Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H20N2O2.ClH |
| Molecular Weight | 296.792 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.O=C1NCC2(CCN(CCC3=CC=CC=C3)CC2)O1
InChI
InChIKey=FIKFLLIUPUVONI-UHFFFAOYSA-N
InChI=1S/C15H20N2O2.ClH/c18-14-16-12-15(19-14)7-10-17(11-8-15)9-6-13-4-2-1-3-5-13;/h1-5H,6-12H2,(H,16,18);1H
Fenspiride is an oxazolidinone spiro compound used as a drug in the treatment of certain respiratory diseases. It is approved for use in Russia for the treatment of acute and chronic inflammatory diseases of ENT organs and the respiratory tract (like rhinopharyngitis, laryngitis, tracheobronchitis, otitis and sinusitis), as well as for maintenance treatment of asthma. Fenspiride is marketed under the brand names Eurespal, Pneumorel, SYRESP, Oxofen and others. Erespal (fenspiride) is a drug with a bronchodilator and spasmolytic effect, which is often used in the complex therapy of bronchial asthma. Fenspiride has a clinically proven ability to increase the activity of the cilia of the bronchial ciliated epithelium, normalize the secretion of the bronchi and reduce its viscosity. Effectively removes bronchial obstruction, restores pulmonary gas exchange. Inhibits the metabolism of arachidonic acid, in parallel blocking histamine H1-receptors, since it is histamine that stimulates the chemical reactions of the transformation of arachidonic acid into the final metabolites-factors of inflammation. Reduces the production of other mediators of inflammation - serotonin and bradykinin.
It blocks α-adrenergic receptors, the activation of which increases the secretion of bronchial glands. The complex effect of fenspiride reduces the pathological effect of a number of factors that promote hypersecretion of anti-inflammatory substances and cause obstruction of the bronchial tree. Has a pronounced antispasmodic and myotropic effect.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL231 |
|||
Target ID: P16599 Gene ID: 103694380|||24835 Gene Symbol: Tnf Target Organism: Rattus norvegicus (Rat) |
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Target ID: CHEMBL2093863 |
4.16 null [pIC50] | ||
Target ID: CHEMBL2094125 |
3.44 null [pIC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Erespal Approved UseThe drug is indicated in the complex therapy of respiratory diseases (upper and lower divisions):
pharyngitis;
Rhinopharyngitis;
laryngitis;
tracheitis;
Tracheobronchitis;
Bronchitis (with or without chronic respiratory failure);
bronchial asthma;
Respiratory symptoms with influenza, measles and whooping cough;
sinusitis;
otitis;
Infection of the respiratory system, in the symptomatic complex of which there is a cough. |
|||
| Primary | Erespal Approved UseThe drug is indicated in the complex therapy of respiratory diseases (upper and lower divisions):
pharyngitis;
Rhinopharyngitis;
laryngitis;
tracheitis;
Tracheobronchitis;
Bronchitis (with or without chronic respiratory failure);
bronchial asthma;
Respiratory symptoms with influenza, measles and whooping cough;
sinusitis;
otitis;
Infection of the respiratory system, in the symptomatic complex of which there is a cough. |
|||
| Primary | Erespal Approved UseThe drug is indicated in the complex therapy of respiratory diseases (upper and lower divisions):
pharyngitis;
Rhinopharyngitis;
laryngitis;
tracheitis;
Tracheobronchitis;
Bronchitis (with or without chronic respiratory failure);
bronchial asthma;
Respiratory symptoms with influenza, measles and whooping cough;
sinusitis;
otitis;
Infection of the respiratory system, in the symptomatic complex of which there is a cough. |
|||
| Primary | Erespal Approved UseThe drug is indicated in the complex therapy of respiratory diseases (upper and lower divisions):
pharyngitis;
Rhinopharyngitis;
laryngitis;
tracheitis;
Tracheobronchitis;
Bronchitis (with or without chronic respiratory failure);
bronchial asthma;
Respiratory symptoms with influenza, measles and whooping cough;
sinusitis;
otitis;
Infection of the respiratory system, in the symptomatic complex of which there is a cough. |
|||
| Primary | Eurespal Approved UseIndications:
Rinofaringitis, laryngitis
— otitis, sinusitis
— rinotraheobronhit
— bronchitis
— bronchial asthma (maintenance therapy)
respiratory effects in measles, pertussis and influenza (syrup). |
|||
| Primary | Eurespal Approved UseIndications:
Rinofaringitis, laryngitis
— otitis, sinusitis
— rinotraheobronhit
— bronchitis
— bronchial asthma (maintenance therapy)
respiratory effects in measles, pertussis and influenza (syrup). |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
206 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7901024/ |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
329.35 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21899503/ |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
381.58 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21899503/ |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1034.09 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21899503/ |
80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6.03 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7901024/ |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.73 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7901024/ |
80 mg single, intravenous dose: 80 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10259.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21899503/ |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
9576.89 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21899503/ |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
11208.73 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21899503/ |
80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
16 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7901024/ |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
