trandolapril 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
angiotensin-converting enzyme inhibitors	2712	87679-37-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: trandolapril gopten mavik odrik	The effect of trandolapril in hypertension appears to result primarily from the inhibition of circulating and tissue ACE activity thereby reducing angiotensin II formation, decreasing vasoconstriction, decreasing aldosterone secretion, and increasing plasma renin. Decreased aldosterone secretion leads to diuresis, natriuresis, and a small increase of serum potassium. Trandolapril is deesterified to the diacid metabolite, trandolaprilat, which is approximately eight times more active as an inhibitor of ACE activity. Molecular weight: 430.55 Formula: C24H34N2O5 CLOGP: 2.10 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 95.94 ALOGS: -4.32 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

trandolapril
gopten
mavik
odrik

The effect of trandolapril in hypertension appears to result primarily from the inhibition of circulating and tissue ACE activity thereby reducing angiotensin II formation, decreasing vasoconstriction, decreasing aldosterone secretion, and increasing plasma renin. Decreased aldosterone secretion leads to diuresis, natriuresis, and a small increase of serum potassium. Trandolapril is deesterified to the diacid metabolite, trandolaprilat, which is approximately eight times more active as an inhibitor of ACE activity.

Molecular weight: 430.55
Formula: C24H34N2O5
CLOGP: 2.10
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 95.94
ALOGS: -4.32
ROTB: 10

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
2	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.06 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	10 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.25 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	12.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.17 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.26 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
April 26, 1996	FDA	ABBVIE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Paranoia	61.67	18.86	23	3221	11656	63474122
Hallucination, auditory	59.57	18.86	23	3221	12801	63472977
Lactic acidosis	56.74	18.86	31	3213	38256	63447522
Psychotic disorder	56.04	18.86	27	3217	25685	63460093
Focal segmental glomerulosclerosis	49.00	18.86	12	3232	1456	63484322
Cerebellar haematoma	39.89	18.86	8	3236	387	63485391
Endometrial ablation	37.93	18.86	9	3235	955	63484823
Red blood cells urine positive	35.73	18.86	11	3233	3115	63482663
Bacterial test	31.21	18.86	8	3236	1166	63484612
Hyperaesthesia	30.44	18.86	13	3231	9345	63476433
White blood cells urine positive	30.33	18.86	11	3233	5147	63480631
Acute kidney injury	27.97	18.86	49	3195	263366	63222412
Urine abnormality	27.03	18.86	11	3233	7008	63478770
Asthma	25.54	18.86	32	3212	127529	63358249
Vaginal discharge	24.17	18.86	11	3233	9187	63476591
Cardiogenic shock	22.42	18.86	13	3231	17919	63467859
Organising pneumonia	22.07	18.86	9	3235	5767	63480011
Dorsal ramus syndrome	21.12	18.86	4	3240	143	63485635
Dyspnoea	20.50	18.86	77	3167	661236	62824542
Angioedema	20.38	18.86	18	3226	47947	63437831
HLA-B*27 positive	19.62	18.86	4	3240	210	63485568
Palindromic rheumatism	19.42	18.86	4	3240	221	63485557

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Oesophageal obstruction	75.55	19.03	16	3609	492	34952814
Bezoar	62.44	19.03	16	3609	1141	34952165
Arterial disorder	37.92	19.03	11	3614	1248	34952058
Oesophageal haemorrhage	28.83	19.03	9	3616	1309	34951997
Reading disorder	26.78	19.03	7	3618	539	34952767
Wrong product administered	25.50	19.03	12	3613	5322	34947984
Jugular vein distension	25.41	19.03	7	3618	659	34952647
Hypotension	23.73	19.03	63	3562	221586	34731720
Waist circumference increased	23.28	19.03	7	3618	899	34952407
White coat hypertension	22.87	19.03	5	3620	179	34953127
Eosinophil count increased	22.78	19.03	13	3612	8559	34944747
Body mass index increased	22.10	19.03	7	3618	1068	34952238
Cough	21.76	19.03	48	3577	150092	34803214
Bronchial wall thickening	20.44	19.03	7	3618	1361	34951945
Dysgraphia	20.39	19.03	8	3617	2279	34951027
Enterobacter pneumonia	20.12	19.03	4	3621	89	34953217

