• Biomolecules & Therapeutics
• /
• v.5 no.2
• /
• pp.150-157
• /
• 1997

Capsaicin cream has been used to attenuate the pain associated with diabetic neuropathy, rheum-atoid arthritis, osteoarthritis and postherpetic neuralgia. But its common side effect, local irritation, limits the use of it and there is still a need for a new analgesic devoid of this side effect. This study was conducted to compare the local irritant effect of DA-5018, a new capsaicin derivative, with that of capsaicin in various animal models and human beings. Capsaicin, applied topically to the mouse ear, produced dose-dependent increase of ear volume and the frequency of ear scratching behavior in mice. Neither ear volume nor scratching behavior was affected by DA-5018. In eye wiping test of rat, DA-5018 was 10 times less irritant than capsaicin. Capsaicin administered intradermally into the rat paw elicited paw lick/lift response with a potency which was three times that of DA-5018. Zostrix-HP (0.075% capsaicin cream), but not DA-50180.3% cream, increased ear volume of rat and induced thermal hyperalgesia in normal and carrageenan inflamed paws. Six day-treatment of Zostrix-HP failed to develop tolerance against this thermal hyperalgesia. In human beings, Zostrix-HP produced burning sensation and itching in more than 90% of volunteers involved and its maximum irritant effect was significantly higher than that of DA-5018 cream. These results suggest that local irritation and burning sensation produced by DA-5018 is much less than capsaicin.

• The Korean Journal of Physiology and Pharmacology
• /
• v.14 no.3
• /
• pp.191-198
• /
• 2010

The effects of different doses of tramadol on analgesia and electroencephalographic (EEG) spectralparameters were compared in rats. Saline or tramadol 5, 10, 20 or 40 mg/kg was administered. The degree of analgesia was evaluated by tail-flick latency, and the degree of seizure was measured using numerical seizure score (NSS). Additionally, band powers, median power frequency and spectral edge frequency 95 were measured to quantify the EEG response. All doses of tramadol produced spike-wave discharge. Tramadol significantly and dose-dependently increased the analgesia, but these effects did not correspond with the changes in the EEG spectral parameters. NSS significantly increased in the Tramadol 20 and 40 mg/kg treatment groups compared to the Control and TRA5 groups, and two rats given 40 mg/kg had convulsions. In conclusion, tramadol dose-dependently increased the analgesic effect, and the 10 mg/kg dose appears to be a reliable clinical dose for analgesia in rats, but dose-dependent increases in analgesia and seizure severity did not correlate with EEG spectral parameters.

• Korean Journal of Plant Resources
• /
• v.23 no.6
• /
• pp.513-518
• /
• 2010

In the present study, the antinociceptive profiles of Dianthus chinensis L extract were examined in ICR mice. Dianthus chinensis L extract administered orally (200 mg/kg) showed an antinociceptive effect as measured by the tail-flick and hot-plate tests. In addition, Dianthus chinensis L extract attenuated the writhing numbers in the acetic acid-induced writhing test. Furthermore, the cumulative nociceptive response time for intrathecal (i.t.) injection of substance P ($0.7\;{\mu}g$) was diminished by Dianthus chinensis L extract. Intraperitoneal (i.p.) pretreatment with yohimbine ($\alpha_2$-adrenergic receptor antagonist) attenuated antinociceptive effect induced by Dianthus chinensis L extract in the writhing test. However, naloxone (opioid receptor antagonist) or methysergide (5-HT serotonergic receptor antagonist) did not affect antinociception induced by Dianthus chinensis L extract in the writhing test. Our results suggest that Dianthus chinensis L extract shows an antinociceptive property in various pain models. Furthermore, this antinociceptive effect of Dianthus chinensis L extract may be mediated by $\alpha_2$-adrenergic receptor, but not opioidergic and serotonergic receptors.

