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

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Showing 201 - 210 of 218 results

Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(27)(i) antimicrobial:first aid antiseptic thimerosal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Thimerosal is organomercury antiseptic and antifungal agent, used as a preservative in vaccines, immuloglobulins, nasal sprays, contact lens solutions. In USA, European Union countries thiomersal is no longer used in childhood vaccines due to public fears, although the FDA review of 1999 foud no evidence of harm from the use of thimerosal as a vaccine preservative, other than local hypersensitivity reactions. Thimerosal was used as a component of topical antiseptic solution and antiseptic ointment for treating cuts, nasal sprays, eye solutions, vaginal spermicides, diaper rash treatments, but re-evaluation of the drug in 1980-s demonstrated ineffectiveness and toxicity in topical pharmaceutical products, and topical thimerosal was withdrawn from the market. The mechanism of action of thimerosal has not been fully elucidated. It is believed that thimerosal inhibits sulfhydryl-containing active site of various enzymes and binds to sulfhydryl compounds, such as glutathione, cysteine, and SH groups of protein. In addition, thimerosal activates the InsP3 calcium channel on endoplasmic reticular membrane, thereby triggering the release of calcium from intracellular stores resulting in a calcium-induced calcium-influx of extracellular calcium. Consequently, thimerosal may induce or inhibit cellular functions dependent on calcium signaling.
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).
Status:
US Previously Marketed
First marketed in 1929
Source:
secobarbital
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Secobarbital sodium, a barbiturate, is FDA approved for the treatment of insomnia and for pre-anesthetic use. This drug binds at a distinct 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. Adverse reactions are drowsiness, lethargy, hangover, paradoxical excitement in elderly patients, somnolence. Rifampin may decrease secobarbital levels by increasing metabolism.
Sesamin is a naturally occurring compound found in sesame oil and in the bark and fruit of certain plant species. SESAMIN, (±)- is a racemic dl-form. The dl-form is also known as fagarol, and may be isolated from the bark of various fagara species. Sesamin, either as the d-form or the dl-form, has now been found to possess psychotropic activity, i.e., administration of appropriate dosages to a human or animal subject elicits a psychotropic response. Sesamin is catered to be a nutritional supplement that confers antioxidant and antiinflammatory effects (if touting its health properties) or possibly being an estrogen receptor modulator and fat burner (if targeting athletes or persons wishing to lose weight). Sesamin has a few mechanisms, and when looking at it holistically it can be summed up as a fatty acid metabolism modifier. It appears to inhibit an enzyme known as delta-5-desaturase (Δ5-desaturase) which is a rate-limiting enzyme in fatty acid metabolism; inhibiting this enzyme results in lower levels of both eicosapentaenoic acid (EPA, one of the two fish oil fatty acids) as well as arachidonic acid, and this mechanism appears to be relevant following oral ingestion. The other main mechanism is inhibiting a process known as Tocopherol-ω-hydroxylation, which is the rate-limiting step in the metabolism of Vitamin E; by inhibiting this enzyme, sesamin causes a relative increase of vitamin E in the body but particularly those of the gamma subset (γ-tocopherol and γ-tocotrienol) and this mechanism has also been confirmed to be active following oral ingestion. Sesamin is a potent and specific inhibitor of delta 5 desaturases in polyunsaturated fatty acid biosynthesis. Sesamin inhibits particular CYP3A enzymes that are involved in vitamin E metabolism, where the enzyme initially ω-hydroxylates vitamin E (required step) and then the rest of vitamin E is subject to fat oxidation. By inhibiting this step, sesamin causes an increase in circulating and organ concentrations of vitamin E. Sesamin is thought to have PPARα activating potential in the liver, but it is uncertain how much practical relevance this has in humans due to this being a mechanism that differs between species.
Status:
Possibly Marketed Outside US
Source:
Slim 2 by Bionutrigen Co., Ltd.
Source URL:
First approved in 2011

Class (Stereo):
CHEMICAL (RACEMIC)



