Lotensin (Benazepril) has a strong hypotensive effect by inhibiting the conversion of angiotensin I to angiotensin II.

It is used in the treatment of the following conditions:

• Hypertension:

  • It is used in the management of hypertension

• Off Label Usage of Benazepril in Adults:

It is used as off label agent in the following conditions :

• Heart failure

• Non–ST-elevation acute coronary syndrome

• Stable coronary artery disease

• ST-elevation acute coronary syndrome

Benazepril Dose in Adults

Lotensin (benazepril) Dose in the treatment of Hypertension:

• The first dosage is 5–10 mg taken orally once daily.
• Depending on the patient's response, it is titrated as necessary, up to 40 mg per day in 1 or 2 divided doses.

Benazepril Dose in Childrens

Lotensin (Benazepril) Dose in the treatment of Hypertension:

• The dosage is adjusted in response to the patient's response.
• Use of the least effective dose

• Children ≥6 years and Adolescents:

  • As monotherapy, the starting dose is 0.2 mg/kg/dose given orally once daily.
  • Initially, a dose of up to 10 mg per day may be used.
  • The maintenance dose is typically administered once day at 0.1–0.6 mg/kg.
  • The daily maximum dose for maintenance is 40 mg.

Lotensin Pregnancy Risk Category: X

[US Boxed Warning]

• Pregnancy is not a good time to use ACE inhibitors.
  • Drugs that affect the renin-angiotensin system frequently harm or kill the foetus.
  • Once you are aware that you are pregnant, stop taking Benazepril as soon as possible. Benazepril crosses the placenta.
  • It can also be associated with oligohydramnios.
  • Oligohydramnios may also cause fetal lung hypoplasia or skeletal malformations.
  • Additionally, it is used to treat conditions such as hypotension, anuria, renal failure, hypoplasia of the skull, and foetal or neonatal mortality while pregnant.
  • After the first trimester of maternal treatment with an ACE inhibitor, teratogenic effects can occur.
  • Infants are typically administered an ACE inhibitor in utero. They are frequently checked for oliguria, hypotension, and hyperkalemia.
  • After an irreversible, fatal injury has occurred, Oligohydramnios may not be present.
  • To correct hypotension and enhance renal function, dialysis or exchange transfusions may be needed.
  • Adverse outcomes for the mother and foetus can also result from chronic maternal hypertension.
  • Uncomplicated hypertension during pregnancy can be treated with ACE inhibitors
  • Some experts consider them to be contraindicated during pregnancy for treatment of hypertension or chronic heart failure.
  • Women of reproductive age should also avoid ACE inhibitors.

Benazepril use during breastfeeding:

• Breast milk usually contains benazepril or benazeprilat.
• Experts consider benazepril safe for breastfeeding women.
• It is recommended to monitor the weight of the breastfeeding child for the first four weeks.

Benazepril Dose in Renal Disease:

• CrCl ≥30 mL/minute/1.73m² :

  • No dosage adjustment required.

• CrCl <30 mL/minute/1.73m² :

  • Initially 5 mg once daily to a maximum dose of 40 mg/day

• Hemodialysis:

  • 25% to 50% of the usual dose is given
  • Supplemental dosage is not required

• Peritoneal dialysis:

  • 25% to 50% of the usual dose is given
  • The supplemental dose is not required.

Benazepril Dose in Liver Disease:

No dose adjustments have been given by manufacturer in patient with liver disease.

Common Side Effects of Benazepril (Lotensin) Include:

• Cardiovascular:

  • Hypotension

• Central nervous system:

  • Headache
  • Dizziness
  • Drowsiness
  • Orthostatic
  • Dizziness

Contraindication to Benazepril include:

• Hypersensitivity to benazepril 
• ACE inhibitors or any component of the formulation
• Angioedema history 
• Patients with diabetes mellitus should not use aliskiren.
• You should not take neprilysin inhibitor with you or within the first 36 hours.
• Patients with severe or moderate renal dysfunction may also use aliskiren.
• pregnancy
• Breastfeeding
• Rare hereditary galactose intolerance diseases (eg, Galactosemia or Lapp Lactase deficiencies) can occur.

