The effects of exercise and adrenaline infusion upon the blood levels of propranolol and antipyrine in the horse.
Abstract: There are now several examples showing that experimentally induced changes in hepatic blood flow can have a marked effect upon the elimination of certain high clearance drugs. Changes in hepatic blood flow produced by exercise might therefore be expected to influence the clearance of these drugs. There was an increase of up to 100%, compound to control values, in the plasma levels of propranolol in horses given either d- or dl-propranolol, 0.2 mg/kg b.wt., and then subjected to sustained exercise for 30 minutes. There was, however, no similar increase with exercise in the plasma levels of antipyrine in horses given antipyrine, 50 mg/kg b.wt. Intravenous infusions of adrenaline, 1 microgram/kg b.wt./min for 10 minutes also produced an increase of about 70% in the plasma levels of d-propranolol.
Publication Date: 1978-06-01 PubMed ID: 660540
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- Journal Article
Summary
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The study explores the impact of exercise and adrenaline infusion on the blood levels of propranolol and antipyrine in horses. It finds that exercise causes a significant increase in propranolol levels but not in antipyrine, and adrenaline infusion raises d-propranolol levels considerably.
Background
- The research goes into various evidences that demonstrate that experimental changes in hepatic blood flow significantly affect the elimination of certain drugs with high clearance rates.
- The study builds upon the hypothesis that changes in hepatic blood flow brought on by physical exercise can influence the clearance of these drugs in the body.
Impact of Exercise on Drug Levels
- Horses given either d-propranolol or dl-propranolol, and then subjected to sustained exercise for 30 minutes, displayed an increase of up to 100% in their plasma levels of propranolol, as compared to control values/li>
- Interestingly, there was no analogous increase observed in the plasma levels of antipyrine in horses that were administered the substance and subjected to similar exertion.
Impact of Adrenaline on Drug Levels
- Another aspect explored by the study was the impact of intravenous adrenaline infusions on plasma drug levels.
- On integrating adrenaline into the equine system at a rate of 1 microgram/kg body weight per minute over a 10-minute period, a notable surge of about 70% was observed in the plasma levels of d-propranolol.
- Thus, adrenaline infusion was associated with a significant increase in the blood concentration of d-propranolol.
Conclusion
- The research concludes that both exercise and adrenaline infusion have a marked effect on the blood levels of propranolol in a horse’s system.
- Exercise and adrenaline appear to affect the clearance of high clearance drugs like propranolol but not antipyrine, indicating that hepatic blood flow changes likely play a crucial role in the clearance of specific drugs in horses.
Cite This Article
APA
Powis G, Snow DH.
(1978).
The effects of exercise and adrenaline infusion upon the blood levels of propranolol and antipyrine in the horse.
J Pharmacol Exp Ther, 205(3), 725-731.
Publication
Researcher Affiliations
MeSH Terms
- Animals
- Antipyrine / blood
- Blood Proteins / metabolism
- Drug Interactions
- Epinephrine / pharmacology
- Horses / blood
- Physical Exertion
- Propranolol / blood
- Protein Binding / drug effects
- Time Factors
Citations
This article has been cited 8 times.- Lenz TL, Lenz NJ, Faulkner MA. Potential interactions between exercise and drug therapy. Sports Med 2004;34(5):293-306.
- Tesseromatis C, Trichilis A, Tsivos E, Messari J, Triantaphyllidis H, Varonos DD. Does stress influence ampicillin concentration in serum and tissues?. Eur J Drug Metab Pharmacokinet 2001 Jul-Sep;26(3):167-71.
- Vanakoski J, Seppälä T. Effects of a Finnish sauna on the pharmacokinetics and haemodynamic actions of propranolol and captopril in healthy volunteers. Eur J Clin Pharmacol 1995;48(2):133-7.
- Hurwitz GA, Webb JG, Walle T, Bai SA, Daniell HB, Gourley L, Boyd Loadholt C, Gaffney TE. Exercise-induced increments in plasma levels of propranolol and noradrenaline. Br J Clin Pharmacol 1983 Dec;16(6):599-608.
- Arnold JM, McDevitt DG. Heart rate and blood pressure responses to intravenous boluses of isoprenaline in the presence of propranolol, practolol and atropine. Br J Clin Pharmacol 1983 Aug;16(2):175-84.
- McInnes GT, Brodie MJ. Concentration-effect relationships for oxprenolol in patients with essential hypertension. Br J Clin Pharmacol 1988 May;25(5):539-45.
- Van Baak MA. Beta-adrenoceptor blockade and exercise. An update. Sports Med 1988 Apr;5(4):209-25.
- van Baak MA. Influence of exercise on the pharmacokinetics of drugs. Clin Pharmacokinet 1990 Jul;19(1):32-43.
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