Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “ANALGESICS”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 505 records · Page 28Linked to original sources
PubMed2004

Analgesic effect of dextromethorphan in neuropathic pain.

BACKGROUND: Dextromethorphan, a clinically available N-methyl-D-aspartic acid (NMDA) receptor antagonist, has an analgesic effect in patients with diabetic neuropathy. The aim of this study was to evaluate the analgesic and adverse effects of a single high dose of dextromethorphan on spontaneous pain in patients suffering long-term neuropathic pain of traumatic origin. METHODS: Fifteen patients with post-traumatic neuropathic pain participated in this placebo-controlled, double-blind, randomized crossover study. On two separate occasions, the participants received 270 mg of dextromethorphan hydrobromide or placebo. Pain intensity, adverse effects and serum concentrations of dextromethorphan and metabolites were registered. RESULTS: Dextromethorphan had a statistically significant analgesic effect compared with placebo, but the effect varied markedly among the patients. Light-headedness was the most important adverse effect reported. Extensive metabolizers of dextromethorphan had an apparently better analgesic effect than poor metabolizers. CONCLUSION: This report indicates that a single high dose of dextromethorphan has an analgesic effect in patients with neuropathic pain of traumatic origin. The main metabolite dextrorphan seems to be important for the analgesic effect. At the relatively high dose studied, the clinical usefulness of dextromethorphan is limited to that portion of the patient population experiencing analgesia without an unacceptable level of adverse effects.

Adult↗
PubMed1980

Clinical evaluation of mild analgesics.

1 Mild analgesics pose particular problems in evaluation because of difficulty in getting suitable patients, the frequent use of oral administration and their long-term use. 2 Despite their limitations it is possible to quantify both pain severity and pain relief using either 'pain scores' or 'visual analogues'. 3 A trained observer can add information in addition to the patient's interpretation of pain. 4 There are particular problems using crossover studies with analgesics and the sequential method of evaluating results is not as useful with mild analgesics as with more potent drugs. 5 Opinions differ as to the importance of dummy medication in the study of analgesic drugs; difficulties may arise from ethical as well as practical reasons. 6 In the overall evaluation of mild analgesics it is important to consider their long term side effects. 7 Access to a large number of patients with a constant pain of 6-8 h duration and a smaller number with long-term pain is the most important prerequisite in the evaluation of mild analgesic drugs.

Analgesics↗
PubMed1980

Mild analgesics in postoperative pain.

1 The intensity of postoperative pain is influenced by many factors, for example, individual variation, site of incision and type of operation, anaesthetic technique, and the interval from the end of operation to the appearance of pain. 2 These factors affect the efficacy of analgesics. 3 Mild analgesics provide adequate pain relief in half of our patients in the immediate postoperative phase when the pain is slight to moderate. 4 The maximum effect of mild analgesics corresponds to that produced by morphine 6-10 mg. Adequate analgesia may not therefore be provided for the treatment of severe postoperative pain unless narcotic analgesics have been used peroperatively. 5 When mild analgesics are combined with narcotics synergism is achieved. 6 As postoperative pain decreases with time, mild analgesics usually provide adequate pain relief on the first and following postoperative days.

Analgesics↗
PubMed1980

Abuse and paradoxical effects of analgesic drug mixtures.

1 In patients with chronic pain, two types of analgesic drug dependence occur, that is, dependence of the barbiturate-type and of the morphine-type. Eighty cases of analgesic drug dependence of the barbiturate-type were examined. All these patients were dependent on drug combinations, not a single patient being on one analgesic alone. 2 Psychotropic agents were found to be the common pharmacological denominator of all abused preparations. These findings confirm the hypothesis that the addition of psychotropic or dependence-producing substances to analgesics is the crucial factor in the complex of mild analgesic drug abuse. 3 One group of patients with chronic pain, who were dependent on analgesic drug mixtures, had both lowered experimental pain thresholds and tolerances. After drug withdrawal, these parameters showed a tendency to increase in some patients.

