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

Stem definition	Drug id	CAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic)	1985	144689-63-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: olmesartan medoxomil olmetec CS-866 CS866	Olmesartan blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle. Molecular weight: 558.60 Formula: C29H30N6O6 CLOGP: 3.54 LIPINSKI: 2 HAC: 12 HDO: 2 TPSA: 154.34 ALOGS: -4.88 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

olmesartan medoxomil
olmetec
CS-866
CS866

Olmesartan blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle.

Molecular weight: 558.60
Formula: C29H30N6O6
CLOGP: 3.54
LIPINSKI: 2
HAC: 12
HDO: 2
TPSA: 154.34
ALOGS: -4.88
ROTB: 11

Status: OFP

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

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	26 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	2 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.02 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
April 25, 2002	FDA	DAIICHI SANKYO

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
Sprue-like enteropathy	661.67	11.25	137	34437	606	63453842
Malabsorption	385.47	11.25	126	34448	3946	63450502
Intestinal villi atrophy	153.85	11.25	34	34540	216	63454232
Colitis microscopic	116.07	11.25	69	34505	9270	63445178
Hyperkalaemia	93.89	11.25	131	34443	54072	63400376
Dehydration	83.39	11.25	245	34329	173109	63281339
Acute kidney injury	81.46	11.25	321	34253	263094	63191354
Hyponatraemia	76.10	11.25	180	34394	111720	63342728
Renal failure	75.45	11.25	185	34389	117467	63336981
Systemic lupus erythematosus	74.93	11.25	12	34562	208906	63245542

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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
Sprue-like enteropathy	473.73	11.63	101	23278	412	34933140
Malabsorption	341.23	11.63	106	23273	2266	34931286
Gastrointestinal disorder	102.70	11.63	120	23259	33828	34899724
Intestinal villi atrophy	80.24	11.63	19	23360	135	34933417
Colitis microscopic	75.39	11.63	35	23344	2302	34931250
Renal impairment	64.65	11.63	173	23206	94340	34839212
Death	60.42	11.63	109	23270	397940	34535612
Coeliac disease	50.81	11.63	19	23360	721	34932831
Toxicity to various agents	48.31	11.63	38	23341	200324	34733228
Off label use	48.01	11.63	134	23245	419390	34514162

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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
Sprue-like enteropathy	1095.69	10.74	233	47091	1085	79695979
Malabsorption	557.03	10.74	179	47145	4853	79692211
Intestinal villi atrophy	225.52	10.74	53	47271	416	79696648
Colitis microscopic	184.28	10.74	101	47223	10667	79686397
Hyperkalaemia	121.27	10.74	232	47092	114166	79582898
Renal impairment	110.96	10.74	271	47053	157512	79539552
Dehydration	105.05	10.74	355	46969	247832	79449232
Diarrhoea	104.72	10.74	884	46440	879605	78817459
Gastrointestinal disorder	90.30	10.74	214	47110	121991	79575073
Off label use	84.92	10.74	267	47057	906948	78790116

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C09CA08	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain
ATC	C09DA08	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and diuretics
ATC	C09DB02	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	C09DX03	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:35674	antihypertensive drugs
CHEBI has role	CHEBI:61016	angiotensin receptor antagonists
FDA EPC	N0000175561	Angiotensin 2 Receptor Blocker
FDA MoA	N0000000070	Angiotensin 2 Receptor Antagonists
MeSH PA	D047228	Angiotensin II Type 1 Receptor Blockers
MeSH PA	D057911	Angiotensin Receptor Antagonists

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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	off-label use	48447003
Atrial fibrillation	off-label use	49436004	DOID:0060224
Diastolic heart failure	off-label use	418304008	DOID:9775
Nondiabetic Proteinuric Nephropathy	off-label use
Anuria	contraindication	2472002	DOID:2983
Hypercholesterolemia	contraindication	13644009
Hyperkalemia	contraindication	14140009
Secondary angle-closure glaucoma	contraindication	21571006
Hypovolemia	contraindication	28560003

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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	4.25	acidic
pKa2	5.76	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
Type-1 angiotensin II receptor	GPCR	P30556	AGTR1_HUMAN	ANTAGONIST	IC50	8.10		IUPHAR	CHEMBL
Type-1 angiotensin II receptor	GPCR		AGTR1_BOVIN		IC50	8.09		CHEMBL

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External reference:

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ID	Source
OLM	PDB_CHEM_ID
009634	NDDF
009635	NDDF
118463	RXNORM
130881	PUBCHEM_CID
144689-24-7	SECONDARY_CAS_RN
158781	PUBCHEM_CID
16642	MMSL
245076	MMSL
385540001	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Azor	HUMAN PRESCRIPTION DRUG LABEL	2	0713-0870	TABLET, FILM COATED	20 mg	ORAL	NDA	26 sections
Azor	HUMAN PRESCRIPTION DRUG LABEL	2	0713-0870	TABLET, FILM COATED	20 mg	ORAL	NDA	26 sections
Benicar	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0860	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
Benicar	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0860	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
Benicar	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0861	TABLET, FILM COATED	20 mg	ORAL	NDA	32 sections
Benicar	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0861	TABLET, FILM COATED	20 mg	ORAL	NDA	32 sections
Benicar	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0862	TABLET, FILM COATED	40 mg	ORAL	NDA	32 sections
Benicar	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0862	TABLET, FILM COATED	40 mg	ORAL	NDA	32 sections
Benicar HCT	HUMAN PRESCRIPTION DRUG LABEL	2	0713-0863	TABLET, FILM COATED	20 mg	ORAL	NDA	26 sections
Benicar HCT	HUMAN PRESCRIPTION DRUG LABEL	2	0713-0863	TABLET, FILM COATED	20 mg	ORAL	NDA	26 sections

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