Histamine H1 Antagonists, Non-Sedating

Name
Histamine H1 Antagonists, Non-Sedating
Accession Number
DBCAT000772
Description

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.

Drugs
DrugDrug Description
CetirizineA selective Histamine-1 antagonist drug used in allergic rhinitis and chronic urticaria.
LoratadineA second generation antihistamine used to manage the symptoms of allergic rhinitis.
FexofenadineA selective H1-antagonist for the symptomatic treatment of seasonal allergic rhinitis and chronic idiopathic urticaria.
DesloratadineA second generation tricyclic antihistamine used to treat seasonal and non seasonal allergic rhinitis, pruritus, and urticaria.
TerfenadineFor the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
AstemizoleA second generation antihistamine used to treat allergy symptoms.
OlopatadineA histamine H1 antagonist used to treat allergic conjunctivitis and rhinitis.
AzelastineA histamine H1-receptor antagonist used intranasally to treat allergic and vasomotor rhinitis and in an ophthalmic solution to treat allergic conjunctivitis.
LevocabastineA selective histamine H1 receptor antagonist indicated for the management of seasonal allergic conjunctivitis symptoms.
LevocetirizineAn H1-receptor antagonist used to treat symptoms associated with chronic allergic rhinitis and uncomplicated cases of chronic idiopathic urticaria.
AcrivastineAn antihistamine agent used for the symptomatic relief of seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion.
MizolastineMizolastine is under investigation in clinical trial NCT01928316 (A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers).
BilastineA peripheral histamine H1-antagonist used to treat seasonal allergic rhinitis and chronic spontaneous urticaria.
RupatadineA selective histamine H1 receptor antagonist and platelet activating factor (PAF) antagonist used to treat allergic rhinitis.
Drugs & Drug Targets
DrugTargetType
CetirizineHistamine H1 receptortarget
CetirizineP-glycoprotein 1transporter
LoratadineHistamine H1 receptortarget
LoratadineCytochrome P450 3A4enzyme
LoratadineCytochrome P450 2C19enzyme
LoratadineCytochrome P450 2D6enzyme
LoratadineCytochrome P450 2C8enzyme
LoratadineP-glycoprotein 1transporter
LoratadinePotassium voltage-gated channel subfamily H member 2target
LoratadineBile salt export pumptransporter
LoratadineCytochrome P450 1A1enzyme
LoratadineCytochrome P450 1A2enzyme
LoratadineCytochrome P450 2B6enzyme
LoratadineCytochrome P450 2C9enzyme
LoratadineCytochrome P450 3A5enzyme
LoratadineUDP-glucuronosyltransferase 2B10enzyme
LoratadineUDP-glucuronosyltransferase 1-1enzyme
LoratadineUDP-glucuronosyltransferase 1-3enzyme
LoratadineUDP-glucuronosyltransferase 2B15enzyme
FexofenadineHistamine H1 receptortarget
FexofenadineP-glycoprotein 1transporter
FexofenadineSolute carrier organic anion transporter family member 2B1transporter
FexofenadineSolute carrier organic anion transporter family member 1A2transporter
FexofenadineSolute carrier organic anion transporter family member 1B1transporter
FexofenadineSolute carrier organic anion transporter family member 1B3transporter
FexofenadineSolute carrier family 22 member 8transporter
FexofenadineCanalicular multispecific organic anion transporter 1transporter
FexofenadineCanalicular multispecific organic anion transporter 2transporter
FexofenadineSerum albumincarrier
Fexofenadinealpha1-acid glycoproteincarrier
DesloratadineHistamine H1 receptortarget
DesloratadineP-glycoprotein 1transporter
TerfenadineHistamine H1 receptortarget
TerfenadinePotassium voltage-gated channel subfamily H member 2target
TerfenadineCytochrome P450 3A4enzyme
TerfenadineCytochrome P450 2D6enzyme
TerfenadineMuscarinic acetylcholine receptor M3target
TerfenadineCytochrome P450 3A5enzyme
TerfenadineCytochrome P450 3A7enzyme
TerfenadineP-glycoprotein 1transporter
TerfenadineCytochrome P450 2C8enzyme
TerfenadineCytochrome P450 2J2enzyme
TerfenadineMuscarinic acetylcholine receptor M1target
TerfenadineMuscarinic acetylcholine receptor M5target
TerfenadineMuscarinic acetylcholine receptor M4target
TerfenadineMuscarinic acetylcholine receptor M2target
TerfenadineBile salt export pumptransporter
AstemizoleHistamine H1 receptortarget
AstemizolePotassium voltage-gated channel subfamily H member 2target
AstemizoleCytochrome P450 3A4enzyme
AstemizoleCytochrome P450 3A5enzyme
AstemizoleCytochrome P450 3A7enzyme
AstemizoleP-glycoprotein 1transporter
AstemizoleCytochrome P450 2D6enzyme
AstemizoleCytochrome P450 2J2enzyme
AstemizolePotassium voltage-gated channel subfamily H member 1target
AstemizoleMicrotubule-associated protein tautarget
AstemizoleBile salt export pumptransporter
OlopatadineHistamine H1 receptortarget
OlopatadineProtein S100-A1target
OlopatadineProtein S100-A12target
OlopatadineProtein S100-Btarget
OlopatadineProtein S100-A13target
OlopatadineProtein S100-A2target
OlopatadineCytochrome P450 3A4enzyme
OlopatadineSerum albumincarrier
OlopatadineDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
OlopatadineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
OlopatadineP-glycoprotein 1transporter
OlopatadineHistamine H2 receptortarget
OlopatadineHistamine H3 receptortarget
AzelastineHistamine H1 receptortarget
AzelastineCytochrome P450 1A2enzyme
AzelastineCytochrome P450 2D6enzyme
AzelastineCytochrome P450 3A4enzyme
AzelastineCytochrome P450 2C19enzyme
AzelastineCytochrome P450 1A1enzyme
AzelastineCytochrome P450 3A5enzyme
AzelastineCytochrome P450 2C9enzyme
AzelastineCytochrome P450 2C8enzyme
AzelastineP-glycoprotein 1transporter
AzelastineCytochrome P450 2A6enzyme
AzelastineCytochrome P450 2E1enzyme
AzelastineHistamine H2 receptortarget
AzelastinePhospholipase A2target
AzelastineLeukotriene C4 synthasetarget
AzelastineCytochrome P450 2B6enzyme
LevocabastineNeurotensin receptor type 2target
LevocabastineHistamine H1 receptortarget
LevocetirizineHistamine H1 receptortarget
LevocetirizineSolute carrier family 22 member 11transporter
LevocetirizineCytochrome P450 3A4enzyme
LevocetirizineSerum albumincarrier
AcrivastineHistamine H1 receptortarget
MizolastineCytochrome P450 2D6enzyme
BilastineHistamine H1 receptortarget
BilastineATP-binding cassette sub-family B member 5transporter
BilastineSolute carrier organic anion transporter family member 1A2transporter
BilastineSolute carrier organic anion transporter family member 2B1transporter
RupatadineCytochrome P450 3A4enzyme
RupatadineCytochrome P450 2C9enzyme
RupatadineCytochrome P450 2C19enzyme
RupatadineCytochrome P450 2D6enzyme
RupatadinePlatelet-activating factor receptortarget
RupatadineHistamine H1 receptortarget