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

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Showing 721 - 730 of 1216 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Artemotil (also known as beta-arteether) is an antimalarial artemisinin derivative, approved for the treatment of severe cases of P. falciparum malaria. The mixture of artemotil and alpha-arteether is used in patients with cerebral malaria. Most of the artemisinin compounds including artemotil are metabolized into dihydroartemisinin, which is responsible for antimalarial activity. These compounds contain stable endoperoxide bridge. The antimalarial activity of the drug thus is dependent on the cleavage of the endoperoxide by intraparasitic heme. The cleaved endoperoxide ultimately becomes a carbon centered free radical, which then functions as an alkylating agent, reacting with both heme and parasitic proteins (but not DNA). In P. falciparum, one of the principal alkylation target is the translationally controlled tumor protein (DHA-TCTP) homolog. Some intraparasitic TCTP is situated in the membrane surrounding the heme-rich food vacuole, where heme could catalyse the formation of drug-protein (DHA-TCTP) adduct and inhibit the parasite's growth.
Status:
Possibly Marketed Outside US
Source:
Japan:Bisibuthiamine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Sulbutiamine (isobutyryl thiamine disulfide) is a lipophilic derivative of thiamine. It is available over-the-counter in several countries either as a component of nutritional supplements or as a pharmaceutical preparation. Arcalion (Sulbutiamine) is prescribed as a treatment to help patients with a range of conditions such as asthenia, chronic fatigue, diabetes, hypothyroidism, renal disease, fibromyalgia, and depression (post partum). It remedies the symptoms of weakness by increasing focus, strength (both physical and mental), and energy, making you more alert, less lethargic, and more upbeat whilst also helping to stabilize sleeping patterns. In addition, this medication can also help a patient`s memory, and strengthen thinking processes. Some patient`s have even reported slight eyesight improvements. This product is also popular with athletes as a nutritional supplement as it is a vitamin compound which will not show up in competitive sports blood testing. It can help to achieve your maximum potential and replenish energy after strenuous activities, making it possible to maintain your edge. The presence of sulbutiamine in urinary doping control samples was monitored to evaluate the relevance of its use in sports. The motivating, confidence enhancing effects of sulbutiamine are thought to be related to its ability to enhance dopamine sensitivity. In animal models sulbutiamine has been shown to increase the number of dopamine binding sites (specifically D1) in the prefrontal cortex, this effect is achieved through reduction of dopamine release. Sulbutiamine could be best thought of as a dopamine modulator rather than a compound that directly inhibits or enhances the release of dopamine. Additionally sulbutiamine has been found to enhance memory, possibly by cholinergic transmission. Research indicates that high affinity choline uptake (HACU) was moderately increased in rodent brains following sulbutiamine consumption. However it should be noted the doses used were high (300 mg/kg).
Status:
Possibly Marketed Outside US
Source:
Japan:Prosultiamine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Prosultiamine (Alinamin®), a well-known thiamine derivative, was first developed by Takeda Pharmaceutical Company in Japan in the 1950s. The drug is a homolog of allithiamine produced by thiol-type vitamin B1 and allicin. Prosultiamine is converted to vitamin B1 after absorption from the gut. The drug thus enables a long-lasting high blood concentration of vitamin B1, resulting in efficient access of vitamin B1 to nervous tissue. Prosultiamine has cured many patients with vitamin B1 deficiency resulting in beriberi neuropathy and Wernicke’s encephalopathy. Prosultiamine is also a potential treatment for HTLV, since it has been shown to reduce viral load and symptoms.
Pyridoxamine (PM) is one of three natural forms of vitamin B6. It is a critical transient intermediate in catalysis of transamination reactions by vitamin B6-dependent enzymes. In preclinical or clinical trials PM has demonstrated pharmacological potential for treatment of diabetic nephropathy, diabetic retinopathy, and hyperlipidemia, and for use in kidney stone preventive therapies. Although its precise mode of action in vivo is not yet clear, it is likely that at least three mechanisms are at play: inhibition of post-Amadori steps of the Maillard reaction; scavenging of reactive carbonyl compounds; and inhibition of toxic effects of ROS. Pyridoxamine was marketed as a dietary supplement, often as the hydrochloride salt, pyridoxamine dihydrochloride. However, in the United States, the FDA ruled in January 2009 that pyridoxamine must be regulated as a pharmaceutical drug because it is the active ingredient in Pyridorin, a drug designed to prevent the progression of diabetic nephropathy.
Status:
Possibly Marketed Outside US
Source:
WHO-ESSENTIAL MEDICINES LIST:6.5.5.1
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Suramin is an antiprotozoal and anthelmintic compound. It is indicated for the treatment of African trypanosomiasis (African sleeping sickness; trypanosome fever) and Onchocerciasis (river blindness). Additionally, suramin exhibits antineoplastic action. It was discovered that suramin produced dramatic, but transient, improvement of core symptoms of autism spectrum disorder.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Niridazole is used (but not officially recommended) for the treatment of schistosomiasis, dracunculiasis and tungiasis. The mode of action of niridazole is not fully understood. The major action of niridazole seems to be on the glycogen metabolism of the helminths. The drug also case structural damage to the reproductive system of female schistosomes. Another possible mechanism of action of niridazole involves the inhibition of DNA synthesis in schistosomes. It is metabolized in the liver. The most serious side effects were those connected with the nervous area (convulsion, hallucination, etc.).
Status:
Possibly Marketed Outside US
Source:
Apo-nitrazepam Tablets BP by Apotex Corporation [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nitrazepam (trade names: Alodorm, Apodorm, Arem, Mogadon, Nitrados, Nitrazadon, Nitrosun, Ormodon, Paxadorm, Remnos, and Somnite) is a hypnotic drug of the benzodiazepine class, indicated for the short-term relief of severe, disabling anxiety and insomnia. Nitrazepam has sedative and motor-impairing properties, as well as amnestic, anticonvulsant, and skeletal muscle relaxant effects. Nitrazepam is used to treat short-term sleeping problems (insomnia), namely difficulty falling asleep, frequent awakening, early awakening, or a combination of each. Nitrazepam is sometimes tried to treat epilepsy when other medications fail. It has been found to be more effective than clonazepam in the treatment of West syndrome, which is age-dependent epilepsy, affecting the very young. In uncontrolled studies, nitrazepam has shown effectiveness in infantile spasms and is sometimes considered when other anti-seizure drugs have failed. However, drowsiness, hypotonia, and most significantly tolerance to anti-seizure effects typically develop with long-term treatment, generally limiting Nitrazepam to acute seizure management. More common side effects may include: Central nervous system depression, including somnolence, dizziness, depressed mood, rage, violence, fatigue, ataxia, headache, vertigo, impairment of memory, impairment of motor functions, hangover feeling in the morning, slurred speech, decreased physical performance, numbed emotions, reduced alertness, muscle weakness, double vision, and inattention have been reported. Unpleasant dreams and rebound insomnia have also been reported. Nitrazepam is a long-acting benzodiazepine with an elimination half-life of 15–38 hours (mean elimination half-life 26 hours).
Status:
Possibly Marketed Outside US
Source:
UK NHS:Acetomenaphthone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Acetomenaphthane, A vitamin K analogue used to treat and prevent hypoprothrombinemia caused by vitamin K deficiency. Also called menadiol diacetate. Hypoprothrombinemia is a blood disorder in which a deficiency of prothrombin results in impaired blood clotting, leading to an increased physiological risk for bleeding, especially in the gastrointestinal system, cranial vault, and superficial integumentary system.
Status:
Possibly Marketed Outside US
Source:
Moclobemide by Aa Pharma Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Moclobemide ia an antidepressant that acts on the monoaminergic cerebral neurotransmitter system by reversibly inhibiting monoamine oxidase, primarily type A (RIMA). The metabolism of noradrenaline, dopamine and serotonin is thereby reduced, resulting in increased extracellular concentrations of these neurotransmitters. Increase in the level of serotonin is the most pronounced. Moclobemide administration also leads to increased monoamine receptor stimulation, reversal of reserpine induced behavioral effects, selective depression of the rapid eye movement (REM) sleep, down regulation of beta-adrenoceptors and increases in plasma prolactin and growth hormone levels. It reduces scopolamine-induced performance decrement and alcohol induced performance deficit which suggest a neuroprotective role. Moclobemide is indicated for the treatment of major depressive episodes.
Gentamicin C1 is a part of gentamicin C complex, containing gentamicin C1, gentamicin C1a, and gentamicin C2 which compose approximately 80% of gentamicin and have been found to have the highest antibacterial activity. Commercial gentamicin C is a mixture of gentamicin C1, C1a, and C2. Gentamicin C1 has a methyl group in the 6' position of the 2-amino-hexose ring and is N methylated at the same position. Gentamicin is a broad spectrum aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. Aminoglycosides like gentamicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically gentamicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. Gentamicin complex is used for treatment of serious infections caused by susceptible strains of the following microorganisms: P. aeruginosa, Proteus species (indole-positive and indole-negative), E. coli, Klebsiella-Enterobactor-Serratia species, Citrobacter species and Staphylococcus species (coagulase-positive and coagulase-negative).