Adult↗
PubMed1996

Effects of pH and buffer capacity modulation on the analgesic efficacy of lignocaine and pethidine solutions.

BACKGROUND: Objectives were to study the effects of variations in the pH and the buffer capacity of solutions of lignocaine or pethidine on their analgesic efficacy in peripheral nerve block. METHODS: Infraorbital nerve blocks (IONB) were induced in rats during light pentobarbitone anaesthesia employing 0.2 ml of test solutions containing 10 mg center dot ml-1 of lignocaine or pethidine dissolved in normal saline, 50 mmol and 150 mmol tris-hydroxymethylaminomethane (THAM) hydrochloride (THAM center dot HCl) of pH 4.8 and 4.5, respectively, or 100 mmol THAM + THAM center dot HCl of pH 7.4. The pH of solutions in saline was varied from 3.0 to 9.3 by adding HCl or NaHCO3. The analgesic efficacy is expressed as the interval from injection to elicitation of a minimal response to electric stimulation at various intensities (threshold intensities) within the blocked area (IONB 3 to 10), and in terms of the area under the curve (AUC, threshold intensities vs. time). RESULTS: When dissolved in saline, pH 7.4, pethidine exerted more pronounced effects than lignocaine [AUC by 3.5 times (P<0.001), IONB 3 to 10 by 2.7 (P<0.05) to 3.6 (P<0.001) times]. Variations of the pH of solutions did not affect their analgesic efficacy. Lignocaine exerted more pronounced local analgesic effects when mixed with 150 mmol THAM center dot HCl than when mixed with saline (pH 7.4), but manifested even more pronounced effects when dissolved in THAM + THAM center dot HCl [AUC by 3.7 times (P<0.001), IONB 3 to 10 by 2.7 (P<0.01) to 3.8 (P<0.001) times]. When dissolved in THAM + THAM center dot HCl, the analgesic efficacy of pethidine increased by 2.0 to 2.8 times (P<0.001), as compared to a solution in saline at the same pH. CONCLUSIONS: It is concluded that variations in the pH of solutions of lignocaine or pethidine in saline does not affect the analgesic efficacy of the drugs, presumably due to the low buffer capacity of the medium, whereas when dissolved in THAM + THAM center dot HCl, their effect is enhanced.

Analgesics, Opioid↗
PubMed2006

Geographic variation in the prescription of schedule II opioid analgesics among outpatients in the United States.

OBJECTIVE: To measure geographic variation in opioid use in a large, commercially insured, outpatient population in the United States. DATA SOURCES: Outpatient prescription drug claims database of a national pharmaceutical benefit manager for 7,873,337 subjects with at least one prescription drug claim in 2000. STUDY DESIGN: We measured the period prevalence of claims for opioid analgesics and controlled-release oxycodone at the state level. We measured geographic variation using the weighted coefficient of variation and systematic component of variation. In county-level multivariable regression, we explored associations between potential explanatory variables and claims for opioid analgesics and controlled-release oxycodone. PRINCIPAL FINDINGS: A total of 567,778 (64.2 per 1,000 total claims) were for oral opioid analgesics. Claim rates by state ranged from <20 to >100 claims per 1,000 total claims. States with long-standing prescription monitoring programs had among the lowest rates. In the county-level data, presence of a statewide prescription monitoring program and proportions of the population aged 15-24 and 65 years and older were independently and negatively associated with claim rates for all opioid analgesics. Surgeons per 1,000, proportion of the population reporting illicit drug use, and proportion who were female were independently and positively associated with claim rates for all opioid analgesics. Only the proportion of the population aged 25-34 and number of surgeons per 1,000 were independently and positively associated with claim rates for oxycodone. CONCLUSIONS: Claim rates for opioid analgesics vary significantly by state. Presence of a statewide prescription monitoring program is associated with lower claim rates at the county level. Future research should use individual-level data to assess whether these findings reflect a reduction in abuse and diversion or suboptimal treatment of pain.

