Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C12H18ClNO.ClH |
| Molecular Weight | 264.191 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC(C)(C)NCC(O)C1=C(Cl)C=CC=C1
InChI
InChIKey=RSLNRVYIRDVHLY-UHFFFAOYSA-N
InChI=1S/C12H18ClNO.ClH/c1-12(2,3)14-8-11(15)9-6-4-5-7-10(9)13;/h4-7,11,14-15H,8H2,1-3H3;1H
DescriptionCurator's Comment: description was created based on several sources, including:
http://www.mylan.co.jp/-/media/MylanJP/documents/epd_products/interview_updated/if_hokunalin.pdf
Curator's Comment: description was created based on several sources, including:
http://www.mylan.co.jp/-/media/MylanJP/documents/epd_products/interview_updated/if_hokunalin.pdf
Tulobuterol is a long-acting beta2-adrenergic receptor agonist. Tulobuterol has almost no effects on blood pressure and heart rate and is highly selective for the tracheal muscle. It is indicated to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, bronchitis, chronic obstructive pulmonary disease (COPD) and emphysema. Serious side effects detected were: tremor, palpitations and serum potassium level decrease.
CNS Activity
Sources: http://www.mylan.co.jp/-/media/MylanJP/documents/epd_products/interview_updated/if_hokunalin.pdf
Curator's Comment: Known to be CNS penetrant in rats. Human data not available.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | Hokunalin Approved UseIt is usually used to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, acute bronchitis, chronic bronchitis, or emphysema. Launch Date1981 |
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| Palliative | Hokunalin Approved UseIt is usually used to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, acute bronchitis, chronic bronchitis, or emphysema. Launch Date1981 |
|||
| Palliative | Hokunalin Approved UseIt is usually used to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, acute bronchitis, chronic bronchitis, COPD or emphysema. Launch Date1981 |
|||
| Palliative | Hokunalin Approved UseIt is usually used to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, acute bronchitis, chronic bronchitis, or emphysema. Launch Date1981 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Induction and reduction of muscle tremor upon acute and repeated administration of the beta 2-agonists terbutaline, salbutamol and tulobuterol. | 1987 Dec |
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| Quantitative determination of clenbuterol, salbutamol and tulobuterol enantiomers by capillary electrophoresis. | 2001 Feb |
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| Clinical characteristics of asthmatic patients prescribed various beta-agonist metered-dose inhalers at Yamagata University Hospital. | 2001 Jan |
|
| Effects of sustained-release tulobuterol on asthma control and beta-adrenoceptor function. | 2002 Dec |
|
| [Pharmacological action and clinical aspects of salmeterol]. | 2003 Sep |
|
| [Patchs: the success of transdermal administration]. | 2004 Apr |
|
| [Clinical evaluation of tulobuterol patch in patients with mild or moderate persistent bronchial asthma-effects of long-term treatment on airway inflammation and hypersensitivity]. | 2004 Feb |
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| Evaluation of MISPE for the multi-residue extraction of beta-agonists from calves urine. | 2004 May 5 |
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| Clinical efficacy and safety of transdermal tulobuterol in the treatment of stable COPD: an open-label comparison with inhaled salmeterol. | 2005 |
|
| Alteration of the circadian rhythm in peak expiratory flow of nocturnal asthma following nighttime transdermal beta2-adrenoceptor agonist tulobuterol chronotherapy. | 2005 |
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| High-performance liquid chromatography electrospray ionization mass spectrometry determination of tulobuterol in rabbit's plasma. | 2005 Feb 7 |
|
| Determination of beta-agonists in liver and retina by liquid chromatography-tandem mass spectrometry. | 2005 Jan-Feb |
|
| Determination of beta-agonist residues in bovine urine using liquid chromatography-tandem mass spectrometry. | 2005 Jan-Feb |
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| Comparison of the effects of tulobuterol patch and salmeterol in moderate to severe asthma. | 2006 Nov |
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| Treatment with beta2-adrenoceptor agonist in vivo induces human clock gene, Per1, mRNA expression in peripheral blood. | 2007 |
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| Improvement of pulmonary function and dyspnea by tiotropium in COPD patients using a transdermal beta(2)-agonist. | 2007 |
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| Bioequivalence of marketed transdermal delivery systems for tulobuterol. | 2007 Aug |
|
| [The efficacy and safety of tulobuterol tape in mild and moderate persistent asthma patients]. | 2007 Jan |
|
| [Simultaneous determination of nine beta2-agonists residues in urines by ultra performance liquid chromatography-electrospray tandem mass spectrometry]. | 2007 Jul |
|
| Transdermal treatment with tulobuterol increases isometric contractile properties of diaphragm muscle in mice. | 2007 Jul |
|
| Addition of transdermal or inhaled long-acting Beta2-agonists in adult asthmatic patients treated with inhaled corticosteroids: switchover study from tulobuterol patch to salmeterol dry powder inhaler. | 2007 Mar |
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| Adherence to treatment by patients with asthma or COPD: comparison between inhaled drugs and transdermal patch. | 2007 Sep |
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| Comparison of bronchodilatory properties of transdermal and inhaled long-acting beta 2-agonists. | 2008 |
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| Characterization of monolithic matrix patch system containing tulobuterol. | 2008 Aug |
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| Anti-inflammatory effects and clinical efficacy of theophylline and tulobuterol in mild-to-moderate chronic obstructive pulmonary disease. | 2008 Dec |
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| [Simultaneous determination of nine beta-agonist residues in animal derived foods by ultra performance liquid chromatography-tandem mass spectrometry]. | 2008 Nov |
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| Tulobuterol patch maintains diaphragm muscle contractility for over twenty-four hours in a mouse model of sepsis. | 2009 Aug |
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| Chronic eosinophilic pneumonia: a case report and review of the literature. | 2009 Jul 2 |
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| Detection of tulobuterol crystal in transdermal patches using terahertz pulsed spectroscopy and imaging. | 2009 Jun |
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| Comparative study of skin permeation profiles between brand and generic tulobuterol patches. | 2010 |
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| Generic sample preparation combined with high-resolution liquid chromatography-time-of-flight mass spectrometry for unification of urine screening in doping-control laboratories. | 2010 Apr |
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| Simultaneous determination of beta2-agonists in human urine by fast-gas chromatography/mass spectrometry: method validation and clinical application. | 2010 Apr |
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| Characterization and release behaviors of porous PCL/Eudragit RS microcapsules containing tulobuterol. | 2010 Apr 1 |
|
| [Determination of fifteen beta-agonists in animal urine by high performance liquid chromatography-tandem mass spectrometry]. | 2010 Aug |
|
| Effect of porous silica on sustained release behaviors of pH sensitive pluronic F127/poly(acrylic acid) hydrogels containing tulobuterol. | 2010 Oct 15 |
Patents
Sample Use Guides
In general, for adults and children aged 9 or older, apply 2 mg of the tape to the chest, back, or upper arm, once daily. For children aged 6 months to 2 years, apply 0.5 mg of the tape to the chest, back, or upper arm, once daily. For children aged 3 to 8 years, apply 1 mg of the tape to the chest, back, or upper arm, once daily. This preparation contains 2 mg of the active ingredients in a piece of tape.
Route of Administration:
Transdermal
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ACTIVE MOIETY
SUBSTANCE RECORD
