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PubMedDate not supplied

Use of analgesics in self-medication.

Self-medication with analgesics is common and accepted and even recommended by health systems in order to avoid reimbursement. Self-medication, nevertheless, is not an easy task, since making choices is difficult for patients on the basis of the available standard information. Guiding information for patients has to be improved, but also physicians need to be trained how to handle self-medication of their patients. Special attention should be paid to the approval of combination analgesics for the treatment of headache and migraine. There were two major points of discussion during the last decades: possible risks of nephropathy and possible drug-induced overuse. According to a very recent evaluation, analgesic-associated nephropathy appears to have been primarily caused by phenacetin rather than any other single or combination analgesics. Analgesic-induced overuse is also caused by the psychotropic actions of phenacetin in presentations providing rapid absorption, such as powders, rather than by other analgesics or caffeine.

Analgesics, Non-Narcotic↗

PubMed1976

[Limits of pure analgesic anesthesia].

Before dealing with this subject, the author believes that it is useful to give a definition of this technique and justify it. He then recalls the results which he obtained with various analgesic drugs, few products permit this technique, either because of too low analgesic power, or because of the appearance in high dosage, of troublesome or dangerous side-effects. At present, in this type of anesthetic, one may use either morphine or fentanyl or fentathienyl. Analgesic anesthesia with morphine. This technique presents advantages and disadvantages. The author has no personal experience of high doses of morphine and can only report that of other authors who have studied this problem. Anesthesia analgesia with fentanyl and fentathienyl. The author believes that this technique presents advantages over the previous technique, he has personally studied the clinical pharmacology of high doses of fentanyl and he believes that this drug used by the intravenous route, at a dose of 0.05 mg/kg associated with a curare derivative, possesses favourable cardiovascular and respiratory metabolic effects during the surgical operation, but one must recognize that +/-20 p. 100 of cases, fentanyl associated only with curare is not sufficient to give a stable anesthetic. At present, the author has replaced, in his technique, fentanyl by fentathienyl which is a morphine derivative 6 to 7 times more powerful. He found with this drug most of the properties of high doses of fentanyl but the analgesia obtained is deeper, one does not find more than 20 p. 100 of resistant cases. However, the author noted the fairly frequent appearance of tachycardia for which there was no valid explanation. In conclusion. The author believes that in the reproaches which are made to analgesic anesthesia, some are justified, others are less so. It requires prolonged post-operative supervision, but the latter would be advisable for any other type of anesthesia. It dose not always permit one, in its pure form, to obtain stable anesthesia, but this is less and less true with the appearance of more and more powerful derivatives. The use of analgesic anesthesia as a routine technique is only possible in the form of sequential analgesic anesthesia, a technique which uses an antimorphine drug to awaken the patient. In this field, various new products are presented are discussed.

Analgesia↗

PubMed1977

Prenatal administration of levorphanol or dextrorphan to the rat: analgesic effect of morphine in the offspring.

We have recently demonstrated that prenatal administration of morphine to the rat results in tolerance to the analgesic effects of morphine in the offspring at 3 to 11 weeks of age. To extend these findings, levorphanol or dextrorphan was administered to female CFE rats during days 5 to 12 of gestation. Control animals were injected with 0.9% saline on the same schedule. At 5 weeks of age all offspring were tested with graded doses of morphine in the hot-plate test for analgesia. Morphine produced a dose-related increase in analgesia in all offspring, but the effect of morphine in the offspring of levorphanol-treated females was significantly reduced compared to the offspring of saline-treated females; the analgesic effect of morphine did not differ between the offspring of the dextrorphan- and saline-treated females. The analgesic effect of morphine remained reduced in 9-week old offspring of levorphanol-treated females compared to the corresponding offspring of females that had received saline. Diminished analgesic activity of morphine in the offspring of levorphanol-treated females compared to the offspring of females that had received dextrorphan or saline was still observed even when the offspring were rendered tolerant to morphine by daily drug injections over a period of 5 days. Thus, the protracted tolerance to the analgesic effects of morphine can also be produced by a morphine congener (levorphanol), but not by its analgesically inactive (+) isomer (dextrorphan).

