Benazepril

Name: Benazepril

What brand names are available for benazepril?

Lotensin HTC

Which drugs or supplements interact with benazepril?

  • Combining benazepril with potassium supplements, potassium containing salt substitutes, and potassium conserving diuretics such as amiloride (Moduretic), spironolactone (Aldactone), and triamterene (Dyazide, Maxzide), can lead to dangerously high blood levels of potassium.
  • Combining benazepril or other ACE inhibitors with nonsteroidal anti-inflammatory drugs (NSAIDs) in patients who are elderly, fluid-depleted (including those on diuretic therapy), or with poor kidney function may result in reduced kidney function, including kidney failure. These effects usually are reversible.
  • There have been reports that aspirin and other NSAIDs such as ibuprofen (Advil, Children's Advil/Motrin, Medipren, Motrin, Nuprin, PediaCare Fever, and many others), indomethacin (Indocin, Indocin-SR), and naproxen (Anaprox, Naprelan, Naprosyn, Aleve) may reduce the effects of ACE inhibitors. When taken with lithium (Eskalith, Lithobid), benazepril can increase lithium to toxic levels in the blood.
  • Nitritoid reactions (symptoms include facial flushing, nausea, vomiting and hypotension) may occur when injectable gold (sodium aurothiomalate), used in the treatment of rheumatoid arthritis, is combined with ACE inhibitors, including benazepril.

Clinical pharmacology

Mechanism Of Action

Benazepril and benazeprilat inhibit angiotensin-converting enzyme (ACE) in human subjects and animals. Benazeprilat has much greater ACE inhibitory activity than does benazepril.

ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex.

Inhibition of ACE results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion. The latter decrease may result in a small increase of serum potassium.

Removal of angiotensin II negative feedback on renin secretion leads to increased plasma renin activity. In animal studies, benazepril had no inhibitory effect on the vasopressor response to angiotensin II and did not interfere with the hemodynamic effects of the autonomic neurotransmitters acetylcholine, epinephrine, and norepinephrine.

ACE is identical to kininase, an enzyme that degrades bradykinin. Whether increased levels of bradykinin, a potent vasodepressor peptide, play a role in the therapeutic effects of Lotensin remains to be elucidated. While the mechanism through which benazepril lowers blood pressure is believed to be primarily suppression of the renin-angiotensin-aldosterone system, benazepril has an antihypertensive effect even in patients with low-renin hypertension.

Pharmacodynamics

Single and multiple doses of 10 mg or more of Lotensin cause inhibition of plasma ACE activity by at least 80%-90% for at least 24 hours after dosing. Pressor responses to exogenous angiotensin I were inhibited by 60%-90% (up to 4 hours post-dose) at the 10-mg dose.

Drug Interactions

Lotensin has been used concomitantly with beta-adrenergic-blocking agents, calcium- channel-blocking agents, diuretics, digoxin, and hydralazine, without evidence of clinically important adverse interactions. Benazepril, like other ACE inhibitors, has had less than additive effects with betaadrenergic blockers, presumably because both drugs lower blood pressure by inhibiting parts of the renin-angiotensin system

Pharmacokinetics

The pharmacokinetics of benazepril are approximately dose-proportional within the dosage range of 10-80 mg.

Following oral administration of Lotensin, peak plasma concentrations of benazepril, and its active metabolite benazeprilat are reached within 0.5-1.0 hours and 1-2 hours, respectively. While the bioavailability of benazepril is not affected by food, time to peak plasma concentrations of benazeprilat is delayed to 2 – 4 hours.

The serum protein binding of benazepril is about 96.7% and that of benazeprilat about 95.3%, as measured by equilibrium dialysis; on the basis of in vitro studies, the degree of protein binding should be unaffected by age, hepatic dysfunction, or concentration (over the concentration range of 0.24- 23.6 µmol/L).

Benazepril is almost completely metabolized to benazeprilat by cleavage of the ester group (primarily in liver). Both benazepril and benazeprilat undergo glucuronidation.

