Zofenopril
- IUPAC: (2S, 4S ) -1 - [( 2S) -3 - ( Benzoylsulfanyl ) -2 - methylpropanoyl ]-4- phenylsulfanyl -pyrrolidine- 2-carboxylic acid
- 81872-10-8 ( zofenopril )
- 81938-43-4 ( zofenopril hemicalcium )
C09AA15
Inhibition of angiotensin converting enzyme
Template: Infobox chemical / molecular formula search available
Zofenopril is a drug from the group of ACE inhibitor used to treat high blood pressure. It is used medicinally in the form of its calcium salt. The drug has already been developed in the late 1980s, but currently only allowed in a few countries as a medicine.
Pharmacology
Mechanism of Action
Zofenopril through inhibition of the angiotensin converting enzyme to a reduced formation of angiotensin II from angiotensin I. This reduced formation of angiotensin II causes a decrease in the tonus of the blood vessels, thereby reducing blood pressure. The lower angiotensin II levels also leads to a reduction of aldosterone release from the adrenal cortex and thus to influence the water budget. (see also the renin-angiotensin -aldosterone system )
Areas of application
The drug is used in the treatment of arterial hypertension and for the treatment of acute myocardial infarction. In both indications, doses from 7.5 to 60 mg per day are used in two divided doses, and the dose is slowly titrated to the desired effect.
Side effects
The most common side Wirkunge almost 10 % of patients is a cough which is causally related to the slow degradation and the accumulation of bradykinin in combination. In addition, gastrointestinal complaints, headache and rarely, rashes are dizziness, possible. Hyperkalemia is also possible, but can be through the monitoring of potassium levels in the blood easily notice.
Interactions
Because of the possibility of hyperkalemia should be dispensed with the use of potassium-sparing diuretics. An involvement of the cytochrome system is not yet known.
Contraindications
Contraindications pregnancy and advanced hepatic insufficiency apply. The compatibility during lactation is not documented and therefore also considered to be a contraindication.
Fertigarzneinittel
There are preparations with 7.5 mg, 15 mg, 30 mg and 60 mg, and a combination of 30 mg zofenopril 12.5 mg hydrochlorothiazide available.
Bifril (A), Zofenil (A, CH)
- With hydrochlorothiazide: Bifril plus (A), Zofenil plus (A, CH)
Literature and studies
- Ettore Ambrosioni, Claudio Borghi, Bruno Magnani: The effect of the angiotensin-converting - enzyme inhibitor zofenopril on mortality and morbidity after anterior myocardial infarction. In: The New England Journal of Medicine. Vol 12, No. 2, January 1995, pp. 80-5, PMID 7990904 doi: 10.1056/NEJM199501123320203.
- Claudio Borghi, Ettore Ambrosioni: zofenopril: A Review of the Evidence of its Benefits in Hypertension and Acute Myocardial Infarction. In: Clinical Drug Investigation. Vol 20, No. 5, 2000, ISSN 1173-2563, pp. 371-384.
- Claudio Borghi, Ettore Ambrosioni: Double-blind comparison in between zofenopril and lisinopril in patients with acute myocardial infarction: results of the Survival of Myocardial Infarction Long -term Evaluation -2 ( SMILE -2) study. In: American Heart Journal. Vol 145, No. 1, January 2003, pp. 80-87, PMID 12514658, doi: 10.1067/mhj.2003.24.
- Antonio Marzo, Lorenzo Dal Boa, Paolo Mazzucchellia, Nunzia Ceppi Montia, Rosella Aleotti Tettamantia, Fabrizio Crivellia, Mario Richard clock, Shevquet Ismaili, Andrea Giusti: Pharmacokinetics and pharmacodynamics of zofenopril in healthy volunteers. In: Drug Discovery. Vol 49, No. 2, December 1999, pp. 992-996, PMID 10635443, doi: 10.1055/s-0031-1300539.
- Marcus D. Flather, Salim Yusuf, Lars Kober, Marc Pfeffer, Alistair Hall, Gordon Murray, Christian Torp - Pedersen, Stephen Ball, Janice Pogue, Lemuel Moyé, Eugene Braunwald: Long -term ACE - inhibitor therapy in patients with heart failure or left- ventricular dysfunction: a systematic overview of data from individual patients. In: The Lancet. Vol 355, No. 9215, May 2000, ISSN 0140-6736, pp. 1575-1581, PMID 10821360, doi: 10.1016/S0140-6736 (00) 02212-1.
- A. Flückiger: ACE inhibitors after myocardial infarction. In: pharma - criticism. Vol 17, No 15, 1995, pp. 57-60, digitized (PDF, 33.44 KB).