• Biomolecules & Therapeutics
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• v.7 no.2
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• pp.198-203
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• 1999

Loxoprofen-Na (sodium 2-〔4-(2-oxocyclopentylmethyl)pheny)propionate dihydrate) is a potent analgesic drug. We developed loxoprofen-Na plasters to extend duration time of analgesic activity and to reduce side effect on gastrointestinal tract. Analgesic effect of Loxoprofen-Na plasters was investigated. Loxoprofen-Na plaster had good analgesic effect in rat paw pressure test, Tail-flick latency test and acetic acid-induced writhing test. Also, it had anti-inflammatory effect on carrageenan-induced rat hind paw edema. In pharmacokinetic study of Loxoprofen-Na, plasters dosage form showed that plasma drug concentration was prolonged up to 14 hours. So, we can conclude that loxoprofen-Na plasters, when applied on skin, will be a new type of drug for controlling the various local pain or inflammation.

• Journal of Pharmacopuncture
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• v.23 no.4
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• pp.230-236
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• 2020

Objectives: Trachyspermum khasianum H. Wolff is a rare medicinal plant characteristically used by the traditional healers in traditional medicine for the treatment of throat-pain, toothache, and stomach ache. The study was designed to determine the anthelmintic and analgesic properties of the aerial parts of Trachyspermum khasianum H. Wolff (Family: Apiaceae). The aqueous and ethanol extract of T. khasianum H. Wolff was prepared and subjected for evaluation to determine the possible therapeutic effects. Methods: Anthelmintic activities of the extracts were determined by observing the time taken to paralyze and the time taken for the death of earthworms (Eisenia foetida) as compared to the standard drug-Albendazole (20 mg/ml) and control. Analgesic potential of the extracts was evaluated using Eddy's hot plate method to understand the analgesic activity in rats (Wistar rats) at 100 mg/kg and 200 mg/kg body weight doses and compared with the standard reference (Diclofenac sodium: 10 mg/kg of animals). Results: The extracts showed a significant dose-dependent anthelmintic effect at the different concentrations (10, 20, and 40) mg/ml, compared to that of the standard drug (20 mg/ml). Also, the results suggested that the plant extracts possess significantly analgesic activity in rats. Conclusion: The studies indicate that Trachyspermum khasianum shows anthelmintic and potent analgesic activities. Further research should be carried out to identify the specific phytoconstituents responsible for both analgesic and anthelmintic activities and its possible mechanism of action.

• The Korean Journal of Pain
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• v.27 no.2
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• pp.103-111
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• 2014

Nefopam (NFP) is a non-opioid, non-steroidal, centrally acting analgesic drug that is derivative of the nonsedative benzoxazocine, developed and known in 1960s as fenazocine. Although the mechanisms of analgesic action of NFP are not well understood, they are similar to those of triple neurotransmitter (serotonin, norepinephrine, and dopamine) reuptake inhibitors and anticonvulsants. It has been used mainly as an analgesic drug for nociceptive pain, as well as a treatment for the prevention of postoperative shivering and hiccups. Based on NFP's mechanisms of analgesic action, it is more suitable for the treatment of neuropathic pain. Intravenous administration of NFP should be given in single doses of 20 mg slowly over 15-20 min or with continuous infusion of 60-120 mg/d to minimize adverse effects, such as nausea, cold sweating, dizziness, tachycardia, or drowsiness. The usual dose of oral administration is three to six times per day totaling 90-180 mg. The ceiling effect of its analgesia is uncertain depending on the mechanism of pain relief. In conclusion, the recently discovered dual analgesic mechanisms of action, namely, a) descending pain modulation by triple neurotransmitter reuptake inhibition similar to antidepressants, and b) inhibition of long-term potentiation mediated by NMDA from the inhibition of calcium influx like gabapentinoid anticonvulsants or blockade of voltage-sensitive sodium channels like carbamazepine, enable NFP to be used as a therapeutic agent to treat neuropathic pain.

• YAKHAK HOEJI
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• v.25 no.1
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• pp.27-35
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• 1981

Etomidoline is a new synthetic atropine-like drug. The present investigation aimed to study the combined effects of etomidoline and neofopam hydrochloride which has an analgesic and muscle relaxant activity, compared with the effects of each drugs. Acute toxicities (ID$_{50}$) in mouse were 132mg/Kg (p.o.) and 49mg/Kg (i.p.) when combination ratio of etomidoline and neofopam was 1:5 and 103 mg/Kg (p.o.) and 30mg/Kg (i.p.) with the ratio of 1:10. Etomidoline showed more potent anticholinergic effects than neofopam in the isolated rat intestine. Whereas, antibarium effects were twice as active with neofopam than with etomidoline. When etomidoline and neofopam were added in combination ratio of 1 : 5, papaverine-like avtivity was increased, but no changes of anticholinergic effect were observed. Analgesic effect was measured by the anti-writhing method of Whittle in mice. Both of the concurrent and single administration of etomidoline and nefopam reduced significantly the writhing number and the effect of the concurrent administration was more active than that of single, and 1 : 5 combination was slightly more potent than 1:10. Each drug or the combined drug was administered to mice and observed the change of the pupil size. Pupil sizes were increased with each drug and with combined drug, although there were no significant differences between the each group of drugs. However, those effects were less than that of atropine sulfate.e.

• YAKHAK HOEJI
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• v.23 no.1
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• pp.11-16
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• 1979

Benorylate and ethoxybenzamide have been used alone or in combination as an analgesic, antipyretic and antiinflammatory agent. We investigated the significance of the differences of analgesic activities between single and concurrent administration of benorylate and ethoxybenzamide and lorazepam in mice and also antipyretic activity between single and concurrent administration of benorylate and ethoxybenzamide in rats. 1). Concurrent administration of each half dose of benorylate and ethoxybenamide showed much inhibiting effect on the acetic acid-induced writhing syndrome of mice than the above drug alone, and the some increased analgesic response by hot plate method. 2). The synergistic and analgesic effect of combined administration of benorylate and lorazepam was found to be significant. 3). Antipyretic effect of half-dose combined administration of benorylate and ethoxybenzamide on the rat pyrexia induced by yeast(s.c.) and T.T.G. (i.v.) was shown to be similar to the effect of each drug.

• Natural Product Sciences
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• v.9 no.4
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• pp.210-212
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• 2003

In the present study Momordica dioica fruit pulp was successively extracted with hexane and methanol. To the concentrated methanolic extract ethyl acetate was added and ethyl acetate soluble portion was separated. Both hexane extract (HE) and ethyl acetate soluble portion (EASP) of methanolic extract was vacuum dried to yield the respective HE and EASP. HE and EASP were evaluated for its analgesic and anti-inflammatory activities in a dose of 50 and 100 mg/kg in mice and rats. Both HE and EASP significant exhibited analgesic and anti-inflammatory activities when compare to standard drug.

• The Journal of Internal Korean Medicine
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• v.18 no.1
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• pp.69-85
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• 1997

This study was designed to elucidate the anti-inflammatory, cardiovascular, anti-thrombotic and analgesic effects of Shintongchugeotang. The anti-inflammatory effect was measured by the method of carragenin induced edema, protein leakage test using CMC-pouch, and the analgesic effect was measured by the acetic acid method and hot plate method, and the effect of Shintongchugeotang on the cardiovascular system was observed by the change of flow rate of Ringer solution in the vascular system in the ear of rabbit, and the contraction and dilatation of rat tail artery. Death rate, platelet aggregation, plasma coagulation activity was observed for the measurement of the anti-coagurative effect of Shintongchugeotang. The result was as follows : 1. After the administration of Shintongchugeotang extract, Carragenin induced edema and CMC-pouch protein leakage were significantly decreased. 2. The slight analgesic effect of Shintongchugeotang extract was confirmed by the observation of writhing syndrome, paw licking time, and escape time. 3. The drug increased the auricular blood flow in rabbit. 4. The drug relaxed the artery contraction by pretreated norepinephrine in rat. 5. The drug inhibited the death rate of mouse which was led to thromboembolism by serotonin and collagen. 6. The drug inhibited the platelet aggregation in rat. 7. The drug prolonged the prothrombin time and activated partial thromboplastin time on the test of plasma coagulation factor activity in rat, but was not valuable.

