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

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Showing 91 - 100 of 257 results

Status:
US Previously Marketed
Source:
RETROPAQUE by WINTHROP
(1959)
Source URL:
First approved in 1959

Class (Stereo):
CHEMICAL (ACHIRAL)

Methiodal is used in lumbar myelography as a contrast agent.
Status:
US Previously Marketed
First approved in 1957

Class (Stereo):
CHEMICAL (ACHIRAL)



Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell. Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose.
Status:
US Previously Marketed
Source:
Dionosil by Picker
(1954)
Source URL:
First approved in 1954
Source:
Dionosil by Picker
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Propyliodone (INN, trade name Dionosil) is a molecule used as a contrast medium. It was developed by a team at Imperial Chemical Industries in the late 1930s. Propyliodone used as radiopque medium for brochographic use. When directly instilled into the bronchi resulting in well-defined bronchograms for atleast 30 min. Because of its toxicity, Propyliodone should only be used if absolutely essential. It is of Synthetic origin and belongs to Iodinated Radio-opaque Compounds. It belongs to Radiopaque Agents pharmacological group on the basis of mechanism of action and also classified in Diagnostic Aids pharmacological group. Oral absorption of Propyliodone is found to be 101% and metabolism is reported Lungs and Gut wall. Propyliodone is primarily indicated in conditions like Paget's disease of bone, Radiological contrast agent. Propyliodone produces potentially life-threatening effects which include Fever, Anaphylaxis, Repiratory obstruction, Cerebral embolization, which are responsible for the discontinuation of Propyliodone therapy. The signs and symptoms that are produced after the acute overdosage of Propyliodone include Airway obstruction. The symptomatic adverse reactions produced by Propyliodone are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Fever, Malaise, Nausea and vomiting, Aching joints.
Iodipamide is used as a contrast agent for cholecystography and intravenous cholangiography. Following intravenous administration of Cholografin Meglumine, iodipamide is carried to the liver where it is rapidly secreted. The contrast medium appears in the bile within 10 to 15 minutes after injection, thus permitting visualization of the hepatic and common bile ducts, even in cholecystectomized patients. Iodipamide (Cholografin Meglumine) is indicated for intravenous cholangiography and cholecystography as follows: (a) visualization of the gallbladder and biliary ducts in the differential diagnosis of acute abdominal conditions, (b) visualization of the biliary ducts, especially in patients with symptoms after cholecystectomy, and (c) visualization of the gallbladder in patients unable to take oral contrast media or to absorb contrast media from the gastrointestinal tract. The biliary ducts are readily visualized within about 25 minutes after administration, except in patients with impaired liver function. The gallbladder begins to fill within an hour after injection; maximum filling is reached after two to two and one-half hours. Organic iodine compounds block x-rays as they pass through the body, thereby allowing body structures containing iodine to be delineated in contrast to those structures that do not contain iodine. The degree of opacity produced by these iodinated organic compounds is directly proportional to the total amount (concentration and volume) of the iodinated contrast agent in the path of the x-rays. Iodipamide's primary excretion through the hepato-biliary system and concentration in bile allows visualization of the gallbladder and biliary ducts.
Status:
US Previously Marketed
Source:
Histalog by Eli Lilly
(1954)
Source URL:
First approved in 1954
Source:
Histalog by Eli Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



BETAZOLE is a histamine H2 receptor agonist used clinically to test gastric secretory function.
Status:
US Previously Marketed
Source:
CYSTOKON by MALLINCKRODT
(1961)
Source URL:
First approved in 1953

Class (Stereo):
CHEMICAL (ACHIRAL)



Acetrizoic acid (trade names Gastrografina, Urografina in Portugal) is a palatable lemon-flavored water-soluble iodinated radiopaque X-ray contrast medium for oral or rectal administration only. Acetrizoic acid is indicated for radiographic examination of segments of the gastrointestinal tract (esophagus, stomach, proximal small intestine, and colon). The preparation is particularly indicated when a more viscous agent such as barium sulfate, which is not water-soluble, is not feasible or is potentially dangerous. Administration of hypertonic Gastrografin solutions may lead to hypovolemia and hypotension due to fluid loss from the intestine.
Status:
US Previously Marketed
Source:
Nalline HCl by Merck Sharp & Dohme
(1952)
Source URL:
First approved in 1952
Source:
Nalline HCl by Merck Sharp & Dohme
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Nalorphine has a mixed opioid agonist-antagonist properties. Nalorphine inhibits the cholinesterases of mouse brain, bovine erythrocytes and horse serum. It acts on mu-, k- and sigma-opioid receptors. Nalorfin by virtue of the agonistic effect has an analgesic effect but to a much lesser extent than morphine. Initially, before the appearance of a "pure" morphine-naloxone antagonist, nalorphine was used as an antidote for severe respiratory depression and other body function disorders caused by acute poisoning in case of an overdose of morphine, promedol, fentanyl or other narcotic analgesics, or with increased sensitivity to them. At present, nalorphine is practically not used for this purpose. It was replaced by naloxone. Large doses of nalorphine can cause nausea, cramps, drowsiness, headache, mental stimulation.
Status:
US Previously Marketed
Source:
Aurcoloid by ABBOTT
(1950)
Source URL:
First approved in 1950

Class (Stereo):
CHEMICAL (ACHIRAL)

The therapeutic use of radioactive colloidal gold Gold Au-198 (Au198) was first described by Sheppard et al., who reported on intravenous use in 1947. Its possibilities for the treatment of various malignant processes have been explored in great variation. Gold Au-198 is an antineoplastic, diagnostic aid (liver imaging) and radioactive agent. Thus, intracavitary instillation of colloidal radioactive gold Au-198 was used for treatment of patients with multiple papillomata of the bladder. Approximately 300 mc. of gold was instilled into the bladder for four to six hours to deliver a dose of about 4,000 to 5,000 r to the bladder epithelium. The treatment had no harmful side-effects locally or on the general condition of the patient. It was also used to estimate the hepatic blood flow in children with active or progressive chronic hepatitis. Gold Au-198 was used in the combination therapy of rectal cancer.
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).