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Transdermal nitrate therapy: bioavailability during exercise increases transiently after the daily change of patch
K Gjesdal1, T O Klemsdal, E O Rykke
1Oslo University Hospital Ullevål, Department of Cardiology, Norway.
British Journal of Clinical Pharmacology
|May 1, 1991
Summary
Transdermal glyceryl trinitrate (GTN) patches significantly increase nitrate availability during exercise. Replacing the patch further augmented GTN levels, enhancing exercise performance.
Area of Science:
- Pharmacology
- Exercise Physiology
- Cardiovascular Research
Background:
- Transdermal glyceryl trinitrate (GTN) is used for managing cardiovascular conditions.
- Understanding GTN pharmacokinetics during physical activity is crucial for optimizing its therapeutic effects.
Purpose of the Study:
- To investigate the impact of transdermal GTN on plasma nitrate concentrations during moderate exercise.
- To determine if renewing the GTN patch affects nitrate availability during sustained exercise.
Main Methods:
- Ten healthy volunteers applied a 10 mg/24h transdermal GTN patch.
- Plasma GTN concentrations were measured before, during, and after moderate exercise.
- Measurements were taken after initial patch application and after patch renewal.
Main Results:
- Plasma GTN concentrations increased by 19% (P<0.05) during exercise with the initial patch.
- Following patch renewal, repeat exercise led to a 56% increase in GTN concentration (P<0.001).
- The GTN concentration profiles differed significantly between the initial and renewed patch conditions (P<0.0001).
Conclusions:
- Transdermal GTN effectively increases systemic nitrate availability during moderate exercise.
- Renewing the transdermal GTN patch significantly augments nitrate availability during prolonged exercise.
- These findings suggest that optimizing GTN patch application can enhance its benefits during physical exertion.