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:

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

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Approvals:

Date	Agency	Company	Orphan
April 26, 1996	FDA	ABBVIE

FDA Adverse Event Reporting System (Female)

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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

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FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
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
FDA EPC	N0000175562	Angiotensin Converting Enzyme Inhibitor
FDA MoA	N0000000181	Angiotensin-converting Enzyme Inhibitors
MeSH PA	D000806	Angiotensin-Converting Enzyme Inhibitors

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

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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

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🐶 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:

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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

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External reference:

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ID	Source
X93	PDB_CHEM_ID
004452	NDDF
107488	MMSL
108562001	SNOMEDCT_US
1546379	RXNORM
1T0N3G9CRC	UNII
386871006	SNOMEDCT_US
4020971	VUID
4020971	VANDF
5448	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	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
Trandolapril	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6061	TABLET	4 mg	ORAL	ANDA	14 sections

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