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 222.92 13.04 221 17138 127340 63344323
Infective pulmonary exacerbation of cystic fibrosis 141.84 13.04 62 17297 8755 63462908
Chronic obstructive pulmonary disease 121.32 13.04 115 17244 62571 63409092
Pneumonia 94.98 13.04 307 17052 456460 63015203
Bronchitis 89.15 13.04 138 17221 124797 63346866
Dyspnoea 78.99 13.04 373 16986 660940 62810723
Sinusitis 78.64 13.04 184 17175 226469 63245194
Infusion site erythema 54.43 13.04 36 17323 11643 63460020
Product quality issue 51.44 13.04 56 17303 35809 63435854
Cystic fibrosis 49.21 13.04 22 17337 3274 63468389
Cough 48.68 13.04 183 17176 292560 63179103
Wheezing 45.08 13.04 88 17271 95507 63376156
Drug intolerance 43.62 13.04 15 17344 308646 63163017
Chest discomfort 43.33 13.04 94 17265 109875 63361788
Drug ineffective 42.92 13.04 145 17214 1044620 62427043
Maternal exposure during pregnancy 42.82 13.04 5 17354 220057 63251606
Upper respiratory tract infection 41.72 13.04 78 17281 81969 63389694
Treatment failure 37.56 13.04 5 17354 199038 63272625
Infusion site swelling 35.85 13.04 26 17333 9744 63461919
Ear infection 35.68 13.04 48 17311 38165 63433498
Systemic lupus erythematosus 35.50 13.04 7 17352 208911 63262752
Rheumatoid arthritis 34.72 13.04 13 17346 253806 63217857
Joint swelling 34.10 13.04 24 17335 327642 63144021
Wound 33.59 13.04 3 17356 163260 63308403
Product dose omission issue 32.89 13.04 139 17220 234174 63237489
Infusion site pain 32.70 13.04 31 17328 16838 63454825
Anaphylactic reaction 32.56 13.04 62 17297 66038 63405625
Productive cough 32.02 13.04 60 17299 63148 63408515
Respiratory tract infection 31.20 13.04 47 17312 41436 63430227
Pulmonary function test decreased 30.96 13.04 17 17342 3930 63467733
Respiratory failure 29.23 13.04 77 17282 101781 63369882
Cardiac failure congestive 28.72 13.04 72 17287 92361 63379302
Alopecia 28.69 13.04 30 17329 337506 63134157
Hepatic enzyme increased 26.61 13.04 11 17348 202317 63269346
Pericarditis 25.56 13.04 3 17356 131576 63340087
Chest pain 24.97 13.04 121 17238 215838 63255825
Pseudomonas infection 24.43 13.04 22 17337 11191 63460472
Acute respiratory failure 24.42 13.04 38 17321 34447 63437216
Discomfort 23.85 13.04 8 17351 167366 63304297
Infusion site extravasation 23.80 13.04 21 17338 10405 63461258
Haemoptysis 23.70 13.04 34 17325 28692 63442971
Nasal congestion 23.46 13.04 54 17305 65606 63406057
Anxiety 23.11 13.04 119 17240 217422 63254241
Headache 22.49 13.04 268 17091 632973 62838690
Respiratory distress 22.10 13.04 36 17323 33915 63437748
Bronchospasm paradoxical 21.17 13.04 5 17354 93 63471570
Off label use 21.03 13.04 104 17255 674358 62797305
Viral infection 20.79 13.04 36 17323 35627 63436036
Impaired quality of life 20.59 13.04 22 17337 13761 63457902
Administration site swelling 20.40 13.04 9 17350 1298 63470365
Bronchospasm 19.74 13.04 24 17335 17256 63454407
Therapeutic product effect incomplete 19.60 13.04 5 17354 125051 63346612
Infusion related reaction 19.55 13.04 23 17336 245498 63226165
Poor quality device used 19.28 13.04 10 17349 2061 63469602
Migraine 19.15 13.04 67 17292 103279 63368384
Therapeutic product effect decreased 18.98 13.04 15 17344 193172 63278491
Arthropathy 18.69 13.04 22 17337 234770 63236893