Cianidanol is an antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms. One of the polyphenols present in green tea, (+)-catechin (Cianidanol), has been studied for its effects on animal models of hepatitis, as well as in human clinical studies. Pure (+)-catechin (also known as (+)- cyanidanol-3 – trade name Catergen) has been used to treat hepatitis since 1976. This compound has been shown to be an efficient immune stimulator, promoting activation of macrophages, cytotoxic-T-lymphocytes, and natural killer cells in mice. Several clinical studies demonstrate the effectiveness of (+)-catechin in the treatment of viral hepatitis. Pure (+)-catechin has been found to cause hemolysis in some patients, possibly by the promotion of antibody formation against (+)-catechin, which might cross-react with red blood cells. However, there are no reports in the literature of green tea, green tea extracts, or green tea polyphenols causing this side-effect.
Status:
Possibly Marketed Outside US
Source:
NCT04308317: Phase 4 Interventional Unknown status Corona Virus Disease 2019,COVID-19
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tetrandrine, isolated from the root of Stephania tetrandra S Moore, is a traditional Chinese clinical agent for silicosis, autoimmune disorders, inflammatory pulmonary diseases, cardiovascular diseases and hypertension. Tetrandrine is a potent MDR-reversing agent and is an ABCB1/ABCC1 inhibitor. Tetrandrine (CBT-1) is being developed by CBA Pharma, as an adjunctive therapy to chemotherapy in various cancer types with multiple drug resistance (MDR), including acute myelogenous leukemia , Breast, Non-Hodgkin’s Lymphoma, Hodgkin’s disease, Non-Small Cell Lung Cancer, Multiple Myeloma, Gallbladder, Pancreatic, Gastrointestinal Tract, Small Cell Lung Cancer, Bladder, Head & Neck, and Sarcoma.
Status:
Possibly Marketed Outside US
Source:
Japan:Tandospirone Citrate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sediel (generic name: tandospirone citrate, marketed as Sediel in Japan) is a new type of antianxiety drug developed independently by Sumitomo Pharmaceuticals. It acts selectively on only the serotonin nerves in the brain that play an important part in the formation of anxiety and depression, and demonstrates antianxiety and anti-depression effects. Since it does not act on the other nerves that are so extensive in the brain, there is virtually no hypnotic or sedative effect, and the drug displays virtually no drug-dependence or side effects such as drowsiness and dizziness. Sediel has been on sale in Japan since December 1996, and is recognized for recognized as effective in the treatment of generalized anxiety disorders. Tandospirone acts as a potent and selective 5-HT1A receptor partial agonist. It was also investigated the usefulness of 5-HT1A agonists for enhancing some types of cognitive performance and possibly social and work function in patients with schizophrenia, and related to this was discovered, that tandospirone in combination with atypical antipsychotic drugs can improve cognitive function in Schizophrenia.
mixture
Status:
Possibly Marketed Outside US
Source:
Cetrimide Cream 0.5% by Canadian Custom Packaging Company [Canada]
Source URL:

Class:
MIXTURE



Cetrimide is a quaternary ammonium compound. Cetrimide was first introduced as a combined cleanser and skin antiseptic by Barnes (1942). Cetrimide combines excellent detergent properties and minimal toxicity with a useful antiseptic action. Cetrimide affects membrane permeability allowing ‘leaking’ of essential cell constituents leading to cell death. This medication is a skin antiseptic and disinfectant prescribed for seborrhoeic dermatitis and wound cleansing. The cream has a bactericidal activity against gram-positive bacteria and incompatible with soaps and other anionic surfactants.
nucleic acid
Status:
US Previously Marketed
First approved in 2013

Class:
NUCLEIC ACID

Нeparin (or Unfractionated heparin ) is an anticoagulant indicated for both the prevention and treatment of thrombotic events such as deep vein thrombosis (DVT) and pulmonary embolism (PE) as well as atrial fibrillation (AF). Heparin can also be used to prevent excess coagulation during procedures such as cardiac surgery, extracorporeal circulation or dialysis, including continuous renal replacement therapy. Heparin administration can be by intravenous (or subcutaneous route. Intravenous heparin is continuously administered for therapeutic anticoagulation, while intermittent subcutaneous administration is used to prevent thromboembolism. Once administered, heparin binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin (factor IIa) and factor Xa. The heparin-ATIII complex can also inactivate factors IX, XI, XII, and plasmin, but the antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Typical adverse effects from heparin use include bleeding, thrombocytopenia, injection site reactions, and other adverse effects only seen with chronic heparin administration. Bleeding is a major complication associated with heparin use. Patients should undergo monitoring for new bleeding that may present in the urine or stool. Bleeding may also present as bruising, petechial rash and nosebleeds.

Showing 201 - 210 of 218 results