topically

Triamcinolone acetonide (Azmacort) is a Corticosteroid. The mechanism of action of triamcinolone acetonide is as a Corticosteroid Hormone Receptor Agonist. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.

Camphor (2-Camphanone) is a bicyclic monoterpene ketone found widely in plants, especially CINNAMOMUM CAMPHORA. It is used topically as a skin antipruritic and as an anti-infective agent.

Algestone acetophenide (Neolutin) is progesterone that used in estrus synchronization and has been evaluated as an injectable contraceptive in combination with estradiol enanthate. It is also used therapeutically as a topical anti-inflammatory and is applied topically in the therapy of ACNE.

Lonapalene (RS4317) is a 5-lipoxygenase (5-LO) inhibitor with anti-psoriasis efficacy.Lonapalene topically blocks skin inflammation.

Hexylresorcinol (4-Hexylresorcinol) is a substituted dihydroxybenzene used topically as an antiseptic for the treatment of minor skin infections.

Miconazole (R18134) is an imidazole antifungal agent that is used topically and by intravenous infusion.

Promestriene (3-propyl ethyl) (INN) is a synthetic estrogen and glucocorticoid used topically in a 1% cream formulation. It is described as a tropic agent and antiseborrheic.

PGF2α isopropyl ester is an ester prodrug of PGF2α with enhanced lipid solubility. Due to better membrane penetration, PGF2α isopropyl ester is more suitable than PGF2α or PGF2α tromethamine salt for topical application in studies on intraocular pressure. The ester functionality is readily hydrolyzed in vivo to release the active compound PGF2α. When administered topically to the eyes of cynomolgus monkeys, a 5 μg dose reduces intraocular pressure by 68% after the fourth day of treatment.

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

Dichlorphenamide-13C6is intended for use as an internal standard for the quantification of dichlorphenamide by GC- or LC-MS. Dichlorphenamide is a sulfonamide and an orally bioavailable carbonic anhydrase (CA) inhibitor (Kis = 1.20, 38, 50, and 50 nM for the human CA isoforms CAI, CAII, CAIX, and CAXII, respectively).1It lowers intraocular pressure in rabbits when 50 μl of a 10% solution is applied topically to the eye.2Dichlorphenamide rescues the potassium deficiency and prevents insulin-induced paralysis in a rat model of familial hypokalemic periodic paralysis when administered at a dose of 5.6 mg/kg per day for ten days.3Formulations containing dichlorphenamide have been used in the treatment of glaucoma and primary periodic paralysis.

Sulfacetamide sodium (Sulamyd sodium) is an anti-infective agent. It is used topically to treat orally for urinary tract infections and skin infections.

Candicidin is an antifungal heptaene macrolides from Streptomyces griseus or Actinomyces levoris used topically in candidiasis. The antibiotic is composed of candicidins A, B, C, and D, of which D is the major component.

Tetracaine hydrochloride (Amethocalne HCl) (Pontocaine), a potent local anaesthetic, is a channel function allosteric inhibitor. It is primarily used as an antipruritic and topically in ophthalmology, and it has been used for surface and spinal anesthesia.

Meclocycline sulfosalicylate salt (Mecloderm), a tetracycline antibiotic, is used topically (i.e. for skin infections) as it is totally insoluble in water and may damage kidney and liver if given systemically.

KAA-276 HCl is the salt form of KAA-276 free base, a novel potent and long-lasting histamine HI-receptor antagonist with less-topical irritation, and can be topically administered by inhalation for the treatment of bronchial asthma.

Imiquimod maleate is an immune response modifier. It acts as a toll-like receptor 7 agonists and is commonly used topically to treat warts on the skin of the genital and anal areas.

KAA-276 free base is a novel potent and long-lasting histamine HI-receptor antagonist with less-topical irritation, and can be topically administered by inhalation for the treatment of bronchial asthma.

Levobunolol is a nonselective beta-blocker. It is used topically to treat glaucoma.

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.

Triamcinolone acetonide-d6 is a deuterated compound of Triamcinolone acetonide. Triamcinolone acetonide has a CAS number of 76-25-5. Triamcinolone acetonide is a Corticosteroid. The mechanism of action of triamcinolone acetonide is as a Corticosteroid Hormone Receptor Agonist. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.

Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when used topically. fluocortin butyl ester appears to be an effective, well-tolerated topical steroid that can be used in studies of perennial rhinitis.

Bimatoprost grenod(15-(6-nitroxyhexanoyl)-17-phenyl trinor PGF2α) is a nitric oxide-donating derivative of 17-phenyl trinor PGF2α.1It increases cGMP levels in rabbit aqueous humor and iris ciliary body when topically administered at a concentration of 0.042%. Topical administration of 15-(6-nitroxylhexanoyl)-17-phenyl trinor PGF2α(0.14%) reduces intraocular hypertension (IOP) in a rabbit model of hypertonic saline-induced transient ocular pressure. It also reduces IOP in a cynomolgus monkey model of laser-induced ocular hypertension when administered topically at a concentration of 0.042%.