Warnings and precautions

• Angioedema
  • It can happen at any stage of treatment, especially after the first dose.
  • It might impact the colon, head and neck, which would seriously compromise the airway (presenting as abdominal pain).
  • African Americans and those with hereditary or idiopathic angioedema are more susceptible.
  • When used with an ACE inhibitor, mTOR inhibitor therapy (such as everolimus) or a neprilysin inhibitor (such as sacubitril) can increase risk.
  • It is important to monitor your airway regularly, especially if you have a problem with the tongue, glottis or larynx.
  • Patients who have had previous airway surgery may be at greater risk for obstruction.
  • It is crucial to intervene quickly and manage the situation appropriately.
  • Patients with angioedema that has been treated with or without ACE inhibitor therapy are not advised to use this medication.
• Cholestatic jaundice
  • Cholestatic jaundice is a rare side effect of ACE inhibitors
  • It can lead to fulminant liver necrosis.
  • If there is a marked increase in hepatic transaminases and jaundice, it can be stopped.
• Cough:
  • The cough caused by an ACE inhibitor is dry, hacking, and ineffective.
  • The first few months following therapy are when it occurs most frequently. After the ACE inhibitor has been discontinued, it should normally go away in one to four weeks.
  • Before stopping, it's crucial to look into alternative cough causes (eg, pulmonary congestion in heart failure patients).
• Hematologic effects
  • It has been connected to anaemia, agranulocytosis, neutropenia, and myeloid hypoplasia.
  • Patients who have kidney disease run the chance of getting neutropenia.
  • Neutropenia is more likely to occur in patients who have both collagen-vascular disease, such as systemic lupus, and renal impairment.
  • Regularly check CBC for differences in these individuals.
• Hyperkalemia:
  • ACE inhibitors can cause this side effect.
  • Kidney dysfunction, concurrent use of potassium-sparing diuretics, and diabetes mellitus are all risk factors.
  • When utilising these substances, use caution. Regularly check your potassium levels as well.
• Hypersensitivity reactions
  • ACE inhibitors can cause anaphylactic/anaphylactoid responses as well.
  • Hemodialysis (CVVHD, for example), high-flux dialysis membranes (AN69), and, in rare cases, low-density lipoprotein apheresis utilising dextran sulfatecellulose, can all cause severe anaphylactoid reactions.
  • Patients who have had sensitization therapy with ACE inhibitors and venom from Hymenoptera (bee or wasp) may have anaphylactic responses.
• Hypotension/ Syncope
  • ACE inhibitors may occasionally result in syncope along with hypotension symptoms. Typically, the first few dosages are plenty.
  • These effects are most common in patients with low volume.
  • Before initiation, volume correction should be performed
  • Careful monitoring is necessary for initial dosing, and subsequent dosing increases.
  • The patient's clinical condition dictates that blood pressure should be lowered.
  • Even though it could be required to lower doses, hypotension is not a reason to stop using ACE inhibitors in the future.
  • This is especially true for heart disease patients, for whom a reduction in systolic pressure is essential.
• Renal function deterioration:
  • Particularly in patients with limited renal flow (such as those with kidney artery stenosis or heart failure) and GFR that depends on efferent arterial vasoconstriction via angiotensin 2, it might result in a loss in renal function and/or an increase in serum creatinine and/or BUN.
  • Oliguria, severe kidney failure, or progressive azotemia can all result from a disordered condition.
  • Small increases in serum creatinine may happen after starting.
  • Patients whose renal function has significantly and steadily declined should be treated.
• Aortic stenosis
  • Patients with severe aortic blockage should be cautious
  • It could lead to decreased coronary perfusion, which can cause ischemia.
• Ascites:
  • Patients with ascites from cirrhosis and refractory ascites should avoid it
  • To avoid renal failure, monitor blood pressure and kidney function closely.
• Cardiovascular disease
  • Patients with ischemic heart disease and cerebrovascular diseases should be closely monitored as falling blood pressure can have serious consequences (e.g, MI, stroke).
  • Blood pressure can be raised if needed by replacing lost fluids. Then, therapy might be resumed.
  • Stop treating hypotension-recurring patients.
• Collagen vascular disease:
  • Patients with collagen vascular disease should exercise caution, especially if they also have concurrent renal impairment.
  • They are more at risk of hematologic toxicities.
• Diabetes:
  • Patients with diabetes who are taking insulin or oral anti-inflammatory agents should be cautious
  • They could be at greater risk of developing hypoglycemia episodes.
• Hypertrophic cardiomyopathy with outflow tract obstruction (HCM)
  • Patients with HCM or outflow tract obstruction can experience worsening symptoms.
• Renal artery stenosis
  • Patients who have unilateral or bilateral renal artery stenosis that is untreated should exercise caution.
  • Unstented bilateral renal arterial stenosis should be avoided.
• Renal impairment
  • Preventive measures should be taken if you have a pre-existing condition such as renal insufficiency.
  • It is possible to adjust the dosage.
  • Do not increase your dose too quickly as this can cause further renal impairment.

Benazepril: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitor:

• Blood pressure
• BUN
• Serum creatinine and potassium
• CBC

How to take Benazepril (Lotensin)?

• It can be taken orally and with or without food.

Mechanism of action of Benazepril (Lotensin):

• It prevents angiotensin 1 from angiotensin 2 conversion.
• Angiotensin II, a powerful vasoconstrictor, is also available.
• It can be taken orally and with or without food.

Reduction in plasma angiotensin-converting enzyme (ACE) activity:

The onset of action:

• Peak impact is visible 1–2 hours after a dose of 2–20 mg.

Duration of action:

• greater than 90% inhibition for 24 hours following a dosage of 5 to 20 mg

Reduction in blood pressure:

Peak effect:

• After a single-dose is 2 to 4 hours
• Continuous therapy takes 2 weeks

Absorption:

• It is rapidly absorbed (37%)
• Food doesn't change significantly.
• Due to its low absorption, the metabolite (benazeprilat) is not suited for oral administration.

Protein binding: Benazepril: ~97% Benazeprilat: ~95%

Metabolism:

• By enzymatic hydrolysis, it is rapidly and widely hepatic to its active metabolite, benazeprilat.
• It has a significant first-pass impact.

Half-life elimination:

• The terminal effect in  children is in 5 hours while in adults, it is 22 hours

Time to peak:

• Parent drug: 0.5 to 1 hour
• Active metabolite (benazeprilat):
• Fasting: 1- 2 hours;
• Nonfasting: 2 - 4 hours

Excretion:

• Benazepril, benazeprilat, and other metabolites make up 12% of its urine excretion.

Clearance:

• Benazeprilat is eliminated (11%–12%) primarily in patients with severe renal impairment thanks to nonrenal clearance (i.e. biliary, metabolic).
• The main method through which unaltered benazepril is eliminated is by hepatic clearance.
• Dialysis:
  • After taking 10 mg of benazepril two hours before to the surgery, about 6% of the metabolite was eliminated within four hours of the treatment.
• The dialysate doesn't contain the parent chemical.

Benazepril International Brands:

• Benace
• Boncordin
• Cibacen
• Lotensin
• Sotrel
• Unitense
• Xbenzi
• Zaprace
• PMS-Benazepril

Benazepril Brands in Pakistan:

Benazepril is not available in Pakistan