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At least 19 recordsLinked to original sources
PubMed1975

A study of the effect of d-amphetamine on the toxicity, analgesic potency and swimming impairment caused by potent analgesics in mice.

The addition of d-amphetamine to morphine has been reported to result in an increase of analgesic potency in experimental animals and man, but no data on the toxicity of such combinations are available. This study is intended to provide systematic information on the toxicity, analgesic potency and degree of physical impairment (swimming endurance) of a combination of 12 mg morphine sulfate with 10 mg d-amphetamine HCl per ml which is now under clinical investigation. Mice were used as experimental subjects. Meperidine, methadone and pentazocine were substituted for morphine using clinically equally analgesic doses and keeping the d-amphetamine amount constant. The toxicity of all analgesics especially that of morphine was enhanced in the combination, least so in the case of meperidine. The degree of increase of analgesic power by the addition of d-amphetamine was greatest with morphine and quantitatively in satisfactory agreement with present clinical experiences. However, the relationship between the increases of toxicity and of analgesia is not necessarily most favorable for this drug. For the other three analgesics increases in toxicity and analgesia were more in line, meperidine showing the best ratio. Swimming endurance was decreased with full analgesic doses of all four compounds. The presence of d-amphetamine tended to reverse this depression. The data were analyzed in relation to their possible predictive value for the use of such combinations in man for the therapeutic dose range and in the event of overdosage.

Analgesics, Opioid↗
PubMedDate not supplied

Central action of narcotic analgesics. I. Catalepsy and stereotypy in rats and narcotic analgesics.

The action of four analgesics, belonging to various pharmacological groups (morphine, codeine, fentanyl, pentazocine), was investigated in rats in tests for catalepsy and stereotypy, the tests depending on dopaminergic brain mechanisms. Interactions of the analgesics with a number of compounds known to affect dopaminergic brain functions in tests of catalepsy and stereotypy were also studied. In some experiments nalorphine, an antagonist of narcotic analgesics, was used. Morphine, codeine and fentanyl produced catalepsy, while pentazocine, at doses up to 60 microgram/kg, did not produce this effect. Reserpine, 2 mg/kg 3 hr before drugs, potentiated catalepsy produced by analgesics, while haloperidol, 0.2 mg/kg, 2 hr earlier, did not influence morphine and codeine catalepsy, but moderately potentiated fentanyl-induced catalepsy. alpha-methyl-p-tyrosine potentiated the cataleptogenic action of fentanyl and codeine, and also, less markedly, the action morphine. D-amphetamine (2.5-10 mg/kg) and apomorphine (5 mg/kg) moderately antagonized the catalepsy induced by analgesics, while atropine did not affect it. Nalorphine, 5 mg/kg, effectively abolished the catalepsy produced by narcotic analgesics, but did not affect that produced by neuroleptics. Morphine, codeine and fentanyl slightly inhibited apomorphine stereotypy, and evidently antagonized stereotypy produced by amphetamine. Pentazocine did not affect or slightly potentiated the both types of stereotypy. It is concluded that morphine, codeine and fentanyl, in contrast to pentazocine, inhibit behavioral activities depending on central dopaminergic functions in the rat. The mechanism of this action is most probably indirect, and seems to be related to the dopaminergic presynaptic functions.

Animals↗
PubMed1976

A new analgesic testing method using ultrasonic stimulation. I. Effects of narcotic and nonnarcotic analgesics.

A quantitative method for measuring pain threshold by the use of ultrasonic stimulation in mice has been designed. The method had the advantage of precision, simplicity of technique, rapidity of measurement, and the fact that the stimuli is innocuous upon repeated application. The nature of the senstaions induced by ultrasonic stimulus is somewhat like that felt with a prick type of pain. Pentazocine (30, 100, 150 mg/kg i.p.) aminopyrine (15,50, 100, 150 mg/kg i.p.), phenacetin (100,150, 200, 250 mg/kg i.p.) sodium salicylate (150, 200, 250 mg/kg i.p.) and other antipyretic analgesics were active in a wide range of doses indicating that this technique is sensitive to the narcotic antagonist and to the weak analgesics as well as to the narcotic analgesics as well as to the narcotic analgesics such as morphine (2.5, 5, 10, 15 mg/kg i.p.), codeine (10, 20, 25, 30, 50 mg/kg i.p.) and pethidine (5,10, 15, 20, 25 mg/kg i.p.). The ultrasonic method is, therefore, applicable in screening procedures when attempting to evaluate the analgesic potency of a wide variety of chemical agents.

