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PubMed1995

[Treatment of postoperative pain with peridural administration of opioids].

The advantages and disadvantages associated with epidural opioids require careful selection of the opioid and its dose regimen. There is no ideal opioid available for epidural use. Comparative pharmacokinetic data help selection of the appropriate epidural opioid. Morphine (provided it is given in small doses and volumes) is very appropriate for epidural pain treatment, especially for longer periods of treatment, due to the excellent analgesia and very low systemic morphine concentrations. The faster onset of analgesia makes the epidural application of pethidine, alfentanil and fentanyl recommendable. However, due to the increased risk of respiratory depression during continuous treatment, these opioids should not be given over longer treatment periods. Epidural administration of methadon, sufentanil and buprenorphine cannot be recommended since the advantages over systemic use do not outweigh the risks. Epidural tramadol is useful in clinical routine if opioids are not available and supervision of the patient is not guaranteed, because the opioid is not restricted by law and has a low potential for central depressive effects. Nalbuphine and butorphanol should not be selected for epidural use until the benefit/risk ratio is defined. The safety of patients is paramount. If patients are harmed by inappropriate opioids or dose regimens, this will unjustly discredit a valuable treatment of postoperative pain.

Analgesia, Epidural↗
PubMed1996

Discriminative stimulus effects of nalbuphine in rhesus monkeys.

Three rhesus monkeys discriminated between 0.178 mg/kg of nalbuphine and saline while responding under a fixed-ratio 5 schedule of stimulus-shock termination. Nalbuphine produced dose-related increases in drug-lever responding with > or = 90% of responses occurring on the drug lever at doses larger than 0.1 mg/kg. The duration of action of the discriminative stimulus effects of nalbuphine was less than 5.25 hr. Rank order potency of compounds that substituted for the nalbuphine discriminative stimulus (i.e., > or = 90% responding on the nalbuphine lever) in all three subjects was fentanyl > butorphanol > methadone > morphine. Compounds that did not substitute completely in all monkeys included the kappa agonists ethylketocyclazocine, enadoline, spiradoline and U-50,488 and the nonopioids cocaine, d-amphetamine, clonidine, ketamine and phencyclidine. Naltrexone antagonized the discriminative stimulus effects of nalbuphine, shifting the nalbuphine dose-effect curve in a manner that was consistent with mu receptor mediation. Results from the current study demonstrate that, in rhesus monkeys, the discriminative stimulus effects of nalbuphine are mediated by mu opioid receptors. Although there is evidence suggesting that nalbuphine has kappa agonist effects (e.g., subjective effects in humans), results from several studies, including the current study, strongly suggest that in rhesus monkeys nalbuphine does not exert agonist actions at kappa receptors. Moreover, these data indicate that differences in behavioral effects between nalbuphine and prototypic mu opioids (e.g., morphine) probably result from differences in activity (e.g., efficacy) at mu receptors rather than any kappa agonist actions of nalbuphine.

Analgesics, Opioid↗
PubMedDate not supplied

[Effect of morphine derivatives on the function of glucocorticoid receptors in shock].

The effects of opiate receptor agonists and antagonists on the function of glucocorticoid receptors in the hepatic cytosol were examined in male Wistar rats weighing 180-240 g. With the Scatchard analysis, in vitro experiments by using labelled ligands revealed that the pure opiate agonist morphine in the wide range of concentrations (0,01-10,0 mM) failed to affect the function Type II glucocorticoid receptors, though inhibited the function of Type III glucocorticoid receptors in the dose-dependent manner. Buprenorphine and diprenorphine depressed the function of Types II and III glucocorticoid receptors. Buterphanol, an opiate receptor antagonist-agonist, like naltrexone, an opiate receptor antagonist, decreased the function of Type III glucocorticoid receptors, but modulated that of Type II glucocorticoid receptors by lowering the association constant of the ligand-Type II glucocorticoid receptor complex, but by enhancing the density of Type II glucocorticoid receptors. In vivo studies established that butorphanol dose-dependently increased the density of Type II glucocorticoid receptors in the hepatic cytosol and elevating blood pressure in rat traumatic shock. Whether glucocorticoid receptors involve in the mechanism of the antishock effect of morphine derivatives is discussed in the paper.

Animals↗
PubMed1996

Determination of the lifespan of erythrocytes from greyhounds, using an in vitro biotinylation technique.

