U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
Pirbuterol (trade name Maxair) is a short-acting β2 adrenoreceptor agonist with bronchodilating action used in the treatment of asthma. The pharmacologic effects of beta-adrenergic agonist drugs, including pirbuterol, are at least in proof attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. Pirbuterol is used in asthma for reversal of acute bronchospasm, and also as a maintenance medication to prevent future attacks. It should be used in patients 12 years of age and older with or without concurrent theophylline and/or inhaled corticosteroid. After inhalation of doses up to 800 μg (twice the maximum recommended dose) systemic blood levels of pirbuterol are below the limit of assay sensitivity (2–5 ng/ml). A mean of 51% of the dose is recovered in urine as pirbuterol plus its sulfate conjugate following administration by aerosol. Pirbuterol is not metabolized by catechol-O-methyltransferase.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
MAXAIR

Approved Use

Unknown

Launch Date

5.36284791E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
6.2 μg/L
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIRBUTEROL plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
9.8 μg/L
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIRBUTEROL plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIRBUTEROL plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
400 ug single, respiratory
Dose: 400 ug
Route: respiratory
Route: single
Dose: 400 ug
Sources:
unhealthy, 32 years (range: 21-56 years)
n = 14
Health Status: unhealthy
Condition: asthma
Age Group: 32 years (range: 21-56 years)
Sex: M+F
Population Size: 14
Sources:
40 mg 1 times / day multiple, oral
Highest studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
unhealthy, 62 years (range 42-71 years)
n = 26
Health Status: unhealthy
Condition: chronic heart failure
Age Group: 62 years (range 42-71 years)
Sex: M+F
Population Size: 26
Sources:
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Potential value of oral beta 2-adrenoceptor agonists in congestive heart failure: a haemodynamic and metabolic study.
1984 Mar
Patents

Sample Use Guides

Bronchospasm, prevention and treatment: Inhalation: 1 to 2 inhalations (200mcg) every 4 to 6 hours; not to exceed 12 inhalations daily. Patients should be advised to promptly consult healthcare provider or seek medical attention if no relief from acute treatment
Route of Administration: Respiratory
MDA-MB-231, SF-539, ACHN, A-549, HCT-116, SNB-19 were used for activity evaluation. Cells (1x10^5) were plated in 60mm dishes and treated with various doses of ARA-211 (Pirbuterol) or vehicle for 48 h. Apoptosis was analysed using the Cell Death Detection ELISA (Roche, Indianapolis, IN, USA) measuring cytoplasmic histoneassociated mono- and oligonucleosome DNA fragments.
Substance Class Protein
Created
by admin
on Sat Jun 26 17:13:20 UTC 2021
Edited
by admin
on Sat Jun 26 17:13:20 UTC 2021
Protein Sub Type
Sequence Type COMPLETE
Record UNII
VZX139UJO5
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BETA-2 ADRENERGIC RECEPTOR
Common Name English
ADRB2
Common Name English
B2AR
Common Name English
BETA-2 ADRENORECEPTOR
Common Name English
ADRB2R
Common Name English
Code System Code Type Description
FDA UNII
VZX139UJO5
Created by admin on Sat Jun 26 17:13:22 UTC 2021 , Edited by admin on Sat Jun 26 17:13:22 UTC 2021
PRIMARY
UNIPROT
P07550
Created by admin on Sat Jun 26 17:13:22 UTC 2021 , Edited by admin on Sat Jun 26 17:13:22 UTC 2021
PRIMARY
From To
1_106 1_191
1_184 1_190
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_6
N 1_15
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Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT CHEMICAL