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

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Showing 1781 - 1790 of 8583 results

Status:
US Previously Marketed
Source:
Mercuhydrin Sodium by Lakeside (MerrellNational)
(1943)
Source URL:
First approved in 1943
Source:
Mercuhydrin Sodium by Lakeside (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

MERALLURIDE ACID is an organomercuric compound. It was used as a diuretic in a 1:1 mixture with theophylline.
Status:
US Previously Marketed
Source:
Sulfamerazine by Lederle
(1943)
Source URL:
First approved in 1943
Source:
Sulfamerazine by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfamerazine is a sulfonamide antibiotic, which acts by inhibiting folic acid synthesis in bacterias. The primary target of sulfamerazine is believed to be dihydropteroate synthetase. Sulfamerazine (in comination with Sulfadiazine and Sulfamethazine) was used in the US under different names, including the earliest brand of Neotrizine. Nowdays, the drugs containing sulfamerazine are no longer available for use in humans in the US, however, they may be prescribed for veterinary purposes.
Status:
US Previously Marketed
Source:
Emko Foam by Endo
(1959)
Source URL:
First approved in 1942
Source:
Phemerol Chloride by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Benzethonium chloride, also known as hyamine, is a synthetic quaternary ammonium salt. It has surfactant, antiseptic, and anti-infective properties and it is used as a topical antimicrobial agent in first aid antiseptics. It is also found in cosmetics and toiletries such as mouthwashes, anti-itch ointments, and antibacterial moist towelettes. Benzethonium chloride exhibits a broad spectrum of microbiocidal activity against bacteria, fungi, mold and viruses. The US Food and Drug Administration (FDA) specifies that the safe and effective concentrations for benzethonium chloride are 0.1-0.2% in first aid products. Aqueous solutions of benzethonium chloride are not absorbed through the skin. It is not approved in the US or Europe for use as a food additive. Being a quaternary ammonium salt, it is more toxic than negatively charged surfactants. However, in a two-year study on rats, there was no evidence of carcinogenic activity. Benzethonium chloride was characterized as a novel anticancer compound possessing both in vitro and in vivo efficacy justifying further investigation.
Status:
US Previously Marketed
Source:
Nethamine by Merrell (MerrellNational)
(1942)
Source URL:
First approved in 1942
Source:
Nethamine by Merrell (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Etafedrine, a sympathomimetic agent that acts on the sympathetic receptors of the bronchial tree relaxing spasm in a manner similar to that of ephedrine, is a bronchodilator and a selective β2-adrenoreceptor agonist. Contraction of the guinea pig tracheal chain by acetylcholine or histamine was antagonized by etafedrine with a higher potency then ephedrine but with a lower potency than epinephrine (adrenaline). Etafedrine did not increase heart rate or force of contraction in guinea pig atria. Unlike ephedrine and tyramine, etafedrine did not induce the release of noradrenaline as was demonstrated in vitro in the perfused rabbit heart and instead acted as a selective β2 adrenoreceptor agonist. Etafedrine also belongs to the family of medications called decongestants. It works by narrowing blood vessels in the nasal passages, helping to relieve nasal stuffiness. Etafedrine has been used in pharmaceutical compositions, such as NETHAPRIN Expectorant, Nethaprin Dospan and Dalmacol, useful in the treatment of asthma and other respiratory disorders including chronic bronchitis.
Status:
US Previously Marketed
Source:
Synkayvite by Hoffmann-La Roche
(1941)
Source URL:
First approved in 1941
Source:
Synkayvite by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Menadiol diphosphate is given as a vitamin K supplement to prevent bleeding caused by vitamin K deficiency. Vitamin K is normally obtained from the diet; for example it is found in green leafy vegetables, root vegetables, cereals and dairy products. Although it cannot be made by the human body itself, a certain amount of vitamin K is also made by bacteria that live in the gut. The body normally produces bile to help it absorb fats from the gut. In conditions where there is a problem with the production of bile, for example in certain liver diseases, or if there is a blockage of the bile duct, there can be problems absorbing fats. This can lead to vitamin K deficiency, decreased production of clotting factors and an increased risk of bleeding. In these situations, menadiol diphosphate is given