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

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Showing 41 - 50 of 100 results

Status:
US Previously Marketed
First approved in 1974

Class (Stereo):
CHEMICAL (ABSOLUTE)


Isosorbide is an effective hyperosmotic agent which can be administered orally without gastrointestinal irritation. It is absorbed quantitatively and more than 95% of the administered dose is excreted unchanged in the urine. Oral administration of a 50% solution to rabbits or man results in prompt increases in osmolarity of the serum and profound decreases in intraocular pressure. The drug proves useful in acute primary and secondary glaucomas, and as preoperative medication for various surgical procedures including cataract extraction, retinal detachment, corneal transplant, and glaucoma operations.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

DIMETHYL ISOSORBIDE is an inactive component of VANOS® Cream indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses in patients 12 years of age or older.
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.

Class (Stereo):
CHEMICAL (ABSOLUTE)



Sertaconazole is a azole antifungal that is FDA approved for the treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by: Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum. Sertaconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Common adverse reactions include contact dermatitis, dry skin, burning skin and application site skin tenderness.

Class (Stereo):
CHEMICAL (RACEMIC)



Sertaconazole is a azole antifungal that is FDA approved for the treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by: Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum. Sertaconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Common adverse reactions include contact dermatitis, dry skin, burning skin and application site skin tenderness.
Sildenafil (Viagra, Revatio) is a PDE5 inhibitor which was approved by FDA for the treatment of erectile disfunction and adults with pulmonary arterial hypertension. Upon administration sildenafil inhibits PDE5 and results in elevated level of cyclic guanosine monophosphate and smooth muscle relaxation.
Latanoprostene Bunod (LBN) is a topical ophthalmic therapeutic for the reduction of intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. There is no cure for glaucoma and therapeutic management is predominantly focused on minimizing disease progression and clinical sequelae via the reduction and maintenance of appropriate target IOPs. Latanoprostene Bunod is thought to lower intraocular pressure via a dual mechanism of action since the medication is metabolized into two relevant moieties upon administration: latanoprost acid, and butanediol mononitrate. As a prostaglandin F2-alpha analog, the latanoprost acid moiety operates as a selective PGF2-alpha (FP) receptor agonist. Since FP receptors occur in the ciliary muscle, ciliary epithelium, and sclera the latanoprost acid moiety primarily acts in the uveoscleral pathway where it increases the expression of matrix metalloproteinases (MMPs) like MMP-1, -3, and -9 which promote the degradation of collagen types I, III, and IV in the longitudinal bundles of the ciliary muscle and surrounding sclera. The resultant extracellular matrix remodeling of the ciliary muscle consequently produces reduced outflow resistance via increased permeability and increased aqueous humor outflow through the uveoscleral route. Conversely, the butanediol mononitrate undergoes further metabolism to NO and an inactive 1,4-butanediol moiety. As a gas that can freely diffuse across plasma membranes, it is proposed that the relaxing effect of NO to induce reductions in the cell volume and contractility of vascular smooth muscle-like cells is dependent upon activation of the sGC/cGMP/PKG cascade pathway. NO released from butanediol mononitrate consequently enters the cells of the TM and an inner wall of SC, causing decreases in myosin light chain-2 phosphorylation, increased phosphorylation of large-conductance calcium-activated potassium (BKCa) channels, and a subsequent efflux of potassium ions through such BKCa channels. All of these changes serve to decrease the cell contractility and volume, as well as to rearrange the actin cytoskeleton of the TM and SC cells. These biomechanical changes ultimately allow for enhanced conventional outflow of aqueous humor.