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

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Showing 221 - 230 of 4351 results

Phenylephrine is a powerful vasoconstrictor. It is used as a nasal decongestant and cardiotonic agent. Phenylephrine is a postsynaptic α1-receptor agonist with little effect on β-receptors of the heart. Parenteral administration of phenylephrine causes a rise in systolic and diastolic pressures, a slight decrease in cardiac output, and a considerable increase in peripheral resistance; most vascular beds are constricted, and renal, splanchnic, cutaneous, and limb blood flows are reduced while coronary blood flow is increased. Phenelephrine also causes pulmonary vessel constriction and subsequent increase in pulmonary arterial pressure. Vasoconstriction in the mucosa of the respiratory tract leads to decreased edema and increased drainage of sinus cavities. In general, α1-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. α1-receptors are 7-transmembrane domain receptors coupled to G proteins, Gq/11. Three α1-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: α1A (chromosome 8), α1B (chromosome 5), and α1D (chromosome 20). Phenylephrine appears to act similarly on all three receptor subtypes. All three receptor subtypes appear to be involved in maintaining vascular tone. The α1A-receptor maintains basal vascular tone while the α1B-receptor mediates the vasocontrictory effects of exogenous α1-agonists. Activation of the α1-receptor activates Gq-proteins, which results in intracellular stimulation of phospholipases C, A2, and D. This results in mobilization of Ca2+ from intracellular stores, activation of mitogen-activated kinase and PI3 kinase pathways and subsequent vasoconstriction. Phenylephrine produces its local and systemic actions by acting on α1-adrenergic receptors peripheral vascular smooth muscle. Stimulation of the α1-adrenergic receptors results in contraction arteriolar smooth muscle in the periphery. Phenylephrine decreases nasal congestion by acting on α1-adrenergic receptors in the arterioles of the nasal mucosa to produce constriction; this leads to decreased edema and increased drainage of the sinus cavities. Phenylephrine is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs.
Status:
US Approved OTC
Source:
21 CFR 344.1 otic:earwax removal aid carbamide peroxide 6.5% (in anhydrous glycerin)
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First marketed in 1921
Source:
Hydrogen Peroxide
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Class (Stereo):
CHEMICAL (ACHIRAL)



Hydrogen peroxide has been used in medicine for more than 100 years. It is known in surgery as a highly useful irrigation solution by virtue of both its hemostatic and its antimicrobial effects. Hydrogen peroxide is a mild antiseptic used on the skin to prevent infection of minor cuts, scrapes, and burns. It may also be used as a mouth rinse to help remove mucus or to relieve minor mouth irritation (e.g., due to canker/cold sores, gingivitis). This product works by releasing oxygen when it is applied to the affected area. The release of oxygen causes foaming, which helps to remove dead skin and clean the area. Hydrogen peroxide is a strong oxidizing agent used in aqueous solution as a ripening agent, bleach, and topical anti-infective. It is relatively unstable and solutions deteriorate over time unless stabilized by the addition of acetanilide or similar organic materials.
Status:
US Approved OTC
Source:
21 CFR 350.10(b) antiperspirant aluminum chlorohydrate
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First marketed in 1921
Source:
Aluminum Hydroxide U.S.P.
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Class (Stereo):
CHEMICAL (ACHIRAL)



Algeldrate (Aluminium hydroxide) is the amphoteric inorganic compound used as an antacid in the treatment of Duodenal, Peptic and Stomach Ulcer and some other conditions. Aluminium hydroxide is preferred over other alternatives such as sodium bicarbonate because Al(OH)3, being insoluble, does not increase the pH of stomach above 7 and hence, does not trigger secretion of excess acid by the stomach. Brand names include Alu-Cap, Aludrox, Gaviscon or Pepsamar. It reacts with the excess acid in the stomach, reducing the acidity of the stomach content, which may relieve the symptoms of ulcers, heartburn or dyspepsia. Such products can cause constipation, because the aluminum ions inhibit the contractions of smooth muscle cells in the gastrointestinal tract, slowing peristalsis and lengthening the time needed for stool to pass through the colon. Some such products (such as Maalox) are formulated to minimize such effects through the inclusion of equal concentrations of magnesium hydroxide or magnesium carbonate, which have counterbalancing laxative effects. This compound is also used to control phosphate (phosphorus) levels in the blood of people suffering from kidney failure. Precipitated aluminum hydroxide is included as an adjuvant in some vaccines (e.g. anthrax vaccine). One of the well-known brands of aluminum hydroxide adjuvant is Alhydrogel, made by Brenntag Biosector. Since it absorbs protein well, it also functions to stabilize vaccines by preventing the proteins in the vaccine from precipitating or sticking to the walls of the container during storage. Aluminium hydroxide is sometimes mistakenly called "alum", which properly refers to aluminum potassium sulfate. Vaccine formulations containing aluminum hydroxide stimulate the immune system by inducing the release of uric acid, an immunological danger signal. This strongly attracts certain types of monocytes which differentiate into dendritic cells. The dendritic cells pick up the antigen, carry it to lymph nodes, and stimulate T cells and B cells. It appears to contribute to induction of a good Th2 response, so is useful for immunizing against pathogens that are blocked by antibodies. In the 1960s and 1970s, it was speculated that aluminum was related to various neurological disorders including Alzheimer's disease. Since then, multiple epidemiological studies have found no connection between exposure to aluminum and neurological disorders.
Status:
US Approved OTC
Source:
21 CFR 347.10(h) skin protectant glycerin
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First marketed in 1921
Source:
Glycerin U.S.P.
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Class (Stereo):
CHEMICAL (ACHIRAL)


