levosalbutamol Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
bronchodilators, phenethylamine derivatives 1575 34391-04-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • xopenex
  • levalbuterol HCl
  • levosalbutamol
  • (-)-Salbutamol
  • (R)-Salbutamol
  • levalbuterol
  • levalbuterol hydrochloride
  • levalbuterol tartrate
The R-isomer of albuterol.
  • Molecular weight: 239.32
  • Formula: C13H21NO3
  • CLOGP: 0.06
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 4
  • TPSA: 72.72
  • ALOGS: -2.05
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 180 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 46 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 2.23 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
March 25, 1999 FDA OAK 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 211.75 13.86 195 14143 91347 46580377
Chronic obstructive pulmonary disease 145.36 13.86 129 14209 57504 46614220
Infective pulmonary exacerbation of cystic fibrosis 117.11 13.86 60 14278 10747 46660977
Dyspnoea 71.73 13.86 330 14008 515218 46156506
Pneumonia 67.93 13.86 261 14077 376059 46295665
Sinusitis 61.48 13.86 128 14210 129640 46542084
Wheezing 57.08 13.86 76 14262 53310 46618414
Bronchitis 54.29 13.86 108 14230 105871 46565853
Cystic fibrosis 50.44 13.86 24 14314 3664 46668060
Product quality issue 44.80 13.86 55 14283 35593 46636131
Cough 42.47 13.86 161 14177 230088 46441636
Rheumatoid arthritis 40.11 13.86 12 14326 240203 46431521
Chest discomfort 38.07 13.86 85 14253 90184 46581540
Anaphylactic reaction 30.69 13.86 57 14281 53055 46618669
Infusion site erythema 29.60 13.86 22 14316 7620 46664104
Toxicity to various agents 28.12 13.86 15 14323 211751 46459973
Respiratory failure 28.06 13.86 78 14260 94738 46576986
Productive cough 25.11 13.86 51 14287 50664 46621060
Chest pain 23.66 13.86 112 14226 176212 46495512
Acute respiratory failure 23.09 13.86 36 14302 29102 46642622
Nasal congestion 22.20 13.86 47 14291 48066 46623658
Pulmonary function test decreased 21.89 13.86 14 14324 3806 46667918
Haemoptysis 21.65 13.86 33 14305 26156 46645568
Drug ineffective 20.71 13.86 123 14215 677715 45994009
Upper respiratory tract infection 20.51 13.86 54 14284 63502 46608222
Administration site swelling 20.39 13.86 9 14329 1156 46670568
Headache 20.25 13.86 230 14108 478122 46193602
Cardiac failure congestive 20.14 13.86 68 14270 91682 46580042
Anxiety 19.81 13.86 109 14229 181848 46489876
Pseudomonas infection 19.10 13.86 19 14319 9739 46661985
Respiratory distress 18.11 13.86 34 14304 31882 46639842
Bronchospasm 17.76 13.86 23 14315 15684 46656040
Maternal exposure during pregnancy 17.32 13.86 5 14333 102544 46569180
Drug intolerance 17.30 13.86 12 14326 147037 46524687
Infusion site swelling 16.87 13.86 14 14324 5685 46666039
Treatment failure 16.74 13.86 4 14334 93083 46578641
Hyperacusis 16.37 13.86 9 14329 1855 46669869
Heart rate increased 16.03 13.86 55 14283 74736 46596988
Dysphonia 15.98 13.86 36 14302 38378 46633346
Poor quality device used 15.32 13.86 9 14329 2103 46669621
Bronchospasm paradoxical 15.28 13.86 4 14334 102 46671622
Enterovirus infection 14.95 13.86 6 14332 608 46671116
Respiratory tract infection 14.66 13.86 30 14308 29942 46641782
Rhinitis allergic 14.54 13.86 14 14324 6894 46664830
Bronchitis chronic 13.95 13.86 11 14327 4156 46667568

FDA Adverse Event Reporting System (Male)

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 95.86 16.96 69 5761 36105 29910543
Infective pulmonary exacerbation of cystic fibrosis 92.07 16.96 41 5789 8531 29938117
Chronic obstructive pulmonary disease 72.92 16.96 65 5765 46061 29900587
Dyspnoea 55.73 16.96 166 5664 333129 29613519
Respiratory distress 37.88 16.96 39 5791 32933 29913715
Cough 37.17 16.96 78 5752 125564 29821084
Pneumonia 36.81 16.96 145 5685 334161 29612487
Upper respiratory tract infection 30.66 16.96 32 5798 27444 29919204
Bronchospasm paradoxical 29.90 16.96 6 5824 72 29946576
Toxic optic neuropathy 29.09 16.96 9 5821 673 29945975
Status asthmaticus 26.01 16.96 7 5823 318 29946330
Respiratory failure 22.53 16.96 56 5774 100586 29846062
Sinusitis 20.95 16.96 29 5801 33316 29913332
Cystic fibrosis 18.56 16.96 9 5821 2265 29944383
Oxygen saturation decreased 17.77 16.96 31 5799 43409 29903239
Product quality issue 17.67 16.96 20 5810 18754 29927894

Pharmacologic Action:

SourceCodeDescription
FDA MoA N0000009922 Adrenergic beta2-Agonists
FDA EPC N0000175779 beta2-Adrenergic Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Bronchospasm indication 4386001
Acute exacerbation of asthma indication 708038006
Bronchospasm Prevention indication
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Ketoacidosis contraindication 56051008
Diabetes mellitus contraindication 73211009 DOID:9351
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Chronic myocardial ischemia contraindication 413844008 DOID:3393