OBJECTIVE: To determine the RBC lifespan of Greyhounds, using an in vitro labeling technique. DESIGN: RBC from dogs were labeled with NHS-biotin and their disappearance measured over time to determine RBC lifespan. SAMPLE POPULATION: 5 Greyhounds that had been vaccinated against distemper, adenovirus 1 and 2 infections, parainfluenza, leptospirosis, parvovirus, and coronavirus infections, Bordetella bronchiseptica infection, and rabies the previous year; 3 sexually intact 14-month-old Beagles served as controls. PROCEDURE: After venipuncture for CBC, catheters were inserted in the cephalic vein of each dog. Butorphanol was then administered to achieve mild sedation and analgesia, and glycopyrrolate was administered to ensure maintenance of adequate heart rate during phlebotomy. Dogs were positioned in lateral recumbency; blood was removed via jugular venipuncture, using a standard laboratory donor blood bag containing citrate-phosphate-dextrose solution. Blood was transferred aseptically into sterile polystyrene containers and NHS-biotin was added. After incubation, the labeled RBC were reinfused into the dogs and the blood was allowed to recirculate for 1 hour before the first postinfusion sample was taken. At frequent intervals, blood to be analyzed was taken by jugular venipuncture, and the percentage of labeled cells was determined by flow cytometry. RESULTS: The mean RBC lifespan of non-Greyhounds was significantly longer than that of Greyhounds (104.3 +/- 2.2 days vs 53.6 +/- 6.5 days; P = 0.001). A negative linear correlation was also found between age of the Greyhounds and their RBC lifespan (P = 0.01, R2 = 0.91). CONCLUSIONS: The shorter RBC lifespan of the Greyhounds may explain the finding of macrocytosis reported in earlier work. The reason for the shorter RBC lifespan in Greyhounds may be caused by differences in Greyhound RBC membrane structure or accelerated RBC removal from the circulation.

Animals↗
PubMed1996

Evaluation of a survey of the diplomates of the American College of Laboratory Animal Medicine on use of analgesic agents in animals used in biomedical research.

OBJECTIVE: To determine the analgesic agents administered to animals frequently used in biomedical research. DESIGN: Telephone survey. SAMPLE POPULATION: Diplomates of the American College of Laboratory Animal Medicine. PROCEDURE: 200 of 429 active diplomates listed in the 1993 directory of the American College of Laboratory Animal Medicine were selected at random for telephone interviews. Diplomates were asked to identify the species that they cared for and the dosages, dosing intervals, and routes of administration for analgesic agents. RESULTS: 90 of 200 (45%) diplomates completed the survey. Twenty-two analgesic agents were identified for use in 472 applications in 16 species. Opioid analgesics were the most frequently selected agents, with buprenorphine hydrochloride and butorphanol being most frequently used. Intramuscular and subcutaneous routes of administration were used most frequently. CLINICAL IMPLICATIONS: Among diplomates of the American College of Laboratory Animal Medicine, opioids are the most frequently selected agents used to induce analgesia in animals used in biomedical research. Dosages and dosing intervals used vary widely among animals of various species as well as for animals in each species.

Analgesics↗
PubMed1996

Characterization of opioid agonist efficacy in a C6 glioma cell line expressing the mu opioid receptor.

In C6 glioma cells stably expressing a homogeneous population of the cloned rat mu opioid receptor, the binding affinities of opioid agonists and subsequent activation of G protein were examined. Opioid receptor number in membranes of these cells was high (10-30 pmol/mg protein [3H]diprenorphine binding sites). Opioids were found to bind to the receptor with high affinity [Tyr-D-Ala-Gly-(Me)Phe-Gly-ol (DAMGO) 0.23 nM; sufentanil 0.034 nM; morphine 0.16 nM]. Activation of G protein by opioid agonists was examined by measuring the stimulation of guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTP gamma S) binding. Sufentanil increased [35S]GTP gamma S binding by 326% with an EC50 value of 2.39 nM. Agonist stimulation of [35S]GTP gamma S binding was stereoselective, naltrexone-reversible, and pertussis toxin-sensitive. The "intrinsic activity" of opioids at the mu receptor was reflected by the magnitude of agonist-mediated activation of G protein. The rank order of the stimulation of [35S]GTP gamma S binding was etonitazene = sufentanil = DAMGO = PLO17 = fentanyl > morphine > profadol > meperidine > butorphanol = nalbuphine = pentazocine > cyclazocine = nalorphine > levallorphan > naltrexone. High affinity binding of ligands to the mu opioid receptor was reduced by the addition of sodium and guanosine diphosphate at concentrations used in the [35S]GTP gamma S binding assay. Ligand affinity was reduced in a manner correlating with "intrinsic activity". DAMGO, 1229-fold, nalbuphine 35-fold, naltrexone, 3-fold. The results presented show that the stable expression of the rat mu opioid receptor in C6 cells provides an effective tool to examine opioid receptor signal transduction mechanisms and evaluate the activity of novel opioids at the mu receptor.

Animals↗
PubMed1996

Postoperative use of analgesics in dogs and cats by Canadian veterinarians.

Four hundred and seventeen Canadian veterinarians were surveyed to determine their postoperative use of analgesics in dogs and cats following 6 surgical procedures, and to determine their opinions toward pain perception and perceived complications associated with the postoperative use of potent opioid analgesics. Three hundred and seventeen (76%) returned the questionnaire. The percentage of animals receiving analgesics postoperatively ranged from 84% of dogs and 70% of cats following orthopedic surgery to 10% of dogs and 9% of cats following castration. In general, with the exception of orthopedic surgery, roughly equal percentages of dogs and cats received postoperative analgesics. Opioids were used almost exclusively to provide postoperative analgesia, with butorphanol the most commonly administered drug to both dogs and cats. Analgesics were usually administered either once or twice postoperatively. With regard to the administration of potent opioid agonists, the 3 major concerns included respiratory depression, bradycardia, and sedation in dogs, and excitement, respiratory depression, and bradycardia in cats. Seventy-seven percent of veterinarians considered their knowledge of issues related to the recognition and control of postoperative pain to be inadequate. Experience in practice is currently the major source of knowledge, with undergraduate veterinary school and research articles in journals ranked as the least important sources. Lectures or seminars delivered at the regional level were the preferred format for continuing education.

Analgesics↗
PubMedDate not supplied

[The problem of opioid tolerance and dependence during clinical use thereof].

Presents a clinician's viewpoint on the tolerance of and dependence on opiates and opioids in total anesthesia and management of acute (postoperative) and chronic (cancer) pain. Clinical observations are assessed with due consideration for the theoretical (pharmacological) studies. The author analyzes prolonged therapy with different opiates and opioids and the short-term use in massive doses at different stages of surgery. Tolerance to morphine rapidly forms during therapy of chronic pain, and the narcotic doses have to be progressively increased. Tolerance to opioids, such as tramal and buprenorphine, is less expressed. These agents are less hazardous as regards drug dependence, which was proven for tramal by the naloxone test. Clinical manifestations of physical dependence on opiates at different stages of surgical treatment are discussed for the first time. The main last-generation opiates are characterized (tramal, buprenorphine, nalbufin, butorphanol, prosidol) by their capacity to cause physical and mental dependence. The author emphasizes the importance of a proper selection of opiates, opioids, and combinations thereof with the optimal nonopiate components in general anesthesia, postoperative analgesia, and treatment of chronic pain in order to improve the efficacy and narcological safety of analgesia.

Acute Disease↗
PubMed1997

Ventilation in morphine-maintained rhesus monkeys. II: Tolerance to the antinociceptive but not the ventilatory effects of morphine.

The antinociceptive and ventilatory effects of morphine and other opioid agonists were determined in three rhesus monkeys during a period of morphine maintenance, as well as before and after the chronic exposure to morphine. Before the onset of the daily dosing regimen, morphine increased tail-withdrawal latencies from 50 degrees C water, with an ED50 of 6.4 +/- 2.1 mg/kg. Daily injection of 3.2 mg/kg morphine produced a rightward displacement of the morphine dose-response curve, increasing the ED50 of morphine to 28.4 +/- 12.3 mg/kg. Doubling the daily morphine dose to 6.4 mg/kg resulted in a further shift to the right of the dose-response curve of morphine. After cessation of the daily dosing regimen, the morphine dose-response curve for producing antinociceptive effects returned toward baseline. The antinociceptive effects of the kappa opioid agonist, ethylketazocine, were similar during the period of daily exposure to morphine, and after cessation of the daily dosing regimen. Before the onset of the daily dosing regimen, morphine, ethylketazocine, fentanyl, butorphanol and nalbuphine decreased ventilation in the presence of air or air mixed with CO2. The baseline ED50 value of morphine for decreasing minute volume in the presence of 5% CO2 was 2.9 +/- 0.8 mg/kg. The ventilatory effects of morphine and other mu opioid agonists tested were not attenuated during the daily morphine-dosing regimen. After 40 weeks of daily injections of 3.2 mg/kg morphine, the ED50 of morphine for decreasing minute volume in 5% CO2 was 2.3 +/- 1.0 mg/kg, and when the daily dose was doubled to 6.4 mg/kg morphine, the ED50 of morphine was 1.5 +/- 0.5 mg/kg. The ventilatory depressant effects of the daily injection 3.2 mg/kg morphine were also unchanged during morphine maintenance. The differential development of tolerance to the antinociceptive and ventilatory effects of morphine demonstrates a separation of these two mu opioid agonist effects in rhesus monkeys.

