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Status:
US Previously Marketed
Source:
FACTIVE by LG CHEM LTD
(2003)
Source URL:
First approved in 2003
Source:
FACTIVE by LG CHEM LTD
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin mesylate is marketed under the brand name Factive, indicated for the treatment of bacterial infection caused by susceptible strains such as S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis, S. pneumoniae (including multi-drug resistant strains [MDRSP]), M. pneumoniae, C. pneumoniae, or K. pneumoniae. Gemifloxacin has in vitro activity against a wide range of Gram-negative and Grampositive
microorganisms. Gemifloxacin is bactericidal with minimum bactericidal concentrations (MBCs) generally within one dilution of the minimum inhibitory
concentrations (MICs). Gemifloxacin acts by inhibiting DNA synthesis through the
inhibition of both DNA gyrase and topoisomerase IV (TOPO IV), which are essential for
bacterial growth. Streptococcus pneumoniae showing mutations in both DNA gyrase and
TOPO IV (double mutants) are resistant to most fluoroquinolones. Gemifloxacin has the
ability to inhibit both enzyme systems at therapeutically relevant drug levels in S.
pneumoniae (dual targeting), and has MIC values that are still in the susceptible range for
some of these double mutants.
Status:
US Previously Marketed
Source:
ZELNORM by ALFASIGMA
(2002)
Source URL:
First approved in 2002
Source:
ZELNORM by ALFASIGMA
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tegaserod (3‐(5‐methoxy‐1H‐indol‐3ylmethylene)‐N‐pentyl‐carbazimidamide), an aminoguanidine indole derivative of serotonin, is a selective partial agonist highly selective for 5‐HT4 receptor with an affinity constant in the nanomolar range. Tegaserod, by acting as an agonist at neuronal 5-HT4 receptors, triggers the release of further neurotransmitters such as calcitonin gene-related peptide from sensory neurons. The activation of 5-HT4 receptors in the gastrointestinal tract stimulates the peristaltic reflex and intestinal secretion, as well as inhibits visceral sensitivity. In vivo studies showed that tegaserod enhanced basal motor activity and normalized impaired motility throughout the gastrointestinal tract. Zelnorm® (tegaserod maleate) is indicated for the short-term treatment of women with irritable bowel
syndrome (IBS) whose primary bowel symptom is constipation. In addition Zelnorm® is indicated for the treatment of patients less than 65 years of age with
chronic idiopathic constipation.
Status:
US Previously Marketed
Source:
CHIROCAINE by PURDUE PHARMA LP
(1999)
Source URL:
First approved in 1999
Source:
CHIROCAINE by PURDUE PHARMA LP
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Levobupivacaine (CHIROCAINE®) is a (S)-enantiomer of bupivacaine and it is related chemically and pharmacologically to the amino amide class of local anesthetics. Local anesthetics block the generation and the conduction of nerve impulses by increasing the threshold for electrical excitation in the nerve, by slowing propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: 1) pain, 2) temperature, 3) touch, 4) proprioception and 5) skeletal muscle tone. Levobupivacaine (CHIROCAINE®) is a safer alternative for regional anesthesia than bupivacaine. It demonstrated less affinity and strength of depressant effects onto myocardial and central nervous vital centers in pharmacodynamic studies, and a superior pharmacokinetic profile.
Status:
US Previously Marketed
Source:
ALAMAST by SANTEN
(1999)
Source URL:
First approved in 1999
Source:
ALAMAST by SANTEN
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Pemirolast is a mast cell stabilizer that acts as an antiallergic agent, it is approved in Japan for the treatment of bronchial asthma and of allergic rhinitis. Pemirolast strongly inhibits extracellular Ca2+ influx and the release of intracellular Ca2+, an important factor in the release of chemical mediators, by inhibiting inositol-phospholipid metabolism in mast cells. It also inhibits the release of arachidonic acid. Furthermore contribution of increasing effect on c-AMP based on inhibiting phosphodiesterase is suggested. Main pharmacological effects is an inhibition of release of chemical mediators, e.g. histamine, LTB4, LTC4, LTD4, PGD2, TXB2 and PAF from human lung tissues, abraded fragments of the nasal mucosa, and peripheral leukocytes, rat peritoneal exudate cells, and rat and guniea pig lung tissues.
Status:
US Previously Marketed
Source:
MERIDIA by ABBOTT
(1997)
Source URL:
First approved in 1997
Source:
MERIDIA by ABBOTT
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Targets:
Conditions:
Subitramine is a potent inhibitor of monoamines (serotonin, dopamine, noradrenaline) reuptake that was approved by FDA for the treatmen of obesity. Sibutramine is metabolized to metabolites M1 and M2 which are more active toward the monoamine transporters.The drug was withdrawn from the market because of clinical trial data indicating an increased risk of heart attack and stroke. It was sold under a variety of brand names including Reductil, Meridia and Sibutrex.
Status:
US Previously Marketed
Source:
MERIDIA by ABBOTT
(1997)
Source URL:
First approved in 1997
Source:
MERIDIA by ABBOTT
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Subitramine is a potent inhibitor of monoamines (serotonin, dopamine, noradrenaline) reuptake that was approved by FDA for the treatmen of obesity. Sibutramine is metabolized to metabolites M1 and M2 which are more active toward the monoamine transporters.The drug was withdrawn from the market because of clinical trial data indicating an increased risk of heart attack and stroke. It was sold under a variety of brand names including Reductil, Meridia and Sibutrex.
Status:
US Previously Marketed
Source:
MERIDIA by ABBOTT
(1997)
Source URL:
First approved in 1997
Source:
MERIDIA by ABBOTT
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Subitramine is a potent inhibitor of monoamines (serotonin, dopamine, noradrenaline) reuptake that was approved by FDA for the treatmen of obesity. Sibutramine is metabolized to metabolites M1 and M2 which are more active toward the monoamine transporters.The drug was withdrawn from the market because of clinical trial data indicating an increased risk of heart attack and stroke. It was sold under a variety of brand names including Reductil, Meridia and Sibutrex.
Status:
US Previously Marketed
Source:
MERIDIA by ABBOTT
(1997)
Source URL:
First approved in 1997
Source:
MERIDIA by ABBOTT
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Subitramine is a potent inhibitor of monoamines (serotonin, dopamine, noradrenaline) reuptake that was approved by FDA for the treatmen of obesity. Sibutramine is metabolized to metabolites M1 and M2 which are more active toward the monoamine transporters.The drug was withdrawn from the market because of clinical trial data indicating an increased risk of heart attack and stroke. It was sold under a variety of brand names including Reductil, Meridia and Sibutrex.
Status:
US Previously Marketed
Source:
FENOLDOPAM MESYLATE by HIKMA
(2004)
Source URL:
First approved in 1997
Source:
CORLOPAM by HOSPIRA
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
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.
Status:
US Previously Marketed
Source:
TEVETEN HCT by ABBVIE
(2001)
Source URL:
First approved in 1997
Source:
TEVETEN by ABBVIE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
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).