Effect of the Cation-Chloride Cotransporter Inhibitor Furosemide in a Rat Model of Postoperative Pain

He, Yanbing; Ji, Wenjin; Huang, Huansen

doi:10.1111/j.1526-4637.2011.01193.x

Cited by 5 publications

(3 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Sodium-potassium-chloride cotransporter 1 regulates chloride ions influx, while KCC2 adjusts efflux of chloride ions [13][14][15]. The present study showed that, compared with normal rats, NKCC1 expression was higher in spinal dorsal horn of model rats, while the expression of KCC2 was lower in the spinal dorsal horn, which is similar to data from other studies [16][17]. The expression of NKCC1 in spinal dorsal horn of rats in ROPOS group was significantly decreased on the second day.…”

Section: Toxicokinetics Of Ropossupporting

confidence: 90%

Local anesthetic effect and safety of ropivacaine oily solution

Lu,

Yao,

Hui

et al. 2024

Trop. J. Pharm Res

View full text Add to dashboard Cite

Purpose: To investigate the effectiveness and safety of ropivacaine oily solution (ROPOS). Methods: After effecting nerve block in postoperative rats by injection of ROPOS near the sciatic nerve, the expression levels of sodium-potassium-chloride co-transporter 1 (NKCC1) and potassium-chloride co-transporter 2 (KCC 2) in the spinal dorsal horn, were assayed. The safety of ROPOS in beagle dogs was evaluated through subcutaneous injection. Results: The duration of anesthetic effect of ROPOS was 5 times longer than that of ropivacaine hydrochloride injection. The analgesic effect occurred via downregulation of the expression of NKCC1. Dogs administered ROPOS had acute inflammatory reactions at the injection sites within 3 days, but they recovered after 14 days. No other toxic reactions were observed. The Tmax values for dogs subcutaneously injected with ROPOS at doses of 15, 30 and 60 mg/kg were 2.15 ± 3.09, 6.25 ± 9.62 and 14.85 ± 11.82 h; with the Cmax values of 0.78 ± 0.51, 1.35 ± 0.38 and 2.09 ± 0.53 µg/mL, while the AUC(0-48h) values were 15.88 ± 5.41, 31.46 ± 11.45 and 66.10 ± 17.81 h·µg/mL, respectively. The values of Tmax, Cmax and AUC(0-48h) were positively correlated with ROPOS dose. Conclusion: Ropivacaine oily solution has a longer duration of local anesthetic effect than ropivacaine hydrochloride injection and it also possesses a good safety profile. The acute inflammatory reactions are noteworthy and will be further investigated in subsequent studies.

show abstract

Section: Toxicokinetics Of Ropossupporting

confidence: 90%

Local anesthetic effect and safety of ropivacaine oily solution

Lu,

Yao,

Hui

et al. 2024

Trop. J. Pharm Res

View full text Add to dashboard Cite

show abstract

“…Yet loop diuretics may have different effects on pain depending on the baseline state of the subject. For example, one study found that intrathecal furosemide increased the pain threshold in rats that had been subjected to trauma but decreased the pain threshold in intact rats [10]. Thus, in the setting of inflammation and NKCC1 upregulation, there may be an increased NKCC1/KCC2 receptor expression and/or activity ratio that would result in a net effect of analgesia after bumetanide exposure.…”

mentioning

confidence: 99%

Syndrome of severe pain associated with a continuous bumetanide infusion

Shisler¹,

Austin²,

Delpire³

et al. 2014

International Journal of Cardiology

View full text Add to dashboard Cite

“…The diuretic effect of furosemide is accomplished by inhibition of the Na . At high concentrations furosemide inhibits platelet aggregation [12], water �lux via aquaporin-1 water channels [13], adenosine transport in erythrocytes [14], postoperative pain in rats [15] and the new permeability pathways (NPP) induced by the malaria pathogens plasmodia in parasitized erythrocytes [16][17][18]. Moreover, furosemide may counteract apoptosis [5,8].…”

Section: Introductionmentioning

confidence: 99%

Inhibitory Effect of Furosemide on Non-Selective Voltage-Independent Cation Channels in Human Erythrocytes

Kucherenko

Läng

2012

Cell Physiol Biochem

View full text Add to dashboard Cite

Background: Furosemide, a loop diuretic inhibiting the renal tubular Na⁺,K⁺,2Cl^- cotransporter, has been shown to decrease cytosolic Ca²⁺ concentration ([Ca²⁺]_i) in platelets and erythrocytes. [Ca²⁺]_i in erythrocytes is a function of Ca²⁺ permeable cation channels. Activation of those channels e.g. by energy depletion or oxidative stress leads to increase of [Ca²⁺]_i, which in turn triggers eryptosis, a suicidal erythrocyte death characterized by cell membrane scrambling. The present study was performed to explore whether furosemide influences the cation channels and thus influences eryptosis. Methods: Cation channel activity was determined by whole-cell patch clamp, [Ca²⁺]_i utilizing Fluo3 fluorescence and annexin V binding to estimate cell membrane scrambling with phosphatidylserine exposure. Results: A 45 min exposure to furosemide (10 and 100 µM) slightly, but significantly decreased cation channel activity and [Ca²⁺]_i in human erythrocytes drawn from healthy individuals. ATP-depletion (> 3 hours, +37°C, 6 mM ionosine and 6 mM iodoacetic acid) enhanced the non-selective cation channel activity, increased [Ca²⁺]_i and triggered cell membrane scrambling, effects significantly blunted by furosemide (10 – 100 µM). Oxidative stress by exposure to tert-butylhydroperoxide (0.1 –1 mM) similarly enhanced the non-selective cation channels activity, increased [Ca²⁺]_i and triggered cell membrane scrambling, effects again significantly blunted by furosemide (10 – 100 µM). Conclusions: The present study shows for the first time that the loop diuretic furosemide applied at micromolar concentrations (10 – 100 µM) inhibits non-selective cation channel activity in and eryptosis of human erythrocytes.

show abstract

Effect of the Cation-Chloride Cotransporter Inhibitor Furosemide in a Rat Model of Postoperative Pain

Abstract: Intrathecal administration of the CCC inhibitor furosemide had antinociceptive effects in rats with incisional pain. Furosemide may be a novel treatment for postoperative pain.

Cited by 5 publications

References 26 publications

Local anesthetic effect and safety of ropivacaine oily solution

Local anesthetic effect and safety of ropivacaine oily solution

Syndrome of severe pain associated with a continuous bumetanide infusion

Inhibitory Effect of Furosemide on Non-Selective Voltage-Independent Cation Channels in Human Erythrocytes

Contact Info

Product

Resources

About