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Liranaftate
Liranaftate (trade name Zefnart) is a topical antifungal drug. It is used as a 2% cream used to treat tinea pedis (athlete's foot), tinea corporis (ringworm), and tinea cruris (jock itch). It was approved for use in Japan in August 2000. Liranaftate works by inhibiting the fungal enzyme squalene epoxidase that is necessary for the fungus to synthesize sterol Sterol is an organic compound with formula , whose molecule is derived from that of gonane by replacement of a hydrogen atom in position 3 by a hydroxyl group. It is therefore an alcohol of gonane. More generally, any compounds that contain the gon ...s which are essential for cell membrane integrity. References Thiocarbamates Antifungals Tetralins Pyridines Methoxy compounds {{antiinfective-drug-stub ...
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Topical Medication
A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes including creams, foams, gels, lotions, and ointments. Many topical medications are epicutaneous, meaning that they are applied directly to the skin. Topical medications may also be inhalational, such as asthma medications, or applied to the surface of tissues other than the skin, such as eye drops applied to the conjunctiva, or ear drops placed in the ear, or medications applied to the surface of a tooth. The word ''topical'' derives from Greek τοπικός ''topikos'', "of a place". Justification Topical drug delivery is a route of administering drugs via the skin to provide topical therapeutic effects. As skin is one of the largest and most superficial organs in the human body, pharmacists utilise it to deliver various dr ...
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Topical
A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes including creams, foams, gels, lotions, and ointments. Many topical medications are epicutaneous, meaning that they are applied directly to the skin. Topical medications may also be inhalational, such as asthma medications, or applied to the surface of tissues other than the skin, such as eye drops applied to the conjunctiva, or ear drops placed in the ear, or medications applied to the surface of a tooth. The word ''topical'' derives from Greek τοπικός ''topikos'', "of a place". Justification Topical drug delivery is a route of administering drugs via the skin to provide topical therapeutic effects. As skin is one of the largest and most superficial organs in the human body, pharmacists utilise it to deliver various dr ...
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Antifungal Drug
An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually yes obtained by a doctor's prescription, but a few are available over the counter (OTC). Types of antifungal There are two types of antifungals: local and systemic. Local antifungals are usually administered topically or vaginally, depending on the condition being treated. Systemic antifungals are administered orally or intravenously. Of the clinically employed azole antifungals, only a handful are used systemically. These include ketoconazole, itraconazole, fluconazole, fosfluconazole, voriconazole, posaconazole, and isavuconazole. Examples of non-azole systemic antifungals include griseofulvin and terbinafine. Classes Polyenes A polyene is a molecule with multiple ...
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Tinea Pedis
Dermatophytosis, also known as ringworm, is a fungal infection of the skin. Typically it results in a red, itchy, scaly, circular rash. Hair loss may occur in the area affected. Symptoms begin four to fourteen days after exposure. Multiple areas can be affected at a given time. About 40 types of fungus can cause ringworm. They are typically of the ''Trichophyton'', ''Microsporum'', or ''Epidermophyton'' type. Risk factors include using public showers, contact sports such as wrestling, excessive sweating, contact with animals, obesity, and poor immune function. Ringworm can spread from other animals or between people. Diagnosis is often based on the appearance and symptoms. It may be confirmed by either culturing or looking at a skin scraping under a microscope. Prevention is by keeping the skin dry, not walking barefoot in public, and not sharing personal items. Treatment is typically with antifungal creams such as clotrimazole or miconazole. If the scalp is involv ...
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Tinea Corporis
Tinea corporis is a fungal infection of the body, similar to other forms of tinea. Specifically, it is a type of dermatophytosis (or ringworm) that appears on the arms and legs, especially on glabrous skin; however, it may occur on any superficial part of the body. Signs and symptoms It may have a variety of appearances; most easily identifiable are the enlarging raised red rings with a central area of clearing (ringworm). The same appearances of ringworm may also occur on the scalp (tinea capitis), beard area (tinea barbae) or the groin (tinea cruris, known as jock itch or dhobi itch). Other classic features of tinea corporis include: * Itching occurs on infected area. * The edge of the rash appears elevated and is scaly to touch. * Sometimes the skin surrounding the rash may be dry and flaky. * Almost invariably, there will be hair loss in areas of the infection. Causes Tinea corporis is caused by a tiny fungus known as dermatophyte. These tiny organisms normally live on the su ...
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Tinea Cruris
Tinea cruris, also known as jock itch, is a common type of contagious, superficial fungal infection of the groin and buttocks region, which occurs predominantly but not exclusively in men and in hot-humid climates. Typically, over the upper inner thighs, there is an intensely itchy red raised rash with a scaly well-defined curved border. It is often associated with athletes foot and fungal nail infections, excessive sweating and sharing of infected towels or sports clothing. It is uncommon in children. Its appearance may be similar to some other rashes that occur in skin folds including candidal intertrigo, erythrasma, inverse psoriasis and seborrhoeic dermatitis. Tests may include microscopy and culture of skin scrapings. Treatment is with topical antifungal medications and is particularly effective if symptoms have recent onset. Prevention of recurrences include treating concurrent fungal infections and taking measures to avoid moisture build-up including keeping the groin re ...
