Telmisartan

Millions of people worldwide again watch the Olympic Games (in Rio). These are organized by a highly corrupt organization called the IOC, similar to FIFA. To conceal their corruption and extreme luxurious global lifestyle, these organizations abuse the athletes on which they parasitize. By accusing athletes of cheating and abuse of illegal substances, which are declared illegal by the same organization.

This through organizations to combat doping, and to test athletes also off-season, such as WADA. The sensational mass media report faithfully what WADA tells them. Naturally, the IOC is also abused for political purposes. Now Russia, and especially Russian athletes are being victimized. An innocent drug as Meldonium was only used an excuse. I wrote about it here. Meldonium is banned since January 2016 but Telmisartan is still allowed by WADA and has much benefits for athletes as well as bodybuilders.

Hypertension

High blood pressure (hypertension) is a cardiovascular risk factors that affects a huge percentage of the population. The estimation is that one out of every three American adults suffers from hypertension with systolic readings greater than 140. Another one out of three has prehypertension levels of between 120 and 140. Normal systolic blood pressure is 120 or less. This means that tens of millions of Americans at increased risk for heart attack, stroke and serious cardiovascular incidents due to prehypertension and hypertension.

Starting an steroid cycle will increase cardiovascular risks. An occasional steroid cycle may only cause transient changes in blood lipid values (e.g. triglycerides, HDL cholesterol, etc.) and blood pressure readings. However, the current patterns of steroid use are such that increasing numbers of users are doing multiple cycles per year for several years or even decades. Some bodybuilders are even using steroids continuously (or cruising on supra-physiological dosages of testosterone e.g. 200-400mg/week) for the same extended periods of time. This type of chronic steroid use could lead to more long-term problems.

It's not so much that steroids cause people to develop cardiovascular disease. Many men already have risk factors and/or may develop problems as they get older, with or without steroids, due to genetics and/or other lifestyle factors unrelated to steroids. But if any of these factors are present, bodybuilding dosages of steroids generally only make matters worse.

Telmisartan (brand name Micardis) is an angiotensin II receptor antagonist (angiotensin receptor blocker, ARB) used in the management of hypertension. It may not be the most popular anti-hypertension drug currently prescribed. Doctors may prefer to prescribe other drugs such as lisinopril (brand names Prinivil and Zestril) from the angiotensin-converting enzyme (ACE) inhibitor cateogry; metoprolol (brand name Lopressor) from the beta blocker category; or even losartan (brand name Cozaar) from the same ARB category as telmisartan. However, telmisartan may be the best choice for steroid users particularly those with prehypertension or borderline high blood pressure.

Telmisartan

Telmisartan has been used by endurance athletes as an alternative to the banned substances AICAR and GW1516. It is also a relatively safe and non-toxic drug used by athletes in dosages of 80-160 mg/day in divided dosages. The latter two drugs have been banned. Sanchis-Gomar et al concluded in 2012 that Telmisartan has been shown to act by a similar mechanism as AICAR and GW1516.

Specifically, telmisartan promises to enhance running ability, increase fat burning ability, reduce lactic acid formation and enhance recovery from exercise. It is broadly assumed that telmisartan has performance-enhancing effects well beyond the health-promoting benefits. It is rumored that professional cyclists have been using telmisartan for many years to enhance endurance. Telmisartan's pharmacological effect of PPAR-delta activation can significantly increase muscular endurance via increased oxidative capacity of type II muscle fibers. However, its actual performance-enhancing effects remain the subject of debate.

Not all ARB's are equal

Fabian Sanchis-Gomar and Giuseppe from the University of Valencia, in 2012 concluded that telmisartan prevents adipogenesis and weight gain through the activation of PPAR-d-dependent lipolytic pathways and energy uncoupling in several tissues.

The authors reported however that 2 other ARBs such as candesartan and losartan do not affect PPAR-d pathway. It has been suggested that the chemical structure of telmisartan (delta lock) is involved in its strongest binding affinity to angiotensin 1 receptor, thereby displaying greater properties in vivo than any other ARB. Nevertheless, the precise mechanism of the PPAR-d-AMPK pathway activation by telmisartan (Micardis), and not by other ARBs remains unclear so far.

Other research revealed that telmisartan is more effective than other ARBs in reducing body weight gain, renal inflammation, and renal injury in a rat model of cardiometabolic syndrome. Other ARBs include candesartan (Atacand), Valsartan (Diovan), and fimasartan (Kanarb).

Burks et al. 2011 were interested in the beneficial impact on the muscle remodeling process of sarcopenic mice by losartan, an angiotensin II receptor antagonist (ARA) commonly used to treat high blood pressure. In their study, they showed that immobilized mice treated with losartan were protected against loss of muscle mass and that this protective mechanism was mediated by an increased activation of the insulin-like growth factor 1 (IGF-1) /Akt/mammalian target of rapamycin (mTOR) pathway. Thus, blockade of the AT1 (angiotensin II type I) receptor improved muscle remodeling and protected against disuse atrophy.

