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

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Showing 1251 - 1260 of 3134 results

Status:
US Previously Marketed
Source:
TOPOCIDE DDT by LILLY
(1946)
Source URL:
First approved in 1946

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

DDT (dichlorodiphenyltrichloroethane) is a colorless, crystalline, tasteless and almost odorless organochloride known for its insecticidal properties and environmental impacts. First synthesized in 1874, DDT's insecticidal action was discovered by the Swiss chemist Paul Hermann Müller in 1939. It was used in the second half of World War II to control malaria and typhus among civilians and troops. After the war, DDT was also used as an agricultural insecticide and its production and use duly increased. The United States banned the use of DDT in 1972, but some countries still use the chemical. In December 2000, in a convention organized by the United Nations Environment Program, 122 nations agreed to a treaty banning twelve very toxic chemicals. Included among the twelve was DDT. However, the treaty allowed the use of DDT to combat malaria until other alternatives become available. Before it can take effect the treaty must be ratified by 50 of the nations that agreed to it in principle. DDT has also been used in the past for the treatment of lice. It is still in use outside the United States for the control of mosquitoes that spread malaria. DDT and related chemicals persist for a long time in the environment and in animal tissues. People are most likely to be exposed to DDT from food, including meat, fish, and dairy products. DDT can be absorbed by eating, breathing, or touching products contaminated with DDT. In the body, DDT is converted into several metabolic products, including the metabolite dichlorodiphenyldichloroethene (DDE). DDT and DDE are stored in the body’s fatty tissues. In pregnant women DDT and DDE can be passed to the fetus. Both chemicals are found in breast milk, resulting in exposure to nursing infants. Human health effects from DDT at low environmental doses are unknown. However, following exposure to high doses human symptoms can include vomiting, tremors or shakiness, and seizures. Laboratory animal studies showed effects on both the liver and reproduction. DDT is considered a possible human carcinogen. DDE acts as a weak androgen receptor antagonist, but not as an estrogen. p,p'-DDT, DDT's main component, has little or no androgenic or estrogenic activity. The minor component o,p'-DDT has weak estrogenic activity.
Status:
US Previously Marketed
First approved in 1946

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Mephenytoin is an antiepileptic drug which can be useful in the treatment of epilepsy. The primary site of action appears to be the motor cortex where spread of seizure activity is inhibited. Possibly by promoting sodium efflux from neurons, mephenytoin tends to stabilize the threshold against hyperexcitability caused by excessive stimulation or environmental changes capable of reducing membrane sodium gradient. This includes the reduction of posttetanic potentiation at synapses. Loss of posttetanic potentiation prevents cortical seizure foci from detonating adjacent cortical areas. Mephenytoin reduces the maximal activity of brain stem centers responsible for the tonic phase of tonic-clonic (grand mal) seizures. The mechanism of action of mephenytoin is not definitely known, but extensive research strongly suggests that its main mechanism is to block frequency-, use- and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials. Mephenytoin is no longer available in the US or the UK. It is still studied largely because of its interesting hydroxylation polymorphism.
Status:
US Previously Marketed
Source:
CREMOTHALIDINE PHTHALYLSULFATHIAZOLE by MERCK
(1961)
Source URL:
First approved in 1946
Source:
Sulfathalidine by Sharp & Dohme (MSD)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phthalylsulfathiazole is a sulfonamide antibiotic. Phthalylsulfathiazole is an effective remedy in the treatment of dysentery, diarrhea and other intestinal fluxes. It inhibits dihydropteroate synthetase activity of bacteria. In veterinary, it is used for the treatment of diarrhea and enteritis of the calves, dysentery in sheep, gastroenteritis in foals and adult equines, enteritis caused by food poisoning. Phthalylsulfathiazole is only slightly absorbed from the gut, about 5 percent of the quantity ingested being eliminated in the urine. Consequently, it produces little or no systemic effects with virtually no risk of crystalluria, haematuria or oliguria. In hyper-susceptible people, it may cause gastrointestinal side effects, like nausea, vomiting, etc.
Status:
US Previously Marketed
First approved in 1946

Class (Stereo):
CHEMICAL (ACHIRAL)



Trimethadione (brand name is TRIDIONE) is an oxazolidinedione compound that was developed as an antiepileptic agent for control of petit mal seizures that are refractory to treatment with other drugs. Tridione does not modify the maximal seizure pattern in patients undergoing electroconvulsive therapy and has a sedative effect that may increase to the point of ataxia when excessive doses are used. Trimethadione acts as a voltage-activated T-type Ca2+ channel blocker. Trimethadione is rapidly absorbed from the gastrointestinal tract. It is demethylated by liver microsomes to the active metabolite, dimethadione. Approximately 3% of a daily dose of tridione is recovered in the urine as the unchanged drug. The majority of trimethadione is excreted slowly by the kidney in the form of dimethadione.
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.
Nitrofurazone is used to treat burns that have become infected. It is also used to treat skin infections due to skin grafts. It works by killing bacteria or preventing their growth. The exact mechanism of action is unknown. Nitrofurazone inhibits several bacterial enzymes, especially those involved in the aerobic and anaerobic degradation of glucose and pyruvate. The severe or irreversible adverse effects of Nitrofurazone, which give rise to further complications include Peripheral neuropathy, Thromboembolic disorder.
Status:
US Previously Marketed
First approved in 1945
Source:
Methionine by Various Mfrs.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Methionine is an non-polar, aliphatic, essential α-amino acid that is used in the biosynthesis of proteins. High levels of methionine can be found in eggs, sesame seeds, Brazil nuts, fish, meats and some other plant seeds; methionine is also found in cereal grains. Most fruits and vegetables contain very little of it. Most legumes are also low in methionine. However, it is the combination of methionine and cystine which is considered for completeness of a protein. There is scientific evidence that restricting methionine consumption can increase lifespans in some animals. However, since methionine is an essential amino acid, it cannot be entirely removed from animals' diets without disease or death occurring over time. For example, rats fed a diet without methionine developed steatohepatitis (fatty liver), anemia and lost two thirds of their body weight over 5 weeks. Administration of methionine ameliorated the pathological consequences of methionine deprivation.
Status:
US Previously Marketed
First approved in 1944

Class (Stereo):
CHEMICAL (ACHIRAL)


Aminohippurate (p-aminohippuric acid, PAH, PAHA) is the glycine amide of p-aminobenzoic acid. Aminohippuric acid sodium salt is an agent to measure effective renal plasma flow (ERPF).
Dicumarol is an coumarin-like compound found in sweet clover. It is used as oral anticoagulant and acts by inhibiting the hepatic synthesis of vitamin K-dependent coagulation factors (prothrombin and factors VII, IX, and X). It results in decresed prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots. Dicumarol is also used in biochemical experiments as an inhibitor of reductases.
Status:
US Previously Marketed
Source:
Tuamine Sulfate by Lilly
(1943)
Source URL:
First approved in 1943
Source:
Tuamine Sulfate by Lilly
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Tuaminoheptane (or 2-aminoheptane), a nasal decongestant that is on the list of prohibited substances published by the World Anti-Doping Agency due to its stimulating properties. Tuaminoheptane is a stimulant of the sympathetic nervous system, similarly to several other known drugs targeting norepinephrine transporter

Showing 1251 - 1260 of 3134 results