Dosing and uses of Lotensin (benazepril)
Adult dosage forms and strengths
tablet
- 5mg
- 10mg
- 20mg
- 40mg
Hypertension
Patients taking a diuretic: 5 mg/day PO initially, to avoid excessive hypotension
Patients not taking a diuretic: 10 mg/day PO
May increase to maintenance dose of 20-40 mg/day PO qDay or divided q12hr
Nephropathy-Nondiabetic (Off-label)
10-20 mg PO qDay
Dosing Modifications
Renal Impairment
- CrCl< 30 mL/min: 5 mg PO qDay initially; not to exceed 40 mg/day
Hepatic Impairment
- Not studied
Dosing Considerations
Consider starting an ACE inhibitor in high-risk patients, even if no hypertension or CHF
No sexual dysfunction side effect
Good choice in hyperlipidemia patients
Requires weeks for full effect; to start, use low dose and titrate q1-2wk
Abrupt discontinuance not associated with rapid increase in Bp
Beneficial for many patients at risk for heart disease
Reduces risk of MI, stroke, diabetic nephropathy, microalbuminuria, new-onset diabetes mellitus
May preserve renal function in diabetes mellitus
May help to prevent migraine headaches
Pediatric dosage forms and strengths
tablet
- 5mg
- 10mg
- 20mg
- 40mg
Hypertension
<6 years: Safety and efficacy not established
≥6 years: 0.1-0.6 mg/kg PO qDay initially, not to exceed 5 mg/day; THEn
Adjust dose based on BP response; not to exceed 0.6 mg/kg/day or 40 mg/day
Suspension preparation
- The following prepares 150 mL of 2 mg/mL oral suspension
- Add 75 mL of Ora-Plus oral suspending vehicle to an amber polyethylene terephthalate (PET) bottle containing fifteen benazepril 20 mg tablets, and shake for at least 2 minutes
- Allow the suspension to stand for a minimum of 1 hr
- After the standing time, shake the suspension for a minimum of 1 additional minute, then add 75 mL of Ora-Sweet oral syrup vehicle to the bottle and shake the suspension to disperse the ingredients
- Store refrigerated at 2-8°C (36-46°F) for up to 30 days in the PET bottle with a child-resistant screw-cap closure
- Shake the suspension before each use
Dosing Modification
Renal impairment (CrCl <30 mL/min): Insufficient data to recommend dosage adjustment
Geriatric dosage forms and strengths
Hypertension
5-10 mg/day PO initially in single or divided doses
Maintenance: 20-40 mg/day PO adjust for renal function
Dosing Modifications
Adjust dose for renal function; benazepril and benazeprilat are substantially excreted by the kidney
Because elderly patients are more likely to have decreased renal function, take care in dose selection; it may be useful to monitor renal function
Lotensin (benazepril) adverse (side) effects
1-10%
Cough (1-10%)
Headache (6%)
Dizziness (4%)
Fatigue (2%)
Postural dizziness (2%)
Serum creatinine increased (2%)
Somnolence (2%)
Nausea (1%)
ARF if renal artery stenosis (1%)
<1% (selected)
Anaphylactoid reaction
Angina
Angioedema
ECG changes
Flushing
Hypotension
Palpitations
Postural hypotension
Syncope
Insomnia
Alopecia
Dermatitis
Rash
Hyperglycemia
Pancreatitis
Gastritis
Vomiting
Agranulocytosis
Eosinophilia
Hemolytic anemia
Hyperkalemia
Hyponatremia
Leukopenia
Neutropenia
Thrombocytopenia
Transaminases increased
Arthritis
Arthralgia
Impotence
Proteinuria
Asthma
Dyspnea
Stevens-Johnson syndrome
Uric acid increased
Postmarketing Reports
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 and psychiatric: Anxiety, decreased libido, hypertonia, insomnia, nervousness, and paresthesia
Fatigue
Asthma
Bronchitis
Dyspnea
Sinusitis
Urinary tract infection
Frequent urination
Infection
Arthritis
Impotence
Alopecia
Arthralgia
Myalgia
Asthenia
Sweating
Warnings
Black box warnings
Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system, causing oligohydramnios, which may result in fetal injury and/or death
Contraindications
Hypersensitivity
History of hereditary or idiopathic angioedema
Concomitant administration with aliskiren in patients with diabetes mellitus or with renal impairment
Cautions
Excessive hypotension with or without syncope may occur if hypovolemia/hyponatremia present or if coadministered with diuretics
Dual blockade of the renin-angiotensin system with ARBs, ACE inhibitors, or aliskiren associated with increased risk for hypotension, hyperkalemia, and renal function changes (including acute renal failure), compared with monotherapy
Most patients receiving the combination of two RAS inhibitors do not obtain any additional benefit compared to monotherapy; avoid combined use of RAS inhibitors; closely monitor blood pressure, renal function and electrolytes in patients on benazepril and other agents that affect the RAs
Not for coadministration with aliskiren in patients with diabetes; avoid use of aliskiren with benazepril in patients with renal impairment (GFR <60 ml/min/1.73 m²)
ACE inhibition causes increased bradykinin levels, which putatively mediates angioedema (higher incidence in black patients)
Cough may occur due to increased bradykinin levels
Cholestatic jaundice reported with use
Avoid use in bilateral renal artery stenosis
Angioedema may occur; coadministration with mTOR inhibitors (eg, temsirolimus) may increase risk for angioedema; discontinue therapy and treat appropriately if angioedema occurs
Discontinue immediately if pregnancy occurs (see Black box warnings)
ACE inhibitors are less effective in black patients
Renal impairment may occur
Rare cases of agranylocytosis reported ACE inhibitor therapy
May cause hypotension during surgery; additive hypotensive effects may occur with anesthetic agents that produce hypotension (correct by volume expansion)
Deterioration of renal function may occur; may consider discontinuation of therapy in patients with progressive and/or significant deterioration in renal function
Monitor for jaundice or signs of liver failure
Pregnancy and lactation
Pregnancy category: d
Discontinue as soon as pregnancy detected; during the second and third trimesters of pregnancy, drugs that act directly on the renin-angiotensin system have been associated with fetal injury that includes hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death
Lactation: Minimal amount excreted in breast milk; use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Lotensin (benazepril)
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%)
