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Identification
NameTrandolapril
Accession NumberDB00519  (APRD01269)
TypeSmall Molecule
GroupsApproved
Description

Trandolapril is a non-sulhydryl prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is metabolized to its biologically active diacid form, trandolaprilat, in the liver. Trandolaprilat inhibits ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Trandolapril may be used to treat mild to moderate hypertension, to improve survival following myocardial infarction in clinically stable patients with left ventricular dysfunction, as an adjunct treatment for congestive heart failure, and to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy.

Structure
Thumb
Synonyms
Mavik
Trandolaprilum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Maviktablet1 mg/1oralAbb Vie Inc.1996-04-26Not applicableUs
Mavikcapsule2 mgoralBgp Pharma Ulc1998-01-14Not applicableCanada
Mavikcapsule1 mgoralBgp Pharma Ulc1998-01-07Not applicableCanada
Mavikcapsule0.5 mgoralBgp Pharma Ulc1998-01-28Not applicableCanada
Mavikcapsule4 mgoralBgp Pharma Ulc2003-11-01Not applicableCanada
Maviktablet4 mg/1oralPhysicians Total Care, Inc.2004-06-25Not applicableUs
Maviktablet4 mg/1oralAbb Vie Inc.1996-04-26Not applicableUs
Maviktablet2 mg/1oralAbb Vie Inc.1996-04-26Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Trandolapriltablet1 mg/1oralAurobindo Pharma Limited2007-06-12Not applicableUs
Trandolapriltablet4 mg/1oralAv Kare, Inc.2013-07-30Not applicableUs
Trandolapriltablet1 mg/1oralTeva Pharmaceuticals USA Inc2007-02-072016-02-29Us
Trandolapriltablet2 mg/1oralAurobindo Pharma Limited2007-06-12Not applicableUs
Trandolapriltablet4 mg/1oralCitron Pharma LLC2007-06-12Not applicableUs
Trandolapriltablet2 mg/1oralAv Kare, Inc.2013-07-30Not applicableUs
Trandolapriltablet4 mg/1oralLupin Pharmaceuticals, Inc.2007-06-11Not applicableUs
Trandolapriltablet2 mg/1oralCitron Pharma LLC2007-06-12Not applicableUs
Trandolapriltablet1 mg/1oralAv Kare, Inc.2013-07-30Not applicableUs
Trandolapriltablet2 mg/1oralLupin Pharmaceuticals, Inc.2007-06-11Not applicableUs
Trandolapriltablet1 mg/1oralCitron Pharma LLC2007-06-12Not applicableUs
Trandolapriltablet4 mg/1oralCobalt Laboratories2007-06-12Not applicableUs
Trandolapriltablet1 mg/1oralLupin Pharmaceuticals, Inc.2007-06-11Not applicableUs
Trandolapriltablet4 mg/1oralPhysicians Total Care, Inc.2009-08-26Not applicableUs
Trandolapriltablet2 mg/1oralCobalt Laboratories2007-06-12Not applicableUs
Trandolapriltablet4 mg/1oralDispensing Solutions, Inc.2007-02-07Not applicableUs
Trandolapriltablet2 mg/1oralCarilion Materials Management2007-02-07Not applicableUs
Trandolapriltablet4 mg/1oralEpic Pharma, LLC2015-03-31Not applicableUs
Trandolapriltablet1 mg/1oralCobalt Laboratories2007-06-12Not applicableUs
Trandolapriltablet2 mg/1oralEpic Pharma, LLC2015-03-31Not applicableUs
Trandolapriltablet4 mg/1oralTeva Pharmaceuticals USA Inc2007-02-07Not applicableUs
Trandolapriltablet1 mg/1oralCarilion Materials Management2007-06-11Not applicableUs
Trandolapriltablet1 mg/1oralEpic Pharma, LLC2015-03-31Not applicableUs
Trandolapriltablet2 mg/1oralTeva Pharmaceuticals USA Inc2007-02-072016-03-31Us
Trandolapriltablet4 mg/1oralAurobindo Pharma Limited2007-06-12Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
TarkaAbb Vie Inc.
