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Status:
US Previously Marketed
Source:
MAXAQUIN by PHARMACIA
(1992)
Source URL:
First approved in 1992
Source:
MAXAQUIN by PHARMACIA
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Lomefloxacin hydrochloride (marketed under the following brand names in English speaking countries Maxaquin, Okacyn, Uniquin) is a fluoroquinolone antibiotic used to treat bacterial infections. It is used to treat chronic bronchitis, as well as complicated and uncomplicated urinary tract infections. It is also used as a prophylactic or preventative treatment to prevent urinary tract infections in patients undergoing transrectal or transurethral surgical procedures. Flouroquinolones such as lomefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter. Lomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Status:
US Previously Marketed
Source:
TILADE by SANOFI AVENTIS US
(1997)
Source URL:
First approved in 1992
Source:
TILADE by KING PHARMS LLC
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Nedocromil is a medication considered as mast cell stabilizer used to treat itching associated with allergic conjunctivitis. Nedocromil has been shown to inhibit the in vitro activation of, and mediator release from, a variety of inflammatory cell types associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits activation and release of inflammatory mediators such as histamine, prostaglandin D2 and leukotrienes c4 from different types of cells in the lumen and mucosa of the bronchial tree. These mediators are derived from arachidonic acid metabolism through the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of nedocromil may be due partly to inhibition of axon reflexes and release of sensory neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil does not possess any bronchodilator, antihistamine, or corticosteroid activity. Nedocromil is indicated for the treatment of itching associated with allergic conjunctivitis.
Status:
US Previously Marketed
Source:
HALFAN by GLAXOSMITHKLINE
(1992)
Source URL:
First approved in 1992
Source:
HALFAN by GLAXOSMITHKLINE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Halofantrine is a blood schizonticidal antimalarial agent with no apparent action on the sporozoite, gametocyte or hepatic stages of the infection. It is used only to treat but not to prevent malaria. Has been marketed by GlaxoSmithKline as HALFAN (halofantrine hydrochloride) in 250 mg tablets indicated for the treatment of adults who can tolerate oral medication and who have mild to moderate malaria (equal to or less than 100,000 parasites/mm3) caused by Plasmodium falciparum or Plasmodium vivax. Among side effects is cardiac arrhythmia. It belongs to the phenanthrene class of compounds that includes quinine and lumefantrine. It was reported that halofantrine binds to hematin in vitro (crystal structure of the complex) and to to plasmpesin, a haemoglobin degrading enzyme unique to the malarial parasites.
Status:
US Previously Marketed
Source:
MIVACRON by ABBVIE
(1992)
Source URL:
First approved in 1992
Source:
MIVACRON by ABBVIE
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
Mivacurium chloride (Mivacron) is a new benzylisoquinolinium choline-like diester neuromuscular blocking drug with an onset of action at equipotent doses that is comparable to atracurium and vecuronium but slower than succinylcholine. MIVACRON (a mixture of three stereoisomers) binds competitively to cholinergic receptors on the
motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular
transmission. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine. MIVACRON is a short-acting neuromuscular blocking agent indicated for inpatients and outpatients,
as an adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle
relaxation during surgery or mechanical ventilation.
Status:
Possibly Marketed Outside US
Source:
NCT00483795: Phase 4 Interventional Completed Corneal Staining
Source URL:
First approved in 1992
Source:
21 CFR 358A
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Aminomethylpropanol is a synthetic ingredient that functions as a buffer to adjust the pH of cosmetics and personal care products. In cosmetics and personal care products, aminomethylpropanol is used in the formulation of creams and lotions, hair sprays, wave sets, hair dyes and colors, eye and facial products, and other hair and skin care products. The main function of aminomethylpropanol in these products is to establish and hold the pH. The Food and Drug Administration (FDA) includes aminomethylpropanol on its list of indirect food additives as a component of adhesives that are in contact with food. The European Chemicals Agency (ECHA) identifies that “substance causes serious eye irritation, is harmful to aquatic life with long lasting effects and causes skin irritation, causes serious eye damage.” Toxicologically significant concentrations of AMP are unlikely to be achieved in the systemic circulation and/or target tissues in humans as a result of dermal application of products containing aminomethylpropanol. Systemically absorbed dose will be rapidly eliminated from the body with little remaining at the application site.
Status:
Possibly Marketed Outside US
Source:
NCT01939145: Phase 4 Interventional Completed Wound Infection
(2013)
Source URL:
First approved in 1992
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Polihexanide is a broad-spectrum antiseptic with excellent cell and tissue tolerability, ability to bind to the organic matrix, low risk of contact sensitization, and wound healing promoting effect. Polihexanide interacts with acidic, negatively charged phospholipids in the bacterial membrane, leading to increased fluidity, permeability and loss of integrity, followed by the death of the organism. Polihexanide is also transferred to the cytoplasm, where it leads to disruption of the bacterial metabolism. Neutral phospholipids on the other hand are little or not affected by Polihexanide. This is commonly seen as the main reason for the low toxicity of Polihexanide against human cells and its high therapeutic range. Due to its nonspecific, strong interaction with negatively charged phospholipids, Polihexanide has a broad antimicrobial spectrum, including Gram-positive and Gramnegative bacteria, plaque-forming and biofilm-building bacteria, spore-forming bacteria (but not bacterial spores), intracellular bacteria such as chlamydiae and mycoplasma, and fungi including Candida spp. as well as Aspergillus spp. Polihexanide is classified as ‘practically nontoxic’. The therapeutic index of Polihexanide is more than 200-fold that of chlorhexidine.
Status:
Possibly Marketed Outside US
First approved in 1992
Source:
21 CFR 331
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Adipic acid has been incorporated into controlled-release formulation matrix tablets to obtain a pH-independent release for both weakly basic and weakly acidic drugs. It has also been incorporated into the polymeric coating of hydrophilic monolithic systems to modulate the intragel pH, resulting in zero-order release of hydrophilic drugs. The disintegration at intestinal pH of the enteric polymer shellac has been reported to improve when adipic acid was used as a pore-forming agent without affecting release in the acidic media. Adipic acid is used to make bisobrin an antifibrinolytic.
Status:
Possibly Marketed Outside US
First approved in 1992
Source:
21 CFR 331
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Adipic acid has been incorporated into controlled-release formulation matrix tablets to obtain a pH-independent release for both weakly basic and weakly acidic drugs. It has also been incorporated into the polymeric coating of hydrophilic monolithic systems to modulate the intragel pH, resulting in zero-order release of hydrophilic drugs. The disintegration at intestinal pH of the enteric polymer shellac has been reported to improve when adipic acid was used as a pore-forming agent without affecting release in the acidic media. Adipic acid is used to make bisobrin an antifibrinolytic.
Status:
Possibly Marketed Outside US
First approved in 1992
Source:
21 CFR 331
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Adipic acid has been incorporated into controlled-release formulation matrix tablets to obtain a pH-independent release for both weakly basic and weakly acidic drugs. It has also been incorporated into the polymeric coating of hydrophilic monolithic systems to modulate the intragel pH, resulting in zero-order release of hydrophilic drugs. The disintegration at intestinal pH of the enteric polymer shellac has been reported to improve when adipic acid was used as a pore-forming agent without affecting release in the acidic media. Adipic acid is used to make bisobrin an antifibrinolytic.
Status:
Possibly Marketed Outside US
Source:
NDA020131
(1992)
Source URL:
First approved in 1992
Source:
NDA020131
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Calteridol is tetraazacyclododecane-1,4,7-triacetic acid derivative patented by Bracco and Dibra S.P.A.