Benazepril Hcl (benazepril HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Benazepril is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor.
Benazepril is an angiotensin-converting enzyme (ACE, bradykininase, kininase II) inhibitor, the peptidyl dipeptidase that catalyzes the conversion of angiotensin I to angiotensin II. Angiotensin II is a vasoconstrictor substance that stimulates aldosterone secretion; inhibition of ACE results in decreased plasma angiotensin II, leading to reduced vasopressor activity and aldosterone secretion. Decreased aldosterone secretion may result in a small increase in serum potassium.
Kininase, an enzyme that is identical to ACE, degrades the potent vasodepressor bradykinin. Whether increased levels of bradykinin play a role in the therapeutic effects of benazepril remains unknown. The effects of benazepril on lowering blood pressure appear to be primarily from suppression of the renin-angiotensin-aldosterone system.
However, benazepril is antihypertensive in patients with low-renin hypertension. Benazepril, the ethylester of benazeprilat, is a prodrug and has little pharmacologic activity until hydrolyzed in the liver to benazeprilat. Like enalapril, fosinopril, lisinopril, quinapril, and ramipril, but unlike captopril, benazepril does not contain a sulfhydryl group.
In adults, peak serum concentrations of benazepril and benazeprilat are reached within 0.5-1 hour and 1-2 hours, respectively, after oral administration. The bioavailability of benazepril is not affected by food; however, food delays the time to peak plasma concentration of benazeprilat to 2-4 hours. The onset of antihypertensive activity was observed within 1 hour following administration of a single dose of benazepril, with peak reductions of blood pressure achieved between 2 and 4 hours.
Single and multiple doses of benazepril 10 mg or more 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. After a single dose, the antihypertensive effect persisted for 24 hours. In multiple dose studies, dosages of benazepril between 20-80 mg once daily decreased seated systolic blood pressure by about 6-12 mmHg and seated diastolic blood pressure by 4-7 mmHg.
The serum trough levels of benazepril represent blood pressure reductions of approximately 50% of the reductions seen at peak. Steady state concentrations of benazeprilat should be reached after 2 or 3 doses of once-daily benazepril.
Benazepril and benazeprilat are approximately 96.7 and 95.3% protein bound, respectively. Benazepril is largely metabolized by cleavage of the ester group to benazeprilat, primarily in the liver. Both benazepril and benazeprilat undergo glucuronidation, and both are excreted predominantly by the kidneys.
After oral administration, about 37% was recovered in the urine: 20% as benazeprilat, 8% as benazeprilat glucuronide, 4% as benazepril glucuronide, and as trace amounts of benazepril. About 11-12% of benazeprilat excretion occurs through nonrenal (i.e., biliary) excretion. After repeat oral administration of benazepril, the effective half-life of benazeprilat is 10-11 hours.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Benazepril belongs to a class of drugs known as ACE inhibitors.
It works by relaxing blood vessels so blood can flow more easily.
Generic name: benazepril HCl
Pronunciation: (ben-AZ-e-pril)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Benazepril Hcl
Indications
The following indications are listed for Benazepril Hcl:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
Benazepril is available as benazepril hydrochloride; dosage is expressed in terms of the salt.
Benazepril hydrochloride is administered orally. The drug is commercially available as single-entity 5, 10, 20, or 40 mg tablets. Benazepril hydrochloride is also commercially available as a fixed-combination capsule containing amlodipine besylate and benazepril hydrochloride and as a fixed-combination tablet containing benazepril hydrochloride and hydrochlorothiazide; see the full prescribing information for administration of these fixed-combination products.
Store benazepril tablets in a tightly closed bottle, protected from light and moisture at 20-25degreesC.
For adult or pediatric patients unable to swallow tablets or those children for whom the daily dosage does not correspond exactly to the strength of commercially available tablets, benazepril may be administered orally as an extemporaneously prepared suspension.
An extemporaneous suspension containing benazepril hydrochloride 2 mg/mL can be prepared in the following manner. First, 75 mL of suspending vehicle (Ora-Plus(R)) is added to an amber polyethylene terephthalate (PET) bottle containing fifteen 20-mg tablets of benazepril hydrochloride, and the contents are shaken for at least 2 minutes. The concentrated suspension should be allowed to stand for at least 60 minutes following reconstitution, and then should be shaken for a minimum of 1 additional minute. The concentrated suspension of benazepril hydrochloride should be diluted with 75 mL of syrup (Ora-Sweet(R)), and the container then shaken to disperse the ingredients. The suspension should be shaken before dispensing each dose. The extemporaneous suspension is stable for 30 days when stored at 2-8degreesC.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to benazepril or to any other angiotensin-converting enzyme (ACE) inhibitor.
*History of angioedema with or without prior ACE inhibitor therapy.
*Concomitant use with aliskiren in patients with diabetes mellitus.
*Use in combination with a neprilysin inhibitor (e.g., sacubitril); do not administer within 36 hours of switching to or from sacubitril/valsartan.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported at an incidence >=1% include headache, dizziness, somnolence, and postural dizziness.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of benazepril have not been established in children younger than 6 years of age or in pediatric patients with creatinine clearance <30 mL/minute.
Benazepril can cause fetal harm when administered to pregnant females.
Use of medications that impact the RAS, such as benazepril, during the second and third trimesters of pregnancy decreases fetal renal function and increases fetal/neonatal morbidity and mortality. Oligohydramnios caused by medications that act on the RAS can result in fetal lung hypoplasia, skeletal deformations (including skull hypoplasia), anuria, hypotension, renal failure, and death.
Discontinue benazepril as soon as possible when pregnancy is detected. In the rare case that there is no appropriate alternative to therapy with drugs affecting the RAS, apprise the mother of the potential hazard to the fetus.
Perform serial ultrasound examinations to assess the intra-amniotic environment. Based on the week of pregnancy, fetal testing may be appropriate. However, patients and clinicians should be aware that oligohydramnios may not manifest until after the fetus has sustained irreversible injury. Closely observe neonates with a history of in utero exposure to benazepril for hypotension, oliguria, and hyperkalemia. If oliguria or hypotension occurs, support blood pressure and renal perfusion. Exchange transfusions or dialysis may be required.
Monitor pregnant females with hypertension carefully and manage accordingly.
Benazepril and benazeprilat (active metabolite of benazepril) are distributed into human milk in minimal amounts. Because of the unknown effects of benazepril or benazeprilat in nursing infants, a decision should be made whether to discontinue nursing or benazepril, taking into account the potential risk in breast-feeding infants and the importance of the drug to the woman.
The manufacturers make no specific dosage recommendations for geriatric patients.
Because of the greater frequency of decreased renal function in geriatric patients, the manufacturers state that dosage selection should be made with caution and that it may be useful to monitor renal function in geriatric patients receiving benazepril.
No substantial differences in safety and efficacy have been observed in geriatric patients relative to younger adults, but increased sensitivity cannot be ruled out.
Because geriatric patients are more likely to have decreased renal function, dosage should be selected cautiously; it may be useful to monitor renal function in such patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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