Analgesics, Opioid↗

PubMed2003

Recovery of male rats from major abdominal surgery after treatment with various analgesics.

The objective of this study was to compare the recovery of male rats after a major abdominal surgical procedure (the implantation of a radiotelemetry transmitter) when treated with buprenorphine, butorphanol, or ketoprofen and subcutaneous fluids (5% dextrose) or with subcutaneous fluids only. The parameters for assessing recovery were heart rate (HR), mean arterial blood pressure (MAP), home cage activity, food and water consumption, and body weight. HR, MAP, and activity were continuously monitored by radiotelemetry methods, food and water intakes were determined daily, and body weights were measured once or three times a week. In light of HR, nocturnal home cage activity, water consumption, and body weight gain, animals were recovered by about 7 days after surgery. MAP normalized by 1 to 2 days postsurgery, and food consumption returned to presurgical levels 5 to 12 days after surgery, depending on the analgesic treatment. On the basis of nocturnal activity, HR, and food and water intakes, buprenorphine-treated animals recovered more slowly than did the other two analgesic-treated groups. By the other parameters, all three analgesic-treated groups showed very similar responses across time. Surprisingly, when compared with the groups receiving only subcutaneous fluids, buprenorphine and butorphanol delayed or did not advance recovery, whereas ketoprofen neither retarded nor advanced recovery. Explanations for these results include: (a) the analgesics were effective in relieving pain but had pharmacological side effects that altered the measured parameters, making it difficult to determine recovery; (b) the level of pain experienced did not notably affect recovery; (c) the analgesics, at the doses and/or dosing schedules used, were not effective in the relief of pain, thereby causing both groups of animals to recover at the same rate; and (d) the analgesics interfered with recovery. Final resolution of these issues awaits further investigation.

Abdomen↗

PubMed2003

[Heroin: a useful analgesic?].

BACKGROUND: In some countries, heroin is widely used as an analgesic agent. MATERIAL AND METHODS: The literature describing the history, pharmacology and analgesic use of heroin was reviewed. RESULTS: Heroin is a semi-synthetic morphine derivative. A century ago it was considered a panacea with numerous indications. Today it is best known as a drug of abuse, but is still in use as an analgesic. Most studies that compare heroin with other analgesics have methodological shortcomings; however, they generally indicate that heroin has a clinical effect not very different from morphine. An better aqueous solubility as compared to morphine may in some situations be advantageous. Because of a proposed incomplete cross-tolerance between heroin and other opioid analgesics, it may be used if the patient shows sub-therapeutic response to first-line opioids. INTERPRETATION: Although not well documented, heroin appears to be an effective analgesic with certain properties different from those of morphine. It may be of clinical value in conditions with acute and/or terminal pain.

Adult↗

PubMed2004

Analgesic activity of new synthetic thiazolidine-4-ones derivatives.

Ten new synthetic thiazolidine-4-ones derivatives (5 chlorothiazolidine-4-ones, 3 methoxythiazolidine-4-ones and 2 hydoxythiazolidine-4-ones) having different substituents at R1, R2 and R3 were evaluated for their analgesic activity using different animal models and their structure activity relationship was also elucidated. Chlorothiazolidine-4-ones and methoxythiazolidine-4-ones exhibited analgesic activity in tail flick test, tail immersion test and acetic acid writhing test. C-III (chloride substituents at R1 and R2) produced higher latencies than any other compounds in tail flick test and C-I (no substituents at R1 and R2) was not effective in acetic acid writhing test. Hydroxythiazolidine-4-ones did not show analgesic activity in any of the animal models used. In conclusion, the character of substituents at R3 of thiazolidine moiety position may have an effect on the analgesic activity of thiazolidine-4-ones and either chloride or methoxy substitution may be necessary to produce analgesic activity. Two chloride substituents in a compound may increase the central analgesic activity of the compound.

Analgesics, Non-Narcotic↗

PubMed2005

Levetiracetam as an adjunctive analgesic in neoplastic plexopathies: case series and commentary.

Certain types of pain associated with cancer may be difficult to treat with standard therapies, often resulting in intractable pain and suffering for the patient. The use of an opioid as analgesic monotherapy can lead to poorly controlled pain as well as multiple side effects. Non-opioid adjunctive analgesics, such as antidepressants and antiepileptic drugs (AEDs) often improve both pain control, and side effect prevalence. Levetiracetam is an AED with unique mechanisms of action that may have analgesic properties in various pain syndromes. Seven patients with neoplasms involving neural structures (four invading the brachial plexus, and three the lumbosacral plexus) had severe pain of 8 to 9 out of 10 on a visual analog scale (VAS), despite the use of parenteral opioids and various adjunctive therapies. These patients were treated with oral levetiracetam titrated over days to two weeks, depending on the location of pain, drug response, and tolerance to tapering of opioid analgesics. Opioid and adjunctive analgesic use and VAS scores were recorded periodically. The maximum levetiracetam dose ranged from 500 mg to 1500 mg BID. All patients experienced pain control improvement after the addition of levetiracetam, with VAS scores decreasing from 8-9 out of 10 to 0-3 out of 10 within two to 14 days of therapy initiation. Overall opioid use decreased by at least an estimated 70%, without drug related adverse events. In this small series of patients, levetiracetam effectively and safely improved pain relief in patients with neoplastic plexopathies previously resistant to standard analgesic approaches.

Adult↗

PubMed2006

Analgesic activity of high-dose intravenous calcitonin in cancer patients with bone metastases.

We undertook a prospective, nonrandomized study with the objective to evaluate the efficacy of salmon calcitonin (sCT) in controlling pain secondary to bone metastases. Our study population consisted of 45 cancer patients with bone metastases (26 men) with a mean age of 64 years (range, 48-70) who had completed chemotherapy, hormonal therapy and radiation therapy at least 30 days prior to enrollment in the study, and had intractable pain despite the use of common analgesics (acetaminophen, nonsteroidal anti-inflammatory agents, opioids) and bisphosphonates. The study medication was a 300-IU dose of sCT administered intravenously daily for 5 consecutive days and repeated every two weeks until no response was noticeable. The analgesic efficacy of sCT was evaluated by means of Huskisson's visual analogue scale and Keele's pain scale; the daily consumption of analgesic drugs and performance status were also monitored. None of the patients managed to completely discontinue the use of other analgesics, but 5 patients (11% of the total number) had an analgesic response that lasted 4 weeks and less than 5% of the patients continued to respond for 6 weeks. No significant side effects were observed. Our data show that intravenous calcitonin administered in a relatively high dose has a very limited therapeutic potential as an adjuvant analgesic for a short period of time in selected cancer patients with bone metastases.

Aged↗

PubMed2006

Is endogenous opioid system involved in non-opioid analgesics tolerance?

Recent investigations using metamizol and lysine-acetylsalicylate have shown that these non-opioid analgesics produce central anti-nociceptive effects probably through neural substrates that also support the analgesic effects of opiates. The aim of this study was to examine whether a clinically relevant approach, e.g. systemic administration of analgine, ketorolac and xefocam causes tolerance to them, and cross-tolerance to morphine. The experiments were carried out on experimental and control rats with saline by the model of tail-flick reflex to the stimulation of focusing light. Latency increase of this reflex indicates the degree of antinociception. This study of non-opioid analgesic effects on the latency of tail-flick reflex in rats has shown that systemic injections of analgine, ketorolac and xefocam result in significant antinociception as compared with the control group of rats with saline. Repeated administrations of these drugs revealed tolerance to them and cross-tolerance to morphine. Intraperitoneal injections of naloxone did not significantly decrease the morphine analgesic effect in analgine- and ketorolac-tolerant rats, whereas in saline-treated animals morphine analgesic effect was reverted. Taken together the present and previous findings support the notion that the contribution of the CNS, particularly of downstream pain-control structures, to the analgesic effects of NSAIDs involves endogenous opioidergic mechanisms. Thus, obtained data support the suggestion about a close relation between non-opioid tolerance and endogenous opioid system.

