• 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.

• The Korean Journal of Pain
• /
• v.1 no.1
• /
• pp.87-90
• /
• 1988

In recent years the use of epidural opiates has increased and although this method of pain relief has shown good results in clinical practice It is still subject to certain drawbacks, the most serious of which appears to be delayed respiratory depression. Since ketamine administered systemically is unlikely to produce respiratory depression it seemed worthwhile to investigate the possibility of exploiting the potent analgesic property to ketamine by its epidural administration. The analgesic effect of ketamine 4 mg, administered epidural space, was evaluated. The duration of pain relief varied from less than 3 hours in 20% to over 24 hours in 30% of the cases. In 62.5% of the cases pain relief exceeded 6 hours. There was no evidence of respiratory depression, and there no postoperative neurologic sequelae. The present results indicated the need for further studies to compare the efficacy and safety of epidural ketamine with the response to epidural opioids for the relief of postoperative pain.

• The Journal of Korean Physical Therapy
• /
• v.8 no.1
• /
• pp.15-20
• /
• 1996

The purpose of this study were to 1) determine the analgesic effect of 632.8 nm of helium-neon (He-Ne) laser stimulation on acupuncture point in rat and 2) determine the reversal of analgesic effect by naloxone injection. Eighteen Sprague-Dawley rats were devided into three groups : control (n=6) : laser (n=6), laser stimulation at $3.58\;J/cm^2$ ; and naloxone (n=6), 1 mg/kg of naloxone chloride inject into peritoneum before laser stimulation at $3.63J/cm^2$. Tail-flick latency were measured pretreat and posttreat with hot plate $(55^{\circ}C)$. Data were analyzed using one-way ANOVA and paired t-teat for tail-flick latency. No significant change was noted in the tail-flick latency in either control or naloxone groups. But significant increased in tail-flick latency in taller group. The results suggest that He-Ne laser induced analgesic effect, and endogenous opioids may be involved in He-Ne laser induced analgesia.

• The Korean Journal of Pain
• /
• v.25 no.1
• /
• pp.47-51
• /
• 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.

• The Korean Journal of Pharmacology
• /
• v.16 no.1 s.26
• /
• pp.15-24
• /
• 1980

As it has been reported that opioids such as morphine and methionine-enkephalin induced antidiuresis and antinatriuresis along with decrease in renal hemodynamics when given intracerebroventricularly(ivt), the renal action of ivt naloxone, a pure antagonist of morphine, and its influence upon the morphine action were investigated in this study. Less than $0.3{\mu}M/kg$ naloxone ivt did not change renal funtion. $1{\mu}M/kg$ ivt tended to, increase urine flow rate and induce transient natriuresis. $3{\mu}M/kg$ ivt produced transient: natriuresis. $3{\mu}M/kg$ ivt produced marked diuresis and natriuresis without any changes of renal hemodynamics. $10{\mu}M/kg$ ivt produced significant increases of urine flow rate and excretion of sodium without any changes of renal hemodynamics. Morphine $0.03{\mu}M/kg$ ivt produced marked decrement in renal hemodynamics along with decreases of water and sodium excretion, as previously shown by Kang. These effects of ivt morphine were completely abolished by the pretreatment with $0.3{\mu}M/kg$ naloxone. These observations provide further evidence that opiate receptors and endorphins in the brain might play an important role in the center-mediated regulation of the renal function in the rabbit.

• The Korean Journal of Physiology and Pharmacology
• /
• v.7 no.1
• /
• pp.1-3
• /
• 2003

To investigate the receptors mediating the regulation of norepinephrine (NE) release in human cerebral cortex slices, we examined the effects of opioid agonists for ${\mu}$-, ${\delta}$-, and ${\kappa}$-receptors on the high potassium (15 mM)-evoked release of [$^3H$]NE. [$^3H$]NE release induced by high potassium was calcium-dependent and tetrodotoxin-sensitive. [$D-Pen^2$, $D-Pen^5$]enkephalin (DPDPE) and deltorphin II (Delt II) inhibited the stimulated release of norepinephrine in a dose-dependent manner. However, Tyr-D-Ala-Gly-(Me)Phe-Gly-ol and U69,593 did not influence the NE release. Inhibitory effect of DPDPE and Delt-II was antagonized by naloxone, naltrindole, 7-benzylidenaltrexone and naltriben. These results suggest that both ${\delta}_1$ and ${\delta}_2$ receptors are involved in regulation of NE release in human cerebral cortex.

• International Journal of Contents
• /
• v.11 no.2
• /
• pp.69-73
• /
• 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.

• Journal of Ginseng Research
• /
• v.26 no.4
• /
• pp.187-190
• /
• 2002

Crude synaptic membrane fractions from the frontal cortex, striatum, brain stem and whole brain of rat were prepared to assay the effects of ginseng total saponin (GTS) on [$^3$H]DAGO bindings of the opioid $\mu$-receptors. Scatchard plots analysis binding data demonstrated that GTS (0.1 mg/ml) decreased the affinity of specific [$^3$H]DAGO bindings without changes in B$\_$max/ in the frontal cortex and striatum. On the other hand, GTS did not affect the [$^3$H]DAGO bindings iii the brain stem and whole brain. These results suggest that the regulation of [$^3$H]DAGO bindings by GTS may play roles in the change of the pharmacological responses of $\mu$-opioids.

• Bulletin of the Korean Chemical Society
• /
• v.30 no.3
• /
• pp.599-607
• /
• 2009

A series of conjugated cyclic and linear enkephalin analogs, Tyr-c[D-A2bu-Gly-Phe-Asp(NH-X)], where X = methyl, stearyl or$ PEG_350$, and Tyr-D-Ala-Gly-Phe-Cys(S-X), where X = methyl, octyl, or farnesyl, were synthesized in solution to investigate the receptor selectivity of opioids based on Schwyzer's membrane compartment $concepts.^{5,6}$ Cyclizations of the target compounds were achieved in high yields (> 60%) employing BOP, $NaHCO_3$ in DMF despite the steric hindrance of the bulky pendant groups. In the binding assay, the hydrophobic fatty acyl conjugates retained $\mu$-receptor selectivity. The unsaturated farnesyl conjugate exhibited the increased binding affinity than the saturated stearyl conjugate for both $\mu$-and $\delta$-opioid receptors. The PEG conjugates displayed the $\delta$-receptor selectivity. The low molecular weight $PEG_350$ conjugate exhibited the increase selectivity than the high molecular weight $PEG_5000$ conjugate to the $\delta$-receptor. The results of this study support the membrane compartment concepts.

• Journal of The Korean Dental Society of Anesthesiology
• /
• v.13 no.4
• /
• pp.195-201
• /
• 2013

Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease caused by the degeneration of upper and lower motor neurons. The disorder causes muscle weakness and atrophy in airway muscles including pharyngeal, laryngeal and other respiratory muscles. The response to muscle realxant is also altered in patients with ALS. Because of the inherent muscle weakness and associated respiratory insufficiency, particular attentions are needed in anesthetic management of ALS patients. We used proper doses of inhalation anesthetics and opioids under EEG-entropy (electroencephalography-entropy)-monitoring without the use of muscle realxants in the anesthetic management of a patient with ALS. The patient early recovered and was discharged on the same day without any respiratory complications.