Benazepril and benazeprilat are cleared predominantly by renal excretion. About 37% of an orally administered dose was recovered in urine as benazeprilat (20%), benazeprilat glucuronide (8%), benazepril glucuronide (4%) and as trace amounts of benazepril. Nonrenal (i.e., biliary) excretion accounts for approximately 11%-12% of benazeprilat excretion. The effective half-life of benazeprilat following once daily repeat oral administration of benazepril hydrochloride is 10-11 hours. Thus, steady-state concentrations of benazeprilat should be reached after 2 or 3 doses of benazepril hydrochloride given once daily.

Accumulation ratio based on AUC of benazeprilat was 1.19 following once daily administration.

Specific Populations

Renal Impairment

The pharmacokinetics of systemic exposure to benazepril and benazeprilat in patients with mild-tomoderate renal insufficiency (creatinine clearance >30 mL/min) is similar to that in patients with normal renal function. In patients with creatinine clearance ≤30 mL/min, peak benazeprilat levels and the initial (alpha phase) half-life increase, and time to steady state may be delayed (see DOSAGE AND ADMINISTRATION.

When dialysis was started 2 hours after ingestion of 10 mg of benazepril, approximately 6% of benazeprilat was removed in 4 hours of dialysis. The parent compound, benazepril, was not detected in the dialysate.

Hepatic Impairment

In patients with hepatic insufficiency (due to cirrhosis), the pharmacokinetics of benazeprilat are essentially unaltered.

Drug Interactions

The pharmacokinetics of benazepril are not affected by the following drugs: hydrochlorothiazide, furosemide, chlorthalidone, digoxin, propranolol, atenolol, nifedipine, amlodipine, naproxen, acetylsalicylic acid, or cimetidine. Likewise the administration of benazepril does not substantially affect the pharmacokinetics of these medications (cimetidine kinetics were not studied)

Pediatrics

The pharmacokinetics of benazaprilat, evaluated in pediatric patients with hypertension following oral administration of a single dose is presented in table below.

Age group Cmax
(ng/mL)
Tmax*
(h)
AUC0-inf (ng/mL*h) CL/F/wt
(L/h/Kg)
T1/2 (h)
>1 to ≤ 24 months n=5 277
(192, 391)
1
(0.6, 2)
1328
(773, 2117)
0.26
(0.18, 0.4)
5.0
(4, 5.8)
>2 to ≤ 6 years n=7 200
(168, 244)
2
(1.4, 2.4)
978
(842, 1152)
0.36
(0.31, 0.42)
5.5
(4.7, 6.5)
>6 to ≤ 12 years n=7 221
(194, 258)
2
(1.2, 2.2)
1041
(855, 1313)
0.25
(0.21, 0.31)
5.5
(4.7, 6.5)
>12 to ≤ 17 years n=8 287
(217, 420)
2
(1.3, 2.3)
1794
(1478, 2340)
0.16
(0.13, 0.21)
5.1
(4.2, 5.7)

Clinical Studies

Hypertension

Adult Patients

In single-dose studies, Lotensin lowered blood pressure within 1 hour, with peak reductions achieved between 2 and 4 hours after dosing. The antihypertensive effect of a single dose persisted for 24 hours. In multiple-dose studies, once-daily doses of between 20 mg and 80 mg decreased seated pressure 24 hours after dosing by about 6 to 12mmHg systolic and 4 to 7 mmHg diastolic. The trough values represent reductions of about 50% of that seen at peak.

Four dose-response studies using once-daily dosing were conducted in 470 mild-to-moderate hypertensive patients not using diuretics. The minimal effective once-daily dose of Lotensin was 10 mg; but further falls in blood pressure, especially at morning trough, were seen with higher doses in the studied dosing range (10-80 mg). In studies comparing the same daily dose of Lotensin given as a single morning dose or as a twice-daily dose, blood pressure reductions at the time of morning trough blood levels were greater with the divided regimen.

The antihypertensive effects of Lotensin were not appreciably different in patients receiving high- or low-sodium diets.

In normal human volunteers, single doses of benazepril caused an increase in renal blood flow but had no effect on glomerular filtration rate.

Use of Lotensin in combination with thiazide diuretics gives a blood-pressure-lowering effect greater than that seen with either agent alone. By blocking the renin-angiotensin-aldosterone axis, administration of Lotensin tends to reduce the potassium loss associated with the diuretic.

