Anidulafungin is an echinocandin anti-fungal agent used for intravenous (IV) infusion. It is chemically designated as C58H73N7O17, and its molecular weight is 1140.3. This white to off-white lyophilized powder is available as a single-use, 50-mg vial that is supplied with an accompanying 15-ml diluent vial (20% weight in weight [w/w] dehydrated alcohol in water, or 20 g/100 g).
Figure 1 illustrates the agent’s chemical structure.
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Figure 1 Chemical structure of anidulafungin. (From Eraxis product information.)
As a semisynthetic lipopeptide, ani-dulafungin is synthesized from a fermentation product of Aspergillus nidulans. It possesses potent fungicidal activity against most Candida species, including those resistant to azoles. Anidulafungin also has in vitro activity against Asper-gillus, but it is less active against other filamentous fungi.
MECHANISM OF ACTION
The activity of anidulafungin is similar to that of other antifungal agents; it interferes with the synthesis of the fungal cell wall. As with all agents of the echino-candin class, its spectrum of activity is largely limited to Candidaand Aspergillus species.
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Anidulafungin exerts its antifungal activity by noncompetitively inhibiting 1,3-p-D-glucan synthase, which results in inhibition of glucan synthesis. Glucan is an essential component of the fungal cell wall, making it a selective target for anti-fungal agents.
PHARMACOKINETICS
The pharmacokinetic parameters in 225 patients with fungal infections were similar to those found in healthy subjects (Table 1).
Table 1 Mean (Percent Coefficient of Variation) Steady-State Pharmacokinetic Parameters
| Parameter | Loading Dose, Loading Dose, 100 mg 200 mg
Maintenance Dose, Maintenance Dose, 50 mg 50 mg |
|
| C (mg/liter)
max о > |
4.2 (22.4) | 7.2 (23.3) |
| C (mg/liter) | 1.6 (42.1) | 3.3 (41.8) |
| AUCss (mg • hours/liter) | 55.2 (32.5) | 110.3 (32.5) |
| Clearance (liters/hour) | 1.0 (33.5) | |
| Half-life (hours) | 26.5 (28.5) | |
| AUCss = steady-state area under the curve; Cmax = steady-state peak concentration; Cmin = steady-state minimum concentration. From Eraxis product information.8 | ||
Steady state is achieved on the first day of treatment following a loading dose of anidulafungin. The volume of distribution is similar to total body fluid volume at 30 to 50 liters. Binding to plasma protein is moderate at 84%. cialis canadian pharmacy
Anidulafungin does not appear to go through hepatic metabolism. It is not a clinically relevant substrate, inducer, or inhibitor of cytochrome P450 (CYP 450) isoenzymes.
Table 2 presents the results of some drug-interaction studies.
Table 2 Drug Interactions and Anidulafungin
| Drug | CYP Isoenzyme | Result |
Dose Adjustment |
| Cyclosporine | 3A4 substrate | Cmax of anidulafungin not significantly altered
AUC increased by 22% No effect on cyclosporine metabolism |
No |
| Voriconazole
(Vfend) |
3A4 inhibitor and substrate Neither Cmax nor AUC of either drug significantly altered 2C19,2C9 |
No |
|
| Tacrolimus generic (Canadian Prograf capsules or injection) | 3A4 substrate | Neither Cmax nor AUC of either drug significantly altered |
No |
| Liposomal ampho-tericin B (AmBisome) | — | Pharmacokinetics of anidulafungin not significantly altered |
No |
| Rifampin | Potent CYP inducer | Pharmacokinetics of anidulafungin not significantly altered |
No |
| AUC = area-under-the-curve concentration; Cmax =
‘ max From Eraxis product information. |
peak concentration; CYP = cytochrome. | ||
More than 90% of anidulafungin undergoes a slow chemical degradation in the blood, and the agent’s half-life is approximately 24 hours. No dose adjustments are needed in patients with renal or hepatic impairment because most degradation products are eliminated via the biliary system.
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