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PubMed1992

Discrimination of agonist-antagonist opioids in humans trained on a two-choice saline-hydromorphone discrimination.

The stimulus properties of four opioid agonist-antagonists were assessed in postaddict volunteers trained in a two-choice drug discrimination procedure to discriminate between the effects of i.m. saline and hydromorphone (3 mg/70 kg). Behavioral, subjective and physiological measures were concurrently collected. After training, generalization curves were determined for hydromorphone, pentazocine, butorphanol, nalbuphine and buprenorphine. In generalization testing, hydromorphone produced dose-related increases in hydromorphone-appropriate responses and in characteristic opioid agonist-like subjective effects measures. In general, each of the study drugs produced a profile of subjective and physiological effects similar to that reported in other human studies. These subjective indices showed the study drugs to be heterogeneous. However, in this two-choice drug discrimination procedure, they were discriminated as homogeneous (i.e., all were discriminated as hydromorphone-like). The present study also found that all test drugs were subjectively identified as being opiates, and all were subjectively rated as similar to the hydromorphone training condition. A previous three-choice discrimination was sensitive to the heterogeneity among these drugs on both the discrimination measures and subjective ratings of similarity to the hydromorphone training condition. Thus, the specific procedures of drug discrimination studies may have an effect on some subjective indices, although this interaction is not apparent for the majority of subjective effect measures. Also, the characterization of opioids in drug discrimination testing appears to depend upon the specific training subjects receive; this is most clear with discrimination measures, and to a more limited extent, with subjective measures.

Adult↗

PubMed1977

Further evaluation of the discriminative effects of morphine in the rat.

Rats were trained in a two-choice discrete trial avoidance paradigm to discriminate between saline and 3.0 mg/kg of morphine. Behavior was considered to be under stimulus ocntrol when the rats completed at least 90% of the trials in a 20-trial session on the morphine-appropriate choice lever after receiving morphine and when they completed at least 90% of the trials on the saline-appropriate choice lever after receiving saline. The discriminative effects of morphine, measured by responding on the morphine-appropriate lever, were then evaluated by determining the dose-response characteristics of representative narcotic analgesics, analgesics with mixed agonist and narcotic antagonist properties and nonopioid psychoactive drugs. Eight narcotic analgesics each produced dose-related responding on the morphine-appropriate lever. The relative potency for producing discriminative effects equivalent to those produced by 3.0 mg/kg of morphine ranged form etonitazene = 1000 x morphine to propoxyphene = 0.0175 x morphine. Of the narcotic antagonist analgesics tested, butorphanol and nalmexone produced discriminative effects equivalent to those of the morphine training dose whereas nalorphine, levallorphan, oxilorphan, nalbuphine and ketocyclazocine did not. The nonopioid psychoactive drugs, mescaline, ketamine, physostigmine and scopolamine, also failed to produce discriminative effect equivalent to those produced by 3.0 mg/kg of morphine. These results confirm and extend our previous findings that of those drugs which have also been evaluated in man, discriminative effects equivalent to the training dose of morphine are produced uniquely by narcotic analgesics and narcotic antagonists which produce morphine-like subjective effects. These results are compatible with the hypothesis that the properties of morphine which enable it to function as a discriminative stimulus in the rat are analogous to those responsible for producing subjective effects in man.

Analgesics↗

PubMed2004

Midazolam/ketamine induction and isoflurane maintenance of anaesthesia in a 2-month-old, hand-raised African buffalo (Syncerus caffer).

The use of a midazolam/ketamine combination for induction of anaesthesia in a 2-month-old, hand-raised buffalo calf (Syncerus caffer) is described to allow endotracheal intubation for the maintenance of anaesthesia with isoflurane and oxygen. Intraoperative complications were hypotension and hypothermia. For postoperative analgesia meloxicam and butorphanol was administered intramuscularly.

Anesthetics, Combined↗

PubMed2006

Technique for performance and evaluation of parapharyngeal hypophysectomy in mice.

