topical

Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride (Proparacaine HCl) stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, and resulting in a loss of sensation.

Betamethasone valerate (Luxiq) is a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions.

(Rac)-MGV354 (MGV354) is the racemate of MGV354. MGV354 is a soluble activator of guanylate cyclase (sGC)(EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively).

Taraxasterol acetate has anti-inflammatory activity in bino rats against carrageenan, formaldehyde and adjuvant induced inflammations. Taraxasterol acetate also displays potential antibacterial activities.

Topterone (Win 17,665) is a potent topical antiandrogen that inhibits the stimulation of lumbar organ development by testosterone and dihydrotestosterone in castrated immature male hamsters.

Omidenepag isopropyl (DE-117) is a selective prostaglandin EP2 receptor agonist and a novel topical ocular blood pressure lowering compound.Omidenepag isopropyl has a weak affinity for EP1, EP2, and FP receptors.Omidenepag isopropyl is used in studies of glaucoma and hypertension. Omidenepag isopropyl can be used to study glaucoma and hypertension.

Efletirizine (UCB-28754) is a histamine receptor antagonist with inhibitory effects on the enzyme 5-lipoxygenase (5-LO), and is useful in the topical treatment of allergic diseases.

Ticolubant is orally active leukotriene B4 antagonist with high affinity for the human neutrophil LTB4 receptor (Ki = 0.78 nM), blocks LTB4-induced Ca2+ migration with an IC50 of 6.6 ± 1.5 nM, and shows topical anti-inflammatory activity in a mouse model of skin inflammation.

Safotibant (LF-22-0542) is a bradykinin B1 receptor antagonist with anti-inflammatory and analgesic activity for the topical treatment of diabetic macular edema.

Tanimilast (CHF-6001) is a novel, potent, and selective phosphodiesterase 4 inhibitor with an IC50 value of 0.026 ± 0.006 nM. It exhibits potent anti-inflammatory activity and is indicated for topical use in the lungs. Tanimilast was studied for its effects on obstructive lung disease.

Halcinonide (Halciderm), a high-efficiency corticosteroid, is served as an anti-inflammatory agent used in topical preparations.

Crotamiton (Eurax) is an antipruritic and a scabicidal agent available as a lotion or cream for topical use only. It is a colorless to slightly yellowish oil with a faint amine-like odor. It is miscible with methanol and with alcohol.

Phthalylsulfacetamide (Tamid) is a sulfonamide antibiotic used for topical application to the skin and the conjunctiva.

Econazole ((±)-Econazol) is an imidazole derivative that is commonly used as a topical antifungal agent.

Pramocaine hydrochloride (Pramoxine HCl), a topical anesthetic, is served as an antipruritic.

Chloroxine (Capitrol) is a synthetic quinoline derivative with antibacterial activity. Although the mechanism of action is not fully understood, topical administration of chloroxine diminishes mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp, including psoriasis and eczema.

Diiodohydroxyquinoline (Iodoquinol), a topical therapeutic agent, has satisfactory antibacterial properties.

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

Felbinac (Dapson), a topical medicine, is an active metabolite of fenbufen. It is belonging to the family of medicines known as non-steroidal anti-inflammatory drugs (NSAIDs) of the arylpropionic acid class, which is used to treat muscle arthritis and inflammation.

Nitrofurazone (Nitrofural; Furacilin) is an orally active nitroaromatic broad-spectrum antibiotic with activity against both Gram-positive and Gram-negative bacteria. It is commonly used for establishing breast cancer models.

Sulfabenzamide (N-Sulfanilylbenzamide) is a sulfonamide antibacterial agent used alone or with sulfathiazole and sulfacetamide as a topical, intravaginal antibacterial preparation.

Chlorhexidine (Rotersept) is a biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram-positive bacteria are more negatively charged, they are more sensitive to this agent.

Chlorhexidine diacetate (Bactigras) is a disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.

Mafenide hydrochloride (4-Aminomethylbenzenesulfonamide hydrochloride) is a sulfonamide that inhibits the enzyme carbonic anhydrase and is used as topical anti-infective, especially in burn therapy.