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PubMed1979

4-Anilidopiperidine analgesics. 2. A study of the conformational aspects of the analgesic activity of the 4-anilidopiperidines utilizing isomeric N-substituted 3-(propananilido)nortropane analogues.

Relatively little information is available concerning the influence of conformational factors on the potent analgesic actions of the 4-anilidopiperidines. A series of N-substituted 3 alpha- and 3 beta-(propananilido)nortropanes have been designed, synthesized, and stereochemically characterized as semirigid analogues of the 4-anilidopiperidine analgesics in an attempt to study the influence of certain stereochemical factors on analgesia in this class of compounds. Conformational analysis of 3 alpha-propananilides (4) reveals a boat conformation for the preferred conformation of the piperidine ring of these tropane analogues. Evaluation of the analgesic potencies of the isomeric N-substituted 3-(propananilido)nortropanes of this study indicates greater potency for the 3 beta-(propananilido) isomers (5) with N-benzyl and N-phenethyl substitution as compared to the corresponding N-substituted 3 alpha-propananilides. Analysis of relative solubility differences among these isomers suggests that both structural and stereochemical influences predominate in affecting analgesic potency.

Analgesics↗
PubMed1990

Analgesic side effects and minor surgery: which analgesic for minor and day-case surgery?

A retrospective study was carried out to determine analgesic requirements in a group of orthopaedic outpatients (n = 145) and oral surgery inpatients (n = 172). The orthopaedic patients received a codeine-paracetamol premedication, an opioid during operation, or no analgesic. Less than 50% of the orthopaedic patients in these groups required any postoperative analgesia. However, there was a high incidence of vomiting (40%) in those receiving an opioid during operation, associated with overnight admission in more than 50% of those who vomited. In the patients undergoing oral surgery, ibuprofen administered before operation significantly reduced analgesic requirement, without unwanted side effects. The use of codeine-paracetamol or a non-steroidal anti-inflammatory agent before body surface surgery appeared to be advantageous in reducing postoperative analgesic needs, without causing problems associated with the stronger opioids.

Acetaminophen↗
PubMed1980

Analgesic and other pharmacological activities of a new narcotic antagonist analgesic (-)-1-(3-methyl-2-butenyl)-4-[2-(3-hydroxyphenyl)-1-phenylethyl]-piperazine and its enantiomorph in experimental animals.

Of 1-chclohexyl-4-[2-(3-hydroxyphenyl)-1-phenylethyl]piperazine (I) and its 1-(3-methyl-2-butenyl) derivative (II), the S(+)-isomers were analgesically more active than either their +(-)-isomers or their racemates, having 15 to 44 times the potency of morphine in mice and rats. R(-)-I had comparable analgesic activity to morphine R(-)-II to pentazocine in mice, rats and dogs and they were nearly equipotent with pentazocine in reversing some actions of morphine. The S(+)-isomers and racemates lacked this action. R(-)-II required about 10 times more naloxone to reverse its analgesic activity than was needed to antagonise the S(+)-isomers, morphine and pentazocine. The S(+)-isomers and racemates produce a typical Straub tail reaction and increased spontaneous locomotor activity in mice, but the R(-)-isomers did not. R(-)-II had no significant physical dependence liability in mice, rats and monkeys. From these results, it is suggested that the compounds show an uncommon steroselectivity in comparison with morphine and its surrogates, and that R(-)-II is worth investigating further as a narcotic antagonist analgesic.

Analgesics↗
PubMedDate not supplied

Analgesic pharmacology: II. Specific analgesics.

Methods of treatment are different for acute and chronic pain. For acute pain, analgesics such as nonsteroidal anti-inflammatory drugs and opiates are commonly used, sometimes combined with regional anesthesia, such as peripheral nerve block or peridural local anesthesia. The mechanism of transition from an acute to a chronic pain state is poorly understood. Only NMDA receptor antagonists and epidural morphine have shown relatively consistent results as preemptive analgesics. Agents more successfully used to manage chronic pain include those that modify the neurochemistry of the spinal cord dorsal horn, such as tricyclic antidepressants, anticonvulsants, gamma-amino butyric acid agonists, local anesthetic analogs, and NMDA antagonists. Opiates may be used chronically, but tolerance and lack of efficacy may then develop. In selected patients with refractory chronic pain, centrally administered analgesics may be considered, including opiates, dilute local anesthetic, NMDA receptor antagonists, clonidine, midazolam, baclofen, or calcium channel blockers. For both acute and chronic pain, a single agent may be less effective than combinations of analgesics with different mechanisms of action.

Acute Disease↗
PubMed1976

[Analgesic effects of Neurotropin in mice, and a comparison with analgesic effect of other drugs in SART-stressmice].

Analgesic effects of a neuroleptica "Neurotropin" (NSP) were studied in mice while the analgesic effects of other agents were studied in SART-stress mice (specific stress caused by alterating rhythm in temperature) and the results compared with those in normal mice. NSP is an extract containing many conjugated polysaccarides isolated from the skin or tissues of rabbits which had been inoculated with the living cowpox virus. (a) NSP given alone to normal mice resulted in slight analgesic effects as observed with the application of the acetic acid-, phenylquinon-writhing method or the modified Randall-Selitto method. Little effect was seen when the D'Amour-Smith was used. (b) Synergism was evident when NSP and aminopyrine or NSP and morphine were given concomitantly and the acetic acid- or phenylquinon-writhing methods were applied. (c) Analgesic effects of morphine, levomepromazine, imidazole acetic acid and particularly NSP were greater in SART-stress mice than in normal mice. With the D'Amour-Smith method, only NSP had a greater effect in SART-stress mice than in normal mice.

Aminopyrine↗
PubMed1975

Analgesic and tolerance studies with AP-237, a new analgesic.

1-n-Butyryl-4-cinnamylpiperazine hydrochloride, AP-237, is a new analgesic that has been reported in both Japan and the United States to have good analgesic activity in animals and is currently undergoing clinical trials. A detailed study of the analgesic and side effect profile of this compound is presented. AP-237 was an effective analgesic in a variety of species by several different routes of administration. Results of studies in an inflamed paw pressure and tail flick test in rats, hot plate and writhing test in mice, tooth pulp test in rabbits and intra-arterial bradykinin test in dogs are reported. AP-237 had a low physical dependence liability in rodents as measured by a mouse jumping test and a lack of withdrawal syndrom. Tolerance and cross tolerance results are reported. AP-237 is compared to morphine and pentazocine in most tests.

Acetylcholine↗
PubMed1975

The induction of renal papillary necrosis in Gunn rats by analgesics and analgesic mixtures.

Homozygous members of the mutant Gunn strain of Wistar rats genetically lack the enzyme uridine diphosphate glucuronyl transferase. "High" and "low" dose gavage feeding for 18-34 days of an analgesic mixture containing aspirin, phenacetin and caffeine (APC) confirmed the previously reported susceptibility of these animals to analgesic induced renal papillary necrosis. Heterozygotes do not share the gross enzyme deficiency of homozygotes and, when treated with APC under identical conditions, failed to develop renal papillary necrosis. Groups of homozygotes were dosed by gavage with aspirin, phenacetin and paracetamol for 4 weeks. Renal papillary necrosis was produced by all 3 drugs, the lowest frequency of lesions occurring with phenacetin. It is postulated that the enzyme deficiency of homozygous Gunn rats influences the metabolism of analgesics to favour the excretion of nephrotoxic metabolites. The renal papillary necrosis appearing in these experiments is essentially an acute lesion, differing both in natural history and morphology from the renal papillary necrosis of analgesic nephropathy, suggesting that the pathogeneses of the experimental and human lesions differ.

Acetaminophen↗
PubMedDate not supplied

Central action of narcotic analgesics. Part IV. Noradrenergic influences on the activity of analgesics in rats.

The effect of clonidine, naphazoline and xylometazoline on analgesia induced by morphine, codeine, fentanyl and pentazocine, and on cataleptic effect of morphine, codine and fentanyl was studied in rats. The biochemical assays on the influence of four analgesics on the brain concentration and turnover of noradrenaline (NA) were also performed. It was found that three drugs stimulating central NA receptors failed to affect the analgesic ED50 of all antinociceptive agents and they enhanced catalepsy induced by morphine and fentanyl. Codeine catalepsy was increased by clonidine and decreased by naphazoline and xylometazoline. The brain concentration of NA was not changed by morphine and fentanyl, but one of the doses of codeine (45 mg/kg) slightly enhanced it. Pentazocine dose-dependently decreased the brain level of NA. The rate of NA turnover was not altered by analgesics except for the higher dose of fentanyl (0.2 mg/kg) following which the disappearance of NA from the brain was diminished. The results are discussed in the light of various and non-uniform data from the literature. It is suggested that in rats the brain NA plays a less important function than the other monoamines in the behavioural activity of potent analgesics.

Analgesics, Opioid↗
PubMedDate not supplied

Central action of narcotic analgesics. VI. Further studies on the participation of serotonin in the action of analgesics.

The effects of agents changing the cerebral serotonin (5-HT) level on the action of morphine, codeine, fentanyl and pentazocine were tested in rats with the tests of catalepsy and analgesia (hot plate). In addition, the effect of analgesics of the level and turnover of cerebral 5-HT was studied. Depression of the cerebral level of 5-HT usually antagonized the behavioral effects of analgesics, but the effect varied with the agent depressing the 5-HT level. The serotonergic influences in catalepsy seem to be more pronounced than in analgesia. An increase in the cerebral level of 5-HT may potentiate the analgesic and prolonged the cataleptogenic effects of some drugs (morphine and pentazocine), not affecting the effect of others (fentanyl, codeine). The potentiation by morphine of the turnover of cerebral 5-HT in rats is not a common property of analgesics agents.

