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Status:
US Previously Marketed
Source:
KANAMYCIN SULFATE by PHARMAFAIR
(1987)
Source URL:
First approved in 1958
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Kanamycin A is aminoglycoside anti-bacterial agent. Active against many strains of Gram-negative bacteria and Gram-positive Staphylococcus aureus and epidermis. Some strains of Mycobacterium bacterium are sensitive. Most active in alkaline solution. It binds to bacterial ribosomes and reduces mRNA translation hence reduces protein biosynthesis. However, it also exhibits some toxic effects towards mammalian cells.
Status:
First approved in 1956
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Oleandomycin is a macrolide antibiotic, which was first described under the designation P.A.105 by Sobin, English, and Celmer (1954-5). Later it appeared on the market under three names and in two forms: as pure oleandomycin ("matromycin," Pfizer; "romicil," Hoffmann-La Roche) and as a mixture with twice its weight of tetracycline ("sigmamycin," Pfizer). Oleandomycin can be employed to inhibit the activities of bacteria responsible for causing infections in the upper respiratory tract much like Erythromycin can. Both can affect staphylococcus and enterococcus genera. Oleoandomycin is reported to inhibit most gram-positive bacteria, but has only a slight inhibiting effect on gram-negative bacteria, rickettsiae, and larger viruses. The spectrum of activity on micro-organisms is therefore wider than that of penicillin and streptomycin, but narrower than that of chloramphenicol and the tetracyclines. Oleandomycin is approved as a veterinary antibiotic in some countries. It has been approved as a swine and poultry antibiotic in the United States. However, it is currently only approved in the United States for production uses. Oleandomycin is a bacteriostatic agent. Like erythromycin, oleandomycin binds to the 50s subunit of bacterial ribosomes, inhibiting the completion of proteins vital to survival and replication. It interferes with translational activity but also with 50s subunit formation. However, unlike erythromycin and its effective synthetic derivatives, it lacks a 12-hydroxyl group and a 3-methoxy group. This change in structure may adversely affect its interactions with 50S structures and explain why it is a less powerful antibiotic.
Status:
US Previously Marketed
Source:
MYTELASE by SANOFI AVENTIS US
(1956)
Source URL:
First approved in 1956
Source:
MYTELASE by SANOFI AVENTIS US
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Ambenonium is a cholinesterase inhibitor with all the pharmacologic actions of
acetylcholine, both the muscarinic and nicotinic types. It was marketed under the brand name Mytelase, but was withdrawn from the market in the United States in 2010. Ambenonium, similar to pyridostigmine and neostigmine, is used for the treatment of muscle weakness and fatigue in people with myasthenia gravis.Ambenonium exerts its actions against myasthenia gravis by competitive, reversible inhibition of acetylcholinesterase. The disease myasthenia gravis occurs when the body inappropriately produces antibodies against acetylcholine receptors, and thus inhibits proper acetylcholine signal transmission (when acetylcholine binds to acetylcholine receptors of striated muscle fibers, it stimulates those fibers to contract). Ambenonium reversibly binds acetylcholinesterase at the anionic site, which results in the blockage of the site of acetycholine binding, thereby inhibiting acetylcholine hydrolysis and enhancing cholinergic function through the accumulation of acetycholine at cholinergic synpases. In turn this facilitates transmission of impulses across the myoneural junction and effectively treats the disease.
Status:
US Previously Marketed
Source:
ALBAMYCIN T NOVOBIOCIN by UPJOHN
(1964)
Source URL:
First approved in 1956
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Novobiocin (also known as streptonivicin) is an aminocoumarin antibiotic, active against Staphylococcus epidermidis. Novobiocin and other aminocoumarin antibiotics act as a potent competitive inhibitor of DNA gyrase B. The oral form of the drug was withdrawn from the market in 1999 due to safety or effectiveness reasons. Later it was discovered that novobiocin inhibited Hsp90 and topoisomerase II, and novobiocin was investigated in clinical trials against metastatic breast cancer and non-small cell lung cancer. Topical form of novobiocin was investigated in combination with nalidixic acid for treatment of psoriasis.
Status:
US Previously Marketed
Source:
CANTIL by SANOFI AVENTIS US
(1956)
Source URL:
First approved in 1956
Source:
CANTIL by SANOFI AVENTIS US
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Mepenzolate is a postganglionic parasympathetic inhibitor. It decreases gastric acid and pepsin secretion and suppresses spontaneous contractions of the colon. It specifically antagonizes muscarinic receptors. Mepenzolate is marketed under the brand name CANTIL. CANTIL is indicated for use as adjunctive therapy in the treatment of peptic ulcer. It has not been
shown to be effective in contributing to the healing of peptic ulcer, decreasing the rate of recurrence, or
preventing complications.