Age Factors↗
PubMed1979

A model for evaluating the analgesic effect of a new fixed ratio combination analgesic in patients undergoing oral surgery.

A special model designed for evaluating the analgesic effect of oral analgesics was based on a short-time registration period of immediate postoperative pain. One-hour intervals in pain registration and a minimum of 2 h between the tablet intake allowed a good estimation of changes in pain levels. The patient material consisted of 112 patients and from each patient a lower impacted wisdom tooth was removed. The test model was used to compare two analgesic drugs with placebo. The two pharmacologically active preparations were Doleron (dextropropoxyphene, acetylsalicylic acid, phenazone, caffeine and Transergan) and Astra 2167 (dextropropoxyphene and acetylsalicylic acid). The trial was double blind and the tablets were administered according to a crossover design. There was no statistically significant difference in analgesic effect between Astra 2167 and Doleron, and both drugs were superior to placebo. Finally, the trial showed that a reduction of the number of components of a compound analgesic to some degree reduced the pain relieving effect on this particular postoperative pain. This observed reduction was however, not statistically significant.

Adult↗
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↗
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↗
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↗
PubMed1976

Discriminative stimulus properties of analgesic drugs: narcotic versus non-narcotic analgesics.

Using a food-reinforced two-lever operant procedure, rats (n=6) were trained to discriminate fentanyl (1.25 mg/kg, p.o., t-60') from solvent (1 ml/100 g B.W., p.o., t-60'). The administration of another narcotic analgesic (pethidine) produced a dose-related generalization with the standard fentanyl treatment; six non-narcotic analygesics (suprofen, acetylsalicylic acid, indomethacin, phenacetin, phenylbutazone, tolmetin) were found not to do so. It is concluded that the ability of drugs to produce analgesia is not a sufficient condition for the drugs to produce the narcotic cue as well.

Analgesics↗
PubMed1978

Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.

A series of N-sec- and N-tert-alkylnormorphines was synthesized and evaluated for analgesic potency, antagonist activity, and opiate receptor binding. Computer-assisted conformational analysis profiles were utilized to assist in the selection of compounds for synthesis and correlation of receptor events with in vivo observations. N-tert-Alkylnormorphines 5a-c were devoid of agonist activity; however, some sec-alkyl analogues showed interesting mixed agonist-antagnoist actions. N-sec-Butyl- and N-(alpha-methylally)normorphine were separated into R and S isomers, which exhibited quantitative pharmacological differences. The N-sec-butyl S isomer 10a showed analgesia approximating morphine with nalorphine-like antagonist activity. Preliminary testing indicates only slight evidence for physical dependence with this compound.

Analgesics↗
PubMedDate not supplied

Central action of narcotic analgesics. II. Locomotor activity and narcotic analgesics.

The effect of morphine, codeine, fentanyl and pentazocine on locomotor activity of rats and mice and open-field performance of rats were tested. All the analgesics tested produced a depressive action in the rat. In mice a depressive action was produced by pentazocine and codeine. Fentanyl increased the exploratory and basal locomotor activity of mice. Morphine increased the exploratory activity, but, given at doses of 2.5 and 10 mg/kg decreased the basal locomotor activity. The increase of locomotor activity in mice by morphine and fentanyl is caused by an indirect stimulation of catecholamine receptors.

Analgesics, Opioid↗
PubMedDate not supplied

Central action of narcotic analgesics. V. Participation of serotonin in the mechanism of action of narcotic analgesics.

The influence of serotonergic system on the changes in locomotor activity of mice and rats brought about by morphine, fentanyl, codeine and pentazocine and on morphine induced catalepsy in rats was studied. p-Chlorophenylalanine (pCPA) did not affect the behavioral changes produced in mice by morphine, fentanyl, codeine and pentazocine but reduced the behavioral depression produced by these drugs in rats. 5-Hydroxytryptophan (5-HTP) but not tryptophan (TP) reversed the action of pCPA on the effect of morphine and fentanyl. After reserpine the depression produced in rats by morphine and fentanyl was more pronounced. TP did not change the depression produced by combination of reserpine and morphine but counteracted the depression observed after combination of reserpine and fentanyl. In mice reserpine protected against hypermotility produced by morphine or fentanyl and TP potentiated the depression produced by the combination of reserpine and morphine or reserpine and fentanyl. Serotonin precursors, 5-HTP and TP evidently potentiated the morphine induced catalepsy. pCPA counteracted only the enhancement of the catalepsy observed after TP administration. Naloxone abolished the catalepsy after combined treatment with morphine and TP. Similarly but weaker acted cyproheptadine. The results suggest that the serotonin system plays a role in the effects of morphine and fentanyl on rat locomotor activity. An increase in the cerebral serotonin level increases the morphine catalepsy in rats.

