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

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Selegiline, also known as L-deprenyl, is a substituted phenethylamine, a selective, irreversible inhibitor of Type B monoamine oxidase. Selegiline is available in pill form under many brand names (Eldepryl, Carbex, Atapryl) and is used to reduce symptoms in early-stage Parkinson's disease. Selegiline delays the time point when the L-DOPA (levodopa) treatment becomes necessary from about 11 months to about 18 months after diagnosis, which is beneficial despite not being definitive evidence of neuroprotection. The rationale for adding selegiline to levodopa is to decrease the required dose of levodopa and thus reduce the motor complications of levodopa therapy. Selegiline is also delivered via a transdermal patch (brand name, Emsam) and in this form, Selegiline is used as a treatment for the major depressive disorder. Selegiline (brand name Anipryl) is also used (at extremely high dosages relative to humans) in veterinary medicine to treat the symptoms of Cushing's disease and cognitive dysfunction (Canine Cognitive Dysfunction) in dogs. Side effects of the pill form include, in decreasing order of frequency, nausea, hallucinations, confusion, depression, loss of balance, insomnia, increased involuntary movements, agitation, arrhythmia, slow heart rate, delusions, hypertension, new or increased angina pectoris, and syncope. The main side effects of the patch form for depression included application site reactions, insomnia, diarrhea, and sore throat.
Status:
Investigational
Source:
INN:morsuximide [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Morsuximide is succinimide derivative patented by Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt. as an antiepileptic agent. In cats, Morsuximide had mild hypnotic effects when given i.p., and the status epileptic induced by Tetracor was brought under control. Tetracor, given after the administration of Morsuximide, caused only subconvulsive seizures in cats accompanied by an occasional jerk of the skeletal musculature. When 16 epileptic patients were treated with oral Morsuximide (1.0-2.0 g. daily for an av. of 42 days) the drug produced a favorable effect in all forms of human epilepsy, particularly in cases of psychomotor attacks, atypical forms, and petit mal. The major type of epilepsy (grand mal) did not respond to the drug therapy as markedly as the other forms, although drug caused some improvement in these cases.
Status:
Investigational
Source:
INN:prazocillin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Prazocillin is 6-aminopenicillanic acid derivative patented by Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt. as a bactericidal compound. The activity of Prazocillin against Staphylococcus aureus strains was the same as that of dikloxacillin, but Prazocillin was more active against Bacillus subtilis ATCC 6633. Prazocillin had a bactericidal effect on a penicillin-resistant S. aureus strain at concentrations of 1 μg/ml. Pyrazocillin inhibits bacterial penicillinase in vitro.
Status:
Possibly Marketed Outside US
Source:
Japan:Ipriflavone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ipriflavone (chemical structure: 7-isopropoxyisoflavone), derived from the soy isoflavone, daidzein, holds great promise for osteoporosis prevention and treatment. Ipriflavone (IP) was discovered in the 1930s but has only recently begun to be embraced by the medical community in this country. Over 150 studies on safety and effectiveness, both animal and human, have been conducted in Italy, Hungary, and Japan. As of 1997, 2,769 patients had been treated a total of 3,132 patient years. Preliminary studies have pointed to its effectiveness in the treatment of other conditions involving bone pathology, including Paget’s disease, hyperparathyroidism, renal osteodystrophy, and tinnitus due to otosclerosis. Ipriflavone appears to have several mechanisms of action, all of which enhance bone density, making them seemingly superior to many of the other treatments available for osteoporosis prevention and treatment. IP also inhibits osteoclastic activity (motility and resorptive activity) by modulating intracellular free calcium. IP’s bone-forming mechanisms include stimulation of cell proliferation and maturation of osteoblasts by inhibiting calcium influx into osteoblasts and phosphoinositide hydrolysis. Despite similarities to estrogen, IP possesses no intrinsic estrogenic activity, but does potentiate estrogen. Importantly, IP does not change bone mineral composition or crystalline structure. A clinical trial reported in 2001 that it was not effective in prevention or treatment of osteoporosis.
Selegiline, also known as L-deprenyl, is a substituted phenethylamine, a selective, irreversible inhibitor of Type B monoamine oxidase. Selegiline is available in pill form under many brand names (Eldepryl, Carbex, Atapryl) and is used to reduce symptoms in early-stage Parkinson's disease. Selegiline delays the time point when the L-DOPA (levodopa) treatment becomes necessary from about 11 months to about 18 months after diagnosis, which is beneficial despite not being definitive evidence of neuroprotection. The rationale for adding selegiline to levodopa is to decrease the required dose of levodopa and thus reduce the motor complications of levodopa therapy. Selegiline is also delivered via a transdermal patch (brand name, Emsam) and in this form, Selegiline is used as a treatment for the major depressive disorder. Selegiline (brand name Anipryl) is also used (at extremely high dosages relative to humans) in veterinary medicine to treat the symptoms of Cushing's disease and cognitive dysfunction (Canine Cognitive Dysfunction) in dogs. Side effects of the pill form include, in decreasing order of frequency, nausea, hallucinations, confusion, depression, loss of balance, insomnia, increased involuntary movements, agitation, arrhythmia, slow heart rate, delusions, hypertension, new or increased angina pectoris, and syncope. The main side effects of the patch form for depression included application site reactions, insomnia, diarrhea, and sore throat.
Status:
Possibly Marketed Outside US
Source:
Japan:Ipriflavone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ipriflavone (chemical structure: 7-isopropoxyisoflavone), derived from the soy isoflavone, daidzein, holds great promise for osteoporosis prevention and treatment. Ipriflavone (IP) was discovered in the 1930s but has only recently begun to be embraced by the medical community in this country. Over 150 studies on safety and effectiveness, both animal and human, have been conducted in Italy, Hungary, and Japan. As of 1997, 2,769 patients had been treated a total of 3,132 patient years. Preliminary studies have pointed to its effectiveness in the treatment of other conditions involving bone pathology, including Paget’s disease, hyperparathyroidism, renal osteodystrophy, and tinnitus due to otosclerosis. Ipriflavone appears to have several mechanisms of action, all of which enhance bone density, making them seemingly superior to many of the other treatments available for osteoporosis prevention and treatment. IP also inhibits osteoclastic activity (motility and resorptive activity) by modulating intracellular free calcium. IP’s bone-forming mechanisms include stimulation of cell proliferation and maturation of osteoblasts by inhibiting calcium influx into osteoblasts and phosphoinositide hydrolysis. Despite similarities to estrogen, IP possesses no intrinsic estrogenic activity, but does potentiate estrogen. Importantly, IP does not change bone mineral composition or crystalline structure. A clinical trial reported in 2001 that it was not effective in prevention or treatment of osteoporosis.