Histamine H1 Antagonists
- Name
- Histamine H1 Antagonists
- Accession Number
- DBCAT000665 (DBCAT003330)
- Description
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
- Drugs
Drug Drug Description Aceprometazine Aceprometazine is often used in combination with meprobamate for the treatment of sleep disorders. Acrivastine An antihistamine agent used for the symptomatic relief of seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion. Alcaftadine A H1 histamine receptor antagonist for ophthalmic use to prevent itching associated with allergic conjunctivitis. Alimemazine An antihistamine agent used to prevent and relieve allergic conditions which cause pruritus and other allergic skin conditions, including urticaria. Amitriptyline A tricyclic antidepressant indicated in the treatment of depressive illness, either endogenous or psychotic, and to relieve depression associated anxiety. Amoxapine A tricyclic antidepressant used in the treatment of neurotic or reactive depressive disorders and endogenous or psychotic depression. Antazoline An antihistamine agent used for the symptomatic treatment of nasal congestion and allergic conjunctivitis. Aripiprazole An atypical antipsychotic used in the treatment of a wide variety of mood and psychotic disorders, such as schizophrenia, bipolar I, major depressive disorder, irritability associated with autism, and Tourette's syndrome. Aripiprazole lauroxil An antipsychotic used to treat schizophrenia in adults. Asenapine An atypical antipsychotic used to treat patients with bipolar I disorder and patients with schizophrenia. Astemizole A second generation antihistamine used to treat allergy symptoms. Azatadine An H1 receptor antagonist used to treat perennial and allergic rhinitis as well as eustachian tube congestion. Azelastine A histamine H1-receptor antagonist used intranasally to treat allergic and vasomotor rhinitis and in an ophthalmic solution to treat allergic conjunctivitis. Benzatropine An anticholinergic drug used to treat Parkinson's disease (PD) and extrapyramidal symptoms, except tardive dyskinesia. Benzquinamide Used to prevent and treat nausea and vomiting associated with anesthesia and surgery, administered intramuscularly or intravenously. Bepotastine An ophthalmic H1 antagonist used to treat itchiness associated with allergic conjunctivitis. Bilastine A peripheral histamine H1-antagonist used to treat seasonal allergic rhinitis and chronic spontaneous urticaria. Bromodiphenhydramine For management of symptoms related to hay fever and other types of allergy and used to help bring up phlegm, thin secretions, and make a cough productive. Brompheniramine A histamine H1 antagonist used to treat coughs, upper respiratory symptoms, and nasal congestion associated with allergies and the common cold. Buclizine An antihistamine and antiemetic drug for the treatment of allergy symptoms and prevention of nausea and vomiting. Butriptyline Butriptyline is a tricyclic antidepressant which has been used in Europe since 1974. It is the isobutyl side chain homologue of amitriptyline. Carbinoxamine A first generation antihistamine used to treat allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis, allergic reactions, and mild allergic reactions. Cariprazine An atypical antipsychotic used to treat schizophrenia and acute manic or mixed episodes due to bipolar I disorder. Cetirizine A selective Histamine-1 antagonist drug used in allergic rhinitis and chronic urticaria. Chlorcyclizine Chlorcyclizine is a first generation phenylpiperazine class antihistamine used to treat urticaria, rhinitis, pruritus, and other allergy symptoms. Chlorcyclizine also has some local anesthetic, anticholinergic, and antiserotonergic properties, and can... Chloropyramine For the treatment of allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic (allergic) conditions. Chlorpheniramine A histamine-H1 receptor antagonist indicated for the management of symptoms associated with upper respiratory allergies. Chlorpromazine A phenothiazine antipsychotic used to treat nausea, vomiting, preoperative anxiety, schizophrenia, bipolar disorder, and severe behavioral problems in children. Chlorprothixene A thioxanthene antipsychotic. Cinnarizine A drug used for the management of labyrinthine disorder symptoms, including vertigo, tinnitus, nystagmus, nausea, and vomiting. Clemastine An antihistamine with sedative and anticholinergic effects used to treat the symptoms of allergic rhinitis. Clofedanol An antitussive used for the symptomatic relief of acute cough