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

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Showing 581 - 590 of 1216 results

Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(20) weight control choline
Source URL:
First approved in 2001
Source:
Vitamin B Complex 150 by Covetrus North America
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



CHOLINE is a basic constituent of lecithin that is found in many plants and animal organs. Choline was officially recognized as an essential nutrient by the Institute of Medicine in 1998.1 Its role in the body is complex. It is needed for neurotransmitter synthesis (acetylcholine), cell-membrane signaling (phospholipids), lipid transport (lipoproteins), and methyl-group metabolism (homocysteine reduction). It is the major dietary source of methyl groups via the synthesis of S-adenosylmethionine (AdoMet). At least 50 AdoMet-dependent reactions have been identified in mammals, and it is likely that the number is much higher. Choline is required to make the phospholipids phosphatidylcholine, lysophosphatidylcholine, choline plasmalogen, and sphingomyelin—essential components for all membranes. It plays important roles in brain and memory development in the fetus and appears to decrease the risk of the development of neural tube defects. The importance of choline in the diet extends into adulthood and old age. In a study of healthy adult subjects deprived of dietary choline, 77% of the men and 80% of the postmenopausal women developed signs of subclinical organ dysfunction (fatty liver or muscle damage). Less than half of premenopausal women developed such signs. Ten percent of the subjects studied developed fatty liver, muscle damage, or both when they consumed the Adequate Intake (AI) of choline. The damage was reversed when they consumed a high-choline diet. Plasma choline concentration has been found to vary in response to diet, decreasing approximately 30 percent in humans fed a choline-deficient diet for 3 weeks. Based on estimated dietary intakes and studies reporting liver damage with lower choline intakes, the Institute of Medicine, Food and Nutrition Board set the AI for choline at 425 milligrams/per day for women aged 19 and older, and 550 milligrams/per day for men aged 19 and older.
Saquinavir (brand names Invirase and Fortovase) is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS. Saquinavir is an inhibitor of HIV protease. HIV protease is an enzyme required for the proteolytic cleavage of viral polyprotein precursors into individual functional proteins found in infectious HIV. Saquinavir is a peptide-like substrate analog that binds to the protease active site and inhibits the activity of the enzyme. Saquinavir inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious virus particles. The most frequent adverse events with saquinavir in either formulation are mild gastrointestinal symptoms, including diarrhea, nausea, loose stools & abdominal discomfort. Invirase is better tolerated than Fortovase.
Status:
US Previously Marketed
Source:
LAMIVUDINE; STAVUDINE by MATRIX LABS
(2007)
Source URL:
First approved in 1994

Class (Stereo):
CHEMICAL (ABSOLUTE)



Stavudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Stavudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. Stavudine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Stavudine is used for the treatment of human immunovirus (HIV) infections. Stavudine is sold under the brand name Zerit among others.
Cholesterol is a sterol (a combination steroid and alcohol) and a lipid found in the cell membranes of all body tissues, and transported in the blood plasma of all animals. The high level of cholesterol in the blood is a marker of hypercholesterolemia, also called dyslipidemia. As a part of homeopathic product, it helps to support general liver and gallbladder health, and is used for temporary relief of symptoms related to adrenal glands such as fatigue and low energy. Cholesterol binds to and affects the gating of a number of ion channels such as the nicotinic acetylcholine receptor (nAChR) Inwardly-rectifying K+ channels (Kir); Transient receptor potential vanilloid 1 channels (TRPV1) and Large-conductance Ca2+-sensitive voltage-gated K+ channels (BK). It was shown the new mechanistic insights into the role of cholesterol in the regulation of nAChR, showing that cholesterol regulates the channels by two distinct mechanisms: stabilization of the channels in a resting state that depends on specific lipid-protein interactions and facilitation of the transitions between uncoupled and coupled states that depends on the hydrophobic thickness of the membrane
Status:
US Previously Marketed
First approved in 1991

Class (Stereo):
CHEMICAL (ABSOLUTE)



Didanosine was developed by Bristol-Myers Squibb in collaboration with the NIH for the treatment of HIV-1 infections. Upon administration the drug is metabolized to the active metabolite which inhibits HIV-1 reverse transcriptase both by competing with deoxyadenosine 5'-triphosphate and by its incorporation into viral DNA. Didanosine was approved by FDA under the name Videx (among the other names).
Status:
US Previously Marketed
First approved in 1986

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Clofazimine (Lamprene®) is a fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine (Lamprene®) exerts a slow bactericidal effect on Mycobacterium leprae (Hansen’s bacillus). It inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. It also exerts anti-inflammatory properties in controlling erythema nodosum leprosum reactions. However, its precise mechanisms of action are unknown.
Status:
US Previously Marketed
Source:
SHADE UVAGUARD by BAYER HEALTHCARE LLC
(1992)
Source URL:
First approved in 1984
Source:
NU-DERM SUNFADER Skin Lightener with Sunscreen (SPF 15) PABA FREE by OMP, INC.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Octinoxate, also called Octyl methoxycinnamate or (OMC), is a UV filter. It can be absorbed rapidly through skin.Octinoxate filters UV‐B rays from the sun, although it does not protect against UV-A rays. Octinoxate dissolves in oil, which makes it a fat-seeking substance in the body. It is formed by combining methoxycinnamic acid and 2-ethylhexanol compounds which are not harmful on their own. When mixed together, they form a clear liquid that does not dissolve in water. Octinoxate is found in hair color products and shampoos, sunscreen, lipstick, nail polish, and skin creams. In products other than sunscreens, it is used as a UV filter to protect the products from degrading when exposed to the sun.
Status:
US Previously Marketed
Source:
EXOSURF NEONATAL by GLAXOSMITHKLINE
(1990)
Source URL:
First approved in 1984
Source:
NU-DERM SUNFADER Skin Lightener with Sunscreen (SPF 15) PABA FREE by OMP, INC.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cetyl alcohol is the 16-carbon alcohol corresponding to palmitic acid, so called because it is isolated from among the hydrolysis products of spermaceti. This medication is used as a moisturizer to treat or prevent dry, rough, scaly, itchy skin and minor skin irritations (e.g., diaper rash, skin burns from radiation therapy). Most emollients can be used safely and effectively with no side effects. However, burning, stinging, redness, or irritation may occur. A very serious allergic reaction to this drug is rare.
Niclosamide is an antihelminth used against tapeworm infections. It may act by the uncoupling of the electron transport chain to ATP synthase. The disturbance of this crucial metabolic pathway prevents creation of adenosine tri-phosphate (ATP), an essential molecule that supplies energy for metabolism. Niclosamide works by killing tapeworms on contact. Adult worms (but not ova) are rapidly killed, presumably due to uncoupling of oxidative phosphorylation or stimulation of ATPase activity. The killed worms are then passed in the stool or sometimes destroyed in the intestine. Niclosamide may work as a molluscicide by binding to and damaging DNA. Niclosamide is used for the treatment of tapeworm and intestinal fluke infections: Taenia saginata (Beef Tapeworm), Taenia solium (Pork Tapeworm), Diphyllobothrium latum (Fish Tapeworm), Fasciolopsis buski (large intestinal fluke). Niclosamide is also used as a molluscicide in the control of schistosomiasis. Niclosamide was marketed under the trade name Niclocide, now discontinued.
Status:
US Previously Marketed
First approved in 1981

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfadoxine is an antimalarial agent which, together with pyrimethamine, composes an FDA-approved drug, Fansidar. Sulfadoxine acts by inhibiting dihydropteroate synthase; it crosses the blood-brain barrier and achieves 30% to 60% of the plasma concentration.