Original contributionAmitriptyline plasma protein binding: Effect of plasma pH and relevance to clinical overdose☆
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Cited by (53)
An automated online three-phase electro-extraction setup with machine-vision process monitoring hyphenated to LC-MS analysis
2022, Analytica Chimica ActaCitation Excerpt :Plausible causes are that dilution reduced the concentration of the proteins from the plasma presenting at the interface between the sample and the organic phase, which improved the migration of analytes from sample to acceptor droplet [23,24], and/or less ion suppression induced by the dilution. For all model compounds, the enrichment factor in plasma appeared to be lower after protein precipitation, which may be due to the protein binding of some compounds and loss of analytes during protein precipitation [46–52]. However, it also indicates that the optimized EE method is able to separate the molecules with high protein affinity from the proteins (in the samples without PP).
Comparison of cerebral Open Flow Microperfusion and Microdialysis when sampling small lipophilic and small hydrophilic substances
2019, Journal of Neuroscience MethodsCitation Excerpt :Moreover, the integrity of BBB in the vicinity of the probe during sampling has major influence on the drug concentration in the sample. The protein binding of AMI is very high (approximately 95%) in tissue and plasma (Burch et al., 1981; Levitt et al., 1986; https://www.drugbank.ca/drugs/DB00321) which reduces the ability of AMI to cross the BBB due to increased size and altered physicochemical properties. The equilibrium between the bound and unbound AMI fraction is rather sensititve to pH and to the protein concentration (unpublished data from our group).
Differential inhibition of cardiac and neuronal Na<sup>+</sup> channels by the selective serotonin-norepinephrine reuptake inhibitors duloxetine and venlafaxine
2016, European Journal of PharmacologyCitation Excerpt :The most likely explanation may be the aforementioned strong protein binding of duloxetine in human plasma (>90%). On the other hand, more than 90% of the plasma concentration of amitriptyline is bound to plasma proteins as well (Levitt et al., 1986). Another relevant issue is of course the fact that cardiotoxicity of several therapeutics is likely to result from an interaction with several cardiac target molecules.
Amitriptyline overdose treatment by pegylated anionic liposomes
2008, Journal of Colloid and Interface ScienceCitation Excerpt :A 90% free drug reduction implies a substantial drug–liposome affinity and a high degree of binding selectivity despite the presence of serum proteins. While these values may not correlate directly to in vivo applications due to the presence of the immune system and other factors, a free drug reduction in the blood stream of even 20% could be significant [30]. Thus, the systems tested here have a high likelihood of reducing toxicity in an overdosed patient.
Uptake of amitriptyline and nortriptyline with liposomes, proteins, and serum: Implications for drug detoxification
2008, Journal of Colloid and Interface ScienceCitation Excerpt :Finally, uptake studies conducted with nortriptyline, the major metabolite of amitriptyline, suggests that systems developed for amitriptyline overdose treatment may also be useful for reducing the free concentration of nortriptyline. While the presence of serum proteins reduces the drug binding capacity of liposomes, a 35–70% reduction in drug concentration, which is attainable by the systems explored here, may have significant benefits for overdosed patients [18]. Additionally, even the highest lipid loading used in this study is below the lipid loadings used in other related studies and so it may be feasible to increase the lipid loading or give multiple liposome injections to the overdosed patients.
Tricyclic and Other Cyclic Antidepressants
2007, Haddad and Winchester's Clinical Management of Poisoning and Drug Overdose, Fourth Edition
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Presented at the American Academy of Clinical Toxicology, San Diego, California, October 1984.