caused by minor throat and bronchial irritation. Clozapine An atypical or second-generation antipsychotic drug used in treatment-resistant schizophrenia and to decrease suicide risk in schizophrenic patients. Cyclizine An antihistamine and antiemetic drug used for the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness, and vertigo. Cyproheptadine A combined serotonin and histamine antagonist used in the treatment of allergic symptoms, for appetite stimulation, and off-label in the treatment of serotonin syndrome. Deptropine Not Annotated Desipramine A tricyclic antidepressant used in the treatment of depression. Desloratadine A second generation tricyclic antihistamine used to treat seasonal and non seasonal allergic rhinitis, pruritus, and urticaria. Dexbrompheniramine An antihistamine used to treat allergy symptoms including upper respiratory tract symptoms. Dexchlorpheniramine A chlorpheniramine enantiomer antihistamine indicated in the treatment of sunburns, insect bites, and allergic reactions of the skin. Dexchlorpheniramine maleate A first generation antihistamine used to treat allergic and vasomotor rhinitis, allergic conjunctivitis, and mild urticaria and angioedema. Dimenhydrinate A medication used to prevent and treat nausea, vomiting, vertigo, and motion sickness. Dimetindene A 1st generation selective H1 antagonist used topically as an antipruritic and orally to treat allergies. Dimetotiazine Dimetotiazine has considerable antiemetic & serotonin antagonistic action used mainly in allergic skin conditions. Diphenhydramine A H1 receptor antihistamine used in the treatment of seasonal allergies, and various allergic reactions including sneezing, runny nose, itchy/watery eyes, itching of nose or throat, pruritus, urticaria, insect bites/stings, and allergic rashes. Diphenylpyraline An antihistamine used for the treatment of allergic rhinitis, hay fever, and allergic skin disorders. Dosulepin A tricyclic antidepressant commonly used only in patients for whom alternative therapies are ineffective due to its toxicity potential. Doxepin A psychotropic agent used for the treatment of depression, anxiety, manic-depressive disorder, and insomnia. Doxylamine An antihistamine used to treat insomnia and allergy symptoms and is used with pyridoxine in the treatment of nausea and vomiting in pregnancy. Ebastine A second generation H1-receptor antagonist useful in the treatment of allergic rhinitis and urticaria. Emedastine A selective H1-receptor antagonist used topically to manage symptoms of allergic conjunctivitis. Epinastine An H1 receptor antagonist used to prevent itching in allergic conjunctivitis. Esmirtazapine Investigated for use/treatment in insomnia and sleep disorders. Fexofenadine A selective H1-antagonist for the symptomatic treatment of seasonal allergic rhinitis and chronic idiopathic urticaria. Flunarizine A selective calcium-entry blocker used as migraine prophylaxis in patients with severe and frequent episodes who have not responded adequately to more common treatments. GSK-1004723 Gsk1004723 has been investigated for the treatment of Allergic Rhinitis and Rhinitis, Allergic, Seasonal. Hydroxyzine An antihistamine used to treat anxiety and tension associated with psychoneuroses, as well as allergic conditions such as pruritus and chronic urticaria. Iloperidone An atypical antipsychotic agent used to treat schizophrenia and manic or mixed episodes associated with bipolar I disorder in adults. Imipramine A tricyclic antidepressant indicated for the treatment of depression and to reduce childhood enuresis. Isospaglumic acid Isospaglumic acid is a small molecule drug. Isospaglumic acid is under investigation in clinical trial NCT06800274 (Clinical and Biological Evaluation of NAAGA Versus Azelastine Eye Drops in Allergic Subjects With... Isothipendyl A 1st generation histamine H1 antagonist primarily applied topically as an antipruritic. Ketotifen A histamine H1 receptor blocker and mast cell stabilizer used to treat mild atopic asthma and allergic conjunctivitis. Levocabastine A selective histamine H1 receptor antagonist indicated for the management of seasonal allergic conjunctivitis symptoms. Levocetirizine An H1-receptor antagonist used to treat symptoms associated with chronic allergic rhinitis and uncomplicated cases of chronic idiopathic urticaria. Loratadine A second generation antihistamine used to manage the symptoms of allergic rhinitis. Maprotiline A tetracyclic antidepressant used to treat depressive illness, major depressive disorder, bipolar