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Fungicidal, binds to ergosterol in fungal membrane, creates channel, 'leaky cell' Stored in body tissues, slowly elim in urine Tox: perm kidney damage in 80% given extensive doses, mycardial tox, hepatotox, CNS damage Use: systemic, rapidly growing fungal infections; fungal infection in immunocompromised
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Mech: fungal cytosine deaminase converts drug->5-FU->5FUTP+5-dFUMP. 5dFUMP inhib thymidylate synthetase->reduces dTTP and inhib fungal DNA synthesis Tox: hepato, bone marrow suppression, CNS effects-headache, euphoria, sedation
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Definition
Imidazole, anti fungal Mech: Inhib 14a demethylase, prevents ergosterol formation in fungal membrane=cidal Inhib steroid syn, decr aldosterone, cortisol, testosterone, estrogen; inhib TXA2-used for ARDS; incr bp and pulmonary edema Tox: N,V, altered steroid syn, CNS, photophobia
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Triazole, anti fungal broader than ketoconazole Inhib 14a demethylase converting lanosterol to ergosterol in fungal membrane-cidal Res. if given alone; given in combo Tox: NVD, headache, vertigo, allergy, hepato, teratogenesis
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Echinocandin, anti fungal Inhibits β(1,3)D glucan syn in fungal wall=cidal no effect on cytochrome P450, elim urine/bile Tox: N,V,D, fever, hypokalemia, anemia Combine w/ amphotericinB, fluconazole=additive or synergistic Treatment for Candida, Aspergillis, Histoplasma, Blastomyces, Coccidiodes, NOT Cryptococcus
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Definition
Antiparasitic, free radical generator Mech: anaerobic orgs have low redox potentiol req for reduction of nitro group->reactive intermediates disrupt NA and prot structure=cidal Used for oblig. anaer. bact and selected parasites Tox: CNS-ataxia, convlusions; +etoh=acetaldehyde poisoning (Antabuse), Candida superinfection, Immunosuppressive
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Definition
Antimalarial, free rad generator Mech: Blood schizonticide, inhib plasmodial heme polymerase->free rad gen by reactive Fe in heme Tx for prophylaxis and P. falciparum(+primaquine for hepatic P.vivax and P. ovale) Resistance widespread Tox: allergy, CNS, GI, retinopathy/ototox/myopathy(prolonged use); quinoline like on heart=decr conduction and excitability
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Definition
Antimalarial, free rad generator Inhib heme pol->cidal free rad generation hep metab, elim in bile Tox: Hepato, bone marrow suppression, psych, quinidine like effects on heart (slows conduction and excitibility)
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Definition
Antimalarial,parasitic, neoplastic; free rad gen Mech: int. endoperoxide bridge forms free rad interm. when cleaved by Plasmodium in presence of heme; free rad kill Plasmodium by arylation Tox: none; derivs cause neurotox, and heart Tx for combination chemo w/ mefloquine
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Definition
Atovaquone and Proguanil, antimalarial Mech: (Atov)-damage to plasmodial mitochondria; (Proguanil)-inhib of DHF Red Tox: Atov=N,V,D, headache, rash, incr liver enzymes; Proguanil=N,V,D, ab pain, hematuria
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