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Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. Re ...
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Squalene Epoxidase
Squalene monooxygenase (also called squalene epoxidase) is a eukaryotic enzyme that uses NADPH and diatomic oxygen to oxidize squalene to 2,3-oxidosqualene (squalene epoxide). Squalene epoxidase catalyzes the first oxygenation step in sterol biosynthesis and is thought to be one of the rate-limiting enzymes in this pathway. In humans, squalene epoxidase is encoded by the ''SQLE'' gene. Several eukaryote genomes lack a squalene monooxygenase encoding gene, but instead encode an alternative squalene epoxidase that performs the same task. Mechanism The canonical squalene monooxygenase is a flavoprotein monooxygenase. Flavoprotein monooxygenase form flavin hydroperoxides at the enzyme active site, which then transfer the terminal oxygen atom of the hydroperoxide to the substrate. Squalene monooxygenase differs from other flavin monooxygenases in that the oxygen is inserted into the substrate as an epoxide rather than as a hydroxyl group. This enzyme contains a loosely bound ...
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Sterol
Sterol is an organic compound with formula , whose molecule is derived from that of gonane by replacement of a hydrogen atom in position 3 by a hydroxyl group. It is therefore an alcohol of gonane. More generally, any compounds that contain the gonane structure, additional functional groups, and/or modified ring systems derived from gonane are called steroids. Therefore, sterols are a subgroup of the steroids. They occur naturally in most eukaryotes, including plants, animals, and fungi, and can also be produced by some bacteria (however likely with different functions). The most familiar type of animal sterol is cholesterol, which is vital to cell membrane structure, and functions as a precursor to fat-soluble vitamins and steroid hormones. While technically alcohols, sterols are classified by biochemists as lipids ( fats in the broader sense of the term). Types Sterols of plants are called ''phytosterols'' and sterols of animals are called ''zoosterols''. The most impor ...
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Cell Membrane
The cell membrane (also known as the plasma membrane (PM) or cytoplasmic membrane, and historically referred to as the plasmalemma) is a biological membrane that separates and protects the interior of all cells from the outside environment (the extracellular space). The cell membrane consists of a lipid bilayer, made up of two layers of phospholipids with cholesterols (a lipid component) interspersed between them, maintaining appropriate membrane fluidity at various temperatures. The membrane also contains membrane proteins, including integral proteins that span the membrane and serve as membrane transporters, and peripheral proteins that loosely attach to the outer (peripheral) side of the cell membrane, acting as enzymes to facilitate interaction with the cell's environment. Glycolipids embedded in the outer lipid layer serve a similar purpose. The cell membrane controls the movement of substances in and out of cells and organelles, being selectively permeable to i ...
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Thiocarbamates
In organic chemistry, thiocarbamates (thiourethanes) are a family of organosulfur compounds. As the prefix ''thio-'' suggests, they are sulfur analogues of carbamates. There are two isomeric forms of thiocarbamates: ''O''-thiocarbamates, (esters), and ''S''-thiocarbamates, ( thioesters). Synthesis Thiocarbamates can be synthesised by the reaction of water or alcohols upon thiocyanates ( Riemschneider thiocarbamate synthesis): :RSCN + H2O → RSC(=O)NH2 :RSCN + R'OH → RSC(=O)NR'H Similar reactions are seen between alcohols and thiocarbamoyl chlorides such as dimethylthiocarbamoyl chloride; as well as between thiols and cyanates. Alternatively, they arise by the reaction of amines with carbonyl sulfide. :2 R2NH + COS → 2NH2+R2NCOS−] Reactions In the Newman-Kwart rearrangement ''O''-thiocarbamates can isomerise to ''S''-thiocarbamates. This reaction, which generally requires high temperatures, is an important method for the synthesis of thiophenols. Dithiocarbam ...
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Antifungals
An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually yes obtained by a doctor's prescription, but a few are available over the counter (OTC). Types of antifungal There are two types of antifungals: local and systemic. Local antifungals are usually administered topically or vaginally, depending on the condition being treated. Systemic antifungals are administered orally or intravenously. Of the clinically employed azole antifungals, only a handful are used systemically. These include ketoconazole, itraconazole, fluconazole, fosfluconazole, voriconazole, posaconazole, and isavuconazole. Examples of non-azole systemic antifungals include griseofulvin and terbinafine. Classes Polyenes A polyene is a molecule with multiple conjugat ...
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