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H1 receptor antagonists

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Aripiprazole (129722-12-9)

Aripiprazole, sold under the brand name Abilify among others, is an atypical antipsychotic. From April 2013 to March 2014, sales of Abilify amounted to almost $6.9 billion.. It is recommended by some doctors and used in the treatment of schizophrenia and bipolar disorder.

Risperidone (106266-06-2)

Risperidone, sold under the trade name Risperdal among others, is an antipsychotic medication. It is mainly used to treat schizophrenia, bipolar disorder, and irritability in people with autism. It is taken either by mouth or by injection into a muscle.

azelastine (58581-89-8)

Astelin · Optivar · azelastine hydrochloride

Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H1-receptor antagonist) used as a first line therapy of mild intermittent, moderate/severe intermittent and mild persistent rhinitis (new classification system for rhinitis). Azelastine has been formulated both as a nasal spray and as eye drops and are available worldwide under many brand names.

BROMPHENIRAMINE (86-22-6)

Dimetane · Brompheniramine Maleate · Chlorphed

Brompheniramine (Bromfed, Dimetapp, Bromfenex, Dimetane, BPN, Lodrane), commonly marketed as its salt brompheniramine maleate, 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.

chlorpheniramine (113-92-8, 32188-09-3, 132-22-9)

Chlorpheniramine Maleate · Teldrin · Piriton

Chlorphenamine (also known as chlorpheniramine, CP, or CPM) is a first-generation antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria. Its sedative effects are relatively weak compared to other first-generation antihistamines. Chlorphenamine is one of the most commonly used antihistamines in small-animal veterinary practice.

fexofenadine (83799-24-0)

Allegra · fexofenadine hydrochloride · Aventis brand of fexofenadine hydrochloride

Fexofenadine, sold under the trade name Allegra among others is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria. Therapeutically, fexofenadine is a selective peripheral H1-blocker. Fexofenadine is classified as a second-generation antihistamine because it is less able to pass the blood-brain barrier and cause sedation, compared to first-generation antihistamines.

astemizole (68844-77-9)

Hismanal · Romadin · Elfar Brand of Astemizole

Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that has a long duration of action. Astemizole was discovered by Janssen Pharmaceutica in 1977. It has been withdrawn from the market in most countries because of rare but potentially fatal side effects (QTc interval prolongation and related arrhythmias due to hERG channel blockade).

mirtazapine (61337-67-5, 85650-52-8)

Remeron · Rexer · ORG 3770

Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant which is used primarily in the treatment of depression. In addition to its antidepressant properties, mirtazapine has anxiolytic, sedative, antiemetic, and appetite stimulant effects and is sometimes used in the treatment of anxiety disorders, insomnia, nausea and vomiting, and to produce weight gain when desirable. It is taken by mouth.

METHDILAZINE (1982-37-2)

methdilazine hydrochloride

Methdilazine (Dilosyn, Tacaryl) is a first-generation antihistamine with anticholinergic properties of the phenothiazine class.

loratadine (79794-75-5)

Claritin · Alavert · Clarium

Loratadine, sold under the brand name Claritin among others, is a medication used to treat allergies. This includes allergic rhinitis (hay fever) and hives. It is also available in combination with pseudoephedrine, a decongestant, known as loratadine/pseudoephedrine.

antazoline (91-75-8)

Antistine · Antazoline Phosphate · Antazoline Hydrochloride

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.

orphenadrine (83-98-7)

Norflex · Orphenadrine Citrate · Disipal

Orphenadrine (sold under many brand names worldwide) is an anticholinergic drug of the ethanolamine antihistamine class; it is closely related to diphenhydramine. It is used to treat muscle pain and to help with motor control in Parkinson's disease, but has largely been superseded by newer drugs. It was discovered and developed in the 1940s.

clemastine (15686-51-8)

Clemastine, also known as meclastin, is an antihistamine and anticholinergic. Unlike loratadine or fexofenadine, clemastine is a sedating antihistamine; however, it exhibits fewer other side effects than most of the widely used antihistamines. Clemastine is also classified as an antipruritic (i.e., it stops itching).

Desloratadine (100643-71-8)

Desloratadine (trade name Clarinex in the US and Aerius in Europe) is a tricyclic H1-antihistamine that is used to treat allergies. It is an active metabolite of loratadine.

methapyrilene (91-80-5)

Thionylan · Lullamin · Tenalin

Cinnarizine-d8 (298-57-7)

tripelennamine (91-81-6)

Pyribenzamine · Tripelennamine Hydrochloride · Tripelennamine Citrate

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.

propiomazine (362-29-8)

Largon

Propiomazine (Largon, Propavan, Indorm, Serentin, Dorevane, Dorevan) is an antihistamine blocking H1 receptors. It is used to treat insomnia, and to produce sleepiness or drowsiness and to relieve anxiety before or during surgery or other procedures and in combination with analgetics also during labor. Propiomazine is a phenothiazine, but is not used as a neuroleptic because it does not block dopamine receptors well.

cinnarizine (298-57-7, 16699-20-0)

Cinna · Stugeron · R 516

Cinnarizine is an antihistamine and calcium channel blocker of the diphenylmethylpiperazine group. It is also known to promote cerebral blood flow, and so is used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis. However, it is more commonly prescribed for nausea and vomiting due to motion sickness or other sources such as chemotherapy, vertigo, or Ménière's disease.

DEXCHLORPHENIRAMINE (25523-97-1)

Polaramine · dexchlorpheniramine maleate · Polaramin

Dexchlorpheniramine (trade name Polaramine) 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 chlorpheniramine.

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