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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↗
PubMed1987

Analgesic activity following combined oral administration of flupirtine maleate and peripherally acting analgesics in mice and rats.

Concomitant administration of flupirtine maleate at a single low dose (15 mg/kg, mice; 35 mg/kg, rats) with a wide range of doses of each of the peripherally acting analgesics enhanced the antinociceptive activity of paracetamol, acetylsalicyclic acid and ibuprofen in the acetic acid writhing test, acetylsalicylic acid in the hot plate test and paracetamol, acetylsalicyclic acid and ibuprofen in the Randall-Selitto test. The concomitant administration of a single low dose of the peripherally acting analgesics (at about 1/2 ED50) with a wide range of doses of flupirtine maleate resulted in enhancement of flupirtine maleate analgesic activity by paracetamol (in the hot plate and Randall-Selitto tests), acetylsalicyclic acid (in the acetic acid writhing test), ibuprofen (in the Randall-Selitto test) and indomethacin (in the acetic acid and Randall-Selitto tests). Thus flupirtine maleate enhanced the analgesic activity of paracetamol, acetylsalicyclic acid and ibuprofen in mice and rats. Each of the peripherally acting analgesics enhanced the analgesic activity of flupirtine maleate in one or more of the analgesic tests used.

Acetaminophen↗
PubMed2005

The analgesic effect of etoricoxib relative to that of cetaminophen analgesics: a randomized, controlled single-dose study in acute dental impaction pain.

BACKGROUND: To compare the analgesic effect of single doses of etoricoxib 120 mg, oxycodone/ acetaminophen 10 mg/650 mg and codeine/ acetaminophen 60 mg/600 mg in acute pain using the dental impaction model. METHODS: In this randomized, double-blind, placebo-controlled, parallel-group study, patients reported pain intensity and pain relief (16 times) and global scores (twice) during a 24-h period. The primary endpoint was the overall analgesic effect, total pain relief over 6 h (TOPAR6). Other endpoints were patient global evaluation, time to onset (2-stopwatch method), duration of analgesic effect (median time to and amount of rescue medication use). Tolerability was evaluated by overall and opioid-related (nausea and vomiting) adverse experiences. RESULTS: 302 patients (mean age 23; 63% women; 63 % White) were randomized to etoricoxib 120 mg, oxycodone/acetaminophen 10 mg/650 mg, codeine/acetaminophen 60 mg/600 mg, and placebo (2:2:1:1). Etoricoxib demonstrated significantly greater overall analgesic efficacy (TOPAR6) (13.2 units) versus oxycodone/acetaminophen (10.2 units); and codeine/acetaminophen (6.0 units); p < 0.001 for all. All active treatments were superior to placebo. Median time to onset was significantly (p < 0.001) shorter for oxycodone/acetaminophen (20 min) and numerically but not significantly shorter (p = 0.259) for codeine/acetaminophen (26 min) compared with etoricoxib (40 min). Etoricoxib (24 h) had a significantly longer lasting analgesic effect than oxycodone/acetaminophen (5.3 h), codeine/acetaminophen (2.7 h), and placebo (1.7 h) (p < 0.001 for all). Etoricoxib patients experienced fewer clinical adverse experiences than patients on oxycodone/acetaminophen and codeine/acetaminophen, specifically, significantly (p < 0.05) fewer episodes of nausea. CONCLUSION: Etoricoxib 120 mg provided superior overall analgesic effect with a smaller percentage of patients experiencing nausea versus both oxycodone/acetaminophen 10 mg/650 mg and codeine/acetaminophen 60 mg/600 mg.

Acetaminophen↗
PubMed1996

Additive analgesic effect of codeine and paracetamol can be detected in strong, but not moderate, pain after Caesarean section. Baseline pain-intensity is a determinant of assay-sensitivity in a postoperative analgesic trial.

BACKGROUND: A randomized, double-blind, placebo-controlled single oral dose study was done in order to examine whether codeine has an additive analgesic effect to that of paracetamol for moderate and strong postoperative pain after abdominal surgery. The maximum recommended single dose of paracetamol 1000 mg (Paracet) was compared with a combination of a submaximal dose of paracetamol 800 mg plus codeine 60 mg (Paralgin forte) and placebo for pain relief after Caesarean section in 125 patients. METHODS: Visual analogue pain intensity score (VAS 0-100 mm) and categorical pain relief score were recorded for 6 hours after the study drug intake. The main efficacy variables analyzed were: pain intensity difference and summed pain intensity differences during the first 3 and 6 h after study drug intake, total pain relief during the first 3 and 6 h, global evaluation score at the end of the observation period, and time to rescue analgesic. RESULTS: Because of protocol violations, 17 patients were excluded from the analysis of effects. Among the 108 patients included in the analysis of analgesic effect, 49 patients had moderate baseline pain (VAS between 40 and 60 mm on a 100 mm scale), and 59 patients had strong baseline pain (VAS more than 60 mm). In patients with strong baseline pain, statistically highly significant differences were documented in efficacy variables between the active drugs and placebo and between the two active drugs. However, in patients with moderate baseline pain, no differences were found between the study drugs in any of the analgesic efficacy variables. CONCLUSION: This study thus confirms that codeine has additive analgesic effect to paracetamol in pain after surgery. Our results show the importance of initial pain intensity in postoperative assessment of analgesic drugs. Assay-sensitivity and test power are increased by selecting patients with sufficiently high initial pain intensity and by comparing groups of patients with identical surgery and similar demographic variables.