Moreover, telmisartan, has been suggested to improve skeletal muscle function and to prevent adipogenesis and weight gain through activation of PPAR-delta-dependent pathways (Feng et al., 2010; He et al., 2010). Consequently, telmisartan may be used as a pharmacological intervention to treat sarcopenia.

Promoting the quality of life of elderly persons (health span) by preventing the age-associated decrease in muscle mass (sarcopenia) is one of the most important challenges in current clinical medicine. On the other hand, preventing the muscle mass loss due for instance to immobilization is one of the most important aims in today's medical care. The translation of discoveries in basic science into clinical care rarely comes easy but drugs such as losartan, telmisartan or allopurinol, all of them approved by the Food and Drug Administration for the treatment other diseases, may be useful to prevent muscle loss in the fields of Geriatrics, Sport Medicine, Traumatology, and Rehabilitation

Slowing down the loss of brain function with age, or even potentially improving brain function, no fiction but thorough scientific research.

Gąseckii et al 2013: There is growing evidence that hypertension is the most important modifiable vascular risk factor for development and progression of both cognitive decline and dementia.

Possitive effect of telmisartan on cognition and regional cerebral blood flow in hypertensive patients with Alzheimer Disease.

Kishi et al 2012: Telmisartan protects against cognitive decline via up-regulation of BDNF/TrkB in the hippocampus of SHRSPs, partly because of PPAR-gamma activation independent of blood pressure-lowering effect.

Singh et al 2013: Hence on the basis of the above discussion it may be concluded that the ACEI, lisinopril, as well as the ARB, telmisartan, provide beneficial effects by improving learning, memory, brain cholinergic activity, inflammatory status and oxidative stress in i.c.v. STZ induced dementia of AD in mice. Furthermore, the beneficial effects of lisinopril and telmisartan also involve PPAR-Оі modulation. Nevertheless further studies are needed to establish the full potential and mechanism of these drugs in dementia of AD type.

Younis et al 2016: Type 2 diabetes and hypertension are associated with cognitive dysfunction that includes pathological changes in brain tissue. It was speculated that the beneficial hypotensive effect of telmisartan, an angiotensin receptor 1 blocker, and its unique hypoglycemic effect due to its PPARγ-activation, could ameliorate the ​ pathological changes in the brain​ that accompany​ these diseases.

LVH (left ventricular hypertrophy)

Animal models have also shown that telmisartan reduces left ventricular hypertrophy (LVH) and reduces visceral fat. This should be of particular interest to bodybuilders. LVH is an adaptive response to intense weight training whose effects are amplified by steroid use. LVH is generally benign in highly trained athletes but it is associated with decreased cardiac function particularly as an athlete ages. Reductions in visceral fat are also associated with decrease cardiovascular risk.

A Japanese animal study in 2006 wanted to clarify the effect of telmisartan on the development of obesity and related metabolic disorders in diet-induced obese mice. Treatment with telmisartan dissolved in drinking water at a dosage of 5 mg/kg per day for 14 days attenuated the diet-induced weight gain without affecting food intake in diet-induced obese mice compared with controls using non-treated water. Telmisartan treatment decreased the weight of visceral adipose tissue and the triglyceride content in the liver and skeletal muscle. In addition, hyperglycemia, hyperinsulinemia, and hypertriglyceridemia in diet-induced obese mice all improved with telmisartan treatment. Furthermore, telmisartan treatment increased adiponectin mRNA in visceral white adipose tissue and was associated with a concomitant change in the serum adiponectin level. In contrast, the treatment reduced the serum level of resistin. Finally, telmisartan treatment increased the mRNA expression of uncoupling protein 1 in brown adipose tissue and was accompanied by an increase in oxygen consumption. In conclusion, telmisartan treatment might prevent the development of obesity and related metabolic disorders by altering the levels of adiponectin, resistin, and uncoupling protein 1 in diet-induced obese mice. The results indicated that telmisartan can be used as a therapeutic tool for metabolic syndrome, including visceral obesity. In the figure CONT stands for the animals in the control group. CONT - TEL = control + telmisartan. HF = animals fattened with high fat. HF + TEL = high fat + telmisartan.

ARBs on ED (erectile dysfunction)

Drugs known as ARBs (angiotensin II receptor blockers) are not only unlikely to cause erection problems, but they may improve sexual function in men with high blood pressure.

In one study after 10 weeks of treatment with an ARB called losartan (Cozaar), 88% of hypertensive males with sexual dysfunction reported improvement in at least one area of sexuality, and overall sexual satisfaction improved from 7.3% to 58.5%

The percentage of men who reported having erectile dysfunction dropped from 75% to 12%.

Another study compared the drug Diovan, an ARB, with Coreg, a beta-blocker. The study compared the effect of the two drugs on blood pressure and frequency of sexual intercourse.

The drugs controlled blood pressure equally well. But people who took the ARB reported having sex more often during the 16 weeks of treatment. They said they had sex about eight times a month before, and 10 times a month after. People taking the beta-blocker had sex much less often: eight times a month before, and four times a month after.

Manolis et al 2012: Older antihypertensive drugs (diuretics, beta blockers) exert detrimental effects on erectile function whereas newer drugs (angiotensin receptor blockers) have neutral or even beneficial effects.