5-Hydroxytryptophan↗
PubMed1988

Residual analgesic effects of morphine in 55 four-period crossover analgesic studies.

Subjective response data from 55 postoperative pain studies were examined for the residual analgesic effects of morphine. The studies were planned as four-period crossover designs for four treatments. Each patient received 5 and 10 mg of morphine and two doses of a test preparation. Two measures of analgesia were used: Sum of the Pain Intensity Difference (SPID) and Total Pain Relief (TOTPAR). To facilitate analysis, two two-period groups were defined. Morphine data for periods 1 and 2 were designated as group A, and morphine data for periods 3 and 4 were designated as group B. Residual analgesic effects were 0.12 for both SPID and TOTPAR in group A and were 0.65 and 0.17 for SPID and TOTPAR, respectively, in group B. In these 55 studies, there was no evidence of significant residual analgesic effects. Thus the crossover design is an appropriate method for the evaluation of selected parenteral analgesics in the postoperative pain model.

Dose-Response Relationship, Drug↗
PubMed2000

Pain treatment after tonsillectomy: advantages of analgesics regularly given compared with analgesics on demand.

The aim of the present prospective study was to evaluate pain treatment during the first postoperative 24 h for 40 patients (age over 18) undergoing tonsillectomy. Patients were divided into two groups: group A (n = 20) received analgesics on demand and group B (n = 20) on a regular basis. Basic pain treatment consisted of paracetamol 750 mg x 6 and diclofenac 50 mg x 3. Pain measurement was performed using a visual analogue scale (VAS): a 10 cm line with 0 cm equalling no pain and 10 cm equalling the worst pain ever felt. The following parameters were studied: VAS values, the need for rescue analgesics, intra- and postoperative bleeding, nausea and vomiting, postoperative food intake and hospital time. Only 4 of 20 (20%) patients in group B needed rescue analgesics in the postoperative ward compared with 15 of 20 (75%) in group A (p < 0.01, chi2 test). In group B, 13 of 20 (65%) patients could eat solid food before they were discharged from the ward, compared with 7 of 19 (37%) monitored patients in group A (p < 0.01, chi2 test). The observed VAS values were generally rather low in both groups. The mean value for all observed VAS values was less than 4 in both study groups. However, no significant difference in VAS values was observed between the two study groups. Our results suggest that regularly given postoperative pain treatment after tonsillectomy, starting intraoperatively with paracetamol and diclofenac, has significant advantages compared with a regimen in which patients receive analgesics only on demand.

Adolescent↗
PubMedDate not supplied

[Influence of klofelin on the analgesic and autonomotropic effects of narcotic analgesics].

In conscious rats clopheline (0.1-0.25 mg/kg), in contrast to promedol, morphine and fentanyl administered at analgesic doses, suppressed nociceptive reactions of arterial blood pressure produced by a mechanical stimulation and intracardiac infusion of bradykinin. The use of clopheline in combination with narcotic analgesics potentiated the analgesic effect and significantly inhibited nociceptive hemodynamic reactions without changing the background level of arterial blood pressure.

Analgesics↗
PubMed1978

Narcotic cuing and analgesic activity of narcotic analgesics: associative and dissociative characteristics.

By using a discrete-trial, two-lever, food-reinforced discrimination learning paradigm, rats were trained to discriminate the narcotic analgesic fentanyl (0.05 mg/kg) from saline. Stimulus generalization experiments with lower fentanyl doses (0.0025 to 0.02 mg/kg) were carried out to generate individual threshold doses. The latter were compared with the sensitivity of the same rats to the analgesic effect of fentanyl, and it was found that there is no correlation between these two sets of data. In a time-effect experiment, the duration of fentanyl's cuing effect was compared with that of its analgesic effect, and it was found that the time-effect characteristics of the narcotic cue are similar to those of analgesia. Again, however, there was no correlation between the duration of both effects within the same group of animals. The results further deliniate the associative and dissociative characteristics of the narcotic cue and narcotic analgesia.

Analgesics↗
PubMed2000

Brain uptake and the analgesic effect of oxytocin--its usefulness as an analgesic agent.

