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

Stem definition	Drug id	CAS RN
antihistaminics	82	87848-99-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: BW-270C BW-825C acrivastine semprex	a second generation antihistamine Molecular weight: 348.45 Formula: C22H24N2O2 CLOGP: 1.46 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 53.43 ALOGS: -4.54 ROTB: 6 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

BW-270C
BW-825C
acrivastine
semprex

a second generation antihistamine

Molecular weight: 348.45
Formula: C22H24N2O2
CLOGP: 1.46
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 53.43
ALOGS: -4.54
ROTB: 6

Status: OFM

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

Drug dosage:

Dose	Unit	Route
24	mg	O

ADMET properties:

Show entries

Search:

Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	67 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	18 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.31 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.70 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.16 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Showing 1 to 6 of 6 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
March 25, 1994	FDA	AUXILIUM PHARMS INC

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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
Asthma-chronic obstructive pulmonary disease overlap syndrome	186.43	40.12	35	1914	2026	63485047
Total lung capacity increased	182.44	40.12	35	1914	2275	63484798
Hypomania	173.69	40.12	40	1909	6290	63480783
Jaundice cholestatic	167.88	40.12	40	1909	7284	63479789
Schizophrenia	155.70	40.12	40	1909	9912	63477161
Nasal polyps	148.92	40.12	35	1914	6004	63481069
Sarcoidosis	143.18	40.12	35	1914	7087	63479986
Rhinitis allergic	130.47	40.12	36	1913	11691	63475382
Cardiac murmur	118.40	40.12	35	1914	14517	63472556
Psychotic disorder	118.21	40.12	40	1909	25672	63461401

Showing 1 to 10 of 20 entries

Previous1 2Next

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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
Total lung capacity increased	187.33	35.27	35	2103	2263	79739987
Asthma-chronic obstructive pulmonary disease overlap syndrome	175.53	35.27	35	2103	3186	79739064
Hypomania	172.06	35.27	40	2098	7504	79734746
Jaundice cholestatic	156.05	35.27	40	2098	11244	79731006
Nasal polyps	146.88	35.27	35	2103	7292	79734958
Schizophrenia	143.62	35.27	40	2098	15400	79726850
Sarcoidosis	142.39	35.27	35	2103	8300	79733950
Rhinitis allergic	133.66	35.27	36	2102	12233	79730017
Cardiac murmur	120.15	35.27	35	2103	15789	79726461
Bronchiectasis	108.18	35.27	35	2103	22351	79719899

Showing 1 to 10 of 22 entries

Previous1 2 3Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	R06AX18	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
CHEBI has role	CHEBI:37955	H1 receptor antagonists
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D039563	Histamine H1 Antagonists, Non-Sedating
MeSH PA	D018377	Neurotransmitter Agents

Showing 1 to 9 of 9 entries

Previous1Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Vasomotor rhinitis	indication	8229003	DOID:4730
Allergic rhinitis	indication	61582004
Nasal discharge	indication	64531003
Nasal congestion	indication	68235000
Sneezing	indication	76067001
Common cold	indication	82272006	DOID:10459
Seasonal allergic rhinitis	indication	367498001
Allergic conjunctivitis	indication	473460002	DOID:11204
Hyperthyroidism	contraindication	34486009	DOID:7998
Hypertensive disorder	contraindication	38341003	DOID:10763

Showing 1 to 10 of 16 entries

Previous1 2Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.78	acidic
pKa2	9.42	Basic
pKa3	1.55	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	IC50	7.16	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Histamine H1 receptor	GPCR		HRH1_CAVPO		IC50	5.21	CHEMBL

Showing 1 to 3 of 3 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
003921	NDDF
19959	RXNORM
320813002	SNOMEDCT_US
391716003	SNOMEDCT_US
4020857	VUID
4020857	VANDF
4130	MMSL
5284514	PUBCHEM_CID
5548	INN_ID
A20F9XAI7W	UNII

Showing 1 to 10 of 18 entries

Previous1 2Next

Pharmaceutical products:

None