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| {{Lotensin}}
| | #REDIRECT [[Benazepril]] |
| <div style="width: 80%">
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| __NOTOC__
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| {{CMG}}; {{AE}} {{AM}}; {{AZ}}
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| '''''For information about Benazepril, click [[Benazepril|here]].'''''
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| ==Disclaimer==
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| '''''WikiDoc Drug Project is a constellation of drug information for healthcare providers and patients vigorously vetted on the basis of FDA package insert, MedlinePlus, Practice Guidelines, Scientific Statements, and scholarly medical literature. The information provided is not a medical advice or treatment. WikiDoc does not promote any medication or off-label use of drugs. Please read our full disclaimer [[wikidoc:General_disclaimer|{{fontcolor|#FF0000|here}}]].'''''
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| ==<span style="color:#FF0000; background:#000000;">Black Box Warning</span>==
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| {| style="border: 3px solid #696969;"
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| | style="background: #000000; border: 0px; padding: 20px 20px; width: 800px;" |
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| <center>
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| <font color="#F8F8FF" style="font-weight: bold;">WARNING</font>
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| </center>
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| <center>
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| <font color="#F8F8FF" size="1" style="font-style: italic;">See full prescribing information for complete boxed warning.</font>
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| </center>
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| <font color="#F8F8FF" style="font-weight: bold;">
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| ''{{fontcolor|#FF0000|Condition Name:}}'' (Content)
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| </font>
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| |}
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| ==Overview==
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| {{PAGENAME}} is a _______ drug that is FDA approved for the treatment of _______. There is a Black Box Warning for this drug as shown <span style="background:#000000;">'''[[{{PAGENAME}}#Black Box Warning|{{fontcolor|#FF0000|here}}]]'''</span>. Common adverse reactions include _______.
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| ==Adult Indications and Dosage==
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| ===FDA-Labeled Indications and Dosage (Adult)===
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| =====Condition 1=====
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 2=====
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| * Dosing Information
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| :: (Dosage)
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| ===Off-Label Use and Dosage (Adult)===
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| ====Guideline-Supported Use====
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| =====Condition 1=====
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| * Developed by: (Organisation)
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| * Class of Recommendation: (Class) (Link)
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| * Strength of Evidence: (Category A/B/C) (Link)
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 2=====
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| * Developed by: (Organisation)
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| * Class of Recommendation: (Class) (Link)
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| * Strength of Evidence: (Category A/B/C) (Link)
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| * Dosing Information
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| :: (Dosage)
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| ====Non–Guideline-Supported Use====
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| =====Condition 1=====
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 2=====
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 3=====
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| * Dosing Information
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| :: (Dosage)
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| ==Pediatric Indications and Dosage==
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| ===FDA-Labeled Indications and Dosage (Pediatric)===
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| =====Condition 1=====
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 2=====
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| * Dosing Information
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| :: (Dosage)
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| ===Off-Label Use and Dosage (Pediatric)===
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| ====Guideline-Supported Use====
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| =====Condition 1=====
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| * Developed by: (Organisation)
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| * Class of Recommendation: (Class) (Link)
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| * Strength of Evidence: (Category A/B/C) (Link)
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 2=====
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| * Developed by: (Organisation)
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| * Class of Recommendation: (Class) (Link)
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| * Strength of Evidence: (Category A/B/C) (Link)
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| * Dosing Information
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| :: (Dosage)
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| ====Non–Guideline-Supported Use====
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| =====Condition 1=====
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 2=====
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| * Dosing Information
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| :: (Dosage)
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| =====Condition 3=====
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| * Dosing Information
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| :: (Dosage)
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| ==Contraindications==
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| * [[Hypersensitivity]] to [[benazapril]] or to any other [[ACE inhibitor]]
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| * History of [[angioedema]] with or without previous [[ACE inhibitor]] treatment
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| ==Warnings==
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| =====Anaphylactoid and Possibly Related Reactions=====
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| Presumably because angiotensin-converting enzyme inhibitors affect the metabolism of [[eicosanoids]] and polypeptides, including endogenous [[bradykinin]], patients receiving [[ACE inhibitors]] (including Lotensin) may be subject to a variety of adverse reactions, some of them serious.