Adolescent↗
PubMed2005

Postoperative analgesic requirements - total laparoscopic hysterectomy versus vaginal hysterectomy.

BACKGROUND: There is limited information available on the requirement for postoperative analgesic drugs in patients submitted to total laparoscopic hysterectomy (TLH) compared with patients undergoing vaginal hysterectomy (VH). AIM: To compare the postoperative analgesic requirements in patients who underwent a TLH with patients who had a VH. METHODS: Chart review of 53 patients who had TLH and 47 who had VH and were seen postoperatively by an acute pain management service in order to assess postoperative analgesic requirements. Patient controlled analgesia (PCA) was part of the standard protocol for postoperative pain management. Analgesic requirement was recorded as the mean doses of morphine and number of days that patients used non-steroidal anti-inflammatory drugs (NSAIDs), oxycodone and tramadol. RESULTS: The requirement for total morphine was approximately half the dose in patients who had a TLH (10.8 +/- 12.6 mg) compared with patients who had a VH (19.4 +/- 21.9 mg) (P 0.017). The length of use of NSAIDs was significantly reduced in patients who had undergone a TLH (2.0 +/- 0.95 days) as compared with patients who had a VH (2.85 +/- 1.1 days) (P < 0.0001). CONCLUSIONS: Patients submitted to TLH require less postoperative analgesic drugs when compared with patients who had VH. Prospective randomised trials are warranted to compare analgesic requirements between patients submitted to TLH and VH.

Adult↗
PubMed2002

Dihydroetorphine: a potent analgesic: pharmacology, toxicology, pharmacokinetics, and clinical effects.

Dihydroetorphine (DHE) is one of the strongest analgesic opioid alkaloids known; it is 1000 to 12000 times more potent than morphine. Several in vitro and in vivo studies have shown that DHE is a selective mu-opioid receptor (OP(3)) agonist that also binds and activates all human recombinant mu-, delta-, and kappa-opioid receptors (OP(3), OP(1), and OP(2)). The onset of the analgesic effect of DHE in rodents is rapid, 5 to 15 min after parenteral administration; the duration of action is short, the analgesic effect disappears within 120 min after administration. By oral administration much higher doses of DHE are required to produce analgesic effects. These characteristics are accounted for by the pharmacokinetic properties of DHE in the rat, namely, by rapid distribution of DHE from the injection site to the brain and rapid metabolism by glucuronidation in the gut and liver followed by elimination into the bile. Continuous infusion and repeated administration of DHE lead to the development of tolerance to analgesia, physical dependence, and a rewarding effect in normal rats but not in animals with formalin-induced inflammation. Although formalin-induced inflammation is only one type of pain stimulus, these findings suggest that DHE addiction would be observed only in the case of pain-free conditions. Clinical reports in China show that sublingual doses of DHE, 20 to 180 microg, produce a potent analgesic effect with only mild side effects, including dizziness, somnolence, nausea, vomiting, constipation, and shortness of breath. To improve the short-lasting effect following sublingual administration, transdermal delivery of DHE via a patch has been investigated. The patch formulation of DHE produces continuous analgesic effect with minimal physical dependence and rewarding effect in rats suffering from chronic pain. This patch formulation, which is very suitable for DHE, may be viable for the treatment of severe pain and is likely to improve patients' quality of life.

Administration, Cutaneous↗
PubMed1989

Narcotic analgesics, their detection and pain measurement in the horse: a review.

