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

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Showing 4491 - 4500 of 4602 results

Bleomycin sulfate is an antineoplastic antibiotic isolated from Streptomyces verticillus. It is a mixture of glycopeptide antibiotics containing primarily Bleomycin A2 (~70%) and B2 (~30%). Bleomycin binds to DNA, inhibits DNA synthesis, and causes single strand scission of DNA in vivo and in vitro at specific base sequences.
Doxepin is a dibenzoxepin tricyclic antidepressant marketed worldwide. It is a white crystalline solid readily soluble in water, lower alcohols and chloroform. The mechanism of action of doxepin is not definitely known. It is not a central nervous system stimulant nor a monoamine oxidase inhibitor. The current hypothesis is that the clinical effects are due, at least in part, to influences on the adrenergic activity at the synapses so that deactivation of norepinephrine by reuptake into the nerve terminals is prevented. Antidepressants may increase risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (18–24 years of age) with major depressive disorder and other psychiatric disorders. Drowsiness is the most commonly noticed side effect. This tends to disappear as therapy is continued. Other infrequently reported CNS side effects are confusion, disorientation, hallucinations, numbness, paresthesias, ataxia, extrapyramidal symptoms, seizures, tardive dyskinesia, and tremor. : Cardiovascular effects including hypotension, hypertension, and tachycardia have been reported occasionally. Skin rash, edema, photosensitization, and pruritus have occasionally occurred. Eosinophilia has been reported in a few patients. There have been occasional reports of bone marrow depression manifesting as agranulocytosis, leukopenia, thrombocytopenia, and purpura. Doxepin is used to treat depression, anxiety disorders, itchiness, trouble sleeping, and as a second-line treatment of chronic idiopathic urticaria (hives). Its oral formulations are FDA-approved for the treatment of depression, anxiety, and insomnia and its topical formulations are FDA-approved the short-term management (up to 8 days) of atopic dermatitis and lichen simplex chronicus. Whereas in Australia and the UK, the only licensed indication(s) is/are in the treatment of major depression and pruritus in eczema, respectively.
Clomiphene (CLOMID®) is a triphenyl ethylene stilbene derivative which is an estrogen agonist or antagonist depending on the target tissue. It is an orally administered, nonsteroidal, ovulatory stimulant. Clomiphene (CLOMID®) is a mixture of two geometric isomers [cis (zuclomiphene) and trans (enclomiphene)] containing between 30% and 50% of the cis-isomer. Clomiphene (CLOMID®) initiates a series of endocrine events culminating in a preovulatory gonadotropin surge and subsequent follicular rupture. The first endocrine event in response to a course of clomiphene therapy is an increase in the release of pituitary gonadotropins. This initiates steroidogenesis and folliculogenesis, resulting in growth of the ovarian follicle and an increase in the circulating level of estradiol. Following ovulation, plasma progesterone and estradiol rise and fall as they would in a normal ovulatory cycle.
Gentamicin is an antibiotic of the aminoglycoside group, is derived by the growth of Micromonospora purpurea, an actinomycete. Gentamicin is a complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1a. Gentamicin is a broad-spectrum antibiotic, but may cause ear and kidney damage. Gentamicin binds to the prokaryotic ribosome, inhibiting protein synthesis in susceptible bacteria. It is bactericidal in vitro against Gram-positive and Gram-negative bacteria. Adverse reactions include adverse renal effects, neurotoxicity (dizziness, vertigo, tinnitus, roaring in the ears, hearing loss, peripheral neuropathy or encephalopathy), respiratory depression, lethargy, confusion, depression, visual disturbances, etc.
Colistin sulfate is a polypeptide antibiotic which penetrates into and disrupts the bacterial cell membrane. It is a cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C). Colistin was first isolated in Japan in 1949 from a flask of fermenting Bacillus polymyxa var. colistinus and became available for clinical use in 1959. The following local adverse events have been reported with topical corticosteroids, especially under occlusive dressings: burning, itching, irritation, dryness, folliculitis, hypertrichosis, etc. Healthcare providers had largely stopped using colistin in the 1970s because of its toxicity. However, with antibacterial resistance on the rise, colistin is increasingly being used today to treat severe, multidrug-resistant Gram-negative bacterial infections, particularly among intensive care-based patients. The problem with re-introducing an older drug, such as colistin, though, is that techniques for evaluating new drugs have evolved since the 1950s, and therefore, little is known about the dose needed to effectively fight infection while limiting the potential emergence of antimicrobial resistance and reducing potentially toxic side effects. More data are needed to guide optimal use of these older medications. An international team of NIAID-funded researchers is making progress in obtaining better dosing information about colistin and how best to use the antibiotic to treat Gram-negative bacterial infections. Resistance to colistin is rare. The first colistin-resistance gene that is carried in a plasmid and can be transferred between bacterial strains was described in 2016. This plasmid-borne mcr-1 gene has since been isolated in China, Europeand the United States.
mixture
Status:
First approved in 1961
Source:
Coly-Mycin Injectable by Warner/Chilcott
Source URL:

