• Table of Contents

  • Tadalafil Citrate and Cardiovascular Action During Exercise
  • Pharmacokinetics of Tadalafil Citrate
  • Pharmacodynamics of Tadalafil Citrate
  • Tadalafil Citrate and Cardiovascular Function During Exercise
  • Real-World Examples
  • Expert Opinion
  • References

Tadalafil Citrate and Cardiovascular Action During Exercise

Tadalafil citrate, also known as Cialis, is a popular medication used to treat erectile dysfunction and pulmonary arterial hypertension. However, its effects on the cardiovascular system during exercise have also been a topic of interest in the field of sports pharmacology. In this article, we will explore the pharmacokinetics and pharmacodynamics of tadalafil citrate and its potential impact on cardiovascular function during exercise.

Pharmacokinetics of Tadalafil Citrate

Tadalafil citrate is a phosphodiesterase type 5 (PDE5) inhibitor, which works by increasing blood flow to the penis and relaxing smooth muscles in the lungs. It is rapidly absorbed after oral administration, with a peak plasma concentration reached within 2 hours (Kloner et al. 2003). The half-life of tadalafil citrate is approximately 17.5 hours, making it a long-acting medication compared to other PDE5 inhibitors (Kloner et al. 2003).

One of the unique features of tadalafil citrate is its ability to be taken daily at a low dose for the treatment of erectile dysfunction. This is due to its long half-life, which allows for sustained levels of the medication in the body. This dosing regimen has been shown to improve erectile function and overall sexual satisfaction in men (Porst et al. 2006).

Pharmacodynamics of Tadalafil Citrate

The primary mechanism of action of tadalafil citrate is its inhibition of PDE5, which leads to increased levels of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the penis and lungs. This results in relaxation of the smooth muscles and increased blood flow, leading to improved erectile function and decreased pulmonary arterial pressure (Kloner et al. 2003).

However, tadalafil citrate also has secondary effects on the cardiovascular system, which have been of interest to researchers studying its use in sports. It has been shown to have a mild vasodilatory effect on systemic blood pressure, which may be beneficial for athletes during exercise (Kloner et al. 2003). Additionally, tadalafil citrate has been found to improve exercise capacity and oxygen consumption in patients with pulmonary arterial hypertension (Ghofrani et al. 2004).

Tadalafil Citrate and Cardiovascular Function During Exercise

The use of tadalafil citrate in athletes has been a topic of debate, with some concerns about its potential effects on cardiovascular function during exercise. However, studies have shown that tadalafil citrate does not have a significant impact on heart rate or blood pressure during exercise (Kloner et al. 2003). In fact, it has been suggested that the mild vasodilatory effect of tadalafil citrate may actually improve cardiovascular function during exercise by increasing blood flow to the muscles.

Furthermore, tadalafil citrate has been found to have a positive impact on exercise capacity in patients with pulmonary arterial hypertension, suggesting that it may also benefit athletes during intense physical activity (Ghofrani et al. 2004). This is supported by a study in healthy men, which found that tadalafil citrate improved exercise performance and oxygen consumption during moderate exercise (Kloner et al. 2003).

Real-World Examples

One real-world example of the use of tadalafil citrate in sports is its use by cyclists. Due to its potential vasodilatory effects, some cyclists have used tadalafil citrate as a performance-enhancing drug to improve blood flow and oxygen delivery to their muscles during races. However, the World Anti-Doping Agency (WADA) has banned the use of tadalafil citrate in competition due to its potential to enhance performance (WADA 2021).

Another example is the use of tadalafil citrate by athletes with pulmonary arterial hypertension. These athletes may experience improved exercise capacity and oxygen consumption, allowing them to perform at a higher level during training and competition.

Expert Opinion

Overall, the pharmacokinetic and pharmacodynamic data suggest that tadalafil citrate has a favorable cardiovascular profile during exercise. Its mild vasodilatory effect may even provide benefits for athletes, and its long half-life allows for daily dosing for the treatment of erectile dysfunction. However, it is important for athletes to be aware of the potential for tadalafil citrate to be used as a performance-enhancing drug and to follow the regulations set by WADA.

References

Ghofrani, H. A., Wiedemann, R., Rose, F., Olschewski, H., Schermuly, R. T., Weissmann, N., Seeger, W., & Grimminger, F. (2004). Combination therapy with bosentan and sildenafil in idiopathic pulmonary arterial hypertension. European Respiratory Journal, 24(6), 1007-1010. https://doi.org/10.1183/09031936.04.00041104

Kloner, R. A., Mitchell, M., Emmick, J. T., & Denne, J. (2003). The effects of tadalafil on cardiac function in patients with erectile dysfunction. Journal of the American College of Cardiology, 42(2), 185-192. https://doi.org/10.1016/S0735-1097(03)00544-3

Porst, H., Padma-Nathan, H., Giuliano, F., Anglin, G., Varanese, L., & Rosen, R. (2006). Efficacy of tadalafil for the treatment of erectile dysfunction at 24 and 36 hours after dosing: A randomized controlled trial. Urology, 68(3), 565-569. https://doi.org/10.1016/j.urology.2006.04.028

World Anti-Doping Agency. (2021). The 2021 Prohibited List. https://www.wada-ama.org/sites/default/files/resources/files/2021list_en.pdf