Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C35H36ClNO3S |
Molecular Weight | 586.183 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(O)C1=CC=CC=C1CC[C@@H](SCC2(CC(O)=O)CC2)C3=CC=CC(\C=C\C4=CC=C5C=CC(Cl)=CC5=N4)=C3
InChI
InChIKey=UCHDWCPVSPXUMX-TZIWLTJVSA-N
InChI=1S/C35H36ClNO3S/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39)/b15-10+/t32-/m1/s1
Molecular Formula | C35H36ClNO3S |
Molecular Weight | 586.183 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 1 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020829s069,020830s071,021409s047lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/67093875
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020829s069,020830s071,021409s047lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/67093875
Montelukast (SINGULAIR®) is a selective and orally active leukotriene D4 (LTD4) receptor antagonist that inhibits the cysteinyl leukotriene CysLT1 receptor. It is indicated for the prophylaxis and chronic treatment of asthma, for prevention of exercise-induced bronchoconstriction, and for the relief of symptoms of seasonal allergic rhinitis. LTD4 is a product of arachidonic acid metabolism and is released from various cells, including mast cells and eosinophils. This eicosanoid binds to CysLT1 receptor found in the human airway (including airway smooth muscle cells and airway macrophages) and on other pro-inflammatory cells (including eosinophils and certain myeloid stem cells). Cysteinyl leukotriene receptors (CysLTs) have been correlated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process. In allergic rhinitis, CysLTs are released from the nasal mucosa after allergen exposure during both earlyand late-phase reactions and are associated with symptoms of allergic rhinitis. Montelukast (SINGULAIR®) binds with high affinity and selectivity to the CysLT1 (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or beta-adrenergic receptor). It inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.
CNS Activity
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020829s069,020830s071,021409s047lbl.pdf
Curator's Comment: Neuropsychiatric events have been reported with SINGULAIR®.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7621356
Curator's Comment: # Merck & Co., Inc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1798 |
2.3 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | SINGULAIR Approved UseMontelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older. Launch Date1998 |
|||
Preventing | SINGULAIR Approved UseMontelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older. Launch Date1998 |
|||
Primary | SINGULAIR Approved UseMontelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older. Launch Date1998 |
|||
Primary | SINGULAIR Approved UseMontelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older. Launch Date1998 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
23.4 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg 1 times / day multiple, respiratory dose: 1 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
242 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg 1 times / day multiple, respiratory dose: 10 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
225 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg 1 times / day multiple, respiratory dose: 10 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
76 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg 1 times / day multiple, respiratory dose: 3 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
64.8 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg 1 times / day multiple, respiratory dose: 3 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
5.1 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
0.3 mg single, respiratory dose: 0.3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
5.24 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
0.3 mg single, respiratory dose: 0.3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
18.5 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg single, respiratory dose: 1 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
13.8 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg single, respiratory dose: 1 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
224 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg single, respiratory dose: 10 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
233 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg single, respiratory dose: 10 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
184 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg single, respiratory dose: 10 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
54.3 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg single, respiratory dose: 3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
60 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg single, respiratory dose: 3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
44.3 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg single, respiratory dose: 3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
541.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9429741/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
MONTELUKAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
602.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9429741/ |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
MONTELUKAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
214 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg 1 times / day multiple, respiratory dose: 1 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
1850 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg 1 times / day multiple, respiratory dose: 10 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
1880 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg 1 times / day multiple, respiratory dose: 10 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
576 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg 1 times / day multiple, respiratory dose: 3 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