Analgesics, Non-Narcotic↗

PubMed2005

[Dextromethorphan enhances analgesic activity of propacetamol--experimental study].

While many pre-clinical and clinical studies have suggested that the addition of N-methyl-d--aspartate (NMDA) receptor antagonists, such as dextromethorphan, to opioid analgesics, such as morphine may enhance the analgesic effects. The aim of the study was to assess the effect of non-competitive NMDA antagonists and paracetamol (propacetamol) on pain threshold and analgesic potency of this drugs and their combinations in formalin model for pain in rats. Intraperitoneal administration of paracetamol only in doses of 100 g/kg or higher resulted in increase of pain threshold in tail flick and paw pressure tests. The results of our study suggest that there was no significant difference in pain threshold between separate administration of dextromethorphan and in combination with paracetamol. In a formalin model for pain we have shown that paracetamol in non-analgesic doses (10 mg/kg) administered in combination with dextrometorphan, ketamine and mamantine was more effective than those drugs given separately but the best analgesic effect was obtained when combination of paracetamol and dextromethorphan was applied. The addition of higher doses of these combined drugs, that is paracetamol and all three NMDA antagonists did not result in enhancement of dose-dependant analgesia. In conclusion it should be stated that NMDA antagonists improve analgesic effect of paracetamol in the formalin model for pain. although only to a limited extend.

Acetaminophen↗

PubMed1991

[Central analgesic effects of antidepressant drugs with various mechanisms of action: desipramine, fluvoxamine and moclobemide].

Analgesic properties of antidepressants are not yet well established. The aim of this study was to investigate the analgesic effect of three antidepressants after single oral dose administration to healthy volunteers. The late spinal R-III reflex threshold (objective pain threshold) and the subjective pain threshold (numerical categorical scale) were markers of analgesic effect. Desipramine induced significant increases in both thresholds. Fluvoxamine and moclobemide also exerted a significant analgesic effect, although displaying distinct patterns depending on the analgesic marker considered. Antidepressants exert a central analgesic effect independent of their antidepressive effect and, depending on their mode of action, already detectable at spinal level.

Analgesics↗

PubMed1991

Renal parenchymal disease related to over-the-counter analgesic use.

The occurrence of parenchymal renal disease has been attributed in many case reports to heavy use of over-the-counter (OTC) analgesics. To quantify this putative relationship, we carried out a comprehensive case history review of newly diagnosed parenchymal renal disease requiring hospitalization among patients who ever used acetaminophen, aspirin, or ibuprofen, at Group Health Cooperative of Puget Sound. During the 6-year period 1984-1989, 17 cases of newly diagnosed, unexplained renal disease were identified among the 378,769 users of OTC analgesics, among whom 26,931 filled at least 20 prescriptions for the analgesics studied. Six of the 17 were possibly attributable to outpatient drug use. Of these, OTC analgesics were suspected clinically as a possible causal factor in two, but in both patients other causes seemed equally likely. We did not find any patients with anatomic or pathologic findings associated with analgesic nephropathy. We conclude that parenchymal renal disease attributable to OTC analgesic use and requiring hospitalization is a rare occurrence.

Adult↗

PubMed1989

Effect of potassium ethylxanthogenate on the toxicity and analgesic effect of acetaminophen.

The effect of potassium ethylxanthogenate (PEX) on the toxicity and the analgesic effect of acetaminophen (AAP) were investigated on male albino mice. PEX in a dose of 80 mg/kg body weight, administered subcutaneously or orally one hour before AAP, or simultaneously with it, induces prolongation of the survival of the experimental animals and increases LD50 of AAP. The protective effect of PEX (s.c. and p.o.) is more pronounced when this agent is introduced one hour before AAP (i.p. and p.o.), compared with the simultaneous administration, and when it is applied orally, compared with the subcutaneous administration. The average lethal dose of the combination (AAP p.o. + PEX p.o. 1 hour previously) increases 2.57 times after observation for 7 days, compared with that of AAP. Although it does not possess its own analgesic effect, PEX potentiates the analgesic effect of AAP (which is more pronounced for the low AAP doses) and reduces its average effective dose. After 14-day administration, AAP potentiates its own analgesic effect in the lower doses. The potentiating effect of PEX on the analgesic effect of AAP is similar on the first and on the 14th day of the treatment. The principal mechanism through which PEX decreases the toxicity and potentiates the analgesic effect of AAP is assumed to be the inhibition of its metabolism by inhibition of the cytochrome P-450-linked monooxygenases, not ruling out the possibility of a certain effect on the AAP absorption.

