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

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Showing 171 - 180 of 432 results

Hydroflumethiazide is a thiazide diuretic that inhibits water reabsorption in the nephron by inhibiting the sodium-chloride symporter (SLC12A3) in the distal convoluted tubule, which is responsible for 5% of total sodium reabsorption. Normally, the sodium-chloride symporter transports sodium and chloride from the lumen into the epithelial cell lining the distal convoluted tubule. The energy for this is provided by a sodium gradient established by sodium-potassium ATPases on the basolateral membrane. Once sodium has entered the cell, it is transported out into the basolateral interstitium via the sodium-potassium ATPase, causing an increase in the osmolarity of the interstitium, thereby establishing an osmotic gradient for water reabsorption. By blocking the sodium-chloride symporter, Hydroflumethiazide effectively reduces the osmotic gradient and water reabsorption throughout the nephron. Hydroflumethiazide is used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Also used in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension.
Phenprocoumon is the dominant anticoagulant in clinical use in several continental European countries. It used for the prevention and treatment of thromboembolic disease including venous thrombosis, thromboembolism, and pulmonary embolism as well as for the prevention of ischemic stroke in patients with atrial fibrillation. Phenprocoumon inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). Bleedings are the most important side -effects of oral anticoagulants. The gastrointestinal and the urinary tract are often affected; the most dangerous are intracerebral hemorrhages. A great number of drugs increase the risk of bleeding of oral anticoagulants. Enzyme inhibitors (e.g. allopurinol, androgens, cimetidine, ciprofloxacin, co-trimoxazole, certain anti-inflammatory agents, fibrates, imidazoles, macrolide antibiotics, etc.) reinforce, and enzyme inducers (e.g. barbiturates, rifampicin) and oral contraceptives reduce, the anticoagulant action.
Status:
US Previously Marketed
Source:
Sintrom by Geigy
(1957)
Source URL:
First approved in 1957
Source:
Sintrom by Geigy
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Acenocoumarol is mono-coumarin derivative with racemic mixture of R (+) and S (-) enantiomers. Acenocoumarol is structurally similar to vitamin K and is competitively able to inhibit the enzyme vitamin K-epoxide reductase. It exerts anticoagulant action by preventing the regeneration of reduced vitamin K by interfering with action of vitamin K epoxide reductase. Acenocoumarol is prescribed as the anticoagulant in various thromboembolic disorders.
Anisindione (brand name Miradon) is a synthetic anticoagulant and an indanedione derivative with action similar to these of Warfarin. It is indicated for the prophylaxis and treatment of venous thrombosis and its extension, the treatment of atrial fibrillation with embolization, the prophylaxis and treatment of pulmonary embolism, and as an adjunct in the treatment of coronary occlusion. Anisindione prevents the formation of active procoagulation factors II, VII, IX, and X, as well as the anticoagulant proteins C and S, in the liver by inhibiting the vitamin K–mediated gamma-carboxylation of precursor proteins. Hemorrhage and/or necrosis are among the hazards of treatment with any anticoagulant and are the main serious complications of therapy. Drugs that have been reported to diminish oral anticoagulant response, ie, decreased prothrombin time response, in man significantly include: adrenocortical steroids; alcohol; antacids; antihistamines; barbiturates and others.
Status:
US Previously Marketed
First approved in 1957
Source:
Cardrase by Upjohn
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ethoxzolamide is a carbonic anhydrase I inhibitor. It is used in the treatment of glaucoma and duodenal ulcers, and as a diuretic. Ethoxzolamide was marketed under trade name Cadrase, but is now discontinued.
Status:
US Previously Marketed
Source:
ROLICTON by SEARLE
(1961)
Source URL:
First approved in 1956
Source:
Rolicton by Searle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

AMISOMETRADINE, a pyrimidinedione-based diuretic, is an isomer of aminometradine with less toxicity and a reasonable diuretic potency.
Status:
US Previously Marketed
Source:
Dipaxin by Upjohn
(1955)
Source URL:
First approved in 1955
Source:
Dipaxin by Upjohn
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Diphenadione is a vitamin K antagonist that exhibits anticoagulant effects and is used as a rodenticide against rats, mice, voles, ground squirrels and others. When orally ingested it is toxic to mammals causing irregular heartbeat and major maladies associated with its impact on blood clotting. It is also used in South America to control vampire bat populations.
Status:
US Previously Marketed
Source:
Mictine (Mincard) by Searle
(1954)
Source URL:
First approved in 1954
Source:
Mictine (Mincard) by Searle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

AMINOMETRADINE, a uracil derivative, is a diuretic. It appears to inhibit the reabsorption of sodium ions by the renal tubules. AMINOMETRADINE is used in the management of edema and in the treatment of congestive heart failure.
Status:
US Previously Marketed
Source:
Adrenosem by Massengill
(1953)
Source URL:
First approved in 1953
Source:
Adrenosem by Massengill
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
US Previously Marketed
First approved in 1952

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenindione is an anticoagulant which functions as a Vitamin K antagonist. The drug was discontinued in USA, but still in use worldwide.

Showing 171 - 180 of 432 results