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PubMedDate not supplied

[The effect of cholinergic agents on the analgesic effect of nonnarcotic analgesics].

The effect of cholinergic agents on the analgetic effect of analgin (pyrazoline derivative) and chemical compounds (quinazoline and triazole derivatives) has been studied in experiments on white mice using a "hot plate" technique. It has been found that an M-cholinomimetic pilocarpine decreases pain sensitivity and enhances considerably the analgetic effect of non-narcotic analgesics, especially that of quinazoline and triazole derivatives. At high doses (10 mg/kg) pilocarpine increases drastically the toxicity of analgin. Contrastingly, an M-cholinoblocker atropine does not affect considerably the pain sensitivity, however blocks completely the analgetic effect of all the drugs studied. The role of cholinergic mechanisms in the maintenance of pain sensitivity level and the onset of the analgetic effect of non-narcotic analgesics as well as the clinical value of the data obtained are discussed.

Aminopyrine↗
PubMed1981

An evaluation of the analgesic efficacy of three opioid-analgesic combinations in postoperative oral surgery pain.

The analgesic efficacy of a hydrocodone-acetaminophen combination, a codeine-acetaminophen combination, a codeine-APC (aspirin, phenacetin, and caffeine) combination, and a placebo was evaluated in outpatients who had moderate or severe pain after the surgical removal of impacted third molars. Each of the active medications had a significant effect on essentially all measures of total and peak analgesia; they did not differ significantly on any measure of analgesia. Adverse effects were transitory and, in general, appear to have been related to the centrally acting component of each combination analgesic.

Acetaminophen↗
PubMed1998

[Non-opioid analgesics and co-analgesics in therapy of chronic pain].

Efficacy and side effects of non-opioid-analgesics were analysed in a standardized review of placebo-controlled or double-blind studies. In rheumatoid arthritis, ibuprofen showed the best ratio of effectiveness and side-effects. Naproxen, diclofenac and meloxicam may serve as alternatives. In osteoarthritis, naproxen seems to be superior to diflunisal, meloxicam and diclofenac. In cancer pain, ibuprofen is the treatment of the first choice followed by naproxen and diclofenac. No sufficient data on non-opioids in neuropathic pain were available. The dose administered in the management of chronic pain should be low in order to reduce the incidence of side-effects. The frequency of side-effect-related discontinuation of chronic pain medication was calculated as follows: ibuprofen 3.8%, aspirin 4.7%, piroxicam 4.8%, naproxen 7.4%, meloxicam 13.0% and diclofenac 17.8%. Since differences in efficacy were not clinically relevant, the indication for a special non-opioid-analgesic medication should focus on the prevention of side-effects.

Analgesics↗
PubMed1990

Analgesic and antiinflammatory effects of glucamethacin (a nonsteroidal antiinflammatory analgesic) after the removal of impacted third molars.

A double-blind study was undertaken to compare the effects of glucamethacin, aspirin, and placebo in the control of pain, trismus, and postoperative swelling of 59 outpatients who underwent the surgical removal of impacted lower third molars. Aspirin (1000 mg three times a day) was superior to placebo in one of the analgesic parameters studied, whereas glucamethacin (140 mg three times a day) was not superior to placebo. Both drugs significantly reduced the occurrence of trismus on the day after surgery, but no differences with placebo were found 48 hours postoperatively. In the study of postoperative swelling, no significant differences were found between the medications and the placebo in the postoperative period. It is concluded that glucamethacin, a nonsteroidal antiinflammatory drug, produces a minimal analgesic effect and does not relieve postoperative swelling in the dental patient undergoing surgical removal of impacted third molars.

Adolescent↗
PubMed1981

Analgesic tolerance produced by morphine pellets is facilitated by analgesic testing.

Analgesic tolerance induced by morphine pellets was examined in rats using the nociceptive tail flick reflex. Analgesic responses of animals who received preliminary tail flick tests after morphine implantation were significantly lower than responses of naive, nontested animals. Previously tested animals were also significantly more tolerant to a morphine challenge than nontested animals. A dose response curve to morphine was not obtained, at the doses used here, from previously tested animals, where as naive animals responded to in a dose dependent manner. Environmental modulation of the tail flick represents an elementary form of behavioral plasticity which may prove useful for neural analyses of simple reflex systems.

Analgesia↗
PubMed1976

A double-blind clinical trial of the analgesic effects of R & S 218-M, a new potent analgesic for the relief or pain following abdominal surgery: comparison with morphine sulphate.

The analgesic effects of R & S 218-M, administered in doses of 0.56 mg/70 kg and 0.35 mg/70 kg, were compared with those of morphine sulphate 10.5 mg/70 kg for the relief of abdominal pain following surgery in healthy adults. The drugs were given as the first potent analgesic after operation and the subjects were interviewed at 30-min intervals until the pain became severe again. All the interviews were conducted by the one observer. R & S 218-M 0.56 mg/70 kg was as effective as morphine sulfate 10.5 mg/70 kg, while R & S 218-M 0.35 mg/70 kg was inferior. No evidence was found to support the claim that R & S 218-M causes less respiratory depression when compared with morphine sulphate.

