Telmiz Mechanism of Action

Pharmacology: Telmisartan is an orally effective and specific angiotensin II receptor (type AT₁) antagonist. Telmisartan displaces angiotensin II with very high affinity from its binding site at the AT₁ receptor subtype, which is responsible for the known actions of angiotensin II. Telmisartan does not exhibit any partial agonist activity at the AT₁ receptor. Telmisartan selectivity binds the AT₁ receptor. The binding is long lasting. Telmisartan does not show affinity for other receptor, including AT₂ and other less characterized AT receptors. The functional role of these receptors is unknown, nor is the effect of their possible over-stimulation by angiotensin II, whose levels are increased by telmisartan. Plasma aldosterone levels are decreased by telmisartan. Telmisartan does not inhibit human plasma renin or block ion channels. Telmisartan does not inhibit angiotensin converting enzyme (kininase II), the enzyme which also degrades bradykinin. Therefore, it is not expected to potentiate bradykinin-mediated adverse effects.
In patients with hypertension telmisartan reduces both systolic and diastolic blood pressure without affecting pulse rate. The antihypertensive efficacy of telmisartan has been compared to antihypertensive drugs such as amlodipine, atenolol, enalapril, hydrochlorothiazide, losartan, lisinopril, ramipril and valsartan.
Upon abrupt cessation of treatment with telmisartan, blood pressure gradually returns to pre-treatment values over a period of several days without evidence of rebound hypertension. Telmisartan treatment has been shown to be associated with reductions in left ventricular mass index in patients with hypertension and left ventricular hypertrophy.
Telmisartan treatment has been shown to be associated with reductions in proteinuria (including microalbuminuria and macroalbuminuria) in patients with hypertension and diabetic nephropathy.
The incidence of dry cough was significantly lower in patients treated with telmisartan than in those given angiotensin converting enzyme inhibitors.
Pharmacokinetics: Telmisartan is well absorbed following oral administration. TELMIZ tablet has been studied in a randomized, open-label, three-period, three-sequence, partial replicate design study under fasting conditions which included 33 healthy adult male subjects.
After oral administration of 80 mg TELMIZ tablet, the mean of AUC_0-72h was 5916.94 ng·h·mL^-1. The mean of maximum plasma concentration (C_max) was 1147.19 ng·mL^-1 and reached within 1.00 hour (0.50-4.00 hours). The mean elimination half-life (t_½) of TELMIZ tablet was 18.76 hours. The geometric mean ratios (90% confidence intervals) of TELMIZ tablet were 97.51% (92.73-102.54%) for AUC_0-72h and 88.90% (78.37-100.84%) for C_max. The result of this study showed that the pharmacokinetic parameters of TELMIZ tablet were within the acceptance range for bioequivalence, therefore, TELMIZ tablet were similar or bioequivalent to the reference drug.