• The Korean Journal of Pain
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• 제37권3호
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• pp.211-217
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• 2024

Background: Tolerance to the analgesic effects of opioids and non-steroidal anti-inflammatory drugs (NSAIDs) is a major concern for relieving pain. Thus, it is highly valuable to find new pharmacological strategies for prolonged therapeutic procedures. Biguanide-type drugs such as metformin (MET) are effective for neuroprotection and can be beneficial for addressing opioid tolerance in the treatment of chronic pain. It has been proposed that analgesic tolerance to NSAIDs is mediated by the endogenous opioid system. According to the cross-tolerance between NSAIDs, especially sodium salicylate (SS), and opiates, especially morphine, the objective of this study was to investigate whether MET administration can reduce tolerance to the anti-nociceptive effects of SS. Methods: Fifty-six male Wistar rats were used in this research (weight 200-250 g). For induction of tolerance, SS (300 mg/kg) was injected intraperitoneally for 7 days. During the examination period, animals received MET at doses of 50, 75, or 100 mg/kg for 7 days to evaluate the development of tolerance to the analgesic effect of SS. The hot plate test was used to evaluate the drugs' anti-nociceptive properties. Results: Salicylate injection significantly increased hot plate latency as compared to the control group, but the total analgesic effect of co-treatment with SS + Met50 was stronger than the SS group. Furthermore, the effect of this combination undergoes less analgesic tolerance over time. Conclusions: It can be concluded that MET can reduce the analgesic tolerance that is induced by repeated intraperitoneal injections of SS in Wister rats.

• 생약학회지
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• 제38권1호
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• pp.22-26
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• 2007

Leaves and stem of Viburnum sargentii for. sterile(Caprifoliaceae) has been used as therapeutic agents as a pain of the joints, skin disease as styptics, analgesics for traditional folk medicines. The present study describes the preliminary evaluation of biological activities-analgesic, anti-inflammatory, hepatoprotective activities, of its methanol extract, ethyl acetate fraction and butanol fraction. Among them butanol fraction showed the highest activity in inflammation and writhing test.

• Natural Product Sciences
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• 제5권3호
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• pp.142-147
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• 1999

Tiliacora racemosa Colebr. belonging to the family Menispermaceae is the biggest store-house of diphenyl bisbenzylisoquinoline (DBBI) alkaloids. Exhaustive chemical processing of the root of T. racemosa by the application of modern separation techniques yielded a DBBI alkaloid which was identified as tiliacorine using sophisticated spectroscopic methods (UV, IR, $1^H-NMR$, Mass). Tiliacorine potentiated the sleeping time induced by standard hypnotics viz. chlorpromazine (CPZ), pentobarbitone (PB) and diazepam (DZ) in a dose dependent manner. Tiliacorine potentiated the analgesic action of standard analgesic agents viz., morphine and meperidine. It was also found to possess anti convulsive activity in the strychnine induced convulsion model.

• Journal of Pharmaceutical Investigation
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• 제4권1_2호
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• pp.19-24
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• 1974

The comparative studies were made on the analgesic antipyretic effects of aminopyrine used individually and combined with parasympathetic agents (atropine sulfate). The analgesic antipyretic effects were eximined by Writhing's method to the experimental groups(mouse), and the following effects were found : 1) The active intensity of aminopyrine by it's oral administration combined with atropine sulfate is as follows. Amiinopyrine 80 mg/kg combided with Atropine sulfate 0.005 mg/kg=Aminopyrine 100 mg/kg 2) The most active range of intensity of Atropine sulfate(adjuvant) by it's oral administration is as follows. Atropine sulfate $0.004{\sim}0.005\;mg/kg$.

• Natural Product Sciences
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• 제13권4호
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• pp.347-354
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• 2007

In this study, we investigated the potential of Resina Pini (RP) for anti-inflammatory and analgesic agents to treat inflammatory diseases such as gingivitis and periodontitis. Crude RP (RP1), recrystallized RP (RP2), and Ramus Mori Albae-treated RP (RP3), plus their respective water extracts (RP1-WE, RP2-WE and RP3-WE) were prepared for in vitro and in vivo tests. We couldn't find any signs of heavy metals pollution in all the RP samples. RP2-WE exhibited the highest viability of human gingival fibroblasts (HGF) and the strongest scavenging activity on superoxide anion. RP1, RP2 and RP3, RP2 showed potent scavenging activity on DPPH free radical. RP2-WE displayed a stronger inhibition on hyaluronidase (HAase) activity and RP3 also displayed potent HAase inhibition. RP2-WE, RP3-WE, RP3 and RP2 were reduced admirably the production of $PGE_2$ in HGF. In addition, RP2-WE and RP3-WE exhibited potent inhibitory activities on arachidonic acid-induced ear edema in mouse. Moreover, RP-2 prevented completely acetic acid-induced writhing by 100.0% and RP1, RP3, RP1-WE and RP2-WE also exhibited excellent protective activities against writhing. While aminopyrine, the positive control, showed 76.9% analgesic effect at the same dose. Taken together, these results suggest that recrystallized aqueous extract of Resina Pini could be a promising drug for the treatment of periodontal diseases.

