U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 271 - 280 of 1617 results

Status:
US Previously Marketed
Source:
Phenoxene by Pitman-Moore (Dow Chem., USA)
(1959)
Source URL:
First approved in 1959
Source:
Phenoxene by Pitman-Moore (Dow Chem., USA)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Chlorphenoxamine is an antihistamine and anticholinergic used as an antipruritic and was formerly used in the sympathomimetic treatment of parkinsonism. Histamine receptor H1 antagonist. Chlorphenoxamine is used to treat Allergic conditions, it is reported as an ingredient of Systral in Germany, Malta, Portugal, Thailand, Turkey.
Status:
First approved in 1958
Source:
Suvren by Ayerst
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

CAPTODIAME, also known as captodiamine, is a diphenylmethane derivative. It is a 5-HT2c receptor antagonist and agonist at sigma-1 and D3 dopamine receptors. It is an antihistamine which is used as a sedative and anxiolytic. CAPTODIAME is probably useful in preventing benzodiazepine withdrawal syndrome.
Status:
US Previously Marketed
Source:
THERUHISTIN ISOTHIPENDYL HYDROCHLORIDE by AYERST
(1961)
Source URL:
First approved in 1957
Source:
Theruhistin by Ayerst
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Isothipendyl is a first generation H1 antagonist (antihistamine) and anticholinergic used as an antipruritic. It is nowadays scarcely used in the first line relief of allergies due to the anticholinergic side effect of somnolence but does have some limited use through topical application in the relief of insect bites and related itching (pruritus).
Status:
US Previously Marketed
Source:
Sandostene Tartriate by Sandoz
(1956)
Source URL:
First approved in 1956
Source:
Sandostene Tartriate by Sandoz
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Thenalidine is an antihistamine with anticholinergic properties used as an antipruritic drug. It was withdrawn from the US, Canadian, and UK markets due to a risk of neutropenia. Thenalidine is an antagonist of the H1-receptor.
Promazine (Sparine) is a phenothiazine neuroleptic used for short-term management of moderate to severe psychomotor agitation and treatment of agitation and restlessness in the elderly. Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tuberoinfundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine. Promazine is not approved for human use in the United States. It is available in the US for veterinary use under the names Promazine and Tranquazine.
Status:
US Previously Marketed
First approved in 1954
Source:
Softran by Stuart
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Buclizine, a piperazine derivative, is a sedating antihistamine with antimuscarinic and moderate sedative action. The drug is used mainly for its antiemetic action, particularly in the prevention of motion sickness, and in the treatment of migraine in combination with analgesics. The following side/adverse effects have been selected on the basis of their potential clinical significance: drowsiness; Incidence less frequent; blurred vision; dryness of mouth, nose, and throat; headache; nervousness, restlessness, or trouble in sleeping; upset stomach. The following drug interactions have been selected on the basis of their potential clinical significance: alcohol; anticholinergics or other medications with anticholinergic activity; apomorphine.
Status:
US Previously Marketed
Source:
Histalog by Eli Lilly
(1954)
Source URL:
First approved in 1954
Source:
Histalog by Eli Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



BETAZOLE is a histamine H2 receptor agonist used clinically to test gastric secretory function.
Status:
US Previously Marketed
Source:
Diafen by SchenLabs (Riker)
(1953)
Source URL:
First approved in 1953
Source:
Diafen by SchenLabs (Riker)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Diphenylpyraline is an antihistamine that prevents but does not reverse, responses mediated by histamine alone. Diphenylpyraline antagonizes most of the pharmacological effects of histamine, including urticaria and pruritus. Also, diphenylpyraline may exhibit anticholinergic actions (as do most of the antihistamines) and may thus provide a drying effect on the nasal mucosa. Antihistamines such as diphenylpyraline used in the treatment of allergy act by competing with histamine for H1-receptor sites on effector cells. This reduces the effects of histamine, leading to a temporary reduction of allergy symptoms.
Status:
US Previously Marketed
Source:
SYNDECON PHENYLTOLOXAMINE CITRATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1952
Source:
Bristamin by Bristol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenyltoloxamine is an ethanolamine derivative with antihistaminic property, which is used in combination with some analgesics for the temporary relief of minor aches and pains associated with headache; backache; muscular aches; temporarily reduces fever and some others disorders. Phenyltoloxamine blocks H1 histamine receptor, thereby inhibiting phospholipase A2 and production of endothelium-derived relaxing factor, nitric oxide. Subsequent lack of activation of guanylyl cyclase through nitric oxide results in decreased cyclic GMP levels, thereby inhibiting smooth muscle constriction of various tissues, decreasing capillary permeability and decreasing other histamine-activated allergic reactions.
Status:
US Previously Marketed
Source:
CO-PYRONIL PYRROBUTAMINE NAPHTHALENE DISULFONATE by DISTA PRODUCTS
(1961)
Source URL:
First approved in 1952
Source:
Pyronil by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

PYRROBUTAMINE is a potent H1-antihistamine. H1-antihistamines interfere with the agonist action of histamine at the H1 receptor and are administered to attenuate the inflammatory process in order to treat conditions such as allergic rhinitis, allergic conjunctivitis, and urticaria.