Antifungal agents macrolide

Cisapride 10 mg t.i.d. 20 mg q.i.d. 5% 100% 100% 50%- 75% Avoid with azole antifungal agents, macrolide antibiotics, and other P450 3A-4 inhibitors... 

Patients allergic to penicillin may be cross-sensitive to cephalosporins. Cephalosporins (cefaclor, first-generation cephalosporin) are therefore avoided in these patients and instead macrolides (for example, erythromycin) are generally administered. Ketoconazole is an imidazole antifungal agent. 

A4 inhibitors - Patients receiving cytochrome P450 3A4 inhibitors, such as macrolide antibiotics (erythromycin and clarithromycin), antifungal agents (ketoconazole, itraconazole, and miconazole), or cyclosporine or vinblastine should not receive doses of tolterodine greater than 1 mg twice/day (greater than 2 mg/day for ER capsules). 

Drugs that may interact with rifabutin include the following Anticoagulants, azole antifungal agents, benzodiazepines, beta blockers, buspirone, corticosteroids, cyclosporine, delavirdine, doxycycline, hydantoins, indinavir, rifamycins, losartan, macrolide antibiotics, methadone, morphine, nelfinavir, quinine, quinidine, theophylline, aminophylline, tricyclic antidepressants, and zolpidem. 

Inhibitors of the CYP3A4 isoenzyme could increase systemic dofetilide exposure. Inhibitors of this isoenzyme (e.g., macrolide antibiotics, azole antifungal agents, protease inhibitors, serotonin reuptake inhibitors, amiodarone, cannabinoids, diltiazem, grapefruit juice, nefazadone, norfloxacin, quinine, and zafirlukast) should be cautiously coadministered with TIKOSYN, because they can potentially increase dofetilide levels... 

The complex polyene macrolide antibiotics are clinically effective as antifungal agents. Scott Rychnovsky of the University of California at Irvine has reported (Angew. Chem. hit. Ed. 2004,43, 2822) the first synthesis of rimocidinolide methyl ester 4, the aglycone of rimocidin 1. The key step in the synthesis is the condensation of the aldehyde 2 with the phosphonate 3, leading to 4. 

Macrolides. Antibiotics in the macrolide group are macrocyclic lactones that can be further classified into two main subgroups (I) polyene macrolides that are antifungal agents and include compounds like nystatin and amphotericin B and (2) antibacterial antibiotics represented by erythromycin and tylosin. A number of other subfamilies of antibacterial and antifungal antibiotics fall into the broad category of macrolides,... 

Due to its structural complexity and interesting physiological activities as an antifungal agent and especially as an immunosuppressive drug, the macrolide rapamycin has been a target of many total syntheses [54-58]. In their approach, Ley and co-workers used a lipase-catalyzed desymmetrization of a meso diol (Fig. 3). In early studies, the selective acetylation of 7W w-2.4-dimethylpentane-1,5-diol was achieved by a PPL immobilized on celite with moderate yields and 92%... 

Iatsimirskaia E, Tulebaev S, Storozhuk E, et al. Metabolism of rifabutin in human enterocyte and liver microsomes kinetic paramters, identification of enzyme systems, and drug interactions with macrolides and antifungal agents. Clin Pharmacol Ther 1997 61 554-562. 

Concomitant use of macrolide antibiotics or imidazole antifungal agents may lead to serious ventricular arrhythmias. Fexofenadine ... 

Thus, azole antifungal agents (such as ketoconazole and itraconazole), macrolide antibiotics, and protease inhibitors may also raise alprazolam plasma levels Inducers of CYP450 3A, such as carbamazepine, may increase clearance of alprazolam and lower alprazolam plasma levels and possibly reduce therapeutic effects... 

Rapamycin (sirolimus) is another macrolide antibiotic that possesses potent immunosuppressant activity. Rapamycin has a chemical structure partially similar to that of tacrolimus (Fig. 2). It was first isolated from Streptomyces hygro-scopicus strains found in soil obtained on Rapa Nui (Easter Island), hence the name rapamycin [19, 20]. This compound was initially investigated as an antifungal agent and later found to have immunosuppressive activity [21]. Rapamycin also binds to FKBP, but its immunosuppressive mechanisms are distinct from those of tacrolimus and cyclosporin in that it does not act via the calcineurin pathway [22, 23]. The immunosuppressive effects of rapamycin result from its inhibition of T-cell [23, 24] and B-cell [25] proliferation. The key effect on those cells results from the blocking of the signals of several cytokines (IL-2 and IL-4), leading to interruption of the cell cycle from the G, to the S phase. Unlike tacrolimus, the complex of rapamycin and FKBP-12 does not inhibit the dephosphorylase... 

Amphotericin Fungizone Amfostet Polyene macrolide Amphozone antifungal agent... 

Macrolide antibiotic. Prod, by Streptomyces sp. 83-364. Antifungal agent. 

Macrolide pentaene antibiotic. Isol. from Streptomyces roseoflavus var. jenensis and S. maghwi. Antifungal agent with antiprotozoal props. Yellow-green cryst. (EtOH aq.). Mp 161-163°. [a]j - —45 (c. 1 in dioxan). Related to Dermostatin. 

Macrolide antibiotic. Prod, by Streptomyces hygroscopicus. Antibacterial and antifungal agent. Powder. Mp 130° dec. [a] +60 (c, 1 in MeOH). Related to Azalomycin F, A-03185 and Malolactomycin, M-30015. 240 (e... 

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