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

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Showing 51 - 60 of 106 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)

Rociverine is the antispasmodic agent with balanced neurotropic and myotropic activity. The muscle-relaxant activity of rociverine is achieved by inhibiting the availability of Ca2+ at contraction site and not through an antiphosphodiesterasic mechanism, which might explain the absence of muscle-relaxant effects on the smooth musculature of the blood vessels. Rociverine did not differ statistically from the reference antispasmodic drug hyoscine butylbromide in premedication for endoscopy of the upper gastro-intestinal tract. No adverse effects were noted. Intrapartum administration of rociverine to nulliparous women may help to reduce the duration of the first stage of labor in a context of uniform labor management. Orally administered rociverine produced a dose-related reversal of the reserpine-induced detrusor hyperreflexia in anaesthetized rats. In experimental models rociverine was more effective than flavoxate. These results point to the usefulness of rociverine in the treatment of urinary bladder motility disorders.
Status:
Possibly Marketed Outside US
Source:
Japan:Bisbentiamine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Bisbentiamine is an O-benzoyl thiamine disulfide or vitamin B1 disulfide derivative. Thiamine derivatives and thiamine-dependent enzymes are present in all cells of the body, thus a thiamine deficiency would seem to adversely affect all of the organ systems. Lipid-soluble thiamine precursors such as Bisbentiamine have a much higher bioavailability than genuine thiamine and therefore are more suitable for therapeutic purposes. It is also used as a dietary supplement.
Status:
Possibly Marketed Outside US
Source:
Japan:Nemonapride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Nemonapride, benzamide derivative (YM-09151-2) is essentially a typical antipsychotic drug, similar in structure to sulpiride. This drug was manufactured by Yamanouchi Pharmaceuticals and released in Japan. The mechanism of action of nemonapride is not proven, but its unique antipsychotic effect arises from its selective binding to the dopamine D2 receptor family. Since nemonapride has high affinity for D3 and D4 dopamine receptors, it is conceivable that its effect on negative symptoms might result from blockade of these receptors. Animal studies have suggested that nemonapride has pharmacological features that are different from those of typical neuroleptics. The low extrapyramidal side effect profile of nemonapride treatment appears to coincide with the characteristic features of another benzamide derivative, remoxipride.
Status:
Possibly Marketed Outside US
Source:
Japan:Pentetoreotide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Pentetic acid or diethylenetriaminepentaacetic acid (DTPA) is an aminopolycarboxylic acid consisting of a diethylenetriamine backbone with five carboxymethyl groups. The molecule can be viewed as an expanded version of EDTA and is used similarly. Pentetreotide is a modified DTPA attached to a peptide segment. Pentetreotide binds to somatostatin receptors on cell surfaces throughout the body. Indium 111 pentetreotide, is a diagnostic radiopharmaceutical.
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.
mixture
Status:
Possibly Marketed Outside US

Class:
MIXTURE

Actinomycin C is an antibiotic complex composed of actinomycin C1, C2 and C3 and produced by Streptomyces chrysomallus. Actinomycin C reversibly binds to DNA, interfering with the synthesis of RNA, prevention of RNA polymerase elongation and, consequently, with protein synthesis. Actinomycin C exert an inhibitory effect on gram-positive and gram-negative bacteria and on some fungi. However, the toxic properties of the Actinomycin C in relation to antibacterial activity is such as to preclude its use as antibiotics in the treatment of infectious diseases. Because Actinomycin C is cytotoxic, it has an antineoplastic effect which has been demonstrated in experimental animals with various types of tumor implant. This cytotoxic action is the basis for its use in the treatment of certain types of cancer.
Lypressin is synthetic analog of porcine antidiuretic hormone vasopressin. Itis a cyclic nonapeptide that differs from Arg-vasopressin by one amino acid, containing Lys at residue 8 instead of Arg. Lypressin-containing nasal spray was used to treat diabetes insipidus, but its marketing by Sandoz (Novartis) was discontinued.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Felypressin
Source URL:

Class:
PROTEIN


Conditions:

Felypressin is a non-catecholamine vasoconstrictor that is chemically related to vasopressin, the posterior pituitary hormone. Felypressin is added to some local anesthetics such as prilocaine in a concentration of 0.03 IU/ml. Its antidiuretic effects are less than those of vasopressin. Felypressin is used as a vasoconstrictor in local anesthetic injections for dental use and is an ingredient of preparations that have been used for the treatment of pain and inflammation of the mouth.
Enoxaparin is a low molecular weight heparin used as anticoagulant medication to treat and prevent deep vein thrombosis (DVT) and pulmonary embolism (PE) including during pregnancy and following certain types of surgery. Enoxaparin is a depolymerized derivative of Unfractionated heparin produced by controlled depolymerization using alkaline hydrolysis of the heparin benzylic ester. Like Unfractionated heparin, its major anticoagulant effect is mediated by interaction with antithrombin III, which in turn inactivates serine proteases like factors IIa (thrombin), IXa and Xa. Therefore, enoxaparin indirectly inhibits the conversion of prothrombin to thrombin and reduces the thrombin-mediated conversion of fibrinogen to fibrin, thus preventing clot formation. Among parenteral anticoagulants, enoxaparin stands out for certain major advantages: rapid onset of action, higher bioavailability, once- or twice-daily dosing that can be administered by patients at home without any need for monitoring, and no reported association with catheter thrombosis. Enoxaparin has been shown to be a safe and effective drug in a wide variety of thromboembolic conditions, and two decades of available data have undoubtedly inspired significant confidence. Although these properties make it a preferred option in a wide range of clinical disorders, lack of reliable antidote and accumulation in renal dysfunction are major concerns associated with its use, which are shared, apart from Unfractionated heparin, by most other available anticoagulants.
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.