Acetaminophen↗
PubMedDate not supplied

Patient-controlled analgesic therapy, Part II: Individual analgesic demand and analgesic plasma concentrations of pethidine in postoperative pain.

20 survival patients were allowed to self-administer small intravenous doses of pethidine to relieve pain after major abdominal surgery. Pethidine injections were given by means of a programmable drug injector. Pethidine consumption varied from 12 to 50mg/h with a mean +/- SD of 26 +/- 10mg/h. The mean measured plasma concentration of pethidine during self-administration was 551 +/- 182 ng/ml, with a range of 132 to 896 ng/ml. Minimum effective concentrations averaged 455 +/- 174 ng/ml. Individual pethidine consumption and mean plasma concentrations did not differ between men and women, and were not correlated to variations in age, anthropometric factors, plasma clearance or elimination rate constant for pethidine. Individual consumption of pethidine was consistent, with stable plasma concentrations throughout most of the trial period. Pseudo-steady-state plasma concentrations of pethidine were established and maintained at widely different levels. 19 of the 20 patients obtained subjectively satisfactory analgesia.

Adult↗
PubMed1981

Postoperative analgesics for superficial surgery. Comparison of four analgesics.

The efficacy of mild analgesics after 160 various superficial operations was studied by comparing intravenous lysine-acetylsalicylate (LAS) 1.8 g, Litalgin 4 ml (metamizole = dipyrone 2.0 g+ pitophenone 8.0 mg) or paracetamol 0.5 g to oxycodone 4 mg. At 15 min postdrug, oxycodone 4 mg had the best peak effect but this significant (P less than 0.05) difference to mild analgesics disappeared at 30 min, and thereafter all test analgesics showed an equally low effect. Two-thirds of the patients anaesthetized without peroperative analgesics needed pain relief when recovering from superficial surgery. The need for pain relief was lowest after varicose vein operations 40% of the patients as compared to about 70% after other types of superficial surgery. In 42% of the patients requiring pain relief, the test analgesics alone gave sufficient pain relief. The rest needed an additional 5 mg of oxycodone, on average, to be comfortable. The combined use of mild analgesics and oxycodone for adequate pain relief did not seem to reduce the postdrug sedation as compared to oxycodone alone. The results indicate that in traditional clinical dosages LAS, dipyrone or paracetamol can substitute about 5 mg oxycodone but offer sufficient analgesia only in about 40% of the patients recovering from superficial surgery.

Acetaminophen↗
PubMed1986

Two modes of analgesic action of aspirin, and the site of analgesic action of salicylic acid.

The analgesic activities of aspirin and salicylic acid were investigated by means of the lame-walking test in adjuvant-induced hind-paw-oedematous rats. Aspirin showed ca. 4 times more potent analgesic activity than did salicylic acid in the lame-walking test. The analgesic activity of aspirin was decreased to the level of that of salicylic acid by injection of prostaglandin E2 into the inflamed tissue. The analgesic activity of salicylic acid was not decreased by the same treatment. Salicylic acid inhibited the lame-walking reaction when given intracerebroventricularly. On the other hand, salicylic acid did not inhibit the lame-walking reaction by topical administration on the inflamed hind paw. However, with topical administration, salicylic acid inhibited the carrageenin-induced hind-paw oedema. These results suggest that aspirin has two analgesic effects on the inflammatory pain; one may be the inhibition of prostaglandin biosynthesis by acetylation of cyclo-oxygenase, and the other may be an action due to salicylic acid. Salicylic acid may produce its analgesic action mainly via a central mechanism.

Analgesia↗
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↗
PubMed1983

Post-operative dental pain and analgesic efficacy. Part II. Analgesic usage and efficacy after dental surgery.

