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Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Lidamidine, also known as WHR-1142A and Lidaral, is an alpha2-adrenergic receptor agonist that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction. Lidamidine hydrochloride is used to treat diarrhoea and other gastrointestinal disorders. Lidamidine’s intestinal antisecretory effects are
mediated through the activation of peripheral alpha-2 adrenoceptors. Lidamidine crosses
the blood brain barrier poorly and is therefore devoid of the centrally mediated alpha-2
effects that have limited the use of other alpha-2 adrenoceptor agonists in the intestinal
tract.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Celiprolol is beta blocker, used to treat high blood pressure. Celiprolol is a selective β1 receptor antagonist, β2 receptor partial agonist. Celiprolol is not approved by the FDA, but is available worldwide under brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm. It is used to treat mild to moderate hypertension and angina prectoris. In 2010 celiprolol has demonstrated positive results in the prevention of vascular complications of Ehlers-Danlos syndrome. Celiprolol has fewer CNS-related side effects than other beta blockers presumably because of limited penetration through blood-brain barrier because of its solubility.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Distigmine is an acetylcholinesterase (AChE) inhibitor. Distigmine shows direct binding to muscarinic receptors in the rat bladder, and repeated oral administration of distigmine causes downregulation of muscarinic receptors in the rat bladder. The observed direct interaction of distigmine with the bladder muscarinic receptors may partly contribute to the therapeutic and/or side effects seen in the treatment of detrusor underactivity. It is usually used to treat myasthenia gravis, dysuria due to hypotonic bladder such as neurogenic bladder or after surgery. Common side effects are: nausea/vomiting, abdominal pain, diarrhea, increased salivation, hypersecretion in respiratory tract, sweating, bradycardia, miosis, difficulty in breathing. Distigmine has a greater risk of causing cholinergic crisis because of accumulation of the drug being more likely than with neostigmine or pyridostigmine and so distigmine is rarely used as a treatment for myasthenia gravis, unlike pyridostigmine and neostigmine.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Debrisoquin is an antihypertensive drug having guanethidine-like properties, which inhibits monoamine oxidase
(MAO) and does not enter the brain. Debrisoquine was used for the treatment of hypertension. Debrisoquine hydroxylation phenotype has been the most used test in humans to evaluate CYP2D6 activity. Two debrisoquine hydroxylation phenotypes have been described: poor and extensive metabolizers. A group with a very low debrisoquine metabolic ratio within the extensive metabolizers, named ultrarapid metabolizers, has also been distinguished. This CYP2D6 variability can be for a large part alternatively determined by genotyping, which appears to be of clinical importance given CYP2D6 involvement in the metabolism of a large number of commonly prescribed drugs.
Status:
US Approved Rx
(2014)
Source:
NDA021883
(2014)
Source URL:
First approved in 2014
Source:
NDA021883
Source URL:
Class:
MIXTURE
Targets:
Dalbavancin is a second-generation lipoglycopeptide antibiotic that was designed to improve on the natural glycopeptides currently available, such as vancomycin and teicoplanin. Modifications from these older glycoprotein classes allowed a similar mechanism of action with increased activity and once weekly dosing. Its use is indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by the following gram-positive microorganisms: Staphylococcus aureus (including methicillin-susceptible and methicillin-resistant strains), S. pyogenes, S. agalactiae, and S. anginosus group (including S. anginosus, S. intermedius, and S. constellatus). Under the brand name DALVANCE Dalbavancin is indicated for acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible strains of Gram-positive microorganisms. The bactericidal action of dalbavancin results primarily from inhibition of cell-wall biosynthesis. Specifically, dalbavancin prevents incorporation of N-acetylmuramic acid (NAM)- and N-acetylglucosamine (NAG)-peptide subunits from being incorporated into the peptidoglycan matrix; which forms the major structural component of Gram-positive cell walls. The large hydrophilic molecule is able to form hydrogen bond interactions with the terminal D-alanyl-D-alanine moieties of the NAM/NAG-peptides, which is normally a five-point interaction. Binding of dalbavancin to the D-Ala-D-Ala prevents the incorporation of the NAM/NAG-peptide subunits into the peptidoglycan matrix. In addition, dalbavancin alters bacterial-cell-membrane permeability and RNA synthesis.
Status:
US Approved Rx
(2021)
Source:
ANDA209708
(2021)
Source URL:
First approved in 1992
Source:
MIVACRON by ABBVIE
Source URL:
Class:
MIXTURE
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:
US Approved Rx
(2012)
Source:
ANDA065351
(2012)
Source URL:
First approved in 1991
Source:
CEFZIL by CORDEN PHARMA
Source URL:
Class:
MIXTURE
Targets:
Conditions:
Cefprozil is a 2nd generation cephalosporin that is FDA approved for the treatment of mild to moderate infections of upper respiratory tract, lower respiratory tract, and uncomplicated skin and skin-structure infections. Cefprozil, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Common adverse reactions include diarrhea, nausea, vomiting, dizziness, abdominal pain and vaginitis. Nephrotoxicity has been reported following concomitant administration of aminoglycoside antibiotics and cephalosporin antibiotics. Concomitant administration of probenecid doubled the AUC for cefprozil.
Status:
US Approved Rx
(1997)
Source:
ANDA074900
(1997)
Source URL:
First approved in 1983
Source:
TRACRIUM PRESERVATIVE FREE by HOSPIRA
Source URL:
Class:
MIXTURE
Conditions:
Atracurium is an intermediate-duration, nondepolarizing, skeletal muscle relaxant for intravenous administration. It is used, as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Most adverse reactions were suggestive of histamine release. Common side effects include flushing of the skin and low blood pressure. Drugs which may enhance the neuromuscular blocking action of atracurium include: enflurane; isoflurane; halothane; certain antibiotics, especially the aminoglycosides and polymyxins; lithium; magnesium salts; procainamide; and quinidine.
Status:
US Approved Rx
(2001)
Source:
ANDA065042
(2001)
Source URL:
First approved in 1973
Source:
BLENOXANE by BRISTOL MYERS SQUIBB
Source URL:
Class:
MIXTURE
Conditions:
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.
Status:
US Approved Rx
(2001)
Source:
ANDA065042
(2001)
Source URL:
First approved in 1973
Source:
BLENOXANE by BRISTOL MYERS SQUIBB
Source URL:
Class:
MIXTURE
Conditions:
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.