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| <u>'''Head and Neck Angioedema'''</u>: [[Angioedema]] of the face, extremities, lips, tongue, glottis, and larynx has been reported in patients treated with [[angiotensin-converting enzyme inhibitors]]. In U.S. clinical trials, symptoms consistent with [[angioedema]] were seen in none of the subjects who received placebo and in about 0.5% of the subjects who received Lotensin. [[Angioedema]] associated with [[laryngeal edema]] can be fatal. If laryngeal [[stridor]] or angioedema of the face, tongue, or [[glottis]] occurs, treatment with Lotensin should be discontinued and appropriate therapy instituted immediately. Where there is involvement of the tongue, [[glottis]], or [[larynx]], likely to cause airway obstruction, appropriate therapy, e.g., subcutaneous [[epinephrine]] injection 1:1000 (0.3 mL to 0.5 mL) should be promptly administered (see ADVERSE REACTIONS).
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| Black patients receiving ACE inhibitors have been reported to have a higher incidence of angioedema compared to nonblacks.
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| <u>'''Intestinal Angioedema'''</u>: Intestinal angioedema has been reported in patients treated with [[ACE inhibitors]]. These patients presented with [[abdominal pain]] (with or without [[nausea]] or [[vomiting]]); in some cases there was no prior history of facial angioedema and [[C-1 esterase]] levels were normal. The angioedema was diagnosed by procedures including abdominal [[CT scan]] or [[ultrasound]], or at surgery, and symptoms resolved after stopping the [[ACE inhibitor]]. Intestinal angioedema should be included in the differential diagnosis of patients on [[ACE inhibitors]] presenting with [[abdominal pain]].
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| <u>'''Anaphylactoid Reactions During Desensitization'''</u>: Two patients undergoing desensitizing treatment with [[hymenoptera venom]] while receiving [[ACE inhibitor]]s sustained life-threatening [[anaphylactoid reaction]]s. In the same patients, these reactions were avoided when [[ACE inhibitor]]s were temporarily withheld, but they reappeared upon inadvertent rechallenge.
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| <u>'''Anaphylactoid Reactions During Membrane Exposure'''</u>: [[Anaphylactoid reaction]]s have been reported in patients dialyzed with high-flux membranes and treated concomitantly with an [[ACE inhibitor]]. [[Anaphylactoid reaction]]s have also been reported in patients undergoing [[low-density lipoprotein]] apheresis with dextran sulfate absorption (a procedure dependent upon devices not approved in the United States).
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| =====Hypotension=====
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| Lotensin can cause symptomatic [[hypotension]]. Like other ACE inhibitors, benazepril has been only rarely associated with [[hypotension]] in uncomplicated hypertensive patients. Symptomatic [[hypotension]] is most likely to occur in patients who have been volume-and/or salt-depleted as a result of prolonged [[diuretic]] therapy, dietary salt restriction, [[dialysis]], [[diarrhea]], or [[vomiting]]. Volume-and/or salt-depletion should be corrected before initiating therapy with Lotensin.
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| In patients with [[congestive heart failure]], with or without associated [[renal insufficiency]], ACE inhibitor therapy may cause excessive [[hypotension]], which may be associated with [[oliguria]] or [[azotemia]] and, rarely, with [[acute renal failure]] and death. In such patients, Lotensin therapy should be started under close medical supervision; they should be followed closely for the first 2 weeks of treatment and whenever the dose of benazepril or diuretic is increased.
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| If [[hypotension]] occurs, the patient should be placed in a supine position, and, if necessary, treated with intravenous infusion of physiological [[saline]]. Lotensin treatment usually can be continued following restoration of blood pressure and volume.
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| =====Fetal toxicity=====
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| '''Pregnancy category D'''
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| Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Resulting [[oligohydramnios]] can be associated with fetal [[lung hypoplasia]] and skeletal deformations. Potential neonatal adverse effects include skull [[hypoplasia]], [[anuria]], [[hypotension]], [[renal failure]], and death. When pregnancy is detected, discontinue Lotensin as soon as possible. These adverse outcomes are usually associated with use of these drugs in the second and third trimester of pregnancy. Most epidemiologic studies examining fetal abnormalities after exposure to [[antihypertensive]] use in the first trimester have not distinguished drugs affecting the renin-angiotensin system from other [[antihypertensive agent]]s. Appropriate management of [[maternal hypertension]] during pregnancy is important to optimize outcomes for both mother and fetus.
