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{{Short description|Medication used to treat high blood pressure and heart failure}} |
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{{Drugbox |
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{{Use dmy dates|date=October 2022}} |
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{{cs1 config |name-list-style=vanc |display-authors=6}} |
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| verifiedrevid = 443414091 |
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{{Infobox drug |
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| IUPAC_name = 2-amino}- |
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| verifiedrevid = 459529583 |
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| image = Benazepril.svg |
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| image = Benazepril structure.svg |
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| alt = |
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| caption = |
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| image2 = Benazepril-3D-balls.png |
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| alt2 = |
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<!--Clinical data--> |
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<!-- Clinical data --> |
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| pronounce = {{IPAc-en|b|ə|ˈ|n|æ|z|ə|p|r|ɪ|l}} |
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| tradename = Lotensin |
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| tradename = Lotensin, others |
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| Drugs.com = {{drugs.com|monograph|benazepril-hydrochloride}} |
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| Drugs.com = {{drugs.com|monograph|benazepril-hydrochloride}} |
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| MedlinePlus = a692011 |
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| MedlinePlus = a692011 |
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| pregnancy_category = D |
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| DailyMedID = Benazepril |
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| legal_status = Rx-only |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| routes_of_administration = Oral |
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| pregnancy_AU_comment = |
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| pregnancy_category = |
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| routes_of_administration = ] |
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| class = |
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| ATC_prefix = C09 |
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| ATC_suffix = AA07 |
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| ATC_supplemental = |
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<!--Pharmacokinetic data--> |
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<!-- Legal status --> |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled --> |
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| bioavailability = |
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| legal_AU_comment = |
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| protein_bound = 96.7% |
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| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F --> |
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| metabolism = ] ] |
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| legal_BR_comment = |
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| legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_CA_comment = |
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| legal_DE = <!-- Anlage I, II, III or Unscheduled --> |
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| legal_DE_comment = |
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| legal_NZ = <!-- Class A, B, C --> |
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| legal_NZ_comment = |
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| legal_UK = <!-- GSL, P, POM, CD, CD Lic, CD POM, CD No Reg POM, CD (Benz) POM, CD (Anab) POM or CD Inv POM / Class A, B, C --> |
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| legal_UK_comment = |
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| legal_US = Rx-only |
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| legal_US_comment = <ref name="Lotensin FDA label">{{cite web | title=Lotensin- benazepril hydrochloride tablet | website=DailyMed | date=21 January 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2abb091b-a53e-46b0-9b84-e5ee8f2bdd8e | access-date=11 February 2024}}</ref> |
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| legal_EU = |
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| legal_EU_comment = |
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| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV --> |
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| legal_UN_comment = |
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| legal_status = Rx-only |
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<!-- Pharmacokinetic data --> |
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| bioavailability = |
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| protein_bound = 96.7% |
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| metabolism = ] ] |
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| metabolites = |
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| onset = |
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| elimination_half-life = 10-11 hours |
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| elimination_half-life = 10-11 hours |
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| duration_of_action = |
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| excretion = ] and biliary |
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| excretion = ] and ] |
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<!--Identifiers--> |
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<!-- Identifiers --> |
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| CASNo_Ref = {{cascite|correct|CAS}} |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 86541-75-5 |
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| CAS_number = 86541-75-5 |
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| CAS_supplemental = |
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| ATC_prefix = C09 |
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| PubChem = 5362124 |
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| ATC_suffix = AA07 |
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| IUPHAR_ligand = 6374 |