Analgesics, Opioid↗
PubMed1978

Kinetics of analgesic response in man; an example with two non-steroidal anti-inflammatory analgesic drugs.

A double-blind, controlled trial is described in which a total of forty hospital in-patients suffering from severe post-operative pain were randomly allocated to treatment with one of two non-steroidal anti-inflammatory drugs, namely, either indoprofen which has a short half-life (two-hours) or naproxen which has a long half-life (thirteen hours). The drugs were administered orally on a single-dose basis. The doses used in this way were 300 mg of indoprofen or 250 mg of naproxen. Patients scored the severity of their pain on a five-point scale and these scores were recorded prior to and at fixed time intervals up to eight hours following administration of medication. No significant differences emerged between the two test drugs and the duration of the response was also found to be similar for the two compounds despite their very different plasma half-life values.

Adolescent↗
PubMed1979

[Asthma caused by analgesics].

Asthma, caused by analgesics, a relatively frequent phenomenon in bronchial asthma conditioned by infection, often remains unrecognized and is then sometimes a danger of high degree for these patients. Pathogenetically, the asthma caused by analgesics perhaps does not underlie an immunological mechanism, but an induced by analgesics prostaglandin-E-synthesis inhibition. For this speak the results of skin tests, of the LTT with analgesics and of IgE concentration measurements. Concomitant phenomena of the asthma caused by analgesics are: initial rhinirrhoe, alcohol intolerance, polyposis nasi and NNH affections. Among the evoking noxae the pyrazolones (regard: pyrazolone containing asthma mixed preparations!) are of greatest importance. Since already the smallest doses of analgesics may evoke considerable asthmatic reactions the indication to the exposition test should be made cautiously. In an anamnestic suspicion on asthma caused by analgesics a strict avoidance of analgesics, antirheumatic drugs and antipyretic drugs is necessary. Salicyl amide does not cause in vitro a prostaglandin synthesis inhibition. Still further clinical examinations are necessary, whether it amy generally be recommended as a possible alternative of analgesics in asthma caused by analgesics.

Analgesics↗
PubMed1978

Analgesic nephropathy: etiology, clinical syndrome, and clinicopathologic correlations in Australia.

Analgesic abuse is a major public health hazard in Australia, and analgesic nephropathy with consequent terminal renal failure is the underlying cause in 20% of the patients requiring dialysis and transplantation. Analgesics are invariably taken in the form of compounds and mixtures. In the aspirin-phenacetin-caffeine (APC) mixture, aspirin appears to be the major nephrotoxic agent and phenacetin appears to play a secondary and synergistic role. The renal disease associated with abuse of analgesics is characteristic and is part of a much wider clinical syndrome, the analgesic syndrome, which includes peptic ulcer disease (35%), anemia (60 to 90%), hypertension (15 to 70%), ischemic heart disease (35%), psychological and psychiatric manifestations, pigmentation, and possible gonadal- and pregnancy-related effects. The primary lesion in analgesic nephropathy is renal papillary necrosis (RPN), and this is a nephrotoxic effect common to all nonsteroid antiinflammatory agents. The most important factor in the management of patients with analgesic nephropathy is the cessation of analgesic abuse, and this leads to improvement and stabilization of renal function. A small proportion of patients will, however, deteriorate in relation to accelerated hypertension, persistent proteinuria, ischemic heart disease, and complications leading to nephrectomy. Patients with analgesic nephropathy are poor risk patients and have a poor prognosis, even after dialysis and transplantation.

Adult↗
PubMed1979

Prevalence of compound analgesic in Newcastle (NSW).

A household survey of analgesic use was carried out in two areas of different social advantage in Newcastle, New South Wales, during November 1977. The survey was preliminary to evaluating the proposed rescheduling of compound analgesics in the region. Approximately 16.5 per cent of the over 18-year-olds in the population claimed to use compound analgesics from time to time, and over 90 per cent used analgesics of some kind. Analgesic patterns varied between the two areas studied; of women living in the socially disadvantaged areas, about five per cent used compound analgesics daily. Rescheduling of compound analgesics may initially increase the workload of general practitioners, as up to one third of women who regularly use analgesics seek alternatives. A programme of public education and support is needed to assist compound analgesic users when rescheduling occurs.

Adolescent↗