Assessment of Differential Blockade by Amitriptyline and Its N -Methyl Derivative in Different Species by Different Routes

Gerner, Peter; Haderer, Anna E.; Mujtaba, Mustafa G.; Sudoh, Yukari; Narang, Subina; Abdi, Salahadin; Srinivasa, Venkatesh; Pertl, Christof; Wang, Ging Kuo

doi:10.1097/00000542-200306000-00028

Cited by 52 publications

(26 citation statements)

References 13 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Amitriptyline was more potent than bupivacaine in a subcutaneous infiltration model 126 and when applied intrathecally in rat and sheep. 83 However, when amitriptyline was evaluated for ulnar nerve blockade in healthy human volunteers, it was found to be less effective than bupivacaine-contrary to the results from a large number of animal studies. This might be due to the thicker nerve sheaths present in humans as compared to rats, presenting a larger barrier to penetration for amitriptyline into the nerve.…”

Section: Potent Blockers Of Sodium Channelsmentioning

confidence: 90%

The Role of Sodium Channels in Chronic Inflammatory and Neuropathic Pain

Amir

Argoff

Bennett

et al. 2006

The Journal of Pain

Self Cite

319

262

View full text Add to dashboard Cite

Section: Potent Blockers Of Sodium Channelsmentioning

confidence: 90%

The Role of Sodium Channels in Chronic Inflammatory and Neuropathic Pain

Amir

Argoff

Bennett

et al. 2006

The Journal of Pain

Self Cite

319

262

View full text Add to dashboard Cite

“…Conversely, a predominantly proprioceptive block causes a delayed hopping followed by greater lateral hops to prevent the animal from falling. In the case of full blockade, there would be no hopping maneuvers (16).…”

Section: Proprioceptionmentioning

confidence: 99%

Effect of Brain Cooling on Brain Ischemia and Damage Markers After Fluid Percussion Brain Injury in Rats

Chio¹,

Kuo²,

Hsiao

et al. 2007

Shock

View full text Add to dashboard Cite

Although systemic cooling had recently been reported as effective in improving the neurological outcome after traumatic brain injury, several problems are associated with whole-body cooling. The present study was conducted to test the effectiveness of brain cooling without interference with the core temperature in rats after fluid percussion traumatic brain injury (TBI). Brain dialysates ischemia (e.g., glutamate and lactate-to-pyruvate ratio) and injury (e.g., glycerol) markers before and after TBI were measured in rats with mild brain cooling (33 degrees C) and in the sham control group. Brain cooling was accomplished by infusion of 5 mL cold saline via the external jugular vein under general anesthesia. The weight loss was determined by the difference between the first and third day of body weight after TBI. The maximum grip angle in an inclined plane was measured to determine motor performance, whereas the percentage of maximal possible effect was used to measure blockade of proprioception. The triphenyltetrazolium chloride staining procedures were used for cerebral infarction assay. As compared with those of the sham-operated controls, the animals with TBI had higher values of extracellular levels of glutamate, lactate-to-pyruvate ratio, and glycerol in brain and intracranial pressure, but lower values of cerebral perfusion pressure. Brain cooling adopted immediately after TBI significantly attenuated the TBI-induced increased cerebral ischemia and injury markers, intracranial hypertension, and cerebral hypoperfusion. In addition, the TBI-induced cerebral infarction, motor and proprioception deficits, and body weight loss evaluated 3 days after TBI were significantly attenuated by brain cooling. We successfully demonstrate that brain cooling causes attenuation of TBI in rats by reducing cerebral ischemia and injury resulting from intracranial hypertension and cerebral hypoperfusion. Because jugular venipuncture is an easy procedure frequently used in the emergency department, for preservation of brain function, jugular infusion of cold saline may be useful in resuscitation for trauma patients.

show abstract

“…Unlike the earlier published studies with QX-314, 11 however, we also noted a rather prominent analgesic effect of EN3427 alone-findings that would appear to be at odds with the impermeable quaternary ammonium rationale discussed earlier. There is, in fact, ample precedent for QX-314 and other quaternary ammonium local anesthetics being effective in a variety of pain models and by a variety of routes of administration [31][32][33][34][35] that is sufficiently expansive as to suggest that the observation by Binshtok et al 11 may be more the exception than the rule.…”

Section: Discussionmentioning

confidence: 99%

En3427

Banerjee

Baranwal

Saha

et al. 2015

Anesthesia &Amp; Analgesia

View full text Add to dashboard Cite

The present studies demonstrate that a new molecular entity, EN3427, produces effective and long-lasting analgesia in 2 rodent pain models. The analgesic effects of EN3427 are significantly longer-lasting than lidocaine and are further extended when EN3427 is combined with lidocaine. The results are discussed with respect to a possible lidocaine-mediated TRP channel activation and facilitated neuronal access of EN3427, with subsequent entrapment conferring extended-duration efficacy.

show abstract

Assessment of Differential Blockade by Amitriptyline and Its N -Methyl Derivative in Different Species by Different Routes

Abstract: Amitriptyline and N-methyl amitriptyline are potent Na+ channel blockers and show greater differential blockade in sheep than in rats. This differential blockade in sheep is greater than that produced by lidocaine or bupivacaine.

Cited by 52 publications

References 13 publications

The Role of Sodium Channels in Chronic Inflammatory and Neuropathic Pain

The Role of Sodium Channels in Chronic Inflammatory and Neuropathic Pain

Effect of Brain Cooling on Brain Ischemia and Damage Markers After Fluid Percussion Brain Injury in Rats

En3427

Contact Info

Product

Resources

About