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benazepril (Lotensin)
Tradename: Lotensin.
Indications:
1) hypertension, especially in combination with diuretics
2) congestive heart failure
3) diabetic nephropathy
4) scleroderma renal crisis
5) nondiabetic proteinuric nephropathy [3]
Contraindications:
Caution: elderly patient may have exaggerated response
Dosage: HTN. Start 10 mg PO QD, max 80 mg/day.
Tabs: 5, 10, 20, 40 mg. Adjust for renal clearance < 30 mL/min
Pharmacokinetics:
1) 37% bioavailability, not affected by food
2) extensive 1st pass metabolism in the liver, by hydrolysis to its active metabolite (benazeprilat), via enzymatic hydrolysis
2) volume of distribution is 8-9 L
3) protein binding 96.7%
4) elimination 1/2life (benazeprilat):
a) 22 hours initially
b) 10-11 hours after after multiple dosing
5) eliminated (benazeprilat) by kidney (11-12% by non renal metabolism)
6) angiotensin converting enzyme (ACE)
a) peak effect in 1-2 hours after oral administration (2-20 mg)
b) > 90% inhibition of ACE for 24 hours after 5-20 mg dose
7) blood pressure
a) peak effect after 1 dose: 2-6 hours
b) maximum effect 2 weeks
8) 6% of benazeprilat eliminated after 4 hours of hemodialysis
Monitor: K+, BUN, creatinine, WBC (see ACE inhibitor)
Adverse effects:
1) cardiovascular
- orthostasis, angina, palpitations, chest pain, hypotension, syncope, flushing
2) central nervous system
- nervousness, depression, anxiety, somnolence, fatigue, dizziness, headache, insomnia
3) skin: rash, pruritus, angioedema
4) metabolic: hyperkalemia, hyponatremia
5) gastrointestinal:
-> ageusia, pancreatitis, xerostomia, constipation, nausea, vomiting, abdominal pain
6) genitourinary: impotence, decreased libido
7) hematologic: neutropenia, eosinophilia
8) neuromuscular:
-> myalgia, arthralgia, arthritis, paresthesia, weakness
9) ocular: blurred vision
10) hepatic: hepatitis
11) renal: proteinuria, oliguria, azotemia, renal insufficiency
12) respiratory:
a) chronic cough
1] non-productive
2] persistent
3] more often in women
4] 5-29% of patients
b) asthma, bronchitis, bronchospasm, dyspnea
c) sinusitis
13) diaphoresis
14) increased serum creatinine
a) 15-20% initial increase is acceptable [5]; up to 30% acceptable [4]
b) decline in creatinine within 1 month [5] (2 months [4]), otherwise discontinue
Drug interactions:
1) benazepril & K+ sparing diuretics may increase risk of hyperkalemia
2) non-steroidal anti-inflammatory drugs (NSAIDs) may reduce anti-hypertensive action of benazepril
3) allopurinol & benazepril may increase risk of neutropenia
4) antacids may diminish absorption of ACE inhibitors
5) probenecid may increase serum levels of ACE inhibitors
6) phenothiazines may increase ACE inhibitor effect
7) rifampin may increase ACE inhibitor effect
8) ACE inhibitors may increase serum digoxin levels
9) ACE inhibitors may increase serum lithium levels
10) ACE inhibitors may decrease tetracycline absorption (up to 37%) Mechanism of Action:
-> competitive inhibitor of angiotensin converting enzyme
Interactions
drug interactions
drug adverse effects (more general classes)
monitor with ACE inhibitors
General
angiotensin-converting enzyme (ACE) inhibitor
Properties
INHIBITS: angiotensin converting enzyme
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category D
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
- Geriatric Dosage Handbook, 6th edition, Selma et al eds,
Lexi-Comp, Cleveland, 2001
- Deprecated Reference
- NEJM Knowledge+ Complex Medical Care
- Medical Knowledge Self Assessment Program (MKSAP) 11, 16,
American College of Physicians, Philadelphia 1998, 2012
- Dicpinigaitis PV.
Angiotensin-converting enzyme inhibitor-induced cough:
ACCP evidence-based clinical practice guidelines.
Chest. 2006 Jan;129(1 Suppl):169S-173S.
PMID: 16428706
Component-of
amlodipine/benazepril (Lotrel)
benazepril/hydrochlorothiazide; benazepril/HCTZ (Lotensin HCTZ)