526 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg 1 times / day multiple, respiratory dose: 3 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
155 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg single, respiratory dose: 1 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
132 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg single, respiratory dose: 1 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
1600 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg single, respiratory dose: 10 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
1576 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg single, respiratory dose: 10 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
1500 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg single, respiratory dose: 10 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
491 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg single, respiratory dose: 3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
403 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg single, respiratory dose: 3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
357 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg single, respiratory dose: 3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
3540 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9429741/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
MONTELUKAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3978 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9429741/ |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
MONTELUKAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.2 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg 1 times / day multiple, respiratory dose: 1 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
7.7 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg 1 times / day multiple, respiratory dose: 10 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
7.4 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg 1 times / day multiple, respiratory dose: 10 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
7.6 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg 1 times / day multiple, respiratory dose: 3 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
8.1 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg 1 times / day multiple, respiratory dose: 3 mg route of administration: respiratory experiment type: multiple co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
5.7 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
1 mg single, respiratory dose: 1 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
5.7 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
10 mg single, respiratory dose: 10 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
6.9 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00636207 |
3 mg single, respiratory dose: 3 mg route of administration: respiratory experiment type: single co-administered: |
MONTELUKAST plasma | Homo sapiens population: unhealthy age: sex: food status: |
|
5.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9429741/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
MONTELUKAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9429741/ |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
MONTELUKAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
800 mg single, oral Highest studied dose |
healthy, 21-40 years |
|
7 mg single, intravenous Dose: 7 mg Route: intravenous Route: single Dose: 7 mg Sources: |
unhealthy, 29.8 years (range: 15.0–56.0 years) Health Status: unhealthy Age Group: 29.8 years (range: 15.0–56.0 years) Sex: M+F Sources: |
Other AEs: Headache... |
80 mg single, oral Overdose |
unhealthy, 3 years |
|
200 mg 3 times / day multiple, oral Highest studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, 34 years (range: 18-54 years) Health Status: unhealthy Age Group: 34 years (range: 18-54 years) Sex: M+F Sources: |
Other AEs: Bilirubin total increased, Alanine aminotransferase increase... Other AEs: Bilirubin total increased (mild, 1 patient) Sources: Alanine aminotransferase increase (mild, 1 patient) |
10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: |
unhealthy, 37 years |
Disc. AE: Jaundice, Pruritus... AEs leading to discontinuation/dose reduction: Jaundice (1 patient) Sources: Pruritus (severe, 1 patient) Nausea (1 patient) |
1000 ug single, respiratory Dose: 1000 ug Route: respiratory Route: single Dose: 1000 ug Sources: |
unhealthy, 39.1 years (range: 16.0–63.0 years) Health Status: unhealthy Age Group: 39.1 years (range: 16.0–63.0 years) Sex: M+F Sources: |
|
135 mg single, oral Overdose |
unhealthy, 5 years |
|
10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: |
unhealthy, >15 years Health Status: unhealthy Age Group: >15 years Sources: |
Other AEs: Psychiatric disorder NOS... Other AEs: Psychiatric disorder NOS (serious) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Headache | 2% | 7 mg single, intravenous Dose: 7 mg Route: intravenous Route: single Dose: 7 mg Sources: |
unhealthy, 29.8 years (range: 15.0–56.0 years) Health Status: unhealthy Age Group: 29.8 years (range: 15.0–56.0 years) Sex: M+F Sources: |
Alanine aminotransferase increase | mild, 1 patient | 200 mg 3 times / day multiple, oral Highest studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, 34 years (range: 18-54 years) Health Status: unhealthy Age Group: 34 years (range: 18-54 years) Sex: M+F Sources: |
Bilirubin total increased | mild, 1 patient | 200 mg 3 times / day multiple, oral Highest studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, 34 years (range: 18-54 years) Health Status: unhealthy Age Group: 34 years (range: 18-54 years) Sex: M+F Sources: |
Jaundice | 1 patient Disc. AE |
10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: |
unhealthy, 37 years |
Nausea | 1 patient Disc. AE |
10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: |
unhealthy, 37 years |
Pruritus | severe, 1 patient Disc. AE |
10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: |
unhealthy, 37 years |
Psychiatric disorder NOS | serious | 10 mg 1 times / day steady, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: |