Pediatric Patients

In a clinical study of 107 pediatric patients, 7 to 16 years of age, with either systolic or diastolic pressure above the 95th percentile, patients were given 0.1 or 0.2 mg/kg then titrated up to 0.3 or 0.6 mg/kg with a maximum dose of 40 mg once daily. After four weeks of treatment, the 85 patients whose blood pressure was reduced on therapy were then randomized to either placebo or benazepril and were followed up for an additional two weeks. At the end of two weeks, blood pressure (both systolic and diastolic) in children withdrawn to placebo rose by 4 to 6 mmHg more than in children on benazepril. No dose-response was observed.

Benazepril Precautions

Do not take benazepril if you are allergic to any of the ingredients. Each manufacturer may use different inactive ingredients. Ask your doctor or pharmacist for a complete list. Tell your doctor if you are allergic to any other ACE inhibitors.

Do not take benazepril if you have ever had angioedema, with or without prior ACE inhibitor treatment.

Benazepril, if taken while pregnant, can harm or cause death to the unborn baby. Tell your doctor right away if you become pregnant while taking this medication.

ACE inhibitors, including benazepril, have caused liver failure. While this is rare, be sure to tell your doctor right away if you show symptoms of liver damage including nausea, lack of appetite, tiredness, diarrhea, yellowing of skin or eyes (jaundice), stomach pain, flu-like symptoms, and bleeding easily.

Benazepril may cause extreme low blood pressure. The symptoms are lightheadedness, dizziness, and fainting. Until you know how benazepril affects you, do not drive or operate heavy machinery. Extreme low blood pressure is more likely to happen if you:

  • are taking a diuretic
  • are on dialysis
  • have diarrhea
  • are vomiting
  • are not drinking enough liquids
  • are sweating a lot

 

What is benazepril?

Benazepril is an ACE inhibitor. ACE stands for angiotensin converting enzyme.

Benazepril is used to treat high blood pressure (hypertension).

Benazepril may also be used for purposes not listed in this medication guide.

What should I avoid while taking benazepril?

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Avoid becoming overheated or dehydrated during exercise, in hot weather, or by not drinking enough fluids. Benazepril can decrease sweating and you may be more prone to heat stroke.

Drinking alcohol can further lower your blood pressure and may increase certain side effects of benazepril.

Do not use salt substitutes or potassium supplements while taking benazepril, unless your doctor has told you to.

What other drugs will affect benazepril?

Other drugs may interact with benazepril, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Proper Use of benazepril

In addition to the use of benazepril, treatment for your high blood pressure may include weight control and changes in the types of foods you eat, especially foods high in sodium (salt). Your doctor will tell you which of these are most important for you. You should check with your doctor before changing your diet.

Many patients who have high blood pressure will not notice any signs of the problem. In fact, many may feel normal. It is very important that you take your medicine exactly as directed and that you keep your appointments with your doctor even if you feel well.

Remember that benazepril will not cure your high blood pressure but it does help control it. Therefore, you must continue to take it as directed if you expect to lower your blood pressure and keep it down. You may have to take high blood pressure medicine for the rest of your life. If high blood pressure is not treated, it can cause serious problems such as heart failure, blood vessel disease, stroke, or kidney disease.

If your child cannot swallow the tablets, an oral liquid may be given. Ask your doctor or pharmacist about this.

Dosing

The dose of benazepril will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of benazepril. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For high blood pressure:
      • Adults—At first, 10 milligrams (mg) once a day. Your doctor may increase your dose up to 20 to 40 mg per day, taken as a single dose or divided into two doses.
      • Children 6 years of age and older—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.2 milligram (mg) per kilogram (kg) of body weight per day. Your doctor may adjust the dose as needed. However, the dose is usually not more than 0.6 mg per kg of body weight or 40 mg per day.
      • Children younger than 6 years of age—Use is not recommended.

