Details
Stereochemistry | RACEMIC |
Molecular Formula | C20H24N2 |
Molecular Weight | 292.418 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C1=C(CCN(C)C)CC2=C1C=CC=C2)C3=CC=CC=N3
InChI
InChIKey=MVMQESMQSYOVGV-UHFFFAOYSA-N
InChI=1S/C20H24N2/c1-15(19-10-6-7-12-21-19)20-17(11-13-22(2)3)14-16-8-4-5-9-18(16)20/h4-10,12,15H,11,13-14H2,1-3H3
DescriptionSources: https://www.drugbank.ca/drugs/DB08801
Sources: https://www.drugbank.ca/drugs/DB08801
Dimetindene (trade name Fenistil; other name dimethindene maleate) is a potent antipruritic antihistamine, characterized by the small size of its effective dose and its rapidity of action. Dimetindene is an antihistamine/anticholinergic that is a selective H1 antagonist. Its effect sets in after 20 to 60 minutes and lasts several hours. Dimetindene drops as well as Dimetindene syrup is particularly indicated in pediatric practice. Dimetindene is indicated as symptomatic treatment of allergic reactions: urticaria, allergies of the upper respiratory tract such as hay fever and perennial rhinitis, food, and drug allergies; pruritus of various origins, except pruritus due to cholestasis; insect bites. Dimetindene is also indicated for pruritus in eruptive skin diseases such as chicken-pox. Dimetindene can be as an adjuvant in eczema and other pruriginous dermatoses of allergic origin.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12593665 |
0.692 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Sources: http://pcm.me/fenistil-%C2%AE/ |
Primary | Fenistil Approved UseUnknown |
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Sources: http://pcm.me/fenistil-%C2%AE/ |
Primary | Fenistil Approved UseUnknown |
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Sources: http://pcm.me/fenistil-%C2%AE/ |
Primary | Fenistil Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
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14.6 ng/mL |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
DIMETHINDENE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
101.3 ng × h/mL |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
DIMETHINDENE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.41 h |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
DIMETHINDENE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
0.28 mg 2 times / day multiple, intranasal Recommended Dose: 0.28 mg, 2 times / day Route: intranasal Route: multiple Dose: 0.28 mg, 2 times / day Sources: |
unhealthy, 18 -69 n = 76 Health Status: unhealthy Condition: seasonal allergic rhinitis Age Group: 18 -69 Sex: M+F Population Size: 76 Sources: |
|
0.1 % 1 times / day single, topical Highest studied dose Dose: 0.1 %, 1 times / day Route: topical Route: single Dose: 0.1 %, 1 times / day Sources: |
healthy, 33 (21-54) n = 24 Health Status: healthy Age Group: 33 (21-54) Sex: M+F Population Size: 24 Sources: |
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6 mg 1 times / day single, oral Highest studied dose Dose: 6 mg, 1 times / day Route: oral Route: single Dose: 6 mg, 1 times / day Sources: |
healthy, adult n = 60 Health Status: healthy Age Group: adult Sex: M Population Size: 60 Sources: |
PubMed
Title | Date | PubMed |
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[Mesenteric traction syndrome during the operation of aneurysms of the abdominal aorta--histamine release and prophylaxis with antihistaminics]. | 2003 |
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Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists. | 2003 Feb 27 |
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Effects of dimethindene maleate nasal spray on the quality of life in seasonal allergic rhinitis. | 2003 Sep |
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[Prescription and safety of dimethindene maleate micropellet capsules in Hungary]. | 2004 Feb 15 |
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[Systemic mastocytosis. Classification, symptoms, therapy]. | 2004 Mar 15 |
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Antimuscarinic agents exhibit local inhibitory effects on muscarinic receptors in bladder-afferent pathways. | 2005 Feb |
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Acute ST-segment elevation myocardial infarction after amoxycillin-induced anaphylactic shock in a young adult with normal coronary arteries: a case report. | 2005 Feb 25 |
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A simplified premedication schedule for 1-hour paclitaxel administration. | 2005 Jan-Feb |
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Comparison of capillary zone electrophoresis and isotachophoresis determination of dimethindene enantiomers in pharmaceuticals using charged carboxyethyl-beta-cyclodextrin as a chiral selector. | 2006 Nov |
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[Aso an inspection of the family dog is warrented here]. | 2006 Oct 19 |
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Characterization of antihistamine-human serum protein interactions by capillary electrophoresis. | 2007 Apr 20 |
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Determination of dimethindene enantiomers in pharmaceuticals by capillary electrophoresis with carboxyethyl-beta-cyclodextrin. | 2007 Jan |
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[Quincke's edema: diagnosis and management of 102 patients with sudden upper airway obstruction]. | 2007 Jun |
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Application of HILIC stationary phase to determination of dimethindene maleate in topical gel. | 2009 Aug 15 |
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Glioblastoma cells express functional cell membrane receptors activated by daily used medical drugs. | 2009 Dec |
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Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia. | 2010 Oct 1 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://pcm.me/fenistil-%C2%AE/
Drops: Infants up to 1 year, 10-30 drops; Infants of 1 to 3 years, 30-45 drops; Children over 3 years, 45-60 drops; Adults, 60-120 drops.
Syrup: Infants up to 1 year, 1-3 teaspoons; Infants of 1 to 3 years, 3-4 teaspoons; Children over 3 years, 4-6 teaspoons; Adults, 6-12 teaspoons. 1 teasponful Fenistil syrup = 5ml = 0.5mg
Coated tablets: Adults, 3-6 tablets.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6832322
Experiments were carried out on isolated right ventricular papillary muscle of cat and guinea-pig, and on left atrial muscle of guinea-pig. The animals were anesthetized
with ether, and the muscles were dissected from the heart as quickly as possible and mounted in an organ chamber. The preparations were driven electrically at 2.0 or 0.5 Hz. The transmembrane potentials were recorded by means of conventional glass microelectrode technique. The slow response APs were elicited with histamine (10^-5 M) ) or caffeine (2 mM) in partially depolarized (up to -40 mV) left atrial and right ventricular.myocardium of guinea-pigs. The membrane was depolarized by means of elevated K + (26 mM)-Krebs solution. Dimetindene was freshly dissolved and added to the organ chamber containing Krebs solution (composition in mM): NaC1 118, KCl 4.7, CaC12 2.5, NaH2PO4 1.0, MgC12 1.2, NaHCO3 24.9, glucose 11.5, which was gassed with 95% 02 and 5% CO2 and kept at 37C
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Classification Tree | Code System | Code | ||
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WHO-ATC |
D04AA13
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WHO-ATC |
R06AB03
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WHO-VATC |
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QR06AB03
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NCI_THESAURUS |
C29578
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903
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D004115
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C83675
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Dimetindene
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21855
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5636-83-9
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SUB07179MIG
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m4508
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100000082645
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661FH77Z3P
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661FH77Z3P
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1403
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DB08801
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DTXSID9022942
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CHEMBL22108
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3449
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227-083-8
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)