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

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Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Oxolamine under brand names Symphocal, Perebron is used in some countries as a cough suppressant for the treatment of pharyngitis, tracheitis, bronchitis, bronchiectasis, pertussis. Oxolamine possesses anti-inflammatory activity, which causes a reduction in the irritation of the nervous receptors of the respiratory tract.
Status:
Possibly Marketed Outside US
Source:
Japan:Rolitetracycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rolitetracycline nitrate is an antibiotic formed by N-aminomethylation of the carboxamide group of tetracycline. Rolitetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis. It is formulated for intravenous or intramuscular injections and is used in cases requiring high concentrations or when oral administration is impractical. In combinations with chloramphenicol and colistin, it is used as the eye drops for the treatment of external eye infections such as catarrhal conjunctivitis, purulent, trachoma, blepharitis, blepharoconjunctivitis, bacterial keratitis, septic corneal ulcers.
Ribostamycin sulfate is an aminoglycoside-aminocyclitol antibiotic isolated from a streptomycete. It is an important broad-spectrum antibiotic with important use against human immunodeficiency virus and is considered a critically important antimicrobial by the World Health Organization. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit (some work by binding to the 50S subunit), inhibiting the translocation of the peptidyl-tRNA from the A-site to the P-site and also causing misreading of mRNA, leaving the bacterium unable to synthesize proteins vital to its growth. Ribostamycin is usually used to treat sepsis, superficial skin infection, deep skin infection, lymphangitis/lymphadenitis, chronic pyoderma, osteomyelitis, pharyngitis/laryngitis, tonsillitis, acute bronchitis, pneumonia, pulmonary abscess, pyothorax, secondary infection in chronic respiratory lesions, cystitis, pyelonephritis, gonococcal infection, peritonitis, cholecystitis, dacryocystitis, keratitis (including corneal ulcer), otitis media, sinusitis and gnathitis. The most commonly reported adverse reactions include renal dysfunction, liver disorder and rash.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Noxiptiline (brand names Agedal, Elronon, Nogedal), is a tricyclic antidepressant (TCA) that was introduced in Europe in the 1970s for the treatment of depression. In a double-blind comparison of noxiptiline and amitriptyline in hospitalized patients with primary depressive illness for 3-6 weeks there were no significant differences, but noxiptiline had a faster onset of action. A comparison with imipramine also showed no difference in therapeutic efficacy. As regards adverse effects, noxiptiline seemed to cause more mental symptoms, such as delirium. In one study in 44 patients, 9 developed delirium, there were mild manic symptoms in 6, dry mouth in 21, disturbed micturition in 2. and difficulty in accommodation in 3.
S-Adenosylmethionine (often referred to as SAMe) is a methyl donor and a cofactor for enzyme-catalyzed methylations, including catechol O-methyltransferase (COMT) and DNA methyltransferases (DNMT). Although present in all cells, it is concentrated in liver where 85% of all methylation reactions occur. SAM is anti-apoptotic in normal hepatocytes and normal colon epithelial cells but pro-apoptotic in liver human hepatocellular carcinoma (HCC), HepG2 cells and colon cancer cells. Because of structural instability, stable salt forms of SAM are required for its use as an oral drug. The commonly used salts: tosylate, butanedisulfonate, disulfate tosylate, disulfate ditosylate, and disulfate monotosylate. SAMe has been marketed in some European countries since the mid-1980s for the treatment of depression and for other medical conditions such as osteoarthritis (joint disease that causes joint pain and stiffness), fibromyalgia (widespread pain and stiffness). In addition, it is used to treat liver disease and migraine headaches. However, it is not formally approved in the UK for the treatment of depression, and in the USA, it is classified only as a dietary supplement. Some research suggests that it is more effective than placebo in treating mild-to-moderate depression and is just as effective as antidepressant medications without the side effects (headaches, sleeplessness, and sexual dysfunction). In addition, antidepressants tend to take 6 to 8 weeks to begin working, while It seems to begin more quickly. Researchers are not sure how SAMe works to relieve depression. But they speculate it might increase the amount of serotonin in the brain just as some antidepressants do. Many studies have examined injectable forms of SAMe, not oral supplements.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

trans-Sobrerol is a mucolytic known due its emplyment in therapy for respiratory diseases. In preclinical studies sobrerol, administered daily at the oral dose of 400 mg/rat, markedly decreased the monocrotaline-induced alterations and regulate the development of pulmonary hypertension. Treatment with sobrerol was well tolerated and significantly reduced frontal headache and rhinorrhoea, efficacy being confirmed by rhinomanometry.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxetorone is an antimigraine drug used for the disease-modifying treatment of migraines and marketed in several European countries. It works by non-selective inhibition of serotonin receptors and antihistamine agent. The therapeutic effects of oxetorone are primarily linked to antiserotonergic and also antihistamine and anti-adrenergic properties. Antidopaminergic properties are also suspected because hyperprolactinemia and extrapyramidal reactions have been observed. Adverse effects are: hypertonia, drowsiness at the start of treatment, diarrhoea and lymphocytic colitis. Acute intoxications by oxetorone, although uncommon, are potentially severe poisonings.
Status:
First approved in 1977
Source:
Colestid by Upjohn
Source URL:

Class:
POLYMER



Tetraethylenepentamine (TEPA) is a low-molecular-weight linear polyamine exerting metal-chelating properties. TEPA is widely used in industrial applications. The principal hazards that arise in working with TEPA are those associated with similar organic amines; namely, a corrosive action on skin and eyes. TEPA biological activity was attributed to its effect on cellular Cu levels as (a) treatment with TEPA resulted in reduction of cellular Cu, and (b) excess of Cu reversed TEPA's activity and accelerated differentiation. TEPA was shown to attenuate the differentiation of ex vivo cultured hematopoietic cells resulting in preferential expansion of early progenitors. A phase I/II trial was performed to test the feasibility and safety of transplantation of CD133+ cord blood (CB) hematopoietic progenitors cultured in media containing stem cell factor, FLT-3 ligand, interleukin-6, thrombopoietin and TEPA. Transplanting a population of CD133+ CB cells which were expanded ex vivo for 21 days using SCF, FLT3, IL-6, TPO and the copper chelator TEPA (StemEx) was feasible. The expanded cells were well tolerated, with no infusion-related adverse events observed.