Telmisartan is a nonpeptide AT1 angiotensin II receptor antagonist. It exerts antihypertensive activity by preventing angiotensin II from binding to AT1 receptors thus inhibiting the vasoconstricting and aldosterone-secreting effects of angiotensin II.

Onset: 1-2 hr.

Duration: Up to 24 hr.

Absorption: Rapidly absorbed from the GI tract. Food may slightly decrease the bioavailability. Absolute bioavailability: Dose-dependent (approx 42% after 40-mg dose; 58% after 160-mg dose). Time to peak plasma concentration: Approx 0.5-1 hr.

Distribution: Volume of distribution: 500 L. Plasma protein binding: >99%.

Metabolism: Undergoes conjugation w/ glucuronic acid to form inactive metabolites

Excretion: Via faeces (97%, as unchanged drug). Terminal elimination half-life: Approx 24 hr.

Dizziness, fatigue, headache, sinusitis, upper resp tract infection, pharyngitis, UTI, back pain, myalgia, diarrhoea, abdominal pain, dyspepsia, nausea. Potentially Fatal: Intermittent claudication and skin ulcer.

Volume- or salt-depleted patients including patients on prolonged diuretic therapy. Patients w/ renal artery stenosis, aortic or mitral stenosis, obstructive biliary disease. Renal and mild to moderate hepatic impairment. Lactation. Monitoring Parameters Monitor BP, electrolytes and serum creatinine levels.

HTN Initial: 40 mg once daily, may be adjusted to 20-80 mg once daily. CV risk reduction 80 mg once daily.