Analgesics, Opioid↗
PubMed1997

Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists.

The purpose of this investigation was to evaluate the discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine. In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine). (-)-N-allylnormetazocine and (+)-propoxyphene substituted partially for the dezocine stimulus, an effect obtained even when tested up to doses that suppressed responding. Naloxone (0.1 - 10 mg/kg) antagonized the stimulus effects of dezocine, (+)-propoxyphene and fentanyl in a dose-related manner, whereas doses of naloxone that antagonized fentanyl's rate-decreasing effects failed to antagonize the rate-decreasing effects of dezocine and (+)-propoxyphene. A 10-mg/kg dose of the mu-selective, noncompetitive antagonist beta-funaltrexamine was more effective against the stimulus effects of dezocine and nalbuphine than against morphine and fentanyl. As was observed with naloxone, beta-funaltrexamine failed to antagonize dezocine's rate-decreasing effects. The delta agonists BW373U86 and SNC80 substituted partially for the dezocine stimulus, and these effects were reversed by doses of the delta-selective antagonist naltrindole (0.1 and 1.0 mg/kg) that had no effect on the dezocine stimulus. Naltrindole also antagonized the rate-decreasing effects produced by BW373U86 and SNC80, but not those of dezocine. The kappa agonists bremazocine, spiradoline, U50,488 and U69,593 failed to substitute for the dezocine stimulus. The kappa-selective antagonist norbinaltorphimine (1.0 mg/kg) failed to antagonize dezocine's stimulus or rate-decreasing effects. The present findings indicate that dezocine shares similar stimulus effects with both mu and delta agonists, its stimulus effects are reversed by mu-selective antagonists, and its rate-decreasing effects are not mediated by activity at mu, kappa or delta opioid receptors.

Analgesics, Opioid↗
PubMed1998

[Thoracic epidural analgesia in the postoperative period of pediatric surgery for the repair of pectus excavatum and pectus carinatum].

To assess thoracic analgesia by continuous infusion in surgery to repair pectus excavatum and carinatum in children. This prospective study enrolled 14 children aged 6 to 14 years old scheduled for surgery to correct pectus excavatum and carinatum. After induction of general anesthesia, the T8-T9 epidural space was accessed and a catheter was inserted to T3-T7 with radioscopic monitoring. A loading dose of 0.03-0.04 ml/kg per segment to be blocked (5 segments: T3-T8) of 0.125% bupivacaine and 3 micrograms/ml fentanyl was given to children under 7 years of age; a dose of 0.02-0.03 ml/kg per segment was administered to children over the age of 7 years. A continuous perfusion of 0.1-0.4 ml/kg/h was maintained, with the possibility of additional boluses of 1 ml at 20 min intervals during surgery and the first three days thereafter. An intraoperative bolus was given when the level of blockade was not reached or when mean blood pressure and heart rate increased 15% over baseline. Pain relief was assessed on a numerical scale of 0 to 5 or on a scale of facial icons, depending on the patient's age. During the postoperative period, the pediatric ICU nurse administered a bolus if pain was [symbol see text]3 or heart rate increased 75% over age-based reference values. Top-up analgesia was provided with Metamizole at a dose of 25 mg/kg. No complications attributable to the technique or to sympathetic blockade were observed. All tubes were removed in the operating room. The thoracic epidural catheter was left in place for 70.3 +/- 2.6 h. Mean initial doses of analgesia were 0.45 microgram/kg of fentanyl and 0.2 mg/kg of bupivacaine. The mean number of complementary boluses was 3 +/- 1 during surgery, 5 +/- 2 on the first postoperative day and 4 +/- 1 on the second day. No patient required top-up analgesia on the third day. Hemodynamic stability during surgery and the postoperative period was good. Analgesia was excellent (< 2) for 78.5% of the patients on the first day after surgery, for 85.7% on the second day and for all patients on the third day. We recorded one case of pruritus (7.1%), three of nausea (21.4%) that subsided when butorphanol was given epidurally (20 micrograms/kg), and two cases of light sedation. Thoracic epidural analgesia is effective for alleviating postoperative pain from corrective thoracic surgery in children. Side effects were minimal and no anesthetic complications were observed.

