levosalbutamol ๐Ÿถ Veterinary Use | 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 ยตM/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 190.12 14.26 179 14841 89158 50500946
Infective pulmonary exacerbation of cystic fibrosis 136.92 14.26 60 14960 7849 50582255
Chronic obstructive pulmonary disease 113.40 14.26 107 14913 53328 50536776
Pneumonia 80.87 14.26 271 14749 378130 50211974
Dyspnoea 73.04 14.26 338 14682 547270 50042834
Bronchitis 68.55 14.26 116 14904 104043 50486061
Sinusitis 59.57 14.26 146 14874 170412 50419692
Wheezing 59.02 14.26 82 14938 61965 50528139
Product quality issue 54.63 14.26 56 14964 30802 50559302
Cystic fibrosis 47.21 14.26 21 14999 2843 50587261
Cough 47.18 14.26 168 14852 241096 50349008
Infusion site erythema 43.66 14.26 29 14991 8698 50581406
Chest discomfort 43.11 14.26 89 14931 92633 50497471
Drug ineffective 33.48 14.26 128 14892 819205 49770899
Anaphylactic reaction 32.64 14.26 58 14962 53997 50536107
Infusion site swelling 31.51 14.26 22 14998 7154 50582950
Maternal exposure during pregnancy 31.24 14.26 5 15015 159773 50430331
Respiratory failure 30.66 14.26 77 14943 91104 50499000
Rheumatoid arthritis 30.52 14.26 11 15009 202539 50387565
Pulmonary function test decreased 29.29 14.26 16 15004 3372 50586732
Drug intolerance 28.11 14.26 15 15005 219089 50371015
Upper respiratory tract infection 28 14.26 61 14959 65837 50524267
Treatment failure 27.60 14.26 4 15016 137633 50452471
Anxiety 26.77 14.26 114 14906 177492 50412612
Chest pain 26.25 14.26 113 14907 176769 50413335
Productive cough 26.16 14.26 52 14968 52642 50537462
Joint swelling 25.79 14.26 21 14999 245265 50344839
Nasal congestion 24.84 14.26 50 14970 51070 50539034
Systemic lupus erythematosus 24.14 14.26 6 15014 140616 50449488
Cardiac failure congestive 24.03 14.26 67 14953 84315 50505789
Toxicity to various agents 23.85 14.26 17 15003 212482 50377622
Headache 23.82 14.26 242 14778 506293 50083811
Haemoptysis 23.11 14.26 33 14987 25540 50564564
Acute respiratory failure 22.93 14.26 35 14985 28747 50561357
Bronchospasm paradoxical 21.71 14.26 5 15015 76 50590028
Administration site swelling 21.61 14.26 9 15011 1038 50589066
Wound 21.38 14.26 3 15017 105791 50484313
Pseudomonas infection 20.20 14.26 19 15001 9411 50580693
Respiratory tract infection 20.16 14.26 35 14985 31982 50558122
Respiratory distress 20.08 14.26 34 14986 30455 50559649
Alopecia 20.06 14.26 26 14994 245021 50345083
Product dose omission issue 19.72 14.26 107 14913 183731 50406373
Poor quality device used 19.57 14.26 10 15010 1841 50588263
Bronchospasm 19.41 14.26 23 14997 14831 50575273
Infusion site pain 19.34 14.26 21 14999 12325 50577779
Infusion site extravasation 18.79 14.26 16 15004 6960 50583144
Ear infection 18.49 14.26 30 14990 25940 50564164
Heart rate increased 17.88 14.26 57 14963 77193 50512911
Dysphonia 17.66 14.26 37 14983 38855 50551249
Infusion related reaction 17.21 14.26 15 15005 169542 50420562
Tracheitis 17.06 14.26 7 15013 777 50589327
Hepatic enzyme increased 16.75 14.26 10 15010 137370 50452734
Viral infection 16.60 14.26 31 14989 29955 50560149
Rhinitis allergic 16.37 14.26 15 15005 7185 50582919
Discomfort 16.12 14.26 6 15014 108374 50481730
Migraine 16.03 14.26 54 14966 75226 50514878
Pulmonary embolism 15.86 14.26 66 14954 101638 50488466
Bronchitis chronic 14.99 14.26 11 15009 3866 50586238
Off label use 14.59 14.26 82 14938 474344 50115760

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
Infective pulmonary exacerbation of cystic fibrosis 105.17 17.98 41 5643 6195 29562648
Asthma 75.63 17.98 58 5626 33791 29535052
Dyspnoea 50.46 17.98 157 5527 326575 29242268
Chronic obstructive pulmonary disease 48.62 17.98 49 5635 40906 29527937
Pneumonia 39.71 17.98 143 5541 320029 29248814
Respiratory distress 35.53 17.98 37 5647 32069 29536774
Cough 35.08 17.98 76 5608 126651 29442192
Upper respiratory tract infection 32.95 17.98 33 5651 27316 29541527
Toxic optic neuropathy 32.67 17.98 10 5674 731 29568112
Sinusitis 28.40 17.98 34 5650 34316 29534527
Status asthmaticus 26.84 17.98 7 5677 285 29568558
Cystic fibrosis 22.31 17.98 9 5675 1483 29567360
Pulmonary function test decreased 21.31 17.98 12 5672 4151 29564692
Respiratory failure 21.08 17.98 53 5631 97078 29471765
Product quality issue 20.66 17.98 20 5664 15875 29552968
Bronchospasm paradoxical 19.28 17.98 4 5680 58 29568785
Toxicity to various agents 18.96 17.98 5 5679 173656 29395187