Trandolapril and Verapamil HydrochlorideGlenmark Pharmaceuticals Inc., Usa
Trandolapril and Verapamil Hydrochloride ERGreenstone LLC
SaltsNot Available
Categories
UNII1T0N3G9CRC
CAS number87679-37-6
WeightAverage: 430.5372
Monoisotopic: 430.246772208
Chemical FormulaC24H34N2O5
InChI KeyInChIKey=VXFJYXUZANRPDJ-WTNASJBWSA-N
InChI
InChI=1S/C24H34N2O5/c1-3-31-24(30)19(14-13-17-9-5-4-6-10-17)25-16(2)22(27)26-20-12-8-7-11-18(20)15-21(26)23(28)29/h4-6,9-10,16,18-21,25H,3,7-8,11-15H2,1-2H3,(H,28,29)/t16-,18+,19-,20-,21-/m0/s1
IUPAC Name
(2S,3aR,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-octahydro-1H-indole-2-carboxylic acid
SMILES
[H][C@@]12C[[email protected]](N(C(=O)[[email protected]](C)N[C@@H](CCC3=CC=CC=C3)C(=O)OCC)[C@@]1([H])CCCC2)C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as peptides. These are compounds containing an amide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentPeptides
Alternative Parents
Substituents
  • Alpha peptide
  • N-acyl-alpha amino acid or derivatives
  • N-acyl-alpha-amino acid
  • Alpha-amino acid ester
  • Alpha-amino acid amide
  • Phenylpropylamine
  • Alpha-amino acid or derivatives
  • N-substituted-alpha-amino acid
  • Indole or derivatives
  • Pyrrolidine carboxylic acid or derivatives
  • Pyrrolidine carboxylic acid
  • N-acylpyrrolidine
  • Aralkylamine
  • Fatty acid ester
  • Fatty acyl
  • Benzenoid
  • Dicarboxylic acid or derivatives
  • Monocyclic benzene moiety
  • Tertiary carboxylic acid amide
  • Pyrrolidine
  • Tertiary amine
  • Carboxylic acid ester
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Secondary aliphatic amine
  • Carboxylic acid
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of mild to moderate hypertension, as an adjunct in the treatment of congestive heart failure (CHF), to improve survival following myocardial infarction (MI) in individuals who are hemodynamically stable and demonstrate symptoms of left ventricular systolic dysfunction or signs of CHF within a few days following acute MI, and to slow progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy.
PharmacodynamicsTrandolapril is the ethyl ester prodrug of a nonsulfhydryl ACE inhibitor, trandolaprilat. Trandolapril is deesterified in the liver to the diacid metabolite, trandolaprilat, which is approximately eight times more active as an inhibitor of ACE than its parent compound. ACE is a peptidyl dipeptidase that is part of the RAAS. The RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from the granular cells of the juxtaglomerular apparatus in the kidneys. In the blood stream, renin cleaves circulating angiotensinogen to ATI, which is subsequently cleaved to ATII by ACE. ATII increases blood pressure via a number of mechanisms. First, it stimulates the secretion of aldosterone from the adrenal cortex. Aldosterone travels to the distal convoluted tubule (DCT) and collecting tubule of nephrons where it increases sodium and water reabsorption by increasing the number of sodium channels and sodium-potassium ATPases on cell membranes. Second, ATII stimulates the secretion of vasopressin (also known as antidiuretic hormone or ADH) from the posterior pituitary gland. ADH stimulates further water reabsorption from the kidneys via insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules. Third, ATII increases blood pressure through direct arterial vasoconstriction. Stimulation of the Type 1 ATII receptor on vascular smooth muscle cells leads to a cascade of events resulting in myocyte contraction and vasoconstriction. In addition to these major effects, ATII induces the thirst response via stimulation of hypothalamic neurons. ACE inhibitors inhibit the rapid conversion of ATI to ATII and antagonize RAAS-induced increases in blood pressure. ACE (also known as kininase II) is also involved in the enzymatic deactivation of bradykinin, a vasodilator. Inhibiting the deactivation of bradykinin increases bradykinin levels and may further sustain the effects of trandolaprilat by causing increased vasodilation and decreased blood pressure. The blood pressure lowering effect of trandolaprilat is due to a decrease in peripheral vascular resistance, which is not accompanied by significant changes in urinary excretion of chloride or potassium or water or sodium retention.
