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

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Showing 781 - 790 of 2546 results

Benzthiazide (trade names Aquatag, Dihydrex, Diucen, Edemax, Exna, Foven and others) is a thiazide diuretic used in the treatment of high blood pressure and edema. It is no longer available in the United States. As a diuretic, benzthiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. The following is a list of possible side effects that may occur from all constituting ingredients of Exna Tablet: vomiting, diarrhoea, photosensitivity reactions, increased in uric acid concentrations, megaloblastic anaemia, thrombocytopenia. Exna tablet may interact with the following drugs and products: ACE inhibitors, angiotensin II receptor antagonists, potassium-sparing diuretics.
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:
Oxaine by Wyeth
(1960)
Source URL:
First approved in 1960
Source:
Oxaine by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oxethazaine is a potent local anesthetic. It is administered orally (usually in combination with an antacid) for the relief of pain associated with peptic ulcer disease or esophagitis. Its effectiveness at the acidity of the gastric environment is due to the fact that oxethazaine, a weak base, is relatively non-ionized at pH 1. It is also used topically in the management of hemorrhoid pain. Oral oxetacaine preparations are available in several countries, including India, South Africa and Brazil, but not the United States. It is marketed under the name Strocain in Japan.
Status:
US Previously Marketed
Source:
GUANETHIDINE MONOSULFATE by WATSON LABS
(1985)
Source URL:
First approved in 1960
Source:
lsmelin Sulfate by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Guanethidine belongs to the general class of medicines called antihypertensives. It was used to treat high blood pressure (hypertension). It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles.
Biperiden, sold under the brandname Akineton was used as an adjunct in the therapy of all forms of parkinsonism (postencephalitic, arteriosclerotic and idiopathic). Was also useful in the control of extrapyramidal disorders due to central nervous system drugs such as phenothiazines and other groups of psychotropics. Biperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance. Atropine-like side effects such as dry mouth; blurred vision; drowsiness; euphoria or disorientation; urinary retention; postural hypotension; constipation; agitation; disturbed behavior may been seen. Only limited pharmacokinetic studies of biperiden in humans are available.
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.
Status:
US Previously Marketed
Source:
TACE 25 MG ERGONOVINE by MERRELL
(1959)
Source URL:
First approved in 1959
Source:
TACE 25 MG ERGONOVINE by MERRELL
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ergonovine (also known as ergometrine) is the active water soluble component of ergot of rye. Ergonovine is being used as a maleate salt to prevent or treate postpartum haemorrhage and postabortion haemorrhage. Ergonovine stimulates alpha-adrenergic and serotonin receptors, thus activating contractions of uterine and vascular smooth muscle. Ergonovine may have depressant effect on CNS system as it binds to dopamine receptors.
Status:
US Previously Marketed
Source:
Cyclamycin by Wyeth
(1958)
Source URL:
First approved in 1958
Source:
Cyclamycin by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Troleandomycin (also known Triacetyl-oleandomycin and having brand name Tao) is a macrolide antibiotic which used to for the treat of infections of the upper and lower respiratory tract: such as tonsillitis, bronchitis, sinusitis, and pneumonia. However, the brand name Tao was discontinued. Troleandomycin acts by penetrating the bacterial cell membrane and reversibly binding to the 50 S subunit of bacterial ribosomes or near the "P" or donor site so that binding of tRNA (transfer RNA) to the donor site is blocked. Translocation of peptides from the "A" or acceptor site to the "P" or donor site is prevented, and subsequent protein synthesis is inhibited.
Status:
US Previously Marketed
First approved in 1958

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlorpropamide (DIABINESE®), is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. It appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which chlorpropamide (DIABINESE®) lowers blood glucose during long-term administration has not been clearly established. Extra-pancreatic effects may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. While chlorpropamide is a sulfonamide derivative, it is devoid of antibacterial activity. Chlorpropamide (DIABINESE®) may also prove effective in controlling certain patients who have experienced primary or secondary failure to other sulfonylurea agent.
Status:
US Previously Marketed
Source:
PROPOXYPHENE HYDROCHLORIDE by ALRA
(1982)
Source URL:
First approved in 1957

Class (Stereo):
CHEMICAL (RACEMIC)



Propoxyphene is a centrally acting opiate analgesic. Propoxyphene is an odorless, freely soluble in water, white crystalline powder with a bitter taste. In vitro studies demonstrated propoxyphene and the metabolite norpropoxyphene inhibit sodium channels (local anesthetic effect) with norpropoxyphene being approximately 2 fold more potent than propoxyphene and propoxyphene approximately 10 fold more potent than lidocaine. Propoxyphene and norpropoxyphene inhibit the voltage-gated potassium current carried by cardiac rapidly activating delayed rectifier (hERG) channels with approximately equal potency. It is unclear if the effects on ion channels occur within therapeutic dose range. Propoxyphene is indicated for the relief of mild to moderate pain.