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

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Showing 11 - 18 of 18 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

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.
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.
Pentaerythritol tetranitrate is an organic nitrate that has been used for the treatment of angina pectoris. Upon administration, the drug undergoes exstensive metabolism to NO which causes vasodilation and the relaxation of smooth muscle cells. The compound belongs to a familiy of explosive substances and may be used accordingly.
Pentaerythritol tetranitrate is an organic nitrate that has been used for the treatment of angina pectoris. Upon administration, the drug undergoes exstensive metabolism to NO which causes vasodilation and the relaxation of smooth muscle cells. The compound belongs to a familiy of explosive substances and may be used accordingly.
Status:
US Previously Marketed
Source:
VERA-TENSIL R-S POTASSIUM NITRATE by RICHLYN
(1961)
Source URL:
First marketed in 1921
Source:
Nitric Acid U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Nitrate ion (NO3 −) is found naturally in the environment and is an important plant nutrient. It is present at varying concentrations in all plants and is a part of the nitrogen cycle. Nitrate probably has a role in protecting the gastrointestinal tract against a variety of gastrointestinal pathogens, as nitrous oxide and acidified nitrite have antibacterial properties. Significant bacterial reduction of nitrate to nitrite does not normally take place in the stomach, except in individuals with low gastric acidity or with gastrointestinal infections. These may include individuals using antacids, particularly those that block acid secretion. Potassium nitrate is used as mild local desensitizer in toothpastes.

Showing 11 - 18 of 18 results