Mice at our institution were hypophysectomized to evaluate the effects of growth hormone on the expression of a transfected human factor IX gene. The hypophysectomy was performed in-house by using a parapharyngeal approach modified from previously published surgical techniques. Modifications included: 1) choice of ketamine-xylazine and isoflurane for anesthesia, with butorphanol for postoperative analgesia; 2) use of a V-trough for positioning mice correctly and consistently; 3) selection of increasing sizes of dental burrs to create a foramen in the cranial base through which the pituitary gland was removed; and 4) disuse of a tracheotomy for airway patency. In addition, verification of successful gland removal was assessed by measuring major urinary protein (MUP) in the urine; presence of MUP indicated incomplete hypophysectomy. This assessment enabled antemortem determination of surgical success by using a single urine collection. Each of these modifications contributed to the success of the surgical procedure. We had a safe and reliable anesthetic regimen, consistent positioning of the surgical patient, and smooth and rapid penetration of the cranium. In our experience, the tracheotomy described in previous techniques was unnecessary, as the mice tolerated brief periods of apnea (approximately 5 sec maximum) while the trachea was retracted. Here we seek to provide details that will assist those interested in learning this technique and that will reduce the number of mice needed for practice. Other applications include a method of evaluating the production of growth hormone without euthanizing the animal.

Anesthesia↗

PubMed1991

Increased analgesic potency of mu agonists after continuous naloxone infusion in rats.

Chronic opioid antagonist administration increases opioid binding sites and potentiates behavioral responses to morphine. The present study was designed to examine in rats the temporal and dosage parameters of naloxone-induced potentiation of morphine analgesia and the effect of continuous infusion of naloxone on the analgesic potency of other mu agonists. Cumulative dose-response curves were generated in a tail-flick procedure for each drug tested. Naloxone-filled osmotic pumps were then implanted s.c. for 1 week after which the rats were retested with the agonist. The potency ratio of morphine (ED50 before naloxone/ED50 after naloxone) showed orderly increases over a range of naloxone doses (0.03-1.0 mg/kg/hr) and increased, then decreased, over a range of time points (6-72 hr) after removal of the osmotic pumps. The relative potency of morphine was 2.1 at 24 hr after a 7-day infusion of 0.3 mg/kg/hr of naloxone. These parameters were then used in tests of other mu agonists. Five drugs produced maximum increases in tail-flick latencies before naloxone. Of these, naloxone increased the analgesic potency of fentanyl, methadone and levorphanol (relative potencies ranged from 1.7-2.1) but not of etorphine and propoxyphene. The naloxone infusion increased the maximum analgesic effect of meperidine, profadol and pentazocine, but had no effect on the analgesic activity of buprenorphine, butorphanol, ethylketocyclazocine and nalbuphine. Our results demonstrate that 7-day naloxone infusion increases the analgesic potency of some, but not all, opioids with mu agonist activity.

Analgesia↗

PubMed2006

Development of a technique for serial bilateral renal biopsy in steers.

A biopsy procedure was developed to provide serial kidney samples from standing steers. Ten clinically normal steers were given intramuscular injections of gentamicin sulfate, 4 mg/kg body weight. Renal biopsy was performed at 5 separate times. After feed was withheld for 24 h, laparoscopic surgery was performed in standing stocks. Acepromazine, xylazine, and butorphanol were used for sedation and analgesia, and 2% lidocaine was used for local anesthesia. Two incisions approximately 2 cm long were made in the paralumbar fossa to allow for trocar introduction. The abdomen was insufflated with CO2 and, with endoscopic guidance, a biopsy forceps used to remove a kidney sample 2 to 3 mm in diameter, by either a left or a right abdominal approach. Each operation was recorded on videotape, and images were also captured with a digital medical device system. Respiration, heart rate, temperature, appetite, attitude, and postural positions were evaluated at 12, 24, 48, and 72 h after surgery. The 51 laparoscopic procedures provided 48 renal samples (approximately 100 mg each). The 1st and 2nd samples were from the right kidney, and the 3rd sample was from either the left or the right kidney; the 4th and 5th samples were from the left kidney. Adhesions made an approach from the right side difficult for the 3rd sample. No clinical changes were observed in 9 steers after the procedure. One steer died after the 3rd procedure owing to hemorrhage.