Narcotic analgesics produce pharmacological effects by interacting with specific opiate receptors. At least five major types of opiate receptors have been recognised. These include mu (morphine) and kappa (ethylketazocine) receptor types. Narcotic analgesics which interact with mu receptors produce locomotor and autonomic stimulation at doses that produce little or no analgesia. Therefore, use of these drugs as analgesics in equine medicine has not been very satisfactory. Theoretical considerations suggested that the role of kappa agonists in equine analgesia be investigated. Using a pure kappa agonist, U-50, 488H, good analgesia was produced in the horse with little or no locomotor stimulation or autonomic effects. These data suggest that kappa agonists may be superior analgesics for clinical use in the horse. On the other hand, the locomotor stimulant effects of mu agonist analgesics enable their use as illegal medications. Specifically, these agents produce a good running response, signs of central nervous stimulation and analgesia, all potentially useful effects in a racehorse. Regulatory control of most narcotic analgesics can be obtained by high performance thin layer chromatographic screening. However, effective screening for the fentanyls and small doses of etorphine can only be achieved by use of immunoassay.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMedDate not supplied

Oral provocation test in the diagnosis of anaphylactoid reactions to 'mild' analgesic preparations.

'Mild' analgesic preparations (MAPs) are well known elicitors of anaphylactoid reactions (ARs). The identification of the causative agent is often difficult since reliable skin tests or in vitro methods are not available. In 128 patients (32 males, 96 females) with a history of ARs to MAPs containing only one single analgesic compound, placebo-controlled oral provocation tests (OPTs) were performed. Among 100 of them undergoing the OPT with the suspected drug, there was a concordance between the patient's history and the OPT in 44 patients. Concomitant ARs to other mild analgesics (without a history of previous incompatibility) were observed in 113 of 413 OPTs, but in almost all cases one or more alternative analgesics were tolerated in the OPT. Our results confirm that the OPT remains at present the most reliable diagnostic procedure alongside a comprehensive history in patients with ARs to MAPs. Because many of the patients showed concomitant ARs to unsuspicious analgesics OPTs should include a standard battery of different analgesics. The simple recommendation of one single preparation, such as acetaminophen, as a 'safe' substitute without an OPT is not recommended.

Administration, Oral↗
PubMed1978

Nephropathies due to analgesics.

Analgesic drugs causing kidney functional disturbances and histologically evident kidney derangements are reviewed. Today, not the pathological changes, which have dominated the scene of pathogenesis for analgesic nephropathies are in the foreground of investigative interest, but rather the biochemical interactions of analgesics or their metabolites in the renal cell and prospective epidemiologic studies. As the term 'phenacetin nephropathy' has been replaced by 'analgesic nephropathy', it seems likely that metabolic activation responsible for renal injury caused by analgesic mixtures will be of primary importance in furture investigations as well as the unravelling of immunogenic processes for a variety of analgesics and their metabolites.

Acetaminophen↗
PubMed2003

Low-dose methadone has an analgesic effect in neuropathic pain: a double-blind randomized controlled crossover trial.

The analgesic effectiveness and adverse effect incidence of a daily dose of 10 or 20 mg of oral methadone were evaluated in 18 patients with a diverse range of chronic neuropathic pain syndromes, who had all responded poorly to traditional analgesic regimens. Analgesia was seen after each dose of methadone. As compared with placebo, the 20 mg daily dose (given as 10 mg bd) resulted in statistically significant (P = 0.013-0.020) improvements in patient Visual Analogue Scale ratings of maximum pain intensity, average pain intensity and pain relief, recorded at the same time daily. The analgesic effects extended over 48 hours, as shown by statistically significant (P = 0.013-0.020) improvements in all three outcomes on the rest days instituted between each daily dose. Analgesic effects (lowered maximum pain intensity and increased pain relief, on the day of dosing only) were also seen when the lower daily dose of 10 mg methadone (given as 5 mg bd) was used, but these failed to reach statistical significance (P = 0.064 and 0.065, respectively). Interpatient analysis showed that the analgesic effects were not restricted to any particular type of neuropathic pain. Patient compliance was high throughout the trial. One patient withdrew during the 10 mg and six during the 20 mg methadone treatment periods. This is the first double-blind randomized controlled trial to demonstrate that methadone has an analgesic effect in neuropathic pain.

Adult↗
PubMed2005

Opioid peptide-derived analgesics.