Class:
MIXTURE



Colistimethate is a methanesulfonate of polymyxin antibacterial colistin. Colistimethate is a nonactive prodrug. In aqueous solutions, colistimethate is hydrolyzed and forms a complex mixture of partially sulfomethylated derivatives and colistin. The antimicrobial activity of colistin is similar to that of polymyxin B and is restricted to gram-negative bacteria, including P aeruginosa, Acinetobacter species, Enterobacter-Klebsiella tribe, Escherichia coli, Salmonella and Shigella species, Citrobacter species, Yersinia pseudotuberculosis, Morganella morganii and Haemophilus influenzae. Colistin has also been shown to possess considerable in vitro activity against Stenotrophomonas maltophilia. Colistin and polymyxin B, however, do not have activity against Proteus, Providencia, Serratia species, Pseudomonas mallei, Burkholderia cepacia, Brucella species, most gram-positive bacteria, gram-negative cocci, anaerobes, fungi and parasites. Parenteral or nebulized colistimethate is indicated for the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli. It is particularly indicated when the infection is caused by sensitive strains of Pseudomonas aeruginosa.
Dexamethasone is an anti-inflammatory agent that is FDA approved for the treatment of many conditions, including rheumatic problems, a number of skin diseases, severe allergies, asthma, chronic obstructive lung disease, croup, brain swelling and others. Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic glucocorticoid receptors. Adverse reactions are: Glaucoma with optic nerve damage, visual acuity and field defects; cataract formation; secondary ocular infection following suppression of host response; and perforation of the globe may occur; muscle weakness; osteoporosis and others. Aminoglutethimide may diminish adrenal suppression by corticosteroids. Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.
mixture
Status:
First approved in 1949

Class:
MIXTURE


Crotamiton is a scabicidal and antipruritic agent available as a cream or lotion for topical use. The drug was approved by FDA for the treatment of scabies and pruritic skin. Crotamiton is a mixture of the cis and trans isomers of N-ethyl-N-(o-methylphenyl)-2butenamide. Although the activity of crotamiton was shown both in vitro and in vivo, the mechanism of its action is still unknown.
mixture
Status:
First marketed in 1921
Source:
Sodium Glycerophosphate U.S.P.
Source URL:

Class:
MIXTURE



Synthetic glycerophosphates have been known for many years and have been prepared in several ways. The acid may exist in two isomeric forms, alpha and beta. The L-a-acid is the naturally occurring form; the b-acid, present in hydrolyzates of lecithins from natural sources, arises from migration of the phosphoryl group from the a-carbon atom. Dehydrogenation of L-glycerol 3-phosphate produces Dihydroxyacetone phosphate and is part of the entry of glycerol (sourced from triglycerides) into the glycolytic pathway.
mixture
Status:
First marketed in 1921

Class:
MIXTURE



Glucose is a sugar with the molecular formula C6H12O6. The D-isomer (D-glucose), also known as dextrose, occurs widely in nature, but the L-isomer (L-glucose) does not. Glucose is made during photosynthesis from water and carbon dioxide, using energy from sunlight. The reverse of the photosynthesis reaction, which releases this energy, is a very important source of power for cellular respiration. Glucose is stored as a polymer, in plants as starch and in animals as glycogen, for times when the organism will need it. Glucose circulates in the blood of animals as blood sugar. Glucose can be obtained by hydrolysis of carbohydrates such as milk, cane sugar, maltose, cellulose, glycogen etc. It is however, manufactured by hydrolysis of cornstarch by steaming and diluting acid. Glucose is the human body's key source of energy, through aerobic respiration, providing about 3.75 kilocalories (16 kilojoules) of food energy per gram. Breakdown of carbohydrates (e.g. starch) yields mono- and disaccharides, most of which is glucose. Use of glucose as an energy source in cells is by either aerobic respiration, anaerobic respiration, or fermentation. All of these processes follow from an earlier metabolic pathway known as glycolysis. The insulin reaction, and other mechanisms, regulate the concentration of glucose in the blood. Glucose supplies almost all the energy for the brain, so its availability influences psychological processes. When glucose is low, psychological processes requiring mental effort (e.g., self-control, effortful decision-making) are impaired. Ingested glucose is absorbed directly into the blood from the intestine and results in a rapid increase in the blood glucose level. Glucose is used to manage hypoglycemia and for intravenous feeding. Nausea may occur after ingesting glucose, but this also may be an effect of the hypoglycemia which is present just prior to ingestion. Other adverse effects include increased blood glucose, injection site leakage of fluid (extravasation), injection site inflammation, and bleeding in the brain.

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