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.07 acidic
pKa2 9.46 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
Beta-2 adrenergic receptor GPCR AGONIST Ki 5.42 CHEMBL CHEMBL

External reference:

IDSource
D02281 KEGG_DRUG
50293-90-8 SECONDARY_CAS_RN
4021157 VANDF
C0772501 UMLSCUI
CHEBI:8746 CHEBI
68H PDB_CHEM_ID
123600 PUBCHEM_CID
CHEMBL1002 ChEMBL_ID
CHEMBL1201061 ChEMBL_ID
CHEMBL3989693 ChEMBL_ID
DB13139 DRUGBANK_ID
D064412 MESH_DESCRIPTOR_UI
9816 IUPHAR_LIGAND_ID
7681 INN_ID
EDN2NBH5SS UNII
237159 RXNORM
14178 MMSL
167701 MMSL
20402 MMSL
8043 MMSL
d04427 MMSL
007763 NDDF
007764 NDDF
010710 NDDF
116090007 SNOMEDCT_US
398965008 SNOMEDCT_US
412236007 SNOMEDCT_US
426604008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0093-4145 SOLUTION 0.31 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0093-4146 SOLUTION 0.63 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0093-4147 SOLUTION, CONCENTRATE 1.25 mg RESPIRATORY (INHALATION) ANDA 26 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0093-4148 SOLUTION 1.25 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0115-9930 SOLUTION 0.31 mg RESPIRATORY (INHALATION) ANDA 31 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0115-9931 SOLUTION 0.63 mg RESPIRATORY (INHALATION) ANDA 31 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0115-9932 SOLUTION 1.25 mg RESPIRATORY (INHALATION) ANDA 31 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0378-6993 SOLUTION, CONCENTRATE 1.25 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0378-9690 SOLUTION 0.31 mg RESPIRATORY (INHALATION) ANDA 28 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0378-9691 SOLUTION 0.63 mg RESPIRATORY (INHALATION) ANDA 28 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 0378-9692 SOLUTION 1.25 mg RESPIRATORY (INHALATION) ANDA 28 sections
Levalbuterol tartrate HFA inhalation HUMAN PRESCRIPTION DRUG LABEL 1 0591-2927 AEROSOL, METERED 45 ug ORAL NDA AUTHORIZED GENERIC 27 sections
Levalbuterol Inhalation Solution Human Prescription Drug Label 1 16714-094 SOLUTION 0.31 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol Inhalation Solution Human Prescription Drug Label 1 16714-095 SOLUTION 0.63 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol Inhalation Solution Human Prescription Drug Label 1 16714-096 SOLUTION 1.25 mg RESPIRATORY (INHALATION) ANDA 27 sections
Xopenex HUMAN PRESCRIPTION DRUG LABEL 1 17478-171 SOLUTION, CONCENTRATE 1.25 mg RESPIRATORY (INHALATION) NDA 27 sections
Xopenex HUMAN PRESCRIPTION DRUG LABEL 1 17478-172 SOLUTION 0.31 mg RESPIRATORY (INHALATION) NDA 27 sections
Xopenex HUMAN PRESCRIPTION DRUG LABEL 1 17478-173 SOLUTION 0.63 mg RESPIRATORY (INHALATION) NDA 27 sections
Xopenex HUMAN PRESCRIPTION DRUG LABEL 1 17478-174 SOLUTION 1.25 mg RESPIRATORY (INHALATION) NDA 27 sections
Xopenex HUMAN PRESCRIPTION DRUG LABEL 1 21695-153 SOLUTION 1.25 mg RESPIRATORY (INHALATION) NDA 24 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 35573-443 SOLUTION 0.31 mg RESPIRATORY (INHALATION) ANDA 18 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 35573-444 SOLUTION 0.63 mg RESPIRATORY (INHALATION) ANDA 18 sections
Levalbuterol HUMAN PRESCRIPTION DRUG LABEL 1 35573-445 SOLUTION 1.25 mg RESPIRATORY (INHALATION) ANDA 18 sections
levalbuterol inhalation HUMAN PRESCRIPTION DRUG LABEL 1 43598-409 SOLUTION 1.25 mg RESPIRATORY (INHALATION) ANDA 27 sections
levalbuterol inhalation HUMAN PRESCRIPTION DRUG LABEL 1 43598-410 SOLUTION 0.63 mg RESPIRATORY (INHALATION) ANDA 27 sections
levalbuterol inhalation HUMAN PRESCRIPTION DRUG LABEL 1 43598-412 SOLUTION 0.31 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol Inhalation Solution Human Prescription Drug Label 1 47335-743 SOLUTION 0.31 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol Inhalation Solution Human Prescription Drug Label 1 47335-746 SOLUTION 0.63 mg RESPIRATORY (INHALATION) ANDA 27 sections
Levalbuterol Inhalation Solution Human Prescription Drug Label 1 47335-753 SOLUTION 1.25 mg RESPIRATORY (INHALATION) ANDA 27 sections
Xopenex HUMAN PRESCRIPTION DRUG LABEL 1 54868-4409 SOLUTION 0.63 mg RESPIRATORY (INHALATION) NDA 14 sections