• Korean Journal of Bronchoesophagology
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• v.4 no.2
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• pp.171-176
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• 1998

Postoperative pain following tonsillectomy remains a significant obstacle to speedy recovery and smooth convalescence. Inadequate analgesia causes poor oral intake and influences the length of hospital stay and ability to return to normal activity. Patient Controlled Analgesia (PCA) is a method of analgesia adminstration that consists of a computer driven pump with a button that the patient may press to adminster a small dose of analgesic drug. The aim of this study was to examine whether Intravenous Patient Controlled Analgesia (IV-PCA) can reduce postoperative pain after tonsillectomy. The 100 patients undergoing tonsillectomy with general anesthesia were divided into two groups. The PCA group patients (n=80) received a mixture of nalbuphine and ketorolac by Walkmed PCA infusor during first 48 postoperative hours. In control group (n=20), the patients received oral acetoaminophen (Tyrenol) regularly and tiaprofenic acid (Surgam) intramuscularly on a p.r.n basis. Analgesic efficacy was evaluated with visual linear analogue scale (VAS) and the adverse effects were evaluated with 4 point scale. The patients of PCA group had less pain than those of control group. The adverse effects in the PCA group were nausea and vomiting. This study suggests that IV-PCA may be safe and effective method of pain control after adult tonsillectomy and is better accepted than oral or intramuscular pain medications.

• Bulletin of the Korean Chemical Society
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• v.29 no.3
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• pp.656-662
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• 2008

Antagonists of the d -opioid receptor are effective in overcoming resistance against analgesic drugs such as morphine. To identify novel antagonists of the d -opioid receptor that display high potency and low resistance, we performed 3D-QSAR analysis using chemical feature-based pharmacophore models. Chemical features for d -opioid receptor antagonists were generated using quantitative (Catalyst/HypoGen) and qualitative (Catalyst/HipHop) approaches. For HypoGen analysis, we collected 16 peptide and 16 non-peptide antagonists as the training set. The best-fit pharmacophore hypotheses of the two antagonist models comprised identical features, including a hydrophobic aromatic (HAR), a hydrophobic (HY), and a positive ionizable (PI) function. The training set of the HipHop model was constructed with three launched opioid drugs. The best hypothesis from HipHop included four features: an HAR, an HY, a hydrogen bond donor (HBD), and a PI function. Based on these results, we confirm that HY, HAR and PI features are essential for effective antagonism of the d -opioid receptor, and determine the appropriate pharmacophore to design such antagonists.

• The Korean Journal of Pain
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• v.27 no.3
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• pp.200-209
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• 2014

Background: Spinal opioid administration is an excellent option to separate the desirable analgesic effects of opioids from their expected dose-limiting side effects to improve postoperative analgesia. Therefore, physicians must better identify either specific opioids or adequate doses and routes of administration that result in a mainly spinal site of action rather than a cerebral analgesic one. Methods: The purpose of this topical review is to describe current available clinical evidence to determine what opioids reach high enough concentrations to produce spinally selective analgesia when given by epidural or intrathecal routes and also to make recommendations regarding their rational and safety use for the best management of postoperative pain. To this end, a search of Medline/Embase was conducted to identify all articles published up to December 2013 on this topic. Results: Recent advances in spinal opioid bioavailability, based on both animals and humans trials support the theory that spinal opioid bioavailability is inversely proportional to the drug lipid solubility, which is higher in hydrophilic opioids like morphine, diamorphine and hydromorphone than lipophilic ones like alfentanil, fentanyl and sufentanil. Conclusions: Results obtained from meta-analyses of RTCs is considered to be the 'highest' level and support their use. However, it's a fact that meta-analyses based on studies about treatment of postoperative pain should explore clinical surgery heterogeneity to improve patient's outcome. This observation forces physicians to use of a specific procedure surgical-based practical guideline. A vigilance protocol is also needed to achieve a good postoperative analgesia in terms of efficacy and security.

• Journal of Pharmaceutical Investigation
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• v.27 no.3
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• pp.165-171
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• 1997

Ibuprofen, a nonsteroidal antiinflammatory, analgesic and antipyretic drug, has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. Effect of ibuprofen/$2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP{\beta}CD)$ inclusion compound on release of suppository was investigated. Complex formation was confirmed by $^{1}H-\;and\;^{13}C-NMR$ spectroscopy. The release of ibuprofen from suppository base in vitro was significantly increased by the complexation with $HP{\beta}CD$. The release of ibuprofen from hydrophilic base was faster than that from hydrophobic base. In vivo studies, the release rate of ibuprofen from suppository was accelerated after rectal administration in complex form. This results suggested that ibuprofen/$HP{\beta}CD$ complex can be practically used for suppository to have faster effect of ibuprofen with reduced side effect.

