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

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Showing 671 - 680 of 2252 results

Status:
US Previously Marketed
Source:
Cyclamycin by Wyeth
(1958)
Source URL:
First approved in 1958
Source:
Cyclamycin by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Troleandomycin (also known Triacetyl-oleandomycin and having brand name Tao) is a macrolide antibiotic which used to for the treat of infections of the upper and lower respiratory tract: such as tonsillitis, bronchitis, sinusitis, and pneumonia. However, the brand name Tao was discontinued. Troleandomycin acts by penetrating the bacterial cell membrane and reversibly binding to the 50 S subunit of bacterial ribosomes or near the "P" or donor site so that binding of tRNA (transfer RNA) to the donor site is blocked. Translocation of peptides from the "A" or acceptor site to the "P" or donor site is prevented, and subsequent protein synthesis is inhibited.
Status:
US Previously Marketed
First approved in 1958

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlorpropamide (DIABINESE®), is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. It appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which chlorpropamide (DIABINESE®) lowers blood glucose during long-term administration has not been clearly established. Extra-pancreatic effects may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. While chlorpropamide is a sulfonamide derivative, it is devoid of antibacterial activity. Chlorpropamide (DIABINESE®) may also prove effective in controlling certain patients who have experienced primary or secondary failure to other sulfonylurea agent.
Status:
US Previously Marketed
Source:
PROPOXYPHENE HYDROCHLORIDE by ALRA
(1982)
Source URL:
First approved in 1957

Class (Stereo):
CHEMICAL (RACEMIC)



Propoxyphene is a centrally acting opiate analgesic. Propoxyphene is an odorless, freely soluble in water, white crystalline powder with a bitter taste. In vitro studies demonstrated propoxyphene and the metabolite norpropoxyphene inhibit sodium channels (local anesthetic effect) with norpropoxyphene being approximately 2 fold more potent than propoxyphene and propoxyphene approximately 10 fold more potent than lidocaine. Propoxyphene and norpropoxyphene inhibit the voltage-gated potassium current carried by cardiac rapidly activating delayed rectifier (hERG) channels with approximately equal potency. It is unclear if the effects on ion channels occur within therapeutic dose range. Propoxyphene is indicated for the relief of mild to moderate pain.
Levallorphan (brand name Lorfan), is an opiate antagonist of morphine family. Levallorphan was formerly used in general anesthesia, mainly to reverse the respiratory depression produced by opioid analgesics and barbiturates used for induction of surgical anaesthesia whilst maintaining a degree of analgesia. Levallorphan was also used in combination with opioid analgesics to reduce their side effects, mainly in obstetrics. The combination of levallorphan with pethidine was used so frequently, a standardized formulation was made available, known as Pethilorfan, by Roche Products Ltd in later 1950s. Is known to be used for narcotic overdose. Levallorphan is similar to naloxone but differs from naloxone in that it also possesses some agonist properties. It acts as an antagonist and partial agonist of the mu opioid receptor (MOR). Levallorphan can produce severe mental reactions at sufficient doses including hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety, confusion, dizziness, disorientation, derealization, feelings of drunkenness, and bizarre, unusual, or disturbing dreams.
Status:
US Previously Marketed
Source:
Synatan by Irwin, Neisler (Mallinckrodt)
(1955)
Source URL:
First approved in 1955
Source:
Synatan by Irwin, Neisler (Mallinckrodt)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


DEXTROAMPHETAMINE TANNATE is a salt of dextroamphetamine, amphetamine enantiomer. It is used as CNS stimulant in the treatment of attention deficit hyperactivity disorder.
Status:
US Previously Marketed
Source:
METATENSIN #2 by SANOFI AVENTIS US
(1982)
Source URL:
First approved in 1954

Class (Stereo):
CHEMICAL (ABSOLUTE)



Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.
Status:
US Previously Marketed
Source:
Dactil by lakeside (MerrellNational)
(1954)
Source URL:
First approved in 1954
Source:
Dactil by lakeside (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs. It’s usually used to kill the cramp-like pain of gastric/duodenal ulcer, gastritis, enteritis, gallstones, cholecystitis and biliary tract dyskinesia and to improve some symptoms in threatened miscarriage/premature delivery. Piperidolate blocked the contraction of ACh, Ba ++ and electrical stimulations on the isolated rat, mouse and guinea-pig ileum and trachea. In guinea-pig teania caeci, piperidolate like papaverine blocked specifically the tonic response, however, piperidolate in high doses completely blocked both spike and tonic responses. These results indicate that spasmolytic action of piperidolate like that of papaverine may depend upon inhibition of the release of store Ca++. Moreover piperidolate, given at high doses, may inhibit the contractile elements in the smooth muscle. In the rat uterus pretreated with sex hormones, piperidolate nonspecifically blocked the contraction of ACh, Ba ++ and oxytocin and sex hormones had no influence on the spasmolytic action of piperidolate.
Thiamylal is a barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. Thiamylal, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia. Thiamylal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
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:
Piperate Tartrate by Lincoln
(1954)
Source URL:
First approved in 1954
Source:
Piperate Tartrate by Lincoln
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)