salbutamol indications/contra

Stem definitionDrug idCAS RN
bronchodilators, phenethylamine derivatives 105 18559-94-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • salbutamol
  • albuterol
  • sabumol
  • dl-Albuterol
  • dl-Salbutamol
  • albuterol sulfate
A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.
  • Molecular weight: 239.32
  • Formula: C13H21NO3
  • CLOGP: 0.06
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 4
  • TPSA: 72.72
  • ALOGS: -2.05
  • ROTB: 5

Drug dosage:

DoseUnitRoute
0.80 mg Inhal.aerosol
0.80 mg Inhal.powder
10 mg Inhal.solution
12 mg O
12 mg P

Approvals:

DateAgencyCompanyOrphan
May 1, 1981 FDA SCHERING

FDA Adverse Event Reporting System

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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
Drug ineffective 2138.63 28.74 800 3678 115290 3266091
Asthma 1874.89 28.74 441 4037 11961 3369420
Dyspnoea 1345.64 28.74 558 3920 102376 3279005
Product quality issue 1069.58 28.74 334 4144 26401 3354980
Wheezing 603.53 28.74 165 4313 8006 3373375
Cough 502.60 28.74 213 4265 39645 3341736
Chronic obstructive pulmonary disease 494.35 28.74 151 4327 10858 3370523
Lactic acidosis 437.38 28.74 126 4352 7374 3374007
Tachycardia 362.02 28.74 145 4333 23226 3358155
Device malfunction 318.64 28.74 88 4390 4396 3376985
Condition aggravated 301.84 28.74 149 4329 39084 3342297
Lower respiratory tract infection 279.91 28.74 87 4391 6582 3374799
Device use error 267.06 28.74 56 4422 840 3380541
Drug hypersensitivity 260.93 28.74 131 4347 35549 3345832
Pneumonia 253.05 28.74 162 4316 69981 3311400
Stress cardiomyopathy 219.48 28.74 52 4426 1390 3379991
Heart rate increased 217.38 28.74 88 4390 14398 3366983
Tremor 213.43 28.74 106 4372 28038 3353343
Chest discomfort 189.38 28.74 84 4394 17201 3364180
Palpitations 187.69 28.74 86 4392 18997 3362384
Tachypnoea 177.28 28.74 53 4425 3503 3377878
Respiratory failure 171.89 28.74 86 4392 23055 3358326
Hypokalaemia 167.13 28.74 72 4406 13733 3367648
Drug effect decreased 166.81 28.74 69 4409 11900 3369481
Bronchospasm paradoxical 165.44 28.74 26 4452 58 3381323
Chest pain 157.18 28.74 98 4380 40177 3341204
Oxygen saturation decreased 157.12 28.74 63 4415 10028 3371353
Malaise 155.57 28.74 117 4361 65060 3316321
Exposure during pregnancy 154.94 28.74 85 4393 27478 3353903
Medication error 150.55 28.74 64 4414 11807 3369574

Pharmacologic Action:

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SourceCodeDescription
ATC R03AC02 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Selective beta-2-adrenoreceptor agonists
ATC R03CC02 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS FOR SYSTEMIC USE
Selective beta-2-adrenoreceptor agonists
ATC R03AK04 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AK13 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AL02 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combinations with anticholinergics incl. triple combinations with corticosteroids
FDA MoA N0000009922 Adrenergic beta2-Agonists
FDA EPC N0000175779 beta2-Adrenergic Agonist
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058666 Adrenergic beta-2 Receptor Agonists
MeSH PA D000318 Adrenergic beta-Agonists
MeSH PA D018927 Anti-Asthmatic Agents
CHEBI has role CHEBI:35522 beta-adrenergic agonist
CHEBI has role CHEBI:35523 bronchodilator agent
MeSH PA D001337 Autonomic Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D012102 Reproductive Control Agents
MeSH PA D019141 Respiratory System Agents
MeSH PA D015149 Tocolytic Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Bronchospasm indication 4386001
Acute exacerbation of asthma indication 708038006
Chronic Obstructive Pulmonary Disease with Bronchospasms indication
Exercise-Induced Bronchospasm Prevention indication
Bronchospasm Prevention indication
Ocular hypertension contraindication 4210003 DOID:9282
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Ketoacidosis contraindication 56051008
Metabolic acidosis contraindication 59455009
Diabetes mellitus contraindication 73211009 DOID:9351
Paradoxical bronchospasm contraindication 102578005
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002 DOID:1826
Bladder outflow obstruction contraindication 236645006
Benign prostatic hyperplasia contraindication 266569009 DOID:2883
Retention of urine contraindication 267064002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Myocardial ischemia contraindication 414795007 DOID:3393
Congenital long QT syndrome contraindication 442917000
Chronic obstructive lung disease off-label use 13645005 DOID:3083

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.07 acidic
pKa2 9.46 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.021% BASE ACCUNEB MYLAN SPECIALITY LP N020949 April 30, 2001 RX SOLUTION INHALATION 6702997 Dec. 28, 2021 INDICATED FOR THE RELIEF OF BRONCHOSPASM IN PATIENTS 2-12 YEARS OF AGE WITH ASTHMA (REVERSIBLE OBSTRUCTIVE AIRWAY DISEASE)
EQ 0.042% BASE ACCUNEB MYLAN SPECIALITY LP N020949 April 30, 2001 RX SOLUTION INHALATION 6702997 Dec. 28, 2021 INDICATED FOR THE RELIEF OF BRONCHOSPASM IN PATIENTS 2-12 YEARS OF AGE WITH ASTHMA (REVERSIBLE OBSTRUCTIVE AIRWAY DISEASE)
EQ 0.083% BASE DUONEB MYLAN SPECIALITY LP N020950 March 21, 2001 DISCN SOLUTION INHALATION 6632842 Dec. 28, 2021 TREATMENT OF BRONCHOSPASM ASSOCIATED WITH COPD IN PATIENTS REQUIRING MORE THAN ONE BRONCHO DILATOR

