Trandolapril

Trandolapril Basic information
Product Name:Trandolapril
Synonyms:(2s-(1(r*(r*)),2-alpha,3a-alpha,7a-beta))-)amino)-1-oxopropyl);ru44570;(2s,3ar,7as)-1-[(2s)-2-[[(1s)-1-ethoxycarbonyl-3-phenyl-propyl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid;Mavik, (2S,3aR,7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydro-1H-Indole-2-carboxylic acid;(3αR.7αS)-1-[N-[1(S)-(Ethoxycarbonyl)-3-phenylpropy]-(S)-alanyl]oetahydroindole-2(S)-carboxylic acid;TrandolaprilC24H34N205;Mavik, Odrik, Gopten, RU-44570;1H-Indole-2-carboxylic acid, 1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydro-, (2S,3aR,7aS)- (9CI)
CAS:87679-37-6
MF:C24H34N2O5
MW:430.54
EINECS:618-046-0
Product Categories:TERRAMYCIN;API;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File:87679-37-6.mol
Trandolapril Structure
Trandolapril Chemical Properties
Melting point 122-123°C
Boiling point 626.0±55.0 °C(Predicted)
density 1.181±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: ≥20mg/mL
pka3.15±0.20(Predicted)
form white powder
color White to Off-White
CAS DataBase Reference87679-37-6(CAS DataBase Reference)
Safety Information
WGK Germany 3
RTECS NL6015178
HS Code 2933995300
Hazardous Substances Data87679-37-6(Hazardous Substances Data)
Trandolapril Usage And Synthesis
DescriptionTrandolapril is a new ACE inhibitor that is rapidly hydrolyzed, mainly in the liver, to its biologically active form, trandolaprilat. Compared with all other ACE inhibitors, trandolaprilat is reported to have the highest lipophilicity and the most prolonged ACE inhibitory activity. In hypertensive patients, trandolapril at a dose of 2 mg reduces blood pressure consistently throughout the 24 hour period after intake, making it one of the best once a day antihypertensive drugs. It has also been demonstrated to inhibit aortic atherosclerosis in the hyperlipidemic rabbit.
Chemical PropertiesWhite or almost white powder.
OriginatorRoussel Uclaf (France)
UsesTrandolapril has been used as an angiotensin-converting enzyme (ACE) inhibitor to study its effects on responsiveness of human retinal endothelial cells (HRECs) to vascular endothelial growth factor (VEGF).
UsesAn antihypertensive. Angiotensin converting enzyme (ACE) inhibitor
Usesantibacterial
DefinitionChEBI: Trandolapril is a heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension. It has a role as a prodrug, an antihypertensive agent and an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor. It is a dicarboxylic acid monoester, a dipeptide, an ethyl ester, a secondary amino compound, a tertiary carboxamide and an organic heterobicyclic compound. It is functionally related to a trandolaprilat.
Brand nameOdrik; Udrik; Gopten
General DescriptionTrandolapril, 1-[2-(1-ethoxycarbonyl-3-phenylpropylamino)propionyl]octahydroindole-2-carboxylicacid (Mavik), is an indole-containing ACE inhibitorthat is structurally related to most of the precedingagents discussed. Enalapril is very similar to trandolapril,with the primary difference occurring in the heterocyclicsystems. The pyrrolidine of enalapril has been replacedwith an octahydroindole system. Much like enalaprilate,trandolapril must be hydrolyzed to tranolaprilate, which isthe bioactive species.
Biochem/physiol ActionsTrandolapril is an ACE inhibitor. Trandolapril differs from other ACE inhibitors in that it has a longer biological half-life and a high degree of lipophilicity.
Clinical UseAngiotensin converting enzyme inhibitor:
Hypertension
Heat failure
After myocardial infarction


Drug interactionsPotentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Analgesics: antagonism of hypotensive effect and increased risk of renal impairment with NSAIDs; hyperkalaemia with ketorolac and other NSAIDs.
Antihypertensives: increased risk of hyperkalaemia, hypotension and renal failure with ARBs and aliskiren.
Bee venom extract: possible severe anaphylactoid reactions when used together.
Ciclosporin: increased risk of hyperkalaemia and nephrotoxicity.
Cytotoxics: increased risk of angioedema with everolimus.
Diuretics: enhanced hypotensive effect; hyperkalaemia with potassium-sparing diuretics.
ESAs: increased risk of hyperkalaemia; antagonism of hypotensive effect.
Gold: flushing and hypotension with sodium aurothiomalate.
Lithium: reduced excretion (possibility of enhanced lithium toxicity).
Potassium salts: increased risk of hyperkalaemia.
Tacrolimus: increased risk of hyperkalaemia and nephrotoxicity.





MetabolismTrandolapril is metabolised in the liver to the active trandolaprilat and to some inactive metabolites. About 33
% of an oral dose of trandolapril is excreted in the urine, mainly as trandolaprilat; the rest is excreted in the faeces.
Trandolapril Preparation Products And Raw materials
Raw materialsN,N-Dimethylformamide-->Dicyclohexylcarbodiimide-->1-Hydroxybenzotriazole-->N-Ethylmorpholine
Trandolapril-d5 Phenetidine TRANDOLAPRIL-PHENYL-D5 Propyl gallate ZOPICLONE OXIDE Trandolapril Acyl--D-glucuronide, 85% TRANDOLAPRIL IMPURITY C 4-Ethoxyphenol DIETHOXYMETHANE Trandolaprilat Ethoxyquin PHENYL VALERATE Trandolapril Propyl butyrate acetic acid, triethoxy-, ethyl ester Diethoxymethyl acetate Phenylhydrazine 2-Ethoxyphenol

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