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Identification
- Summary
Procaterol is a beta-2 adrenergic receptor agonist and bronchodilator used for the treatment of asthma and chronic obstructive pulmonary disease (COPD).
- Generic Name
- Procaterol
- DrugBank Accession Number
- DB01366
- Background
A long-acting beta-2-adrenergic receptor agonist. It is a potent bronchodilator that may be administered orally or by aerosol inhalation.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Procaterol (DB01366)
- Weight
- Average: 290.363
Monoisotopic: 290.163042576 - Chemical Formula
- C16H22N2O3
- Synonyms
- Procaterol
- Procaterolo
- Procaterolum
Pharmacology
- Indication
For the treatment of asthma and chronic obstructive pulmonary disease (COPD).
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Bronchial asthma •••••••••••• ••••••• ••••••••• •••••• •••••• Treatment of Bronchospasm •••••••••••• •••••• Treatment of Chronic bronchitis •••••••••••• ••••••• ••••••••• •••••• •••••• Treatment of Emphysema •••••••••••• ••••••• ••••••••• •••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Procaterol is a long-acting beta-2-adrenergic receptor agonist. It is a potent bronchodilator that may be administered orally or by aerosol inhalation.
- Mechanism of action
Beta(2)-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and increased bronchial airflow.
Target Actions Organism ABeta-2 adrenergic receptor agonistHumans - Absorption
Because of the small therapeutic dose, systemic levels of salmeterol are low or undetectable after inhalation of recommended doses.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Symptoms of overdose include angina (chest pain), dizziness, dry mouth, fatigue, flu-like symptoms, headache, heart irregularities, high or low blood pressure, high blood sugar, insomnia, muscle cramps, nausea, nervousness, rapid heartbeat, seizures, and tremor.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol The therapeutic efficacy of Procaterol can be decreased when used in combination with Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Procaterol is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Procaterol is combined with Acemetacin. Acetylsalicylic acid The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Procaterol. Aclidinium The risk or severity of Tachycardia can be increased when Procaterol is combined with Aclidinium. - Food Interactions
- Take with or without food. The onset of action of procaterol may be delayed when taken with food, however, there is no impact on the efficacy or duration of action of procaterol.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Procaterol hydrochloride 4VD1BRT7T8 62929-91-3 AEQDBKHAAWUCMT-KKJWGQAZSA-N Procaterol hydrochloride hemihydrate 8404I5HKFJ 81262-93-3 RZKAQAPBCFPJTK-GOPHCVLGSA-N - International/Other Brands
- Pro-Air
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Pro-air Aerosol 10mcg/aem Aerosol, metered 10 mcg / act Respiratory (inhalation) Parke Davis Division, Warner Lambert Canada Inc. 1989-12-31 1996-09-10 Canada 
Categories
- ATC Codes
- R03CC08 — Procaterol
- R03CC — Selective beta-2-adrenoreceptor agonists
- R03C — ADRENERGICS FOR SYSTEMIC USE
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- Drug Categories
- Adrenergic Agents
- Adrenergic Agonists
- Adrenergic beta-2 Receptor Agonists
- Adrenergic beta-Agonists
- Adrenergics for Systemic Use
- Adrenergics, Inhalants
- Agents producing tachycardia
- Agents that produce hypertension
- Alcohols
- Amines
- Amino Alcohols
- Anti-Asthmatic Agents
- Autonomic Agents
- Bronchodilator Agents
- Drugs for Obstructive Airway Diseases
- Ethanolamines
- Heterocyclic Compounds, Fused-Ring
- Hydroxyquinolines
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Quinolines
- Respiratory System Agents
- Selective Beta 2-adrenergic Agonists
- Sympathomimetics
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- X7I3EMM5K0
- CAS number
- 72332-33-3
- InChI Key
- FKNXQNWAXFXVNW-WBMJQRKESA-N
- InChI
- InChI=1S/C16H22N2O3/c1-4-12(17-9(2)3)16(21)11-5-7-13(19)15-10(11)6-8-14(20)18-15/h5-9,12,16-17,19,21H,4H2,1-3H3,(H,18,20)/t12-,16+/m1/s1
- IUPAC Name
- 8-hydroxy-5-[(1S,2R)-1-hydroxy-2-[(propan-2-yl)amino]butyl]-1,2-dihydroquinolin-2-one
- SMILES
- CC[C@@H](NC(C)C)[C@@H](O)C1=CC=C(O)C2=C1C=CC(=O)N2
References
- Synthesis Reference
Mitsuji Akazawa, Teruo Hama, Yukio Kimura, Yoshinobu Yasuda, "Procaterol-containing preparation for application to the skin." U.S. Patent US5480649, issued February, 1989.