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
Infective pulmonary exacerbation of cystic fibrosis 186.89 14.33 78 14755 11718 64472181
Asthma 138.39 14.33 138 14695 95087 64388812
Chronic obstructive pulmonary disease 122.18 14.33 113 14720 70935 64412964
Dyspnoea 90.82 14.33 365 14468 718309 63765590
Product quality issue 66.48 14.33 55 14778 29744 64454155
Cystic fibrosis 65.66 14.33 26 14807 3408 64480491
Pneumonia 64.79 14.33 277 14556 559299 63924600
Cough 58.38 14.33 177 14656 301971 64181928
Bronchitis 51.70 14.33 91 14742 108652 64375247
Wheezing 48.49 14.33 75 14758 80504 64403395
Respiratory distress 45.32 14.33 58 14775 52273 64431626
Toxicity to various agents 41.30 14.33 16 14817 363497 64120402
Pulmonary function test decreased 36.12 14.33 21 14812 6440 64477459
Acute respiratory failure 35.09 14.33 50 14783 49884 64434015
Chest discomfort 32.41 14.33 78 14755 116028 64367871
Toxic optic neuropathy 32.37 14.33 11 14822 936 64482963
Respiratory failure 31.59 14.33 95 14738 161088 64322811
Bronchospasm paradoxical 30.27 14.33 7 14826 142 64483757
Status asthmaticus 28.28 14.33 10 14823 958 64482941
Infusion site erythema 27.38 14.33 18 14815 6855 64477044
Bronchospasm 27.06 14.33 29 14804 21653 64462246
Respiratory syncytial virus infection 26.46 14.33 18 14815 7250 64476649
Product dose omission issue 26.03 14.33 101 14732 194646 64289253
Nasal congestion 25.87 14.33 48 14785 59610 64424289
Tracheitis 25.48 14.33 10 14823 1280 64482619
Chest pain 22.81 14.33 111 14722 235869 64248030
Headache 22.75 14.33 203 14630 529264 63954635
Upper respiratory tract infection 22.60 14.33 51 14782 72734 64411165
Poor quality device used 21.22 14.33 10 14823 1997 64481902
Sinusitis 20.57 14.33 77 14756 145851 64338048
Pulmonary hypertension 20.34 14.33 36 14797 43103 64440796
Drug interaction 19.81 14.33 33 14800 362050 64121849
Anxiety 19.34 14.33 95 14738 202554 64281345
Infusion site swelling 18.63 14.33 13 14820 5452 64478447
Hypoxia 18.24 14.33 53 14780 88096 64395803
Heart rate increased 18.23 14.33 57 14776 98618 64385281
Viral infection 18.14 14.33 31 14802 36109 64447790
Enterovirus infection 17.72 14.33 8 14825 1449 64482450
Rheumatoid arthritis 17.39 14.33 8 14825 164286 64319613
Pseudomonas infection 17.36 14.33 21 14812 17862 64466037
Hospitalisation 17.31 14.33 47 14786 75160 64408739
Haemoptysis 17.08 14.33 36 14797 49012 64434887
Anhedonia 16.52 14.33 18 14815 13688 64470211
Off label use 16.05 14.33 83 14750 632723 63851176
Carbon dioxide increased 15.35 14.33 8 14825 1981 64481918
Dysphonia 14.95 14.33 33 14800 46349 64437550
Supraventricular tachycardia 14.88 14.33 20 14813 18887 64465012
Therapeutic product effect incomplete 14.60 14.33 3 14830 103479 64380420
Joint swelling 14.39 14.33 17 14816 215365 64268534

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Drug Use | Suggest Off label Use Form| |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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.045MG BASE/INH XOPENEX HFA SUNOVION N021730 March 11, 2005 RX AEROSOL, METERED INHALATION 7256310 Oct. 8, 2024 TREATMENT OR PREVENTION OF BRONCHOSPASM OR ASTHMATIC SYMPTOMS

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
661464-94-4 SECONDARY_CAS_RN
4021157 VANDF
C0772501 UMLSCUI
CHEBI:8746 CHEBI
68H PDB_CHEM_ID
CHEMBL1002 ChEMBL_ID
DB13139 DRUGBANK_ID
CHEMBL1201061 ChEMBL_ID
CHEMBL3989693 ChEMBL_ID
123600 PUBCHEM_CID
9816 IUPHAR_LIGAND_ID
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
D064412 MESH_DESCRIPTOR_UI
7681 INN_ID
EDN2NBH5SS UNII

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