Mechanism of actionThere are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Trandolaprilat, the active metabolite of trandolapril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Trandolaprilat also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors.
Related Articles
Absorption~ 40-60% absorbed; extensive first pass metabolism results in a low bioavailability of 4-14%
Volume of distribution
  • 18 L
Protein bindingSerum protein binding of trandolapril is ~ 80% (independent of concentration and not saturable) while that of trandolaprilat is 65 to 94% (concentration-dependent and saturable).
Metabolism

Cleavage of the ester group of trandolapril, primarily in the liver, is responsible for conversion to trandolaprilat, the active metabolite. Seven other metabolites, including diketopiperazine and glucuronide conjugated derivatives of trandolapril and trandolaprilat, have been identified.

SubstrateEnzymesProduct
Trandolapril
Not Available
DiketopiperazineDetails
Trandolapril
Not Available
TrandolaprilatDetails
Route of eliminationAfter oral administration of trandolapril, about 33% of parent drug and metabolites are recovered in urine, mostly as trandolaprilat, with about 66% in feces.
Half lifeThe elimination half lives of trandolapril and trandolaprilat are about 6 and 10 hours, respectively, but, similar to all ACE inhibitors, trandolaprilat also has a prolonged terminal elimination phase that involves a small fraction of administered drug. This likely represents drug binding to plasma and tissue ACE. The effective half life of elimination for trandolaprilat is 16-24 hours.
Clearance
  • 52 L/h [After approximately 2 mg IV doses]
ToxicityMost likely clinical manifestations of overdose are symptoms of severe hypotension. Most common adverse effects include cough, headache and dizziness. The oral LD50 of trandolapril in mice was 4875 mg/kg in males and 3990 mg/kg in females. In rats, an oral dose of 5000 mg/kg caused low mortality (1 male out of 5; 0 females). In dogs, an oral dose of 1000 mg/kg did not cause mortality and abnormal clinical signs were not observed.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Trandolapril Metabolism PathwayDrug metabolismSMP00599
Trandolapril Action PathwayDrug actionSMP00157
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9303
Blood Brain Barrier-0.8908
Caco-2 permeable-0.8501
P-glycoprotein substrateSubstrate0.7744
P-glycoprotein inhibitor IInhibitor0.5527
P-glycoprotein inhibitor IIInhibitor0.7759
Renal organic cation transporterNon-inhibitor0.8336
CYP450 2C9 substrateNon-substrate0.8227
CYP450 2D6 substrateNon-substrate0.8935
CYP450 3A4 substrateSubstrate0.5515
CYP450 1A2 substrateNon-inhibitor0.915
CYP450 2C9 inhibitorNon-inhibitor0.785
CYP450 2D6 inhibitorNon-inhibitor0.9018
CYP450 2C19 inhibitorNon-inhibitor0.796
CYP450 3A4 inhibitorNon-inhibitor0.5339
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6906
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9188
BiodegradationNot ready biodegradable0.9587
Rat acute toxicity2.2048 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9811
hERG inhibition (predictor II)Non-inhibitor0.5531
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Abbott laboratories pharmaceutical products div
  • Aurobindo pharma ltd
  • Cipla ltd
  • Corepharma llc
  • Dr reddys laboratories ltd
  • Epic pharma llc
  • Invagen pharmaceuticals inc
  • Lupin ltd
  • Mylan pharmaceuticals inc
  • Teva pharmaceuticals usa
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Capsuleoral0.5 mg
Capsuleoral1 mg
Capsuleoral2 mg
Capsuleoral4 mg
Tabletoral1 mg/1
Tabletoral2 mg/1
Tabletoral4 mg/1
Tablet (extended-release)oral
Tablet, film coated, extended releaseoral
Prices
Unit descriptionCostUnit
Tarka 1-240 mg Controlled Release Tabs3.46USD tab
Tarka 4-240 mg Controlled Release Tabs3.4USD tab
Tarka 1-240 mg tablet sa3.33USD tablet
Tarka 2-180 mg tablet sa3.33USD tablet
Tarka 2-240 mg Controlled Release Tabs3.33USD tab
Tarka 2-240 mg tablet sa3.33USD tablet
Tarka 4-240 mg tablet sa3.33USD tablet
Tarka 2-180 mg Controlled Release Tabs3.29USD tab