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| PubChem = 5362124 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = DB00542 |
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| DrugBank = DB00542 |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = 4514935 |
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| ChemSpiderID = 4514935 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = UDM7Q7QWP8 |
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| UNII = UDM7Q7QWP8 |
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| KEGG = D07499 |
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| ChEBI_Ref = {{ebicite|correct|EBI}} |
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| KEGG2 = D00620 |
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| ChEBI = 3011 |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEBI_Ref = {{ebicite|correct|EBI}} |
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| ChEBI = 3011 |
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| ChEMBL = 838 |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL = 838 |
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| NIAID_ChemDB = |
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| PDB_ligand = |
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| synonyms = |
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<!--Chemical data--> |
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<!-- Chemical and physical data --> |
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| IUPAC_name = 2-amino]-2-oxo-4,5-dihydro-3''H''-1-benzazepin-1-yl]acetic acid |
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| C=24 | H=28 | N=2 | O=5 |
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| C = 24 |
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| molecular_weight = 424.49 g/mol |
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| H = 28 |
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| smiles = O=C(OCC)(N2C(=O)N(c1ccccc1CC2)CC(=O)O)CCc3ccccc3 |
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| N = 2 |
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| InChI = 1/C24H28N2O5/c1-2-31-24(30)20(14-12-17-8-4-3-5-9-17)25-19-15-13-18-10-6-7-11-21(18)26(23(19)29)16-22(27)28/h3-11,19-20,25H,2,12-16H2,1H3,(H,27,28)/t19-,20-/m0/s1 |
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| O = 5 |
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| InChIKey = XPCFTKFZXHTYIP-PMACEKPBBT |
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| SMILES = O=C(OCC)(N2C(=O)N(c1ccccc1CC2)CC(=O)O)CCc3ccccc3 |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI = 1S/C24H28N2O5/c1-2-31-24(30)20(14-12-17-8-4-3-5-9-17)25-19-15-13-18-10-6-7-11-21(18)26(23(19)29)16-22(27)28/h3-11,19-20,25H,2,12-16H2,1H3,(H,27,28)/t19-,20-/m0/s1 |
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| StdInChI = 1S/C24H28N2O5/c1-2-31-24(30)20(14-12-17-8-4-3-5-9-17)25-19-15-13-18-10-6-7-11-21(18)26(23(19)29)16-22(27)28/h3-11,19-20,25H,2,12-16H2,1H3,(H,27,28)/t19-,20-/m0/s1 |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey = XPCFTKFZXHTYIP-PMACEKPBSA-N |
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| StdInChI_comment = |
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| StdInChIKey = XPCFTKFZXHTYIP-PMACEKPBSA-N |
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| density = |
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| density_notes = |
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| melting_point = |
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| melting_high = |
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| melting_notes = |
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| boiling_point = |
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| boiling_notes = |
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| solubility = |
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| sol_units = |
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| specific_rotation = |
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}} |
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}} |
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'''Benazepril''', brand name '''Lotensin''', is a medication used to treat high blood pressure (]), ], and ]. Upon cleavage of its ] group by the ], benazepril is converted into its active form benazeprilat, a non-sulfhydryl ] (ACE) ]. |
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<!-- Definition and medical uses --> |
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==Dosage forms== |
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'''Benazepril''', sold under the brand name '''Lotensin''' among others, is a ] used to treat ], ], and ].<ref name=AHFS2019/> It is a reasonable initial treatment for high blood pressure.<ref name=AHFS2019/> It is taken by mouth.<ref name=AHFS2019/> Versions are available as the combinations benazepril/] and ].<ref name=AHFS2019/> |
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<!-- Side effects and mechanisms --> |
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Oral tablets, 5 mg, 10 mg, 20 mg, and 40 mg. |
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Common side effects include feeling tired, ], cough, and ].<ref name=AHFS2019/> Serious side effects may include ], ], ], and ].<ref name=AHFS2019/> Use in ] may harm the baby, while use when ] may be safe.<ref name=Preg2019>{{cite web |title=Benazepril Pregnancy and Breastfeeding Warnings |url=https://www.drugs.com/pregnancy/benazepril.html |website=Drugs.com |access-date=3 March 2019 }}</ref> It is an ] and works by decreasing ] activity.<ref name=AHFS2019>{{cite web |title=Benazepril Hydrochloride Monograph for Professionals |url=https://www.drugs.com/monograph/benazepril-hydrochloride.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |access-date=3 March 2019 }}</ref> |
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<!-- Society and culture --> |
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Benazepril is also available in combination with ], under the trade name '''Lotensin HCT''', and with ] (trade name '''Lotrel'''). |
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Benazepril was patented in 1981 and came into medical use in 1990. It is available as a ].<ref name=AHFS2019/> In 2022, it was the 159th most commonly prescribed medication in the United States, with more than 3{{nbsp}}million prescriptions.<ref>{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Benazepril Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Benazepril | access-date = 30 August 2024 }}</ref> |
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==Medical uses== |
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Lotensin is ] for the treatment of hypertension, to lower blood pressure.<ref name="Lotensin FDA label" /><ref name=AHFS2019/> |