Anesthesia, Local↗

PubMed2006

Perioperative use of analgesics in dogs and cats by Canadian veterinarians in 2001.

A random sample of 652 Canadian veterinarians was surveyed to determine perioperative use of analgesics in dogs and cats following common surgeries. The response rate was 57.8%. With the exception of taildocking in puppies, at least 85% of animals received preincisional analgesics, and 30% to 98.1% received postincisional analgesics. A similar survey was conducted in 1994; since then, analgesic usage has increased markedly, as have ratings of the pain caused by different surgeries. In 2001 most veterinarians (62%) used at least 2 classes of analgesic perioperatively. However, strong opioids, local anesthetics, and alpha-2 agonists were underused, and there was an overreliance on weak opioids (butorphanol, meperidine). Up to 12% of veterinarians did not use any analgesics. Nationally, this may have affected many animals monthly; for example, approximately 6000 dogs or cats undergoing ovariohysterectomy. Continuing education (provincial level) and review articles were considered effective ways to inform veterinarians about optimal analgesic practices.

Analgesics↗

PubMed1991

Prevention of sudden coronary death.

The following results were obtained in an experimental study in the dogs in general pentobarbital anaesthesia: Lidocaine type antiarrhythmics (lidocaine, Xylocaine ASTRA, Ethmozin USSR) administered shortly before artery ligation have a pro-fibrillation effect. This effect is indirectly proportional to the ischaemic focus development. A 3rd-generation beta blocker with intrinsic sympathetic activity (celiprolol, Selectol Chemie-Linz) had the same electrostabilizing effect on the ventricles in the acute phase of ischaemia as a 1st-generation beta blocker (metipranolol, Trimepranol SPOFA). The 3rd-generation blocker, however, stopped short of provoking a drop in the heart rate invariably associated with the 1st-generation beta blocker. The analgesic fentanyl (G. Richter) in combination with benzodiazepine (m,idazolam, Dormicum Hoffmann-La Roche) inducs analgosedation. In this way the dose of the analgetic can be reduced and yet the analgesia and electrostability of the heart remain the same. Due to the lower dose of the analgesic there is a lesser decrease in the heart rate and blood pressure. Analgosedation can be discontinued by administering an antagonist-agonist of benzodiazepines (flumazenil, Anexate Hoffmann-La Roche) or an antagonist of potent analgesics (butorphanol, Beforal SPOFA) without the risk of eliminating, at the same time, the electrostabilizing effect of analgosedation on the ischaemically damaged ventricles of the heart. For the prevention of sudden coronary death due to ventricular fibrillation in the acute phase of local myocardial ischaemia we can, on the basis of our experimental results, recommend analgosedation and the use of beta blockers with intristic sympathetic action. The use of lidocaine antiarrhythmics may lead to a reduction in the electric stability of the heart ventricles the ischaemic focus is developing under a certain "critical" blood level of the antiarrhythmics.

Adrenergic beta-Antagonists↗

PubMed1991

Opiate receptors and analgesia: an update.

Opiates remain the choice of analgesia for severe pain despite numerous side effects. They possess the unique ability to alter the interpretation of noxious sensations normally sensed as pain, while leaving the sensations of touch, temperature, and proprioception essentially unchanged. Opiates act by mimicking naturally occurring endogenous peptides at a variety of receptors in the central nervous system (CNS). Disruption of pain sensation occurs because of the action of different opiate receptor types located along pain pathways in the CNS. Analgesic activity and adverse side effects of all narcotic analogs are directly related to the activity of the drugs at a combination of opiate receptors. The currently known opiate receptors (mu 1, mu 2, kappa, sigma, and delta) are described with respect to function and location along pain pathways. A brief description of nociceptive (pain) pathway anatomy is also presented. Application of knowledge has allowed the development of mixed agonist-antagonist drugs such as butorphanol (Stadol; Anaquest, Madison, WI/Bristol Meyers Squibb, Evansville, IN) that capitalize on specific opiate receptor activation or antagonism to decrease adverse side effects and abuse-dependence potential. Future research areas are discussed.

