Azilsartan

Structural formula
General
Surname	Azilsartan
other names	2-ethoxy-1 - {[2 ′ - (5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl) biphenyl-4-yl] methyl} -1 H -benzimidazol-7- carboxylic acid
Molecular formula	C 25 H 20 N 4 O 5 (azilsartan) ; C 30 H 24 N 4 O 8 (azilsartan medoxomil) ; C 30 H 23 N 4 O 8 K (azilsartan medoxomil potassium) ;
External identifiers / databases
EC number	808-058-6
ECHA InfoCard	100.235.975
PubChem	9825285
Wikidata	Q27074832
Drug information
ATC code	C09 CA09
properties
Molar mass	456.46 g · mol -1 (Azilsartan) ; 568.53 g · mol -1 (Azilsartanmedoxomil) ;
Physical state	firmly
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances	no GHS pictograms
	no GHS pictograms
H and P phrases	H: no H-phrases
	P: no P-phrases
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Azilsartan is a synthetically produced chemical compound from the group of benzimidazoles that acts as an angiotensin II receptor antagonist and is therefore used as a drug for the treatment of essential hypertension in adults.

Clinical information

Type and duration of application

Therapy with azilsartan can be carried out as monotherapy or as combination therapy with other antihypertensive drugs . The recommended starting dose is 40 mg once a day. If this does not adequately control blood pressure, the dose can be increased to a maximum of 80 mg once daily.

Contraindications

As with other sartans, azilsartan is contraindicated in the second and third trimesters of pregnancy; use in the first trimester is not recommended.

Mechanism of action

The compound azilsartan medoxomil used as a progdrug

The active ingredient is used as the potassium salt of its prodrug azilsartan medoxomil (an ester of the carboxylic acid azilsartan, trade name Edarbi ), which is quickly converted into the active form, azilsartan, after oral administration. The mechanism of action corresponds to that of the other AT ₁ antagonists and is described in detail in the article on the active ingredient group of sartans .

Early benefit assessment

An early benefit assessment according to AMNOG is not available for azilsartan. The active ingredient was therefore assigned to a fixed amount group in 2012 .

Individual evidence

↑ ^a ^b Azilsartan data sheet from Sigma-Aldrich , accessed on May 22, 2017 ( PDF ).

↑ ^a ^b pharmische-zeitung.de : Azilsartan, Edarbi® (Takeda Pharma)

↑ ^a ^b ^c Technical information Edarbi.

↑ Federal Joint Committee: Benefit assessment according to Section 35a SGB V - Benefit assessment procedure for the active ingredient Azilsartan Medoxomil , March 15, 2012.

[Sigma-1] Azilsartan data sheet from Sigma-Aldrich , accessed on May 22, 2017 ( PDF ).

[PZ_Neue_ASt-2] rmische-zeitung.de : Azilsartan, Edarbi® (Takeda Pharma)

[Fachinfo-3] Technical information Edarbi.

[4] Federal Joint Committee: Benefit assessment according to Section 35a SGB V - Benefit assessment procedure for the active ingredient Azilsartan Medoxomil , March 15, 2012.