To establish the usefulness of oxytocin (OT) as an analgesic for women in delivery, the pharmacokinetic parameters and blood-brain barrier (BBB) permeability of [3H]OT were obtained using an intravenous injection technique or the internal carotid artery perfusion/capillary depletion (ICAP/CDM) method. Brain uptake of OT was similar to that of sucrose, plasma space marker, indicating that OT has a poor BBB permeability. Moreover, the analgesic effects of OT injected through the jugular vein on nociception were evaluated by the tail-flick method. The antinociceptive effects of OT injected at a dose of 0.2 mg/kg or 2 mg/kg were dose-dependent. In addition, the analgesic effects of OT on the CNS were unaffected by naloxone, a m-receptor antagonist. In a similar manner to the opioid system, OT may play a modulatory role in antinociception.

Analgesics, Non-Narcotic↗
PubMed1984

Mechanism of analgesic action of mesaconitine. I. Relationship between analgesic effect and central monoamines or opiate receptors.

The contribution of the central monoamines and the opiate receptor to mesaconitine (MA)-induced analgesia was investigated by means of pharmacological and neurochemical methods in which morphine (Mor) was used for comparison. The analgesic action of MA (i.c.) determined by the acetic acid-induced writhing method and the tail flick method was dose-dependent, indicating that its activity is elicited through the central nervous system. MA-induced analgesia was decreased by alpha-methyl-p-tyrosine (alpha-MT), 6-hydroxydopamine, diethyldithiocarbamate, disulfiram and reserpine, and increased by methamphetamine and norepinephrine (NE). The mode of action of MA was similar to that of Mor except for the results obtained upon combined administration with 1-dopa, dopamine, alpha-MT or chemicals related to 5-hydroxytryptamine. In addition, MA promoted the alpha-MT-induced decrease in NE levels in hippocampus, medulla oblongata plus pons and spinal cord. Levallorphan did not affect the analgesic activity of MA, showing that its activity is not mediated via the opiate receptors. Consequently, it is concluded that the analgesic activity mediated by MA is closely related to responses involving the central catecholaminergic system, in particular, the noradrenergic system.

Aconitine↗
PubMed1995

Is epibatidine really analgesic? Dissociation of the activity, temperature, and analgesic effects of (+/-)-epibatidine.

The experiments in the present study were designed to determine if the activity, temperature, and analgesic effects of (+/-)-epibatidine treatment could be dissociated. Initially (i.e., 15 min) (+/-)-epibatidine treatment (0.1 mumol/kg = 28 micrograms/kg, IP) impaired rotorod performance, decreased activity, decreased temperature, and increased jump latency (e.g., analgesic effect). For the remaining time points measured (i.e., 30, 60, and 120 min), activity and temperature remained significantly reduced. In contrast, by 120 min (+/-)-epibatidine's effects on rotorod performance and analgesia (jump latency) were not observed. When administered after (+/-)-epibatidine (0.05 mumol/kg, IP), mecamylamine treatment (5 mumol/kg = 1 mg/kg, IP) produced a potentiation of analgesia. This potentiation effect was not observed on activity and temperature measures. The effect of (+/-)-epibatidine treatment (0.1 mumol/kg, IP) was also determined in mice with central nicotinic receptor blockade induced by treatment with chlorisondamine (23 mumol/kg = 10 mg/kg, IP). An (+/-)-epibatidine-induced reduction in activity was not attenuated in chlorisondamine-treated mice and only a minimal effect was observed on (+/-)-epibatidine-induced hypothermia in chlorisondamine-treated mice. In contrast, in chlorisondamine-treated mice (+/-)-epibatidine's analgesic effect was attenuated. Taken together, these data suggest that various centrally mediated effects of (+/-)-epibatidine can be dissociated.

Analgesics, Non-Narcotic↗
PubMed1996

Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.

Structural features of three regions of the capsaicin molecule necessary for agonist properties were delineated by a previously reported modular approach. These in vitro agonist effects were shown to correlate with analgesic potency in rodent models. Combination of optimal structural features from each of these regions of the capsaicin molecule have led to highly potent agonists (eg., 1b). Evaluation in vivo established that 1b had analgesic properties but poor oral activity, short duration of action, and excitatory side effects which precluded further development of this compound. Preliminary metabolism studies had shown that the phenol moiety of 1b was rapidly glucuronidated in vivo, providing a possible explanation for the poor pharmacokinetic profile. Subsequent specific modification of the phenol group led to compounds 2a-j, which retained in vitro potency. The in vivo profiles of two representatives of this series, 2a,h, were much improved over the "parent" phenol series, and they are candidates for development as analgesic agents.

Administration, Oral↗
PubMed1972

Analgesic nephropathy: removal of phenacetin from proprietary analgesics.

Since phenacetin was withdrawn from Askit Powders and Beecham's Powders in 1966 these preparations have declined in importance as a cause of analgesic nephropathy in Western Scotland. In most patients with analgesic nephropathy who persist in abuse of compound analgesics renal function continues to decline. The deterioration, however, is less rapid among those taking aspirin and caffeine mixtures than in those taking preparations which also contain phenacetin.

Analgesics↗