• Telmisartan – cardiometabolic sartan

    January 13, 2015

    Telmisartan, which relates to the group of angiotensin receptor blockers (ARB), is distinguished from other sartans with its optimal pharmacokinetic profile and with some unique pharmacodynamic characteristics.

    Thanks to this, telmisartan has favorable gluco-metabolic effects – cardiometabolic sartan, and can be regarded as an antihypertensive agent of choice in patients with the simultaneous presence of arterial hypertension (AH) and metabolic syndrome and/or impaired glucose tolerance, or diabetes type 2 (DT2).

    The metabolic syndrome, which is associated with insulin resistance, is a combination of common cardiovascular risk factors such as hypertension, impaired glucose homeostasis, visceral obesity and atherogenic dyslipidaemia in the same individual.

    The lack of universally accepted definition hinders the collection of accurate epidemiological data, but it is assumed that 10-25% of the population in the developed countries fulfill the criteria for this disease.

    The reasons for this very high rate of prevalence are probably the widespread availability and easy access to high calorie (high in fat and refined carbohydrates) foods and a sedentary lifestyle. The presence of metabolic syndrome, in turn, implies a two to four-fold higher risk for cardiovascular morbidity and mortality, and five to nine-fold increase in the risk of developing DT2

    Why choose exactly telmisartan in the presence of metabolic syndrome?
    The main aim in the treatment of patients with metabolic syndrome is to reduce insulin resistance, and thus to prevent the occurrence of DT2 and adverse cardiovascular events.

    The renin-angiotensin-aldosterone system (RAAS) plays a key role in the pathogenesis of insulin resistance and cardiovascular complications in patients with or without the presence of DT2. Therefore, blocking the RAS with angiotensin-converting enzyme inhibitors (ACEi) or with ARB is the basis of modern therapy in this population.

    Telmisartan is the only sartan that has the unique effect of partial agonist of peroxisome proliferator activated receptor-gamma (PPAR-gamma). This receptor affects gene expression related to carbohydrate metabolism.

    For its agonists, pioglitazone and rosiglitazone, It is proven that its agonists, pioglitazone and rosiglitazone, improve the insulin resistance in patients with DT2. Accumulated is also significant amount of evidence that activators of PPAR-gamma have anti-inflammatory, antiproliferative and antioxidative effects on vascular cells, thus reducing the risk of developing atherosclerosis.

    The results of some preclinical and clinical studies have shown that administration of telmisartan can improve the carbohydrate and lipid metabolism (due to insulin sensibilisation effect) without exhibiting undesirable side effects associated with taking full PPAR-gamma agonists.

    Furthermore, telmisartan has longer lasting antihypertensive effect compared with the other ARB, which is probably due to the longest half-life the medicament (almost 24 hours) and the highest affinity for the type 1 angiotensin II receptor.
    Telmisartan also has the highest lipophilicity compared to other sartans that provides the largest volume of distribution and facilitate its penetration in various organs and tissues.

    The superiority of telmisartan over other sartans in terms of 24-hour BP control, especially in the early morning hours is proven. The described here unique qualities make telmisartan the recommended sartan, especially in cases where AH is accompanied by metabolic syndrome or DT2.

    Tchaikapharma High Quality Medicines Inc. now produces telmisartan under the trade name Telsart.

    Telsart is on the list of NHIF with the following code and price:

    Telsart 80 mg x 28 tabl. – CG021

    Price of free sale – BGN 5.64

    Reimbursement – BGN 2.64

    Additional payment by the patient – BGN 3.00

    Telsart has lowest price compared to all other competitors on the market – the additional payments under NHIF is only BGN 3.00 For other telmisartans the patient has to pay from BGN 5.15 to BGN 8.25. Calculated on the number of tablets Telsart again has the lowest price – BGN 0.11 per tablet.

    For further information on Telsart please check here: