Telmisartan

Telmisartan
MICARDIS® FDA Package Insert
Indications and Usage
Dosage and Administration
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Labels and Packages
Clinical Trials on Telmisartan
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]

For patient information about Telmisartan, click here.

Synonyms / Brand Names: MICARDIS^®

Overview

Telmisartan (INN) /tɛlmɪˈsɑːrtən/ is an [[AngiotensinII receptor antagonist]] (Angiotensinreceptor blocker, ARB) used in the management of hypertension. It is marketed under the trade name Micardis (by Boehringer Ingelheim), among others.

Category

Category:AngiotensinII receptor antagonists;Benzimidazoles;Benzoic acids;Biphenyls;PPAR agonists;Category:Cardiovascular Drugs

FDA Package Insert

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Mechanism of Action

AngiotensinII is formed from AngiotensinI in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). AngiotensinII is the principal pressor agent of the renin-Angiotensinsystem, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Telmisartan blocks the vasoconstrictor and aldosterone-secreting effects of AngiotensinII by selectively blocking the binding of AngiotensinII to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for AngiotensinII synthesis.

There is also an AT2 receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Telmisartan has much greater affinity (>3,000 fold) for the AT1 receptor than for the AT2 receptor.

Blockade of the renin-Angiotensinsystem with ACE inhibitors, which inhibit the biosynthesis of AngiotensinII from AngiotensinI, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because telmisartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Telmisartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Blockade of the AngiotensinII receptor inhibits the negative regulatory feedback of AngiotensinII on renin secretion, but the resulting increased plasma renin activity and AngiotensinII circulating levels do not overcome the effect of telmisartan on blood pressure.

References

{{AngiotensinII receptor antagonists}}

[[Category:AngiotensinII receptor antagonists]]