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==Side effects== |
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==Side effects== |
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The most common side effects patients experience are a ] or a chronic ]. The chronic cough develops in about 20% of people treated.<ref>{{cite web |url= http://www.medscape.com/viewarticle/484537_2 | vauthors = Dykewicz MS | title=Cough and Angioedema From Angiotensin-Converting Enzyme Inhibitors: New Insights Into Mechanisms and Management|work=Medscape|date=April 2004 |access-date=2 April 2014}}</ref> |
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Most commonly, ] and ]. ] and ] can occur. ], or an elevation of potassium levels, can also occur. |
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Benazepril may cause harm to the ] during ]. |
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==Contraindications== |
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==Contraindications== |
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Benazepril can harm the fetus.<ref>{{Cite web|date=2011|title=Lotensin package insert|url=https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020033s040lbl.pdf|access-date=9 December 2020|website=U.S. ] (FDA) }}</ref> |
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==Dosage forms== |
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Benazepril should be discontinued during pregnancy. |
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It is also available in combination with ], under the brand name Lotensin HCT, and with ] (Lotrel). |
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==Kidney disease== |
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==Veterinary uses== |
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] |
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According to a 2006 article in the '']'', patients with advanced ] taking benazepril showed "substantial" kidney benefits.<ref name = Hou>{{cite journal | author = Hou F, Zhang X, Zhang G, Xie D, Chen P, Zhang W, Jiang J, Liang M, Wang G, Liu Z, Geng R | title = Efficacy and safety of benazepril for advanced chronic renal insufficiency | journal = N Engl J Med | volume = 354 | issue = 2 | pages = 131–40 | year = 2006 | pmid = 16407508 | doi = 10.1056/NEJMoa053107}}</ref> |
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Under the brand names Fortekor (])<ref>{{Cite web |title=Fortekor Flavor Tabs (5 mg) for Animal Use (Canada) |url=https://www.drugs.com/vet/fortekor-flavor-tabs-5-mg-can.html |access-date=2024-06-03 |website=Drugs.com |language=en}}</ref> and VetACE (Jurox Animal Health),<ref>{{Cite web |title=VetACE® - Jurox |url=https://www.jurox.com.au/product/vetace/ |access-date=2024-06-03 |website=www.jurox.com.au |language=en-AU}}</ref> benazepril is used to treat congestive heart failure in dogs<ref>{{cite journal | vauthors = King JN, Mauron C, Kaiser G | title = Pharmacokinetics of the active metabolite of benazepril, benazeprilat, and inhibition of plasma angiotensin-converting enzyme activity after single and repeated administrations to dogs | journal = American Journal of Veterinary Research | volume = 56 | issue = 12 | pages = 1620–1628 | date = December 1995 | doi = 10.2460/ajvr.1995.56.12.1620 | pmid = 8599524 }}</ref><ref>{{cite journal | vauthors = O'Grady MR, O'Sullivan ML, Minors SL, Horne R | title = Efficacy of benazepril hydrochloride to delay the progression of occult dilated cardiomyopathy in Doberman Pinschers | journal = Journal of Veterinary Internal Medicine | volume = 23 | issue = 5 | pages = 977–983 | year = 2009 | pmid = 19572914 | doi = 10.1111/j.1939-1676.2009.0346.x | doi-access = free }}</ref> and ] in cats and dogs.<ref>{{Cite web|title=Fortekor Flavor Tabs (5 mg) (Canada) for Animal Use|url=https://www.drugs.com/vet/fortekor-flavor-tabs-5-mg-can.html|access-date=9 December 2020|website=Drugs.com}}</ref> |
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{{clear-left}} |
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A long term study of patients' kidney disease revealed that patients who took benazepril had better kidney function and a slower progression of kidney disease. ] was much better in the group of patients taking the drug than their peers who took a ] drug.<ref name = Hitti>{{cite web |url= http://www.webmd.com/content/article/117/112524.htm |title= Drug May Treat Advanced Kidney Disease |accessdate= 2006-09-07 |last= Hitti |first= Miranda |coauthors= Chang, Louise |date= January 11, 2006 |publisher = ]}}</ref> This is notable because this category of pharmaceuticals have long been thought to cause further kidney damage or increase the rate of progression for kidney disease. |
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== References == |
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According to coverage of the study on WebMD: |
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{{cquote|]s can pose a potential threat to kidneys as well. The key question was whether damaged kidneys would worsen if patients took ACE inhibitors. In a nutshell, concerns centered on blood levels of ] and ], waste products that are excreted by the kidneys. Testing creatinine levels in the blood is used as a way to monitor kidney function (...) kidney problems worsened more slowly in those taking Lotensin. Overall, there were no major differences in side effects between patients taking Lotensin or the placebo.<ref name = Hitti/>}} |
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This study marks the first indication that benazepril, and perhaps other ACE inhibitors, may actually be beneficial in the treatment of ] in patients with kidney disease. |
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===Veterinary use=== |
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Under the brand names Fortekor (]) and VetACE (Jurox Animal Health), benazepril ] is used to treat ] in ]s and ] in ]s and ]s. |
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==References== |
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{{reflist}} |
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{{reflist}} |
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==External links== |
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* |
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{{ACE inhibitors}} |
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{{ACE inhibitors}} |
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{{Angiotensin receptor modulators}} |
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{{Portal bar | Medicine}} |
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{{Authority control}} |
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