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Oesophageal obstruction	69.10	16.66	16	6115	1010	79737247
Lactic acidosis	60.17	16.66	47	6084	70312	79667945
Bezoar	53.82	16.66	16	6115	2672	79735585
Paranoia	41.42	16.66	23	6108	19409	79718848
Hallucination, auditory	40.07	16.66	23	6108	20670	79717587
Reading disorder	38.75	16.66	10	6121	992	79737265
Arterial disorder	36.19	16.66	11	6120	1979	79736278
Psychotic disorder	36.12	16.66	28	6103	41374	79696883
Endometrial ablation	34.96	16.66	9	6122	884	79737373
Acute kidney injury	33.90	16.66	102	6029	519302	79218955
Cerebellar haematoma	32.83	16.66	8	6123	628	79737629
Hyperkalaemia	30.99	16.66	41	6090	114357	79623900
Oesophageal haemorrhage	28.88	16.66	9	6122	1758	79736499
Bacterial test	27.65	16.66	8	6123	1215	79737042
Red blood cells urine positive	26.37	16.66	11	6120	4952	79733305
Hypoglycaemia	25.37	16.66	35	6096	101559	79636698
Dysgraphia	25.06	16.66	10	6121	4022	79734235
White blood cells urine positive	24.23	16.66	11	6120	6064	79732193
Cough	23.85	16.66	72	6059	366717	79371540
Vaginal discharge	22.07	16.66	11	6120	7452	79730805
Jugular vein distension	22	16.66	7	6124	1463	79736794
Hypotension	21.97	16.66	79	6052	440238	79298019
Urine abnormality	21.07	16.66	11	6120	8208	79730049
Waist circumference increased	21.04	16.66	7	6124	1682	79736575
Body mass index increased	20.12	16.66	7	6124	1926	79736331
Focal segmental glomerulosclerosis	19.82	16.66	8	6123	3313	79734944
Cardiogenic shock	19.76	16.66	20	6111	41894	79696363
Hyperaesthesia	19.52	16.66	12	6119	12210	79726047
Enterobacter pneumonia	19.33	16.66	4	6127	149	79738108
Libido decreased	19.23	16.66	9	6122	5312	79732945
Coagulopathy	18.49	16.66	18	6113	35988	79702269
Eosinophil count increased	18.11	16.66	13	6118	17092	79721165
Combined pulmonary fibrosis and emphysema	18.05	16.66	3	6128	32	79738225
Bronchial wall thickening	17.99	16.66	7	6124	2634	79735623
Itching scar	17.65	16.66	3	6128	37	79738220
White coat hypertension	16.70	16.66	5	6126	855	79737402

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C09AA10	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, PLAIN ACE inhibitors, plain
ATC	C09BB10	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, COMBINATIONS ACE inhibitors and calcium channel blockers
FDA MoA	N0000000181	Angiotensin-converting Enzyme Inhibitors
FDA EPC	N0000175562	Angiotensin Converting Enzyme Inhibitor
MeSH PA	D000806	Angiotensin-Converting Enzyme Inhibitors
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D011480	Protease Inhibitors
CHEBI has role	CHEBI:35457	ACE inhibitor
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:49103	drug metabolites
CHEBI has role	CHEBI:76967	human xenobiotic metabolites

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Chronic heart failure	indication	48447003
Left ventricular cardiac dysfunction	indication	429589006
Atrial fibrillation	off-label use	49436004	DOID:0060224
Diabetic renal disease	off-label use	127013003
Diastolic heart failure	off-label use	418304008	DOID:9775
Nondiabetic Proteinuric Nephropathy	off-label use
Hyperkalemia	contraindication	14140009
Ventricular tachycardia	contraindication	25569003
Complete atrioventricular block	contraindication	27885002
Acute cerebrovascular insufficiency	contraindication	29322000
Sick sinus syndrome	contraindication	36083008	DOID:13884
Immunosuppression	contraindication	38013005
Angioedema	contraindication	41291007	DOID:1558
Low cardiac output syndrome	contraindication	44088000
Low blood pressure	contraindication	45007003
Bradycardia	contraindication	48867003
Lown-Ganong-Levine syndrome	contraindication	55475008	DOID:13087
Aortic valve stenosis	contraindication	60573004	DOID:1712
Wolff-Parkinson-White pattern	contraindication	74390002	DOID:384
Duchenne muscular dystrophy	contraindication	76670001	DOID:11723
Transplantation	contraindication	77465005
Chronic idiopathic constipation	contraindication	82934008
Hereditary angioneurotic edema	contraindication	82966003	DOID:14735
Left heart failure	contraindication	85232009
Cardiogenic shock	contraindication	89138009
Hyponatremia	contraindication	89627008
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Disorder of connective tissue	contraindication	105969002	DOID:65
Liver function tests abnormal	contraindication	166603001
Second degree atrioventricular block	contraindication	195042002
Hypertrophic cardiomyopathy	contraindication	233873004	DOID:11984
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002
Renal artery stenosis	contraindication	302233006
Neutropenic disorder	contraindication	303011007	DOID:1227
Bone marrow depression	contraindication	307762000
Neuromuscular Transmission Deficiency	contraindication
Hemodialysis with High-Flux Membrane	contraindication
First Degree Atrioventricular Heart Block	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.23	acidic
pKa2	5.77	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Angiotensin-converting enzyme	Enzyme	P12821	ACE_HUMAN	INHIBITOR	IC50	8.12		WOMBAT-PK	CHEMBL

