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

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Showing 91 - 100 of 104 results

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:
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:
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:
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:
Possibly Marketed Outside US
Source:
Homoclomin by Eisai
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Homochlorcyclizine (INN) is an antihistamine which has been marketed in Japan since 1965. It is used in the treatment of Itching sensation resulting from skin diseases (eczema or dermatitis, pruritus, drug eruption, toxic erythema and infant strophulus), urticaria and allergic rhinitis. Homochlorcyclizine hydrochloride possesses several pharmacological properties: 1) inhibits bradykinin-induced contractions of isolated guinea pig ileum; 2)partially blocks SRS-A (slow-reacting substance of anaphylaxis )- induced contractions in isolated guinea pig il eum. 3) Homochlorcyclizine hydrochloride completely inhibits histamine-induced contractions at a concentration of 0.1μg/mL, while it completely inhibits serotonin or acetylcholine- induced contractions at a concentration of 1μg/mL.
Levopropylhexedrine acts similar to amphetamine, at therapeutic doses has anorexigenic effect.
Status:
Possibly Marketed Outside US
Source:
Homoclomin by Eisai
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Homochlorcyclizine (INN) is an antihistamine which has been marketed in Japan since 1965. It is used in the treatment of Itching sensation resulting from skin diseases (eczema or dermatitis, pruritus, drug eruption, toxic erythema and infant strophulus), urticaria and allergic rhinitis. Homochlorcyclizine hydrochloride possesses several pharmacological properties: 1) inhibits bradykinin-induced contractions of isolated guinea pig ileum; 2)partially blocks SRS-A (slow-reacting substance of anaphylaxis )- induced contractions in isolated guinea pig il eum. 3) Homochlorcyclizine hydrochloride completely inhibits histamine-induced contractions at a concentration of 0.1μg/mL, while it completely inhibits serotonin or acetylcholine- induced contractions at a concentration of 1μg/mL.
Status:
Possibly Marketed Outside US
Source:
ASTELIN by Muro Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Azelastine (brand names AZEP, ASTEPRO, ASTELIN etc.) a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is a potent antiallergic compound with histamine H1-receptor antagonist activity and a rapid onset and long duration of action. The major metabolite, desmethylazelastine, also exhibits H1- receptor antagonist activity. AZEP Nasal Spray is administered as a racemic mixture. The racemate, R- and S- enantiomers were equally potent at inhibiting eyelid histamine-induced oedema in rats, however the R-enantiomer was 2-fold less active at inhibiting eyeball histamine-induced oedema.
Status:
Possibly Marketed Outside US
Source:
ASTELIN by Muro Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Azelastine (brand names AZEP, ASTEPRO, ASTELIN etc.) a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is a potent antiallergic compound with histamine H1-receptor antagonist activity and a rapid onset and long duration of action. The major metabolite, desmethylazelastine, also exhibits H1- receptor antagonist activity. AZEP Nasal Spray is administered as a racemic mixture. The racemate, R- and S- enantiomers were equally potent at inhibiting eyelid histamine-induced oedema in rats, however the R-enantiomer was 2-fold less active at inhibiting eyeball histamine-induced oedema.
Status:
Possibly Marketed Outside US
Source:
Homoclomin by Eisai
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Homochlorcyclizine (INN) is an antihistamine which has been marketed in Japan since 1965. It is used in the treatment of Itching sensation resulting from skin diseases (eczema or dermatitis, pruritus, drug eruption, toxic erythema and infant strophulus), urticaria and allergic rhinitis. Homochlorcyclizine hydrochloride possesses several pharmacological properties: 1) inhibits bradykinin-induced contractions of isolated guinea pig ileum; 2)partially blocks SRS-A (slow-reacting substance of anaphylaxis )- induced contractions in isolated guinea pig il eum. 3) Homochlorcyclizine hydrochloride completely inhibits histamine-induced contractions at a concentration of 0.1μg/mL, while it completely inhibits serotonin or acetylcholine- induced contractions at a concentration of 1μg/mL.

Showing 91 - 100 of 104 results