Mavik 2 mg tablet1.61USD tablet
Mavik 4 mg tablet1.61USD tablet
Mavik 1 mg tablet1.47USD tablet
Trandolapril 1 mg tablet1.24USD tablet
Trandolapril 2 mg tablet1.23USD tablet
Trandolapril 4 mg tablet1.23USD tablet
Mavik 4 mg Capsule1.03USD capsule
Mavik 2 mg Capsule0.83USD capsule
Mavik 1 mg Capsule0.72USD capsule
Mavik 0.5 mg Capsule0.42USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1341206 No2001-03-202018-03-20Canada
CA2023089 No2003-01-142010-08-10Canada
US5744496 No1995-04-282015-04-28Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point119-123 °CNot Available
logP3.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0207 mg/mLALOGPS
logP1.31ALOGPS
logP1.95ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)3.8ChemAxon
pKa (Strongest Basic)5.21ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area95.94 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity115.79 m3·mol-1ChemAxon
Polarizability46.79 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Narendra Joshi, Shekhar Bhirud, Buddhavarapu Ramam, Arjun Bodkhe, “Process for the preparation of intermediates of trandolapril and use thereof for the preparation of trandolapril.” U.S. Patent US20060079698, issued April 13, 2006.

US20060079698
General References
  1. Berl T: Review: renal protection by inhibition of the renin-angiotensin-aldosterone system. J Renin Angiotensin Aldosterone Syst. 2009 Mar;10(1):1-8. doi: 10.1177/1470320309102747. [PubMed:19286752 ]
  2. Conen H, Brunner HR: Pharmacologic profile of trandolapril, a new angiotensin-converting enzyme inhibitor. Am Heart J. 1993 May;125(5 Pt 2):1525-31. [PubMed:8480624 ]
  3. Diaz A, Ducharme A: Update on the use of trandolapril in the management of cardiovascular disorders. Vasc Health Risk Manag. 2008;4(6):1147-58. [PubMed:19337528 ]
  4. Guay DR: Trandolapril: a newer angiotensin-converting enzyme inhibitor. Clin Ther. 2003 Mar;25(3):713-75. [PubMed:12852701 ]
  5. Jouquey S, Stepniewski JP, Hamon G: Trandolapril dose-response in spontaneously hypertensive rats: effects on ACE activity, blood pressure, and cardiac hypertrophy. J Cardiovasc Pharmacol. 1994;23 Suppl 4:S16-8. [PubMed:7527096 ]
  6. Reynolds NA, Wagstaff AJ, Keam SJ: Trandolapril/verapamil sustained release: a review of its use in the treatment of essential hypertension. Drugs. 2005;65(13):1893-914. [PubMed:16114984 ]
  7. Rubio-Guerra AF, Vargas-Robles H, Vargas-Ayala G, Rodriguez-Lopez L, Escalante-Acosta BA: The effect of trandolapril and its fixed-dose combination with verapamil on circulating adhesion molecules levels in hypertensive patients with type 2 diabetes. Clin Exp Hypertens. 2008 Oct;30(7):682-8. doi: 10.1080/10641960802251941. [PubMed:18855271 ]
  8. Sanbe A, Tanonaka K, Kobayasi R, Takeo S: Effects of long-term therapy with ACE inhibitors, captopril, enalapril and trandolapril, on myocardial energy metabolism in rats with heart failure following myocardial infarction. J Mol Cell Cardiol. 1995 Oct;27(10):2209-22. [PubMed:8576937 ]
  9. Torp-Pedersen C, Kober L: Effect of ACE inhibitor trandolapril on life expectancy of patients with reduced left-ventricular function after acute myocardial infarction. TRACE Study Group. Trandolapril Cardiac Evaluation. Lancet. 1999 Jul 3;354(9172):9-12. [PubMed:10406358 ]
  10. Authors unspecified: Trandolapril: an ACE inhibitor for treatment of hypertension. Med Lett Drugs Ther. 1996 Nov 22;38(988):104-5. [PubMed:8941256 ]
  11. Wiseman LR, McTavish D: Trandolapril. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in essential hypertension. Drugs. 1994 Jul;48(1):71-90. [PubMed:7525196 ]
  12. Zannad F: Trandolapril. How does it differ from other angiotensin converting enzyme inhibitors? Drugs. 1993;46 Suppl 2:172-81; discussion 182. [PubMed:7512472 ]
External Links
ATC CodesC09AA10C09BB10
AHFS Codes
  • 24:32.04
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (57.2 KB)
Interactions
Drug Interactions
Drug
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Trandolapril.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Trandolapril.
