Drugbank Salmeterol, Salmetedur


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For the treatment of asthma and chronic obstructive pulmonary disease (COPD).

Salmeterol is a long acting beta2-adrenoceptor agonist (LABA), usually only prescribed for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed concurrently with a corticosteroid, such as beclometasone. The primary noticable difference of salmeterol to salbutamol is that the duration of action lasts approximately 12 hours in comparison with 4-6 hours of salbutamol. When used regularly every day as presecribed, inhaled salmeterol decreases the number and severity of asthma attacks. However, it is not for use for relieving an asthma attack that has already started. Inhaled salmeterol works like other beta 2-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. Salmeterol is similar in action to formoterol, however formoterol has been demonstrated to have a faster onset of action than salmeterol as a result of a lower lipophilicity, and has also been demonstrated to be more potent - a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol.

Mechanism of action

Salmeterol's long, lipophilic side chain binds to exosites near beta(2)-receptors in the lungs and on bronchiolar smooth muscle, allowing the active portion of the molecule to remain at the receptor site, continually binding and releasing. Beta(2)-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and increased bronchial airflow.

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. By the oral route, no deaths occurred in rats at 1,000 mg/kg (approximately 81,000 times the maximum recommended daily inhalation dose in adults and approximately 38,000 times the maximum recommended daily inhalation dose in children on a mg/m 2 basis).

Humans and other mammals

SNP Mediated Effects

SNP Mediated Adverse Drug Reactions

Predicted ADMET features

Human Intestinal Absorption

Blood Brain Barrier

P-glycoprotein inhibitor I

P-glycoprotein inhibitor II

Renal organic cation transporter

CYP450 2C9 substrate

CYP450 2D6 substrate

CYP450 3A4 substrate

CYP450 1A2 substrate

CYP450 2C9 inhibitor

CYP450 2D6 inhibitor

CYP450 2C19 inhibitor

CYP450 3A4 inhibitor

CYP450 inhibitory promiscuity

Low CYP Inhibitory Promiscuity

Rat acute toxicity

2.0830 LD50, mol/kg

hERG inhibition (predictor I)

hERG inhibition (predictor II)

ADMET data is predicted using admetSAR. a free tool for evaluating chemical ADMET properties. (23092397 )

Glaxosmithkline

Glaxo group ltd dba glaxosmithkline

Aerosol, metered dose

oral; respiratory (inhalation)

oral; respiratory (inhalation)

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Serevent Diskhaler Device

Serevent 50 mcg/dose Disk

Serevent diskus 50 mcg

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pKa (Strongest Acidic)

pKa (Strongest Basic)

Hydrogen Acceptor Count

Hydrogen Donor Count

Polar Surface Area

Rotatable Bond Count

122.39 m 3 ·mol -1

Number of Rings

Panayiotis Procopiou, “Novel process for preparing salmeterol.” U. S. Patent US20030162840, issued August 28, 2003.

Salpeter SR, Buckley NS, Ormiston TM, Salpeter EE: Meta-analysis: effect of long-acting beta-agonists on severe asthma exacerbations and asthma-related deaths. Ann Intern Med. 2006 Jun 20;144(12):904-12. Epub 2006 Jun 5. [PubMed:16754916 ]

Therapeutic Targets Database

Guide to Pharmacology

Drug Product Database

The risk or severity of adverse effects can be increased when 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE is combined with Salmeterol.

Acebutolol may decrease the bronchodilatory activities of Salmeterol.

Alprenolol may decrease the bronchodilatory activities of Salmeterol.

The risk or severity of adverse effects can be increased when Amineptine is combined with Salmeterol.

The serum concentration of Salmeterol can be increased when it is combined with Amiodarone.

Salmeterol may increase the QTc-prolonging activities of Amiodarone.

The risk or severity of adverse effects can be increased when Amitriptyline is combined with Salmeterol.

The serum concentration of Amodiaquine can be increased when it is combined with Salmeterol.

Salmeterol may increase the QTc-prolonging activities of Anagrelide.

The serum concentration of Salmeterol can be increased when it is combined with Aprepitant.

Salmeterol may increase the QTc-prolonging activities of Arsenic trioxide.

Salmeterol may increase the QTc-prolonging activities of Artemether.

Targets

Kind Protein Organism Human Pharmacological action yes Actions agonist General Function: Protein homodimerization activity Specific 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. Gene Name: ADRB2 Uniprot ID: P07550 Molecular Weight: 46458.32 Da

References

Rong Y, Arbabian M, Thiriot DS, Seibold A, Clark RB, Ruoho AE: Probing the salmeterol binding site on the beta 2-adrenergic receptor using a novel photoaffinity ligand, [(125)I]iodoazidosalmeterol. Biochemistry. 1999 Aug 31;38(35):11278-86. [PubMed:10471277 ]

Finney PA, Donnelly LE, Belvisi MG, Chuang TT, Birrell M, Harris A, Mak JC, Scorer C, Barnes PJ, Adcock IM, Giembycz MA: Chronic systemic administration of salmeterol to rats promotes pulmonary beta(2)-adrenoceptor desensitization and down-regulation of G(s alpha). Br J Pharmacol. 2001 Mar;132(6):1261-70. [PubMed:11250877 ]

Green SA, Rathz DA, Schuster AJ, Liggett SB: The Ile164 beta(2)-adrenoceptor polymorphism alters salmeterol exosite binding and conventional agonist coupling to G(s). Eur J Pharmacol. 2001 Jun 15;421(3):141-7. [PubMed:11516429 ]

Meliton AY, Munoz NM, Liu J, Lambertino AT, Boetticher E, Myo S, Myou S, Zhu X, Johnson M, Leff AR: Blockade of LTC4 synthesis caused by additive inhibition of gIV-PLA2 phosphorylation: Effect of salmeterol and PDE4 inhibition in human eosinophils. J Allergy Clin Immunol. 2003 Aug;112(2):404-10. [PubMed:12897749 ]

Brogden RN, Faulds D: Salmeterol xinafoate: a review of its pharmacological properties and therapeutic potential in reversible obstructive airways disease. Allergol Immunopathol (Madr). 1992 Mar-Apr;20(2):72-84. [PubMed:1359777 ]

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind Protein Organism Human Pharmacological action unknown Actions substrate General Function: Vitamin d3 25-hydroxylase activity Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e. g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot. Gene Name: CYP3A4 Uniprot ID: P08684 Molecular Weight: 57342.67 Da

References

Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Drug Interactions: Cytochrome P450 Drug Interaction Table [Link ]

Kind Protein Organism Human Pharmacological action unknown Actions substrate General Function: Oxygen binding Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Gene Name: CYP3A5 Uniprot ID: P20815 Molecular Weight: 57108.065 Da

References

Drug Interactions: Cytochrome P450 Drug Interaction Table [Link ]

Kind Protein Organism Human Pharmacological action unknown Actions substrate General Function: Oxygen binding Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Gene Name: CYP3A7 Uniprot ID: P24462 Molecular Weight: 57525.03 Da

References

Drug Interactions: Cytochrome P450 Drug Interaction Table [Link ]

Kind Protein Organism Human Pharmacological action unknown Actions inhibitor General Function: Steroid hydroxylase activity Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme. Gene Name: CYP2C8 Uniprot ID: P10632 Molecular Weight: 55824.275 Da

References

Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807 ]

Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions. and by The Metabolomics Innovation Centre (TMIC). a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta. Genome British Columbia. and Genome Canada. a not-for-profit organization that is leading Canada's national genomics strategy with $900 million in funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc.