• Journal of Korean Neurosurgical Society
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• 제46권2호
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• pp.165-167
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• 2009

Pain caused by chronic pancreatitis is medically intractable and resistant to conventional interventional or surgical treatment. We report a case of spinal cord stimulation (SCS) for intractable pain due to chronic pancreatitis. The patient had a history of nonalcoholic chronic pancreatitis and multiple emergency room visits as well as repeated hospitalization including multiple nerve block and morphine injection for 3 years. We implanted surgical lead at T6-8 level on this patient after successful trial of percutaneous electrode. The patient experienced a decreased visual analog scale (VAS) scores for pain intensity and amount of opioid intake. The patient was followed for more than 14 months with good outcome and no further hospitalization. From our clinical case, spinal cord stimulation on intractable pain due to chronic pancreatitis revealed moderate pain control outcome. We suggest that SCS is an effective, noninvasive treatment option for abdominal visceral pain. Further studies and long term follow-up are needed to fully understand the effect of SCS on abdominal visceral pain.

• Proceedings of the Korean Society of Applied Pharmacology
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.77-77
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• 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.

• Proceedings of the Korean Society of Applied Pharmacology
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.150-151
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• 1998

Drug delivery to the brain is facilitated by the synthesis of chimeric peptides, where in neuropharmaceuticals are linked to a vector such as an antibody to the transferrin receptor that mediates transcytosis through the blood-brain barrier (BBB). When disulfide linkers are used in the chimeric peptide, it is crucial that the S-S bridge is stable during transit and that cleavage does not occur prematurely within endothelial cells, as the peptide drug moiety would then be sequestered by the BBB instead of passing through it. The present study addressed that problem. As a model drug a metabolically stable opioid peptide, [$^3$H]DALDA (Tyr-dArg-Phe-Lys-NH$_2$), was used. It was monobiotinylated with NHS-SS-biotin to yield bio-[$^3$H]DALDA. The biotinylated peptide was bound to the vector OX26-SA which is a covalent conjugate of OX26 and streptavidin (molar ratio = 1: 1). In vitro treatment of the chimeric peptide, bio-[$^3$H]DALDA/OX26-SA, with a reducing agent, dithiothreitol, released the labeled peptide from the vector by conversion of bio-[$^3$H]DALDA to the desbiotinylated derivative, desbio-[$^3$H]DALDA.

• Biomolecules & Therapeutics
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• 제26권2호
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• pp.101-108
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• 2018

G protein-coupled receptors (GPCRs) are the largest superfamily of transmembrane receptors and have vital signaling functions in various organs. Because of their critical roles in physiology and pathology, GPCRs are the most commonly used therapeutic target. It has been suggested that GPCRs undergo massive genetic variations such as genetic polymorphisms and DNA insertions or deletions. Among these genetic variations, non-synonymous natural variations change the amino acid sequence and could thus alter GPCR functions such as expression, localization, signaling, and ligand binding, which may be involved in disease development and altered responses to GPCR-targeting drugs. Despite the clinical importance of GPCRs, studies on the genotype-phenotype relationship of GPCR natural variants have been limited to a few GPCRs such as b-adrenergic receptors and opioid receptors. Comprehensive understanding of non-synonymous natural variations within GPCRs would help to predict the unknown genotype-phenotype relationship and yet-to-be-discovered natural variants. Here, we analyzed the non-synonymous natural variants of all non-olfactory GPCRs available from a public database, UniProt. The results suggest that non-synonymous natural variations occur extensively within the GPCR superfamily especially in the N-terminus and transmembrane domains. Within the transmembrane domains, natural variations observed more frequently in the conserved residues, which leads to disruption of the receptor function. Our analysis also suggests that only few non-synonymous natural variations have been studied in efforts to link the variations with functional consequences.

• The Korean Journal of Zoology
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• 제34권3호
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• pp.426-431
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• 1991

The present study examines the effect of naloxone, mu-opioid receptor antagonist, on prolactin (PRL) gene expression and secretion induced by estradiol (I) treahent in vivo. Adult rats were ovariectomized (OW) and implanted with Silastic capsules containing either vehicle (oil) or E. Three days later, NAL (2 mg/kg BW) or saline urere injected 30 min prior to sacrifice. To examine PRL secretion in vitro, the pituitaries were incubated in the superfusion system for 3 hrs. Superfusates were collected at 10 min intenrals on ice and subjected to PRL radioimmunoassay. Endogenous release of PRL in OU( + I rats was signifcantlv higher than that in OVX rats (mean $\pm$ SE; 24.5 $\pm$ 3.1 vs 14.5 $\pm$ 2.9 ns/10 min). A single injection of NAL clearly inhibited PRL release in Nitro from pituitaries derived from OW + I rats, but not from OW group. PRL myNA was determined by RNA-blot hybridisation assay with nicktranslated PRL CDNA. E stimulated PRL mRNA about 3 fold over that shown in OW group. Treahent of NAL suppressed the I-stimulated PRL myNA in OVX + I group, but not in OVX group. These data clearly showed that the NAL-induced inhibition of PRL secretion was well correlated with changes in PRL mRNA level and this inhibitory process appears to be mediated in I-dependent manner.