AlfuzosinAlfuzosin may increase the hypotensive activities of Trandolapril.
AliskirenAliskiren may increase the hyperkalemic activities of Trandolapril.
AllopurinolThe risk of a hypersensitivity reaction to Allopurinol is increased when it is combined with Trandolapril.
AmifostineTrandolapril may increase the hypotensive activities of Amifostine.
AprotininAprotinin may decrease the antihypertensive activities of Trandolapril.
ArdeparinArdeparin may increase the hyperkalemic activities of Trandolapril.
AzathioprineTrandolapril may increase the myelosuppressive activities of Azathioprine.
BrimonidineBrimonidine may increase the antihypertensive activities of Trandolapril.
ButabarbitalButabarbital may increase the hypotensive activities of Trandolapril.
ButethalButethal may increase the hypotensive activities of Trandolapril.
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Trandolapril.
CiprofloxacinTrandolapril may increase the arrhythmogenic activities of Ciprofloxacin.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Trandolapril.
DiazoxideDiazoxide may increase the hypotensive activities of Trandolapril.
DrospirenoneTrandolapril may increase the hyperkalemic activities of Drospirenone.
DuloxetineTrandolapril may increase the orthostatic hypotensive activities of Duloxetine.
EplerenoneEplerenone may increase the hyperkalemic activities of Trandolapril.
EverolimusThe risk or severity of adverse effects can be increased when Everolimus is combined with Trandolapril.
HeparinHeparin may increase the hyperkalemic activities of Trandolapril.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Trandolapril.
HexobarbitalHexobarbital may increase the hypotensive activities of Trandolapril.
IcatibantIcatibant may decrease the antihypertensive activities of Trandolapril.
InfliximabThe risk or severity of adverse effects can be increased when Trandolapril is combined with Infliximab.
IronThe risk or severity of adverse effects can be increased when Trandolapril is combined with Iron.
Iron DextranThe risk or severity of adverse effects can be increased when Trandolapril is combined with Iron Dextran.
LanthanumThe serum concentration of Trandolapril can be decreased when it is combined with Lanthanum.
LevodopaTrandolapril may increase the orthostatic hypotensive activities of Levodopa.
LithiumThe serum concentration of Lithium can be increased when it is combined with Trandolapril.
MethohexitalMethohexital may increase the hypotensive activities of Trandolapril.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Trandolapril.
MolsidomineMolsidomine may increase the hypotensive activities of Trandolapril.
MoxonidineMoxonidine may increase the hypotensive activities of Trandolapril.
NicorandilNicorandil may increase the hypotensive activities of Trandolapril.
ObinutuzumabTrandolapril may increase the hypotensive activities of Obinutuzumab.
PentobarbitalPentobarbital may increase the hypotensive activities of Trandolapril.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Trandolapril.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Trandolapril.
PregabalinThe risk or severity of adverse effects can be increased when Trandolapril is combined with Pregabalin.
PrimidonePrimidone may increase the hypotensive activities of Trandolapril.
QuinineQuinine may increase the hypotensive activities of Trandolapril.
RisperidoneTrandolapril may increase the hypotensive activities of Risperidone.