• Journal of The Korean Dental Society of Anesthesiology
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• v.13 no.4
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• pp.167-178
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• 2013

Oxycodone is a semi-synthetic opioid synthesized from poppy-derived thebaine. It is a narcotic analgesic generally indicated for relief of moderate to severe pain. Although developed in an attempt to improve on the existing opioids, the adverse effects of oxycodone are those that are typically found in opioids. In recent years, the use of the opioid oxycodone has increased markedly and replacing morphine as the first line choice of opioid in several countries. There are formulations for oral immediate, oral extended release and intravenous use. In 2013, intravenous oxycodone was approved for marketing by Ministry of Food and Drug Safety (MFDS), with the indication of postoperative intravenous patient-controlled analgesia (IV PAC). Simulation study of oxycodone demonstrated that minimum effective analgesic concentration (MEAC) of oxycodone was most quickly reached with higher loading dose and IV PCA with background infusion, which may reduce the necessity of rescue analgesics during immediate postoperative period. Previous studies for postoperative pain management with intravenous oxycodone are limited in sample size, mostly less than 100 patients, which may not be large enough to assess safety of intravenous oxycodone. The effectiveness and tolerability of IV PCA with oxycodone should, therefore, be evaluated in large scale clinical trials in Korean populations.

• Journal of Yeungnam Medical Science
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• v.35 no.1
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• pp.40-44
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• 2018

Background: Pregabalin has been studied as a single or multimodal analgesic drug for postoperative pain management in different types of surgeries. We evaluated the analgesic effect of 150 mg of pregabalin in resolving post-gastrectomy pain. Methods: Forty-four patients were randomized into two groups: a pregabalin group that received oral pregabalin (150 mg) 2 h before anesthetic induction, and a control group that received placebo tablets at the same time. Data on postoperative pain intensity (visual analog scale [VAS], at 30 min, 2 h, 4 h, and 24 h), consumption of fentanyl in patient-controlled analgesia (PCA), and the proportion of patients requiring rescue analgesics at different time intervals (0-2 h, 2-4 h, and 4-24 h) were collected during the 24 h postoperative period. Results: The VAS scores did not show significant differences at any time point and consumption of fentanyl in PCA and the proportion of patients requiring rescue analgesics did not differ between the two groups. The groups did not differ in the occurrence of dizziness, sedation, and dry mouth. Conclusion: A preoperative 150 mg dose of pregabalin exerts no effect on acute pain after gastrectomy.

• Journal of Yeungnam Medical Science
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• v.38 no.4
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• pp.371-373
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• 2021

Serotonin syndrome (SS) is a potentially life-threatening condition that is caused by the administration of drugs that increase serotonergic activity in the central nervous system. We report a case of serotonin syndrome in a patient with chronic pain who was taking analgesic drugs. A 36-year-old female with chronic pain in the lower back and right buttock area had been taking tramadol hydrochloride 187.5 mg, acetaminophen 325 mg, pregabalin 150 mg, duloxetine 60 mg, and triazolam 0.25 mg daily for several months. After amitriptyline 10 mg was added to achieve better pain control, the patient developed SS, which was mistaken for psychogenic nonepileptic seizure. However, her symptoms completely disappeared after discontinuation of the drugs that were thought to trigger SS and subsequent hydration with normal saline. Various drugs that can increase serotonergic activity are being widely prescribed for patients with chronic pain. Clinicians should be aware of the potential for the occurrence of SS when prescribing pain medications to patients with chronic pain.