Acetaminophen↗

PubMed1988

Analgesic and mechanistic evaluation of spiradoline, a potent kappa opioid.

Spiradoline (a congener of the kappa opioid agonist, U-50488H) was evaluated for analgesic and related activities in rodents. In nine antinociceptive assays utilizing various thermal, pressure and chemical and physical irritants, the potency of spiradoline ranges from 4.7 to 23 (mean = 13) times that of U-50488H. Naloxone blocks the analgesic effect of spiradoline. The in vivo naloxone pA2 for this antagonism is much lower than that for the antagonism of morphine and approximates that of U-50488H. The analgesic potency of spiradoline is greatly reduced in mice made tolerant to U-50488H but not in those made tolerant to morphine. Repeated treatment with spiradoline does not induce physical dependence as evidenced by a lack of naloxone-precipitated jumping and withdrawal-induced hyperalgesia. In sum, these observations suggest that spiradoline is a potent kappa agonist analgesic. However, further evaluation of spiradoline revealed differences between this compound and U-50488H. We have previously shown that the analgesic effect of the latter compound, but not that of morphine, is profoundly antagonized by reserpine or p-chlorophenylalanine. In contrast, spiradoline is only marginally antagonized by these serotonin-depleting treatments. Evaluation of the enantiomers of spiradoline revealed that the (-)-enantiomer is more than 30 times as potent as the (+)-enantiomer in analgesic tests. The (-)-enantiomer is similar to U-50488H with regard to antagonism by p-chlorophenylalanine, lack of physical dependence-inducing properties and cross-tolerance. In contrast the (+)-enantiomer induces physical dependence and displays marked cross-tolerance in morphine-tolerant mice.(ABSTRACT TRUNCATED AT 250 WORDS)

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

PubMed1987

Naloxone-sensitive and GABAA receptor mediated analgesic response of benzodiazepines in mice.

Various benzodiazepines (BZs) were investigated for their analgesic effect by the tail-flick method in mice. Central type BZ-receptor agonists such as clonazepam, chlordiazepoxide and diazepam showed analgesia while the peripheral BZ-receptor binding agent, Ro 5-4864, and the BZ micromolar binding agent phenytoin, failed to show any effect. Other BZs, such as lorazepam and nitrazepam, were ineffective in producing analgesia. Pretreatment with naloxone antagonized the analgesic effect of central type BZ-receptor agonists. Similarly, pretreatment with Ro 15-1788, a central BZ-receptor antagonist, also blocked the analgesic effect. When the involvement of the GABAergic system in the analgesic response of BZ agonists was investigated, a potentiation of BZ action was seen as a combination of a subeffective dose of clonazepam with a subanalgesic dose of muscimol, a specific GABAA agonist, showed an enhanced effect. Moreover, pretreatment with GABAergic substances like pentobarbitone also showed a facilitatory effect on BZ-induced analgesia. On the other hand, a combination of clonazepam with baclofen, a specific GABAB agonist, failed to show any synergistic effect. The analgesic effect of central type BZ-receptor agonists was found to be bicuculline reversible. It is concluded that GABAA receptor activation has a modulatory role in the naloxone sensitive analgesic effect of central type BZ-receptor agonists.

Analgesics↗

PubMed1986

Comparative pharmacology of 'non-opioid' analgesics.