The analgesics taken by patients after oral and periodontal surgery were noted over a three day observation period. Analgesic consumption matched closely the pain experience. The efficacy of self-prescribed analgesics was extrapolated from the pain scores obtained in the first 12 hours after surgery, and overall, the apparent efficacy appears poor. However, those patients who reported taking aspirin recorded significantly less pain than those who took either paracetamol or combination analgesics. Analgesic efficacy was not related to dose, although a significant correlation was noted between the number of paracetamol tablets taken and pain severity.

Adult↗
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↗
PubMed1984

The mode of action of analgesic drugs in adjuvant arthritic rats as an experimental model of chronic inflammatory pain: possible central analgesic action of acidic nonsteroidal antiinflammatory drugs.

The analgesic activities of intracerebroventricular (icv) administrations of some analgesic drugs, morphine, indomethacin, diclofenac, aminopyrine and acetaminophen, were studied in comparison with those of systemic administrations in normal rats and adjuvant arthritic rats. A method for the measurement of analgesic potency in normal rats and adjuvant arthritic rats were developed using the vocalization response as an indicator of pain resulting from electrical stimulation. The systemic and/or icv administered indomethacin and diclofenac produced much more potent analgesic action in adjuvant arthritic rats than in normal rats. Morphine, aminopyrine and acetaminophen given by the two routes showed roughly the same analgesic effect in both types of rats. Simultaneous systemic and icv administrations of indomethacin and/or diclofenac showed an additive effect in normal rats, but showed a synergistic effect rather than a simple additive effect in adjuvant arthritic rats. Those of morphine, aminopyrine and acetaminophen showed only additive effects in both types, except for that of aminopyrine in normal rats. Moreover, the brain and serum levels of non-metabolized indomethacin and aminopyrine were measured after the normal and adjuvant arthritic rats were systemically given these drugs. In adjuvant arthritic rats, the icv effective dose of indomethacin was the same as the brain level of non-metabolized indomethacin after the systemic administration. The effective dose of indomethacin administered icv in the normal rats was 17 times higher than the brain level of non-metabolized indomethacin administered systemically. The icv effective dose of aminopyrine was 4-4.5 times higher than the level of the brain concentration of non-metabolized drug in both types of rats.(ABSTRACT TRUNCATED AT 250 WORDS)

Aminopyrine↗
PubMed1981

The anti-inflammatory, analgesic and antipyretic activities of non-narcotic analgesic drug mixtures in rats.

The effects of non-narcotic analgesics have been examined, separately and in admixture, on carrageenan-induced hind paw oedema and on yeast-induced hyperalgesia and hyperthermia in adult rats. The efficacy of the drugs was evaluated using the kinetics of drug-receptor interaction. In addition, the hypothesis was tested that the anti-inflammatory, analgesic and antipyretic activities of the drug mixtures used equal the addition of the activities of the individual drugs and could be predicted from their intrinsic activities and affinities. Dose-dependent inhibition of paw oedema, hyperalgesia and hyperthermia was observed after oral administration of acetylsalicylic acid (aspirin), paracetamol, phenacetin (60, 125, 250 and 500 mg.kg--1), and caffeine (12.5, 25, 50 and 100 mg.kf--1). Over the dose-ranges used, the anti-inflammatory activities of paracetamol, phenacetin and caffeine tended to be smaller than that of aspirin. The dose producing a semi-maximal effect for caffeine was lower than that for aspirin which in turn was comparable to that for paracetamol or phenacetin. The analgesic activities of phenacetin and caffeine were classified as stronger than that of aspirin, whereas the efficacy of paracetamol was similar. Paracetamol and aspirin were comparable as antipyretics. The antipyretic activity of phenacetin was higher but that of caffeine was lower than that of aspirin. For caffeine the dose producing a semi-maximal effect was lower than that of aspirin. Within the dose-ranges used, low doses of mixtures of aspirin with either paracetamol, phenacetin or caffeine exhibited anti-inflammatory, analgesic and antipyretic activities which were not different from the activities expected on the basis of addition. Incidentally, at some of the higher dose levels potentiation of the activity of the drugs was found. Low doses of the triple combinations: aspirin + paracetamol + caffeine and aspirin + phenacetin + caffeine showed anti-inflammatory and antipyretic activities which were not different from those expected on the basis of addition, but the activities observed with higher doses of these combinations indicated potentiation. It is concluded that, in the rat, the anti-inflammatory, analgesic and antipyretic activities of dual and triple combinations of aspirin, paracetamol, phenacetin and caffeine at least equal the activities expected on the basis of addition.

Analgesics↗
PubMed1994

Use of codeine analgesics in a general population. A Norwegian study of moderately strong analgesics.

