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Bifonazole
Bifonazole (trade name Canespor among others) is an imidazole antifungal drug used in form of ointments. It was patented in 1974 and approved for medical use in 1983. There are also combinations with carbamide for the treatment of onychomycosis. Adverse effects The most common side effect is a burning sensation at the application site. Other reactions, such as itching, eczema or skin dryness, are rare. Bifonazole is a potent aromatase inhibitor ''in vitro''. Pharmacology Mechanism of action Bifonazole has a dual mode of action. It inhibits fungal ergosterol biosynthesis at two points, via transformation of 24-methylendihydrolanosterol to desmethylsterol, together with inhibition of HMG-CoA. This enables fungicidal properties against dermatophytes and distinguishes bifonazole from other antifungal drugs. Pharmacokinetics Six hours after application, bifonazole concentrations range from 1000 µg/ cm³ in the stratum corneum to 5 µg/cm³ in the papillary dermis The ...
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Imidazole
Imidazole (ImH) is an organic compound with the formula C3N2H4. It is a white or colourless solid that is soluble in water, producing a mildly alkaline solution. In chemistry, it is an aromatic heterocycle, classified as a diazole Diazole refers to either one of a pair of isomeric chemical compounds with molecular formula C3H4N2, having a five-membered ring consisting of three carbon atoms and two nitrogen atoms.
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Imidazole Antifungals
Imidazole (ImH) is an organic compound with the formula C3N2H4. It is a white or colourless solid that is soluble in water, producing a mildly alkaline solution. In chemistry, it is an aromatic heterocycle, classified as a diazole, and has non-adjacent nitrogen atoms in meta-substitution. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. This ring system is present in important biological building blocks, such as histidine and the related hormone histamine. Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam. When fused to a pyrimidine ring, it forms a purine, which is the most widely occurring nitrogen-containing heterocycle in nature. The name "imidazole" was coined in 1887 by the German chemist Arthur Rudolf Hantzsch (1857–1935). Structure and properties Imidazole is a planar 5-membered r ...
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Racemic Mixture
In chemistry, a racemic mixture, or racemate (), is one that has equal amounts of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as racemates. History The first known racemic mixture was racemic acid, which Louis Pasteur found to be a mixture of the two enantiomeric isomers of tartaric acid. He manually separated the crystals of a mixture by hand, starting from an aqueous solution of the sodium ammonium salt of racemate tartaric acid. Pasteur benefited from the fact that ammonium tartrate salt that gives enantiomeric crystals with distinct crystal forms (at 77 °F). Reasoning from the macroscopic scale down to the molecular, he reckoned that the molecules had to have non-superimposable mirror images. A sample with only a single enantiomer is an ''enantiomerically pure'' or ''enantiopure'' compound. Etymology From racemic acid found in grapes; from Latin ''racemus'', meani ...
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Aromatase Inhibitors
Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer. Aromatase is the enzyme that catalyzes a key aromatization step in the synthesis of estrogen. It converts the enone ring of androgen precursors such as testosterone, to a phenol, completing the synthesis of estrogen. As such, AIs are estrogen synthesis inhibitors. Because hormone-positive breast and ovarian cancers are dependent on estrogen for growth, AIs are taken to either block the production of estrogen or block the action of estrogen on receptors. Medical uses Cancer In contrast to premenopausal women, in whom most of the estrogen is produced in the ovaries, in postmenopausal women estrogen is mainly produced in peripheral tissues of the bo ...
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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 conjugated do ...
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Papillary Dermis
The dermis or corium is a layer of skin between the epidermis (with which it makes up the cutis) and subcutaneous tissues, that primarily consists of dense irregular connective tissue and cushions the body from stress and strain. It is divided into two layers, the superficial area adjacent to the epidermis called the papillary region and a deep thicker area known as the reticular dermis.James, William; Berger, Timothy; Elston, Dirk (2005). ''Andrews' Diseases of the Skin: Clinical Dermatology'' (10th ed.). Saunders. Pages 1, 11–12. . The dermis is tightly connected to the epidermis through a basement membrane. Structural components of the dermis are collagen, elastic fibers, and extrafibrillar matrix.Marks, James G; Miller, Jeffery (2006). ''Lookingbill and Marks' Principles of Dermatology'' (4th ed.). Elsevier Inc. Page 8–9. . It also contains mechanoreceptors that provide the sense of touch and thermoreceptors that provide the sense of heat. In addition, hair follicles, swe ...
