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

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Showing 1231 - 1240 of 1290 results

Status:
US Previously Marketed
Source:
Allercur by Roerig (Pfizer)
(1960)
Source URL:
First approved in 1960
Source:
Allercur by Roerig (Pfizer)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clemizole is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary regulatory requirements were established for new drug development, and there is very minimal information about its pharmacokinetics and metabolism.
Status:
US Previously Marketed
Source:
Allercur by Roerig (Pfizer)
(1960)
Source URL:
First approved in 1960
Source:
Allercur by Roerig (Pfizer)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clemizole is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary regulatory requirements were established for new drug development, and there is very minimal information about its pharmacokinetics and metabolism.
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:
US Previously Marketed
Source:
TRIMEPRAZINE TARTRATE by MORTON GROVE
(1985)
Source URL:
First approved in 1959
Source:
Temaril by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Trimeprazine (also known as Alimemazine), a phenothiazine used as antipsychotic drug. This drug is used in Russia under brand name TERALIGEN and has anti-histamine, sedative, and anti-emetic (anti-nausea) effects. Teraligen is used to treat neurosis, depression and anxiety of different origins. It prevents and relieves allergic conditions, which cause pruritus and urticaria by blocking histamine produced by the body during an allergic reaction. Trimeprazine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Trimeprazine is not approved for use in humans in the United States. Nevertheless, combination of alimemazine and prednisolone (commonly sold under the brand name Temaril-P) is licensed as an antipruritic and antitussive in dogs.
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
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:
Parsidol HCl by Warner /Chilcott
(1953)
Source URL:
First approved in 1953
Source:
Parsidol HCl by Warner /Chilcott
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ethopropazine is an anticholinergic drug. Ethopropazine is an inhibitor of butyrylcholinesterase and non-selective muscarinic acetylcholine receptor antagonist. Ethopropazine has been used for the treatment of parkinsonism and drug-induced extrapyramidal reactions. Also It used for the symptomatic treatment of hepatolenticular degeneration and congenital athetosis.
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.

Showing 1231 - 1240 of 1290 results