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=C(CC[C@@H](SCC2(CC(O)=O)CC2)C3=CC(\C=C\C4=NC5=CC(Cl)=CC=C5C=C4)=CC=C3)C=CC=C1
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 Date8.8793278E11 |
|||
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 Date8.8793278E11 |
|||
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 Date8.8793278E11 |
|||
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 Date8.8793278E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
|
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: |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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: |
|
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: |
|
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: |
|
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: |
|
7.7 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: |
|
7.6 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: |
Doses
Dose | Population | Adverse events |
---|---|---|
800 mg single, oral Highest studied dose |
healthy, 21-40 years n = 18 Health Status: healthy Age Group: 21-40 years Sex: M Population Size: 18 Sources: |
|
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) n = 50 Health Status: unhealthy Condition: asthma Age Group: 29.8 years (range: 15.0–56.0 years) Sex: M+F Population Size: 50 Sources: |
Other AEs: Headache... |
80 mg single, oral Overdose |
unhealthy, 3 years n = 1 Health Status: unhealthy Condition: asthma Age Group: 3 years Population Size: 1 Sources: |
|
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) n = 28 Health Status: unhealthy Condition: chronic asthma Age Group: 34 years (range: 18-54 years) Sex: M+F Population Size: 28 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 n = 1 Health Status: unhealthy Age Group: 37 years Sex: F Population Size: 1 Sources: |
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) n = 36 Health Status: unhealthy Condition: chronic asthma Age Group: 39.1 years (range: 16.0–63.0 years) Sex: M+F Population Size: 36 Sources: |
|
135 mg single, oral Overdose |
unhealthy, 5 years n = 1 Health Status: unhealthy Condition: asthma Age Group: 5 years Population Size: 1 Sources: |
|
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) n = 50 Health Status: unhealthy Condition: asthma Age Group: 29.8 years (range: 15.0–56.0 years) Sex: M+F Population Size: 50 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) n = 28 Health Status: unhealthy Condition: chronic asthma Age Group: 34 years (range: 18-54 years) Sex: M+F Population Size: 28 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) n = 28 Health Status: unhealthy Condition: chronic asthma Age Group: 34 years (range: 18-54 years) Sex: M+F Population Size: 28 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 n = 1 Health Status: unhealthy Age Group: 37 years Sex: F Population Size: 1 Sources: |
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 n = 1 Health Status: unhealthy Age Group: 37 years Sex: F Population Size: 1 Sources: |
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 n = 1 Health Status: unhealthy Age Group: 37 years Sex: F Population Size: 1 Sources: |
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 |
---|---|---|
Pharmacology of leukotriene receptor antagonists. | 1998 Jun |
|
Inhibition of 5-lipoxygenase diminishes neurally evoked tachykinergic contraction of guinea pig isolated airway. | 1998 May |
|
Montelukast, a leukotriene receptor antagonist, reduces the concentration of leukotrienes in the respiratory tract of children with persistent asthma. | 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 |
|
Leukotriene receptor antagonists may prevent NSAID-induced exacerbations in patients with chronic urticaria. | 2000 Aug |
|
Leukotriene receptor antagonists: efficacy and safety in children with asthma. | 2000 Aug |
|
A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization. | 2000 Dec 29 |
|
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 |
|
Dose selection and dosing interval determination for LTRA use in asthma. | 2000 Sep 15 |
|
Characterization of the human cysteinyl leukotriene 2 receptor. | 2000 Sep 29 |
|
Clinical safety and tolerability of montelukast, a leukotriene receptor antagonist, in controlled clinical trials in patients aged > or = 6 years. | 2001 Jan |
|
Long-term asthma control with oral montelukast and inhaled beclomethasone for adults and children 6 years and older. | 2001 Jun |
|
Acute effects of the cys-leukotriene-1 receptor antagonist, montelukast, on experimental colitis in rats. | 2001 Oct 19 |
|
Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma. | 2002 Apr 15 |
|
The cysteinyl-leukotriene D4 induces cytosolic Ca2+ elevation and contraction of the human detrusor muscle. | 2003 Aug |
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Montelukast-associated Churg-Strauss syndrome. | 2003 Sep |
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Montelukast-induced hepatitis. | 2004 Apr 6 |
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Role of leukotriene inhibitors in the postoperative management of nasal polyps. | 2005 |
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Examination of 209 drugs for inhibition of cytochrome P450 2C8. | 2005 Jan |
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Differential effect of zileuton, a 5-lipoxygenase inhibitor, against nociceptive paradigms in mice and rats. | 2005 Jul |
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Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
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Influence of leukotriene pathway polymorphisms on response to montelukast in asthma. | 2006 Feb 15 |
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Effects of leukotriene receptor antagonists on monocyte chemotaxis, p38 and cytoplasmic calcium. | 2006 Jun |
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Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. | 2007 Dec 13 |
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Prevalence of alpha-1 antitrypsin deficiency in poorly controlled asthma--results from the ALA-ACRC low-dose theophylline trial. | 2007 Oct |
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CysLTR1 promoter polymorphism and requirement for leukotriene receptor antagonist in aspirin-intolerant asthma patients. | 2007 Sep |
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Gastroprotective and antioxidant effects of montelukast on indomethacin-induced gastric ulcer in rats. | 2007 Sep |
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Effects of zileuton and montelukast in mouse experimental spinal cord injury. | 2008 Feb |
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Cysteinyl leukotrienes mediate the enhancing effects of indomethacin and aspirin on eosinophil production in murine bone marrow cultures. | 2008 Feb |
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Leukotriene D4 increases the excitability of capsaicin-sensitive nasal sensory nerves to electrical and chemical stimuli. | 2008 Jul |
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Montelukast inhibits tumour necrosis factor-alpha-mediated interleukin-8 expression through inhibition of nuclear factor-kappaB p65-associated histone acetyltransferase activity. | 2008 May |
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Cysteinyl leucotriene receptor type 1 mediates contraction in human and guinea-pig oesophagus. | 2008 Oct |
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Concentration-dependent noncysteinyl leukotriene type 1 receptor-mediated inhibitory activity of leukotriene receptor antagonists. | 2010 Feb 15 |
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Comparative study of the oxidation of propranolol enantiomers in hepatic and small intestinal microsomes from cynomolgus and marmoset monkeys. | 2010 Jan 5 |
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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 |
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Association of the variants in AGT gene with modified drug response in Korean aspirin-intolerant asthma patients. | 2011 Oct |
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Identification of old drugs as potential inhibitors of HIV-1 integrase - human LEDGF/p75 interaction via molecular docking. | 2012 Dec |
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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
Wed Jul 05 23:16:40 UTC 2023
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Record UNII |
MHM278SD3E
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NDF-RT |
N0000000083
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LIVERTOX |
NBK548264
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WHO-ATC |
R03DC03
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QR03DC03
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R03DC53
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NDF-RT |
N0000175777
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NCI_THESAURUS |
C29712
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MHM278SD3E
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MHM278SD3E
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M7616
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MONTELUKAST
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DB00471
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METABOLIC ENZYME -> SUBSTRATE | |||
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BINDING
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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ORAL, GRANULE PHARMACOKINETIC PHARMACOKINETIC |
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ORAL BIOAVAILABILITY | PHARMACOKINETIC |
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FILM-COATED TABLET PHARMACOKINETIC PHARMACOKINETIC |
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