Benazepril

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Pharmacokinetics 6 Monitor 7 Adverse-effects 8 Drug-interactions 9 More General Terms 10 Internet Database 11 References

Introduction

• Tradename: Lotensin.

Indications

• hypertension, especially in combination with diuretics
• congestive heart failure

Contraindications

• Caution: elderly patient may have exaggerated response
  
• pregnancy category = d
• safety in lactation = ?

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

• 37% bioavailability, not affected by food
• extensive 1st pass metabolism in the liver, by hydrolysis to its active metabolite (benazeprilat), via enzymatic hydrolysis
• volume of distribution is 8-9 L
• protein binding 96.7%
• elimination 1/2life (benazeprilat):

• 22 hours initially
• 10-11 hours after after multiple dosing

• eliminated (benazeprilat) by kidney (11-12% by non renal metabolism)
• angiotensin converting enzyme ( ACE)

• peak effect in 1-2 hours after oral administration (2-20 mg)
• > 90% inhibition of ACE for 24 hours after 5-20 mg dose

• blood pressure

• peak effect after 1 dose: 2-6 hours
• maximum effect 2 weeks

• 6% of benazeprilat eliminated after 4 hours of hemodialysis
  

• elimination via liver
• elimination via kidney

Monitor

• K+, BUN, creatinine, WBC (see ACE inhibitor)
  
• monitor with ACE inhibitors

Adverse-effects

• cardiovascular

• orthostasis, angina, palpitations, chest pain, hypotension, syncope, flushing

• central nervous system

• nervousness, depression, anxiety, somnolence, fatigue, dizziness, headache, insomnia

• skin: rash, pruritis, angioedema
• metabolic: hyperkalemia, hyponatremia
• gastrointestinal:

• ageusia, pancreatitis, xerostomia, constipation, nausea, vomiting, abdominal pain

• genitourinary: impotence, decreased libido
• hematologic: neutropenia, eosinophilia
• neuromuscular:

• myalgia, arthralgia, arthritis, paresthesia, weakness

• ocular: blurred vision
• hepatic: hepatitis
• renal: proteinuria, oliguria, azotemia, renal insufficiency
• respiratory:

• chronic cough

• non-productive
• persistent
• more often in women
• 5-29% of patients

• asthma, bronchitis, bronchospasm, dyspnea
• sinusitis

• diaphoresis
  
• drug adverse effects of ACE inhibitors

Drug-interactions

• benazepril & K+ sparing diuretics may increase risk of hyperkalemia
• non-steroidal anti-inflammatory drugs (NSAIDs) may reduce anti-hypertensive action of benazepril
• allopurinol & benazepril may increase risk of neutropenia
• antacids may diminish absorption of ACE inhibitors
• probenecid may increase serum levels of ACE inhibitors
• phenothiazines may increase ACE inhibitor effect
• rifampin may increase ACE inhibitor effect
• ACE inhibitors may increase serum digoxin levels
• ACE inhibitors may increase serum lithium levels
• ACE inhibitors may decrease tetracycline absorption (up to 37%) Mechanism of Action:

• competitive inhibitor of angiotensin converting enzyme
  

• drug interaction(s) of renin-angiotensin inhibitors with trimethoprim-sulfamethoxazole
• drug interaction(s) of lithium carbonate with ACE inhibitors
• drug interaction(s) of ACE inhibitors with aliskiren
• drug interaction(s) of ACE inhibitors with angiotensin II receptor antagonists
• drug interaction(s) of potassium chloride with ACE inhibitors
• drug interaction(s) of spironolactone with ACE inhibitors
• drug interaction(s) of diuretics with ACE inhibitors
• drug interaction(s) of beta blockers with ACE inhibitors
• drug interaction(s) of NSAIDs with ACE inhibitors
• drug interaction(s) of ACE inhibitors, angiotensin II receptor antagonists & beta-blockers
• drug interaction(s) of NSAIDs, diuretics & ACE inhibitors

More General Terms

• angiotensin-converting enzyme [ACE] inhibitor

Internet Database

PubChem: 55514
PubChem: 2311
PubChem: 55513

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
2. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001

benazepril (Lotensin)