14 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7901024/ |
80 mg single, intravenous dose: 80 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
FENSPIRIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
80 mg 2 times / day multiple, oral Recommended Dose: 80 mg, 2 times / day Route: oral Route: multiple Dose: 80 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Allergy... AEs leading to discontinuation/dose reduction: Allergy (4%) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Allergy | 4% Disc. AE |
80 mg 2 times / day multiple, oral Recommended Dose: 80 mg, 2 times / day Route: oral Route: multiple Dose: 80 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| [Efficiency of combination therapy for acute otitis media]. | 2010 |
|
| [Pathogenetic correction of postoperative inflammation in modern rhinosurgery]. | 2010 |
|
| [Experience in using erespal in the treatment of acute respiratory diseases in children in outpatient practice]. | 2010 |
|
| [Pathogenetic therapy for inflammatory diseases of the middle ear]. | 2009 |
|
| [Experience with fenspiride in a rhinosurgeon's practice]. | 2009 |
|
| [Hearing rehabilitation in patients with acute otitis media treated with fenspiride]. | 2008 |
|
| [Clinicofunctional condition and quality of life in patients with chronic obstructive pulmonary disease before and after outpatient treatment with fenspiride]. | 2008 |
|
| [The role of expired air moisture condensate in assessment of pulmonary inflammation in patients with chronic obstructive pulmonary disease]. | 2008 |
|
| [New pharmaceuticals in treatment of chronic dust bronchitis]. | 2007 |
|
| [The effectiveness of fenspiride in the treatment of patients with chronic obstructive pulmonary disease]. | 2007 |
|
| [Anti-inflammatory therapy of paranasal sinuses diseases]. | 2006 |
|
| Comparison of fenspiride with beclomethasone as adjunctive anti-inflammatory treatment in patients with chronic obstructive pulmonary disease. | 2006 |
|
| [Erespal in combined therapy of acute rhinosinusitis]. | 2006 |
|
| [The effect of fenspiride on the number of exacerbations and the time of first exacerbation in patients with chronic bronchitis]. | 2005-08 |
|
| [Fenspiride in patients with acute bronchitis]. | 2005-07 |
|
| [Usefulness of fenspiride in the treatment of acute otitis media in children]. | 2005-06 |
|
| Efficacy of supplemental anti-inflammatory therapy with fenspiride in chronic obstructive and nonobstructive bronchitis. | 2005 |
|
| [Potential of antiinflammatory therapy in patients with chronic obstructive lung disease]. | 2005 |
|
| [Effectiveness and tolerance of fenspiride treatment in chronic sinusitis. Results of the Polish multicenter study]. | 2005 |
|
| [Fenspiride-a new alternative on the therapy of obstructive lung disease]. | 2004-01-02 |
|
| [Acute intoxication with fenspiride]. | 2004 |
|
| [Erespal effectiveness in exudative otitis media]. | 2003 |
|
| [ENT inflammation and importance of fenspiride]. | 2002-09 |
|
| [Bronchial inflammation during chronic bronchitis, importance of fenspiride]. | 2002-09 |
|
| Detection of fenspiride and identification of in vivo metabolites in horse body fluids by capillary gas chromatography-mass spectrometry: administration, biotransformation and urinary excretion after a single oral dose. | 2002-02-05 |
|
| [Experience in treating patients with chronic obstructive bronchitis with fenspirid]. | 2002 |
|
| [Effectiveness of fenspiride in patients with chronic obstructive bronchitis]. | 2001 |
Sample Use Guides
Tablets: One tablet (80 mg) twice-thrice a day. The maximum dose for a daily intake is 240 mg (3 tablets).Syrup: For 45-90 milliliters (3-6 tablespoons, respectively) per day.
Route of Administration:
Oral
In Vitro Use Guide
Curator's Comment: Fenspiride (10(-7)-10(-5) M) inhibited the histamine H1 receptor-induced Ca2+ increase in a lung epithelial cell line. Fenspiride (10(-5) M) abolished both phases of histamine-induced arachidonic acid release. https://www.ncbi.nlm.nih.gov/pubmed/9652346
Fenspiride (10(-6) to 10(-4) M) inhibited the nonadrenergic, noncholinergic (NANC) component of the contraction of the guinea-pig isolated main bronchus induced by EFS. Fenspiride significantly affected contractions induced by exogenously added substance P or [Nle10]-NKA(4-10) only at concentrations higher than 10(-3) M. In the guinea-pig perfused lung, fenspiride inhibited low pH- but not capsaicin-evoked release of CGRP. At higher concentrations (10(-4) M to 3x10(-4) M) fenspiride exhibited a significant inhibitory effect both on the cholinergic component of contractile response induced by EFS in the guinea-pig isolated main bronchus and on exogenously added acetylcholine.
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NCI_THESAURUS |
C257
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CHEMBL576127
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832NBX878V
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68626
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DBSALT002867
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236281
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5053-08-7
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757825
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m5296
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100000091351
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225-752-9
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DTXSID3045770
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C084775
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C80551
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SUB02128MIG
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ACTIVE MOIETY
SUBSTANCE RECORD