• Asian Pacific Journal of Cancer Prevention
• /
• v.16 no.15
• /
• pp.6381-6384
• /
• 2015

Background: The purpose of this retrospectively study was to examine the effectiveness and tolerability of a radiotherapy technique for the palliation of symptomatic liver metastases. Materials and Methods: Twentyseven patients with liver metastases were enrolled and received targeted whole liver irradiation consisting of mean 1, 8 Gy in five to twelve fractions to a total mean dose 17Gy. Symptoms at baseline were hepatic pain (26 patients), lost of weight (6), lack of appetite (2), and night sweats (1). Seventeen patients (63%) had failed previous treatment with chemotherapy and/or high-dose steroids. Results: Individual symptom response rates were 100% at 4 weeks. Partial or complete global symptomatic responses were noted in 11 patients (40%) after 2 months. After 3 months, 8 patients (28%) reported loss of pain. The treatment was well tolerated with one patient (3%) experiencing grade 3 toxicity (one vomiting and one diarrhoea). Overall the median survival time was 4.9 months (range 1 - 14 months). One year survival was 39%. Conclusions: This is simple and well-tolerated treatment but to achieve good palliation effects we should carefully selected patients whose conventional treatment does not bring good analgesic control.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.29 no.3
• /
• pp.150-158
• /
• 2016

Objectives : We want to know the effect of Gyejakjimo-tang in mice model of acute pain.Methods : We investigated writhing reflex in mice with acetic acid-induced abdominal pain using mice, we observed c-Fos protien expression by immunohistochemistry dyeing method in the paraventricular nucleus(PVN) and supraoptic nucleus(SON) of the hypothalamus.Results : All of Gyejakjimo-tang treated group suppressed acetic acid-induced writhing response as acetic acid injuction group, but in 100㎎/㎏ Gyejakjimo-tang treated group and 200㎎/㎏ Gyejakjimo-tang treated groups represernted significance. All of Gyejakjimo-tang treated groups(50, 100 and 200㎎/㎏ Gyejakjimo-tang-treated group), Fos-positive cells in PNV significantly decreased as acetic acid injuction group, and All of Gyejakjimo-tang-treated groups Fos-positive cells in SON significantly decreased as acetic acid injuction group.Conclusions : The present results showed that the mice pre-treated with the aqueous extract of Gyejakjimo-tang showed analgesic effect on acetic acid-induced abdominal pain.

• Natural Product Sciences
• /
• v.7 no.3
• /
• pp.76-82
• /
• 2001

The pharmacological activities of the acetonitrile (MeCN), hexane extracts and isolated pure terpenoidal compound Lupeol from the leaves of Teclea nobilis, Delile (TN), on inflammation induced by carrageenan an implantation of cotton pellets in rats; the nociceptive response using writhing and tail flick tests and the antipyretic activity in yeast-induced fever were examined in mice. Oral administration of TN extracts at doses of 150 and 300 mg/ks and lupeol 5 and 10 mg/kg showed a significant anti-inflammatory activity in rats. The extracts of TN and lupeol significantly decreased the number of contractions and stretchings induced by acetic acid and heat-induced pain in mice. The antipyretic effect of extracts and lupeol was also found to be significant. The behavioral observation of animals showed that the hexane extract and lupeol caused CNS depressant activity and did not produce any toxic or lethal effects in animals at various dose levels. The results suggest that the Teclea nobilis extracts and lupeol possesses anti-inflammatory, analgesic and antipyretic activities.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1993.04a
• /
• pp.77-77
• /
• 1993

