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

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Showing 11 - 20 of 117 results

Status:
US Approved OTC
Source:
21 CFR 349.18(d) ophthalmic:vasoconstrictor tetrahydrozoline hydrochloride
Source URL:
First approved in 1954
Source:
Tyzine by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Tetrahydrozoline is an alpha adrenergic receptor agonist, which is used in form of nasal solution or spray (Tyzin) for decongestion of nasal and nasopharyngeal mucosa.
Status:
US Approved OTC
Source:
21 CFR 341.14(a)(4) cough/cold:antitussive dextromethorphan hydrobromide
Source URL:
First approved in 1954
Source:
Romilar by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dextromethorphan is a non-narcotic morphine derivative widely used as an antitussive for almost 40 years. It has attracted attention due to its anticonvulsant and neuroprotective properties. It is a cough suppressant in many over-the-counter cold and cough medicines. In 2010, the FDA approved the combination product dextromethorphan/quinidine for the treatment of pseudobulbar affect. Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high-affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives and is used to study the involvement of glutamate receptors in neurotoxicity. Dextromethorphan (DM) is a sigma-1 receptor agonist and an uncompetitive NMDA receptor antagonist. The mechanism by which dextromethorphan exerts therapeutic effects in patients with pseudobulbar affect is unknown. Dextromethorphan should not be taken with monoamine oxidase inhibitors due to the potential for serotonin syndrome. Dextromethorphan is extensively metabolized by CYP2D6 to dextrorphan, which is rapidly glucuronidated and unable to cross the blood-brain barrier.
Status:
US Approved Allergenic Extract (1994)
First approved in 1954
Source:
Sterosan by Geigy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlorquinaldol is a halogenated hydroxyquinoline with properties similar to those of clioquinol. It is mainly applied topically in infected skin conditions and in vaginal infections. The product is applied for local treatment of cortico-sensitive dermatosis with moderately manifested superinfection, acute and subacute eczema, dermatitis, pyodermia, intertrigo, infected wounds, dermatomycosis, pemphigus in newborn. Chlorquinaldol is also used as antiseptic, fungistat, or deodorant. Chlorquinaldol is not commercially available in the U.S. but is used in other countries principally as an amebicide for nonspecific diarrheas and gynecologic infections. It is known most commonly under the proprietary name of Sterosan. Other trade names include Cynotherax, Gyno-Sterosan, Saprosan, Siogeno, Siosteran, Slosteran and Steroxin.
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.
Status:
US Previously Marketed
Source:
Medomin by Geigy
(1955)
Source URL:
First approved in 1954
Source:
Heptabarbital by Ciba-Geigy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

HEPTABARBITAL is an intermediate or short term barbiturate. It binds to the GABAA receptor at either the alpha or the beta subunit. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. HEPTABARBITAL was formerly used as a sedative and hypnotic drug.
PENTHIENATE, a synthetic anticholinergic, depresses the motility and secretion of the stomach and reduces the motor activity of the intestine by blocking vagal stimulation. It is used in the treatment of peptic ulcer and dyspepsia.
Status:
US Previously Marketed
Source:
TOLSERAM 0.5GMTAB by SQUIBB
(1961)
Source URL:
First approved in 1954
Source:
Tolseram by Squibb
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

MEPHENESIN CARBAMATE, a mephenesin derivative, is a centrally acting muscle relaxant.
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.
Status:
US Previously Marketed
First approved in 1954

Class (Stereo):
CHEMICAL (ABSOLUTE)



Digoxin is a cardiac glycoside derived from the purple foxglove flower. In 1785, the English chemist, botanist, and physician Sir William Withering published his findings that Digitalis purpurea could be used to treat cardiac dropsy (congestive heart failure; CHF). Digoxin has been in use for many years, but was not approved by the FDA for treatment of heart failure (HF) until the late 1990s. Another FDA indication for digoxin is atrial fibrillation (AF). Digoxin also has numerous off-label uses, such as in fetal tachycardia, supra-ventricular tachycardia, cor pulmonale, and pulmonary hypertension. Digitoxin inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations. Increased intracellular concentrations of calcium may promote activation of contractile proteins (e.g., actin, myosin). Digoxin also has Para sympathomimetic properties. By increasing vagal tone in the sinoatrial and atrioventricular (AV) nodes, it slows the heart rate and AV nodal conduction.
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.

Showing 11 - 20 of 117 results