PubMed · 15931713
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2005. NME digest.. https://pubmed.ncbi.nlm.nih.gov/15931713/
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PURPOSE: This study was performed to characterize the substrate specificity and mechanism of the intestinal clonidine transport. METHODS: Uptake of [3H]clonidine into Caco-2 cells was investigated. Interaction with drugs was studied in competition assays. RESULTS: Uptake of [3H]clonidine was linear for up to 2 min, Na+-independent, and insensitive to changes in membrane potential, but strongly H+-dependent. The uptake rate of clonidine was saturable with kinetic parameters of 0.5+/-0.1 mM (Kt) and 16.6+/-1.8 nmol/2 min per mg of protein (Vmax) at an outside pH of 7.5. Many drugs such as clonidine, guanabenz, methamphetamine, imipramine, clomipramine, nortriptyline, quinine, xylazine, ephedrine, and diphenhydramine strongly inhibited the [3H]clonidine uptake with Ki values between 0.15 and 1 mM. CONCLUSIONS: Clonidine is transported by a carrier-mediated process. Substrate specificity and mechanism are very similar to the transport described in blood-brain barrier endothelial cells. The transport characteristics do not correspond to carriers for organic cations of the SLC22 family or the choline transporters CHT1 and CLT1. The system might be identical to the H+/tertiary amine antiporter. It interacts with a large number of both hydrophilic and lipophilic cationic drugs, and also, interestingly, with opiates.
Visual neglect after stroke is often associated with a failure to explore contralesional space. Here, we show that guanfacine, a noradrenergic agonist that modulates dorsolateral prefrontal cortex, improves leftward space exploration in selected right-hemisphere patients with neglect. The positive effects of guanfacine were associated with extended ability to maintain attention on task. The results suggest that neuropharmacological targeting of intact frontal areas might be one way to enhance cognitive function after damage to posterior brain regions in selected individuals.
BACKGROUND AND AIM: Clonidine applied intra-articularly into the knee joint has a peripheral analgesic effect. We examined intra-articularly injected clonidine to determine whether resorption with a measurable systemic concentration could be detected. METHODS: A randomised, placebo-controlled double-blind study was carried out on patients undergoing knee arthroscopies. The 69 patients were randomised into three groups: group 1 received 150 ug clonidine intra-articularly, group two 150 ug clonidine intravenously and group three a placebo. Postoperative pain therapy was carried out with i.v. morphine hydrochloride. Pain scores and side-effects were documented for 24 h. RESULTS: There were no significant differences between the three groups in demographics, duration of operation, duration of anaesthesia, diagnoses or type of operation. The pain score at rest was significantly lower in group 1. In the first 20 min, the systemic concentration of clonidine was significantly higher in the intravenous group than in the intra-articular group. CONCLUSION: Intra-articular clonidine has a postoperative analgesic effect after knee arthroscopies due to a peripheral action.