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

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Showing 31 - 40 of 3713 results

Status:
First marketed in 1937
Source:
Oreton-F by Schering
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Testosterone is a steroid sex hormone found in both men and women. In men, testosterone is produced primarily by the Leydig (interstitial) cells of the testes when stimulated by luteinizing hormone (LH). It functions to stimulate spermatogenesis, promote physical and functional maturation of spermatozoa, maintain accessory organs of the male reproductive tract, support development of secondary sexual characteristics, stimulate growth and metabolism throughout the body and influence brain development by stimulating sexual behaviors and sexual drive. In women, testosterone is produced by the ovaries (25%), adrenals (25%) and via peripheral conversion from androstenedione (50%). Testerone in women functions to maintain libido and general wellbeing. Testosterone exerts a negative feedback mechanism on pituitary release of LH and follicle-stimulating hormone (FSH). Testosterone may be further converted to dihydrotestosterone or estradiol depending on the tissue. The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects. Testosterone is used as hormone replacement or substitution of diminished or absent endogenous testosterone. Use in males: For management of congenital or acquired hypogonadism, hypogonadism associated with HIV infection, and male climacteric (andopause). Use in females: For palliative treatment of androgen-responsive, advanced, inoperable, metastatis (skeletal) carcinoma of the breast in women who are 1-5 years postmenopausal; testosterone esters may be used in combination with estrogens in the management of moderate to severe vasomotor symptoms associated with menopause in women who do not respond to adequately to estrogen therapy alone.
Estrone, one of the major mammalian estrogens, is an aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone. It is produced in vivo from androstenedione or from testosterone via estradiol. It is produced primarily in the ovaries, placenta, and in peripheral tissues (especially adipose tissue) through conversion of adrostenedione. Estrone may be further metabolized to 16-alpha-hydroxyestrone, which may be reduced to estriol by estradiol dehydrogenase. Estrogens enter the cells of responsive tissues (e.g. female organs, breasts, hypothalamus, pituitary) where they interact with estrogen receptors. Hormone-bound estrogen receptors dimerize, translocate to the nucleus of cells and bind to estrogen response elements (ERE) of genes. Binding to ERE alters the transcription rate of affected genes. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) release from the anterior pituitary. Estrone dl-Form is a derivative of estrone. As early as 1935 extensive research programs directed toward the total synthesis of the female sex hormone estrone were well under way. These studies have since been continued with increasing interest in laboratories all over the world. In 1942 Bachmann, Kushner and Stevenson succeeded in synthesizing a stereoisomer of the hormone,''estrone a." Using essentially the same synthetic scheme as Bachmann, et al., Anner and Miescher were able to isolate additional stereoisomers including dl-estrone (Estrone, (+-)-Isomer) . Six of the eight possible racemic forms, estrone, a-f, have now been reported. Dl-Estrone (Estrone, (+-)-Isomer) is less active than Estrone.
Status:
First marketed in 1925
Source:
carbon dioxide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Carbon dioxide is a colorless gas occurring naturally in Earth's atmosphere. Carbon dioxide is a primary carbon source for life on Earth. It is produced by all aerobic organisms during metabolism of carbohydrates and lipids. Carbon dioxide is used in food industry as an acidity regulator and for production of carbonated soft drinks and soda water. In medicine, carbon dioxide is commonly used as an insufflation gas for minimally invasive surgery (laparoscopy, endoscopy, and arthroscopy) to enlarge and stabilize body cavities to provide better visibility of the surgical area. A mixture of carbon dioxide and oxygen is used for stimulation of breathing after apnea, in anesthetic procedures to increase the depth of respiration, to facilitate blind intubations in anesthetic practice.
Status:
First marketed in 1921
Source:
Benzoic Acid U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Benzoic acid is a natural ingredient occurring in many foodstuffs and in plant extracts. Benzoic acid, its salts and esters are used as preservatives in cosmetic products, with a maximum concentration of 0.5 %. Benzoic acid and sodium benzoate are on the FDA list of substances that are generally recognized as safe (GRAS). Both may be used as antimicrobial agents, flavouring agents and as adjuvants with a current maximum level of 0.1% in food. Benzoic acid is a constituent of Whitfield Ointment, which is used for the treatment of fungal skin diseases such as tinea, ringworm, and athlete's foot. Adverse effect of Whitfield Ointment: occasionally, a localized mild inflammatory response occurs.
Status:
First marketed in 1921
Source:
Theophylline U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Since its discovery as component of the tea leaf by Albert Kossel in 1888, the history of theophylline (CAS 58-55-9) has been a long and successful one. At the turn of the century, theophylline became less expensive due to chemical synthesis and was primarily used as diuretic in subsequent years. It was Samuel Hirsch who discovered the bronchospasmolytic effect of theophylline in 1992, however, despite this pioneering discovery theophylline continued to be used primarily as diuretic and cardiac remedy. The molecular mechanism of bronchodilatation is inhibition of phosphodiesterase(PDE)3 and PDE4, but the anti-inflammatory effect may be due to histone deacetylase (HDAC) activation, resulting in switching off of activated inflammatory genes. Theophylline is indicated for the treatment of acute exacerbations of the symptoms and reversible airflow obstruction associated with asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.
Cocaine is an alkaloid ester extracted from the leaves of plants including coca. Cocaine is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. Cocaine is addictive due to its effect on the reward pathway in the brain. After a short period of use, there is a high risk that dependence will occur. Its use also increases the risk of stroke, myocardial infarction, lung problems in those who smoke it, blood infections, and sudden cardiac death. Cocaine sold on the street is commonly mixed with local anesthetics, cornstarch, quinine, or sugar which can result in additional toxicity. Following repeated doses, a person may have decreased the ability to feel pleasure and be very physically tired. Cocaine acts by inhibiting the reuptake of serotonin, norepinephrine, and dopamine. This results in greater concentrations of these three neurotransmitters in the brain. It can easily cross the blood-brain barrier and may lead to the breakdown of the barrier.
Status:
US Approved OTC
Source:
21 CFR 341.20(b)(1) cough/cold:nasal decongestant levmetamfetamine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levomethamphetamine is the levorotary (L-enantiomer) form of methamphetamine. Levomethamphetamine is a sympathomimetic vasoconstrictor which is the active ingredient in some over-the-counter (OTC) nasal decongestant inhalers in the United States. Levomethamphetamine crosses the blood-brain-barrier and acts as a TAAR1 agonist, functioning as a selective norepinephrine releasing agent (with few or no effects on the release of dopamine), so it affects the central nervous system, although its effects are qualitatively distinct relative to those of dextromethamphetamine. Levomethamphetamine does not possess the potential for euphoria or addiction that dextromethamphetamine possesses. Among its physiological effects are the vasoconstriction that makes it useful for nasal decongestion. The elimination half-life of levomethamphetamine is between 13.3 and 15 hours, whereas dextromethamphetamine has a half-life of about 10.5 hours. When the nasal decongestant is taken in excess, levomethamphetamine has potential side effects resembling those of other sympathomimetic drugs; these effects include hypertension (elevated blood pressure), tachycardia (rapid heart rate), nausea, stomach cramps, dizziness, headache, sweating, muscle tension, and tremors. Central side effects may include anxiety, insomnia, and anorexia
Status:
US Approved OTC
Source:
21 CFR 347.10(a) skin protectant allantoin
Source URL:
First approved in 1961
Source:
ALLANTOMIDE ALLANTOIN by NATIONAL DRUG
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



