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Restrict the search for
histamine
to a specific field?
Status:
First approved in 1951
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Bromodiphenhydramine also known as bromazine, is an antihistamine and anticholinergic agent, which was used to under brand name ambordyl. Ambordyfor was indicated for the treatment of allergic symptoms, but that usage, was discontinued. It was shown, that bromodiphenhydramine competed with free histamine for binding at HA-receptor sites and lead to a reduction of the negative symptoms brought on by histamine HA-receptor binding.
Status:
US Previously Marketed
Source:
BANTHINE by SHIRE
(1951)
Source URL:
First approved in 1951
Source:
BANTHINE by SHIRE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Methantheline is a synthetic quarternary ammonium antimuscarinic used to relieve cramps or spasms of the stomach, intestines, and bladder. It is indicated for the treatment of peptic ulcer disease, irritable bowel syndrome, pancreatitis, gastritis, biliary dyskinesia, pylorosplasm, and reflex neurogenic bladder in children. It can be used together with antacids or other medicines, such as H2-receptor antagonists, in the treatment of peptic ulcer. Methantheline bromide (diethyl-methyl [2-(9 xanthenyl carbonyloxy) ethyl] ammonium bromide) is marketed to treat neurogenic bladder instability. In comparison with atropine, it influences the parasympathetic nervous transmission more by ganglionic rather than peripheral muscarinic receptor blockade. Methantheline inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. Clinical effects after single therapeutic doses of 50-100 mg last for about 6 hours which is longer than after atropine. The drug relaxes smooth muscles of the gastrointestinal and urogenital tract. Furthermore, it inhibits bronchial, salivary and sweat glands secretion, lowers the production of gastric juice and disturbs accommodation. A recent randomised double-blind placebo-controlled study using a new commercial preparation of methantheline bromide (Vagantin, Germany) demonstrated significant sweat reduction and was evaluated as is an effective and safe treatment of axillary hyperhidrosis.
Status:
US Previously Marketed
Source:
OTODYNE by WHITE
(1951)
Source URL:
First approved in 1951
Source:
OTODYNE by WHITE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Zolamine is an antihistamine with local anesthetic properties. Zolamine is reported to have a low incidence of side effects and is used clinically both as an antihistaminic and a topical local anesthetic.
Status:
US Previously Marketed
Source:
CAMOQUIN HYDROCHLORIDE by PARKE DAVIS
(1950)
Source URL:
First approved in 1950
Source:
CAMOQUIN HYDROCHLORIDE by PARKE DAVIS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Amodiaquine is a medication used to treat malaria, including Plasmodium falciparum malaria when uncomplicated. The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function. The side effects of amodiaquine are generally minor to moderate and are similar to those of chloroquine. Rarely liver problems or low blood cell levels may occur. When taken in excess headaches, trouble seeing, seizures, and cardiac arrest may occur. After oral administration amodiaquine hydrochloride is rapidly absorbed,and undergoes rapid and extensive metabolism to desethylamodiaquine which concentrates in red blood cells. It is likely that desethylamodiaquine, not amodiaquine, is responsible for most of the observed antimalarial activity, and that the toxic effects of amodiaquine after oral administration may in part be due to desethylamodiaquine.
Status:
First approved in 1949
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
PARATHIAZINE, a member of phenothiazines, is a histamine receptor antagonist used for the treatment of allergic diseases. Also, it can be used as an antiemetic agent.
Status:
US Previously Marketed
Source:
Pyrabrom by Brayten
(1949)
Source URL:
First approved in 1949
Source:
Pyrabrom by Brayten
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyrabrom (also known as mepyramine 8-bromotheophyllinate) is a pharmaceutical preparation that causes antidiuresis under conditions of water load. However, under conditions of salt load Pyrabrom increases the speed of urinary excretion.
Status:
US Previously Marketed
Source:
TRIPELENNAMINE HYDROCHLORIDE by WATSON LABS
(1973)
Source URL:
First approved in 1948
Source:
PBZ by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tripelennamine (sold as Pyribenzamine by Novartis) is a drug that is used as an antipruritic and first-generation antihistamine. Histamine acting on H1-receptors produces vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Tripelennamine can be used in the treatment of asthma, hay fever, rhinitis, and urticaria, but is now less common as newer antihistamines have replaced it.
Status:
US Previously Marketed
Source:
PRISCOLINE by NOVARTIS
(1948)
Source URL:
First approved in 1948
Source:
PRISCOLINE by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tolazoline, also known as priscoline, was used in treatment of persistent pulmonary hypertension of the newborn. But that prescription was discontinued. Priscoline given intravenously produces vasodilatation, primarily due to a direct effect on vascular smooth muscle, and cardiac stimulation; the blood pressure response depends on the relative contributions of the two effects. Priscoline usually reduces pulmonary arterial pressure and vascular resistance. The mechanisms of its therapeutic effects are not clear, but is known, that tolazoline is a non-selective competitive α-adrenergic receptor antagonist and it possesses histamine agonist activity.
Status:
US Previously Marketed
Source:
VASOCON-A by NOVARTIS
(1990)
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Antazoline is an antagonist of histamine H1 receptors. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Antazoline in combination with naphazoline (VASOCON-A®) is indicated to relieve the symptoms of allergic conjunctivitis.
Status:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Chlorothen citrate (trade name Tagathen) is an antihistamine and a first generation H1 receptor antagonist, that have been used for the treatment of asthma, bronchitis, and bronchoconstriction.‘-5. Chlorothen is synthesized by condensation of 5-chloro-2-thienylchloride and N,N-dimethyl-N-(2-pyridinyl)ethylenediamine in the presence of sodium or potassium amide