Missed Dose

If you miss a dose of benazepril, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep the mixed oral liquid in the refrigerator and store it for up to 30 days. Do not freeze.

benazepril Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common
  • Chills
  • cold sweats
  • confusion
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • unusual tiredness or weakness
Incidence not known
  • Arm, back, or jaw pain
  • blistering, peeling, or loosening of the skin
  • bloating or swelling of the face, arms, hands, lower legs, or feet
  • chest pain or discomfort
  • diarrhea
  • fast, irregular, pounding, or racing heartbeat or pulse
  • feeling of warmth
  • fever
  • general feeling of tiredness or weakness
  • itching
  • joint or muscle pain
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • nausea
  • rapid breathing
  • rapid weight gain
  • red skin lesions, often with a purple center
  • red, irritated eyes
  • redness of the face, neck, arms, and occasionally, upper chest
  • shortness of breath
  • skin rash
  • sore throat
  • sores, ulcers, or white spots in the mouth or on the lips
  • sweating
  • tingling of the hands or feet
  • unusual weight gain or loss
  • wheezing

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Headache
Less common
  • Cough
  • dizziness
  • sleepiness or unusual drowsiness

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Indications and Usage for Benazepril

Benazepril hydrochloride tablets are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including the class to which this drug principally belongs.

Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC).

Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly.

Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mm Hg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal.

Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in Black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy.

It may be used alone or in combination with thiazide diuretics.

Benazepril Dosage and Administration

Recommended Dosage

ADULTS

The recommended initial dose for patients not receiving a diuretic is 10 mg once a day. The usual maintenance dosage range is 20 mg to 40 mg per day administered as a single dose or in two equally divided doses. A dose of 80 mg gives an increased response, but experience with this dose is limited. The divided regimen was more effective in controlling trough (pre-dosing) blood pressure than the same dose given as a once-daily regimen.

Use with diuretics in adults

The recommended starting dose of Benazepril hydrochloride tablets in a patient on a diuretic is 5 mg once daily. If blood pressure is not controlled with Benazepril hydrochloride tablets alone, a low dose of diuretic may be added.

PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER

The recommended starting dose for pediatric patients is 0.2 mg/kg once per day. Titrate as needed to 0.6 mg/kg once per day. Doses above 0.6 mg/kg (or in excess of 40 mg daily) have not been studied in pediatric patients.

Benazepril hydrochloride tablets are not recommended in pediatric patients less than 6 years of age or in pediatric patients with GFR less than 30 mL/min/1.73m2 [see Use in Specific Populations (8.3)].

. Dose Adjustment for Renal Impairment

For adults with a GFR < 30 mL/min/1.73 m2 (serum creatinine > 3 mg/dL), the recommended initial dose is 5 mg Benazepril hydrochloride tablets once daily. Dosage may be titrated upward until blood pressure is controlled or to a maximum total daily dose of 40 mg. Benazepril hydrochloride tablets can also worsen renal function [see Warnings and Precautions (5.3)].

. Preparation of Suspension (for 150 mL of a 2 mg/mL Suspension)

Add 75 mL of Ora-Plus®* oral suspending vehicle to an amber polyethylene terephthalate (PET) bottle containing fifteen Benazepril hydrochloride 20 mg tablets, and shake for at least two minutes. Allow the suspension to stand for a minimum of 1 hour. After the standing time, shake the suspension for a minimum of one additional minute. Add 75 mL of Ora-Sweet®* oral syrup vehicle to the bottle and shake the suspension to disperse the ingredients. The suspension should be refrigerated at 2° to 8°C (36° to 46°F) and can be stored for up to 30 days in the PET bottle with a child-resistant screw-cap closure. Shake the suspension before each use.

*Ora-Plus® and Ora-Sweet® are registered trademarks of Paddock Laboratories, Inc. Ora Plus® contains carrageenan, citric acid, methylparaben, microcrystalline cellulose, carboxymethylcellulose sodium, potassium sorbate, simethicone, sodium phosphate monobasic, xanthan gum, and water. Ora-Sweet® contains citric acid, berry citrus flavorant, glycerin, methylparaben, potassium sorbate, sodium phosphate monobasic, sorbitol, sucrose, and water.

