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

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Showing 21 - 30 of 186 results

Status:
First approved in 1950
Source:
Chloromycetin by Warner-Lambert
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Chloramphenicol is a broad-spectrum antibiotic that was first isolated from Streptomyces venezuelae in 1947. The drug was subsequently chemically synthesized. It has both a bacteriostatic and bactericidal effect; in the usual therapeutic concentrations it is bacteriostatic. Chloramphenicol is used for the treatment of serious gram-negative, gram-positive, and anaerobic infections. It is especially useful in the treatment of meningitis, typhoid fever, and cystic fibrosis. It should be reserved for infections for which other drugs are ineffective or contraindicated. Chloramphenicol, a small inhibitor of bacterial protein synthesis, is active against a variety of bacteria and readily enters the CSF. It has been used extensively in the last decades for the treatment of bacterial meningitis. In industrialized countries, chloramphenicol is restricted mostly to topical uses because of the risk of induction of aplastic anemia. However, it remains a valuable reserve antibiotic for patients with allergy to β-lactam antibiotics or with CNS infections caused by multiresistant pathogens.
Status:
First marketed in 1921
Source:
Syrup of Ferrous Iodide U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Iron(II) gluconate (also known as a ferrous gluconate) is used in the treatment of hypochromic anemia. The real problem of iron therapy is not the theoretical utilization of iron, or the reticulocyte response, or even the daily increase of hemoglobin. These are important only as they indicate the return of the patients' blood to normal in a reasonably short time without undue inconvenience. Most patients suffering from hypochromic anemia respond well to most forms of iron when administered in adequate dosage. For the patients who cannot tolerate the usual iron compounds, it is important to have a medication which is effective and which causes minimum disturbance. Ferrous gluconate is such a medicament.
Lithium is an alkali metal widely used in industry. Lithium salts are indicated in the treatment of manic episodes of Bipolar Disorder. The use of lithium in psychiatry goes back to the mid-19th century. Early work, however, was soon forgotten, and John Cade is credited with reintroducing lithium to psychiatry for mania in 1949. Mogens Schou undertook a randomly controlled trial for mania in 1954, and in the course of that study became curious about lithium as a prophylactic for depressive illness. In 1970, the United States became the 50th country to admit lithium to the marketplace. The specific mechanisms by which lithium exerts its mood-stabilizing effects are not well understood. Lithium appears to preserve or increase the volume of brain structures involved in emotional regulation such as the prefrontal cortex, hippocampus and amygdala, possibly reflecting its neuroprotective effects. At a neuronal level, lithium reduces excitatory (dopamine and glutamate) but increases inhibitory (GABA) neurotransmission; however, these broad effects are underpinned by complex neurotransmitter systems that strive to achieve homeostasis by way of compensatory changes. For example, at an intracellular and molecular level, lithium targets second-messenger systems that further modulate neurotransmission. For instance, the effects of lithium on the adenyl cyclase and phospho-inositide pathways, as well as protein kinase C, may serve to dampen excessive excitatory neurotransmission. In addition to these many putative mechanisms, it has also been proposed that the neuroprotective effects of lithium are key to its therapeutic actions. In this regard, lithium has been shown to reduce the oxidative stress that occurs with multiple episodes of mania and depression. Further, it increases protective proteins such as brain-derived neurotrophic factor and B-cell lymphoma 2, and reduces apoptotic processes through inhibition of glycogen synthase kinase 3 and autophagy.
Status:
US Approved OTC
Source:
21 CFR 341.12(h) cough/cold:antihistamine doxylamine succinate
Source URL:
First approved in 1948

Class (Stereo):
CHEMICAL (RACEMIC)



Doxylamine is an antihistamine commonly used as a sleep aid. This drug is also used to relieve symptoms of hay fever (allergic rhinitis), hives (rash or itching), and other allergic reactions. Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power far superior to virtually every other antihistamine on the market, with the exception of diphenhydramine (Benadryl). It is also the most powerful over-the-counter sedative available in the United States, and more sedating than many prescription hypnotics. In a study, it was found to be superior to even the barbiturate, phenobarbital for use as a sedative. Doxylamine is also a potent anticholinergic. Like other antihistamines, doxylamine acts by competitively inhibiting histamine at H1 receptors. It also has substantial sedative and anticholinergic effects. Used alone as a short-term sleep aid, in combination with other drugs as a night-time cold and allergy relief drug. Also used in combination with Vitamin B6 (pyridoxine) to prevent morning sickness in pregnant women.
Ferric chloride is a compound used as a food additive, a haemostatic or treatment for hypochromic anaemia. Ferric chloride induced vascular injury is a widely used model of occlusive thrombosis that reports platelet activation and aggregation in the context of an aseptic closed vascular system. Iron i.v. ferric chloride (960 mg) has being shown to be effective in correcting anaemia in HD patients with iron deficiency.
Status:
Investigational
Source:
NCT02783989: Not Applicable Interventional Completed Cardiovascular Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

E-7090 is a novel selective inhibitor of fibroblast growth factor receptors, that displays potent anti-tumor activity. It is a promising candidate as a therapeutic agent for the treatment of tumors harboring FGFR genetic abnormalities. E-7090 is an orally available and selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses E-7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E-7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. E-7090 showed selective antiproliferative activity against cancer cell lines harboring FGFR genetic abnormalities and decreased tumor size in a mouse xenograft model using cell lines with dysregulated FGFR. Furthermore, E-7090 administration significantly prolonged the survival of mice with metastasized tumors in the lung. It is being investigated in a Phase I clinical trial for treatment of patients with solid tumors.
Status:
Investigational
Source:
INN:carsatrin [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Carsatrin (also known as RWJ 24517) is purinylpiperazine derivative patented by Ortho Pharmaceutical Corp. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+,K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin
Status:
Investigational
Source:
INN:lanraplenib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:emilumenib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)