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

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Showing 131 - 140 of 198 results

Micronomicin is a new aminoglycosidic antibiotic discovered and developed by Kyowa Hakko Kogyo Co., Ltd. It is produced by Micromonospora sagamiensis var. nonreducans. Investigation of micronomicin performed in 134 research facilities in Japan led to the following results. 1) Micronomicin showed a broad antibacterial spectrum against Gram positive and Gram negative bacteria. 2) In susceptibility tests of clinical isolates, micronomicin was almost similarly active to GM. 3) Bactericidal activity of micronomicin against Pseudomonas aeruginosa and E. coli was higher than those of TOB and DKB. 4) Micronomicin showed a synergistic antibacterial activity against Pseudomonas aeruginosa and E. coli with CBPC and SBPC. 5) The therapeutic activity of micronomicin in mice infected with Pseudomonas aeruginosa and Serratia sp. was in high correlation with in vitro antibacterial activity similarly to that of GM. Micronomicin (sold under the brand names Sagamicin and Luxomicina among others) is an aminoglycoside antibiotic, and like others in its class, binds to the ribosomes of non-resistant cells causing mistranscription of mRNA which fatally inhibits production of essential proteins. Micronomicin sulfate can inhibit bacterial protein synthesis, while destroy the bacterial cell wall. Micronomicin has an antibacterial activity against gram-negative and gram-positive bacteria such as Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, Shara, Escherichia coli, etc. Streptococcus pneumoniae and Pneumococcus are sensitive to it, but its activity on anaerobic bacteria and some hemolytic streptococcus is weak.
Status:
Possibly Marketed Outside US
Source:
Glaunorm by Rubitsov, M.V.|Muklina, E.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Aceclidine is a parasympathomimetic agent used in the treatment of open-angle glaucoma as topical eye drop solution. It is as a muscarinic acetylcholine receptor agonist with weak anticholinesterase activity. Acting directly on the motor end-plate (cholinergic nerve endings) it decreases intraocular pressure and mediates the contraction of iris muscle. Aceclidine increased outflow facility in human eyes in vitro by a direct stimulation of the outflow tissues in the absence of an intact ciliary muscle. This effect was biphasic, occurring at concentrations of 10 uM and lower with no effect at higher concentrations. Passed numerous clinical trials in Russia, France, Italy and other countries and was widely used in Europe but never been in clinical use in USA.
Dibrompropamidine isetionate is an antiseptic. Ointment containing dibrompropamidine isetionate is used to treat minor eye or eyelid infections, such as conjunctivitis and blepharitis.
Status:
Possibly Marketed Outside US
Source:
NCT01456780: Phase 4 Interventional Completed Meibomian Gland Dysfunction
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Loteprednol (as the ester loteprednol etabonate) is a corticosteroid used to treat inflammations of the eye. It is marketed by Bausch and Lomb as Lotemax. It is a topical corticoid anti-inflammatory. It is used in ophthalmic solution for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitis’s. Lotemax is less effective than prednisolone acetate 1% in two 28-day controlled clinical studies in acute anterior uveitis, where 72% of patients treated with Lotemax experienced resolution of anterior chamber cells, compared to 87% of patients treated with prednisolone acetate 1%. Lotemax is also indicated for the treatment of post-operative inflammation following ocular surgery. Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Corticosteroids are capable of producing a rise in intraocular pressure (IOP). Loteprednol etabonate is structurally similar to other corticosteroids. However, the number 20 position ketone group is absent. It is highly lipid soluble, which enhances its penetration into cells. Loteprednol etabonate is synthesized through structural modifications of prednisolone-related compounds so that it will undergo a predictable transformation to an inactive metabolite. Based upon in vivo and in vitro preclinical metabolism studies, loteprednol etabonate undergoes extensive metabolism to inactive carboxylic acid metabolites. Lotemax possesses some adverse reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Chloroprednisone is a glucocorticoid. The acetated ester prodrug was used as topical anti-inflammatory agent.
Clobetasone is a corticosteroid used in dermatology, for treating such skin inflammation as seen in eczema, psoriasis and other forms of dermatitis, and ophthalmology. Topical clobetasone butyrate has shown minimal suppression of the Hypothalamic-pituitary-adrenal axis. It is available as clobetasone butyrate under the brand names Eumosone or Eumovate both manufactured by GlaxoSmithKline. Trimovate also contains Oxytetracycline, an antibiotic, and nystatin, an antifungal. Clobetasone butyrate is classed as a moderately potent topical corticosteroid. Clobetasone butyrate relieves the symptoms of a flare-up by reducing inflammation, itching and redness. It is not a cure for the condition, but it will help to relieve the symptoms. Although less potent topical steriods are often preferred for use in children, a short course of clobetasone butyrate may be prescribed for a child with severe eczema on the arms or legs. Short courses of clobetasone butyrate may also be prescribed for the treatment of psoriasis for areas such as the face, or the inside of elbows and behind the knees. In ophthalmology, clobetasone butyrate 0.1% eye drops have been shown to be safe and effective in the treatment of dry eyes in Sjögren's Syndrome.
Status:
Possibly Marketed Outside US
Source:
BENTOS by Kakenyaku Kako
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Befunolol is a beta-adrenergic receptor blocker approved in Japan for the treatment of open-angle glaucoma. The current drug status is unknown.
Status:
Possibly Marketed Outside US
Source:
NCT00357019: Phase 4 Interventional Completed Keratoconjunctivitis, Vernal
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Spaglumic acid (NAAG) is the β-aspartyl isoform of N-Acetyl-l-aspartylglutamate (isospaglumic Acid is N-(N-Acetyl-l-α-aspartyl)-l-glutamic acid). In eye drops, spaglumic acid is either a magnesium or sodium salt of N-Acetyl-l-aspartylglutamate. Spaglumic acid is a mast cell stabilizer. Thus it is used in allergic conditions such as allergic conjunctivitis. Specifically spaglumic acid is approved in Portugal under the brand name Naabak and in Greece under the brand name Naaxia for use in patients with allergic conjunctivitis. Spaglumic Acid is a peptide neurotransmitter and the third-most-prevalent neurotransmitter in the mammalian nervous system. It is a weak activator of NMDA receptors and a highly selective agonist for mGlu3 receptors. Spaglumic Acid is neuroprotective under non-hydrolysing conditions in vivo.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Picloxydine is a heterocyclic biguanide with antibacterial and antiplaque activity. 0.4% Picloxydine produces a highly significant drop in the number of aerobic organisms. 0.4% Picloxydine is far more effective than 0.2% Picloxydine or chlorhexidine in reducing the total viable count of oral aerobic and anaerobic organisms. It is used to treat superficial eye infections. Picloxydine is also used in eye drops in the topical therapy of trachoma. This drug can cause side effects - local intolerance reactions (temporary irritation, allergic reactions).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Azidamfenicol is a semi-synthetic chloramphenicol in which the nitro moiety is replaced with a methylsulphone and the dichloroacetamide is replaced with azidoacetamide. Azidamfenicol is a broad spectrum antibiotic with good activity against Gram-negative and anaerobic bacteria.

Showing 131 - 140 of 198 results