooxygenase-2 inhibitor dexketoprofen and opioid drug omnopon on the functional activity of immune cells in tumor excision murine model. Lewis lung carcinoma cells were transplanted into hind paw of C57/black mice. On the 23th day tumor was removed. Analgesic drugs were injected 30 min before and once a day for 3 days after the surgery. Biological material was obtained a day before, 1 day and 3 days after the tumor removal. IFN-γ, IL-4, IL-10 and TGF-β mRNA levels in splenic cells were assessed by quantitative real-time RT-PCR. Cytotoxic activity of splenocytes was estimated by flow cytometry. We found that in splenocytes of mice received opioid analgesia IL-10 mRNA level was increased 2.3 times on day one after the surgery compared to preoperative level (P < 0.05), while in dexketoprofen group this parameter did not change. IFN-γ gene expression level on day 3 after tumor removal was 40% higher in splenocytes of dexketoprofen treated mice as compared with omnopon treated animals (P < 0.05). Cytotoxic activity of splenocytes on day 3 postsurgery was (62.2 ± 2.4)% in dexketoprofen against (50.2 ± 3.3)% in omnopon group. In conclusion, perioperative analgesia with cyclooxygenase inhibitor dexketoprofen in contrast to opioid analgesia with omnopon preserves higher functional activity of murine immune cells in the experimental model of tumor surgery.

Ethnopharmacological Relevance: Past practices of compound drugs from different plant ingredients enjoyed remarkable longevity over centuries yet are largely dismissed by modern science as subtherapeutic, lethal or fanciful., Aim of the Study: To examine the phytochemical content of a popular medieval opiate drug called the "Great Rest" and gauge the bioavailability and combined effects of its alkaloid compounds (morphine, codeine, hyoscyamine, scopolamine) on the human body according to modern pharmacokinetic and pharmacodynamic parameters established for these compounds., Calculations and Theory: We reviewed the most recent studies on the pharmacodynamics of morphine, codeine, hyoscyamine and scopolamine to ascertain plasma concentrations required for different physiological effects and applied these findings to dosage of the Great Rest., Results: Given the proportional quantities of the alkaloid rich plants, we calculate the optimal dose of Great Rest to be 3.1±0.1-5.3±0.76 g and reveal that the lethal dose of Great Rest is double the therapeutic concentration where all three alkaloid compounds are biologically active., Conclusion: This study helps establish the effective dose (ED50), toxic dose (TD50) and lethal dose (LD50) rates for the ingestion of raw opium, henbane and mandrake, and describes their probable combined effects, which may be applied to similar types of pre-modern pharmaceuticals to reveal the empirical logic behind past practices., (Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.)

Illicit drug use can be an important cause of male infertility. The aim of this study was to investigate the effects of an Iranian illicit drug, Kerack, on sperm parameters, testicular structure and CatSper genes expression of mice. In this study, 25 male mice were divided into five groups consisting of control, sham and three experimental groups. All animal in experimental groups were addicted to Kerack for 7 days. These experimental groups include experimental I which was given Kerack at a dose of 5 mg/kg, experimental II, 35 mg/kg and experimental III, 70 mg/kg, intraperitoneally twice a day for a period of 35 days. Mice were then sacrificed and spermatozoas were removed from cauda epididymis and analyzed for count, motility, morphology (normal/abnormal) and viability. Right testes were removed, weighed and processed for light microscopic studies whereas left testes removed were subjected to total mRNA extraction for using in real-time PCR (RT-PCR). The results were analyzed by performing anova (Tukey's tests) and Pearson correlation coefficient. Sperm parameters and seminiferous epithelium thickness were decreased in experimental groups (dose-dependently) vs. sham and control groups (p < 0.05). RT-PCR results showed that CatSper 2, 3, 4 genes expressions were reduced with 35 and 70 mg/kg injected Kerack when compared with control testes (p ≤ 0.05). However, CatSper1 expression was only reduced with high dose injected Kerack (70 mg/kg) in comparison to control testes (p ≤ 0.05). This study shows the deleterious effects of Kerack used in Iran on testis structure and sperm parameters in general, and particularly sperm morphology in adult mouse. It could down-regulate the expression of CatSper genes, resulting in depression of sperm motility., (© 2014 American Society of Andrology and European Academy of Andrology.)

