Tadalafil (Cialis) has been the subject of applications from fitness enthusiasts and bodybuilders for a while now, but why exactly is it. Aside from its use as a treatment for Erectile Dysfunction, it has many pleiotropic benefits (benefits aside from the purpose its taken for). This includes many performance enhancing and even health benefits, as well as orgasmic function, and boosted confidence amongst some users.

Blood Pressure Management: Tadalafil is used to lower blood pressure, especially when using performance-enhancing drugs (PEDs). It helps maintain blood pressure during intense exercises and protects the kidneys (which I will discuss more later). The typical dosage for blood pressure management is between 5-20 mg.

Upregulation of androgen receptors: Androgen receptors are the primary target of androgens in your body as well as synthetic androgens. Binding to androgen receptors leads to the upregulation of genes that leads to muscular hypertrophy. Cialis has been shown to upregulate androgen receptors.

Tadalafil (Cialis) is a substance that increases intracellular cyclic adenosine monophosphate (cAMP) concentrations, which may have both direct and indirect effects on androgen-mediated gene transcription. How does cAMP interact with the AR? cAMP activates a protein called PKA (protein kinase A). PKA can directly add a phosphate group to ARs at certain spots (like Ser81/94/650).

Improved Blood Flow: Tadalafil increases blood flow by opening up capillaries. This can help transport fat away from stubborn areas during a cutting phase and deliver nutrients to muscles. It may also help with fat storage during bulking. By increasing blood flow to the muscles, tadalafil enhances muscle pumps during workouts. This effect is further enhanced by the delivery of nutrients and removal of metabolic waste products.

Improvements of insulin sensitivity, fat loss and metabolism: Tadalafil can increase plasma fatty acids and glycerol levels, promoting fat loss, and improve glucose homeostasis and insulin sensitivity. This seems to be particularly prevelant for those with metabolic syndrome due to improvements in beta-cell function. Low and consistent doses of tadalafil are more effective for fat loss and muscle growth than on-demand higher doses.

Improved Athletic Performance: Tadalafil has potential performance-enhancing effects, including improvements in glucose metabolism and potential enhancements in endurance and stamina.

Kidney Health: Tadalafil is a vasodilator that helps to open up blood vessels, which lowers blood pressure, which for those outside of the healthy range, may help bring them in range and prevents excessive pressure on the kidneys.

Additionally intense exercises like heavy squats and deadlifts can cause a significant spike in blood pressure, of which Tadalafil can reduce and prevent from climbing too high during these exercises, thus protecting the kidneys

Tadalafil may also improve depressive symptoms.

( Kim KS, Jeong TY, Moon HS. Effect of daily tadalafil on reported outcomes in patients with erectile dysfunction and depressive symptoms: STROBE, a case-control study. Medicine (Baltimore). 2020 Jun 5;99(23):e20546. doi: 10.1097/MD.0000000000020546. PMID: 32502017; PMCID: PMC7306377. )

I may explore the cognitive effects of Tadalafil in a separate article, however I want to talk about dosages and timing of administration as I believe this topic is of great importance.

Dosages of Tadalafil range from 2.5 to 20 milligrams. The dose should depending on the purpose, individual needs, and tolerance. Consider booking in a consultation to decide whats best for your goals For daily use, 2.5 to 5 mg is more common. On-demand dosages of 10 to 20 mg are taken 30 minutes before sexual activity, but try not to exceed three times weekly and start of a low dose first. If your taking it before weighlifting, take it 30-60 minutes before. 

Tadalafil has limited with other performance enhancing drugs, however is not apart of WADA prohibited drug list at the time of writing.

References:

Patterson D, McInnes GT, Webster J, Mitchell MM, Macdonald TM. Influence of a single dose of 20 mg tadalafil, a phosphodiesterase 5 inhibitor, on ambulatory blood pressure in subjects with hypertension. Br J Clin Pharmacol. 2006 Sep;62(3):280-7. doi: 10.1111/j.1365-2125.2006.02658.x. PMID: 16934043; PMCID: PMC1885145.

Aversa A, Fittipaldi S, Francomano D, Bimonte VM, Greco EA, Crescioli C, Di Luigi L, Lenzi A, Migliaccio S. Tadalafil improves lean mass and endothelial function in nonobese men with mild ED/LUTS: in vivo and in vitro characterization. Endocrine. 2017 Jun;56(3):639-648. doi: 10.1007/s12020-016-1208-y. Epub 2017 Jan 30. PMID: 28133708.

Marampon F, Antinozzi C, Corinaldesi C, Vannelli GB, Sarchielli E, Migliaccio S, Di Luigi L, Lenzi A, Crescioli C. The phosphodiesterase 5 inhibitor tadalafil regulates lipidic homeostasis in human skeletal muscle cell metabolism. Endocrine. 2018 Mar;59(3):602-613. doi: 10.1007/s12020-017-1378-2. Epub 2017 Aug 7. PMID: 28786077.

Guidetti L, Emerenziani GP, Gallotta MC, Pigozzi F, Di Luigi L, Baldari C. Effect of tadalafil on anaerobic performance indices in healthy athletes. Br J Sports Med. 2008 Feb;42(2):130-3. doi: 10.1136/bjsm.2007.037630. Epub 2007 Jun 22. PMID: 17586581.

Ho JE, Arora P, Walford GA, Ghorbani A, Guanaga DP, Dhakal BP, Nathan DI, Buys ES, Florez JC, Newton-Cheh C, Lewis GD, Wang TJ. Effect of phosphodiesterase inhibition on insulin resistance in obese individuals. J Am Heart Assoc. 2014 Sep 11;3(5):e001001. doi: 10.1161/JAHA.114.001001. PMID: 25213566; PMCID: PMC4323801.

Ceci, R. et al. (2017) Acute tadalafil administration increases plasma fatty acids without changes in the inflammatory response in healthy men. Acta Biochimica Polonica, 64(4):687-691. doi: 10.18388/abp.2017_2205