Classification↗

PubMed1991

[Prevention of hypertension at intubation with intravenous nicardipine].

We administered a calcium channel blocker, nicardipine 0.01 mg.kg-1 i. v. bolus or 5 micrograms.kg-1.min-1 i. v. infusion before induction with thiamylal or modified NLA (thiamylal, droperidol and butorphanol) to prevent hypertension at intratracheal intubation, and measured blood pressure and heart rate before and after intubation. Blood pressure of all experimental groups was significantly reduced in comparison with the control group right after intubated. Nicardipine is effective to prevent hypertension at intubation.

Adult↗

PubMed1991

[The effect of extradurally administered analgesics on somatosensory evoked eyelid microvibration in rabbits].

We examined the effect of various analgesics administered lumboextradurally or intravenously on acceleration of the eyelid microvibration (EMV) due to reflex contraction which was evoked by electrical stimulation of the sciatic and ulnar nerve in rabbits. No significant difference in the inhibition of EMV was observed initially between the sciatic nerve and the ulnar nerve stimulated group after 2 mg of morphine, administered either extradurally or intravenously. However, greater inhibition of EMV by the extradural morphine than by intravenous administration of this drug was observed after 10 min in sciatic nerve stimulated and after 20 min in the ulnar nerve stimulated group. With the extradural administration of 0.05 mg fentanyl, EMV was inhibited more significantly in the sciatic stimulated group than in the ulnar nerve stimulated group. Intravenous administration of this drug failed to reveal any change in either sciatic nerve stimulated or ulnar nerve stimulated group. When butorphanol 0.5 mg or buprenorphine 0.05 mg was administered, no significant difference in the inhibition of EMV was observed between the drugs, regardless of the routes of administration or sites of stimulation. Extradural administration of ketamine 0.5 mg showed none of the inhibition of EMV in both the sciatic nerve stimulated, and the ulnar nerve stimulated groups. These results indicate that various analgesics administered into the extradural space produced characteristic actions depending on the pharmacokinetic properties of each drug, locally and/or generally. In conclusion, monitoring of EMV can be a useful procedure for evaluation of the effect of analgesics.

Analgesia, Epidural↗

PubMed1991

[Effects of epidural clonidine added to lidocaine solution upon the requirements of sedatives during epidural anesthesia].

The authors studied 34 patients undergoing abdominal total hysterectomy in order to evaluate whether epidural clonidine added to lidocaine solution could alter the requirements of sedatives during epidural anesthesia. Patients were randomly assigned to one of four groups; 18 ml of 2% lidocaine with 1:200,000 clonidine (n = 6), 1:100,000 clonidine (n = 7), 1:200,000 epinephrine (n = 13), or neither (plain, n = 8). The requirements of sedatives (diazepam, thiamylal) and analgesic (butorphanol) prior to the second epidural injection were compared among the four groups. The dose of intravenous diazepam or thiamylal required for sedation in the patients receiving lidocaine with 1:100,000 clonidine had a tendency to be smaller as compared with those in other three groups. There was a significant difference (P less than 0.05) in the requirement of diazepam between the patients given lidocaine with 1:100,000 clonidine and those given plain lidocaine. The present results suggest that the addition of clonidine to lidocaine solution could reduce the requirements of sedatives in epidural anesthesia.

Adult↗

PubMed1989

Discriminative stimulus effects of naltrexone in morphine-treated rhesus monkeys.