Adjuvants, Anesthesia↗
PubMed1998

[Actions of drugs affecting the cough reflex].

BACKGROUND AND AIM: Authors evaluated the part of some receptor systems in the antitussive activity of drugs. METHOD: The cough was induced by mechanical stimulation of the airways. Unanesthetized cats were used in this study. RESULTS: They followed: 1. statistically highly significant decrease of cough parameters after administration the drugs influencing the different types of opiate receptors--tramadol, tilidine, pentazocine, codeine and butorphanol. Every of these drugs were administered in a dose 10 mg/kg b.w. intraperitoneally, 2. the antitussive activity of codeine was decreased by pretreatment with naloxone only in part, 3. selective antagonist 5-HT2 receptors ketanserine (1 mg/kg b.w.) decreased antitussive effect of codeine by 10% and effect of tramadol by 20%, 4. the ability of codeine to reduce the cough parameters was unchanged after pretreatment with haloperidol (0.1 mg/kg b.w.), 5. whereas the pretreatment with reserpine decreased the cough-suppressing effect of codeine, 6. the application of gabaergic agent gabalid leads to the highly significant decrease the cough parameters. Results of these experiments showed that gaba-ergic mechanism might be involved in the mechanism of action of narcotic antitussives agents, 7. we showed, that inhibition of glutaminergic synaptic transmissions afferent impulses from cough receptors with dextromethorphan leads to suppressing cough reflex in cats. CONCLUSIONS: Antitussive activity of agents is not only mediated by means of mí opiate receptors. The results suggest, that gabaergic, serotoninergic systems and activity of NMDA receptors play an important role in the mechanism of action of antitussive drugs. Decrease in levels of brain monoamines modifies the cough-depressant effect of codeine. (Fig. 7, Ref. 23.)

Animals↗
PubMed2001

Noninvasive drug delivery.

Advances in biopharmaceutical technology have spawned new drug delivery devices and mechanisms. Noninvasive methods, including iontophoresis and transmucosal drug delivery, have improved treatment of certain patient population. Their use is discussed in the following paper.

Administration, Buccal↗
PubMed1983

Agonist/antagonist analgesics and nigrostriatal dopamine metabolism in the rat: evidence for receptor dualism.

Agonist/antagonist (Ag/Ant) analgesics possess bell-shaped dose-response curves with regard to nigrostriatal dopamine (DA) metabolism in the rat. Using local drug injections as well as parenteral drug, after acute hemisection, we have determined that this phenomenon is not the result of autoinhibition. Our data clearly indicate that the receptor population antagonizing the agonist actions of Ag/Ant is not localized within the striatum or substantia nigra. These results therefore present evidence for receptor dualism with Ag/Ant analgesics.

Animals↗
PubMed1990

Effects of the opiate antagonists diprenorphine and naloxone and of selected opiate agonists on feeding behavior in guinea pigs.

Opiate-sensitive feeding behavior has now been demonstrated in a number of species. We sought information on which opioid receptors might be involved in the observed feeding behaviors. Guinea pigs are known to have higher concentrations of the opioid kappa receptor than any other laboratory animal, so we compared the feeding suppressive potency of the general opiate antagonist, diprenorphine to that of the relatively more mu-specific antagonist, naloxone in that species. We found that diprenorphine was over twenty times more effective than naloxone in suppressing feeding in guinea pigs, suggesting the importance of receptors other than mu in feeding initiation in the guinea pig. Confirmatory evidence for the role of kappa receptors was sought, but not found, in comparisons of the effectiveness of different types of opiate agonists in promoting feeding in these animals. These agonists suppressed, rather than stimulated feeding. We conclude that no feeding stimulatory effects of opiates can be demonstrated in guinea pigs. This observation may indicate that opioids play little role in the natural regulation of feeding in this species or that opioids result in prolonged sedation during which the animals fail to eat. The greater feeding suppressive potency of diprenorphine, a general opiate antagonist, versus naloxone, a mu-preferential antagonist, indicates that to whatever extent opiates are involved in guinea pig feeding, the opiate effect is probably not a mu receptor effect.

Animals↗