disorder, and anxiety associated with depression. Meclizine A histamine H1 antagonist used to treat nausea, vomiting, and dizziness associated with motion sickness. Mepyramine An antihistamine agent used for the symptomatic treatment of allergy, hypersensitivity reactions, and pruritic skin disorders. Mequitazine For the treatment of Hay fever, urticaria (hives) and allergic rhinitis Methapyrilene Methapyrilene, formerly marketed in many drug products, was shown to be a potent carcinogen. Manufacturers voluntarily withdrew methapyriline drug products from the market in May and June 1979. Methdilazine Used for the symptomatic relief of hypersensitivity reactions and particularly for the control of pruritic skin disorders Methotrimeprazine A phenothiazine used in the management of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder. Mianserin A tetracyclic antidepressant with therapeutic activity similar to amitriptyline used to treat depression and anxiety. Mirtazapine A tetracyclic antidepressant used in the treatment of major depression and is used off-label as a drug for insomnia and to increase appetite. Mizolastine A second-generation non-sedating antihistamine used to treat symptoms of allergic rhinoconjunctivitis and urticaria. Nortriptyline A tricyclic antidepressant used in the treatment of depression. Olanzapine An antipsychotic drug used in the management of schizophrenia, bipolar 1 disorder, and agitation associated with these disorders. Olopatadine A histamine H1 antagonist used to treat allergic conjunctivitis and rhinitis. Orphenadrine A muscarinic antagonist used as an adjunct for the symptomatic relief of musculoskeletal pain and discomfort. Oxatomide An antihistamine indicated in the treatment and prevention of allergic symptoms. Phenindamine Used to treat sneezing, runny nose, itching, watery eyes, hives, rashes, itching, and other symptoms of allergies and the common cold. Pheniramine An antihistamine used to treat allergic rhinitis and pruritus. Picumast Picumast is a small molecule drug. Picumast has a monoisotopic molecular weight of 440.19 Da. Pizotifen A serotonin and tryptamine antagonist indicated for migraine prophylaxis. Promazine A phenothiazine used to manage schizophrenia. Promethazine A first-generation antihistamine used for the treatment of allergic conditions, nausea and vomiting, and motion sickness. Propiomazine Propiomazine is largely used for its antihistamininc sleep inducing effects in treating insomnia. Proxicromil Proxicromil is a small molecule drug. Proxicromil has a monoisotopic molecular weight of 302.12 Da. Quetiapine An atypical antipsychotic agent used for the management of bipolar disorder, schizophrenia, and major depressive disorder. Risperidone A second-generation antipsychotic medication used to treat a number of mental health disorders including schizophrenia, bipolar mania, psychosis, or as an adjunct in severe depression. Rupatadine A selective histamine H1 receptor antagonist and platelet activating factor (PAF) antagonist used to treat allergic rhinitis. Temelastine Temelastine is a small molecule drug. The usage of the INN stem '-astine' in the name indicates that Temelastine is a antihistaminic. Temelastine has a monoisotopic molecular weight of 441.12... Terfenadine An antihistamine for the treatment of allergy symptoms. Thonzylamine Thozylamine is indicated for use in the symptomatic control of allergic rhinitis or other upper respiratory allergic symptoms [FDA Label]. It is typically a part of combination over the counter... Trazodone A serotonin uptake inhibitor used to treat major depressive disorder. Trimipramine A tricyclic antidepressant used to treat depression. Tripelennamine A histamine H1 antagonist used to treat hypersensitivity reactions, coughs, and the common cold. Triprolidine A sedating antihistamine combined with pseudoephedrine and guaifenesin in various types of cold and allergy medications to relieve allergy symptoms, hay fever and common cold symptoms, and to aid in sleep. Viloxazine A selective norepinephrine reuptake inhibitor indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in adults in children. Ziprasidone An atypical antipsychotic used to manage schizophrenia, bipolar mania, and agitation in patients with schizophrenia. Zuclopenthixol An antipsychotic indicated for the management of schizophrenia. The acuphase formulation is indicated for initial treatment of acute psychosis or exacerbation of psychosis, while the depot formulation is best for maintenance. - Drugs & Drug Targets