Two recent developments of opioid peptide-based analgesics are reviewed. The first part of the review discusses the dermorphin-derived, cationic-aromatic tetrapeptide H-Dmt-D-Arg-Phe-Lys-NH(2) ([Dmt(1)]DALDA, where Dmt indicates 2',6'-dimethyltyrosine), which showed subnanomolar mu receptor binding affinity, extraordinary mu receptor selectivity, and high mu agonist potency in vitro. In vivo, [Dmt(1)]DALDA looked promising as a spinal analgesic because of its extraordinary antinociceptive effect (3000 times more potent than morphine) in the mouse tail-flick assay, long duration of action (4 times longer than morphine), and lack of effect on respiration. Unexpectedly, [Dmt(1)]DALDA also turned out to be a potent and long-acting analgesic in the tail-flick test when given subcutaneously (s.c.), indicating that it is capable of crossing the blood-brain barrier. Furthermore, little or no cross-tolerance was observed with s.c. [Dmt(1)]DALDA in morphine-tolerant mice. The second part of the review concerns the development of mixed mu agonist/delta antagonists that, on the basis of much evidence, are expected to be analgesics with a low propensity to produce tolerance and physical dependence. The prototype pseudopeptide H-Dmt-TicPsi[CH(2)NH]Phe-Phe-NH(2) (DIPP-NH(2)[Psi], where Tic indicates 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) showed subnanomolar mu and delta receptor binding affinities and the desired mu agonist/delta antagonist profile in vitro. DIPP-NH(2)[Psi] produced a potent analgesic effect after intracerebroventricular administration in the rat tail-flick assay, no physical dependence, and less tolerance than morphine. The results obtained with DIPP-NH(2)[Psi] indicate that mixed mu agonist/delta antagonists look promising as analgesic drug candidates, but compounds with this profile that are systemically active still need to be developed.

Analgesics, Opioid↗
PubMed2006

Role of the opioidergic system and nitric oxide in the analgesic effect of venlafaxine.

The noradrenalin and serotonin re-uptake inhibitor venlafaxine has an analgesic effect that is independent of its antidepressant activity; however, the mechanism of this effect remains to be elucidated. This study was performed to investigate the possible roles of the opioidergic system and nitric oxide (NO) pathway in the analgesic effect of venlafaxine. Eighty Wistar rats of both sexes were allocated to 10 groups. The hot plate test was used to assess the antinociceptive/analgesic effect. The temperature of the hot plate was adjusted to 52.5+/-1 degrees C, the cut-off period was set to be 50 sec; licking of the hind paw was used as a sign of pain perception. Venlafaxine alone (25 mg/kg) showed marked analgesic activity (p<0.05). N-omega-nitro-L-arginine (L-NOARG) alone (20 mg/kg) and naloxone alone (2 mg/kg and 4 mg/kg) showed no analgesic activity (p>0.05). Coadministration of low-dose naloxone (2 mg/kg) and both doses of L-NOARG (20 and 40 mg/kg) with venlafaxine (25 mg/kg) did not modify the analgesic effect but high-dose naloxone (4 mg/kg) decreased it significantly (p<0.05). In conclusion, these results suggest that the opioidergic system but not the NO pathway has a role in the analgesic effect of venlafaxine.

Analgesics↗
PubMed1990

[Analgesic activity of morphine suppository in rats].

Analgesic activity of morphine administered rectally as a suppository was investigated in rats in order to ascertain analgesic activity of morphine suppository. Morphine hydrochloride given rectally as a suppository produced analgesic activity in a dose-related manner in the tail pressure and acetic acid-induced writhing tests, and its potency (ED50 = about 17 and 0.689 mg/kg, respectively) was approximately twice that of morphine hydrochloride administered orally as an aqueous solution. The analgesic action was as durable as that of oral morphine, but its onset was faster. The plasma and brain levels of morphine reached peak until 30 min after rectal administration of morphine suppository, and these time-courses approximately corresponded with that of the analgesic action. These results suggest that morphine given rectally to rats as a suppository produces analgesic action equivalent or superior to orally administered morphine after absorption from the rectum.

Analgesics↗
PubMed1993

[Analgesic effect of benzoylmesaconine].

"Tsumura Shuchi-Bushi Powder for Ethical Dispensing" (TJ-3021) is an herbal drug of processed Aconiti tuber that attenuates its toxicity. A greater part of mesaconitine which is regarded as a main analgesic component in processed Aconiti tuber is hydrolyzed into benzoylmesconine (BM) by its processing. In this study, the analgesic effect of BM was examined in comparison with that of TJ-3021 in mice and rats. BM (10 mg/kg, p.o.) depressed the acetic acid-induced writhing significantly. Its analgesic activity was almost similar in magnitude to that of TJ-3021 (300 mg/kg, p.o.). BM (30 mg/kg, p.o.) significantly increased the pain threshold ratio of paw pressure in repeated cold stress (RCS) rats, and its analgesic potency appeared to be equivalent to that of TJ-3021 (1000 mg/kg, p.o.). These results suggest that the analgesic activity of BM is strong enough for explanation of the analgesic effect of TJ-3021, and it might contribute to that of TJ-3021.

Aconitine↗
PubMed1988

[Experimental knee pain model in rats and analgesic effect of sodium hyaluronate (SPH)].

Using the model of knee pain reaction induced by intra-articular injection of endogenous pain substances, especially bradykinin (BK) in rats, the mechanism of the analgesic effect of sodium hyaluronate (SPH) was investigated. The simultaneous administration of prostaglandin E2 with BK or hyaluronidase digestion of endogenous hyaluronic acid (HA) in our experiments brought remarkable hyperalgesia on BK-induced knee pain. These results suggest that higher sensitivity to the pain reaction is induced in a diseased joint (higher prostaglandin content, lower concentration and molecular size of HA in synovial fluid) than in a normal one. SPH definitely decreased BK-induced pain, and its analgesic effect was observed for a longer period, depending on its dose in pre-treatment and the degree of its distribution in synovial tissues. As the analgesic effect of SPH was observed in the hyaluronidase-treated joint as well, it is suggested that the increasing viscosity of synovial fluid caused by increasing HA concentration can decrease the pain even without normalizing molecular size of HA in the joint. HA oligomer and other compounds with similar viscosity or with similar polyanionic character as SPH showed no analgesic effect. From these results, it seems that the characteristic steric configurations of higher molecular HA are needed for the manifestation of the analgesic effect. SPH seems to show its analgesic effect by covering pain receptors in synovial tissues and holding endogenous pain substances in its molecule.

Analgesics↗
PubMed1989

[Pharmacological studies of a non-steroidal analgesic and antipyretic drug of LFP83].

Pharmacological properties of LFP83, a non-steroidal analgesic and antipyretic drug, were studied in mice, rats and rabbits. LFP83 is a prodrug of flurbiprofen (FP) which is its active major metabolite in vivo. In experimental models of acetic acid writhing, the Randall and Selitto method, arthritic pain, yeast fever, LPS fever, carrageenin edema and adjuvant arthritis, LFP83 (i.v.) showed remarkable analgesic, antipyretic and antiinflammatory activities; and it was more potent than ketoprofen (i.m.) and aspirin DL-lysine (i.v.). The analgesic activity of LFP83 was equal to or more potent than that of pentazocine, and its duration was longer than those of aspirin DL-lysine and pentazocine. In addition, the analgesic potency of LFP83 was approximately the same or more potent than that of FP (p.o.), and the onset of this analgesic effect began earlier. On the other hand, the ulcerogenic activity of LFP83 on rat gastric mucosa was less than that of FP (p.o.) in both single and consecutive (7 days) administrations. The safety index (UD50/ED50) of LFP83 was three to ten-fold higher than that of FP (p.o.). As mentioned above, LFP83 is a potent analgesic, antipyretic and antiinflammatory drug; and in comparison to oral FP, it has a more potent and immediate effect, weak gastric irritation and high safety index.

Analgesics↗