Renin inhibitor

Antihypertensively active substances (reserve antihypertensive) that bind to the enzyme renin produced by the kidney and thus prevent the conversion of angiotensinogen into angiotensin I. The levels of angiotensin II and aldosterone decrease.

The Renin-Angiotensin-Aldosterone System (RAAS) regulates the fluid and electrolyte balance in the body and thus influences blood pressure. The RAAS consists of various components, all of which are closely interrelated. The enzyme renin (endopeptidase) produced in the juxatglomerular cells of the kidney cleaves angiotensinogen into angiotensin I, which is subsequently converted into angiotensin II. Angiotensin II causes an increased release of aldosterone. Aldosterone causes a retention of sodium and water in the kidney. Angiotensin II has a blood pressure-increasing effect via vasoconstriction and volume increase within the vessels.

Renin inhibitors selectively block the endopeptidase renin. The conversion of angiotensinogen into angiotensin I is prevented. Thus, the level of angiotensin II and aldosterone decreases. Although the concentration of renin increases when taking renin inhibitors, its activity decreases. This mode of action is the biggest difference between renin inhibitors and ACE inhibitors or AT II blockers. Furthermore, sodium is reduced and retained in the kidney, while potassium is excreted in the urine to a lesser extent. Remarkably, the main representative of the reni inhibitors, aliskiren antiproliferative and antiinflammatory (inhibition of TNF-alpha and interleukin -6: beneficial effect on psoriatic skin changes - Pawloski PL et al. 2018)

Renin inhibitors are used to treat forms of hypertension that are caused by the adrenal gland's increased production of aldosterone. This form of hypertension affects about 50% of all patients with hypertension. Renin inhibitors must be taken regularly to lower blood pressure. It should be noted that the active ingredient is less easily absorbed in high-fat foods.

Diarrhoea, undesirable chronic cough (somewhat less frequent than with ACE inhibitors).

Other potential ADRs of renin inhibitors:

Nausea, vomiting, fatigue, headaches, upper respiratory tract infections, back and joint pain, undifferentiated "rashes".

Angioedema: the risk of developing angioedema is slightly lower than that of ACE inhibitors, but 3 times higher than that of beta-blockers (Toh S et al. 2012)

Al risk viruses (Rasilez®: average daily dose 150-300mg/p.o.)

Renin inhibitors should be avoided in cases of diabetes mellitus, chronic urticaria or angioedema as well as reduced kidney function. The combination of a renin inhibitor with an ACE inhibitor should be avoided

1. Pawloski PL et al (2018) Aliskiren: Preclinical evidence for the treatment of hyperproliferative skindisorders. Biomed Pharmacother 104:151-157.
2. Toh S et al (2012) Comparative risk for angioedema associated with the use of drugs that target the renin-angiotensin-aldosterone system. Arch Internal Med 172:1582-1589.