Telmisartan

Products

Telmisartan is commercially available in tablet form (Micardis, Micardis Plus + hydrochlorothiazide, generics). It has been approved in many countries since 1998. Generics entered the market in December 2013. In 2010, a fixed combination with amlodipine was registered (Micardis Amlo). Kinzal is no longer marketed in many countries.

Structure and properties

Telmisartan (C33H30N4O2, Mr = 514.6 g/mol) is an indole, carboxybiphenyl and benzimidazole derivative. It exists as a white to yellowish powder that is practically insoluble in water.

Effects

Telmisartan (ATC C09CA07) has antihypertensive properties by selectively and competitively abolishing the physiologic effects of angiotensin II at the AT1 receptor. Angiotensin II is a peptide hormone directly involved in the development of hypertension. It has a potent vasoconstrictor effect and increases aldosterone release, which in turn causes increased water and sodium retention. Telmisartan is also a partial agonist at PPAR-γ, a transcription factor involved in the regulation of glucose and lipid metabolism.

Indications

For the treatment of mild to moderate hypertension and to reduce the risk of myocardial infarction and stroke in patients with increased cardiovascular risk and/or type 2 diabetes mellitus.

Dosage

According to the SmPC. Telmisartan is administered in the morning at the same time of day and can be taken independently of meals. Because of its long half-life of approximately 20 hours, once-daily administration is sufficient. The usual dose is (20)-40-80 mg.

Contraindications

  • Hypersensitivity
  • Pregnancy and lactation
  • Severe liver dysfunction, obstructive biliary disease, cholestasis.
  • Previous angioedema under sartans or ACE inhibitors.
  • Combination with aliskiren in patients with diabetes mellitus or impaired renal function.

Full details of precautions and interactions can be found in the drug label.

Adverse effects

The most common possible adverse effects include low blood pressure, bradycardia, dizziness, hyperkalemia, sleep disturbances, dyspnea, digestive symptoms, rash, muscle pain, muscle cramps, back pain, and renal impairment.