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

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Showing 11 - 20 of 129 results

Status:
US Approved OTC
Source:
21 CFR 341.12(e) cough/cold:antihistamine dexchlorpheniramine maleate
Source URL:
First approved in 1958
Source:
Polaramine by Schering
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dexchlorpheniramine, the d-isomer of the racemic compound chlorpheniramine, is two times more active than chlorpheniramine. Dexchlorpheniramine does not prevent the release of histamine, but rather, competes with free histamine for binding at the H1-receptor sites, and competitively antagonizes the effects of histamine on H1-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Blockade of H1-receptors also suppresses the formation of oedema, flare, and pruritus that result from histaminic activity. Since dexchlorpheniramine binds to central and peripheral H1-receptors, sedative effects are likely to occur. H1-antagonists are structurally similar to anticholinergic agents and therefore possess the potential to exhibit anticholinergic properties of varying degrees. They also have antipruritic effects. Dexchlorpheniramine has high antihistaminic activity, moderate anticholinergic effects and minimal sedative effects. The drug does not possess antiemetic properties.
Status:
US Previously Marketed
Source:
QUIACTIN 400MG by MERRELL
(1961)
Source URL:
First approved in 1958
Source:
Quiactin by Merrell (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Oxanamide is an anxiolytic and muscle relaxant that was effective in the treatment of anxiety resulting from premenstrual syndrome, menopause. The tranquilizing effect of oxanamide was noticeable within two or three days, and improvement in nervous and emotional symptoms was soon evident. Information about the current use of this drug is not available.
Status:
US Previously Marketed
Source:
Cyclospasmol by Ives-Cameron (Ives)
(1958)
Source URL:
First approved in 1958
Source:
Cyclospasmol by Ives-Cameron (Ives)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Cyclandelate is a vasodilator developed for the treatment of cardiovascular diseases. The drug was used in many countries for such diseases as intermittent claudication, arteriosclerosis obliterans, thrombophlebitis, nocturnal leg cramps, local frostbite, Raynaud's phenomenon. In the USA it was also approved for intermittent claudication and cognitive dysfunction in Alzheimer's disease under the name Cyclospasmol. Cyclandelate exerts its effect by blocking calcium channels and inhibiting smooth muscles contration. Cyclandelate was withdrawn from the market in the USA for lack of effectiveness.
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
Source:
TKO/Entrin by Modern
(1958)
Source URL:
First approved in 1958
Source:
TKO/Entrin by Modern
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Diethylamine salicylate is a salicylic acid salt, that is a cost-effective and simple, first-line treatment for rheumatic and minor musculoskeletal conditions including lumbago, fibrositis, sciatica, bruises, and strains. Salicylic acid directly and irreversibly inhibits the activity of both types of cyclo-oxygenases (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid. Salicylate's antirheumatic (nonsteroidal anti-inflammatory) actions are a result of its analgesic and anti-inflammatory mechanisms.
Status:
US Previously Marketed
Source:
CAPSEBON by PITMAN MOORE
(1961)
Source URL:
First approved in 1958
Source:
Capsebon by Pitman-Moore (Dow Chem., USA)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cadmium is a heavy metal that causes toxicity in humans and animals. Cadmium chloride is used due to its solubility in water and its ability to produce high concentrations of cadmium at the target site. Cadmium chloride is used in printing, photocopying, dyeing, analytical chemistry. Experiments on rodents have shown that this compound caused renal toxicity. Oxidative stress plays a key role in cadmium chloride-induced cyto/genotoxicity.
Status:
US Previously Marketed
Source:
Murel by Ayerst
(1958)
Source URL:
First approved in 1958
Source:
Murel by Ayerst
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Valethamate bromide ( sold under many brand names such as Epidosin, Dilaton, Valosin, Valamate, Osdil etc), a quarternary ammonium agent, has been used in augmentation of labor. Valethamate has antimuscarinic action and blocks cholinergic receptors in the ganglia. This action along with the direct action on the smooth muscles of the cervix is thought to help cervical dilatation during labor. Since it is not selective, it exerts anticholinergic side effects such as tachycardia, flushing, cotton mouth and photophobia due to mydriasis. Common side effects are palpitations, increased heart rate, arrhythmia, excessive thirst, reduced bronchial secretions, dry mouth, Photophobia, dry skin, loss of accommodation, slow heart rate, flushing.
Status:
US Previously Marketed
Source:
Sinaxar by Armour
(1958)
Source URL:
First approved in 1958
Source:
Sinaxar by Armour
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Styramate is a nonsedative skeletal muscle relaxant drug, developed by the Armour Pharmaceutical Company in 1952. The drug induces relaxation of skeletal musculus by interruption of nerve transmission in the spinal cord and brain stem rather than by exerting a blocking effect at the junction between the motor nerves and the muscles. In mouse studies styramate was found to exert a selective antagonism to hindleg extensor tonic spasm, induced by maximal electroshock, pentylenetetrazol, and strychnine sulfate. In the clinic, the drug was used in patients with neurologic and neuromuscular disorders, secondary muscular spasms. Styramate is marketed in South Africa under tradename Sinaxamol.
Status:
First approved in 1958
Source:
Suvren by Ayerst
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

CAPTODIAME, also known as captodiamine, is a diphenylmethane derivative. It is a 5-HT2c receptor antagonist and agonist at sigma-1 and D3 dopamine receptors. It is an antihistamine which is used as a sedative and anxiolytic. CAPTODIAME is probably useful in preventing benzodiazepine withdrawal syndrome.

Showing 11 - 20 of 129 results