Three adult, female rhesus monkeys responded under a fixed-ratio 5 schedule of stimulus-shock termination while discriminating between s.c. injections of saline and naltrexone (0.01 mg/kg). In addition, monkeys received daily injections of morphine (1.78 or 3.2 mg/kg) 3 hr before experimental sessions. With increasing doses of naltrexone monkeys switched in a dose-related manner from the saline to the naltrexone lever; complete generalization (greater than 80% responding on the naltrexone lever) occurred in all monkeys at doses of naltrexone larger than 0.0032 mg/kg. Doses of naltrexone that produced responding on the drug lever also produced effects typically observed during opioid withdrawal (e.g., miosis and salivation). Compounds with opioid mu antagonist effects under other conditions (e.g., nalorphine) substituted for naltrexone whereas a wide variety of opioid agonists (e.g., morphine, U-50,488 and butorphanol) as well as nonopioids (e.g., pentobarbital and ketamine) produced responding predominantly on the saline lever. Monkeys also switched to the naltrexone lever in a time-related manner after the daily injection of morphine with complete generalization occurring between 8 and 27 hr after morphine. Among a variety of opioid and nonopioid compounds, including drugs used in the treatment of opioid abuse (e.g., clonidine), only compounds with mu agonist actions under other conditions produced a switch in responding from the naltrexone to the saline lever in 27-hr morphine-abstinent monkeys. These results suggest single, daily injections of morphine are sufficient to produce dependence in rhesus monkeys and indicate further drug discrimination studies in morphine-treated rhesus monkeys might be pharmacologically more specific than observational procedures.

Animals↗

PubMed1989

[Kappa-type opioid receptor in human placental membrane].

Since many opioid receptor preparations are heterogeneous systems containing multiple types of receptor, characterization of each type of the receptor is influenced by contamination with other types of receptor. Demonstrating kappa receptor proved more difficult owing to the ability of kappa ligands to interact with a number of receptor classes and to the lack of the homogeneous preparation. It has been reported that kappa ligands selectively bind to human placental membrane. To establish homogeneous kappa receptor preparation, the kappa binding to human placenta was characterized. The portion which was predominantly villus tissue was removed from freshly collected placenta, and the P3-membrane fraction was prepared. Kappa opioid agonist, such as 3H-Dynorphin A, 3H-ethylketocyclazocine and 3H-U-69593, bound to the human placental membrane fraction in a manner of single class of binding site (Bmax: approximately 40 fmol.mg-1 protein). In contrast, 3H-dihydromorphine, 3H-DAGO (mu agonist), 3H-DADLE (delta agonist) or 3H-SKF-10047 (sigma agonist) showed no binding activity. The specific binding of 3H-diprenorphine was displaced only by kappa-selective ligand (U-50488H, dynorphin, butorphanol). These results suggest that opioid binding in human placental membrane is specific for kappa opioid.

Humans↗

PubMed1989

[Perioperative management of patients with dilated cardiomyopathy].

Dilated cardiomyopathy (DCM) is defined as a syndrome of dilated ventricles with gross impairment of ventricular systolic function. However, few reports on perioperative management of DCM were obtainable. This paper describes perioperative management of two patients with DCM. A 72-year-old man, whose DCM had been treated with medication, was planned for gastrectomy. His cardiac signs indicated NYHA class II. Cardiac function, evaluated prior to the surgery with echocardiography to determine an operative indication, turned out to be well compensated. Minimal cardiac derangements were anticipated perioperatively. The procedure was carried out under general anesthesia with neuroleptanalgesia utilizing butorphanol and vasoactive agents. No circulatory complications were observed throughout the surgery. A 66-year-old man, who had long-standing heart disease, hemiplegia and hydronephrosis due to ureteral stone, was planned for percutaneous nephrolithotomy. However, the planned surgery was withdrawn because he had DCM with minimal compensatory function and perioperative cardiac derangements were anticipated according to the categorized data classified with echocardiography. We conclude that preoperative assessment of cardiac function is essential to minimize perioperative cardiac derangements in patients with DCM.

