Active ingredient: Telmisartan
Type: Antihypertensive agent, angiotensin II receptor antagonist (type AT1)
Form: Oral (pills)

Description

Telmisartan is antihypertensive agent, angiotensin II receptor antagonist (type AT1). It has a very high affinity for this receptor subtype. Telmisartan displaces angiotensin II from its association with AT1 receptors. Affinity for other subtypes of AT receptors was not found. The functional significance of other subtypes of receptors and the effect of elevated (as a result of the appointment of telmisartan) levels of angiotensin II on them is not known.

The Renin-Angiotensin-Aldosterone System (RAAS), is in charge of regulating blood pressure and fluid balance. It regulates its response to things such as angiotensin, a naturally occurring chemical that narrows your blood vessels and can increase blood pressure. One specific type of angiotensin – specifically, angiotensin 2 – is of importance to us here, because the use of anabolic steroids raises levels of this specific type of hormone.

Telmisartan reduces plasma aldosterone levels, but does not inhibit plasma renin, does not block ion channels, does not inhibit ACE (kinase II), which also destroys bradykinin. Therefore, there are no side effects associated with bradykinin.

Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because telmisartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Telmisartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of telmisartan on blood pressure.

Purpose to use

Telmisartan reduces left ventricular hypertrophy (LVH) and reduces visceral fat. This should be of particular interest to athletes. 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 age. Reductions in visceral fat are also associated with decreased cardiovascular risk. The use of telmisartan is a scientifically proven harm-reduction strategy that reduces overall mortality as well as the risks of cardiovascular diseases in particular.

Pharmacokinetics

When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is 50%. When taken simultaneously with food, the decrease in AUC ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, plasma concentration levels off, regardless of whether it is taken with food or on an empty stomach. Communication with plasma proteins is 99.5%. The average values of apparent Vd in the equilibrium stage are 500 l. Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. T1/2 – more than 20 hours. Excreted through the intestines unchanged. Cumulative excretion by the kidneys is less than 1%. Total plasma clearance – 1000 ml / min (renal blood flow – 1500 ml/min).

How to use

For adults, the daily dose is 20-40 mg (1 time/day). In some patients, the hypotensive effect can be achieved at a dose of 20 mg / day. If necessary, the dose can be increased to 80 mg/day.

Patients with impaired renal function, as well as elderly patients, dose adjustment is not required.

For patients with impaired liver function, recommended daily dose is 40 mg.

Dosages for athletes are the same – the use of a daily once-per-day dosage of 20 to 40mg to reduce the risk of atherosclerosis, cardiovascular disease and/or stroke in steroid-using bodybuilders with prehypertension. This can also lead to improvements in HDL cholesterol levels, insulin sensitivity, mitochondrial activity, endothelial function and cognitive function.