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        Optimal dose of dexmedetomidine for sedation during spinal anesthesia

        Hwoe-Gyeong Ok,백승완,신상욱,김경훈,Hae Kyu Kim,백승훈 대한마취통증의학회 2013 Korean Journal of Anesthesiology Vol.64 No.5

        Background: Sedation in spinal anesthesia can reduce patient’s anxiety and discomfort. Dexmedetomidine has a sedative, hypnotic, analgesic, and minimal respiratory depression effect. However, use of the dexmedetomidine is associated with prolonged recovery. This study was designed to investigate the optimal dose of intravenous dexmedetomidine for proper sedation with minimal recovery time in spinal anesthesia. Methods: One hundred twenty eight patients, aged 20-70 years (58.8 ± 0.7), were recruited. After performing the spinal anesthesia with hyperbaric bupivacaine (13 mg), a loading dose of dexmedetomidine (1 μg/kg) was administered for 10 min, followed by the maintenance infusion of the following: Group A (n = 33; normal saline), Group B (n = 35; dexmedetomidine 0.2 μg/kg/hr), and Group C (n = 39; dexmedetomidine 0.4 μg/kg/hr). Heart rate, blood pressure, and the bispectral index score (BIS) were recorded during the operation. In the recovery room, modified aldrete score (MAS) was measured. Results: There were no significant differences in mean blood pressure and heart rate among the three groups. BIS was not significantly different among the three groups from baseline to 60 min after the infusion of dexmedetomidine. BIS were significantly increased in Group A after 70 and 80 min, and Group A and B after 90, 100, 110 min of dexmedetomidine infusion (P < 0.05). MAS was higher in Group A as compared to Group B and C, within 30 min after admission in the recovery room (P < 0.05). Conclusions: The loading dose (1 μg/kg/10 min) of dexmedetomidine was sufficient for surgery of less than 60 min. Dexmedetomidine infusion followed by maintenance dose (0.2 μg/kg/hr) was sufficient for surgery within 90 min.

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        Can oliceridine (TRV130), an ideal novel μ receptor G protein pathway selective (μ-GPS) modulator, provide analgesia without opioid-related adverse reactions?

        ( Hwoe Gyeong Ok ),( Su Young Kim ),( Su Jung Lee ),( Tae Kyun Kim ),( Billy K Huh ),( Kyung Hoon Kim ) 대한통증학회 2018 The Korean Journal of Pain Vol.31 No.2

        All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse reactions, such as nausea, vomiting, and respiratory depression. The opioid ligand binds to μ opioid receptor and non-selectively activates two intracellular signaling pathways: the G protein pathway induce analgesia, while the μ-arrestin pathway is responsible for the opioid-related adverse reactions. An ideal opioid should activate the G protein pathway while deactivating the μ-arrestin pathway. Oliceridine (TRV130) has a novel characteristic mechanism on the action of the μ receptor G protein pathway selective (μ-GPS) modulation. Even though adverse reactions (ADRs) are significantly attenuated, while the analgesic effect is augmented, the some residual ADRs persist. Consequently, a G protein biased μ opioid ligand, oliceridine, improves the therapeutic index owing to increased analgesia with decreased adverse events. This review article provides a brief history, mechanism of action, pharmacokinetics, pharmacodynamics, and ADRs of oliceridine. (Korean J Pain 2018; 31: 73-9)

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        Can denosumab be a substitute, competitor, or complement to bisphosphonates?

        ( Su Young Kim ),( Hwoe Gyeong Ok ),( Christof Birkenmaier ),( Kyung Hoon Kim ) 대한통증학회 2017 The Korean Journal of Pain Vol.30 No.2

        Osteoblasts, originating from mesenchymal cells, make the receptor activator of the nuclear factor kappa B ligand (RANKL) and osteoprotegerin (OPG) in order to control differentiation of activated osteoclasts, originating from hematopoietic stem cells. When the RANKL binds to the RANK of the pre-osteoclasts or mature osteoclasts, bone resorption increases. On the contrary, when OPG binds to the RANK, bone resorption decreases. Denosumab (AMG 162), like OPG (a decoy receptor), binds to the RANKL, and reduces binding between the RANK and the RANKL resulting in inhibition of osteoclastogenesis and reduction of bone resorption. Bisphosphonates (BPs), which bind to the bone mineral and occupy the site of resorption performed by activated osteoclasts, are still the drugs of choice to prevent and treat osteoporosis. The merits of denosumab are reversibility targeting the RANKL, lack of adverse gastrointestinal events, improved adherence due to convenient biannual subcutaneous administration, and potential use with impaired renal function. The known adverse reactions are musculoskeletal pain, increased infections with adverse dermatologic reactions, osteonecrosis of the jaw, hypersensitivity reaction, and hypocalcemia. Treatment with 60 mg of denosumab reduces the bone resorption marker, serum type 1 C-telopeptide, by 3 days, with maximum reduction occurring by 1 month. The mean time to maximum denosumab concentration is 10 days with a mean half-life of 25.4 days. In conclusion, the convenient biannual subcutaneous administration of 60 mg of denosumab can be considered as a first-line treatment for osteoporosis in cases of low compliance with BPs due to gastrointestinal trouble and impaired renal function. (Korean J Pain 2017; 30: 86-92)

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