The prescribing of controlled analgesics (codeine, buprenorphine and pentazocine preparations) was studied, using prescriptions from the three pharmacies in the municipality of Tromsø, Norway. All prescriptions dispensed during one year were analysed. The study sample comprised 3083 women (58%) and 2223 men (42%) between 10 and 99 years of age. About 8% of the population had obtained one or more prescriptions of controlled analgesics. Combined codeine preparations were by far the most frequently prescribed subgroups, and the average amount purchased during 1 year was 30 defined daily doses (DDD). The sporadic users were in the majority. A few users had purchased high amounts of controlled analgesics. The prevalence of use, the mean number of defined daily doses of analgesics, and the proportion of 'weekly' drug users was higher in women than men. The prevalence increased significantly with age, from 0.7 to 22.3% in women and from 0.5 to 14.1% in men. The mean number of DDD during one year also increased with age, from 12.6 to 50.6 DDD in women, and from 6.6 to 40.6 DDD in men. The users of buprenorphine and pentazocine differed in several aspects from the codeine users. The highest use of combined codeine preparations was seen in elderly people especially in women. Use of lower codeine doses or intermittent treatment with other drugs e.g. plain paracetamol in adequate doses, may be appropriate alternatives reducing the risk of adverse drug reactions such as nausea and constipation. Monitoring of prescribing and use of controlled analgesics according to certain criteria may uncover possible misuse.

Adolescent↗
PubMed1981

Central action of narcotic analgesics. VIII. The effect of dopaminergic stimulants on the action of analgesics in rats.

We investigated the influence of apomorphine, amphetamine, amantadine, dimethylaminoadamantane, nomifensine, ergometrine and beta-phenylethylamine on cataleptogenic and antinociceptive action of analgesics in rats. Nomifensine, apomorphine, beta-phenylethylamine, amantadine and ergometrine antagonized the catalepsy induced by morphine and codeine. Catalepsy induced by fentanyl was depressed only by nomifensine and apomorphine. Amphetamine only slightly antagonized the analgesic-induced catalepsy and the effects were not dose-dependent. Dimethylaminoadamantane did not antagonize catalepsy at all. Antinociceptive action of morphine and codeine was antagonized by apomorphine and amphetamine. Ergometrine counteracted the action of morphine, and beta-phenylethylamine decreased the action of pentazocine. The results suggest that: 1. There are differences in the mechanism of cataleptogenic action of the opiates (morphine and codeine) and fentanyl; 2. Catalepsy after analgesia differs from the catalepsy produced by neuroleptics in respect of interaction with such drugs as amphetamine, apomorphine or dimethylaminoadamantane. Analgesic-induced catalepsy seems to depend on the presynaptic inhibition of dopaminergic neurotransmission; 3. Stimulation of the central dopaminergic system in rat brain either does not change or weakly antagonizes the action of analgesics in the hot plate test.

Amphetamine↗
PubMed1991

Differentiating analgesic and non-analgesic drug activities on rat hot plate: effect of behavioral endpoint.

The contribution of behavioral endpoint to results obtained in the 55 degrees C rat hot plate procedure was assessed. Specifically, the use of a hind paw lick-only endpoint was compared to that of a hind paw lick-or-jump endpoint. Effects of prototypical analgesic and non-analgesic compounds on response latency increases were determined under each condition. Whereas the effects of morphine, oxycodone and codeine were similar under each condition, effects of a number of non-analgesic agents differed markedly depending upon the endpoint used. Clozapine, chlorpromazine, thioridazine, atropine, scopolamine, benactyzine, yohimbine, idazoxan and cyproheptadine produced dose-dependent increases in response latency under the hind paw lick-only condition but did not increase latencies when the hind paw lick-or-jump endpoint was used. Haloperidol, sulpiride, benztropine, methyl atropine, phentolamine, prazosin, methiothepin, methysergide, diphenhydramine, pargyline and diazepam failed to increase response latencies under the hind paw lick-only condition. Moreover, whereas diazepam, chlorpromazine, pentobarbital, dantrolene and ethanol produced dose-dependent increases in the height required for successful aerial righting, increases in hind paw lick-or-jump latencies occurred only following near-anesthetic doses of pentobarbital and ethanol. These data indicate that the hind paw lick endpoint is susceptible to perturbation by extraneous pharmacologic activities. Drugs exerting muscarinic cholinergic and alpha 2-adrenergic antagonist effects are particularly able to disrupt this behavior. Disruption is not associated specifically with any other pharmacologic action, although other activities may interfere with the response. In contrast, the hind paw lick-or-jump endpoint fails to detect skeletal muscle relaxant activity and only detects gross motor impairment when near-anesthetic doses of drugs are used. The present data suggest that detection of non-analgesic drug activities by rat hot plate can be minimized by use of a hind paw lick-or-jump endpoint.

Analgesics↗