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
Lactic acidosis	58.60	20.22	31	2755	33324	50569014
Paranoia	55.40	20.22	21	2765	10327	50592011
Psychotic disorder	52.20	20.22	25	2761	21787	50580551
Hallucination, auditory	51.11	20.22	20	2766	10708	50591630
Focal segmental glomerulosclerosis	44.14	20.22	11	2775	1330	50601008
Cerebellar haematoma	39.93	20.22	8	2778	357	50601981
Endometrial ablation	38.26	20.22	9	2777	854	50601484
Red blood cells urine positive	36.22	20.22	11	2775	2764	50599574
White blood cells urine positive	30.81	20.22	11	2775	4567	50597771
Bacterial test	30.74	20.22	8	2778	1149	50601189
Vaginal discharge	29.36	20.22	11	2775	5229	50597109
Hyperaesthesia	27.88	20.22	12	2774	8161	50594177
Urine abnormality	27.50	20.22	11	2775	6227	50596111
Acute kidney injury	25.19	20.22	45	2741	228013	50374325
Cardiogenic shock	23.21	20.22	13	2773	15586	50586752
Organising pneumonia	23.08	20.22	9	2777	4765	50597573
Dorsal ramus syndrome	21.54	20.22	4	2782	119	50602219
Palindromic rheumatism	21.31	20.22	4	2782	126	50602212
Angioedema	20.88	20.22	17	2769	37659	50564679

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	77.44	18.89	16	3271	405	29570835
Bezoar	66.84	18.89	16	3271	803	29570437
Arterial disorder	38.61	18.89	11	3276	1092	29570148
Oesophageal haemorrhage	29.41	18.89	9	3278	1144	29570096
Reading disorder	27.52	18.89	7	3280	451	29570789
Jugular vein distension	25.37	18.89	7	3280	618	29570622
Waist circumference increased	24.09	18.89	7	3280	745	29570495
Body mass index increased	23.39	18.89	7	3280	825	29570415
Bronchial wall thickening	21.77	18.89	7	3280	1045	29570195
Eosinophil count increased	21.05	18.89	12	3275	7357	29563883
Dysgraphia	20.75	18.89	8	3279	2030	29569210
Hypopnoea	20.56	18.89	7	3280	1247	29569993
Wrong product administered	20.40	18.89	10	3277	4521	29566719
Lung opacity	19.85	18.89	7	3280	1385	29569855
Cough	19.21	18.89	43	3244	126684	29444556
Hypotension	19.13	18.89	56	3231	194298	29376942
Chest X-ray abnormal	18.98	18.89	9	3278	3785	29567455

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	71.12	17.88	16	5458	803	64492455
Lactic acidosis	59.54	17.88	46	5428	61364	64431894
Bezoar	55.40	17.88	16	5458	2187	64491071
Reading disorder	39.84	17.88	10	5464	803	64492455
Paranoia	37.48	17.88	21	5453	16331	64476927
Arterial disorder	36.18	17.88	11	5463	1794	64491464
Endometrial ablation	35.05	17.88	9	5465	792	64492466
Hallucination, auditory	34.12	17.88	20	5454	16919	64476339
Cerebellar haematoma	32.58	17.88	8	5466	587	64492671
Hyperkalaemia	31.80	17.88	41	5433	101088	64392170
Psychotic disorder	31.54	17.88	25	5449	34553	64458705
Acute kidney injury	31.09	17.88	96	5378	449144	64044114
Oesophageal haemorrhage	28.98	17.88	9	5465	1575	64491683
Vaginal discharge	27.62	17.88	11	5463	3986	64489272
Bacterial test	26.97	17.88	8	5466	1199	64492059
Red blood cells urine positive	26.41	17.88	11	5463	4467	64488791
Hypoglycaemia	26.02	17.88	35	5439	89857	64403401
Dysgraphia	25.55	17.88	10	5464	3461	64489797
White blood cells urine positive	24.43	17.88	11	5463	5387	64487871
Cardiogenic shock	22.45	17.88	20	5454	32407	64460851
Jugular vein distension	22.05	17.88	7	5467	1315	64491943
Waist circumference increased	21.80	17.88	7	5467	1364	64491894
Urine abnormality	21.19	17.88	11	5463	7351	64485907
Body mass index increased	20.83	17.88	7	5467	1572	64491686
Bronchial wall thickening	19.54	17.88	7	5467	1900	64491358
Cough	19.40	17.88	63	5411	302085	64191173
Libido decreased	19.30	17.88	9	5465	4775	64488483
Coagulopathy	18.82	17.88	18	5456	31902	64461356
Rales	18.31	17.88	13	5461	15216	64478042
Hyperaesthesia	18.03	17.88	11	5463	10003	64483255
Combined pulmonary fibrosis and emphysema	18.03	17.88	3	5471	29	64493229

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
6455	IUPHAR_LIGAND_ID
5746	INN_ID
87679-71-8	SECONDARY_CAS_RN
1T0N3G9CRC	UNII
5464097	PUBCHEM_CID
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
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	65862-165	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	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
Trandolapril	Human Prescription Drug Label	1	71335-1431	TABLET	2 mg	ORAL	ANDA	20 sections