Addiction to opium continues to be a major worldwide medical and social problem. The study addressing the association between opium consumption and serum prostate-specific antigen (PSA) level is lacking. We determined the effects of opium consumption on serum PSA levels in opium-addict men. Our study subjects comprised 438 opium-addict men with a mean age of 52.2 ± 6.4 years (group 1). We compared these men with 446 men who did not indicate current or past opium use (group 2). Serum total PSA (tPSA), free PSA (fPSA), % fPSA, and sex hormones were compared between the 2 groups. The mean serum tPSA level was significantly lower in group 1 (1.05 ng/mL) than in controls (1.45 ng/mL) (P = 0.001). Opium consumption was also associated with lower fPSA (P = 0.001) and % fPSA (P = 0.001). Serum free testosterone level in opium-addict patients (132.5 ± 42 pg/mL) was significantly lower than that in controls (156.2 ± 43 pg/mL) (P = 0.03). However, no significant correlation existed between tPSA and free testosterone levels (r = 0.28, 95% CI, -0.036 to 0.51, P = 0.34). Among the patients with cancer in group 1, 35% were found to have high-grade tumor (Gleason score ≥ 7) compared with 26.7% in group 2 (P = 0.02). Total PSA and fPSA were strongly correlated with duration of opium use (r = -0.06, 95% CI, -0.04 to -0.08, P = 0.0001; and r = -0.05, 95% CI, -0.03 to -0.07, P = 0.0001, respectively). Opium consumption is independently and negatively associated with serum tPSA, fPSA, and % fPSA levels.

Background: There is evidence that opium addiction has immunosuppressant effects. Coronary artery disease (CAD) is a condition resulted from atherosclerosis which is dependent on the immune response., Purpose: To evaluate plasma levels of interleukin-6 and interleukin-1Ra in 30 patients with three-vessel coronary artery disease, ejection fraction of more than 35% and to evaluate their changes after prognostic treadmill test in 15 opium addicted and 15 non-addicted patients., Methods: The participants underwent prognostic treadmill test and plasma levels of interleukin-6 (IL-6) and interleukin-1Ra (IL-1Ra) were evaluated with ELISA method before, just after and 4 hours after the test., Results: IL-1Ra (2183 pg/ml) tended to decrease over time in the opium addicted group (1372 pg/ml after prognostic treadmill test and 1034 pg/ml 4 hours after that), although such decrease did not reach the statistical significance. IL-1Ra levels were significantly higher in opium addicted than in non addicted patients. Opium addiction had no significant effect on IL-6 changes., Conclusion: Consumption of opium in CAD patients is associated with higher IL-1Ra levels.

Background: This experimental study was performed to determine the impact of opium use on serum lipid profile and glucose metabolism in rats with streptozotocin-induced diabetes., Material and Methods: To determine the effect of opium, 20 male rats were divided into control (n = 10) and opium-treated (n = 10) groups. After diabetes induction, the animals were investigated for daily glucose measurements for 35 days. Serum lipid profile and haemoglobin A1c (HbA(1c)) were assayed at the baseline (before induction of diabetes) and at 35-day follow-up., Results: The glycaemia levels in the rats treated with opium were similar to the levels measured in the control rats (544.8 +/- 62.2 mg/dl v. 524.6 +/- 50.0 mg/dl, P = 0.434). In addition, there was no difference between the opium-treated rats and control rats in HbA(1c) (6.5 +/- 0.5% v. 6.6 +/- 0.2%, P = 0.714). Compared to the control rats, the serum total cholesterol, high density lipoprotein (HDL), triglyceride and lipoprotein (a) in the test animals were similar., Conclusion: Opium use has no significant effect on glucose metabolism and serum lipid profile in rats with induced diabetes.