Dosage Forms and Strengths

Tablets: 5 mg, 10 mg, 20 mg, and 40 mg

• Each 5 mg tablet is light yellow, arc triangle coated, debossed with the number “93” on one side and “5124” on the other • Each 10 mg tablet is mustard yellow, arc triangle coated, debossed with the number “93” on one side and “5125” on the other • Each 20 mg tablet is pink, arc triangle coated, debossed with the number “93” on one side and “5126” on the other • Each 40 mg tablet is pink to light red, arc triangle coated, debossed with the number “93” on one side and “5127” on the other

Clinical Studies

Hypertension

Adult Patients

In single-dose studies, Benazepril hydrochloride lowered blood pressure within 1 hour, with peak reductions achieved between 2 and 4 hours after dosing. The antihypertensive effect of a single dose persisted for 24 hours. In multiple-dose studies, once-daily doses of between 20 mg and 80 mg decreased seated pressure 24 hours after dosing by about 6 to 12 mm Hg systolic and 4 to 7 mm Hg diastolic. The trough values represent reductions of about 50% of that seen at peak.

Four dose-response studies using once-daily dosing were conducted in 470 mild-to-moderate hypertensive patients not using diuretics. The minimal effective once-daily dose of Benazepril hydrochloride was 10 mg; but further falls in blood pressure, especially at morning trough, were seen with higher doses in the studied dosing range (10 to 80 mg). In studies comparing the same daily dose of Benazepril hydrochloride given as a single morning dose or as a twice-daily dose, blood pressure reductions at the time of morning trough blood levels were greater with the divided regimen.

The antihypertensive effects of Benazepril hydrochloride were not appreciably different in patients receiving high- or low-sodium diets.

In normal human volunteers, single doses of Benazepril caused an increase in renal blood flow but had no effect on glomerular filtration rate.

Use of Benazepril hydrochloride in combination with thiazide diuretics gives a blood-pressure-lowering effect greater than that seen with either agent alone. By blocking the renin-angiotensin-aldosterone axis, administration of Benazepril hydrochloride tends to reduce the potassium loss associated with the diuretic.

Pediatric Patients

In a clinical study of 107 pediatric patients, 7 to 16 years of age, with either systolic or diastolic pressure above the 95th percentile, patients were given 0.1 or 0.2 mg/kg then titrated up to 0.3 or 0.6 mg/kg with a maximum dose of 40 mg once daily. After four weeks of treatment, the 85 patients whose blood pressure was reduced on therapy were then randomized to either placebo or Benazepril and were followed up for an additional two weeks. At the end of two weeks, blood pressure (both systolic and diastolic) in children withdrawn to placebo rose by 4 to 6 mm Hg more than in children on Benazepril. No dose-response was observed.

Index Terms

  • Benazepril HCl
  • Benazepril Hydrochloride

Brand Names U.S.

  • Lotensin

Duration of Action

Reduction in plasma angiotensin-converting enzyme (ACE) activity: >90% inhibition for 24 hours after 5 to 20 mg dose (Balfour 1991)

Half-Life Elimination

Benazeprilat: Effective: 10 to 11 hours; Terminal: Children: 5 hours, Adults: 22 hours

Protein Binding

Benazepril: ~97%

Benazeprilat: ~95%

Dosing Pediatric

Hypertension: Children ≥6 years and Adolescents: Oral: Initial: 0.2 mg/kg once daily (maximum initial dose: 10 mg/day) as monotherapy; maintenance: 0.1 to 0.6 mg/kg once daily (maximum dose: 0.6 mg/kg/day or 40 mg/day).

Monitoring Parameters

Blood pressure; BUN, serum creatinine and potassium; if patient has collagen vascular disease and/or renal impairment, periodically monitor CBC with differential.

Where can i get more information?

Your pharmacist can provide more information about benazepril.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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Side effects

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.

Lotensin has been evaluated for safety in over 6000 patients with hypertension; over 700 of these patients were treated for at least one year. The overall incidence of reported adverse events was similar in Lotensin and placebo patients.

The reported side effects were generally mild and transient, and there was no relation between side effects and age, duration of therapy, or total dosage within the range of 2 to 80 mg.

Discontinuation of therapy because of a side effect was required in approximately 5% of U.S. patients treated with Lotensin and in 3% of patients treated with placebo. The most common reasons for discontinuation were headache (0.6%) and cough (0.5%).

Adverse reactions seen in at least 1% greater frequency in patients treated with Lotensin than placebo were headache (6% vs 4%), dizziness (4% vs 2%), somnolence (2% vs 0%) and postural dizziness (2% vs 0%).

