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

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Showing 181 - 190 of 198 results

Sodium is the primary cation (positive ion) in extracellular fluids in animals and humans. Sodium ions are necessary for regulation of blood and body fluids, transmission of nerve impulses, heart activity, and certain metabolic functions. Physiologically, it exists as an ion in the body. Sodium is needed by animals, which maintain high concentrations in their blood and extracellular fluids, but the ion is not needed by plants. The human requirement for sodium in the diet is less than 500 mg per day, which is typically less than a tenth as much as many diets "seasoned to taste. " Most people consume far more sodium than is physiologically needed. For certain people with salt-sensitive blood pressure, this extra intake may cause a negative effect on health.
Status:
US Approved OTC
Source:
21 CFR 333.110(a) first aid antibiotic:ointment bacitracin
Source URL:
First marketed in 1921

Class (Stereo):
CHEMICAL (ACHIRAL)



Bacitracin is a polypeptide antibiotic produced by Bacillus subtilis and Bacillus licheniformis. Bacitracin in combination with neomycin and polymyxin B is indicated for the treatment of many bacterial diseases. The antibacterial properties of bacitracin are mediated by its binding to C55-isoprenyl pyrophosphate, resulting in inhibition of cell wall biosynthesis.
Status:
US Approved OTC
Source:
21 CFR 350.10(l) antiperspirant aluminum zirconium octachlorohydrex gly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Burow invented an astringent antiseptic solution of aluminium acetate in water to relieve the itching and inflammation of minor skin irritations. At present the oflicial U. S. P. procedure to made Burow's solution involves the reaction of aluminum sulfate, calcium carbonate and acetic acid to form aluminum sub-acetate, also termed basic aluminum acetate. The solution is available as an over-the-counter drug for topical administration, with brand names including Domeboro. Burow's solution has been shown to be effective against chronic suppurative otitis media and otitis externa. It is active against bacteria resulting in damage to the cell wall.
Status:
US Approved OTC
Source:
21 CFR 341.16(d) cough/cold:bronchodilator epinephrine
Source URL:
First marketed in 1901

Class (Stereo):
CHEMICAL (ABSOLUTE)



Epinephrine is a sympathomimetic catecholamine. It acts as a naturally occurring agonist at both alpha and beta-adrenergic receptors. Three pharmacologic types have been identified: alpha 1-, alpha 2-, and beta-adrenergic receptors. Each of these has three subtypes, characterized by both structural and functional differences. The alpha 2 and beta receptors are coupled negatively and positively, respectively, to adenylyl cyclase via Gi or Gs regulatory proteins, and the alpha 1 receptors modulate phospholipase C via the Go protein. Subtype expression is regulated at the level of the gene, the mRNA, and the protein through various transcriptional and postsynthetic mechanisms. Through its action on alpha-adrenergic receptors, epinephrine lessens the vasodilation and increased vascular permeability that occurs during anaphylaxis, which can lead to loss of intravascular fluid volume and hypotension. Through its action on beta-adrenergic receptors, epinephrine causes bronchial smooth muscle relaxation and helps alleviate bronchospasm, wheezing and dyspnea that may occur during anaphylaxis. Epinephrine also alleviates pruritus, urticaria, and angioedema and may relieve gastrointestinal and genitourinary symptoms associated with anaphylaxis because of its relaxer effects on the smooth muscle of the stomach, intestine, uterus and urinary bladder. Epinephrine increases glycogenolysis, reduces glucose up take by tissues, and inhibits insulin release in the pancreas, resulting in hyperglycemia and increased blood lactic acid.
Status:
US Approved OTC
Source:
21 CFR 331.11(c)(3) antacid:bismuth-containing bismuth subcarbonate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bibrocathol (trade names Noviform and Posiformin) is a well-established topical antiseptic for the treatment of acute eyelid diseases like blepharitis. Eye ointments containing 2 or 5 % bibrocathol and the excipients liquid paraffin, white soft paraffin, and lanolin have been marketed since 1967 for the treatment of eye irritation, chronic blepharitis, and uninfected corneal injuries. Reports of clinical experience with bibrocathol for inflammation of the edge of the palpebra exist since the beginning of the 20th century. Until recently, no controlled, randomized clinical studies according to the guidelines for Good Clinical Practice for Trials on Medical Products for Human Use (GCP) as defined by the International Conference on Harmonisation (ICH) have been performed with bibrocathol 2 % ointment, as these were not required for marketing authorization in the 1960s. A first double-blind, prospective, controlled, GCP-compliant clinical study was recently performed to assess the efficacy of bibrocathol 5 % (Noviform®) in acute blepharitis. It demonstrated superior efficacy of bibrocathol 5 % ointment as compared to an ointment vehicle (placebo) after 2 weeks of treatment as assessed by a combined measure of slit-lamp examination results and patients’ subjective complaints.
Status:
US Previously Marketed
First approved in 1989

