Class: Angiotensin II receptor antagonist
- Tablets, oral 20 mg
- Tablets, oral 40 mg
- Tablets, oral 80 mg
Antagonizes the effect of angiotensin II (vasoconstriction and aldosterone secretion) by blocking the angiotensin II (AT 1 receptor) in vascular smooth muscle and the adrenal gland, producing decreased BP.
T max is 0.5 to 1 h. Food slightly reduces bioavailability of telmisartan, with an AUC reduction of approximately 6% with a 40 mg dose and 20% with a 160 mg dose. At 40 and 160 mg, the bioavailability was 42% and 58%, respectively. Trough plasma concentrations with daily dosing are approximately 10% to 25% of C max .
Telmisartan is more than 99.5% protein bound. Vd is approximately 500 L.
Telmisartan is metabolized by conjugation to form a pharmacologically inactive acyl glucuronide. The glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine.
Telmisartan half-life is approximately 24 h and total plasma Cl is more than 800 mL/min. After IV or oral administration, more than 97% is eliminated unchanged in feces via biliary excretion.
Special PopulationsRenal Function Impairment
Telmisartan is not removed from blood by hemofiltration.Hepatic Function Impairment
Plasma concentrations are increased and absolute bioavailability approaches 100%.Elderly
Pharmacokinetics do not differ between elderly patients and those younger than 65 y.Children
Pharmacokinetics have not been studied in patients younger than 18 y.Gender
Plasma concentrations are generally 2 to 3 times higher in women than in men.
Indications and Usage
Treatment of hypertension; for the reduction of the risk of MI, stroke, or death from CV causes in patients 55 y and older who are at high risk of developing major CV events and are unable to take ACE inhibitors.
Known hypersensitivity (eg, anaphylaxis, angioedema) to telmisartan or any component of this product.
Dosage and AdministrationHypertension
PO 20 to 80 mg/day; usual starting dosage, 40 mg/day.CV risk reduction
PO 80 mg once per day.Hepatic function impairment
PO Initiate at low doses and uptitrate slowly in patients with biliary obstructive disorders or hepatic insufficiency.
- May administer with or without food.
- May administer with other antihypertensive agents.
Store between 59° and 86°F.
Drug InteractionsACE inhibitors (eg, ramipril)
Plasma concentrations of ramipril and the active metabolite, ramiprilat, may be increased, while plasma concentrations of telmisartan may be reduced. When coadministered, the hypotensive response may be increased because of possible additive pharmacodynamic effects, and because of the increased exposure to ramipril and ramiprilat. Coadministration of telmisartan and an ACE inhibitor is not recommended.Digoxin
May increase plasma levels of digoxin, increasing the risk of toxicity. Monitor digoxin concentrations when starting, stopping, or changing the telmisartan dose. Adjust the digoxin dose as needed.Lithium
Plasma concentrations may be increased by telmisartan, resulting in an increase in the pharmacologic effects and adverse reactions of lithium. Monitor lithium serum concentrations. Adjust the lithium dose as needed.NSAIDs (eg, celecoxib, ibuprofen)
The antihypertensive effect of telmisartan may be attenuated by NSAIDs. In patients who are elderly or volume-depleted, or have compromised renal function, coadministration of NSAIDs with telmisartan may result in deterioration of renal function, including possible acute renal failure.Potassium-sparing diuretics (eg, amiloride)
The risk of hyperkalemia may be increased when a potassium-sparing diuretic is coadministered with telmisartan. Closely monitor serum potassium concentrations. Adjust treatment as needed.
Asthenia, dizziness, fatigue, headache, weakness (postmarketing).
Atrial fibrillation, BP increased, bradycardia, CHF, hypertension aggravated, hypotension (including postural hypotension), MI, syncope (postmarketing)
Skin ulcer (3%); erythema, sweating decreased, urticaria (postmarketing).
Sinusitis (3%); pharyngitis (1%).
Diarrhea (3%); abdominal pain, dyspepsia, nausea (postmarketing).
Erectile dysfunction, renal impairment including acute renal failure, UTI (postmarketing).
Decreased hemoglobin (1%); anemia, eosinophilia, thrombocytopenia (postmarketing).
Edema, face edema, hyperkalemia, hypoglycemia (in diabetic patients), increased CPK, lower limb edema, uric acid increased (postmarketing).
Back pain (3%); muscle cramps (including leg cramps), myalgia, rhabdomyolysis, tendon pain (including tendonitis), tenosynovitis (postmarketing).
Upper respiratory tract infection (7%); cough (2%).
Intermittent claudication (7%); abnormal hepatic function/liver disorder, anaphylactic reaction, angioedema (with fatal outcome), angioneurotic edema, chest pain, drug eruption (toxic skin eruption, mostly reported as toxicoderma, rash, and urticaria), hypersensitivity, pain (postmarketing).
When pregnancy is detected, discontinue telmisartan as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus.
Monitor BP closely. Monitor serum electrolytes to detect possible electrolyte imbalance. Dual blockade of the renin-angiotensin-aldosterone system (eg, by adding an ACE inhibitor) should include close monitoring of renal function. Monitor patients with hepatic insufficiency carefully.
Category D . May cause fetal harm.
Safety and efficacy not established.
Treatment may be associated with oliguria and/or progressive azotemia, acute renal failure, and/or death in patients with renal dysfunction.
Use with caution.
May occur, particularly in patients with advanced renal impairment, with heart failure, on renal replacement therapy, or on potassium supplements or other drugs that increase potassium levels.
Hypotension in volume-depleted patients
Symptomatic hypotension may occur after telmisartan initiation in intravascularly volume-depleted patients (eg, those treated with high-dose diuretics). Correct these conditions prior to administration or use a lower starting dose.
Use with caution in patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (eg, patients with severe CHF or renal dysfunction); use may be associated with oliguria, progressive azotemia, acute renal failure, and/or death. Changes in renal function (including acute renal failure) have been reported when adding an ACE inhibitor to an angiotensin II receptor antagonist.
Bradycardia, dizziness, hypotension, tachycardia.
- Inform women of childbearing age about the consequences of exposure to drugs that act directly on the renin-angiotensin system. Discuss treatment options with women planning to become pregnant. Advise these patients to report pregnancies to their health care provider as soon as possible.
Copyright © 2009 Wolters Kluwer Health.