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Echinocandin
Echinocandins are a class of antifungal drugs that inhibit the synthesis of β-glucan in the fungal cell wall via noncompetitive inhibition of the enzyme 1,3-β glucan synthase. The class has been dubbed the "penicillin of antifungals," along with the related papulacandins, as their mechanism of action resembles that of penicillin in bacteria. β-glucans are carbohydrate polymers that are cross-linked with other fungal cell wall components, the fungal equivalent to bacterial peptidoglycan. Caspofungin, micafungin, and anidulafungin are semisynthetic echinocandin derivatives with limited clinical use due to their solubility, antifungal spectrum, and pharmacokinetic properties. Medical uses Drugs and drug candidates in this class are fungicidal against some yeasts (most species of '' Candida'', but not '' Cryptococcus'', '' Trichosporon'', and '' Rhodotorula''). Echinocandins also have displayed activity against ''Candida'' biofilms, especially in synergistic activity with a ...
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Anidulafungin
Anidulafungin (INN) (sold under the brand name Eraxis among others, is a semisynthetic echinocandin used as an antifungal medication. It may also have application in treating invasive ''Aspergillus'' infection when used in combination with voriconazole. It is a member of the class of antifungal drugs known as the echinocandins; its mechanism of action is by inhibition of (1→3)-β-D-glucan synthase, an enzyme important to the synthesis of the fungal cell wall. It is on the World Health Organization's List of Essential Medicines. Indications * Candidemia and other forms of invasive ''Candida'' infections (intra-abdominal abscess and peritonitis) * Esophageal candidiasis Anidulafungin has not been studied in endocarditis, osteomyelitis, and meningitis due to ''Candida'', and has not been studied in sufficient numbers of neutropenic patients to determine efficacy in this group. Pharmacology Pharmacodynamics Anidulafungin significantly differs from other antifungals in that i ...
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Echinocandin B
Echinocandin B, a lipopeptide, is a naturally occurring cyclic hexapeptide with a Linoleic acid, linoleoyl side chain. It belongs to a class of Fungicide, antifungal agents called echinocandins, which inhibits the synthesis of glucan, a major component of the fungal cell wall, via noncompetitive inhibition of a crucial enzyme, 1,3-Beta-glucan synthase, β-(1→3)-D-glucan synthase. Echinocandin B is a fermentation product of ''Aspergillus nidulans'' and the closely related species, Aspergillus rugulosus, ''A. rugulosus''; discovered in 1974 in ''A. nidulans'' var. ''echinulatus'' strain A 32204 in Germany, it was the first of the echinocandin class of antifungals. Echinocandin B can undergo deacylation (removal of the lipid side chain) by the action of a deacylase enzyme from the filamentous bacterium ''Actinoplanes utahensis'', which catalyzes the cleavage of the linoleoyl side chain; in three subsequent synthetic steps, including a chemical reacylation, the antifungal drug anidul ...
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Micafungin
Micafungin, sold under the brand name Mycamine, is an echinocandin antifungal medication used to treat and prevent invasive fungal infections including candidemia, abscesses, and esophageal candidiasis. It inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls that is not found in mammals. Administered intravenously, Micafungin received final approval from the U.S. Food and Drug Administration (FDA) in March 2005, and gained approval in the European Union in April 2008. It is on the '' World Health Organization's List of Essential Medicines''. In August 2023, Mycamine was acquired from Astellas Pharma by Sandoz. Indications Micafungin is indicated for the treatment of candidemia, acute disseminated candidiasis, ''Candida'' peritonitis, abscesses and esophageal candidiasis. Micafungin works by way of concentration-dependent inhibition of 1,3-beta-D-glucan synthase resulting in reduced formation of 1,3-beta-D-glucan, which is an esse ...
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Caspofungin
Caspofungin ( INN; brand name Cancidas) is a lipopeptide antifungal drug from Merck & Co., Inc. It is a member of a class of antifungals termed the echinocandins. It works by inhibiting the enzyme (1→3)-β-D-glucan synthase and thereby disturbing the integrity of the fungal cell wall. Caspofungin was the first inhibitor of fungal (1→3)-β-D-glucan synthesis to be approved by the United States Food and Drug Administration. Caspofungin is administered intravenously. It is on the World Health Organization's List of Essential Medicines. Medical uses Caspofungin acetate for injection was initially approved by both the US Food and Drug Administration (FDA), and the European Medicines Agency (EMA) in 2001. Its approved therapeutic indications by both organizations include the empirical therapy of presumed fungal infections in febrile, neutropenic adults and for salvage therapy in people treatment of invasive aspergillosis in adults whose disease is refractory to, or who ar ...
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Antimicrobial Resistance
Antimicrobial resistance (AMR or AR) occurs when microbes evolve mechanisms that protect them from antimicrobials, which are drugs used to treat infections. This resistance affects all classes of microbes, including bacteria (antibiotic resistance), viruses (antiviral resistance), Parasitic disease, parasites (antiparasitic resistance), and fungi (antifungal resistance). Together, these adaptations fall under the AMR umbrella, posing significant challenges to healthcare worldwide. Misuse and improper management of antimicrobials are primary drivers of this resistance, though it can also occur naturally through genetic mutations and the spread of resistant genes. Antibiotic resistance, a significant AMR subset, enables bacteria to survive antibiotic treatment, complicating infection management and treatment options. Resistance arises through spontaneous mutation, horizontal gene transfer, and increased selective pressure from Antibiotic misuse, antibiotic overuse, both in medicin ...
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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 obtained by a doctor's prescription, but a few are available over the counter (OTC). The evolution of antifungal resistance is a growing threat to health globally. Routes of administration Ocular Indicated when the fungal infection is located in the eye. There is currently only one ocular antifungal available: natamycin. However, various other antifungal agents could be compounded in this formulation. Intrathecal Used occasionally when there's an infection of the central nervous system and other systemic options cannot reach the concentration required in that region for therapeutic benefit. Example(s): amphotericin B. Vaginal This may be used to treat some fungal inf ...
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Ciclosporin
Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. It is taken Oral administration, orally or intravenously for rheumatoid arthritis, psoriasis, Crohn's disease, nephrotic syndrome, eczema, and in organ transplants to prevent transplant rejection, rejection. It is also used as eye drops for keratoconjunctivitis sicca (dry eyes). Common side effects include high blood pressure, headache, kidney problems, increased hair growth, and vomiting. Other severe side effects include an increased risk of infection, liver problems, and an increased risk of lymphoma. Blood levels of the medication should be checked to decrease the risk of side effects. Use during pregnancy may result in preterm birth; however, ciclosporin does not appear to cause birth defects. Ciclosporin is believed to work by decreasing the function of lymphocytes. It does this by forming a complex with cyclophilin to block the phosphatase act ...
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Sirolimus
Sirolimus, also known as rapamycin and sold under the brand name Rapamune among others, is a macrolide compound that is used to coat coronary stents, prevent organ transplant rejection, treat a rare lung disease called lymphangioleiomyomatosis, and treat perivascular epithelioid cell tumour (PEComa). It has immunosuppressant functions in humans and is especially useful in preventing the rejection of kidney transplants. It is a mammalian target of rapamycin (mTOR) kinase inhibitor that reduces the sensitivity of T cells and B cells to interleukin-2 (IL-2), inhibiting their activity. This compound also has a use in cardiovascular drug-eluting stent technologies to inhibit restenosis. It is produced by the bacterium '' Streptomyces hygroscopicus'' and was isolated for the first time in 1972, from samples of ''Streptomyces hygroscopicus'' found on Easter Island. The compound was originally named rapamycin after the native name of the island, Rapa Nui. Sirolimus was initially deve ...
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Rhizopus
''Rhizopus'' is a genus of common saprophytic fungi on plants and specialized parasites on animals. They are found in a wide variety of organic substances, including "mature fruits and vegetables", jellies, syrups, leather, bread, peanuts, and tobacco. They are multicellular. Some ''Rhizopus'' species are opportunistic human pathogens that often cause fatal disease called mucormycosis. This widespread genus includes at least eight species. ''Rhizopus'' species grow as filamentous, branching hyphae that generally lack cross-walls (i.e., they are coenocytic). They reproduce by forming asexual and sexual spores. In asexual reproduction, spores are produced inside a spherical structure, the sporangium. Sporangia are supported by a large apophysate columella atop a long stalk, the sporangiophore. Sporangiophores arise among distinctive, root-like rhizoids. In sexual reproduction, a dark zygospore is produced at the point where two compatible mycelia fuse. Upon germination, a zygosp ...
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Phlebitis
Phlebitis (or venitis) is inflammation of a vein, usually in the legs. It most commonly occurs in superficial veins. Phlebitis often occurs in conjunction with thrombosis (clotting inside blood vessels) and is then called thrombophlebitis or superficial thrombophlebitis. Unlike deep vein thrombosis, the probability that superficial thrombophlebitis will cause a clot to break up and be transported in pieces to the lung is very low. Signs and symptoms * Localized redness and swelling * Pain or burning along the length of the vein * Vein being hard and cord-like There is usually a slow onset of a tender red area along the superficial veins on the skin. A long, thin red area may be seen as the inflammation follows a superficial vein. This area may feel hard, warm, and tender. The skin around the vein may be itchy and swollen. The area may begin to throb or burn. Symptoms may be worse when the leg is lowered, especially when first getting out of bed in the morning. A low-grade ...
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Tacrolimus
Tacrolimus, sold under the brand name Prograf among others, is an immunosuppressive drug. After Allotransplantation, allogenic organ transplant, the risk of organ Transplant rejection, rejection is moderate. To lower the risk of organ rejection, tacrolimus is given. The drug can also be sold as a topical medication in the treatment of T cell-mediated diseases such as atopic dermatitis, eczema and psoriasis. For example, it is prescribed for severe refractory uveitis after a bone marrow transplant, exacerbations of minimal change disease, Kimura's disease, and vitiligo. It can be used to treat Dry eye syndrome#Other, dry eye syndrome in cats and dogs. Tacrolimus inhibits calcineurin, which is involved in the production of interleukin-2, a molecule that promotes the development and cell proliferation, proliferation of T cells, as part of the body's learned (or adaptive immune response, adaptive) immune response. Chemically, it is a macrolide lactone that was first discovered in ...
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Voriconazole
Voriconazole, sold under the brand name Vfend among others, is an antifungal medication used to treat a number of fungal infections. This includes aspergillosis, candidiasis, coccidioidomycosis, histoplasmosis, penicilliosis, and infections by '' Scedosporium'' or ''Fusarium''. It can be taken by mouth or used by injection into a vein. Common side effects include vision problems, nausea, abdominal pain, rash, headache, and seeing or hearing things that are not present. Use during pregnancy may result in harm to the baby. It is in the triazole family of medications. It works by affecting fungal metabolism and fungal cell membranes. Voriconazole was patented in 1990 and approved for medical use in the United States in 2002. It is on the World Health Organization's List of Essential Medicines. Medical uses Voriconazole is used to treat invasive aspergillosis and candidiasis and fungal infections caused by '' Scedosporium'' and ''Fusarium'' species, which may occur in immunoc ...
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