Telmisartan

Last updated on: 29.10.2020

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Synonym(s)

CAS-Nummer:144701-48-4

Definition
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Telmisartan is an orally active and specific angiotensin II receptor antagonist that selectively binds to the AT1 receptor. The effect is based on the displacement of angiotensin II from its binding site at the AT1 receptor. Telmisartan also lowers plasma aldosterone levels. The mean half-life is about 24.0h.

Telmisartan is rapidly absorbed. The mean absolute bioavailability is about 50%.

The drug is excreted after oral administration almost exclusively with the faeces, mainly as an unmodified compound.

Field of application/use
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Telmisartan is offered in tablet form and is available as a mono-preparation and as a combination preparation with amlodipine or hydrochlorothiazide.

Indication
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Treatment of essential hypertension in adults.

Reduction of cardiovascular morbidity in adults with manifest atherothrombotic cardiovascular disease (coronary heart disease, stroke or peripheral arterial occlusive disease in the history) or diabetes mellitus type 2 with documented end organ damage.

Dosage and method of use
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The usual dosage is 40 mg once a day; if the desired blood pressure reduction is not achieved, the dose of telmisartan can be increased to a maximum of 80 mg once a day. Alternatively, telmisartan can be administered in combination with a thiazide diuretic, such as hydrochlorothiazide, for which an additive antihypertensive effect with telmisartan has been proven.

Undesirable effects
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Serious side effects include anaphylactic reactions and angioedema, which occur rarely (≥ 1/10,000 to < 1/1,000), and acute renal failure.

Interactions
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Digoxin: An increase in the concentration of digoxin plasma was observed when used simultaneously.

Drugs which may lead to hyperkalemia: Telmisartan may lead to hyperkalemia. Increased risk is associated with concomitant treatment with the following drugs: potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, NSAIDs including selective COX-2 inhibitors, heparin, immunosuppressive drugs such as cyclosporine or tacrolimus and trimethoprim. The risk is particularly high when potassium-saving diuretics and potassium-containing salt substitutes are administered at the same time.

Lithium: A reversible increase in serum lithium concentration and toxicity has been observed with concomitant use. If concomitant use proves necessary, careful control of serum lithium levels is recommended.

Preparations
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Actelsar®; PUREN®; Kinzalkomb®

Note(s)
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While some Sartans can be displaced from their binding to the AT1 receptor by high concentrations of angiotensin-II, the binding is more permanent by the new substances such as telmisartan and candesartan. Their binding behavior is "insurmountable. Therefore, telmisartan, for example, has a stronger effect than losartan or eprosartan, for example.

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Last updated on: 29.10.2020