Fexofenadine hydrochloride
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Fexofenadine hydrochloride
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CAS No:
153439-40-8
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Formula:
C32H39NO4.ClH
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Chemical Name:
Fexofenadine hydrochloride
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Synonyms:
Benzeneacetic acid,4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-α,α-dimethyl-,hydrochloride (1:1);Benzeneacetic acid,4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-α,α-dimethyl-,hydrochloride;MDL 16455A;Fexofenadine hydrochloride;Allegra;Telfast;Telfast BD;Alernex;Fexo;Fexofen;Feksine;Fexadyne;Vivafeks;Fastofen;Fexodine;Rapido;2-(4-[1-Hydroxy-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butyl]phenyl)-2-methylpropanoic acid hydrochloride;138452-21-8
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CAS No:
Description
Off-White Crystalline SolidFexofenadine hydrochloride (trade name: Allegra) belongs to a second-generation antihistamine pharmaceutical drug. It is mainly used for the treatment of allergy symptoms including watery eyes, hay fever, nasal congestion, urticaria, runny nose, itching eyes/nose, sneezing, hives, and itching. It is a kind of selectively peripheral H1 blocker. Its mechanism of action in vivo is through preventing the histamine-mediated activation of the H1 receptors, thus alleviating
Fexofenadine hydrochloride is a diarylmethane.|Fexofenadine is a second generation antihistamine that is used for the treatment of allergic rhinitis, angioedema and chronic urticaria. Fexofenadine has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent acute liver injury.|Fexofenadine Hydrochloride is the hydrochloride salt form of fexofenadine, a carboxylated metabolic derivative of terfenadine and second generation, long-lasting selective histamine H1 receptor antagonist, with antihistaminic activity. Upon administration, fexofenadine competitively binds of peripheral H1-receptors in the gastrointestinal (GI) tract, blood vessels, and bronchial smooth muscle. This prevents binding of histamine to peripheral H1-receptors and prevents their activation. This prevents a histamine-mediated allergic reaction. Fexofenadine does not cross the blood-brain-barrier (BBB).
Fexofenadine hydrochloride Basic Attributes
538.12
537.265
1308068-626-2
758678
DTXSID5048716
C29050
2933399090
Characteristics
81
white to beige
148-150oC
Soluble in Dimethyl sulfoxide (50 mM), and methanol.
−20°C
Safety Information
3
36/37/38
26-36
CY1633377
Xi
Commercially available fexofenadine hydrochloride capsules have an expiration date of 18 or 24 months after the date of manufacture when packaged in the manufacturer's unopened blister packages or high-density polyethylene bottles, respectively. Commercially available fexofenadine hydrochloride 30-mg conventional tablets have an expiration date of 18 months after the date of manufacture when packaged either in the manufacturer's unopened blister packages or high-density polyethylene bottles, whe
P201, P202, P261, P264, P270, P272, P280, P281, P301+P312, P302+P352, P305+P351+P338, P308+P313, P312, P321, P322, P330, P332+P313, P333+P313, P337+P313, P362, P363, P405, P501
H302
|Danger|H302 (25%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P261, P264, P270, P272, P280, P281, P301+P312, P302+P352, P305+P351+P338, P308+P313, P312, P321, P322, P330, P332+P313, P333+P313, P337+P313, P362, P363, P405, and P501|Aggregated GHS information provided by 6 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Toxicity
Fexofenadine use is not generally associated with liver enzyme elevations but terfenadine, a second generation antihistamine that is metabolized in part to fexofenadine, was the attributed cause of several reported cases of clinically apparent liver injury. Terfenadine was also linked to cardiac arrhythmias and prolongation of the QTc interval for which reason it was withdrawn from use in 1997, just as fexofenadine was introduced. Liver injury from terfenadine typically arose after 1 to 5 months and was associated with a hepatocellular pattern of liver enzyme abnormalities without immunoallergic or autoimmune features. Fexofenadine has not been linked to similar cases of cardiac arrhythmias or liver injury.
Drug Information
Fexofenadine is a second generation antihistamine that is used for the treatment of allergic rhinitis, angioedema and chronic urticaria. Fexofenadine has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent acute liver injury.
Antihistamines
A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment. (See all compounds classified as Histamine H1 Antagonists, Non-Sedating.)|Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475) (See all compounds classified as Anti-Allergic Agents.)
Allegra
Fexofenadine hydrochloride Use and Manufacturing
Fexofenadine is a non-sedating antihistamine that selectively antagonizes the histamine H1 receptor with a Ki value of 10 nM and exhibits anti-inflammatory effects. It is devoid of central nervous system effects in part because it is a good substrate for the P-glycoprotein efflux pump situated within the blood-brain barrier.[Cayman Chemical]
Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients
Computed Properties
Molecular Weight:538.1
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:10
Exact Mass:537.2645865
Monoisotopic Mass:537.2645865
Topological Polar Surface Area:81
Heavy Atom Count:38
Complexity:678
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes
Drug Function and Efficacy
An antihistamine with selective peripheral H1 receptor antagonism. It cannot cross the blood-brain barrier, and no sedation or other central nervous system effects, anticholinergic, α1-adrenergic or β-adrenergic receptor blocking effects have been observed.
Registered Holders
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THINQ PHARMA-CRO LTD
Active
United States
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CHEMECA DRUGS PRIVATE LTD
Active
United States
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Vasudha Pharma Chem Ltd
Active
United States
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