Abdomen↗
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↗
PubMed1989

Do local analgesics injected at the time of third molar removal under general anaesthesia reduce significantly post operative analgesic requirements? A double-blind controlled trial.

A prospective, controlled, randomised, double-blind trial suggested that: 1. The use of bupivacaine 0.5% plain and prilocaine 3% with felypressin 0.03 i.u./ml. as peroperative local analgesics reduce postoperative pain scores recorded on the first postoperative morning (P less than 0.05). 2. Bupivacaine 0.5% plain reduces postoperative opiate requirements (P less than 0.025). 3. Patients do not find peroperative bilateral inferior alveolar and lingual nerve blocks with buccal infiltrations significantly unpleasant. Thus peri-operative bupivacaine 0.5% is a valuable adjunct to third molar removal under general anaesthesia.

Adolescent↗
PubMed1998

Analgesics in the management of chronic pain. Part Three: Step 2 analgesic drug therapy.

In this, the third article in the series, the role of analgesic drugs appropriate for the treatment of moderate to severe pain is reviewed along with therapies frequently applied in the treatment of poorly responsive neurogenic pain. The article should be read in conjunction with part one outlining general principles in the management of chronic pain.

Analgesics, Opioid↗
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↗
PubMed1987

Analgesic dipeptide derivatives. 3. Synthesis and structure-activity relationships of o-nitrophenyl-modified analogues of the analgesic compound H-Lys-Trp(NPS)-OMe.

A series of analogues of the analgesic dipeptide derivative H-Lys-Trp(NPS)-OMe has been designed to determine the influence of the (2-nitrophenyl)sulfenyl (NPS) moiety on the activity. The syntheses and antinociceptive effects of these analogues of general formula H-Lys-Trp(R)-OMe [R = phenylsulfenyl (PS) (9); R = (2-carbomethyoxyphenyl)sulfenyl (CmPS) (10); R = (4-nitrophenyl)sulfenyl (pNPS) (11); R = (2,4-dinitrophenyl)sulfenyl (DNPS) (12); R = [2-(acetylamino)-2-carbomethoxyethyl]sulfenyl (AacCmES) (13); R = [2-(acetylamino)phenyl]sulfenyl (AacPS) (17); R = tert-butylsulfenyl (t-BuS) (23); R = (2-carbomethoxyethyl)sulfenyl (CmES) (24)] are described. Reaction of Z-Lys(Z)-Trp-OMe (3) with PS-, CmPS-, pNPS-, DNPS-, and AacCmES-Cl afforded the corresponding 2-(sulfenyl)tryptophan derivatives, which on treatment with boron-tris(trifluoroacetate)/trifluoroacetic acid or trimethylsilyl iodide in acetonitrile (Me3SiI/CH3CN) provided 9-13, respectively. Sulfenylation of 3 with NPS-Cl gave Z-Lys(Z)-Trp(NPS)-OMe, which, on catalytic hydrogenation of the nitro group using 10% Pd/C followed by acetylation of the resulting amino function and removal of the protecting Z groups, gave 17. Condensation of 2-(tert-butylsulfenyl)- and 2-[(2-carbomethoxyethyl)sulfenyl]tryptophan methyl ester, obtained by reaction of methyl 3a-hydroxy-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indole-2-carboxyla te with the corresponding thiol, with Z-Lys(Z)-OSu afforded Z-Lys(Z)-Trp(t-BuS)-OMe and Z-Lys(Z)-Trp(CmES)-OMe, which on treatment with Me3SiI/CH3CN provided 23 and 24, respectively. Intracerebroventricular administration of 10 elicited a naloxone-reversible antinociceptive effect in mice similar to that of H-Lys-Trp(NPS)-OMe. No analgesia was however found with the phenylsulfenyl or acyclic sulfenyl substituted dipeptides 9, 11, and 17 or 13, 23, and 24. The Trp(DNPS)-containing analogue was neurotoxic. Structure-activity studies indicate that the role of the NPS and CmPS moieties could be related to the adoption of a preferential active conformation.

Analgesics↗
PubMed1988

Analgesic dipeptide derivatives. 4. Linear and cyclic analogues of the analgesic compounds arginyl-2-[(o-nitrophenyl)sulfenyl]tryptophan and lysyl-2-[(o-nitrophenyl)sulfenyl]tryptophan.

The syntheses of Trp(Nps)-Arg-OMe.HCl (15) [Trp(Nps) = 2-[(o-nitrophenyl)sulfenyl]tryptophan], its three stereoisomers, and their corresponding cyclic analogues are reported. The preparation of Trp(Nps)-Lys-OMe (19) and its cyclic analogue is also described. All these compounds have been designed as analogues of the analgesic dipeptide derivatives X-Trp(Nps)-OMe (1b, X = Arg; 2b, X = Lys). In the case of dipeptides containing Arg or D-Arg, the coupling reactions were achieved via the isobutyl chloroformate and N-methylmorpholine mediated mixed anhydride procedure, while in the case of the Lys analogue, the N,N-dicyclohexylcarbodiimide method was employed. Sulfenylation reactions were carried out with Nps-Cl in acidic media. Cyclization to the diketopiperazines was achieved by using acetic acid as catalyst. The antinociceptive effects of all these new Trp(Nps)-containing dipeptides were evaluated after icv administration in mice, and the effects were compared with those of 1b, 2b, Tyr-Arg (Kyotorphin), and Tyr-D-Arg. The most active compounds, 15 and 19, were found to exhibit a naloxone-reversible antinociceptive effect similar to those of 1b and 2b and approximately 50 and 12.5 times higher than those of Kyotorphin and its D isomer, respectively. Trp(Nps)-D-Arg-OMe.HC1, D-Trp(Nps)-Arg-OMe.HC1, and cyclo[Trp(Nps)-Arg].HC1 were also more effective than Kyotorphin (5, 10, and 10 times, respectively). In view of the structure-activity relationships obtained, several similarities between this series of Trp(Nps)-containing dipeptides and that of Kyotorphin analogues have emerged.

Analgesics↗
PubMed1989

Transdermal delivery of narcotic analgesics: comparative permeabilities of narcotic analgesics through human cadaver skin.

Relationships between the in vitro permeation rates of select narcotic analgesics through human skin and their physicochemical properties were investigated by following the permeation kinetics of six representative compounds in small diffusion cells. The relative permeability coefficients of three phenylpiperidine analogues, meperidine, fentanyl, and sufentanil, all measured on a single piece of skin, were 3.7 x 10(-3), 5.6 x 10(-3), and 1.2 x 10(-2) cm/hr, respectively. Using membranes from the same skin section, the permeability coefficients of three opioid alkaloids, morphine, codeine, and hydromorphone, were considerably lower, at 9.3 x 10(-6), 4.9 x 10(-5), and 1.4 x 10(-5) cm/hr, respectively. The high permeability coefficients of the former compounds are due to their highly lipophilic nature as reflected in high octanol/water partition coefficients and low solubility parameters. Generally, the permeability coefficients of the narcotics increase as the lipophilicity increases. When viewed in literature perspective, the data suggest that aqueous tissue control of transport is approached in the case of the phenylpiperidine analogues, all of which have Koctanol/water values greater than 40. Permeability coefficients of fentanyl and sufentanil were also determined as a function of pH over the pH range 7.4 to 9.4, in this instance with membranes prepared from additional samples of skin. The permeability coefficients of each drug varied less than threefold over the pH range, a behavior consistent with the highly hydrophobic natures of the compounds. The low permeability coefficients of morphine, codeine, and hydromorphone coupled with their low potencies make these drugs poor transdermal candidates. It appears that fentanyl and sufentanil can be successfully transdermally delivered.

Administration, Cutaneous↗
PubMed1983

Site of analgesic action of zomepirac sodium, a potent non-narcotic analgesic in experimental animals.

Zomepirac sodium inhibited the reflex hypertension caused by an injection of bradykinin into the splenic artery of anaesthetized dogs, but not that by injection of bradykinin plus PGE1. In the rat acetic acid writhing test, the potency ratio of intraperitoneal (ED50 = 0.41 microgram/kg) to intravenous (ED50 = 33.5 micrograms/kg) anti-writhing activity of zomepirac sodium was 79.2 (37.1-173), though the ratio of codeine phosphate (373 micrograms/kg, i.p., 352 micrograms/kg, i.v.) was 0.934. When equipotent doses of zomepirac sodium were administered to rats receiving intraperitoneally acetic acid, the plasma zomepirac level after i.v. administration was more than 200 times that after i.p. administration, while the peritoneal exudate zomepirac contents were nearly equal after administration by both routes. Zomepirac sodium (5 micrograms/kg) did not produce significant anti-writhing activity after intracerebroventricular administration. From these results, it was suggested that zomepirac sodium produced analgesic action through a strong blockade of the hyperalgesia in the peripheral system.

Alprostadil↗
PubMedDate not supplied

[The analgesic action of narcotic analgesics and clopheline after the ionizing irradiation of rats].

The ionizing radiation (150 Gy) extended the rat tail flick latency, decreased the pain-relief effects of morphine and opioids and enhanced the analgesic effect of clopheline. The radiation was followed by a decrease of vocalization threshold with a reduction of morphine- and clopheline-induced analgesia. Naloxone (0.1 mg/kg) eliminated the postradiation analgesia and did not change the hyperalgesic effect of the radiation.

Analgesics, Opioid↗
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↗