Relative binding of therapeutic drugs by sera of seven mammalian species.
Abstract: The relative binding of acetaminophen, lidocaine, phenobarbital, procainamide, quinidine, and theophylline to sera of seven mammalian species was studied. Pooled commercial sera from cow, goat, horse, human, pig, rabbit, and sheep were supplemented with 5 and 10 mM concentrations of each drug. For each serum, each drug, and each drug concentration, equilibrium dialysis was performed in duplicate against phosphate buffer (pH 7.4, 0.1 M, 4 degrees C). Percent drug bound to serum was calculated. Phenobarbital demonstrated more than 20% binding to goat, horse, human, and sheep serum at both 5 and 10 mM concentrations; more than 20% binding to bovine serum at a concentration of 10 mM; and more than 20% binding to pig and rabbit serum at 5 mM. Quinidine (studied only at 5mM concentration) bound more than 20% to cow, goat, horse, human, pig, and rabbit serum. In contrast, procainamide at both the 5 and 10 mM concentrations showed no binding to cow, horse, pig, rabbit, or sheep serum. Acetaminophen (studied only at 5 mM concentration), lidocaine, and theophylline demonstrated less than 20% binding to each serum. Acetaminophen at 5 mM did not bind to human serum, and lidocaine at 10 mM did not bind to horse or pig serum. Although some interspecies variation in drug binding to the seven sera was noted, the overall magnitude of binding of each drug to each serum was, for the most part, similar. Phenobarbital and quinidine showed stronger (> 20%) binding; procainamide showed negligible binding; and acetaminophen, lidocaine, and theophylline demonstrated intermediate (< 20%) binding.
Publication Date: 1998-12-10 PubMed ID: 9847009DOI: 10.1093/jat/22.7.587Google Scholar: Lookup
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- Journal Article
Summary
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The research paper describes a study into how well different drugs bind to the serum (part of blood) in different mammalian species. The drugs tested were Acetaminophen, Lidocaine, Phenobarbital, Procainamide, Quinidine, and Theophylline. The results of this study provide important information for understanding how these drugs interact within the bodies of different mammals.
Research Methodology
- The researchers used pooled commercial serum extracted from seven different mammalian species: cow, goat, horse, human, pig, rabbit, and sheep.
- The serum was mixed with each drug at two concentrations (5 and 10 mM) and then underwent a process called equilibrium dialysis, which is a method used to study how a drug binds to a substance in the body.
- This process was carried out twice for every combination of serum, drug and drug concentration.
- The percentage of each drug that successfully bound itself to the serum was then calculated.
Research Findings
- Phenobarbital displayed significant binding affinity (>20%) to most of the serums tested at both concentrations, most notably to goat, horse, human, and sheep serum.
- Quinidine also showed similar strong binding affinity, but was only tested at the 5 mM concentration. It bound well to sera of cow, goat, horse, human, pig, and rabbit.
- Procainamide, on the other hand, showed negligible binding to most types of serum at both concentrations.
- Acetaminophen, Lidocaine, and Theophylline demonstrated less binding (<20%) to all the serum types tested. It was noted that Acetaminophen did not bind to human serum and Lidocaine showed no binding to horse or pig serum at the 10 mM concentration.
- Although there were differences (interspecies variations) in how each drug bound to the different types of serum, the overall pattern of binding was relatively similar across the seven mammalian species tested.
In conclusion, the study offers valuable insights on how different drugs bind to the serum in various mammalian species, which has implications for animal and human health, as well as drug design and dosage considerations. Phenobarbital and Quinidine showed the strongest binding, Procainamide showed the least, and Acetaminophen, Lidocaine, and Theophylline showed intermediate binding.
Cite This Article
APA
Bailey DN.
(1998).
Relative binding of therapeutic drugs by sera of seven mammalian species.
J Anal Toxicol, 22(7), 587-590.
https://doi.org/10.1093/jat/22.7.587 Publication
Researcher Affiliations
- Department of Pathology, University of California Medical Center, San Diego 92103-8320, USA.
MeSH Terms
- Acetaminophen / blood
- Animals
- Blood Proteins / analysis
- Cattle
- Horses
- Humans
- Lidocaine / blood
- Pharmaceutical Preparations / metabolism
- Phenobarbital / blood
- Procainamide / blood
- Quinidine / blood
- Rabbits
- Sheep
- Species Specificity
- Swine
- Theophylline / blood
Citations
This article has been cited 2 times.- Yates LM, Aleman M, Knych HK, Knipe MF, Crowe CM, Chigerwe M. Pharmacokinetics of Intravenous and Oral Phenobarbital Sodium in Healthy Goats. Front Vet Sci 2020;7:86.
- Prot JM, Briffaut AS, Letourneur F, Chafey P, Merlier F, Grandvalet Y, Legallais C, Leclerc E. Integrated proteomic and transcriptomic investigation of the acetaminophen toxicity in liver microfluidic biochip. PLoS One 2011;6(8):e21268.
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