as a vitamin K supplement to increase the production of clotting factors. It is water soluble so is readily absorbed from the gut. Also in 1974 was made attempt to develop tritiated derivatives of Synkavit (menadiol sodium diphosphate, MNDP) of high specific activity as a radioactive drug. Among the 203 evaluable treated cases, some form of response was observed in 23 out of 151 (15·2%) receiving the drug by intravenous injections and 13 out of 52 (25%) after intra-arterial injections. For the sites and types of malignant diseases which showed responses after either intravenous or intra-arterial administration among the 55 patients surviving at least 3 months after the first injection, some form of response was observed in 32 but only 5 of these showed either a "complete" or a "partial" response.It is concluded that further investigation is desirable. Kappadione is a Vitamin K derivative, was discontinued. It was manufactured by Eli Lilly and others Company.
Status:
US Previously Marketed
Source:
Ceepryn by Merrell
(1941)
Source URL:
First approved in 1941
Source:
Ceepryn by Merrell
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cetylpyridinium (used in a form of chloride salt) is a cationic surface-active agent and has a broad antimicrobial spectrum, with rapid killing of gram-positive pathogens and yeast in particular. It is suggested that interaction with bacteria occurs by the disruption of membrane function, leakage of cytoplasmic material, and ultimately the collapse of the intra-cellular equilibrium. The drug is used under various trade names as an oral OTC hygiene product (mouthwash, dental kits, etc.) to control the dental plaque and to prevent the subsequent gingivitis.
Status:
US Previously Marketed
Source:
Sulfaguanidine by Lederle
(1941)
Source URL:
First approved in 1941
Source:
Sulfaguanidine by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfaguanidine is used to treat the gastrointestinal infections particularly bacillary dysentery. Sulfaguanidine is a sulfonamide antibiotic that blocks the synthesis of dihydrofolic acid by inhibiting the enzyme dihydropteroate synthase in bacteria. Sulfonamides are active against Gram positive bacteria and Gram negative bacteria.
Diethylstilbestrol is a synthetic non-steroidal estrogen. It is used in the treatment of menopausal and postmenopausal disorders, prostate cancer and in the prevention of miscarriage or premature delivery in pregnant women prone to miscarriage or premature delivery. Diethylstilbestrol is a very potent full agonist of the estrogen receptors. At the cellular level, estrogens increase the synthesis of DNA, RNA, and various proteins in target tissues. Pituitary mass is also increased. Estrogens reduce the release of gonadotropin-releasing hormone from the hypothalamus, leading to a reduction in release of follicle-stimulating hormone and luteinizing hormone from the pituitary. Adverse effects are: breast pain or tenderness, enlargement of breasts, gynecomastia, peripheral edema and others. Estrogens may interfere with the effects of bromocriptine. Dosage adjustment may be needed. Concurrent use with estrogens may alter the metabolism and protein binding of the glucocorticoids, leading to decreased clearance, increased elimination half-life, and increased therapeutic and toxic effects of the glucocorticoids.
Status:
US Previously Marketed
Source:
Hytakerol by Winthrop-Stearns (Winthrop)
(1940)
Source URL:
First approved in 1940
Source:
Hytakerol by Winthrop-Stearns (Winthrop)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dihydrotachysterol (DHT) is a synthetic vitamin D analog activated in the liver that does not require renal hydroxylation like vitamin D2 (ergocalciferol) and vitamin D3 (cholecalciferol). Dihydrotachysterol is used to treat hypocalcemia, hypoparathyroidism, and prevention of tetany. Dihydrotachysterol is hydroxylated in the liver to 25-hydroxy-dihydrotachysterol, which is the major circulating active form of the drug. Once hydroxylated to 25-hydroxy-dihydrotachysterol, the modified drug binds to the vitamin D receptor. The bound form of the vitamin D receptor serves as a transcriptional regulator of bone matrix proteins, inducing the expression of osteocalcin and suppressing synthesis of type I collagen. Dihydrotachysterol also increases renal phosphate excretion.
Status:
US Previously Marketed
Source:
DELVINAL by MSD
(1961)
Source URL:
First approved in 1940
Source:
Delvinal by Sharp & Dohme (MSD)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

VINBARBITAL, a barbiturate derivative, is a hypnotic drug. Also, it was used for analgesia and anesthesia in obstetrics.

Showing 1781 - 1790 of 8583 results