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

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Showing 33661 - 33670 of 34777 results

Grepafloxacin is a monofluorinated quinolone with a cyclopropyl group at position 1, a 3-methyl-1piperazinyl group at position 7 and a methyl substitution at the 5 position, that was synthesized by Otsuka in Japan. It exhibited in vitro activity against a wide variety of both Gram-positive and Gram-negative bacteria including anaerobic species. The compound was reported to have a broad spectrum of activity, particularly against pathogens responsible for community-acquired respiratory infections including those caused by beta-lactam and macrolide-resistant strains of Streptococcus pneumoniae and Haemophilus influenzae. Japanese researchers also reported that unlike other quinolones, grepafloxacin reached high levels in the bile and might also be useful in the treatment of biliary tract infection. Grepafloxacin was administered once daily and did not require dosage adjustment for renal insufficiency, but grepafloxacin tablets were contraindicated in patients with hepatic failure. Otsuka Pharmaceutical signed a licensing agreement for grepafloxacin with GlaxoSmithKline. According to this agreement, GlaxoSmithKline had marketing rights to grepafloxacin in Europe, USA, and certain other markets. Otsuka retained rights for Japan and some Asian countries
Grepafloxacin is a monofluorinated quinolone with a cyclopropyl group at position 1, a 3-methyl-1piperazinyl group at position 7 and a methyl substitution at the 5 position, that was synthesized by Otsuka in Japan. It exhibited in vitro activity against a wide variety of both Gram-positive and Gram-negative bacteria including anaerobic species. The compound was reported to have a broad spectrum of activity, particularly against pathogens responsible for community-acquired respiratory infections including those caused by beta-lactam and macrolide-resistant strains of Streptococcus pneumoniae and Haemophilus influenzae. Japanese researchers also reported that unlike other quinolones, grepafloxacin reached high levels in the bile and might also be useful in the treatment of biliary tract infection. Grepafloxacin was administered once daily and did not require dosage adjustment for renal insufficiency, but grepafloxacin tablets were contraindicated in patients with hepatic failure. Otsuka Pharmaceutical signed a licensing agreement for grepafloxacin with GlaxoSmithKline. According to this agreement, GlaxoSmithKline had marketing rights to grepafloxacin in Europe, USA, and certain other markets. Otsuka retained rights for Japan and some Asian countries
Status:
US Previously Marketed
First approved in 1997

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Fenoldopam (marketed under the brand name Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist. Fenoldopam is a rapid-acting vasodilator. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to α2-adrenoceptors. It has no significant affinity for D2-like receptors, α1 and β adrenoceptors, 5HT1 and 5HT2 receptors, or muscarinic receptors. Fenoldopam is a racemic mixture with the R-isomer responsible for the biological activity. The R-isomer has approximately 250-fold higher affinity for D1-like receptors than does the S-isomer. Fenoldopam Mesylate Injection, USP is indicated for the in-hospital, short-term (up to 48 hours) management of severe hypertension when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including malignant hypertension with deteriorating end-organ function.
Grepafloxacin is a monofluorinated quinolone with a cyclopropyl group at position 1, a 3-methyl-1piperazinyl group at position 7 and a methyl substitution at the 5 position, that was synthesized by Otsuka in Japan. It exhibited in vitro activity against a wide variety of both Gram-positive and Gram-negative bacteria including anaerobic species. The compound was reported to have a broad spectrum of activity, particularly against pathogens responsible for community-acquired respiratory infections including those caused by beta-lactam and macrolide-resistant strains of Streptococcus pneumoniae and Haemophilus influenzae. Japanese researchers also reported that unlike other quinolones, grepafloxacin reached high levels in the bile and might also be useful in the treatment of biliary tract infection. Grepafloxacin was administered once daily and did not require dosage adjustment for renal insufficiency, but grepafloxacin tablets were contraindicated in patients with hepatic failure. Otsuka Pharmaceutical signed a licensing agreement for grepafloxacin with GlaxoSmithKline. According to this agreement, GlaxoSmithKline had marketing rights to grepafloxacin in Europe, USA, and certain other markets. Otsuka retained rights for Japan and some Asian countries
Status:
US Previously Marketed
First approved in 1997

Class (Stereo):
CHEMICAL (ACHIRAL)



Emedastine is an antihistaminic agent, which was approved by FDA for the treatment of allergic conjunctivitis (Emadine brand name). The drug acts selectively on H1 receptors with lower affinity to H2 and H3 subtypes. Emedastine has a relatively unfavorable CNS effect profile. A small percentage of patients reported somnolence as an adverse effect after administration.
Status:
US Previously Marketed
First approved in 1997

Class (Stereo):
CHEMICAL (ACHIRAL)


Mangafodipir (sold under the brand name Teslascan as mangafodipir trisodium) is a contrast agent delivered intravenously to enhance contrast in magnetic resonance imaging (MRI) of the liver. Mangafodipir is a manganese (Mn2+) chelate with the ligand fodipir (dipyridoxyl diphosphate or DPDP). Mangafodipir trisodium is metabolised (dephosphorylated) and partially transmetallated (manganese exchanged for zinc) after intravenous administration. Manganese that is released from mangafodipir is taken up by hepatocytes thereby increasing the SI of normal liver tissue. This may result in an improvement of the detection of liver metastases, which usually have no hepatocytes. The metabolites of fodipir are renally excreted, whilst the biliary route mainly excretes manganese. Mangafodipir was withdrawn from the US market in 2003 and the European market in 2012.
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. It acts on the renin-angiotensin system in two ways to decrease total peripheral resistance. First, it blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle, causing vascular dilatation. Second, it inhibits sympathetic norepinephrine production, further reducing blood pressure. Eprosartan is indicated for the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors).
Status:
US Previously Marketed
First approved in 1997

Class (Stereo):
CHEMICAL (ACHIRAL)



Emedastine is an antihistaminic agent, which was approved by FDA for the treatment of allergic conjunctivitis (Emadine brand name). The drug acts selectively on H1 receptors with lower affinity to H2 and H3 subtypes. Emedastine has a relatively unfavorable CNS effect profile. A small percentage of patients reported somnolence as an adverse effect after administration.
Status:
US Previously Marketed
First approved in 1997

Class (Stereo):
CHEMICAL (ABSOLUTE)



Arbutamine was indicated to elicit acute cardiovascular responses in order to aid in diagnosing the presence or absence of coronary artery disease in patients who cannot exercise adequately. Arbutamine is a synthetic catecholamine with positive chronotropic and inotropic properties. The chronotropic (increase in heart rate [HR]) and inotropic (increase in force of contraction) effects of arbutamine serve to mimic exercise by increasing cardiac work (producing stress) and provoke myocardial ischemia in patients with compromised coronary arteries. In functional assays, arbutamine is more selective for beta-adrenergic receptors than for alpha-adrenergic receptors. The beta-agonist activity of arbutamine provides cardiac stress by increasing HR, cardiac contractility, and systolic blood pressure.
Saquinavir (brand names Invirase and Fortovase) is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS. Saquinavir is an inhibitor of HIV protease. HIV protease is an enzyme required for the proteolytic cleavage of viral polyprotein precursors into individual functional proteins found in infectious HIV. Saquinavir is a peptide-like substrate analog that binds to the protease active site and inhibits the activity of the enzyme. Saquinavir inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious virus particles. The most frequent adverse events with saquinavir in either formulation are mild gastrointestinal symptoms, including diarrhea, nausea, loose stools & abdominal discomfort. Invirase is better tolerated than Fortovase.

Showing 33661 - 33670 of 34777 results