Pain is the most prominent symptom of disease in man and analgesics are the most widely used drugs. More than 90% of the analgesics used belong to the so-called peripherally acting, non-opioid (non-narcotic) or mild analgesics. They all derive from 3 types of compounds: aspirin and other acidic non-steroidal anti-inflammatory drugs (NSAIDs), aniline derivatives such as paracetamol (acetaminophen) and non-acidic pyrazole drugs like propyphenazone and dipyrone (metamizole). These compounds and all of their derivatives differ in their analgesic activity and their typical profile of side effects. While NSAIDs are particularly useful in the treatment of pain related to inflammation these compounds are well known to cause gastrointestinal, haematological and kidney side effects. Aniline derivatives such as paracetamol are not very effective analgesics, but reasonably good antipyretics. These compounds, unlike aspirin-like drugs, do not interfere with inflammatory pain. Their main side effects are allergic but, particularly at overdose, they cause liver and kidney damage. Rarely, they have also been associated with kidney damage and malignomas of the urinary system after long term administration. Non-acidic pyrazole drugs are supposedly particularly active in pain originating from spasms of smooth muscles. They are not very effective anti-inflammatory drugs but are good antipyretics. Their major side effects consist of mild allergic reactions. They have also rarely been associated with agranulocytosis and shock. In addition to these differences in therapeutic application and side effect profile the major representatives of the groups of analgesics mentioned differ in their pharmacokinetic behaviour in the human body. Aspirin shows non-linear pharmacokinetics not seen with ibuprofen, a more modern NSAID.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetaminophen↗

PubMed1986

Renal toxicity of non-narcotic analgesics. At-risk patients and prescribing applications.

Acute and chronic renal damage may occur with many analgesics. Acute effects on the kidney occur mainly with aspirin and other non-steroidal anti-inflammatory drugs (NSAIDs). One of the most obvious effects in healthy individuals is fluid retention which is thought to be mediated through inhibition of the renal effects of prostaglandins. Aspirin and NSAIDs also cause a decrease in glomerular filtration rate and renal blood flow and although these changes may occur in healthy individuals they are more pronounced in high renin states and in patients with pre-existing renal disease. Clinical syndromes associated with the renal effects of NSAIDs include oedema, acute renal failure and the nephrotic syndrome. Advanced age, dehydration, concurrent diuretic use and pre-existing renal disease are risk factors for these syndromes. Chronic effects of non-narcotic analgesics on the kidney were suspected before their acute effects became apparent. The key chronic renal lesion in the kidney attributed to prolonged ingestion of non-narcotic analgesics is renal papillary necrosis. The incidence of analgesic-associated renal papillary necrosis in different countries has generally paralleled the national regular use of analgesics. Although phenacetin was widely implicated as the cause of renal papillary necrosis, there is now increasing evidence that aspirin and other NSAIDs may cause renal papillary necrosis in patients who have not taken phenacetin. There is some evidence that this problem is reduced by legislative control of over-the-counter sales. Uroepithelial tumours have also been attributed to chronic abuse of analgesic mixtures. Such tumours are characterised by a reversal of the usual sex ratio, being more common in females.

Acute Kidney Injury↗

PubMed1986

Modification of the analgesic effect and the effect on body temperature of morphine and fentanyl, included in liposomal suspensions.

The analgesic and thermomodulating effect of the powerful narcotic analgesics morphine and phentanyl, included in liposomal suspensions, was tested in experiments on rats and rabbits. The aim of the experiments was to determine the changes taking place in these effects of the above analgesics, using as their carriers small neutral liposomes formed by phosphatidylcholine (egg lecithin) and cholesterol in molar ratio 7:2. The liposomes were obtained by applying the classical method of A. Bangham (1968), with subsequent ultrasoundtreatment. The changes in the body temperature of the rats and rabbits were traced in dynamics by means of electrothermometry. The analgesic activity was also investigated in dynamics, using two methods: thermal stimulation ("tail flick" test) and mechanical pressure (after Randall-Selitto, 1957). Incorporation of morphin and Fentanyl in liposomal suspensions was found to result in a tendency towards intensification and statistically significant prolongation of their thermomodulating and analgesic effects, compared with these effects of the free preparations. The pharmacological investigations carried out reveal considerable possibilities for a clinically favourable modification of the effects of the narcotic analgesics by means of their incorporation in liposomal carriers.

Analgesics↗