US5480649- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015453
- PubChem Compound
- 688561
- PubChem Substance
- 46507907
- ChemSpider
- 599986
- BindingDB
- 50167071
- 34530
- ChEBI
- 135209
- ChEMBL
- CHEMBL3249705
- ZINC
- ZINC000019632678
- Therapeutic Targets Database
- DAP000944
- PharmGKB
- PA164748908
- Wikipedia
- Procaterol
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Unknown Status Treatment Cough 1 somestatus stop reason just information to hide 4 Completed Treatment Asthma 1 somestatus stop reason just information to hide 4 Not Yet Recruiting Treatment Chronic Obstructive Pulmonary Disease (COPD) 1 somestatus stop reason just information to hide 4 Terminated Treatment Chronic Obstructive Pulmonary Disease (COPD) 1 somestatus stop reason just information to hide 4 Unknown Status Treatment Cough Variant Asthma 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Syrup Oral 0.025 mg Tablet 50 mcg Syrup Oral Syrup Oral 25 mcg/5ml Tablet Powder Respiratory (inhalation) 10 mcg Powder Respiratory (inhalation) 10 mcg/1dose Aerosol, metered Respiratory (inhalation) 10 mcg / act Spray Respiratory (inhalation) Aerosol Respiratory (inhalation) Syrup Oral 00005 % Syrup Oral 25.69 mcg Syrup Oral 5 mcg/ml Tablet 25 mcg - Prices
Unit description Cost Unit ProAir HFA 108 (90 Base)mcg/act Aerosol 8.5 gm Inhaler 45.99USD inhaler DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source logP 0.88 Chemaxon pKa (Strongest Acidic) 8.52 Chemaxon pKa (Strongest Basic) 9.88 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 81.59 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 84.58 m3·mol-1 Chemaxon Polarizability 31.25 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9964 Blood Brain Barrier + 0.5966 Caco-2 permeable - 0.6522 P-glycoprotein substrate Substrate 0.7018 P-glycoprotein inhibitor I Non-inhibitor 0.8943 P-glycoprotein inhibitor II Non-inhibitor 0.9204 Renal organic cation transporter Non-inhibitor 0.9311 CYP450 2C9 substrate Non-substrate 0.8105 CYP450 2D6 substrate Non-substrate 0.6879 CYP450 3A4 substrate Substrate 0.5942 CYP450 1A2 substrate Non-inhibitor 0.538 CYP450 2C9 inhibitor Inhibitor 0.8949 CYP450 2D6 inhibitor Non-inhibitor 0.8986 CYP450 2C19 inhibitor Inhibitor 0.8774 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6783 Ames test Non AMES toxic 0.8558 Carcinogenicity Non-carcinogens 0.9066 Biodegradation Not ready biodegradable 0.9889 Rat acute toxicity 2.4772 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9921 hERG inhibition (predictor II) Non-inhibitor 0.6841
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-007p-0090000000-0ed4be5d76d7db5de606 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-00bi-0290000000-a38a4e4fe7f5b746b376 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-01q9-2190000000-7c1a20acc95f5d05b262 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03mi-1590000000-71229e11ebab672475cf Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-03kc-3940000000-b3c459123a4afab70ce8 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0ff0-8950000000-5ef7011803abf3ba25eb Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine
- Specific Function
- adenylate cyclase binding
- Gene Name
- ADRB2
- Uniprot ID
- P07550
- Uniprot Name
- Beta-2 adrenergic receptor
- Molecular Weight
- 46458.32 Da
References
- Kobayashi M, Kishimoto N, Ohnishi H, Tada S, Ueda N, Kamei T, Fujita J, Taguchi H: [beta 2-adrenoceptor polymorphism and effect of inhaled beta 2-stimulant (procaterol) on airway resistance measured by body plethysmography in healthy volunteers]. Nihon Kokyuki Gakkai Zasshi. 2002 Aug;40(8):637-43. [Article]
- Yamasaki Y, Kishimoto N, Ohnishi H, Fujita J, Kobayashi M, Kamei T, Tada S, Ueda N: [Beta 2-adrenoceptor polymorphism and effects of inhaled beta 2-stimulant (procaterol) and an anti-cholinergic drug (oxitropium) on the airway resistance]. Nihon Kokyuki Gakkai Zasshi. 2004 Mar;42(3):239-46. [Article]
- Noguchi K, Ojiri Y, Chibana T, Moromizato H, Sakanashi M: Cardiac effects of beta-2 adrenoceptor stimulation with intracoronary procaterol in the absence and presence of regional myocardial ischemia in dogs. J Pharmacol Exp Ther. 1991 Nov;259(2):732-7. [Article]
- Aizawa H, Inoue H, Ikeda T, Hirose T, Ito Y: Effects of procaterol, a beta-2-adrenoceptor stimulant, on neuroeffector transmission in human bronchial tissue. Respiration. 1991;58(3-4):163-6. [Article]
- Brodde OE, Daul A, Michel-Reher M, Boomsma F, Man in 't Veld AJ, Schlieper P, Michel MC: Agonist-induced desensitization of beta-adrenoceptor function in humans. Subtype-selective reduction in beta 1- or beta 2-adrenoceptor-mediated physiological effects by xamoterol or procaterol. Circulation. 1990 Mar;81(3):914-21. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at July 06, 2007 20:23 / Updated at October 31, 2024 23:40