Tracheitis 17.42 13.04 7 17352 800 63470863
Heart rate increased 17.37 13.04 61 17298 94177 63377486
Pulmonary embolism 16.95 13.04 70 17289 116614 63355049
Dysphonia 15.74 13.04 38 17321 47576 63424087
Musculoskeletal stiffness 15.01 13.04 17 17342 184601 63287062
Supraventricular tachycardia 14.99 13.04 19 17340 14252 63457411
Hospitalisation 14.77 13.04 54 17305 85027 63386636
Febrile neutropenia 14.68 13.04 7 17352 118442 63353221
Bronchitis chronic 14.66 13.04 11 17348 4342 63467321
Neutropenia 14.35 13.04 16 17343 174989 63296674
Infusion site rash 14.04 13.04 8 17351 1986 63469677
Pharyngeal oedema 13.99 13.04 18 17341 13703 63457960
General physical health deterioration 13.86 13.04 21 17338 201381 63270282
Hyperacusis 13.60 13.04 8 17351 2105 63469558
COVID-19 13.51 13.04 64 17295 113039 63358624
Infusion site pruritus 13.46 13.04 12 17347 6023 63465640
Status asthmaticus 13.39 13.04 6 17353 898 63470765
Candida infection 13.23 13.04 26 17333 28325 63443338

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 114.53 17.06 44 6314 6757 34943816
Asthma 89.84 17.06 69 6289 42587 34907986
Dyspnoea 56.61 17.06 173 6185 376609 34573964
Chronic obstructive pulmonary disease 50.63 17.06 53 6305 48865 34901708
Pneumonia 46.66 17.06 158 6200 362469 34588104
Cough 37.95 17.06 84 6274 150056 34800517
Sinusitis 37.81 17.06 42 6316 41360 34909213
Respiratory distress 35.74 17.06 38 6320 35627 34914946
Upper respiratory tract infection 32.73 17.06 35 6323 33024 34917549
Toxic optic neuropathy 31.86 17.06 10 6348 840 34949733
Status asthmaticus 26.27 17.06 7 6351 328 34950245
Cystic fibrosis 21.87 17.06 9 6349 1649 34948924
Product quality issue 20.42 17.06 20 6338 17015 34933558
Respiratory failure 20.16 17.06 54 6304 108518 34842055
Pulmonary function test decreased 19.93 17.06 12 6346 4963 34945610
Toxicity to various agents 19.69 17.06 6 6352 200356 34750217
Bronchospasm paradoxical 19.50 17.06 4 6354 58 34950515
Ear infection 18.18 17.06 15 6343 10216 34940357

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 185.99 13.96 78 16951 12773 79714586
Asthma 169.95 13.96 175 16854 134920 79592439
Chronic obstructive pulmonary disease 128.40 13.96 122 16907 85297 79642062
Dyspnoea 97.18 13.96 400 16629 856625 78870734
Pneumonia 83.39 13.96 319 16710 659927 79067432
Bronchitis 70.39 13.96 111 16918 130533 79596826
Cystic fibrosis 67.91 13.96 27 17002 3853 79723506
Product quality issue 63.78 13.96 55 16974 33885 79693474
Cough 63.44 13.96 197 16832 366592 79360767
Respiratory distress 46.84 13.96 60 16969 58279 79669080
Acute respiratory failure 39.80 13.96 56 16973 59485 79667874
Wheezing 38.33 13.96 80 16949 116584 79610775
Product dose omission issue 38.23 13.96 128 16901 247409 79479950
Sinusitis 37.49 13.96 109 16920 195392 79531967
Infusion site erythema 37.43 13.96 24 17005 9436 79717923
Pulmonary function test decreased 36.89 13.96 22 17007 7615 79719744
Upper respiratory tract infection 32.89 13.96 65 16964 91103 79636256
Chest discomfort 31.45 13.96 82 16947 137962 79589397
Toxic optic neuropathy 31.04 13.96 11 17018 1142 79726217
Respiratory failure 30.11 13.96 96 16933 180815 79546544
Bronchospasm paradoxical 29.87 13.96 7 17022 163 79727196