To determine the effects of opium on serum glucose, potassium and sodium in male and female Wistar rat, opium solution (60 mg/kg) injected intraperitoneally and the same volume of distilled water was used as control (7 rats in each group). Blood samples were collected at 0, 30, 60, 120, 240 and 360 minutes after injection from orbit cavity and the values of serum glucose, sodium (Na(+)) and potassium (K(+)) were measured. The data were then analyzed by the repeated measure ANOVA based on sex and case-control group. P < 0.05 considered as significant difference. Serum glucose increased significantly at 30, 60, 120 and 240 minutes after opium solution injection, in female rats compared to a control group. However, the male rats had this rise at 30, 60 and 120 minutes after opium solution injection compared to control group. While serum glucose in male rats was significantly higher than females at 30, 60 and 120 minutes, this value was higher in the female rats at 360 minutes. Therefore, serum glucose alterations following opium injection was significantly different in groups and in the sexes at different times. Sodium (Na(+)) rose at 60, 240 and 360 minutes significantly in all rats compared to control group. However, sodium alteration following opium injection was significantly different only between treated and control groups but sex-independent at all times. Potassium (K(+)) increased significantly at 60, 120, 240 and 360 minutes in male rats, compared to a control group. In female rats K(+) significantly raised at 30, 120, 240 and 360 minutes. Therefore, the alteration of K(+) in male and female rats was found time dependent and sex independent. According to our results, opium increased serum glucose in male and female rats differently, and it interferes with metabolic pathways differently on a gender dependent basis. Opium raised serum Na(+) and K(+), thus it interfere with water regulation and blood pressure via different mechanism.

Paregoric elixir is a phytomedicinal product which is used widely as an analgesic, antispasmodic and antidiarrheal agent. Here, we investigated the pharmacological actions and some of the mechanisms of action of paregoric elixir and compared its action with some of its components, the alkaloids morphine and papaverine. The paregoric elixir given orally to mice did not present relevant toxic effects, even when administered in doses up to 2000-fold higher than those used clinically. However, it showed an antinociceptive action that was more potent, but less efficacious, than morphine. In contrast to morphine, its effect was not dose-dependent and not reversed by the non-selective opioid antagonist naloxone. Moreover, paregoric elixir produced tolerance, but did not cause cross-tolerance, with the antinociceptive actions of morphine. When assessed in the gastrointestinal motility in vivo, paregoric elixir elicited graduated reduction of gastrointestinal transit. Finally, like morphine and papaverine, paregoric elixir concentration-dependently inhibited electrically-induced contraction of the guinea pig isolated ileum. In vivo and in vitro gastrointestinal actions of paregoric elixir were not reversed by naloxone. Collectively, the present findings lead us to suggest that the pharmacological actions produced by paregoric elixir are probably due to a synergic action of its constituents.

Exposures to toxins are prevalent, frequently complicate surgical emergencies, and impact critical care. A fundamental understanding of pathophysiologic principles and management strategies is essential for the anesthesiologist frequently responsible for the acute care of patients who have toxicologic exposures. Given their pervasiveness and ability to confound the clinical presentations in the perioperative or intensive care setting, substances of abuse and asphyxiants warrant particular attention and a high degree of vigilance.

People addicted to opium rarely develop intra-abdominal adhesions after abdominal surgery. We aimed to evaluate the effect of opium or morphine on preventing postoperative adhesions in rats. Sixty-three rats were randomly divided into a control group, opium-addicted group, and morphine-addicted group in a double-blind study. Drug dependency was checked by using naloxone. Animals were then operated on and the cecum was abraded. At reoperation 3 weeks later the magnitude of adhesions was evaluated by a scoring system. There was a significant difference between the control, opium-addicted, and morphine-addicted groups with regard to the length (P < .001), thickness (P < .05), and severity of adhesions (P < .05). Opium or morphine reduces the severity of postoperative adhesions. Elucidation of the opioid receptor(s) involved in this process would enable the use of selective ligands and offer a pharmacologic strategy in preventing adhesion formation.