unhealthy, >15 years Health Status: unhealthy Age Group: >15 years Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Montelukast, a leukotriene receptor antagonist, reduces the concentration of leukotrienes in the respiratory tract of children with persistent asthma. | 1999 Dec |
|
Montelukast added to inhaled beclomethasone in treatment of asthma. Montelukast/Beclomethasone Additivity Group. | 1999 Dec |
|
Pulmonary eosinophilia associated with montelukast. | 1999 Jun |
|
Characterization of the human cysteinyl leukotriene CysLT1 receptor. | 1999 Jun 24 |
|
Oral montelukast, inhaled beclomethasone, and placebo for chronic asthma. A randomized, controlled trial. Montelukast/Beclomethasone Study Group. | 1999 Mar 16 |
|
Effect of multiple doses of montelukast, a CysLT1 receptor antagonist, on digoxin pharmacokinetics in healthy volunteers. | 1999 Sep |
|
Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. | 1999 Sep |
|
Montelukast in the prophylaxis of migraine: a potential role for leukotriene modifiers. | 2000 Feb |
|
Recurrent panniculitis in a man with asthma receiving treatment with leukotriene-modifying agents. | 2000 Jun |
|
The protective effects of leukotriene modifiers in aspirin-induced asthma. | 2000 Sep 15 |
|
[A study on the heterogeneous apoptosis of lymphocytes, eosinophils, and neutrophils from peripheral blood of asthmatic patients]. | 2003 Oct |
|
Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1. | 2004 Apr |
|
Antihistamines added to an antileukotriene in treating seasonal allergic rhinitis: histamine and leukotriene antagonism. | 2004 Feb |
|
Examination of 209 drugs for inhibition of cytochrome P450 2C8. | 2005 Jan |
|
Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
|
Montelukast and zafirlukast do not affect the pharmacokinetics of the CYP2C8 substrate pioglitazone. | 2006 Jul |
|
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats. | 2009 Apr 23 |
|
Leukotriene pathways and in vitro adenotonsillar cell proliferation in children with obstructive sleep apnea. | 2009 May |
|
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor. | 2011 Dec 8 |
|
Identification of old drugs as potential inhibitors of HIV-1 integrase - human LEDGF/p75 interaction via molecular docking. | 2012 Dec |
|
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. | 2015 May 18 |
Sample Use Guides
SINGULAIR® should be taken once daily in the evening. The following dose is recommended for adults and adolescents 15 years of age and older: one 10-mg tablet.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7621356
Montelukast is a potent and selective inhibitor of [3H]leukotriene D4 specific binding in guinea pig lung (Ki 0.18 +/- 0.03 nM), sheep lung (Ki 4 nM), and dimethylsulfoxide-differentiated U937 cell plasma membrane preparations (Ki 0.52 +/- 0.23 nM), but it was essentially inactive versus [3H]leukotriene C4 specific binding in dimethylsulfoxide-differentiated U937 cell membranes (IC50 10 microM) and [3H]leukotriene B4 specific binding in THP-1 cell membranes (IC50 40 microM). Montelukast also inhibited specific binding of [3H]leukotriene D4 to guinea pig lung in the presence of human serum albumin, human plasma, and squirrel monkey plasma with Ki values of 0.21 +/- 0.08, 0.19 +/- 0.02, and 0.26 +/- 0.02 nM, respectively.
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:09:12 GMT 2025
by
admin
on
Mon Mar 31 18:09:12 GMT 2025
|
Record UNII |
MHM278SD3E
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Preferred Name | English | ||
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NDF-RT |
N0000000083
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
||
|
LIVERTOX |
NBK548264
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
||
|
WHO-ATC |
R03DC03
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
||
|
WHO-VATC |
QR03DC03
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
||
|
WHO-ATC |
R03DC53
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
||
|
NDF-RT |
N0000175777
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
||
|
NCI_THESAURUS |
C29712
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
7582
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
SUB09054MIG
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
158966-92-8
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
MHM278SD3E
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
MHM278SD3E
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
3340
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
DTXSID9023334
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
CHEMBL787
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
1836
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
7388
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
50730
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
Montelukast
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
100000080382
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
C66189
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
C093875
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
m7616
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | Merck Index | ||
|
MONTELUKAST
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
5281040
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | |||
|
88249
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY | RxNorm | ||
|
DB00471
Created by
admin on Mon Mar 31 18:09:12 GMT 2025 , Edited by admin on Mon Mar 31 18:09:12 GMT 2025
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLIC ENZYME -> SUBSTRATE |
|
||
|
RACEMATE -> ENANTIOMER |
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TARGET -> INHIBITOR |
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR | |||
|
SALT/SOLVATE -> PARENT |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
|
||
|
METABOLITE -> PARENT |
|
||
|
METABOLITE -> PARENT |
|
||
|
METABOLITE -> PARENT |
|
||
|
METABOLITE -> PARENT |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Volume of Distribution | PHARMACOKINETIC |
|
|
|||
Biological Half-life | PHARMACOKINETIC |
|
|
|||
Tmax | PHARMACOKINETIC |
|
ORAL, GRANULE PHARMACOKINETIC PHARMACOKINETIC |
|
||
ORAL BIOAVAILABILITY | PHARMACOKINETIC |
|
FILM-COATED TABLET PHARMACOKINETIC PHARMACOKINETIC |
|
||