• Advances in Traditional Medicine
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• v.6 no.4
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• pp.319-323
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• 2006

The crude ethanolic extract of the leaves of Clerodendrum viscosum (Family: Verbenaceae) was evaluated for its antioxidant and analgesic activities to investigate the scientific basis of the traditional uses. The antioxidant property of the extract was assessed by 1, 1-diphenyl -2- picryl hydrazyl (DPPH) free radical scavenging assay. The extract showed prominent antioxidant activity ($IC_{50}about{\sim}16{\mu}g/ml$) which was comparable to standard drug ascorbic acid ($IC_{50}about{\sim}15{\mu}g/ml$).The extract produced significant (P<0.001) writhing inhibition in acetic acid induced writhing in mice at the dose of 125 mg, 250 mg and 500 mg/kg body weight respectively, which were comparable to the standard drug diclofenac sodium. The results tend to suggest that the crude leaves extract at the above doses have antioxidant and analgesic activities and indicate that it might possess biologically active constituents having free radical scavenging and analgesic activities respectably.

• Korean Journal of Clinical Pharmacy
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• v.24 no.1
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• pp.45-52
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• 2014

Objective: To evaluate the clinical manifestations and causative drugs of the outpatient adverse drug reactions (ADRs) reported by community pharmacy. Methods: From April 2013 to September 2013, all outpatient ADRs reported by community pharmacy to Regional Pharmacovigilance Center of Korean Pharmaceutical Association were included. The causality of ADRs was assessed by the criteria of WHO-Uppsala Monitoring Centre. The clinical features and the offending drugs were analyzed using the WHO-Adverse Reaction Terminology and the classification of American Hospital Formulary Service Drug Information, respectively. Results: 2,826 (97.0%) of the total 2,912 ADRs had causal relationship. The 1,923 patients with mean age of 55.1 years and female fraction of 66.5% were included in the ADRs. Gastrointestinal (33.6%), nervous system (14.9%), and skin (13.5%) symptoms were common in ADRs. Analgesic drugs (19.7%), gastrointestinal drugs (17.7%), and central nervous system drugs (11.0%) were prevalent offending drugs. The leading causative generic drug was the complex of acetaminophen and tramadol. Among 203 ADRs by the nonprescription drugs, the most common clinical features were skin (37.4%) and gastrointestinal (23.6%) symptoms and the most prevalent offending drugs were analgesic drugs (40.0%) and mucocutaneous system drugs (16.3%). The combination of acetaminophen and chlorzoxazone was the leading causative generic in nonprescription drugs. Conclusion: In this study, gastrointestinal symptom was the most common manifestation and analgesic drug was the most common causative drug in outpatient ADRs reported by community pharmacy.

• Journal of Pharmaceutical Investigation
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• v.1 no.1
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• pp.30-33
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• 1971

Comparative studies were made on the analgesic effect of salicylamide, used individually and combined with parasympatholytics (propantheline and atropine) and antihistaminics (tripelennamine, diphenhydramine) as regards the analgesic effect (in thermal contact method) were examined by its oral administration with each combined drug to mouse (three assumption cross-over test), and the following effects were found. 1. The increasing order of the parasympatholytics to the analgesic effect of salicylamide is as follows: propantheline>atropine. 2. The increasing order of the antihistaminics to the analgesic effect of salicylamide is as follows: chlorpheniramine>diphenhdramine>tri pelennamine. In the ratio '1 : 1' salicylamide to parasympatholytics and antihistaminics, the analgesic effect of salicylamide was more increase than the other ratio in this study.