약물 내성 (tolerance) 및 의존성 (dependence)은 그 약물이 지니고 있는 여러 가지 약리작용과 관련되어 형성된다. 약물의 반복투여 후, 나타나는 작용이 처음의 반응 (response) 보다 감소되어 나타나는 현상 즉, 내성과, 이와는 반대로 약물반복 투여 후 나타나는 작용이 처음의 반응보다 점점 증가하는 역내성 (reverse tolerance 또는 sensitization) 측정에 있어서 약물에 따라 적절한 검색 방법을 설명한다. 의존성에 있어서 약물 섭취 결과 mood가 변하거나 도취감 또는 만족감을 일으키게 되면 그 감각을 재 경험하고 싶다는 욕구가 일어나게 되는 정신적 의존성(psychic dependence)과, 약물을 반복 투여하다가 갑자기 투여를 중단 했을때 여러가지 생리학적인 또는 행동적인 변화가 급격히 증가하여 금단증상을 나타내는 신체적 의존성 (physical dependence) 측정 방법을 제시한다. 내성과 의존성은 근본적으로 다르지만 대부분의 경우 내성이 형성되면 의존성이 형성된다. 여기서는 주로 morphine과 psychostimulants를 투여한 후 나타나는 약리작용에 대한 내성과 opioids (마약성 진통제)의 의존성 평가 방법에 대한 model을 설명하고자 한다 진통성 내성(analgesic tolerance)에 있어서 진통제의 진통력은 진통력 측정 방법(tail pinch, paw-withdrawal, tail flick, tail-withdrawal, hot plate, writhing, etc)에 따라 차이가 있기 때문에 각각의 진통제의 정합한 내성 측정 방법을 결정할 필요가 있다. 역내성 (roversetolerance)은 cocaine, amphetamine, opioids둥의 만성투여에서 일어난다. 이들 역내성을 측정하는 한 방법으로 자발운동을 측정하는데 locomotor activity cage나 tilting cage를 이용한다. 정신적 의존성(psychic dependence)은 약물 섭취 욕구를 이용한 CPP (conditioned place preference)법을 소개한다. 신체적 의존성 (physical dependence)은 opioids를 만성적으로 투여한 후 naloxone으로 precipitation하여 나타난 여러 가지 금단증상을 측정하고 몇몇 평가 model을 제시한다.

• YAKHAK HOEJI
• /
• v.29 no.4
• /
• pp.188-192
• /
• 1985

Protopanaxadiol (PD) fraction and protopanaxatriol (PT) fraction were separated from thebutanol fraction of panax ginseng roots. Each group of mice was injected with morphine hydrochloride (40 mg/kg s.c.) three times at 8 hr intervals for a period of 6 days. PD fraction and PT fraction were injected (25, 100 mg/kg i.p.) to mice 1 hr prior to the third morphine injection daily. Inhibition of morphine tolerance was evidenced by the increase in analgesic response to morphine hydrochloride (10mg/ kg i.p.) as estimated by the tail flick method. Inhibition of morphine tolerance by PT fraction was effective but there was no remarkable difference in inhibition of tolerance development between control group andPD fraction group.

• The Korean Journal of Physiology
• /
• v.22 no.1
• /
• pp.89-100
• /
• 1988

Effect of clonidine on the dorsal horn cell responses to mechanical stimulations were studies in 3 spinalized cats and 10 cats with intact spinal cord. The type of dorsal horn cells was determined according to their response patterns to four graded mechanical stimulations (brush, pressure, pinch and squeeze) applied to the respective receptive fields. In the present study the results obtained only from the wide dynamic range (WDR) cells were included. The responses of the WDR cells to noxious mechanical stimuli were selectively suppressed following intravenous administration of clonidine into the experimental animals. The clonidine-induced changes in responses of the WDR cells to mechanical stimulation were not affected by naloxone or propranolol whereas effect of clonidine on WDR cell responses was almost completely abolished after intravenous administration of yohimbine. Also in the spinalized cats results parallel to those observed in cats with intact spinal cord were obtained. The results of present study strongly implies that analgesic action of clonidine can be mediated through excitation of ${\alpha}_{2}-adrenoceptor$ even at the spinal cord level without supraspinal mechanism.

• Journal of Pharmacopuncture
• /
• v.22 no.1
• /
• pp.7-15
• /
• 2019

Portulaca oleracea L. (PO) or Purslane is an annual grassy plant that is distributed in many parts of the world, especially the tropical and subtropical areas. PO has some pharmacological properties such as analgesic, antibacterial, skeletal muscle-relaxant, wound-healing, anti- inflammatory and a radical scavenger. This review article is focused on the anti-inflammatory, immuno-modulatory, anti-oxidant and anti-tumor activities of the PO. Anti-inflammatory, immuno-modulatory, anti-oxidant and Anti-tumor effects of PO were searched using various databases until the end of August 2018. The online literature was searched using PubMed, Science Direct, Scopus, Google Scholar and Web of Science. Our review showed that PO exerts its effects through anti-inflammatory properties and balancing the adaptive and innate immune system depending on situations. PO acts as immune-modulator and anti-oxidant agent in both inflammatory states by the dominance of Th2 response such as asthma, cancer and atopic dermatitis and evoked Th1 disorders including hepatitis and multiple sclerosis.