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.090MG BASE/INH PROAIR RESPICLICK TEVA BRANDED PHARM N205636 March 31, 2015 RX POWDER, METERED INHALATION March 12, 2018 NEW PRODUCT
EQ 0.090MG BASE/INH PROAIR RESPICLICK TEVA BRANDED PHARM N205636 March 31, 2015 RX POWDER, METERED INHALATION April 28, 2019 NEW PATIENT POPULATION

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-2 adrenergic receptor GPCR AGONIST Ki 5.95 WOMBAT-PK CHEMBL
Beta-1 adrenergic receptor GPCR Ki 5.61 PDSP
Beta-2 adrenergic receptor GPCR Kd 6.28 CHEMBL
Beta-2 adrenergic receptor GPCR Kd 5.94 CHEMBL

External reference:

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IDSource
558 IUPHAR_LIGAND_ID
4018796 VUID
N0000147099 NUI
C0001927 UMLSCUI
D02147 KEGG_DRUG
021SEF3731 UNII
51022-70-9 SECONDARY_CAS_RN
DB01001 DRUGBANK_ID
CHEMBL714 ChEMBL_ID
2083 PUBCHEM_CID
435 RXNORM
372897005 SNOMEDCT_US
91143003 SNOMEDCT_US
46702 MMSL
4143 MMSL
d00749 MMSL
4018796 VANDF
N0000007409 NDFRT
N0000147099 NDFRT
001814 NDDF
CHEBI:2549 CHEBI
CHEMBL1201026 ChEMBL_ID
2585 INN_ID
D000420 MESH_DESCRIPTOR_UI
68H PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Proventil HFA HUMAN PRESCRIPTION DRUG LABEL 1 0085-1132 AEROSOL, METERED 108 ug RESPIRATORY (INHALATION) NDA 11 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-0661 SYRUP 2 mg ORAL ANDA 11 sections
Ipratropium Bromide and Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-6723 SOLUTION 2.50 mg RESPIRATORY (INHALATION) ANDA 12 sections
VENTOLIN HUMAN PRESCRIPTION DRUG LABEL 1 0173-0682 AEROSOL, METERED 90 ug RESPIRATORY (INHALATION) NDA 17 sections
Ipratropium Bromide and Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 0185-7322 SOLUTION 3 mg RESPIRATORY (INHALATION) NDA 13 sections
Albuterol HUMAN PRESCRIPTION DRUG LABEL 1 0378-0255 TABLET 2 mg ORAL ANDA 11 sections
Albuterol HUMAN PRESCRIPTION DRUG LABEL 1 0378-0572 TABLET 4 mg ORAL ANDA 11 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-4122 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 11 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-4124 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 11 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6991 SOLUTION 0.75 mg RESPIRATORY (INHALATION) NDA authorized generic 14 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6992 SOLUTION 1.50 mg RESPIRATORY (INHALATION) NDA authorized generic 14 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-8270 SOLUTION 2.50 mg RESPIRATORY (INHALATION) ANDA 13 sections
Ipratropium Bromide and Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-9671 SOLUTION 2.50 mg RESPIRATORY (INHALATION) ANDA 14 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0472-0825 SYRUP 2 mg ORAL ANDA 19 sections
Ipratropium Bromide and Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0487-0201 SOLUTION 3 mg RESPIRATORY (INHALATION) ANDA 15 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0487-0301 SOLUTION 0.75 mg RESPIRATORY (INHALATION) ANDA 15 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0487-9501 SOLUTION 2.50 mg RESPIRATORY (INHALATION) ANDA 13 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0487-9901 SOLUTION 2.50 mg RESPIRATORY (INHALATION) ANDA 15 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0487-9904 SOLUTION 1.50 mg RESPIRATORY (INHALATION) ANDA 15 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0591-3467 SOLUTION 0.63 mg INTRABRONCHIAL ANDA 15 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0591-3468 SOLUTION 1.25 mg INTRABRONCHIAL ANDA 15 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0591-3797 SOLUTION 2.50 mg INTRABRONCHIAL ANDA 14 sections
Ipratropium Bromide and Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0591-3817 SOLUTION 2.50 mg RESPIRATORY (INHALATION) ANDA 14 sections
Combivent Respimat HUMAN PRESCRIPTION DRUG LABEL 1 0597-0024 SPRAY, METERED 120 ug RESPIRATORY (INHALATION) NDA 17 sections
Ipratropium Bromide and Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0781-7146 SOLUTION 3 mg RESPIRATORY (INHALATION) ANDA 14 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0781-7155 SOLUTION 2.50 mg RESPIRATORY (INHALATION) ANDA 13 sections
VENTOLIN HUMAN PRESCRIPTION DRUG LABEL 1 16590-339 AEROSOL, METERED 108 ug RESPIRATORY (INHALATION) NDA 17 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 17856-0740 SYRUP 2 mg ORAL ANDA 11 sections
Albuterol HUMAN PRESCRIPTION DRUG LABEL 1 21695-198 AEROSOL, METERED 90 ug ORAL ANDA 12 sections
Albuterol Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 21695-245 SOLUTION 5 mg RESPIRATORY (INHALATION) ANDA 11 sections