Class (Stereo):
CHEMICAL (RACEMIC)



Metipranolol is a beta-adrenergic antagonist effective for both beta-1 and beta-2 receptors. It is used as an antiarrhythmic, antihypertensive, and antiglaucoma agent. Metipranolol blocks beta1 and beta2 (non-selective) adrenergic receptors. It does not have significant intrinsic sympathomimetic activity, and has only weak local anesthetic (membrane-stabilizing) and myocardial depressant activity. Orally administered beta-adrenergic blocking agents reduce cardiac output in both healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta-adrenergic receptor antagonists may inhibit the sympathetic stimulatory effect necessary to maintain adequate cardiac output. Metipranolol when applied topically in the eye, has the action of reducing elevated as well as normal intraocular pressure (IOP), whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss. The higher the level of intraocular pressure, the greater the likelihood of glaucomatous visual field loss and optic nerve damage. The primary mechanism of the ocular hypotensive action of Metipranolol is most likely due to reduction in aqueous humor production. A slight increase in outflow may be an additional mechanism. Metipranolol reduces IOP with little or no effect on pupil size or accommodation. Metipranolol is known as the brand OptiPranolol. Brand-name OptiPranolol is manufactured by Bausch & Lomb Incorporated. However, the patents for OptiPranolol have expired, and this medication is currently available in generic form. Generic OptiPranolol eye drops are available in one strength -- metipranolol 0.3 percent solution. It is made by Falcon Pharmaceuticals.
Status:
US Previously Marketed
Source:
GUANETHIDINE MONOSULFATE by WATSON LABS
(1985)
Source URL:
First approved in 1960
Source:
lsmelin Sulfate by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Guanethidine belongs to the general class of medicines called antihypertensives. It was used to treat high blood pressure (hypertension). It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles.
Status:
US Previously Marketed
First approved in 1960

Class (Stereo):
CHEMICAL (RACEMIC)



Oxyphenbutazone is a non-steroidal anti-inflammatory drug, cyclooxygenase (prostaglandin synthetase) inhibitors which was marked under brand name tandearil for the treatment rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis. But this drug was withdrawn from markets due to bone marrow suppression.
Status:
US Previously Marketed
Source:
KECTIL DIHYDROSTREPTOMYCIN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1948
Source:
Dihydrostreptomycin Sulfate by Merck
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dihydrostreptomycin is an antibiotic compound derived from streptomycin by reduction with hydrogen. The primary mechanism of action of the antibiotic dihydrostreptomycin is binding to and modifying the function of the bacterial ribosome, thus leading to decreased and aberrant translation of proteins, in addition it binds mechanosensitive channel of large conductance (MscL) and modifies its conformation, thus allowing the passage of K+ and glutamate out of, and dihydrostreptomycin into, the cell. It has about the same degree of antibacterial activity as streptomycin, but it is less effective against some gram-negative microorganisms. Because it has a higher risk of irreversible deafness, and its effectiveness is no greater that that of streptomycin, dihydrostreptomycin is no longer used clinically. To date dihydrostreptomycin is approved for veterinary use to treat bacterial infections.
Status:
US Previously Marketed
Source:
sodium propionate
(1921)
Source URL:
First marketed in 1921
Source:
sodium propionate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Propionic acid (PA), also known as propanoic acid, with chemical formula C3H6O2, is an organic acid used as a food additive and found naturally on the skin and in the gastrointestinal tract. It is a byproduct of fermentation reactions and is also produced industrially from ethylene or ethanol and carbon monoxide. Propionic acid is a fungicide and bactericide, registered to controlfungi and bacteria in stored grains, hay, grain storage areas, poultry litter,and drinking water for livestock and poultry. As a food preservative, propionic acid prevents mold in bread and baked goods, and it is used as a flavoring agent in cheese and other packaged goods. The U.S. Environmental Protection Agency considers it safe and therefore, has no limitation on its use. It has been demonstrated that PA lowers fatty acids content in liver and plasma, reduces food intake, exerts immunosuppressive actions and probably improves tissue insulin sensitivity. Thus increased production of PA by the microbiota might be considered beneficial in the context of prevention of obesity and diabetes type 2. The molecular mechanisms by which PA may exert this plethora of physiological effects are slowly being elucidated and include intestinal cyclooxygenase enzyme, the G-protein coupled receptors 41 and 43 and activation of the peroxisome proliferator-activated receptor γ, in turn inhibiting the sentinel transcription factor NF-κB and thus increasing the threshold for inflammatory responses in general. Taken together, PA emerges as a major mediator in the link between nutrition, gut microbiota and physiology. The sodium salt of propionic acid was previously approved in Canada as an active ingredient in Amino-Cerv (used to treat inflammation or injury of the cervix).

Showing 181 - 190 of 198 results