• The Korean Journal of Pain
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• 제33권2호
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• pp.108-120
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• 2020

From the perspective of the definition of pain, pain can be divided into emotional and sensory components, which originate from potential and actual tissue damage, respectively. The pharmacologic treatment of the emotional pain component includes antianxiety drugs, antidepressants, and antipsychotics. The anti-anxiety drugs have anti-anxious, sedative, and somnolent effects. The antipsychotics are effective in patients with positive symptoms of psychosis. On the other hand, the sensory pain component can be divided into nociceptive and neuropathic pain. Non-steroidal anti-inflammatory drugs (NSAIDs) and opioids are usually applied for somatic and visceral nociceptive pain, respectively; anticonvulsants and antidepressants are administered for the treatment of neuropathic pain with positive and negative symptoms, respectively. The NSAIDs, which inhibit the cyclo-oxygenase pathway, exhibit anti-inflammatory, antipyretic, and analgesic effects; however, they have a therapeutic ceiling. The adverse reactions (ADRs) of the NSAIDs include gastrointestinal problems, generalized edema, and increased bleeding tendency. The opioids, which bind to the opioid receptors, present an analgesic effect only, without anti-inflammatory, antipyretic, or ceiling effects. The ADRs of the opioids start from itching and nausea/vomiting to cardiovascular and respiratory depression, as well as constipation. The anticonvulsants include carbamazepine, related to sodium channel blockade, and gabapentin and pregabalin, related to calcium blockade. The antidepressants show their analgesic actions mainly through inhibiting the reuptake of serotonin or norepinephrine. Most drugs, except NSAIDs, need an updose titration period. The principle of polypharmacy for analgesia in case of mixed components of pain is increasing therapeutic effects while reducing ADRs, based on the origin of the pain.

• 약학회지
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• 제35권5호
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• pp.360-367
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• 1991

Effect of Mylabris sidae(MS) and Epicauta gorhami(EG) polysaccharide fractions on the inflammation and immune responses were studied in vivo. MS and EG contained cantharidin about 0.61 and 0.65%, respectively. It was shown that MS and EG polysaccharide fractions at a oral dose of 100 mg/kg have the significant anti-inflammatory and analgesic activity; They inhibited significantly the carrageenin-induced inflammation and acetic acid-induced writhing syndrome. They accelerated significantly the carbon clearance and the phagocytosis of colloidal carbons by Kupffer cells in liver, but they at a oral dose of 100 mg/kg suppressed significantly the Arthus reaction in the sheep red blood cell(S-RBC)-sensitized mice in accordance with the inhibition of haemaglutinin titer, haemolysin titer and plaque-forming cells. On the other hand, they at a oral dose of 200 mg/kg accelerated slightly the oxazolone-induced dermatitis in rats and delayed hypersensitivity in the S-RBC-challenzed mice in consistent with the increase of rosette forming cells. As the above results, it exhibited that MS and EG polysaccharide fractions inhibited the humoral immune responses, but they accelerated the function of macrophages and cellular immune responses. EG polysaccharide fraction had more active than MS polysaccharide fraction.

• Archives of Pharmacal Research
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• 제21권4호
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• pp.406-410
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• 1998

Biflavonoid is one of unique classes of naturally-occurring bioflavonoids. Certain biflavonoids including amentoflavone were previously reported to have inhibitory effect on the group 11 phospholipase $A_2$ activity. Amentoflavone was also found to inhibit cyclooxygenase from guinea-pig epidermis without affecting lipoxygenase. In this study, anti-inflammatory and analgesic activities of amentoflavone were evaluated. When amentoflavone was administered intraperitoneally, it showed a potent anti-inflammatory activity as determined by amelioration of croton-oil induced mouse ear edema. It also showed a potent anti-inflammatory activity in the rat carrageenan paw edema model ($ED_{50}$=42 mg/kg) compared to the activity of prednisolone (35 mg/kg) and indomethacin (10 mg/kg). However, amentoflavone did not show a significant inhibitory activity against rat adjuvant-induced arthritis, a chronic inflammatory model. In addition, amentoflavone was found to possess a potent analgesic activity in the acetic acid writhing test ($ED_{50}$=9.6 mg/kg) compared to the activity of indomethacin (3.8 mg/kg). These results suggest that amentoflavone may be a potential lead for a new type of anti-inflammatory agents having dual inhibitory activity of group 11 phospholipase $A_2$ and cyclooxygenase.

• The Korean Journal of Pain
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• 제26권3호
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• pp.223-241
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• 2013

Boney metastasis may lead to terrible suffering from debilitating pain. The most likely malignancies that spread to bone are prostate, breast, and lung. Painful osseous metastases are typically associated with multiple episodes of breakthrough pain which may occur with activities of daily living, weight bearing, lifting, coughing, and sneezing. Almost half of these breakthrough pain episodes are rapid in onset and short in duration and 44% of episodes are unpredictable. Treatment strategies include: analgesic approaches with "triple opioid therapy", bisphosphonates, chemotherapeutic agents, hormonal therapy, interventional and surgical approaches, steroids, radiation (external beam radiation, radiopharmaceuticals), ablative techniques (radiofrequency ablation, cryoablation), and intrathecal analgesics.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제1회 추계심포지움 and 제2회 생리분자과학연구센터워크숍
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• pp.1-6
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• 1993

Capsaicin [N-(4-hydroxy-3-methoxybenzyl)-trans-8-methyl -6-nonenamide], a pungent principle of red pepper. is known to induce analgesia. Though it has shown remarkable pharmacological activity, the toxicity and side effects inhibited its wider application. The interest has been renewed by the emergence of its agonists, resineferatoxin and ruthenium red. Recently, few successful capsaicinoids including 01vanil (NE-19550), NE-28345, and NE-21610 were reported.