5(Z),11(Z),14(Z)-Eicosatrienoic acid is a polyunsaturated fatty acid found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. 5(Z),11(Z),14(Z)-Eicosatrienoic acid methyl ester, when topically applied, reduces inflammatory processes, potentially by displacing arachidonic acid from phospholipid pools and reducing downstream inflammatory products such as prostaglandin E2 and leukotrienes.

1-Docosanol (Behenic alcohol) is a saturated 22-carbon aliphatic alcohol with antiviral activity. 1-Docosanol has a distinct mechanism of action and inhibits fusion between the plasma membrane and the herpes simplex virus envelope, thereby preventing viral entry into cells and subsequent viral activity and replication. 1-Docosanol is used topically in the treatment of recurrent herpes simplex labialis episodes and relieves associated pain and may help heal sores faster.

Demecarium Free Base is a quaternary ammonium compound that serves as a long-acting cholinesterase inhibitor with parasympathomimetic activity. When used topically, demecarium inactivates both pseudocholinesterase and acetylcholinesterase, thereby preventing acetylcholine breakdown and increasing acetylcholine activity.

Hydrocortamate Hydrochloride is a synthetic glucocorticoid that has anti-inflammatory and immunosuppressive properties. It is used topically to treat inflammation caused by corticosteroid-responsive skin diseases.

Tiger17, a cyclic peptide derivative of tigerinin-RC1 and tigerinin-RC2—antimicrobial peptides from the crab-eating frog (F. cancrivora) skin secretions—enhances HaCaT keratinocytes and human skin fibroblasts proliferation at 5 to 20 µg/ml concentrations, and promotes HaCaT cell migration at 20 µg/ml. Additionally, Tiger17 augments RAW 264.7 macrophages' recruitment and secretion of TGF-β1 and IL-6. When topically applied at 20 µg/ml, it accelerates wound closure and re-epithelialization in a mouse model of full-thickness dermal wounds.

Diflucortolone valerate (Diflucortolone 21-valerate) is a corticosteroid esterified with valeric acid. It helps to reduce itching, redness, and swelling.

Fluocinolone Acetonide (Flucort-N) is a glucocorticoid derivative used topically in the treatment of various skin disorders. It is usually employed as a cream, gel, lotion, or ointment. It has also been used topically in the treatment of inflammatory eye, ear, and nose disorders.

Aftobetin, also known as ANCA11 and NCE-11, is a novel amyloid–binding compound applied topically in the form of an ophthalmic ointment. Aftobetin may be of useful as an aid in the diagnosis Alzheimer's disease.

10-Undecenoic acid zinc salt (Zinc undecylenate), a synthetic or natural fungistatic fatty acid, is used topically in creams against eczemas, fungal infections, ringworm, and other cutaneous conditions. The zinc offers an astringent action.

D-Panthenol (D-Pantothenyl alcohol) is an alcoholic analogue of D-pantothenic acid and cholinergic agent. D-Panthenol acts as a precursor of coenzyme A necessary for acetylation reactions and is involved in the synthesis of acetylcholine. Although the exact mechanism of the actions of D-Panthenol is unclear, it may enhance the effect of acetylcholine. D-Panthenol acts on the gastrointestinal tract and increases lower intestinal motility. It is also applied topically to the skin to relieve itching and to promote healing.

GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from thesn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.1CAY10641 is an inactive alcohol derivative of a highly potent (IC50= 12 nM) cPLA2α inhibitor.2The parent compound demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.2CAY10641 is rapidly cleared from the blood stream (only 0.5 μg/ml remains 30 minutes after 10 mg/kg intravenous administration to mice).2However, no other biological effects have been reported. 1.Schaloske, R.H., and Dennis, E.A.The phospholipase A2 superfamily and its group numbering systemBiochemica et Biophysica Acta17611246-1259(2006) 2.Drews, A., Bovens, S., Roebrock, K., et al.1-(5-carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α with reduced lipophilicity: Synthesis, biological activity, metabolic stability, solubility, bioavailability, and topical in vivo activityJournal of Medicinal Chemistry535165-5178(2010)

Ethacridine lactate hydrate is a topically applied anti-infective agent.

Sulfiram is an ectoparasiticide and is a drug applied topically to treat scabies.

Mazipredone is a water-soluble, long-acting prednisolone derivative used topically for skin conditions & parenterally as a glucocorticoid.

Unoprostone is a prostaglandin F2α analogs (PGAs), and reduces intraocular pressure and is used topically for glaucoma or ocular hypertension.