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| In the unusual case that there is no appropriate alternative to therapy with drugs affecting the [[renin-angiotensin system]] for a particular patient, apprise the mother of the potential risk to the fetus. Perform serial ultrasound examinations to assess the intra-amniotic environment. If [[oligohydramnios]] is observed, discontinue Lotensin, unless it is considered lifesaving for the mother. Fetal testing may be appropriate, based on the week of pregnancy. Patients and physicians should be aware, however, that [[oligohydramnios]] may not appear until after the fetus has sustained irreversible injury. Closely observe infants with histories of in utero exposure to Lotensin for [[hypotension]], [[oliguria]], and [[hyperkalemia]] [see Precautions, Pediatric Use].
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| No teratogenic effects of Lotensin were seen in studies of pregnant rats, mice, and rabbits. On a mg/m2 basis, the doses used in these studies were 60 times (in rats), 9 times (in mice), and more than 0.8 times (in rabbits) the maximum recommended human dose (assuming a 50-kg woman). On a mg/kg basis these multiples are 300 times (in rats), 90 times (in mice), and more than 3 times (in rabbits) the maximum recommended human dose.
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| =====Hepatic Failure=====
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| Rarely, [[ACE inhibitors]] have been associated with a syndrome that starts with [[cholestatic jaundice]] and progresses to [[fulminant hepatic necrosis]] and (sometimes) death. The mechanism of this syndrome is not understood. Patients receiving [[ACE inhibitor]]s who develop [[jaundice]] or marked elevations of hepatic enzymes should discontinue the ACE inhibitor and receive appropriate medical follow-up.
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| ==Adverse Reactions==
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| ===Clinical Trials Experience===
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| =====Condition 1=====
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| ======Central Nervous System======
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| : (list/description of adverse reactions)
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| ======Cardiovascular======
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| : (list/description of adverse reactions)
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| ======Respiratory======
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| : (list/description of adverse reactions)
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| ======Gastrointestinal======
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| : (list/description of adverse reactions)
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| ======Hypersensitive Reactions======
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| : (list/description of adverse reactions)
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| ======Miscellaneous======
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| : (list/description of adverse reactions)
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| =====Condition 1=====
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| ======Central Nervous System======
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| : (list/description of adverse reactions)
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| ======Cardiovascular======
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| : (list/description of adverse reactions)
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| ======Respiratory======
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| : (list/description of adverse reactions)
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| ======Gastrointestinal======
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| : (list/description of adverse reactions)
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| ======Hypersensitive Reactions======
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| : (list/description of adverse reactions)
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| ======Miscellaneous======
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| : (list/description of adverse reactions)
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| ===Postmarketing Experience===
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| (Description)
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| ==Drug Interactions==
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| * Drug 1
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| * Drug 2
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| * Drug 3
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| * Drug 4
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| * Drug 5
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| =====Drug 1=====
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| (Description)
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| =====Drug 2=====
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| (Description)
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| =====Drug 3=====
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| (Description)
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| =====Drug 4=====
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| (Description)
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| =====Drug 5=====
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| (Description)
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| ==Use in Specific Populations==
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| ====Pregnancy====
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| : '''[[Pregnancy category#United States|Pregnancy Category (FDA)]]: X'''
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| : '''[[Pregnancy category#Australia|Pregnancy Category (AUS)]]: X'''
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| (Description)
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| ====Labor and Delivery====
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| (Description)
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| ====Nursing Mothers====
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| (Description)
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| ====Pediatric Use====
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| (Description)
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| ====Geriatric Use====
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| (Description)
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| ====Gender====
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| (Description)
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| ====Race====
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| (Description)
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| ====Renal Impairment====
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| (Description)
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| ====Hepatic Impairment====
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| (Description)
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| ====Females of Reproductive Potential and Males====
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| (Description)
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| ====Immunocompromised Patients====
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| (Description)
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| ==Administration and Monitoring==
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| ====Administration====
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| (Oral/Intravenous/etc)
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| ====Monitoring====
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| =====Condition 1=====
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| (Description regarding monitoring, from ''Warnings'' section)
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| =====Condition 2=====
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| (Description regarding monitoring, from ''Warnings'' section)
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| =====Condition 3=====
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| (Description regarding monitoring, from ''Warnings'' section)
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| ==IV Compatibility==
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| ===Solution===
