Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H22N2 |
Molecular Weight | 290.4021 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCC(CC1)=C2C3=C(CCC4=C2N=CC=C4)C=CC=C3
InChI
InChIKey=SEBMTIQKRHYNIT-UHFFFAOYSA-N
InChI=1S/C20H22N2/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19/h2-7,12H,8-11,13-14H2,1H3
Molecular Formula | C20H22N2 |
Molecular Weight | 290.4021 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.drugs.com/mtm/optimine.html
Sources: https://www.drugs.com/mtm/optimine.html
Azatadine is an antihistamine, which blocks the effects of the naturally occurring chemical histamine in the body. Azatadine is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; and other symptoms of allergies and the common cold. The antihistamines antagonize those pharmacological effects of histamine, which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2568212 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Sources: https://www.drugs.com/mtm/optimine.html |
Palliative | OPTIMINE Approved UseAzatadine is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; itching; and other symptoms of allergies and the common cold. Launch Date1977 |
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Sources: https://www.drugs.com/mtm/optimine.html |
Palliative | OPTIMINE Approved UseAzatadine is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; itching; and other symptoms of allergies and the common cold. Launch Date1977 |
||
Sources: https://www.drugs.com/mtm/optimine.html |
Palliative | OPTIMINE Approved UseAzatadine is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; itching; and other symptoms of allergies and the common cold. Launch Date1977 |
||
Sources: https://www.drugs.com/mtm/optimine.html |
Palliative | OPTIMINE Approved UseAzatadine is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; itching; and other symptoms of allergies and the common cold. Launch Date1977 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
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1.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21737359/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
AZATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21737359/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
AZATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21737359/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
AZATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
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OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
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Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/11996015/ |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes |
PubMed
Title | Date | PubMed |
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Demonstration of inhibition of mediator release from human mast cells by azatadine base. In vivo and in vitro evaluation. | 1986 Jan 10 |
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"In vivo" and "in vitro" evaluation of four antihistamines (astemizole, azatadine, mequitazine, terfenadine). | 1989 Mar-Apr |
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The effect of antihistamines on the immediate allergic response: a comparative review. | 1993 Jun |
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Fungal biotransformation of the antihistamine azatadine by Cunninghamella elegans. | 1996 Sep |
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Antiallergic effects of H1-receptor antagonists. | 2000 |
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Chromatographic analysis of phenethylamine-antihistamine combinations using C8, C18 or cyano columns and micellar sodium dodecyl sulfate-pentanol mixtures. | 2001 Apr |
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Quantitation of antihistamines in pharmaceutical preparations by liquid chromatography with a micellar mobile phase of sodium dodecyl sulfate and pentanol. | 2001 Nov-Dec |
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Antiallergic anti-inflammatory effects of H1-antihistamines in humans. | 2002 |
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The use of antiserotonin drugs in the nucleoreticular vestibular syndrome: preliminary observations. | 2004 |
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Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/mtm/optimine.html
The maximum amount of azatadine that you should take in 1 day is 2 mg. Azatadine can be taken with or without food.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2424773
Azatadine 0.1-10 uM significantly and dose dependently inhibited the release of leukotrienes from lung by 22-71%. Histamine release was also inhibited by azatadine 10 uM.
Substance Class |
Chemical
Created
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Record UNII |
94Z39NID6C
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WHO-VATC |
QR06AX09
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WHO-ATC |
R06AX09
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NCI_THESAURUS |
C29578
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C77430
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Azatadine
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AZATADINE
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19861
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |