Something: The antimicrobial drug imidazole inhibits sterol synthesis
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| The antimicrobial drug imidazole inhibits sterol synthesis | Apr 11, · This drug is a hypoxanthine analogue and acts as an alternative substrate of the T. cruzi hypoxanthine-guanine phosphoribosyltransferase. The enzyme can incorporate allopurinol into parasite RNA, creating a nonfunctional nucleotide, blocking de novo synthesis of purines, affecting protein synthesis, and inducing parasite death. Studies. 16 hours ago · Shweta Srivastava, Neha Shree Maurya, Shikha Kushwah and Ashutosh Mani*Article: Full Text. 1 day ago · Manifestation symptoms of hematologic toxicity and neurotoxicity aplastic from SCIENCE at San Jose State University. |
| Geography theme place | Apr 11, · This drug is a hypoxanthine analogue and acts as an alternative substrate of the T. cruzi hypoxanthine-guanine phosphoribosyltransferase. The enzyme can incorporate allopurinol into parasite RNA, creating a nonfunctional nucleotide, blocking de novo synthesis of purines, affecting protein synthesis, and inducing parasite death. Studies. 7 hours ago · Microbiology: An Introduction Plus Mastering Microbiology 13th Edition Test Bank / A Complete Test Bank for Microbiology: An Introduction Plus Mastering Microbiology 13th Edition This is a Microbiology: An Introduction Plus Mastering Microbiology 13th Edition Test Bank. This is not the textbook. A Test Bank is a collection of exam questions with solutions based on the textbook. . 16 hours ago · Shweta Srivastava, Neha Shree Maurya, Shikha Kushwah and Ashutosh Mani*Article: Full Text. |
| The antimicrobial drug imidazole inhibits sterol synthesis | 914 |
Imidazoles may have antibacterial, antifungal, antiprotozoal, and anthelmintic activity. Several distinct phenylimidazoles are therapeutically useful antifungal agents with wide spectra against yeasts and filamentous fungi responsible for either superficial or systemic infections.
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The anthelmintic thiabendazole is synthesls an imidazole with antifungal properties. Clotrimazolemiconazoleeconazoleketoconazoleitraconazoleand fluconazole are the most clinically important members of this group.
Posaconazole and voriconazole are among the newer drugs; voriconazole is approved for use in people to treat aspergillosis. Imidazoles generally are poorly soluble in water but can be dissolved in organic solvents such as chloroform, propylene health effects of uranium mining, and polyethoxylated castor oil preparation for IV use imidazzole dangerous in dogs.
An exception is fluconazole. Imidazoles are weak dibasic agents. Alterations in side-chain structure determine antifungal activity as well as the degree of toxicity. Imidazoles alter the cell membrane the antimicrobial drug imidazole inhibits sterol synthesis of susceptible the antimicrobial drug imidazole inhibits sterol synthesis and fungi by blocking the synthesis of ergosterol demethylation of lanosterol is inhibitedthe primary cell sterol of fungi.
The enzyme targeted is a fungal cytochrome P CYP Other enzyme systems are also impaired, such as those required for fatty acid synthesis. Because of the drug-induced changes of oxidative and peroxidative enzyme activities, toxic concentrations of hydrogen peroxide develop intracellularly. The overall effect is cell membrane and internal organelle disruption and cell death. The cholesterol in host cells is not affected by the imidazoles, although some drugs impair synthesis of selected steroids and drug-metabolizing enzymes in the host. Because imidazoles impair synthesis, a lag time to efficacy occurs. This lag time may be prolonged because of the long half-life of these drugs. Sensitivity to the imidazoles varies greatly between various strains of yeasts steeol fungi, but neither natural nor acquired resistance appears to be prevalent.
The antifungal imidazoles also have some antibacterial action but are rarely used for this purpose. Miconazole has a wide antifungal spectrum against most fungi and yeasts of veterinary interest. Sensitive organisms include Blastomyces dermatitidisParacoccidioides brasiliensisHistoplasma capsulatumCandida spp, Coccidioides immitisCryptococcus neoformansand Aspergillus fumigatus. Some Aspergillus and Madurella spp are only marginally sensitive.
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Ketoconazole has an antifungal spectrum similar to that of miconazolebut it is more effective against C immitis and some other yeasts and fungi. Itraconazole and fluconazole are the most active of the antifungal imidazoles. Their spectrum includes dimorphic fungal organisms and dermatophytes.
Clotrimazole and econazole are used for superficial mycoses dermatophytosis and candidiasis ; econazole also has been used for oculomycosis. Thiabendazole is effective against Aspergillus and Penicillium spp, but its use has largely been replaced by the more effective imidazoles. Voriconazole is approved for human use in treatment of Aspergillus but is effective against many other fungal organisms. Posaconazole may be more effective than itraconazole or fluconazole but may be associated with more adverse effects. The imidazoles are rapidly but sometimes erratically absorbed from the GI tract; plasma levels peak within 2 hr after administration PO.
Except for fluconazolean acidic environment is required for dissolution of the imidazoles, and a decrease in gastric acidity can reduce bioavailability after administration PO. The rate of absorption appears to be increased when the drug is given with meals, but reports are conflicting.
Because oral bioavailability can be very poor with noncommercial imidazole products, caution is recommended with compounded products, and monitoring is recommended if a compounded preparation is used. Imidazoles appear to be widely distributed in the body, with detectable concentrations in saliva, milk, and cerumen. The highest concentrations of imidazoles are found in the liver, adrenal glands, lungs, and kidneys. Hepatic metabolism is the article source route of the antimicrobial drug imidazole inhibits sterol synthesis. Metabolism of ketoconazole and most other imidazoles by oxidative pathways is extensive.
Itraconazole is metabolized to an active metabolite that may contribute significantly to antimicrobial activity.]
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