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

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Showing 261 - 270 of 1617 results

Status:
US Previously Marketed
First approved in 1977

Class (Stereo):
CHEMICAL (ACHIRAL)



Azatadine is an antihistamine, which blocks the effects of the naturally occurring chemical histamine in the body. Azatadine is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; and other symptoms of allergies and the common cold. The antihistamines antagonize those pharmacological effects of histamine, which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.
Status:
US Previously Marketed
Source:
Serc by Unimed More
(1966)
Source URL:
First approved in 1966
Source:
Serc by Unimed More
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Betahistine is an orally administered, centrally acting histamine H1 receptor agonist with partial H3 antagonistic activity. It is proposed that betahistine may reduce peripherally the asymmetric functioning of the sensory vestibular organs in addition to increasing vestibulocochlear blood flow by antagonising local H3 heteroreceptors. Betahistine acts centrally by enhancing histamine synthesis within tuberomammillary nuclei of the posterior hypothalamus and histamine release within vestibular nuclei through antagonism of H3 autoreceptors. This mechanism, together with less specific effects of betahistine on alertness regulation through cerebral H1 receptors, should promote and facilitate central vestibular compensation. Betahistine is used to treat the symptoms associated with Ménière's disease, a condition of the inner ear which causes, vertigo (dizziness), tinnitus (ringing in the ears), hearing loss.
Status:
US Previously Marketed
First approved in 1965

Class (Stereo):
CHEMICAL (RACEMIC)



Chlorphenesin carbamate (Maolate, Musil) is a centrally acting muscle relaxant used to treat muscle pain and spasms. Сhlorphenesin acts in the central nervous system (CNS) rather than directly on skeletal muscle. It also has antifungal and some antibacterial properties. The major adverse effects are drowsiness and dizziness.
Chlorprothixene (Taractan, Tarasan, Truxal) is a thioxanthine derivative developed by Lundbeck for the treatment of psychotic disorders. The drug exerts its activity by binding to and inhibiting serotonin receptors, dopamine receptors, muscarinic acetylcholine receptor, histamine H1 receptor and alpha1-adrenergic receptor.
Status:
US Previously Marketed
Source:
Twiston by McNeil
(1960)
Source URL:
First approved in 1960
Source:
Twiston by McNeil
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Rotoxamine ((S)-carbinoxamine) is maleic acid salt of the levorotatory isomer of Carbinoxamine (a first-generation antihistamine of the ethanolamine class). Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to the usual allergic symptoms, the drug also treats an irritant cough and nausea, vomiting, and vertigo associated with motion sickness. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease. Rotoxamine is used to treat runny or stuffy nose, sneezing, itching, watery eyes, hives, skin rash, itching, and other symptoms of allergies and the common cold.
Status:
US Previously Marketed
Source:
METHDILAZINE HYDROCHLORIDE by ALPHARMA US PHARMS
(1981)
Source URL:
First approved in 1960
Source:
Tacaryl HCl by Mead Johnson
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Methdilazine is a phenothiazine compound with antihistaminic activity. Methdilazine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. It is used for the symptomatic relief of hypersensitivity reactions and particularly for the control of pruritic skin disorders.
Status:
US Previously Marketed

Class (Stereo):
CHEMICAL (RACEMIC)



Propiomazine is a typical antipsychotic, blocking H1 receptors and is primarily indicated in conditions Insomnia. Propiomazine was also used under brand name largon for the relief of restlessness and apprehension, preoperatively or during surgery. In addition largon was used as an adjunct to analgesics for the relief of restlessness and apprehension during labor. But this drug was discontinued.
Status:
US Previously Marketed
Source:
Forhistal Maleate by Ciba
(1960)
Source URL:
First approved in 1960
Source:
Forhistal Maleate by Ciba
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Dimetindene (trade name Fenistil; other name dimethindene maleate) is a potent antipruritic antihistamine, characterized by the small size of its effective dose and its rapidity of action. Dimetindene is an antihistamine/anticholinergic that is a selective H1 antagonist. Its effect sets in after 20 to 60 minutes and lasts several hours. Dimetindene drops as well as Dimetindene syrup is particularly indicated in pediatric practice. Dimetindene is indicated as symptomatic treatment of allergic reactions: urticaria, allergies of the upper respiratory tract such as hay fever and perennial rhinitis, food, and drug allergies; pruritus of various origins, except pruritus due to cholestasis; insect bites. Dimetindene is also indicated for pruritus in eruptive skin diseases such as chicken-pox. Dimetindene can be as an adjuvant in eczema and other pruriginous dermatoses of allergic origin.
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:
TRIMEPRAZINE TARTRATE by MORTON GROVE
(1985)
Source URL:
First approved in 1959
Source:
Temaril by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



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.