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CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.020.626 |
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Formula | C18H23NO |
Molar mass | 269.388 g·mol−1 |
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Moxastine (also known as mephenhydramine) is an antihistamine and anticholinergic.
It was developed in Czechoslovakia and sold in hydrochloride form as an antihistamine (Alfadryl).
It is, with 8-chlorotheophylline, a component of cocrystal/salt moxastine teoclate (mephenhydrinate) used as antiemetic (Theadryl; Kinedryl (with caffeine)).
Triprolidine is an over-the-counter antihistamine with anticholinergic properties. It is used to combat the symptoms associated with allergies and is sometimes combined with other cold medications designed to provide general relief for flu-like symptoms. As with many antihistamines, the most common side effect is drowsiness.
H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines.
Loratadine, sold under the brand name Claritin among others, is a medication used to treat allergies. This includes allergic rhinitis and hives. It is also available in combination with pseudoephedrine, a decongestant, known as loratadine/pseudoephedrine. It is taken by mouth.
Brompheniramine, sold under the brand name Dimetapp among others, is an antihistamine drug of the propylamine (alkylamine) class. It is readily available over the counter and is indicated for the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing. It is a first-generation antihistamine and one of the drugs of highest anticholinergic activity.
Chlorphenamine, also known as chlorpheniramine, is an antihistamine used to treat the symptoms of allergic conditions such as allergic rhinitis. It is taken by mouth. The medication takes effect within 6 hours and lasts for about a day.
Hives, also known as urticaria, is a kind of skin rash with red, raised, itchy bumps. They may also burn or sting. Often the patches of rash move around. Typically they last a few days and do not leave any long-lasting skin changes. Fewer than 5% of cases last for more than six weeks. The condition frequently recurs.
Cetirizine, sold under the brand name Zyrtec among others, is a second-generation antihistamine used to treat allergic rhinitis, dermatitis, and urticaria. It is taken by mouth. Effects generally begin within an hour and last for about a day. The degree of benefit is similar to other antihistamines such as diphenhydramine.
Fexofenadine, sold under the trade name Allegra & FX 24 among others is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever and urticaria. Therapeutically, fexofenadine is a selective peripheral H1-blocker.
Clemastine, also known as meclastin, is an ethanolamine-derivative, first generation histamine H1 antagonist (antihistamine) with anticholinergic properties (drying) and sedative side effects. Like all first generation antihistamines, it is sedating.
Levocetirizine, sold under the brand name Xyzal among others, is an antihistamine used for the treatment of allergic rhinitis and long term hives of unclear cause. It is less sedating than older antihistamines. It is taken by mouth.
Dexbrompheniramine is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. It is the pharmacologically active dextrorotatory isomer of brompheniramine. It was formerly marketed in combination with pseudoephedrine under the name Drixoral in the US and Canada. It is an alkylamine antihistamine.
Methapyrilene is an antihistamine and anticholinergic of the pyridine chemical class which was developed in the early 1950s. It was sold under the trade names Co-Pyronil and Histadyl EC. It has relatively strong sedative effects, to the extent that its primary use was as a medication for insomnia rather than for its antihistamine action. Together with scopolamine, it was the main ingredient in Sominex, Nytol, and Sleep-Eze. It also provided the sedative component of Excedrin PM. All of these products were reformulated in the late 1970s when methapyrilene was demonstrated to cause liver cancer in rats when given chronically.
Tripelennamine, sold under the brand name Pyribenzamine by Novartis, is a drug that is used as an antipruritic and first-generation antihistamine. It can be used in the treatment of asthma, hay fever, rhinitis and urticaria, but is now less common as it has been replaced by newer antihistamines. The drug was patented at CIBA, which merged with Geigy into Ciba-Geigy, and eventually becoming Novartis.
Tricyclics are chemical compounds that contain three interconnected rings of atoms.
Mepyramine, also known as pyrilamine, is a first generation antihistamine, targeting the H1 receptor as an inverse agonist. It rapidly permeates the brain often causing drowsiness. It also has anticholinergic properties. However, its anticholinergic potency is negligible compared to its antihistaminergic activity; it has an H1 to muscarinic Ki ratio of 130,000 to 1, compared to a ratio of 20 to 1 for diphenhydramine.
Bamipine (trade name Soventol) is a pharmaceutical drug acting as an H1 antihistamine with anticholinergic properties. It is used as an antipruritic ointment. No oral use is known.
Antihistamines are drugs which treat allergic rhinitis and other allergies. Typically people take antihistamines as an inexpensive, generic, over-the-counter drug that can provide relief from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use.
Antazoline is a 1st generation antihistamine with anticholinergic properties used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis. To treat allergic conjunctivitis, antazoline can be combined in a solution with tetryzoline. The drug is a Histamine H1 receptor antagonist: selectively binding to but not activating the receptor, thereby blocking the actions of endogenous histamine and subsequently leading to the temporary relief of the negative symptoms brought on by histamine.
Thiazinamium metilsulfate (INN) or thiazinam is an antihistamine. The USAN is thiazinamium chloride.
Piperoxan, also known as benodaine, is a drug which was the first antihistamine to be discovered. This compound, derived from benzodioxan, was prepared in the early 1930s by Daniel Bovet and Ernest Fourneau at the Pasteur Institute in France. Formerly investigated by Fourneau as an α-adrenergic-blocking agent, they demonstrated that it also antagonized histamine-induced bronchospasm in guinea pigs, and published their findings in 1933. Bovet went on to win the 1957 Nobel Prize in Physiology or Medicine for his contribution, and one of their students, Anne-Marie Staub, published the first structure-activity relationship (SAR) study of antihistamines in 1939.
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