Active immunization of rats with mouse antibodies to morphine leads to the formation of antiidiotypic antibodies. This is paralleled by an increase in animal sensitivity to the analgesic and positive reinforcing effects of morphine, slower development of tolerance and formation of craving. These data indicate the possibility of active immunization against antibodies to morphine/heroin for the prevention of opium addiction relapses.

Previous studies have related opium and its pyrolysates to the risk of developing certain cancers. The aim of this work was to evaluate the clinical usefulness of determining carcinoembryonic antigen (CEA) and tissue polypeptide antigen (TPA) levels in habitual opium smokers. Serum CEA concentrations were measured in 128 opium smokers and in 44 controls of cigarette only smokers and 47 normal non-smokers by an EIA-based assay. TPA levels were also determined in serum and urine of a subgroup in the study population. The results indicated that serum CEA concentrations are higher in opium smokers than in healthy tobacco smokers (p = 0.004) and non-smokers (p = 0.001). The amount of opium used correlated with the serum CEA level (r = 0.276, p < 0.0001). The mean urine and serum TPA levels of the opium-addicted population were also higher than that of the non-smoking control group, but the differences were not statistically significant. We conclude that opium smoking is associated with elevated serum CEA levels. Therefore, for management of opium users with neoplastic diseases, increased levels of serum CEA should be viewed with caution to avoid misdiagnosis.

The present study was designed to evaluate the effect of repeated oral administration of cryptopine at differential dosing regimens (50, 100, 150, 200 mg/kg bwt) in vivo on lipid peroxide measures, glutathione levels (GSH) and activity of glutathione S-transferase (GST) and glutathione reductase (GR) in the liver, spleen, kidney and lung of Male Wistar rats after a 5 day treatment period. In all the tissues examined, we observed an increase in lipid peroxidation and a decline in glutathione content and activity of glutathione S-transferase and glutathione reductase in a dose-dependent manner. The decrease in GSH content did not definitively correlate with a concomitant increase of lipid peroxidation in all the tissues. Our results ensemble that the enhancement of lipid peroxidation in the tissues investigated is a consequence of depletion of glutathione to certain critical levels and impairment of the glutathione-dependent enzyme systems viz. GST and GR. Our study potentiates that decreased levels of GSH may lead to lipid peroxidation, one of the key events in cellular damage. The inhibition of GST also suggests that the detoxification of the alkaloid could be suppressed following acute exposures. Conclusively, it appears that cryptopine in vivo disturbs the cellular defense system, so that it tips in the direction of autoxidative lipid peroxidation, producing cytotoxicity.

Background: Opiate-induced sphincter of Oddi dysfunction (SOD) as a clinical entity has not been described., Methods: Eight chronic opium addicts (all men, mean age 61.3 years, mean duration of addiction 24.75 years) presenting with pancreatobiliary pain and a dilated bile duct with or without dilated pancreatic duct on abdominal US were studied. All patients underwent ERCP and biliary sphincterotomy. In addition, pancreatic sphincterotomy was performed in 4 patients with a dilated pancreatic duct., Observations: At ERCP, the bile duct was dilated in 8 and pancreatic duct in 4 patients. There was delayed drainage of contrast (>45 minutes) from the bile duct in all 7 patients studied, whereas delayed drainage from the pancreatic duct (>9 minutes) was incidentally observed in 3 patients. In 6 patients followed after sphincterotomy for at least 2 years, there was marked relief of symptoms. Transabdominal US at 2 years follow-up revealed a normal bile duct in 5 and persistent albeit minimal dilatation in 1 patient. Acute pancreatitis developed in 4 patients after ERCP and sphincterotomy, which was fatal in one. No patient had any abnormality in the gallbladder on initial or follow-up transabdominal US., Conclusion: SOD in opium addicts is a distinct clinical entity, mainly seen in men in this population, that is characterized by a long history of opium addiction and the absence of prior cholecystectomy or associated gallstone disease. Most patients are seen with the classic clinical picture of SOD with marked long-term improvement in symptoms after endoscopic sphincterotomy.

Endogenous and exogenous opioids can influence and modulate neuronal and glial cell function via an opioid receptor mediated mechanism, leading to either protection or damage of the brain. Opiates such as morphine have been postulated to promote the progression of HIV-1 and the development of secondary opportunistic infections. Kappa opioid receptor ligands, on the other hand, may play a neuroprotective role. More studies are needed to delineate how opioids exert their effects on glial cells as well as neurons with the goal of developing new therapeutic approaches for neurodegenerative disease.

A patient developing acute pancreatitis with pseudocyst formation after an uncomplicated bone marrow harvest is reported. The diagnosis was confirmed by elevated serum amylase and lipase, and by CT scan. We suggest that the pancreatitis may have been precipitated by spasm of the sphincter of Oddi secondary to opiates administered as premedication and for pain relief.

The high incidence of oesophageal cancer in Northern Iran has been associated with opium. N-Nitrosamines are the only carcinogens known to induce oesophageal cancer in animals. Ethanol, which is the major influence on oesophageal cancer incidence in the West, inhibits the first pass clearance of N-nitrosodimethylamine in animals and increases the alkylation of oesophageal DNA by oesophageal cancer-inducing N-nitrosamines. The experiments now reported were to test whether opium or morphine, which is the major alkaloid in opium, have a similar effect. It is shown that administration of morphine to rats does increase the ethylation of oesophageal DNA by N-nitrosodiethylamine and may reduce the first pass clearance of N-nitrosodimethylamine by the liver, but only at high doses of morphine.

The pharmacokinetics of propofol were investigated in two groups of five Scottish blackface sheep undergoing surgery for the implantation of subcutaneous tissue pouches. After premedication with acepromazine and papaveretum, anaesthesia was induced with either propofol at 4 mg kg-1 intravenously (group 1) or with a mixture of propofol at 3 mg kg-1 and ketamine at 1 mg kg-1 intravenously (group 2). Anaesthesia was maintained with a variable infusion rate of either propofol alone (group 1) or propofol and ketamine (group 2). Both regimens produced satisfactory conditions for superficial surgery of the body surface. The mean (SD) duration of anaesthesia was 64.8 (3.1) minutes for group 1 and 60 (0) minutes for group 2; the mean total dose of propofol given to the sheep in group 1 was 801 (84) mg, and the sheep in group 2 received 470 (46) mg of propofol and 267 (30) mg of ketamine. The mean elimination half-life of propofol was 56.6 (13.1) minutes in group 1 and 50.3 (21.4) minutes in group 2; the mean volume of distribution at steady state was 1.037 (0.480) litre kg-1 in group 1 and 1.515 (0.939) litre kg-1 in group 2; the mean body clearance was 85.4 (28.0) ml kg-1 min-1 in group 1 and 128.0 (35.0) ml kg-1 min-1 in group 2; the mean residence time corrected for a bolus injection was 12.1 (4.2) minutes in group 1 and 11.9 (6.6) minutes in group 2; for the infusion, the mean residence time was 72.1 (4.2) minutes in group 1 and 69.9 (7.9) minutes in group 2. There were wide variations in the blood propofol concentrations reached in individual sheep by using this standard dosing regimen. All the sheep recovered quickly from anaesthesia; the mean times to extubation, sternal recumbency and standing for the animals in group 1 were 2.8 (0.4), 6.3 (1.2) and 10.9 (1.6) minutes from the end of the infusion, and the times for group 2 were 5.3 (0.9), 11.2 (1.7) and 15.1 (2.2) minutes.

The medicinal use of opium and of morphine in different cultures and ancient civilizations is described. Research within the past 40 years have demonstrated the existence of brain opiate receptors. Morphine and related opioid analgetic interact at these sites in the nervous system to produce the characteristic pharmacological effects of these drugs. The opiate receptors have structural homologies with a variety of other cell membrane receptors; they activate second messenger-based chemical transduction systems in the cell membrane and are endowed with several regulation mechanisms. These opiate receptors are presumably activated under specific physiological conditions by endogenous ligands (opiopeptins). It is currently thought that morphine mimicks the opiopeptins by interacting with these receptors either at different molecular subsites or with a different mode of action.