External reference:

ID	Source
4020971	VUID
N0000148444	NUI
D00383	KEGG_DRUG
4020971	VANDF
C0076891	UMLSCUI
CHEBI:9649	CHEBI
CHEBI:141521	CHEBI
X93	PDB_CHEM_ID
CHEMBL1519	ChEMBL_ID
DB00519	DRUGBANK_ID
C052035	MESH_SUPPLEMENTAL_RECORD_UI
5484727	PUBCHEM_CID
6453	IUPHAR_LIGAND_ID
C061095	MESH_SUPPLEMENTAL_RECORD_UI
5746	INN_ID
1T0N3G9CRC	UNII
DB14209	DRUGBANK_ID
1546379	RXNORM
107488	MMSL
5448	MMSL
5606	MMSL
5642	MMSL
d04008	MMSL
004452	NDDF
108562001	SNOMEDCT_US
386871006	SNOMEDCT_US
C0165477	UMLSCUI
CHEMBL1201387	ChEMBL_ID
6370	INN_ID
87679-71-8	SECONDARY_CAS_RN
5464097	PUBCHEM_CID
6455	IUPHAR_LIGAND_ID
RR6866VL0O	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	42806-052	TABLET	1 mg	ORAL	ANDA	18 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	42806-053	TABLET	2 mg	ORAL	ANDA	18 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	42806-054	TABLET	4 mg	ORAL	ANDA	18 sections
Trandolapril	Human Prescription Drug Label	1	50090-4120	TABLET	2 mg	ORAL	ANDA	21 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4128	TABLET	1 mg	ORAL	ANDA	19 sections
Mavik	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5099	TABLET	4 mg	ORAL	NDA	20 sections
Tarka	HUMAN PRESCRIPTION DRUG LABEL	2	54868-5311	TABLET, FILM COATED, EXTENDED RELEASE	2 mg	ORAL	NDA	20 sections
Tarka	HUMAN PRESCRIPTION DRUG LABEL	2	54868-5320	TABLET, FILM COATED, EXTENDED RELEASE	4 mg	ORAL	NDA	20 sections
Tarka	HUMAN PRESCRIPTION DRUG LABEL	2	54868-5548	TABLET, FILM COATED, EXTENDED RELEASE	2 mg	ORAL	NDA	20 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6061	TABLET	4 mg	ORAL	ANDA	14 sections
Trandolapril	Human Prescription Drug Label	1	57237-089	TABLET	1 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	57237-090	TABLET	2 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	57237-091	TABLET	4 mg	ORAL	ANDA	20 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8003	TABLET	2 mg	ORAL	ANDA	18 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8390	TABLET	4 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	65862-164	TABLET	1 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	65862-164	TABLET	1 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	65862-165	TABLET	2 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	65862-165	TABLET	2 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	65862-166	TABLET	4 mg	ORAL	ANDA	20 sections
Trandolapril	Human Prescription Drug Label	1	65862-166	TABLET	4 mg	ORAL	ANDA	20 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	68151-0757	TABLET	1 mg	ORAL	ANDA	18 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	68180-566	TABLET	1 mg	ORAL	ANDA	18 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	68180-567	TABLET	2 mg	ORAL	ANDA	18 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	68180-568	TABLET	4 mg	ORAL	ANDA	18 sections
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	68258-6100	TABLET	4 mg	ORAL	ANDA	20 sections
Trandolapril and Verapamil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	68462-294	TABLET, FILM COATED, EXTENDED RELEASE	1 mg	ORAL	ANDA	20 sections
Trandolapril and Verapamil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	68462-295	TABLET, FILM COATED, EXTENDED RELEASE	2 mg	ORAL	ANDA	20 sections
Trandolapril and Verapamil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	68462-296	TABLET, FILM COATED, EXTENDED RELEASE	2 mg	ORAL	ANDA	20 sections
Trandolapril and Verapamil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	68462-329	TABLET, FILM COATED, EXTENDED RELEASE	4 mg	ORAL	ANDA	20 sections