Infusion site swelling 28.87 13.96 19 17010 7807 79719552
Status asthmaticus 28.35 13.96 10 17019 1024 79726335
Respiratory syncytial virus infection 27.99 13.96 20 17009 9382 79717977
Bronchospasm 27.28 13.96 30 16999 24829 79702530
Treatment failure 25.95 13.96 3 17026 170483 79556876
Tracheitis 25.92 13.96 10 17019 1318 79726041
Toxicity to various agents 25.02 13.96 32 16997 421508 79305851
Impaired quality of life 24.39 13.96 22 17007 14364 79712995
Headache 24.17 13.96 229 16800 653543 79073816
Viral infection 23.76 13.96 37 16992 42979 79684380
Off label use 23.43 13.96 107 16922 907108 78820251
Nasal congestion 23.41 13.96 51 16978 76501 79650858
Infusion site pain 22.71 13.96 21 17008 14155 79713204
Synovitis 22.10 13.96 3 17026 150731 79576628
Drug intolerance 21.59 13.96 15 17014 264104 79463255
Pseudomonas infection 20.85 13.96 24 17005 20879 79706480
Poor quality device used 20.69 13.96 10 17019 2275 79725084
Chest pain 20.30 13.96 116 16913 282188 79445171
Drug abuse 20.08 13.96 5 17024 162686 79564673
Hospitalisation 19.46 13.96 54 16975 94182 79633177
Pulmonary hypertension 19.45 13.96 36 16993 48044 79679315
Hypoxia 19.23 13.96 57 16972 103186 79624173
Respiratory tract infection 19.13 13.96 36 16993 48653 79678706
Drug interaction 18.54 13.96 38 16991 415145 79312214
Rheumatoid arthritis 18.17 13.96 11 17018 208459 79518900
Joint swelling 18.08 13.96 21 17008 288625 79438734
Haemoptysis 17.91 13.96 38 16991 55961 79671398
Heart rate increased 17.35 13.96 61 16968 120663 79606696
Hepatic enzyme increased 16.83 13.96 9 17020 182601 79544758
Ear infection 16.81 13.96 28 17001 34404 79692955
Anhedonia 16.38 13.96 18 17011 14880 79712479
Anaphylactic reaction 16.32 13.96 47 16982 83696 79643663
Enterovirus infection 16.07 13.96 8 17021 1939 79725420
Drug ineffective 15.93 13.96 151 16878 1080762 78646597
Anxiety 15.86 13.96 99 16930 248413 79478946
Supraventricular tachycardia 15.70 13.96 21 17008 21249 79706110
Pancytopenia 15.52 13.96 8 17021 165737 79561622
Chronic respiratory failure 15.36 13.96 9 17020 3013 79724346
Carbon dioxide increased 15.02 13.96 8 17021 2232 79725127
Neutropenia 14.92 13.96 24 17005 287686 79439673
Productive cough 14.80 13.96 47 16982 88284 79639075
Intentional product use issue 14.76 13.96 7 17022 152105 79575254
Therapeutic product effect incomplete 14.56 13.96 6 17023 141639 79585720
Migraine 14.15 13.96 46 16983 87447 79639912
Cardiac failure congestive 14.07 13.96 64 16965 142338 79585021

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 LUPIN 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 0093-4147 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 0115-9930 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 0115-9931 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 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 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 16714-094 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 16714-095 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
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 17478-171 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 17478-172 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 17478-173 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