The aluminum salt of Allantoin, Alcloxa combines the astringent and anti-microbial properties of aluminum with the anti-irritant, soothing and healing properties of Allantoin. Alcloxa is particularly suited for use in anti-perspirants, acne treatments and foot care products. Alcloxa is a compound that combine the properties of aluminum salts with the properties of allantion. The allantion component ehhances the action of the aluminum salts and serves to overcome irritations experienced by many individuals who may be sensitive to the use of aluminum alts. The aluminum component reduces sweat by causing the sweat gland ducts swell. Alcloxa also add to the antiperspirant properties the deodorant effect because of its bacteriostatic action. It showed bacteriostatic properties at concentrations of 0.2% particularly against Gram bectaria (B. subtilis, S. aureus, P. vulgaris, Pityrosporum ovale). This is ascribable to two different mechanisms: first bacterial growth is retarded due to a decrease in the amount of water present, second aluminum salt have itself an antimicrobial action. In baby products is indicated for its healing reparative action, in the treatment of diaper rash. Also is approved in haemorrhoidal product for its soothing and keratolytic action. In oral care products Alcloxa is useful for its astringent antibacterial properties. It is very indicated in formulations for sensitive teeth, periodontal and gum diseases (like gingivitis, irritable and bleeding gums). Use levels: 0.1-1%. − In antiacne products the slightly astringent effect promotes healing of pustules and acne lesions. It reduces the extension of infected skin eruptions, healing them and developing a soothing action. May be used alone or also in combinations with other antimicrobial agents in order to fight acne more effectively. Use levels: 0.5-2.0%.
Status:
US Approved OTC
Source:
21 CFR 341.18 cough/cold:expectorant guaifenesin
Source URL:
First approved in 1961
Source:
BRONKODYL GLYCERYL GUAIACOLATE by PRL
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Guaifenesin is an expectorant the action of which promotes or facilitates the removal of secretions from the respiratory tract. The precise mechanism of action of guaifenesin is not known; however, it is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. In turn, this may increase the efficiency of the cough reflex and facilitate removal of the secretions. Guaifenesin is over-the-counter drug for the treatment of cough and common cold.
Status:
US Approved OTC
Source:
21 CFR 355.10(a)(2) anticaries:dentifrices sodium fluoride powder
Source URL:
First marketed in 1921
Source:
Calcium Chloride U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Olaflur (amine fluoride 297, trade name elmex gel) is a fluoride-containing substance that is an ingredient of toothpastes and solutions for the prevention of dental caries. Especially in combination with dectaflur, it is also used in the form of gels for the treatment of early stages of caries, sensitive teeth, and by dentists for the refluoridation of damaged tooth enamel. Olaflur is a salt consisting of an alkyl ammonium cation and fluoride as the counterion. With a long lipophilic hydrocarbon chain, the cation has surfactant properties. It forms a film layer on the surface of teeth, which facilitates incorporation of fluoride into the enamel. The top layers of the enamel's primary mineral, hydroxylapatite, are converted into the more robust fluorapatite. The fluoridation reaches only a depth of a few nanometres, which has raised doubts whether the mechanism really relies on the formation of fluorapatite.