Glycerin (glycerol) is 3-carbon alcohol naturally occurring in the human body. It is the structural backbone triacylglycerol molecules, and can also be converted to a glycolytic substrate for subsequent metabolism. Glycerin is a colorless, odorless, viscous, sweet-tasting liquid. The FDA classifies glycerol as "generally recognized as safe". Glycerin is used in the pharmaceutical industry as a sweetener in syrups, lozenges, and as an excipient in eyewash solutions. As an individual prescription product, glycerin has uses as a hyperosmotic, osmotic diuretic, and ophthalmic agent. It may be used as an eye drop in the treatment of glaucoma to reduce intraocular pressure, as a solution or suppository for short-term treatment of constipation, to evacuate the bowel prior to a colonoscopy, and in some ocular surgeries. It may be given intravenously to reduce pressure inside the brain and used externally on the skin as a moisturizer. Glycerin has many other uses in the agricultural, food and pharmaceutical industry.
Menthol, (+)- is a fragrance ingredient used in decorative cosmetics, fine fragrances, shampoos, toilet soaps and other toiletries as well as in non-cosmetic products such as household cleaners and detergents. Recent investigations have provided evidence for menthol to increase cough thresholds. Racementhol is used as a topical analgesic.
Resorcinol is a benzenediol. Resorcinol is commonly used in hair dyes and acne medication. Resorcinol works by breaking down rough, scaly, or hardened skin. Resorcinol also disinfects the skin to help fight infection. Resorcinol topical (for the skin) is used to treat pain and itching caused by minor cuts and scrapes, burns, insect bites, poison ivy, sunburn, or other skin irritations. Resorcinol topical is also used to treat acne, eczema, psoriasis, seborrhea, corns, calluses, warts, and other skin disorders. Resorcinol is included in the FDA final rule list of all permitted active ingredients for OTC topical acne products. Permitted combination active ingredient product - Resorcinol in 2 percent concentration in combination with sulfur in concentrations of between 3 and 8 percent. In oxidative hair dyes, resorcinol is regulated to 5% or below in practice, however, many manufacturers limit the level of free resorcinol in oxidative hair dyes to 1.25%. Resorcinol is limited to 0.5% in shampoos and hair lotions. Resorcinol is usually present in anti-acne preparations at a maximum concentration of 2%. The concentration of resorcinol can be much higher in peels, in some cases around 50%. Jessner’s solution (resorcinol in ethyl alcohol, 14% w/v; lactic acid, 14%; and salicylic acid, 14%) is commonly used in chemical peeling. A specialized medical use of resorcinol is in biological glues (gelatin–resorcinol–formaldehyde glue) for cardiovascular surgery, in particular aortic operations.
Status:
US Approved OTC
Source:
21 CFR 358.110(b) wart remover:collodoin-like vehicle salicylic acid
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First marketed in 1860
Source:
sodium salicylate
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Class (Stereo):
CHEMICAL (ACHIRAL)



Methyl salicylate (or methyl 2-hydroxybenzoate), also known as wintergreen oil, is a natural product and is present in white wine, tea, porcini mushroom Boletus edulis, Bourbon vanilla, clary sage, red sage and fruits including cherry, apple, raspberry, papaya and plum. Methyl salicylate is topically used in combination with methanol and under brand name SALONPAS to temporarily relieves mild to moderate aches and pains of muscles and joints associated with: strains, sprains, simple backache, arthritis, bruises. The precise mechanism of action of methyl salicylate is not known, but there is suggested, that it cause dilation of the capillaries thereby increasing blood flow to the area.
Status:
Investigational
Source:
INN:carafiban
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Class (Stereo):
CHEMICAL (ABSOLUTE)

Carafiban is orally active heterocyclic peptide mimetics fibrinogen IIb/IIIa receptor antagonist with antithrombotic activity. Carafiban is a prodrug, that underwent metabolic transformation to active metabolite des-ethyl- Carafiban, that inhibited dose-dependently and reversibly human platelet aggregation. In conscious dogs, Carafiban showed a high plasma availability of the active moiety of 42±8% and a plasma half-life of 9.9 h after oral administration as measured by bioassay. Carafiban may potentially be used for chronic treatment and prophylaxis of thrombotic diseases in humans.
Status:
Investigational
Source:
INN:zapnometinib [INN]
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Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:etanidazole
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Class (Stereo):
CHEMICAL (ACHIRAL)



Etanidazole (also known as Radinyl) is a 2-nitroimidazole with radiosensitizing properties. Etanidazole exerts its therapeutic action by depleting glutathione and inhibiting glutathione S-transferase, thus enhancing the anticancer effects of radiation therapy. Etanidazole was tested in Phase III clinical trials in patients with advanced head and neck cancer, however, its development was stopped. A fluorinated etanidazole (EF5) may also be useful as an imaging agent for identification of hypoxic, drug-resistant regions of primary tumors and metastases.