Telmisartan, sold under the brand name Micardis among others, is a medication used to treat hypertension and heart failure.[ It is a reasonable initial treatment for high blood pressure.][ It is taken by mouth.][
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Common side effects include upper respiratory tract infections, diarrhea, and back pain.[ Serious side effects may include kidney problems, low blood pressure, and angioedema.][ Use in pregnancy may harm the baby and use when breastfeeding is not recommended.]
Telmisartan was patented in 1991 and came into medical use in 1999.
Medical uses
Telmisartan is used to treat hypertension, heart failure, and diabetic kidney disease.[ It is a reasonable initial treatment for high blood pressure.]
Contraindications
Telmisartan is contraindicated during pregnancy.[ It is not known whether the medication passes into breast milk.][
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Side effects
Side effects include tachycardia and bradycardia (fast or slow heartbeat), hypotension (low blood pressure) and edema (swelling of arms, legs, lips, tongue, or throat, the latter leading to breathing problems). Allergic reactions may also occur.[
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Interactions
Due to its mechanism of action, telmisartan increases blood potassium levels. Combination with potassium preparations or potassium-sparing diuretics could cause hyperkalaemia (excessive potassium levels). Combination with NSAIDs, especially in patients with impaired kidney function, has a risk of causing (usually reversible) kidney failure.
Pharmacology
Mechanism of action
Telmisartan 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.
In addition to blocking the renin–angiotensin system, telmisartan acts as a partial agonist of peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. It is believed that telmisartan's dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD).[
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Telmisartan's activity at the peroxisome proliferator-activated receptor delta (PPAR-δ) receptor has prompted speculation around its potential as a sport doping agent as an alternative to GW 501516.
Telmisartan activates PPAR-α in vitro.
Pharmacokinetics
The substance is quickly but to varying degrees absorbed from the gut. The average bioavailability is about 50% (42–100%). Food intake has no clinically relevant influence on the kinetics of telmisartan. Plasma protein binding is over 99.5%, mainly to albumin and alpha-1-acid glycoprotein.[Pritor prescribing information]
History
Society and culture
Telmisartan is available as a generic medication.[
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Research
Telmisartan does not appear effective for slowing the growth of abdominal aortic aneurysm.
Telmisartan does not cause rapid cancer growth like the PPAR-δ agonist GW 501516, but whether it causes a change in cancer rates is disputed. Short-term use is not associated with an increased incidence of cancer over other ARB drugs, according to a large 2016 analysis of UK patients.
Further reading