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Stratum Corneum
The stratum corneum (Latin for 'horny layer') is the outermost layer of the epidermis. The human stratum corneum comprises several levels of flattened corneocytes that are divided into two layers: the ''stratum disjunctum'' and ''stratum compactum''. The skin's protective acid mantle and lipid barrier sit on top of the stratum disjunctum. The stratum disjunctum is the uppermost and loosest layer of skin. The stratum compactum is the comparatively deeper, more compacted and more cohesive part of the stratum corneum. The corneocytes of the stratum disjunctum are larger, more rigid and more hydrophobic than that of the stratum compactum. The stratum corneum is the dead tissue that performs protective and adaptive physiological functions including mechanical shear, impact resistance, water flux and hydration regulation, microbial proliferation and invasion regulation, initiation of inflammation through cytokine activation and dendritic cell activity, and selective permeability to exc ...
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Cubic Centimetre
A cubic centimetre (or cubic centimeter in US English) (SI unit symbol: cm3; non-SI abbreviations: cc and ccm) is a commonly used unit of volume that corresponds to the volume of a cube that measures 1 cm × 1 cm × 1 cm. One cubic centimetre corresponds to a volume of one millilitre. The mass of one cubic centimetre of water at 3.98 °C (the temperature at which it attains its maximum density) is almost equal to one gram. In internal combustion engines, "cc" refers to the total volume of its engine displacement in cubic centimetres. The displacement can be calculated using the formula :d = \times b^2 \times s \times n where is engine displacement, is the bore of the cylinders, is length of the stroke and is the number of cylinders. Conversions *1 millilitre = 1 cm3 *1 litre = 1000 cm3 *1 cubic inch = . Unicode character The "cubic centimetre" symbol is encoded by Unicode at code point . See also * Cubic inch The cubic inch (symb ...
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Microgram
In the metric system, a microgram or microgramme is a unit of mass equal to one millionth () of a gram. The unit symbol is μg according to the International System of Units (SI); the recommended symbol in the United States and United Kingdom when communicating medical information is mcg. In μg the prefix symbol for micro- is the Greek letter μ (mu). Abbreviation and symbol confusion When the Greek lowercase "μ" (mu) in the symbol μg is typographically unavailable, it is occasionally – although not properly – replaced by the Latin lowercase "u". The United States-based Institute for Safe Medication Practices (ISMP) and the U.S. Food and Drug Administration (FDA) recommend that the symbol μg should not be used when communicating medical information due to the risk that the prefix μ (micro-) might be misread as the prefix m (milli-), resulting in a thousandfold overdose. The ISMP recommends the non- SI symbol mcg instead. However, the abbreviation mcg is also the sym ...
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Dermatophyte
Dermatophyte (from Greek '' derma'' "skin" (GEN ''dermatos'') and ''phyton'' "plant") is a common label for a group of fungus of ''Arthrodermataceae'' that commonly causes skin disease in animals and humans. Traditionally, these anamorphic (asexual or imperfect fungi) mold genera are: ''Microsporum'', ''Epidermophyton'' and ''Trichophyton''. There are about 40 species in these three genera. Species capable of reproducing sexually belong in the teleomorphic genus Arthroderma, of the Ascomycota (see Teleomorph, anamorph and holomorph for more information on this type of fungal life cycle). As of 2019 a total of nine genera are identified and new phylogenetic taxonomy has been proposed. Dermatophytes cause infections of the skin, hair, and nails, obtaining nutrients from keratinized material. The organisms colonize the keratin tissues causing inflammation as the host responds to metabolic byproducts. Colonies of dermatophytes are usually restricted to the nonliving cornified laye ...
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