Status:
First approved in 1956
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Oleandomycin is a macrolide antibiotic, which was first described under the designation P.A.105 by Sobin, English, and Celmer (1954-5). Later it appeared on the market under three names and in two forms: as pure oleandomycin ("matromycin," Pfizer; "romicil," Hoffmann-La Roche) and as a mixture with twice its weight of tetracycline ("sigmamycin," Pfizer). Oleandomycin can be employed to inhibit the activities of bacteria responsible for causing infections in the upper respiratory tract much like Erythromycin can. Both can affect staphylococcus and enterococcus genera. Oleoandomycin is reported to inhibit most gram-positive bacteria, but has only a slight inhibiting effect on gram-negative bacteria, rickettsiae, and larger viruses. The spectrum of activity on micro-organisms is therefore wider than that of penicillin and streptomycin, but narrower than that of chloramphenicol and the tetracyclines. Oleandomycin is approved as a veterinary antibiotic in some countries. It has been approved as a swine and poultry antibiotic in the United States. However, it is currently only approved in the United States for production uses. Oleandomycin is a bacteriostatic agent. Like erythromycin, oleandomycin binds to the 50s subunit of bacterial ribosomes, inhibiting the completion of proteins vital to survival and replication. It interferes with translational activity but also with 50s subunit formation. However, unlike erythromycin and its effective synthetic derivatives, it lacks a 12-hydroxyl group and a 3-methoxy group. This change in structure may adversely affect its interactions with 50S structures and explain why it is a less powerful antibiotic.
Status:
US Previously Marketed
Source:
MYTELASE by SANOFI AVENTIS US
(1956)
Source URL:
First approved in 1956
Source:
MYTELASE by SANOFI AVENTIS US
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Ambenonium is a cholinesterase inhibitor with all the pharmacologic actions of
acetylcholine, both the muscarinic and nicotinic types. It was marketed under the brand name Mytelase, but was withdrawn from the market in the United States in 2010. Ambenonium, similar to pyridostigmine and neostigmine, is used for the treatment of muscle weakness and fatigue in people with myasthenia gravis.Ambenonium exerts its actions against myasthenia gravis by competitive, reversible inhibition of acetylcholinesterase. The disease myasthenia gravis occurs when the body inappropriately produces antibodies against acetylcholine receptors, and thus inhibits proper acetylcholine signal transmission (when acetylcholine binds to acetylcholine receptors of striated muscle fibers, it stimulates those fibers to contract). Ambenonium reversibly binds acetylcholinesterase at the anionic site, which results in the blockage of the site of acetycholine binding, thereby inhibiting acetylcholine hydrolysis and enhancing cholinergic function through the accumulation of acetycholine at cholinergic synpases. In turn this facilitates transmission of impulses across the myoneural junction and effectively treats the disease.
Status:
US Previously Marketed
Source:
ALBAMYCIN T NOVOBIOCIN by UPJOHN
(1964)
Source URL:
First approved in 1956
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Novobiocin (also known as streptonivicin) is an aminocoumarin antibiotic, active against Staphylococcus epidermidis. Novobiocin and other aminocoumarin antibiotics act as a potent competitive inhibitor of DNA gyrase B. The oral form of the drug was withdrawn from the market in 1999 due to safety or effectiveness reasons. Later it was discovered that novobiocin inhibited Hsp90 and topoisomerase II, and novobiocin was investigated in clinical trials against metastatic breast cancer and non-small cell lung cancer. Topical form of novobiocin was investigated in combination with nalidixic acid for treatment of psoriasis.
Status:
US Previously Marketed
Source:
PATHILON by LEDERLE
(1982)
Source URL:
First approved in 1954
Source:
PATHILON by LEDERLE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Tridihexethyl is a synthetic anticholinergic agent which was marketed under the brand name Pathilon as an adjunct in the treatment of peptic ulcer disease. However, it is no longer available in the US market. Tridihexethyl may block all three types of muscarinic receptors including M-1 receptors in the CNS and ganglia, M-2 receptors in the heart, and M-3 receptors. The muscarinic acetylcholine receptors mediate various cellular responses including inhibition of adenylate cyclase, the breakdown of phosphoinositides, and modulation of potassium channels through the action of G proteins. Tridihexethyl inhibits vagally mediated reflexes by antagonizing the action of acetylcholine. This, in turn, reduces the secretion of gastric acids in the stomach. Tridihexethyl was also examined for effect on patients with acquired nystagmus where four out of six patients showed improvement, but due to the profile usage of Tridihexethyl to treat nystagmus was limited.
Status:
US Previously Marketed
Source:
PATHILON by LEDERLE
(1982)
Source URL:
First approved in 1954
Source:
PATHILON by LEDERLE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Tridihexethyl is a synthetic anticholinergic agent which was marketed under the brand name Pathilon as an adjunct in the treatment of peptic ulcer disease. However, it is no longer available in the US market. Tridihexethyl may block all three types of muscarinic receptors including M-1 receptors in the CNS and ganglia, M-2 receptors in the heart, and M-3 receptors. The muscarinic acetylcholine receptors mediate various cellular responses including inhibition of adenylate cyclase, the breakdown of phosphoinositides, and modulation of potassium channels through the action of G proteins. Tridihexethyl inhibits vagally mediated reflexes by antagonizing the action of acetylcholine. This, in turn, reduces the secretion of gastric acids in the stomach. Tridihexethyl was also examined for effect on patients with acquired nystagmus where four out of six patients showed improvement, but due to the profile usage of Tridihexethyl to treat nystagmus was limited.