Antinociception by Epidural and Systemic α2-Adrenoceptor Agonists and Their Binding Affinity in Rat Spinal Cord and Brain

Asano, Toshio; Dohi, Shuji; Ohta, Shuichiro; Shimonaka, Hiroyuki; Iida, Hiroki

doi:10.1213/00000539-200002000-00030

Cited by 96 publications

(69 citation statements)

References 28 publications

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“…5,[33][34][35] Also, the potency of α2-adrenoreceptor agonist has been shown to correlate well with their binding affinity to spinal α2-adrenoreceptors. 36,37) Since Coombs et al first introduced the potent antinociceptive effects of intrathecal α2-adrenoreceptor agonists, clonidine (15-150 µg) has been frequently used in spinal anesthesia to improve the quality of local anesthetics. 7,8,38) But, side effect such as hypotension, bradycardia, and sedation is increased as dose of clonidine is increased.…”

Section: Discussionmentioning

confidence: 99%

Effects of Intrathecal Dexmedetomidine on Low-Dose Bupivacaine Spinal Anesthesia in Elderly Patients Undergoing Transurethral Prostatectomy

Kim

Lee

et al. 2013

Biological & Pharmaceutical Bulletin

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Low-dose bupivacaine can limit the spinal block level with minimal hemodynamic effects and yield a rapid recovery, but sometimes it may not provide adequate anesthesia for surgery. Dexmedetomidine, a selective α2-adrenoreceptor agonist, was shown to be a potent antinociceptive agent when given intrathecally in animals and humans. The purpose of this study was to evaluate the adjuvant effects of intrathecal dexmedetomidine in elderly patients undergoing transurethral prostate surgery with low-dose bupivacaine spinal anesthesia. Fifty-four patients undergoing transurethral prostate surgery were randomized into two groups receiving either dexmedetomidine 3 µg (n=27) or normal saline (n=27) intrathecally with 6 mg of 0.5% hyperbaric bupivacaine. The characteristics of the spinal block and postoperative analgesic effects were evaluated. The peak block level was similar for the two groups. However, the dexmedetomidine group demonstrated a faster onset time to the peak block and longer duration of spinal block than the saline group (p<0.01). The motor block scales at the time of peak sensory block and regression of 2-sensory dermatomes were higher in the dexmedetomidine group than in the saline group ( p<0.001). There was less analgesic request and the time to the first analgesic request was longer in the dexmedetomidine group than in the saline group (each 487, 345 min, p<0.05). Dexmedetomidine 3 µg when added to intrathecal bupivacaine 6 mg produced fast onset and a prolonged duration of sensory block and postoperative analgesia in elderly patients for transurethral surgery. However, recovery of motor block could be delayed in dexmedetomidine-added patients.Key words anaesthesia; spinal; dexmedetomidine; transurethral resection of prostate; bupivacaine; elderly patient Spinal block is a common anesthetic technique for patients undergoing transurethral resection of prostate (TURP). Most patients indicated for TURP are elderly and frequently associated with cardiopulmonary, endocrine, or other comorbidities.1) Thus, it is important to limit the block level to minimize hemodynamic changes during the spinal anesthesia in such patients.2,3) Low-dose local anesthetics can limit the block level and induce rapid recovery from anesthesia, but sometimes these low-dose local anesthetics may not provide an adequate anesthetic level for surgery. Intrathecal opioids or clonidine are frequently co-administered with local anesthetics to improve the anesthetic quality and postoperative analgesia [2][3][4][5][6][7][8] ; the synergistic action of clonidine with local anesthetics is well-established.6-8) Unlike opioids, intrathecal clonidine does not produce respiratory depression or pruritus, but usual dose of clonidine (15-150 µg) may be associated with bradycardia, hypotension, or sedation. 6-8)Dexmedetomidine is an S-enantiomer of medetomidine with a higher specificity for α2-adrenoreceptor (α2 : α1, 1620 : 1) compared to clonidine (α2 : α1, 220 : 1). It was first introduced into practical use as intravenous sedative after the appro...

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Section: Discussionmentioning

confidence: 99%

Effects of Intrathecal Dexmedetomidine on Low-Dose Bupivacaine Spinal Anesthesia in Elderly Patients Undergoing Transurethral Prostatectomy

Kim

Lee

et al. 2013

Biological & Pharmaceutical Bulletin

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“…The duration of motor block may be increased when it binds to the motor neurons in the spinal cord. [7][8][9][10] In our study we have evaluated the effects of adding dexmedetomidine and buprenorphine to hyperbaric bupivacaine separately for spinal anaesthesia.…”

Section: Introductionmentioning

confidence: 99%

Comparison of dexmedetomidine and buprenorphine as an adjuvant to bupivacaine during spinal anaesthesia for tibial interlocking nailing surgeries

