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

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Showing 13751 - 13760 of 14117 results

Ribostamycin sulfate is an aminoglycoside-aminocyclitol antibiotic isolated from a streptomycete. It is an important broad-spectrum antibiotic with important use against human immunodeficiency virus and is considered a critically important antimicrobial by the World Health Organization. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit (some work by binding to the 50S subunit), inhibiting the translocation of the peptidyl-tRNA from the A-site to the P-site and also causing misreading of mRNA, leaving the bacterium unable to synthesize proteins vital to its growth. Ribostamycin is usually used to treat sepsis, superficial skin infection, deep skin infection, lymphangitis/lymphadenitis, chronic pyoderma, osteomyelitis, pharyngitis/laryngitis, tonsillitis, acute bronchitis, pneumonia, pulmonary abscess, pyothorax, secondary infection in chronic respiratory lesions, cystitis, pyelonephritis, gonococcal infection, peritonitis, cholecystitis, dacryocystitis, keratitis (including corneal ulcer), otitis media, sinusitis and gnathitis. The most commonly reported adverse reactions include renal dysfunction, liver disorder and rash.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefozopran Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefozopran hydrochloride is a third-generation cephalosporin that was launched for the treatment of severe infections in immunocompromised patients caused by staphylococci and enterococci. While it shows a very broad antibacterial spectrum against Gram-positive and Gram-negative organisms, it is particularly potent against S. aureus, Enterococcus faecalis, P. aeruginosa, and Citrobacter freundii. It is resistant to hydrolysis by most chromosomal and plasmid mediated β-lactamases and is reported to be active against respiratory, urinary tract, obstetrical, gynecological, soft tissue, and surgical infections. Similar to β-lactams, cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases.
Status:
Possibly Marketed Outside US
Source:
Isepamicin by Schering-Plough
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Isepamicin is an aminoglycoside antibacterial with properties similar to those of amikacin, but with better activity against strains producing type I 6'-acetyltransferase. The antibacterial spectrum includes Enterobacteriaceae and staphylococci. Anaerobes, Neisseriaceae and streptococci are resistant. The lower and upper break-points are 8 and 16 mg/L. Like other aminoglycosides, isepamicin exhibits a strong concentration-dependent bactericidal effect, a long post-antibiotic effect (several hours) and induces adaptive resistance. Isepamicin is administered intravenously or intramuscularly at a dosage of 15 mg/kg once daily or 7.5 mg/kg twice daily. Isepamicin is not bound to plasma proteins, and it distributes in extracellular fluids and into some cells (outer hair cells, kidney cortex) by active transport. Isepamicin has been developed and approved for clinical use in the 1990s.
Status:
Possibly Marketed Outside US
Source:
Unknown by Sandoz
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Brovincamine also known as brovincamine fumarate (BV, Sabromin) was used in Japan mainly as an improver of cerebral circulation and metabolism, and also as an inhibitor of the aggregation of platelets through the cyclic AMP pathway in patients with normal tension glaucoma. Brovincamine exerts its action via calcium channels blockade. The current drug status is unknown.
Etafenone is an antiarrhythmic and coronary vasodilator drug. Etafenone exerts negative inotropic action on myocardium. It is able to block calcium channels. As a coronary vasodilator which produces a decrease in the heart rate and myocardial oxygen consumption, etafenone has been used in the therapy of ischemic heart disease.
Cefatrizine is a broad-spectrum, semisynthetic, first-generation cephalosporin with antibacterial activity. Cefatrizine binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. Cefatrizine is used to treat a large variety of bacterial infections, such as respiratory tract, ear, skin and urinary tract infections. Cefatrizine is less effective against gram positive bacteria than first generation drugs. Antibiotics require constant drug level in body for therapeutic effect.
Status:
Possibly Marketed Outside US
Source:
NCT01876628: Phase 4 Interventional Completed Cellulitis
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flucloxacillin is an isoxazolyl penicillin of the β-lactam group of antibiotics, which exerts a bactericidal effect upon many Gram-positive organisms including β-lactamase-producing staphylococci and streptococci. While no longer used in the United States, Flucloxacillin is supplied under a variety of trade names in other countries, including Floxapen, Flopen, Staphylex. Floxapen is indicated for the treatment of infections due to sensitive Gram-positive organisms, including β-lactamase-producing staphylococci and streptococci. Typical indications including, skin and soft tissue infections; respiratory tract infections; other infections caused by floxapen-sensitive organisms, like example, osteomyelitis, urinary tract infection, septicaemia, endocarditis. Floxapen is also indicated for use as a prophylactic agent during major surgical procedures when appropriate; for example cardiothoracic and orthopaedic surgery. Flucloxacillin, by its action on the synthesis of the bacterial wall, exerts a bactericidal effect on streptococci except those of group D (Enterococcus faecalis) staphylococci. It is not active against methicillin-resistant staphylococci. There is evidence that the risk of flucloxacillin induced liver injury is increased in subjects carrying the HLA-B*5701 allele. Despite this strong association, only 1 in 500-1000 carriers will develop liver injury. Consequently, the positive predictive value of testing the HLA-B*5701 allele for liver injury is very low (0.12%) and routine screening for this allele is not recommended. Flucloxacillin diffuses well into most tissue. Specifically, active concentrations of flucloxacillin have been recovered in bones: 11.6 mg/L (compact bone) and 15.6 mg/L (spongy bone), with a mean serum level of 8.9 mg/L. Flucloxacillin diffuses in only small proportion into the cerebrospinal fluid of subjects whose meninges are not inflamed. It is also excreted in small quantities in mother's milk. In normal subjects approximately 10% of the flucloxacillin administered is metabolised to penicilloic acid. The elimination half-life of flucloxacillin is in the order of 53 minutes.
Bucindolol is a third-generation, non-selective β-adrenergic receptor blocker, that acts on both β-1 and β-2 receptors. Bucindolol’s additional α-1 antagonistic activity contributes to its mild vasodilator effect. It was rejected by the FDA for the heart failure, because of the unreviewed submissions deal with comparative effectiveness, clinical pharmacology, some aspects of pharmacogenetic data, and toxicology/metabolism. In addition, bucindolol is in the phase II of clinical trial for the treatment of atrial fibrillation.
Xamoterol (ICI 118,587) is a partial agonist of beta1-adrenoceptors. Xamoterol acts on the cardiac beta 1-adrenergic receptor, modifies the response of the heart to variations in sympathetic activity. At rest, it produces modest improvements in cardiac contractility, relaxation, and filling without increase in myocardial oxygen demand. The improvements are maintained during exercise although the attendant tachycardia is attenuated. The beneficial effects of xamoterol on both systolic and diastolic function suggested that it would be effective in patients with mild-to-moderate heart failure, and this was demonstrated in small placebo-controlled studies where effort tolerance and symptoms were improved. Xamoterol produced improvements in exercise capacity, clinical signs, symptoms and quality of life with a low incidence of adverse experiences. Xamoterol is effective as monotherapy in heart failure.
Maduramicin is antibiotic isolated from actinobacteria Actinomadura rubra. Maduramicin is used in veterinary as an aid in the prevention of coccidiosis in broiler chickens and turkeys. The compound is reported to be toxic to animals and humans if improperly used or by accident, resulting in heart failure, skeletal muscle degeneration, and even death. Studies have shown that toxicity is due to activation of protein phosphatase 2A, and the manipulation of the ROS-PTEN-Akt-Erk1/2 pathway may be a potential approach to prevent maduramicin -induced cardiotoxicity.

Showing 13751 - 13760 of 14117 results