Forty dogs undergoing a variety of surgical procedures were assigned randomly to one of two groups. All the animals were premedicated with acepromazine (0.05 mg/kg bodyweight) intramuscularly, and anaesthesia was induced with thiopentone sodium, or propofol in the case of lean animals, and maintained with halothane in an oxygen/nitrous oxide mixture using a non-rebreathing circuit. The dogs in group 1 were given papaveretum (0.2 mg/kg) slowly intravenously within 35 minutes of induction of anaesthesia and the dogs in group 2 were given carprofen (4 mg/kg) in the same way. The dogs were scored for sedation and pain by a trained theatre nurse, who did not know which group they belonged to, using a visual analogue scale, at 15, 30, 60, 120, 240 and 360 minutes after the halothane was switched off at the end of the procedure. Nine of the dogs were withdrawn from the trial (eight of them from the papaveretum group) because of inadequate pain relief and these animals were given pethidine (3 mg/kg intramuscularly) which produced adequate analgesia within 15 minutes in all but one case. Carprofen provided profound analgesia which was as effective and of longer duration than that produced by papaveretum, and was associated with significantly less postoperative sedation and a quicker return to the normal conscious state.

The transplacental transfer and the neonatal effects of atracurium 0.3 mg.kg-1 (ED95) were compared with those of d-tubocurarine at the usual clinical dose of 0.3 mg.kg-1 (ED90) in 46 patients undergoing elective Caesarean section. The atracurium group (25 patients) was similar to the d-tubocurarine group (21 patients) as far as age, parity and time intervals between precurarization, induction, skin incision, muscle relaxant administration, hysterotomy and birth. The transplacental transfer of atracurium was lower than that of d-tubocurarine, with a feto-maternal ratio of 9 +/- 3% for atracurium and 12 +/- 5% for d-tubocurarine (P less than 0.05). The transplacental transfer of laudanosine was low at 14 +/- 5%, with blood levels of 0.101 +/- 0.032 microM.L-1 in the umbilical vein. Newborns in the two groups were comparable in terms of Apgar scores at one, five and ten minutes, as well as for NACS scores (neurological and adaptive capacity scoring test) at two and 24 hours after birth. However, at 15 min after birth, only 55% of newborns in whom the mothers received atracurium had a normal NACS score (greater than or equal to 35/40) compared with 83% of newborns in whom the mothers received d-tubocurarine (P less than 0.05). Further analysis of the five variables related to active muscle tone revealed that the modal score for active extension of the neck of newborns from the atracurium group was lower than for newborns from the d-tubocurarine group (P less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)

Sixteen otherwise healthy women undergoing cholecystectomy were randomized to receive postoperative analgesia either by continuous infusion of papaveretum (n = 8), or by continuous interpleural infusion of bupivacaine (n = 8). Postoperative pain was assessed by linear analogue and ventilatory capacity. Changes in body protein were measured by in vivo neutron activation analysis. Clinical course was also noted. Pain scores were significantly lower in the interpleural group over the first 48 h (P less than 0.02). Ventilatory capacity was also significantly better for the first 24 h (P less than 0.025). There was no evidence of shortened postoperative ileus; hospital stay and postoperative fatigue were similar for the two groups. Weight and protein losses over a 2 week period were similar in the two groups. It is concluded that the apparent advantages in patient comfort and mobility offered by interpleural infusion are most marked in the first 48 h postoperatively, with an advantage in ventilatory capacity over the first 24 h.

Buprenorphine 0.3 mg and papaveretum 20 mg, both combined with hyoscine 0.4 mg, were used as premedicants in female patients undergoing laparoscopy or abdominal hysterectomy. The effects were compared. It was found that the increase in drowsiness and tranquility was greater following buprenorphine than that following papaveretum. A low frequency of nausea was reported in the buprenorphine-hyoscine group of patients who had undergone hysterectomy. The analgesic effects of the drugs, in these doses, appeared to be similar in degree and duration.