Amitha¹,

Pradeep

2017

Int J Adv Med

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INTRODUCTIONSpinal anesthesia is the choice of regional anesthesia technique for surgeries on the lower limbs, as it preserves consciousness, spontaneous breathing at the same time provides for analgesia and muscle relaxation.1,2 These advantages can be minimized when local anaesthetic alone is used for spinal anaesthesia, as it provides for shorter duration of action.2,3 Many adjuvants like fentanyl, buprenorphine have been tried and are effective to prolong the anaesthetic effects.2,4 Dexmedetomidine, is a selective alpha2-adrenoreceptor agonist has been used for analgesia and intravenous sedation in intensive care unit. 5,6 When used for spinal anasethesia, it acts on the ABSTRACT Background: Buprenorphine is being used as an adjuvant to local anaesthetic for spinal anaesthesia since long. Dexmedetomidine is a new drug which has got alpha 2 agonistic property, and is being tried for spinal anesthesia along with bupivacaine in recent times. Settings and Design: This study was conducted in a prospective, randomized, controlled and double-blind manner. The study included ninety American Society of Anaesthesiologists class I and II patients undergoing tibial interlocking nailing surgeries under spinal anaesthesia. Methods:The patients were randomly divided into three groups (n=30 each) by closed envelope technique. Patients in group 1 received 15 mg of 0.5% hyperbaric bupivacaine, group 2 received 15 mg of 0.5% hyperbaric bupivacaine with 30μg of buprenorphine, and group 3 received 15 mg of 0.5% hyperbaric bupivacaine with 5μg dexmedetomidine for spinal anesthesia. The duration of motor and sensory blockade and any adverse events were recorded. Data were analysed using Chi-square test or Fisher's exact test for categorical data and analysis of variance for continuous data. A value of P<0.05 was considered as statistically significant. Results: In our study the subjects in group 3 (dexmedetomidine) group had significantly longer period of motor blockade (240±20min) and sensory blockade (180±22.2min) compared to other groups, which is statistically significant (P=0.0001 and P= 0.006 respectively). The time to first request of analgesic in the post-operative period was also longer (240±30.2min) in dexmedetomidine group when compared with other groups (P=0.0001). There were no untoward complications (hypotension, sedation) in any groups. Conclusions:We concluded that dexmedetomidine (5μg) with bupivacaine for spinal anesthesia gives significantly longer duration of sensory and motor blockade, than buprenorphine (30μg) with bupivacaine for spinal anaesthesia.

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“…A wide variety of agents have been tested as adjuvant to nerve blocks, which are commonly performed for regional anesthesia, for example opioids (acting in peripheral kappa receptors) [2] , midazolam( via acting on peripheral GABA receptors) [3] naloxone [4] dexmede-tomidine (has synergistic effect in nerve block and it has a high binding affinity to nerve fiber α2-adrenoreceptors) [5,6] clonidine (binding affinity to nerve fiber α2-adrenoreceptors) [7] , epinephrine (induced vasoconstriction with decrease absorption of local anesthetic) [8] , Ketamine (via acting as noncompetitive antagonist of the N-methyl-D aspartate receptor (NMDAR) [9] and recently dexamethasone (may be through its proinflammatory effect) [10] . These drugs have been used along with local anesthetics agents for this purpose with varying degrees of success.…”

Section: Introductionmentioning

confidence: 99%

Effects of Adjuvant in Potentiating the Analgesic Effect of Fascia Iliaca Compartment Block

Attia¹,

Zein²,

Internationals³

2017

J Anesth Surg

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Objective: Nerve blocks for postoperative analgesia have increased significantly lately. Beside the use of adjuvants plus local anesthetics in nerve block in order to extend the analgesia time. Materials and Methods: Sixty elderly patients, ASA grades II and III scheduled for surgery after hip fracture under intrathecal anesthesia with pre-operative FICB, The patients were blindly randomly allocated into three-study groups, all of them received preoperative FICB "bupivacaine 0.25 % with adjuvant either Group K received ketamine (50 mg), Group D received Dexmedetomidine (100 µg) and Group KD received ketamine (50 mg) + Dexmedetomidine (100 µg) plus intrathecal block. Results: Group "KD" showed more satisfactory during positions to receive intrathecal block in compare with either groups due to significant rapid onset of preoperative analgesia in compared with other groups, group KD show significant rapid onset of sensory and motor block, prolonged duration of sensory block, and postoperative analgesia as compare with both group with significant decrease in total analgesic requirement. While group D provided significant prolonged duration of sensory block, and postoperative analgesia when compare with group K with significant decrease in total analgesic requirement. There were no significant difference between the three groups, hemodynamic change (heart rate and blood pressure) and side effects in form of baradycardia, hypotension, nausea, vomiting and sedation. Conclusion: The addition of ketamine, dexmedetomidine with bupivacaine 25% in FICB, is considered the best combination for intrathecal anesthesia for hip repair surgery in elderly patients. It provided intraoperative hemodynamic stability, prolonged motor and sensory block as well as potentiating the postoperative analgesic effect with minimal complications.

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Antinociception by Epidural and Systemic α2-Adrenoceptor Agonists and Their Binding Affinity in Rat Spinal Cord and Brain

Cited by 96 publications

References 28 publications

Effects of Intrathecal Dexmedetomidine on Low-Dose Bupivacaine Spinal Anesthesia in Elderly Patients Undergoing Transurethral Prostatectomy

Effects of Intrathecal Dexmedetomidine on Low-Dose Bupivacaine Spinal Anesthesia in Elderly Patients Undergoing Transurethral Prostatectomy

Comparison of dexmedetomidine and buprenorphine as an adjuvant to bupivacaine during spinal anaesthesia for tibial interlocking nailing surgeries

Effects of Adjuvant in Potentiating the Analgesic Effect of Fascia Iliaca Compartment Block

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