RENIN INHIBITORS | ALISKIREN | REMIKIREN | ENALKIREN | USES | MECHANISM OF ACTION | SIFE EFFECTS
Channel: PHARMAROCKS THE WAY OF SUCCESS
Date: 22/11/2020

RENIN INHIBITORS BASIC USE OF MEDICINES

RENIN INHIBITORS OR DIRECTRENIN INHIBITORS 
Renin inhibitors are pharmaceutical drugs inhibiting the activity of renin that is responsible for hydrolyzing angiotensinogen to angiotensin I, which in turn reducing the formation of angiotensin II that increase blood pressure

#RENININHIBITORS #ALISKIREN #RAMIKIREN #ENALKIREN

From where renin is secreted? 
The main source of renin is the juxtaglomerular cells (JGCs), which release renin from storage granules. 
It release due to stimulation by  β1 receptor activation or due to decreased fluid delivery to macula densa of kidney
There for beta receptor blockers also use to treat high blood pressure cause by RAAS system

RAAS FUNCTION IN OUR BODY
The renin-angiotensin-aldosterone system (RAAS) is one of the most important hormonal mechanisms in controlling hemodynamic stability by regulating blood pressure, fluid volume, and sodium-potassium balance.
The RAAS functions to elevate blood volume and arterial tone in a prolonged manner. 
It does this by increasing sodium reabsorption, water reabsorption, and vascular tone.

RENIN INHIBITORS EXAMPLES
Following are the drugs that inhibit the enzyme renin taken orally by patient
Aliskiren,
Remikiren,
Enalkiren,
So these drugs will decrease the activity of RAAS causing fall in blood pressure. 
These drugs can be used orally for the treatment of chronic hypertension

RENIN INHIBITORS MECHANISM
Renin inhibitors produce vasodilation by inhibiting the activity of renin, which is responsible for stimulating angiotensin II formation.
Direct renin inhibitors block the enzyme renin from triggering a process that helps regulate blood pressure. 
As a result, blood vessels relax and widen, making it easier for blood to flow through the vessels, which lowers blood pressure.

RENIN INHIBITORS USES
Renin inhibitors are used to treat hypertension
In medical terms problem of high blood pressure is called hypertension

RENIN INHIBITORS CONTRAINDICATIONS
Pregnancy
Teratogenic in second half of pregnancy
It have been associated with fetal malformations and neonatal death.
Breastfeeding 
Previous angioedema associated with renin inhibitor therapy.
Hypersensitivity to renin inhibitors.

RENIN INHIBITORS SIDE EFFECTS
The most commonly reported adverse effects were 
Fatigue
Headache
Dizziness
Diarrhoea 
Nausea 
In contrast, the higher dose of 600 mg per day was associated with an increased incidence of diarrhoea
Angioedema
High blood potassium level (particularly when used with ACE inhibitors in diabetic patients)
Low blood pressure (particularly in volume-depleted patients)
Diarrhea and other GI symptoms
Headache
Dizziness
Cough

STUDY ON RENIN INHIBITORS
In December 2011, Novartis halted a trial of the drug after discovering increased 
nonfatal stroke
kidney complications
high blood potassium, and 
low blood pressure in people with diabetes and kidney problems.

As a result, in 2012:
A new contraindication was added to the product label concerning the use of aliskiren with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes because of the risk of 
kidney impairment
low blood pressure, and 
high levels of potassium in the blood

A warning to avoid use of aliskiren with ARBs or ACEIs was also added for patients with moderate to severe kidney impairment (i.e., where glomerular filtration rate is less than 60 ml/min)
Novartis decided to stop marketing Valturna ((aliskiren/valsartan))
Aliskiren was co-developed by the 
Swiss pharmaceutical companies Novartis and Speede

ALISKIREN WARNINGS
the risks of kidney (renal) impairment
low blood pressure (hypotension)
high potassium blood levels (hyperkalemia)
DON’T MAKE COMBINATION WITH ARBS OR ACEIS 
ANGIOTENSIN RECEPTOR BLOCKERS (ARBs)
Losartan, valsartan, Irbesartan, candesartan, telmisartan and eprosartan
ACEIs Captopril, enalapril, lisinopril, ramipril, perindopril, trandolapril, fosinopril moexipril etc


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