Benazepril

BRAND NAMES: 

• Amlobenz: Amlobenz is a combination capsule of Amlodipine and Benazepril that is administered to treat high blood pressure. Amlodipine is effective in treating hypertension at once-daily doses of 2.5mg to 10mg, and benazepril is effective at doses ranging from 10mg to 80mg.

• Lotensin: It is a Benazepril hydrochloride tablet (5, 10, 20 and 40mg) recommended for the treatment of hypertension, which lowers blood pressure.  Lowering blood pressure lowers the risk of both fatal and nonfatal cardiovascular events, particularly strokes and myocardial infarctions.

• Lotrel: It is the combination capsule of Amlodipine and Benazepril hydrochloride. Amlodipine relaxes (widens) arteries in the body, increasing blood flow and benazepril also expanding blood vessels and protects the body from retaining water.

MECHANISM OF ACTION: 

The renin-angiotensin-aldosterone system relies heavily on the angiotensin-converting enzyme. It eventually causes vasoconstriction, increased sympathetic activity, and sodium (Na+) retention, which raises water retention and blood pressure. This process involves the ACE enzyme converting angiotensin I to angiotensin II. As a result, ACE inhibitors disrupt the renin-angiotensin pathway by preventing this phase, resulting in lower systemic arterial blood pressure and greater Na+ excretion in urine.

Due to inadequate cardiac output, patients with heart failure activate the renin-angiotensin-aldosterone pathway, resulting in diminished renal artery perfusion. It stimulates the RAAS pathway, increasing intravascular volume and blood pressure, hence increasing cardiac output.

ACE inhibitors minimize unfavorable cardiac remodeling in people with heart failure. Patients who follow a low-potassium diet, routinely check their blood pressure and renal function, and stick to a rigid schedule of consistent dosing times with benazepril should experience lower blood pressure and less unfavorable cardiac remodeling.

PHARMACOKINETICS: 

Absorption: It takes 0.5 to 1 hour to reach peak plasma concentration to absorb 37% oral benazepril administration. And in some cases, it also takes 1.5 hours to reach peak plasma concentration.

Distribution: The volume of distribution is to be 203±69.9L.

Metabolism: It is metabolized in the liver. Benazepril converts into an active metabolite called benazeprilat.

Ec: It is excreteetiond through urine and also as biliary excretion.

PHARMACODYNAMICS:

Benazepril, an angiotensin-converting enzyme inhibitor, is a prodrug that, when hydrolyzed by esterases, yields the active molecule Benazeprilat. It is used to treat hypertension and heart failure, to minimize proteinuria and renal disease in individuals with nephropathy, and to prevent stroke, myocardial infarction, and cardiac mortality in high-risk patients.

DOSAGE AND ADMINISTRATION: 

It can be consumed with or without meals, once or twice daily. In children, the dose begins at 0.2 mg/kg and should not exceed 0.6 mg/kg Every day. Adults are advised to start with 10 mg once a day and not exceed 40 mg per day.

If a single dose does not produce a reaction, the dosage might be raised depending on the patient's condition. If Benazepril fails to manage the blood pressure, diuretics are used. If you miss a dosage, take it as soon as you recall; if it is time for your next dose, avoid the missing dose and take the dose as directed. 

CONTRAINDICATIONS:

• Should not be used when patients are hypersensitive to Benazepril or any ACE drug.

• Benazepril should not be given to patients under treatment with medicines like valsartan and sacubitril for the last 6 hours.

• Patients treated with Aliskiren for diabetes should not be taking Benzapril.

• It should be avoided for patients suffering from angioedema.

DRUG INTERACTIONS: 

• Benazepril has the potential to increase the hypoglycemia when it is administered with insulin.

• When it is co-administrated with diuretics, it lowers the blood pressure and also sometimes reduces the potassium level in blood serum.

FOOD INTERACTIONS:

Should avoid potassium-included foods as it increases the potassium level and results in hyperkalemia.

ADVERSE EFFECTS:

It may cause serious side effects, as mentioned below.

• Allergic reactions: Sometimes it causes reactions like swelling of the face, rashes, and swollen lymph nodes.

• Neutropenia: It may lower the level of white blood cells and result in the risk of infections, which can easily occur. Infections like sore throat, cough, and fever can easily occur.

• Angioedema: This medication should be avoided if symptoms like swelling of the lips, face, or throat lead to angioedema.

• Hypotension: It may cause low blood pressure. Symptoms included dizziness, confusion, and lightheaded.

• Kidney failure

• Liver damage

• Renal insufficiency

• Hepatic failure

OVERDOSE:

• Dizziness

• Fainting

TOXICITY: 

When compared to other ACE inhibitors, the frequency of neutropenia and proteinuria is negligible; benazepril showed a lower incidence of incorporating systematic hypotension while generating the same number of adverse drug events. It also damages the fetus when given to a pregnant mother.

STORAGE CONDITIONS: 

kept at room temperature storage, 68°F to 77°F (20°C to 25°C).