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

Stem definitionDrug idCAS RN
antihistaminics 82 87848-99-5

Description:

MoleculeDescription

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:

DoseUnitRoute
24 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.70 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 67 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.31 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 18 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
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

Approvals:

DateAgencyCompanyOrphan
March 25, 1994 FDA AUXILIUM PHARMS INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Bronchiectasis 114.81 40.12 35 1914 16107 63470966
Hepatotoxicity 103.94 40.12 40 1909 37001 63450072
Blood bilirubin increased 103.84 40.12 40 1909 37100 63449973
Cholelithiasis 97.33 40.12 40 1909 43885 63443188
Lung neoplasm malignant 88.05 40.12 30 1919 19603 63467470
Chronic obstructive pulmonary disease 77.62 40.12 38 1911 62648 63424425
Wheezing 57.47 40.12 36 1913 95559 63391514
Gastrooesophageal reflux disease 57.45 40.12 36 1913 95603 63391470
Condition aggravated 56.03 40.12 65 1884 402152 63084921
Hepatic enzyme increased 52.73 40.12 46 1903 202282 63284791

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Psychotic disorder 104.85 35.27 40 2098 41362 79700888
Hepatotoxicity 96.49 35.27 40 2098 51312 79690938
Cholelithiasis 95.52 35.27 40 2098 52624 79689626
Blood bilirubin increased 86.71 35.27 40 2098 66192 79676058
Lung neoplasm malignant 81.81 35.27 30 2108 27762 79714488
Chronic obstructive pulmonary disease 71.33 35.27 38 2100 85381 79656869
Hepatic enzyme increased 62.35 35.27 46 2092 182564 79559686
Gastrooesophageal reflux disease 61.65 35.27 37 2101 104209 79638041
Wheezing 57.81 35.27 37 2101 116627 79625623
Condition aggravated 46.81 35.27 62 2076 501062 79241188
Pharyngeal paraesthesia 44.28 35.27 11 2127 2710 79739540
Spleen congestion 37.51 35.27 7 2131 447 79741803

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AX18 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
FDA MoA N0000000190 Histamine H1 Receptor Antagonists
FDA EPC N0000175587 Histamine-1 Receptor Antagonist
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
CHEBI has role CHEBI:37955 H1 receptor antagonists

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

DiseaseRelationSNOMED_IDDOID
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
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Diabetes mellitus contraindication 73211009 DOID:9351
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Hypertensive urgency contraindication 443482000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST IC50 7.16 WOMBAT-PK CHEMBL
Multidrug resistance protein 1 Transporter WOMBAT-PK
Histamine H1 receptor GPCR IC50 5.21 CHEMBL

External reference:

IDSource
4020857 VUID
N0000179060 NUI
D02760 KEGG_DRUG
19959 RXNORM
C0054340 UMLSCUI
CHEBI:83168 CHEBI
CHEMBL1224 ChEMBL_ID
DB09488 DRUGBANK_ID
C043648 MESH_SUPPLEMENTAL_RECORD_UI
5284514 PUBCHEM_CID
5548 INN_ID
A20F9XAI7W UNII
320813002 SNOMEDCT_US
391716003 SNOMEDCT_US
4020857 VANDF
4130 MMSL
d03753 MMSL
003921 NDDF

Pharmaceutical products:

None