acrivastine indications/contra

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

Drug dosage:

DoseUnitRoute
24 mg O

Approvals:

DateAgencyCompanyOrphan
March 25, 1994 FDA AUXILIUM PHARMS INC

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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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
CHEBI has role CHEBI:37955 H1-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

Drug Use (View source of the data)

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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 DOID:2883
Retention of urine contraindication 267064002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Hypertensive urgency contraindication 443482000

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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:

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IDSource
4020857 VUID
N0000179060 NUI
C0054340 UMLSCUI
D02760 KEGG_DRUG
4020857 VANDF
391716003 SNOMEDCT_US
N0000179060 NDFRT
N0000148364 NDFRT
d03753 MMSL
4130 MMSL
19959 RXNORM
320813002 SNOMEDCT_US
003921 NDDF
A20F9XAI7W UNII
5548 INN_ID
CHEMBL1224 ChEMBL_ID
5284514 PUBCHEM_CID
C043648 MESH_SUPPLEMENTAL_RECORD_UI
DB09488 DRUGBANK_ID
CHEBI:83168 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
SEMPREX HUMAN PRESCRIPTION DRUG LABEL 2 52244-404 CAPSULE 8 mg ORAL NDA 12 sections