Telmisartan, sold under the brand name Micardis among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease.
It is taken orally.
It is available as the combination with hydrochlorothiazide, cilnidipine and amlodipine.
It has a relatively high dosing, on average 80 mg/day.
Drug class-Angiotensin II receptor antagonist.
Bioavailability 42–100%.
Protein binding> 99.5%.
Metabolism – Minimal liver by glucuronidation.
Elimination half-life 24 hours
Excretion- Feces 97%
Common side effects: upper respiratory tract infections, diarrhea, and back pain.
Serious side effects: include kidney problems, low blood pressure, and angioedema.
Use in pregnancy and breastfeeding is not recommended.
Contraindications: during pregnancy, as it can cause birth defects, stillbirths, and neonatal deaths.
It is contraindicated in bilateral renal artery stenosis in which it can cause kidney failure.
Side effects are similar to other angiotensin II receptor antagonists: include tachycardia and bradycardia, hypotension, and angioedema.
It increases blood potassium levels.
In combination with potassium preparations or potassium-sparing diuretics could cause hyperkalemia
Combination with NSAIDs, especially in patients with impaired kidney function, has a risk of causing kidney failure.
It is an angiotensin II receptor blocker that shows high affinity for the angiotensin II receptor type 1 (AT1), with a binding affinity 3000 times greater for AT1 than AT2.
It blocks the renin–angiotensin system, and acts as a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism.
It activates PPAR-δ receptors in several tissues.
This dual mode of action provides protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease.
Its average bioavailability is about 50%.
Plasma protein binding is over 99.5%, mainly to albumin and glycoprotein.
Telmisartan has the longest half-life of any angiotensin II receptor blocker (ARB) at 24 hours.
It has the largest volume of distribution among ARBs (500 liters).
97% of the drug eliminated in unchanged form via bile and feces.
Less than 3% of telmisartan is inactivated by glucuronidation in the liver.