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| ====Compatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Not Tested====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Variable====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Incompatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ===Y-Site===
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| ====Compatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Not Tested====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Variable====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Incompatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ===Admixture===
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| ====Compatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Not Tested====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Variable====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Incompatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ===Syringe===
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| ====Compatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Not Tested====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Variable====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Incompatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ===TPN/TNA===
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| ====Compatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Not Tested====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Variable====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ====Incompatible====
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| * Solution 1
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| * Solution 2
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| * Solution 3
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| ==Overdosage==
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| ===Acute Overdose===
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| ====Signs and Symptoms====
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| (Description)
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| ====Management====
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| (Description)
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| ===Chronic Overdose===
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| ====Signs and Symptoms====
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| (Description)
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| ====Management====
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| (Description)
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| ==Pharmacology==
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| {{Drugbox2
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| | verifiedrevid =
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| | IUPAC_name =
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| | image =
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| | drug_name =
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| <!--Clinical data-->
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| | tradename =
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| | MedlinePlus =
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| | licence_US =
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| | pregnancy_AU =
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| | pregnancy_US =
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| | legal_status =
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| | routes_of_administration =
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| <!--Pharmacokinetic data-->
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| | bioavailability =
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| | metabolism =
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| | elimination_half-life =
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| | excretion =
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| <!--Identifiers-->
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| | CAS_number_Ref =
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| | CAS_number =
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| | ATC_prefix =
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| | ATC_suffix =
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| | PubChem =
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| | IUPHAR_ligand =
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| | DrugBank_Ref =
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| | ChemSpiderID =
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| | UNII_Ref =
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| | UNII =
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| | KEGG_Ref =
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| | KEGG =
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| | ChEBI_Ref =
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| | ChEBI =
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| | ChEMBL_Ref =
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| | ChEMBL =
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| <!--Chemical data-->
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| | C= | H= | N= | O=
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| | molecular_weight =
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| | smiles =
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| | InChI =
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| | InChIKey =
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| | StdInChI_Ref =
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| | StdInChI =
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| | StdInChIKey_Ref =
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| | StdInChIKey =
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| | melting_point =
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| }}
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| ===Mechanism of Action===
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| Benazepril and benazeprilat inhibit [[angiotensin-converting enzyme]] ([[ACE]]) in human subjects and animals. [[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]].
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| 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]]. [[Hypertensive]] patients treated with Lotensin alone for up to 52 weeks had elevations of serum [[potassium]] of up to 0.2 mEq/L. Similar patients treated with Lotensin and [[hydrochlorothiazide]] for up to 24 weeks had no consistent changes in their serum potassium (see PRECAUTIONS).
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| 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]].
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| 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.
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| 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]] (see INDICATIONS AND USAGE).
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| ===Structure===
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| (Description with picture)
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| ===Pharmacodynamics===
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| 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.
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| ===Pharmacokinetics===
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| Following oral administration of Lotensin, peak plasma concentrations of benazepril are reached within 0.5-1.0 hours. The extent of absorption is at least 37% as determined by urinary recovery and is not significantly influenced by the presence of food in the GI tract.
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| Cleavage of the ester group (primarily in the liver) converts benazepril to its active metabolite, benazeprilat. Peak plasma concentrations of benazeprilat are reached 1-2 hours after drug intake in the fasting state and 2-4 hours after drug intake in the nonfasting state. 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).
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| Benazepril is almost completely metabolized to benazeprilat, which has much greater [[ACE]] inhibitory activity than benazepril, and to the [[glucuronide]] conjugates of benazepril and benazeprilat. Only trace amounts of an administered dose of Lotensin can be recovered in the urine as unchanged benazepril, while about 20% of the dose is excreted as benazeprilat, 4% as benazepril glucuronide, and 8% as benazeprilat glucuronide.
