Telmisartan

Telmisartan is an AT1 receptor blocker with the longest half-life of all sartans (approx. 24 hours). This means particularly consistent 24-hour blood pressure protection, including in the critical early morning hours.

Well-known brand names are Kinzalmono® and Micardis®. Telmisartan is also available in combination with hydrochlorothiazide (Micardis® Plus). It also causes mild PPAR-gamma activation, which can have a positive effect on metabolism.

Telmisartan blocks the AT1 receptor in a particularly long-lasting way:

Mechanism of action:

• Highly selective and long-lasting AT1 blockade
• Longest half-life of all sartans (approx. 24 hours)
• Lipophilic – high tissue penetration

Additional properties:

• Mild PPAR-gamma activation (metabolism-promoting)
• Can slightly improve insulin resistance
• Favorable effects on lipid metabolism

Clinical significance: In the ONTARGET trial, telmisartan was equivalent to the ACE inhibitor ramipril in high-risk patients.

Telmisartan is suitable for:

• Adults with high blood pressure
• Cardiovascular prevention in high-risk patients
• Patients who need a 24-hour effect

Particularly recommended for:

• Morning hypertension (morning rise in blood pressure)
• Metabolic syndrome
• Patients who do not tolerate ramipril

Not suitable:

• Pregnancy and breastfeeding
• Biliary obstruction
• Severe hepatic impairment

High blood pressure:

• Starting dose: 40 mg once daily
• Usual dose: 40-80 mg once daily
• Maximum dose: 80 mg daily

Cardiovascular prevention:

• 80 mg once daily

Available strengths:

• 20 mg, 40 mg, 80 mg tablets

Combination:

• Telmisartan + hydrochlorothiazide (Micardis® Plus)

How to take:

• Once daily, preferably in the morning
• Regardless of meals
• Take with water
• Do not split or chew the tablet

Notes:

• Regular blood pressure checks
• Laboratory checks (kidneys, potassium)
• Do not stop abruptly

Telmisartan must not be taken in cases of:

• Hypersensitivity to telmisartan
• Pregnancy in the 2nd and 3rd trimesters
• Biliary obstruction
• Severe hepatic impairment
• Concomitant use with aliskiren in diabetes or impaired renal function (GFR < 60 ml/min/1.73 m²)

Caution in cases of:

• Renal impairment
• Renal artery stenosis
• Hyperkalemia
• Primary hyperaldosteronism

Pregnancy and breastfeeding: Telmisartan is not recommended in the 1st trimester of pregnancy and is contraindicated in the 2nd and 3rd trimesters. Treatment must not be started during pregnancy. If pregnancy is detected, treatment must be stopped immediately and, if necessary, another therapy started. Telmisartan is not recommended during breastfeeding.

Uncommon (0.1-1%):

• Dizziness
• Urinary tract infections
• Upper respiratory tract infections
• Back pain
• Gastrointestinal complaints
• Hyperkalemia
• Worsening of kidney function

Rare:

• Angioedema
• Liver function disorders

Well tolerated: In studies, telmisartan has shown a tolerability that is barely above placebo level.

Contraindicated:

• Aliskiren in diabetes or renal impairment

Caution with:

• Potassium-sparing diuretics → hyperkalemia
• NSAIDs → reduced effect
• Lithium → increased levels
• Digoxin → increase in levels possible

Metabolism: Telmisartan is not metabolized by CYP enzymes, so there are few interactions via this pathway.