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

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Showing 1141 - 1150 of 1221 results

Edrophonium is a short and rapid-acting cholinergic drug. Chemically, edrophonium is ethyl (m-hydroxyphenyl) dimethylammonium. Edrophonium is used for the differential diagnosis of myasthenia gravis and as an adjunct in the evaluation of treatment requirements in this disease. It may also be used for evaluating emergency treatment in myasthenic crises. Because of its brief duration of action, it is not recommended for maintenance therapy in myasthenia gravis. It is also useful whenever a curare antagonist is needed to reverse the neuromuscular block produced by curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine. It is not effective against decamethonium bromide and succinylcholine chloride. It may be used adjunctively in the treatment of respiratory depression caused by curare overdosage.
Status:
US Previously Marketed
First approved in 1950
Source:
PIG SWIGFOR SWINE AND POULTRY by LeGear Animal Health
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Piperazine, a six membered nitrogen containing heterocycle, is of great significance to the rational design of drugs. This moiety can be found in a plethora of well-known drugs with various therapeutic uses, such as antipsychotic, antihistamine, antianginal, antidepressant, anticancer, antiviral, cardio protectors, anti-inflammatory, and imaging agents. Slight modification to the substitution pattern on the piperazine nucleus facilitates a recognizable difference in the medicinal potential of the resultant molecules. Piperazine has been used as an antihelmintic drug. Piperazine works by paralyzing the worms. They are then passed in the stool.
Status:
US Previously Marketed
First approved in 1950

Class (Stereo):
CHEMICAL (ACHIRAL)


Diethylcarbamazine is used in humans, dogs and cats for the treatment of parasitic infections, including pulmonary eosinophilia, loiasis, and lymphatic filariasis. The exact mechanism of its action is unknown, however some studies showed the involvment of inducible nitric-oxide synthase and the cyclooxygenase pathway. Although there is no information on whether the drug is marketed in the USA and Europe, it is currently used in India.
Status:
US Previously Marketed
Source:
CAMOQUIN HYDROCHLORIDE by PARKE DAVIS
(1950)
Source URL:
First approved in 1950

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:
US Previously Marketed
Source:
CHLOROMYCETIN HYDROCORTISONE by PARKEDALE
(1953)
Source URL:
First approved in 1950
Source:
Chloromycetin by Warner-Lambert
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Chloramphenicol is a broad-spectrum antibiotic that was first isolated from Streptomyces venezuelae in 1947. The drug was subsequently chemically synthesized. It has both a bacteriostatic and bactericidal effect; in the usual therapeutic concentrations it is bacteriostatic. Chloramphenicol is used for the treatment of serious gram-negative, gram-positive, and anaerobic infections. It is especially useful in the treatment of meningitis, typhoid fever, and cystic fibrosis. It should be reserved for infections for which other drugs are ineffective or contraindicated. Chloramphenicol, a small inhibitor of bacterial protein synthesis, is active against a variety of bacteria and readily enters the CSF. It has been used extensively in the last decades for the treatment of bacterial meningitis. In industrialized countries, chloramphenicol is restricted mostly to topical uses because of the risk of induction of aplastic anemia. However, it remains a valuable reserve antibiotic for patients with allergy to β-lactam antibiotics or with CNS infections caused by multiresistant pathogens.
Status:
US Previously Marketed
First approved in 1950
Source:
PIG SWIGFOR SWINE AND POULTRY by LeGear Animal Health
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Piperazine, a six membered nitrogen containing heterocycle, is of great significance to the rational design of drugs. This moiety can be found in a plethora of well-known drugs with various therapeutic uses, such as antipsychotic, antihistamine, antianginal, antidepressant, anticancer, antiviral, cardio protectors, anti-inflammatory, and imaging agents. Slight modification to the substitution pattern on the piperazine nucleus facilitates a recognizable difference in the medicinal potential of the resultant molecules. Piperazine has been used as an antihelmintic drug. Piperazine works by paralyzing the worms. They are then passed in the stool.
Sulfamethazine is a sulfonamide used to treat a variety of bacterial diseases in animals. It inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase).
Tubocurarine, a naturally occurring alkaloid, is used to treat smoking withdrawl syndrom. Tubocurarine, the chief alkaloid in tobacco products, binds stereo-selectively to nicotinic-cholinergic receptors at the autonomic ganglia, in the adrenal medulla, at neuromuscular junctions, and in the brain. Two types of central nervous system effects are believed to be the basis of Tubocurarine's positively reinforcing properties. A stimulating effect is exerted mainly in the cortex via the locus ceruleus and a reward effect is exerted in the limbic system. At low doses the stimulant effects predominate while at high doses the reward effects predominate. Intermittent intravenous administration of Tubocurarine activates neurohormonal pathways, releasing acetylcholine, norepinephrine, dopamine, serotonin, vasopressin, beta-endorphin, growth hormone, and ACTH. Tubocurarine competes with acetylcholine for post-synaptic nicotinic NM receptors and blocks them.
Status:
US Previously Marketed
Source:
Pabalate by Robins
(1949)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AMINOBENZOATE SODIUM is a salt of Aminobenzoic acid. Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi. Many bacteria, including those found in the human intestinal tract such as E. coli, generate Aminobenzoic acid from chorismate by the combined action of the enzymes 4-amino-4-deoxychorismate synthase and 4-amino-4-deoxychorismate lyase. Plants produce Aminobenzoic acid in their chloroplasts, and store it as a glucose ester (pABA-Glc) in their tissues. Humans lack the enzymes to convert Aminobenzoic acid to folate, so require folate from dietary sources such as green leafy vegetables. In humans, Aminobenzoic acid is considered nonessential and, although it has been referred to historically as "vitamin Bx", is no longer recognized as a vitamin, because most people have colon bacteria that generate Aminobenzoic acid. The potassium salt is used as a drug against fibrotic skin disorders, such as Peyronie's disease, under the trade name Potaba.
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.

Showing 1141 - 1150 of 1221 results