• The Korean Journal of Pain
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• 제25권1호
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• pp.47-51
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• 2012

Intrathecal drug administration system (ITDAS) can reduce the side effects while increasing the effectiveness of opioids compared to systemic opioid administration. Therefore, the use of ITDAS has increased in the management of cancer pain and chronic intractable pain. Catheter obstruction is a serious complication of ITDAS. Here, we present a case of catheter obstruction by a mass formed at the side hole and in the lumen. A 37-year-old man suffering from failed back surgery syndrome received an ITDAS implantation, and the ITDAS was refilled with morphine every 3 months. When the patient visited the hospital 18 months after ITDAS implantation for a refill, the amount of delivered morphine sulfate was much less than expected. Movement of the pump rotor was examined with fluoroscopy; however, it was normal. CSF aspiration through the catheter access port was impossible. When the intrathecal catheter was removed, we observed that the side hole and lumen of the catheter was plugged.

• International Journal of Contents
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• 제11권2호
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• pp.69-73
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• 2015

This study was performed to determine the optimal doses of alfentanil or remifentanil (effect-site concentrations) required to prevent pain and other suffering after abdominal general surgery in ICU patients. A total of 52 general abdominal surgical patients (ASA IIIII) requiring artificial ventilatory care in the ICU were provided with either alfentanil (24 patients) or remifentanil (28 patients) through target controlled infusion (TCI). Alfentanil and remifentanil concentrations were titrated up and down until the pain score became less than 3 (VAS; Visual Analogue Score < 3). The effect-site concentrations (ng/ml) of alfentanil or remifentanil required to adequately control postoperative pain in the ICU were 64 +/- 12 and 1.9 +/- 0.5 for intubation with artificial ventilation, 57 +/- 9 and 1.7 +/- 0.7 for intubation with spontaneous ventilation, and 41 +/- 10 and 1.2 +/- 0.5 after extubation, respectively. Pain scores and the corresponding opioid concentrations were independent from respiratory condition. The three effect-site concentrations of alfentanil and remifentanil obtained from this clinical trial using the TCI technique can be a guideline in the administration of the same opioids to relieve the discomfort of ICU patients who have undergone abdominal general surgery.

• Clinical and Experimental Reproductive Medicine
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• 제17권2호
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• pp.159-165
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• 1990

It has been reported that endogenous opioid peptides play a role in the control of the reproductive function. The goal of this study was to evaluate changs in the serum levels of ${\beta}$-endorphin during hyperstimulated menstrual cycle and their relationship to serum prolactin levels. Serum ${\beta}$-endorphin and prolactin levels were measured during menstrual cycles of 10 normal cylic women hyperstimulated by human menopausal gonadotropin (HMG) and of 10 women by clomiphene/HMG among in vitro fertilization candidates. The results were summarized as follows. 1. In clomiphene/HMG hyperstimulated menstrual cycle the mean serum ${\beta}$-endorphin level insignificantly on 2 day before aspiration of oocyte compared to basal level and reached maximum level on 1 day after aspiration. 2. There was a significant peak of the mean serum ${\beta}$-endorphin level on 1 day before aspiration in HMG hyperstimulated menstrual cycle. 3. On the same day from aspiration, there was no significant differences in the mean serum ${\beta}$-endorphin levels between HMG and clomiphene/HMG hyperstimulated cycles. 4. No significant correlation was noted between serum ${\beta}$-endorphin levels and prolactin levels.

• The Korean Journal of Pain
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• 제25권2호
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• pp.89-93
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• 2012

Background: Hemorrhoid is one of the most common surgical diseases occurring in the anorectal region. In this study, we evaluated the effect of ischiorectal fossa block on alleviating post hemorrhoidectomy pain. Methods: In this study, 90 patients suffering from hemorrhoids were evaluated. They were randomly divided into 3 groups. The first group had no block, the second group an ischiorectal block with placebo (normal saline), and the third group a preemptive ischiorectal block with bupivacaine. Postoperative variables such as pain intensity, pethidine consumption, nausea, and vomiting were compared between the groups. Results: The postoperative pain score in group 1 was $8.5{\pm}1.3$ and $8.1{\pm}0.9$ (P=NS) in group 2. The post operative analgesic demand was $3.1{\pm}1.5$ and $3.3{\pm}1.8$ hours in groups 1 and 2, respectively (P=NS). The post operative pain score and analgesic demand were $4.2{\pm}2.1$ and $9.3{\pm}2.7$ hours, respectively, in group 3 (P < 0.0001). Conclusions: Preemptive ischiorectal block reduces the posthemorrhoidectomy pain and opioid demand.

• The Korean Journal of Pain
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• 제24권1호
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• pp.22-30
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• 2011

Background: Pregabalin has been shown to have analgesic effect in acute pain models. The primary objective was to examine the efficacy a single dose of pregabalin, would have on morphine consumption following lumbar discectomy. Methods: With ethical approval a randomized, placebo-controlled prospective trial was undertaken in 32 patients (ASA I-II, 18-65 years) with radicular low back pain for > 3 months undergoing elective lumbar discectomy. Patients received either oral pregabalin 300 mg (PG Group) or placebo (C Group) one hour before surgery. Pain intensity, the accumulative morphine consumption and adverse effects were recorded for 24 hours following surgery. Functional, psychological and quantitative sensory testing were also assessed. Results: Fourteen patients out of the 32 recruited were randomized to receive pregabalin. Morphine consumption was reduced (absolute difference of 42.3%) between groups with medium effect size. (Mann-Whitney; U =52.5, z-score= 2.84, P = 0.004, r = 0.14). This was not associated with a significant difference in the incidence of adverse effects between the two groups. The median pain intensity (VAS) on movement was not significantly different between groups. Conclusions: A single pre-operative dose of pregabalin (300 mg) did not result in a reduction in pain intensity compared to placebo in this patient cohort but the significant reduction in morphine consumption suggests that a fixed peri-operative dosing regime warrants investigation.