Aged↗

PubMed1985

Further demonstration of kappa opioid binding sites in the brain: evidence for heterogeneity.

By selectively blocking cross-interferences from other types of binding sites, a binding site which likely represents kappa opioid binding sites was obtained in the guinea-pig brain suspension of the particulate fraction. Selective ligands for mu, sigma, delta and epsilon opioid binding sites were poor inhibitors for inhibiting [3H]ethylketocyclazocine binding to this site, whereas kappa opioids like oxilorphan, dynorphin(1-13), ethylketocyclazocine, butorphanol, cyclazocine, ketocyclazocine, tifluadom, nalorphine, pentazocine, U-50-488, nalbuphine and naloxone were potent ligands. Buprenorphine, generally believed to be a mu opiate, was the most potent inhibitor at the kappa site. Scatchard analysis of the saturation curve of [3H]ethylketocyclazocine binding revealed two subtypes of kappa binding sites: a high-affinity site and a low-affinity site with Kd = 0.7 and 78 nM and maximum binding = 22 and 101 fmol/mg of protein, respectively. Analysis of the inhibition curves suggested that tifluadom may be a selective ligand for the high-affinity site and that dynorphin(1-13) and U-50-488 may bind preferentially the high-affinity site but still possess appreciable affinity for the low-affinity site. This study demonstrates a selective assay for kappa opioid binding sites and indicates a possibility of the heterogeneity of kappa opioid binding sites in the brain.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗

PubMed1986

Antinociceptive profiles of mu and kappa opioid agonists in a rat tooth pulp stimulation procedure.

The purpose of the study was to develop a tooth pulp stimulation procedure in the awake, freely moving rat and to then quantitatively assess the analgesic effects of compounds reported to act on mu and/or kappa receptors. The mu receptor agonists produce a biphasic (primary and secondary slope) dose-response curve (DRC) whereas kappa agonist and mixed agonist/antagonist analgesics produce single-slope DRCs. The primary slopes calculated from the mu agonist biphasic DRC are steeper than the slopes calculated for the other types of opioid analgesics. The rank order of analgesic potency for the mu agonist analgesics is oxymorphone greater than morphine = methadone greater than meperidine. The rank order analgesic potency for the kappa agonist analgesics is tifluadom greater than ethylketocyclazocine greater than U50488H and for the mixed agonist/antagonist analgesics, butorphanol greater than nalbuphine greater than pentazocine. The nonsteroidal anti-inflammatory drugs, aspirin and zomepirac, are also effective analgesics in this test procedure; but the DRC slopes for these compounds are lower than all opioid analgesics tested. The opioid antagonist naloxone produces no significant changes in threshold responses. Naloxone did reverse the threshold increases produced by morphine and ethylketocyclazocine but not aspirin. This study demonstrates that the electrical stimulation of the tooth pulp in the rat can be used as an assay for evaluation of opioid and nonopioid analgesics. When minimal effective dose values of each analgesic are plotted as a function of the clinical analgesic dose a high correlation is observed.

Analgesics↗

PubMed1989

Tourniquet-induced hypertension in a horse.

Arterial hypertension developed in a horse anesthetized for arthroscopy and lavage of an inflamed right carpal joint. Anesthesia was induced with xylazine HCl, butorphanol, guaifenesin, and thiamylal Na and was maintained with halothane in oxygen. Arterial hypertension and tachycardia developed within 15 minutes after a pneumatic tourniquet was placed 8 to 10 cm proximal to the right carpus and inflated to 800 mm of Hg. The surgical procedure was expedited, halothane was discontinued and anesthesia was maintained with guaifenesin to facilitate bandaging. Heart rate decreased from 72 to 42 beats/min after the tourniquet cuff was deflated. Mean arterial pressure decreased from 260 mm of Hg to 128 mm of Hg. Differential diagnosis for a rapidly increasing arterial pressure during halothane anesthesia include inadequate plane of anesthesia, signs of pain, hypercapnia, hypoxemia, and/or hyperthermia.

Anesthesia↗