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| The kinetics of benazepril are approximately dose-proportional within the dosage range of 10-80 mg.
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| In adults, the effective half-life of accumulation of benazeprilat following multiple dosing 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.
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| The kinetics did not change, and there was no significant accumulation during chronic administration (28 days) of once-daily doses between 5 mg and 20 mg. Accumulation ratios based on AUC and urinary recovery of benazeprilat were 1.19 and 1.27, respectively.
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| Benazepril and benazeprilat are cleared predominantly by renal excretion in healthy subjects with normal renal function. Nonrenal (i.e., biliary) excretion accounts for approximately 11%-12% of benazeprilat excretion in healthy subjects. In patients with [[renal failure]], biliary clearance may compensate to an extent for deficient [[renal clearance]].
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| In patients with [[renal insufficiency]], the disposition of benazepril and benazeprilat in patients with mild-to-moderate [[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).
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| 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.
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| In patients with [[hepatic insufficiency]] (due to [[cirrhosis]]), the pharmacokinetics of benazeprilat are essentially unaltered. The pharmacokinetics of benazepril and benazeprilat do not appear to be influenced by age.
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| In pediatric patients, (N=45) hypertensive, age 6 to 16 years, given multiple daily doses of Lotensin (0.1 to 0.5 mg/kg), the clearance of benazeprilat for children 6 to 12 years old was 0.35 L/hr/kg, more than twice that of healthy adults receiving a single dose of 10 mg (0.13 L/hr/kg). In adolescents, it was 0.17 L/hr/kg, 27% higher than that of healthy adults. The terminal elimination half-life of benazeprilat in pediatric patients was around 5 hours, one-third that observed in adults.
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| ===Nonclinical Toxicology===
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| (Description)
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| ==Clinical Studies==
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| =====Condition 1=====
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| (Description)
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| =====Condition 2=====
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| (Description)
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| =====Condition 3=====
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| (Description)
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| ==How Supplied==
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| (Description)
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| * National Drug Code (NDC):
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| * Storage:
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| * Manufactured by:
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| * Distributed by:
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| ==Images==
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| ===Drug Images===
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| (PillBox Images)
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| ===Package and Label Display Panel===
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| (Package Images)
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| (Display Panel Images)
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| ==Patient Information==
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| ===Patient Information from FDA===
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| '''Pregnancy''': Female patients of childbearing age should be told about the consequences of exposure to Lotensin during pregnancy. Discuss treatment options with women planning to become pregnant. Patients should be asked to report pregnancies to their physicians as soon as possible.
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| '''Angioedema''': Angioedema, including laryngeal edema, can occur at any time with treatment with ACE inhibitors. Patients should be so advised and told to report immediately any signs or symptoms suggesting angioedema (swelling of face, eyes, lips, or tongue, or difficulty in breathing) and to take no more drug until they have consulted with the prescribing physician.
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| '''Symptomatic Hypotension''': Patients should be cautioned that lightheadedness can occur, especially during the first days of therapy, and it should be reported to the prescribing physician. Patients should be told that if syncope occurs, Lotensin should be discontinued until the prescribing physician has been consulted.
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| All patients should be cautioned that inadequate fluid intake or excessive perspiration, diarrhea, or vomiting can lead to an excessive fall in blood pressure, with the same consequences of lightheadedness and possible syncope.
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| '''Hyperkalemia''': Patients should be told not to use potassium supplements or salt substitutes containing potassium without consulting the prescribing physician.
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| '''Neutropenia''': Patients should be told to promptly report any indication of infection (e.g., sore throat, fever), which could be a sign of neutropenia.
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| ===Patient Information from NLM===
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| For patient information about benazepril from NLM, click [[Benazepril (patient information)|here]].
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| ==Precautions with Alcohol==
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| Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
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| ==Look-Alike Drug Names==
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| There is no look-alike drug names.
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| ==[http://www.fda.gov/drugs/drugsafety/drugshortages/ucm050792.htm Drug Shortage Status]==
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| ==[http://www.goodrx.com/{{urlencode:{{#if:{{{1|}}}|{{{1}}}|{{PAGENAME}}}}}}/price Price]==
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| ==References==
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| {{reflist}}
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| </div>
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