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.

Figure 1 Chemical structure of anidulafungin

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 mgMaintenance 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 alteredAUC 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.

Category: Drugs / Tags: Anidulafungin, Eraxis

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