BioDiaries Blog Lisinopril: a commonly used ACE inhibitor

Lisinopril: a commonly used ACE inhibitor

It is a medicine to treat cardiac conditions like high blood pressure and heart failure. It is usually prescribed as a 20 mg tablet containing anhydrous lisinopril

Uses

It’s uses include treatment of various diseases including hypertension, heart failure, myocardial infarction and to prevent renal complications of diabetes

Hypertension: the most commonly used drug for hypertension is lisinopril

Heart failure: usage of lisinopril along with diuretics or beta blockers

Acute Myocardial Infarction: usage of lisinopril along with other drugs such as thrombolytics, aspirin and beta blockers

Renal complications of Diabetes: usage of lisinopril in order to achieve a diastolic blood pressure below 90 mm Hg

Use in babies: Due to a low efficacy and safety experience in patients above six years, recommendation for children below 6 years is not necessary

Mechanism of action

As a petidyl dipeptidase inhibitor, it inhibits angiotensin converting enzyme (ACE). It is a crucial enzyme catalysing the conversion of angiotensin I to angiotensin II (a peptide involved in vasoconstriction). In addition to its vasoconstriction effect (tightening of blood vessels), it also stimulates the secretion of aldosterone by adrenal cortex. By inhibiting ACE, there is a decreased production of Angiotensisn II. This will reduce the vasoconstriction and also reduce the aldosterone secretion. Overall, these effects relaxes the blood vessels, leading to low blood pressure. This will also ensure increased blood supply to the heart. 

Mode of administration is oral and food doesn’t affect the absorption of this drug. Dosage of the drug depends on the age, weight and pre existing conditions.

Contraindications 

Who should not take this drug? 

  1. Patients with angioedema 
  2. Women in their second and third trimester of pregnancy
  3. Usage along with certain medications like aliskiren containing products and sacubitril
  4. Due to occasional effects of lisinopril like dizziness or tiredness, it affects driving or operation of heavy machinery

The details of the medication given above was taken from the spmc of the drug

Let’s look at the latest research relating to lisinopril

Lisinopril and management of SMI

According to a case report submitted by Kolesova, a silent myocardial infarction is asymptomatic or demonstrates mild symptoms. So, the patients do not seek medical help immediately resulting in complications at a later stage. Lisinopril, along with atrovostatin was crucial for managing the symptoms

Lisinopril and neuroprotective effects

A team led by Ming-Hui Yang tested two ACE inhibitors – lisinopril and benzaperil on neuroblastoma cells in order to study their neuroprotective effects. What they found was interesting. They unregulated (increased) two proteins: lipoprotein-receptor-related protein1B (LRP1B) and 14-3-3-protein zeta/delta. These proteins may contribute to improving cognitive deficits and also help reduce functional decline in Alzheimer’s disease. The increase in calreticulin, the binding partner of APP and LRP1 helps to clear out beta amyloid. Due to the observed effects, its use as a neuroprotectant by promoting the survival of neuronal cells is promising. This could be a promising avenue for the treatment of Alzheimer’s disease. 

Increasing the permeability of lisinopril

Lisinopril has a high water solubility and low permeability (the drug cannot pass through the biological membrane). They have poor bioavailability due to their low permeability and is bile and urine eliminates it as an unchanged drug in the bile and urine. Modhi F Alagili along with his team aimed to solve this problem by formulating it as a sustained release matrix pellet. It is a procedure which mixes the drug with an inert or hydrophobic polymer and compressed into a tablet. It employes a technique called extrusion/spheronization. In conclusion, the LIS-SR pellets were efficient both invitro and exvivo. The above formulation could sustain the release of the drug for upto 8 hours.


Lisinopril and dry cough

Angiotensin Converting Enzyme Inhibitors (like lisinopril) help in the primary and secondary prevention of cardiac mortality and morbidity. They are superior to Angiotensin Receptor Blockers (ARBs). However, a common side effect of ACEI is dry cough. A team led by Yiyun Hu MD ranked the risk of cough induced by different ACEIs and ARBs using meta-analysis. According to the result, ACEIs had a higher incidence of cough than ARBs. Among these, lisinopril ranked the 4th highest  with a surface under the cumulative ranking curve (SUCRA score) of 64.7%. Hence, they came to a conclusion that ACEIs should be avoided in patients who are susceptible to developing cough and an ARB or calcium channel blocker (CCB) would be a better alternative. 

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