RituximabTrandolapril may increase the hypotensive activities of Rituximab.
SacubitrilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Sacubitril.
SecobarbitalSecobarbital may increase the hypotensive activities of Trandolapril.
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Trandolapril.
SitagliptinThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Trandolapril.
Sodium aurothiomalateThe risk or severity of adverse effects can be increased when Trandolapril is combined with Sodium aurothiomalate.
TadalafilTadalafil may increase the antihypertensive activities of Trandolapril.
TemsirolimusThe risk or severity of adverse effects can be increased when Temsirolimus is combined with Trandolapril.
TizanidineTizanidine may increase the hypotensive activities of Trandolapril.
TolvaptanTolvaptan may increase the hyperkalemic activities of Trandolapril.
TorasemideTorasemide may increase the hypotensive activities of Trandolapril.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Trandolapril.
TreprostinilTreprostinil may increase the hypotensive activities of Trandolapril.
TriamtereneTriamterene may increase the hyperkalemic activities of Trandolapril.
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Trandolapril.
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Trandolapril.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Trandolapril.
VardenafilVardenafil may increase the antihypertensive activities of Trandolapril.
YohimbineYohimbine may decrease the antihypertensive activities of Trandolapril.
Food Interactions
  • Herbs that may attenuate the antihypertensive effect of trandolapril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.
  • High salt intake may attenuate the antihypertensive effect of trandolapril.
  • Take without regard to meals.
  • Trandolapril may decrease the excretion of potassium. Salt substitutes containing potassium may increase the risk of hyperkalemia.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Converts angiotensin I to angiotensin II by release of the terminal His-Leu, this results in an increase of the vasoconstrictor activity of angiotensin. Also able to inactivate bradykinin, a potent vasodilator. Has also a glycosidase activity which releases GPI-anchored proteins from the membrane by cleaving the mannose linkage in the GPI moiety.
Gene Name:
ACE
Uniprot ID:
P12821
Molecular Weight:
149713.675 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Piepho RW: Overview of the angiotensin-converting-enzyme inhibitors. Am J Health Syst Pharm. 2000 Oct 1;57 Suppl 1:S3-7. [PubMed:11030016 ]
  3. Song JC, White CM: Clinical pharmacokinetics and selective pharmacodynamics of new angiotensin converting enzyme inhibitors: an update. Clin Pharmacokinet. 2002;41(3):207-24. [PubMed:11929321 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Triglyceride lipase activity
Specific Function:
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester. Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine. Catalyzes the transesterification of cocaine to form cocaethylene. Displays fatty acid ethyl ester synthase activity,...
Gene Name:
CES1
Uniprot ID:
P23141
Molecular Weight:
62520.62 Da
References
  1. Zhu HJ, Appel DI, Johnson JA, Chavin KD, Markowitz JS: Role of carboxylesterase 1 and impact of natural genetic variants on the hydrolysis of trandolapril. Biochem Pharmacol. 2009 Apr 1;77(7):1266-72. doi: 10.1016/j.bcp.2008.12.017. Epub 2009 Jan 6. [PubMed:19185566 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Proton-dependent oligopeptide secondary active transmembrane transporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
Gene Name:
SLC15A1
Uniprot ID:
P46059
Molecular Weight:
78805.265 Da
References
  1. Knutter I, Wollesky C, Kottra G, Hahn MG, Fischer W, Zebisch K, Neubert RH, Daniel H, Brandsch M: Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited. J Pharmacol Exp Ther. 2008 Nov;327(2):432-41. doi: 10.1124/jpet.108.143339. Epub 2008 Aug 19. [PubMed:18713951 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Peptide:proton symporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides.
Gene Name:
SLC15A2
Uniprot ID:
Q16348
Molecular Weight:
81782.77 Da
References
  1. Knutter I, Wollesky C, Kottra G, Hahn MG, Fischer W, Zebisch K, Neubert RH, Daniel H, Brandsch M: Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited. J Pharmacol Exp Ther. 2008 Nov;327(2):432-41. doi: 10.1124/jpet.108.143339. Epub 2008 Aug 19. [PubMed:18713951 ]
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:11