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

Stem definition	Drug id	CAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic)	2583	144701-48-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: telmisartan tolura micardis pritor	A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION. Molecular weight: 514.63 Formula: C33H30N4O2 CLOGP: 7.29 LIPINSKI: 2 HAC: 6 HDO: 1 TPSA: 72.94 ALOGS: -5.17 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

telmisartan
tolura
micardis
pritor

A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.

Molecular weight: 514.63
Formula: C33H30N4O2
CLOGP: 7.29
LIPINSKI: 2
HAC: 6
HDO: 1
TPSA: 72.94
ALOGS: -5.17
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
40	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	8.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	5.30 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	20 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.22 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Nov. 10, 1998	FDA	BOEHRINGER INGELHEIM
Nov. 12, 1998	EMA	KRKA, D.D., NOVO MESTO

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
Hyponatraemia	186.88	10.62	303	43928	111597	63333194
Blood pressure increased	117.47	10.62	311	43920	161751	63283040
Pemphigus	103.80	10.62	6	44225	183720	63261071
Alopecia	86.90	10.62	65	44166	337471	63107320
Hypertensive crisis	86.03	10.62	77	44154	15209	63429582
Bradycardia	85.80	10.62	170	44061	73057	63371734
Maternal exposure during pregnancy	79.60	10.62	27	44204	220035	63224756
Blood pressure systolic increased	75.85	10.62	126	44105	47271	63397520
Renal impairment	71.66	10.62	177	44054	88178	63356613
Glossodynia	68.15	10.62	20	44211	178856	63265935

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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
Cerebral infarction	110.66	11.63	124	28427	27331	34901049
Interstitial lung disease	90.17	11.63	178	28373	65104	34863276
Pericardial disease	60.31	11.63	20	28531	430	34927950
Cardiac failure	59.78	11.63	187	28364	91061	34837319
Death	58.07	11.63	152	28399	397897	34530483
Hepatic function abnormal	57.67	11.63	118	28433	44245	34884135
Pulmonary valve disease	57.22	11.63	18	28533	325	34928055
Hyperkalaemia	55.79	11.63	153	28398	69236	34859144
Completed suicide	53.83	11.63	8	28543	98160	34830220
Altered state of consciousness	50.74	11.63	77	28474	22816	34905564

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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
Cerebral infarction	153.84	10.19	184	62043	45492	79636669
Hyponatraemia	151.22	10.19	389	61838	177459	79504702
Completed suicide	118.13	10.19	24	62203	245743	79436418
Blood pressure increased	114.46	10.19	394	61833	210966	79471195
Hepatic function abnormal	91.01	10.19	186	62041	72921	79609240
Death	85.52	10.19	198	62029	566316	79115845
Altered state of consciousness	83.29	10.19	134	62093	43688	79638473
Interstitial lung disease	83.24	10.19	234	61993	112366	79569795
Hypertensive crisis	82.26	10.19	91	62136	20679	79661482
Hyperkalaemia	80.94	10.19	234	61993	114164	79567997

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FDA Adverse Event Reporting System (Pediatric)

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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
Renal vein thrombosis	23.65	20.13	3	11	0	89778

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Pharmacologic Action:

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Source	Code	Description
ATC	C09CA07	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain
ATC	C09DA07	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and diuretics
ATC	C09DB04	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and calcium channel blockers
ATC	C09DX08	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs), other combinations
CHEBI has role	CHEBI:35457	ACE inhibitor
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:61016	angiotensin receptor antagonists
CHEBI has role	CHEBI:78298	environmental contaminants
FDA EPC	N0000175561	Angiotensin 2 Receptor Blocker

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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
Cerebrovascular accident	indication	230690007
Disorder due to type 2 diabetes mellitus	indication	422014003
History of myocardial infarction due to atherothrombotic coronary artery disease	indication	387786000000000000
Myocardial Infarction Prevention	indication
Chronic heart failure	off-label use	48447003
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

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🐶 Veterinary Drug Use

Species	Use	Relation
Cats	Systemic hypertension	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Semintra	Boehringer lngelheim Animal Health USA Inc.	1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.65	acidic
pKa2	5.79	Basic
pKa3	5.13	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])	Bioact source	MoA source
Type-1 angiotensin II receptor	GPCR	P30556	AGTR1_HUMAN	ANTAGONIST	IC50	9.31	CHEMBL	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.77	CHEMBL
Glycine receptor subunit alpha-1	Ion channel	P23415	GLRA1_HUMAN		EC50	5.49	CHEMBL
Peroxisome proliferator-activated receptor gamma	Nuclear hormone receptor	P37231	PPARG_HUMAN		EC50	5.82	CHEMBL
Type-2 angiotensin II receptor	GPCR	P50052	AGTR2_HUMAN		IC50	9.48	CHEMBL
Angiotensin-converting enzyme	Enzyme	P12821	ACE_HUMAN		Ki	5.22	CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	4.75	CHEMBL
Type-1B angiotensin II receptor	GPCR		AGTRB_RAT		IC50	8.52	CHEMBL
Type-1A angiotensin II receptor	GPCR		AGTRA_RAT		Ki	9.64	CHEMBL

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External reference:

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ID	Source
TLS	PDB_CHEM_ID
007683	NDDF
129487008	SNOMEDCT_US
13913	MMSL
218353	RXNORM
387069000	SNOMEDCT_US
4021146	VUID
4021146	VANDF
53287	MMSL
592	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Micardis	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0039	TABLET	20 mg	ORAL	NDA	26 sections
Micardis	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0039	TABLET	20 mg	ORAL	NDA	26 sections
Micardis	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0040	TABLET	40 mg	ORAL	NDA	26 sections
Micardis	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0040	TABLET	40 mg	ORAL	NDA	26 sections
Micardis	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0041	TABLET	80 mg	ORAL	NDA	26 sections
Micardis	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0041	TABLET	80 mg	ORAL	NDA	26 sections
Micardis HCT	HUMAN PRESCRIPTION DRUG LABEL	2	0597-0042	TABLET	80 mg	ORAL	NDA	30 sections
Micardis HCT	HUMAN PRESCRIPTION DRUG LABEL	2	0597-0042	TABLET	80 mg	ORAL	NDA	30 sections
Micardis HCT	HUMAN PRESCRIPTION DRUG LABEL	2	0597-0043	TABLET	40 mg	ORAL	NDA	30 sections
Micardis HCT	HUMAN PRESCRIPTION DRUG LABEL	2	0597-0043	TABLET	40 mg	ORAL	NDA	30 sections

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