Telmisartan Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Beschreibung
Telmisartan was launched in the US for the treatment of hypertension.
It can be prepared in eight steps starting with methyl 4-amino-3-methyl
benzoate; the first and second cyclization into a benzimidazole ring occur at
steps 4 and 6 respectively. Telmisartan blocks the action of angiotensin II (Ang
II), the primary effector molecule of the renin-angiotensin-aldosterone system
(RAAS). It is the sixth of this class of 《sartans》 to be marketed after the lead
compound Losartan. Its long lasting effect (24h half-life) could be the main
difference with other angiotensin II antagonists. Unlike several other agents in
this category, its activity does not depend upon transformation into an active
metabolite, the 1-O-acylglucuronide being the principal metabolite found in
humans. Telmisartan is a potent competitive antagonist of AT1 receptors that mediate most of the important effects of angiotensin II while lacking affinity for
the AT2 subtypes or other receptors involved in cardiovascular regulation. In
several clinical studies, Telmisartan, at a once daily dosage, produced effective
and sustained blood-pressure lowering effects with a low incidence of side
effects (particularly treatment-related cough associated with ACE inhibitors in
elderly patients).
Chemische Eigenschaften
White or off white crystalline powder
Verwenden
Telmisartan is an angiotensin II receptor antagonist.
Definition
ChEBI: Telmisartan is a member of the class of benzimidazoles used widely in the treatment of hypertension. It has a role as an antihypertensive agent, an angiotensin receptor antagonist, an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor, a xenobiotic and an environmental contaminant. It is a member of biphenyls, a member of benzimidazoles and a carboxybiphenyl.
Allgemeine Beschreibung
Telmisartan, 4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid (Micardis), does not appear to bear any structuralrelationship to this class, but there is actually a great dealof overlap in the chemical architecture with other agents. Thefirst, and most significant, difference is the replacement of theacidic tetrazole system with a simple carboxylic acid. Thisacid, like the tetrazole, plays a role in receptor binding. Thesecond difference is the lack of a carboxylic acid near the imidazolenitrogen that also contributes to receptor binding.As with irbesartan, however, there is not a need for this groupto be acidic but, rather, to be one that participates in receptorbinding. The second imidazole ring, much like a purine basein deoxyribonucleic acid (DNA), can hydrogen bond with theangiotensin II receptor.
Telmisartan Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