• Biomolecules & Therapeutics
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• v.20 no.1
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• pp.50-56
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• 2012

WIN-34B showed analgesic and anti-inflammatory effects in various animal models of pain and osteoarthritis. However, the molecular mechanism by which WIN-34B inhibits pain and inflammation in vivo remains to be elucidated. We investigated the molecular mechanisms of the actions of WIN-34B using various in vitro models using fibroblast-like synoviocytes from patients with rheumatoid arthritis (RA FLSs), RAW264.7 cells and peritoneal macrophages. WIN-34B inhibited the level of IL-6, $PGE_2$, and MMP-13 in IL-$1{\beta}$-stimulated RA FLSs in a dose-dependent manner. The mRNA levels were also inhibited by WIN-34B. The level of $PGE_2$, NO, IL-$1{\beta}$, and TNF-${\alpha}$ were inhibited by WIN-34B at different concentrations in LPS-stimulated RAW264.7 cells. The production of NO and $PGE_2$ was inhibited by WIN-34B in a dose-dependent manner in LPS-stimulated peritoneal macrophages. All of these effects were comparable to the positive control, celecoxib or indomethacin. I${\kappa}B$B signaling pathways were inhibited by WIN-34B, and the migration of NF-${\kappa}B$ into the nucleus was inhibited, which is consistent with the degradation of $I{\kappa}B-{\alpha}$. Taken together, the results suggest that WIN-34B has potential as a therapeutic drug to reduce pain and inflammation by inhibiting the production of pro-inflammatory mediators.

• The Korean Journal of Pain
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• v.8 no.2
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• pp.251-256
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• 1995

Opioids produce strong analgesic effect result with some side effects such as nausea, vomiting, urinary retention, somnolence, and respiratory depression. Nalbuphine, an agonist-antagonist has, at low doses, an analgesic potency comparable to morphine with little side effects. Analgesic effect after continuous infusion of fentanyl-ketorolac-droperidol, or $Nubain^{(R)}$-ketorolac-dropertiodl combination in Cesarean section patients were assessed by numerical rating scale (NRS) and Prince Hednry scale (PHS). The patients were divided into two groups. Each group consists of 30 patients. Group 1 received 20 ${\mu}g$ of fentanyl the end of surgery. And then continuously infused with additional 380${\mu}g$ of fentanyl plus 120 mg of ketorolac and 2.5 mg of droperidol. Group 2 initially received 2 mg of $Nubain^{(R)}$ at the end of surgery and the remaining dose of $Nubain^{(R)}$ 38 mg plus ketorolac 120 mg and droperidol 2.5 mg was continuously infused. With all patients, initial dose of drug was administered by bolus of i.v. injection and the remaining dose was administered via i.v. using a Baxter Two $Infusor^{(R)}$. Pain scores and side effects were recorded at the time of recovery room arrival, and at interval of 30 min, 1 hr, 6 hr, 14 hr, 24 hr, 48 hr after start of continuous infusion. No significant difference was found between the pain scores and side effects of both groups although pain control effect was excellent in both groups. We concluded that $Nubain^{(R)}$ could be an alternative to fentanyl for postoperative pain control.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.6
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• pp.657-666
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• 2017

Paclitaxel, a chemotherapeutic drug, induces severe peripheral neuropathy. Gabapentin (GBT) is a first line agent used to treat neuropathic pain, and its effect is mediated by spinal noradrenergic and muscarinic cholinergic receptors. Electro-acupuncture (EA) is used for treating various types of pain via its action through spinal opioidergic and noradrenergic receptors. Here, we investigated whether combined treatment of these two agents could exert a synergistic effect on paclitaxel-induced cold and mechanical allodynia, which were assessed by the acetone drop test and von Frey filament assay, respectively. Significant signs of allodynia were observed after four paclitaxel injections (a cumulative dose of 8 mg/kg, i.p.). GBT (3, 30, and 100 mg/kg, i.p.) or EA (ST36, Zusanli) alone produced dose-dependent anti-allodynic effects. The medium and highest doses of GBT (30 and 100 mg/kg) provided a strong analgesic effect, but they induced motor dysfunction in Rota-rod tests. On the contrary, the lowest dose of GBT (3 mg/kg) did not induce motor weakness, but it provided a brief analgesic effect. The combination of the lowest dose of GBT and EA resulted in a greater and longer effect, without inducing motor dysfunction. This effect on mechanical allodynia was blocked by spinal opioidergic (naloxone, $20{\mu}g$), or noradrenergic (idazoxan, $10{\mu}g$) receptor antagonist, whereas on cold allodynia, only opioidergic receptor antagonist blocked the effect. In conclusion, the combination of the lowest dose of GBT and EA has a robust and enduring analgesic action against paclitaxel-induced neuropathic pain, and it should be considered as an alternative treatment method.