Forty-four patients scheduled for routine gynaecological surgery through a Pfannenstiel incision were given either nalbuphine or papaveretum as premedication, with hyoscine. Respiratory depression was measured by carbon dioxide rebreathing before and one hour after premedication. Both combinations produced significant respiratory depression as measured by the rebreathing test but no significant difference could be shown between the drugs in this respect.

Midazolam, administered intramuscularly was compared with papaveretum and hyoscine for premedication in patients undergoing gynaecological surgery. Midazolam proved to be a satisfactory agent for premedication compared with papaveretum and hyoscine, producing a similar degree of sedation and anxiolysis, but causing significantly more anterograde amnesia.

The behaviour of in vitro strips from the human choledochoduodenal junction would appear to be related to the anatomical location of origin of the strip. Strips from the papillary region showed low tone and obvious spontaneous rhythmic contractions (0 X 5-6/min). Strips from the region of the inferior choledochal sphincter showed, in ten out of fifteen specimens, spontaneous myogenic tone and gave a relaxation or a biphasic response (relaxation followed by contraction) to electrical field stimulation (0 X 3 ms pulses at 10 Hz for 5 s). All strips from human choledochoduodenal junction are remarkably insensitive to a variety of gastrointestinal hormones and to opioid agents.

Memory tests were administered to 30 patients taking methadone hydrochloride and 31 taking levomethadyl acetate (levo-alpha-acetylmethadol, LAAM) both prior to treatment and after one and three months of continuous treatment. A group of nonopiate using matched control subjects was administered the tests at similar intervals. No statistically significant difference in test performance was found among these groups at any of the three sessions. The methadone and control groups also did not differ significantly in the frequency of subjective reports of decreased memory function. Previous reports of memory deflicits during long-term methadone administration may be a result of comparing methadone and control groups at a single point in time and assuming that prior to methadone maintenance the groups were equivalent.

Contractions evoked by electrical stimulation of isolated longitudinal muscle preparations of guinea pig ileum were inhibited by the addition of opioids in the order of morphine = methionine enkephalin greater than pentazocine pethidine. Incubation of the preparation in the medium containing opioids at 4 degrees C for 22 hr resulted in a tolerance to the inhibitory effect in morphine and pethidine but in the case of pentazocine and met-enkephalin tolerance did not develop under the conditions employed. The same treatment with morphine, pethidine and pentazocine resulted in the development of dependence as demonstrated by naloxone provoked contracture or increase in the height of contraction. Opiate and enkephalin receptors are known to be unevenly distributed in the ileum and a significant difference was also observed in the distribution patterns of both receptors. Distribution of the receptors did not parallel the effect of opioids, thereby indicating a multiplicity in receptors. However, under the conditions employed in the present experiments, our results reflect the in vivo effects of opioids, such as analgesic effect or tolerance and dependence liability, and the validity of this preparation for the evaluation of opioids was confirmed.

An anaesthetic technique suitable for military field anaesthesia was sought which would attenuate the psychic side effects of ketamine. Heavy premedication with 30 mg of papaveretum and induction of anaesthesia with Althesin were evaluated. A combination of the two lowered the incidence of side effects, but they still occurred frequently enough to pose problems. Ketamine sequelae are considered incompatible with the battlefield environment.

The effect of morphine, Tinct. opii, loperamide, pethidine and atropine on intestinal transit and the faecal and urinary excretion of water and electrolytes was studied in ponies. The rate of passage of a particulate marker was slowed by morphine, hastened then slowed by loperamide and Tinct. opii, and hastened by atropine. The liquid marker was slowed by Tinct. opii and hastened then slowed by the other drugs. Only loperamide decreased the faecal sodium excretion. This drug also decreased faecal water and weight; it appeared worthy of clinical trial in diarrhoea. Tinct. opii decreased by morphine, pethidine and atropine increased faecal water.