Adverse reactions reported in controlled clinical trials (less than 1% more on benazepril than on were headache (6% vs 4%), dizziness (4% vs 2%), somnolence (2% vs 0%) and postural dizziness (2% vs 0%).

Adverse reactions reported in controlled clinical trials (less than 1% more on benazepril than on placebo), and rarer events seen in post-marketing experience, include the following (in some, a causal relationship to drug use is uncertain):

Dermatologic: Stevens-Johnson syndrome, pemphigus, apparent hypersensitivity reactions (manifested by dermatitis, pruritus, or rash), photosensitivity, and flushing.

Gastrointestinal: Nausea, pancreatitis, constipation, gastritis, vomiting, and melena.

Hematologic: Thrombocytopenia and hemolytic anemia.

Neurologic/Psychiatric: Anxiety, decreased libido, hypertonia, insomnia, nervousness, and paresthesia

Other: Fatigue, asthma, bronchitis, dyspnea, sinusitis, urinary tract infection, frequent urination, infection, arthritis, impotence, alopecia, arthralgia, myalgia, asthenia, sweating.

Laboratory Abnormalities

Elevations of uric acid, blood glucose, serum bilirubin, and liver enzymes [see WARNINGS AND PRECAUTIONS] have been reported, as have incidents of hyponatremia, electrocardiographic changes, eosinophilia, and proteinuria

Read the entire FDA prescribing information for Lotensin (Benazepril)

Read More »

For the Consumer

Applies to benazepril: oral tablet

Along with its needed effects, benazepril may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking benazepril:

Less common
  • Chills
  • cold sweats
  • confusion
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • unusual tiredness or weakness
Incidence not known
  • Arm, back, or jaw pain
  • blistering, peeling, or loosening of the skin
  • bloating or swelling of the face, arms, hands, lower legs, or feet
  • chest pain or discomfort
  • diarrhea
  • fast, irregular, pounding, or racing heartbeat or pulse
  • feeling of warmth
  • fever
  • general feeling of tiredness or weakness
  • itching
  • joint or muscle pain
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • nausea
  • rapid breathing
  • rapid weight gain
  • red skin lesions, often with a purple center
  • red, irritated eyes
  • redness of the face, neck, arms, and occasionally, upper chest
  • shortness of breath
  • skin rash
  • sore throat
  • sores, ulcers, or white spots in the mouth or on the lips
  • sweating
  • tingling of the hands or feet
  • unusual weight gain or loss
  • wheezing

Some side effects of benazepril may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Headache
Less common
  • Cough
  • dizziness
  • sleepiness or unusual drowsiness

Precautions

US BOXED WARNING:
-FETAL TOXICITY: If pregnancy is detected, discontinue this drug as soon as possible. Drugs that act directly on the renin-angiotensin system (RAS) can cause injury and death to the developing fetus.

Safety and efficacy have not been established in patients younger than 6 years.

Consult WARNINGS section for additional precautions.

Bottom Line

Benazepril is used for the treatment of high blood pressure. Benazepril, as with other ACE inhibitors, may not be as effective in people of African-American descent.

Pharmacology

Mechanism of Action

Angiotensin converting enzyme (ACE) inhibitors dilate arteries and veins by competively inhibiting the conversion of angiotensin I to angiotensin II (a potent endogenous vasoconstrictor) and by inhibiting bradykinin metabolism; these actions result in preload and afterload reductions on the heart

ACE inhibitors also promote sodium and water excretion by inhibiting angiotensin-II induced aldosterone secretion; elevation in potassium may also be observed

ACE inhibitors also elicit renoprotective effects through vasodilation of renal arterioles

ACE inhibitors reduce cardiac and vascular remodeling associated with chronic hypertension, heart failure, and myocardial infarction

Absorption

Bioavailability: 37%

Onset: 1-2 hr (peak effect with 2-20 mg dose)

Duration: 24 hr (with 5-20 mg dose)

Peak plasma time: 0.5-1 hr (parent drug)

Distribution

Protein bound: 95-97%

Vd: 8.7 L

Metabolism

Metabolite: Benazeprilat (active)

Elimination

Half-life: 10-11 hr

Dialyzable: Minimal

Excretion: Urine (primarily); bile (11-12%)

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