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Status:
US Approved OTC
Source:
21 CFR 341.12(d) cough/cold:antihistamine dexbromopheniramine maleate
Source URL:
First approved in 1959
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
DEXBROMPHENIRAMINE is an alkylamine derivative with anticholinergic and sedative properties. It is a histamine H1-receptor antagonist that competes with histamine for the H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. The antagonistic action of this agent blocks the activities of endogenous histamine, which subsequently leads to temporary relief from the negative histamine-mediated symptoms of an allergic reaction such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of the gastrointestinal smooth muscle. DEXBROMPHENIRAMINE as a part of combination medicine is used to treat symptoms of the common cold or seasonal allergies, including sneezing, runny or stuffy nose, and itchy, watery eyes.
Status:
US Approved OTC
Source:
21 CFR 341.12(k) cough/cold:antihistamine pyrilamine maleate
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Pyrilamine (also known as Mepyramine) is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect. It is used in over-the-counter combination products for colds and menstrual symptoms. Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Mepyramine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of Mepyramine occur at the subcortical level of the CNS. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
Status:
US Previously Marketed
Source:
SEMPREX-D by ENDO OPERATIONS
(1994)
Source URL:
First approved in 1994
Source:
SEMPREX-D by ENDO OPERATIONS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Acrivastine is a triprolidine analog antihistamine indicated for the treatment of allergies and hay fever. As an H1 receptor antagonist, it functions by blocking the action of histamine at this receptor thereby preventing the symptoms associated with histamine release such as pruritis, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia. Acrivastine is currently available in combination with pseudoephedrine as the FDA-approved product Semprex-D. It’s used for the relief of symptoms associated with seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion. Acrivastine, a structural analog of triprolidine hydrochloride, exhibits H1-antihistaminic activity in isolated tissues, animals, and humans, and has sedative effects in humans. The propionic acid derivative of acrivastine is a metabolite in several animal species (as well as in man) and also exhibits H1-antihistaminic activity.
Status:
US Previously Marketed
Source:
OPTIMINE by SCHERING
(1977)
Source URL:
First approved in 1977
Source:
OPTIMINE by SCHERING
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
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.
Status:
US Approved OTC
Source:
21 CFR 341.12(d) cough/cold:antihistamine dexbromopheniramine maleate
Source URL:
First approved in 1959
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
DEXBROMPHENIRAMINE is an alkylamine derivative with anticholinergic and sedative properties. It is a histamine H1-receptor antagonist that competes with histamine for the H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. The antagonistic action of this agent blocks the activities of endogenous histamine, which subsequently leads to temporary relief from the negative histamine-mediated symptoms of an allergic reaction such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of the gastrointestinal smooth muscle. DEXBROMPHENIRAMINE as a part of combination medicine is used to treat symptoms of the common cold or seasonal allergies, including sneezing, runny or stuffy nose, and itchy, watery eyes.
Status:
US Approved OTC
Source:
21 CFR 341.12(d) cough/cold:antihistamine dexbromopheniramine maleate
Source URL:
First approved in 1959
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
DEXBROMPHENIRAMINE is an alkylamine derivative with anticholinergic and sedative properties. It is a histamine H1-receptor antagonist that competes with histamine for the H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. The antagonistic action of this agent blocks the activities of endogenous histamine, which subsequently leads to temporary relief from the negative histamine-mediated symptoms of an allergic reaction such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of the gastrointestinal smooth muscle. DEXBROMPHENIRAMINE as a part of combination medicine is used to treat symptoms of the common cold or seasonal allergies, including sneezing, runny or stuffy nose, and itchy, watery eyes.
Status:
US Approved OTC
Source:
21 CFR 341.12(k) cough/cold:antihistamine pyrilamine maleate
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Pyrilamine (also known as Mepyramine) is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect. It is used in over-the-counter combination products for colds and menstrual symptoms. Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Mepyramine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of Mepyramine occur at the subcortical level of the CNS. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
Status:
US Approved OTC
Source:
21 CFR 341.12(k) cough/cold:antihistamine pyrilamine maleate
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Pyrilamine (also known as Mepyramine) is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect. It is used in over-the-counter combination products for colds and menstrual symptoms. Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Mepyramine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of Mepyramine occur at the subcortical level of the CNS. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.