Trade Names:Cancidas- Injection, lyophilized powder for solution 50 mg- Injection, lyophilized powder for solution 70 mg
Inhibits synthesis of beta (1,3)-D-glucan, an integral component of fungal cell wall.
Approximately 97% protein bound (albumin).
Slowly metabolized by hydrolysis and N-acetylation, and undergoes spontaneous chemical degradation.
The half-life is 9 to 11 h (beta phase) and 40 to 50 h (gamma phase). 35% is excreted in feces. 41% in urine (about 1.4% as unchanged drug). Renal Cl is about 0.15 mL/min. Total Cl is 12 mL/min. Not dialyzable.
AUC is increased 30% to 49% in patients with CrCl 49 mL/min or less.Hepatic Function Impairment
AUC is increased by approximately 55% in patients with mild hepatic impairment (Child-Pugh score 5 to 6) and by 76% in patients with moderate hepatic impairment (Child-Pugh score 7 to 9).Elderly
AUC is increased by approximately 28%. No dosage adjustment is needed.Gender
AUC in women was approximately 22% higher than in men after repeat dosing. No dosage adjustment is necessary based on gender.Race
No dosage adjustment is needed based on race.
Treatment of invasive aspergillosis in patients refractory to or intolerant of other antifungal therapies; empirical treatment for presumed fungal infections in febrile neutropenic patients; treatment of esophageal candidiasis; treatment of candidemia and the following Candida infections: intra-abdominal abscesses, peritonitis, and pleural space infections.
IV 50 mg daily by slow infusion over approximately 1 h.Invasive Aspergillosis, Candidemia and Other Candida Infections, Empirical Treatment of Fungal InfectionsAdults Loading dose
IV 70 mg by slow infusion over approximately 1 h on day 1.Maintenance dose
IV 50 mg daily by slow infusion over approximately 1 h thereafter.Candidemia and other Candida infections
Antifungal therapy should be continued for at least 14 days after the last positive culture. Patients who remain neutropenic may warrant a longer duration of therapy pending resolution of the neutropenia.Empirical treatment
Treatment should be continued until resolution of neutropenia. Patients with a fungal infection should be treated for a minimum of 14 days; treatment should continue for at least 7 days after both neutropenia and clinical symptoms are resolved. If the 50 mg dose is well tolerated but does not provide adequate clinical response, the daily dose can be increased to 70 mg.Invasive aspergillosis
Duration of treatment should be based upon the severity of the underlying disease, recovery from immunosuppression, and clinical response.Hepatic Function Impairment
In adults with moderate hepatic insufficiency (Child-Pugh score 7 to 9), reduce maintenance dose to 35 mg daily. A 70 mg loading dose should still be given on day 1 where recommended.Concomitant Rifampin TherapyAdults
IV Daily maintenance dose should be increased to 70 mg.Pediatric DosingChildren 3 mo to 17 yr of age
70 mg/m 2 by slow infusion over approximately 1 h on day 1.Maintenance dose
50 mg/m 2 daily thereafter. The maximum loading and maintenance dose should not exceed 70 mg, regardless of the patient's calculated dose. The duration of treatment should be individualized to each indication as described in adults. If the 50 mg/m 2 dose is well tolerated but does not provide adequate clinical response, the daily dose can be increased to 70 mg/m 2 (max, 70 mg/day).
Store unopened vials in refrigerator (36° to 46°F). Reconstituted caspofungin solution may be stored at temperature less than 77°F for 1 h prior to preparing diluted IV infusion solution. IV infusion solution in IV bag or bottle can be stored at temperatures less than 77°F for 24 h or in refrigerator (36° to 46°F) for 48 h.
Avoid coadministration if possible. Caspofungin plasma levels may be elevated, increasing the pharmacologic effects and risk of adverse reactions.Enzyme inducers (eg, carbamazepine, dexamethasone, efavirenz, nevirapine, phenytoin, rifampin)
Caspofungin plasma levels may be reduced, decreasing the efficacy. In adults, coadministration may require an increase in dose to caspofungin 70 mg daily. In children, coadministration may require an increase in dose to caspofungin 70 mg/m 2 daily (max, 70 mg/day).Tacrolimus
Tacrolimus blood levels may be decreased, reducing the efficacy.
None well documented.
Phlebitis (18%); hypotension (12%); tachycardia (11%); hypertension (10%); arrhythmia, atrial fibrillation, bradycardia, cardiac arrest, flushing, MI (less than 5%).
Headache (15%); anxiety, asthenia, confusional state, convulsion, depression, dizziness, fatigue, insomnia, somnolence, tremor (less than 5%).
Rash (23%); erythema (9%); pruritus (7%); decubitus ulcer (3%); petechiae, skin lesion, urticaria (less than 5%); erythema multiforme, skin exfoliation, Stevens-Johnson syndrome (postmarketing).
Diarrhea (27%); vomiting (17%); nausea (15%); abdominal pain (9%); abdominal distension, constipation, dyspepsia, upper abdominal pain (less than 5%); pancreatitis (postmarketing).
Hematuria, renal failure, UTI (less than 5%); clinically significant renal dysfunction (postmarketing).
Hepatic failure, hepatomegaly, hepatotoxicity, hyperbilirubinemia, jaundice (less than 5%); hepatic necrosis (postmarketing).
Anemia (11%); coagulopathy, febrile neutropenia, neutropenia, thrombocytopenia (less than 5%).
Decreased serum potassium (23%); decreased hemoglobin, increased alkaline phosphatase (21%); decreased hematocrit, increased ALT (18%); increased AST (17%); increased serum bilirubin (13%); decreased WBC (12%); increased serum creatinine (11%); positive urine RBC (10%); increased blood urea (9%); increased conjugated bilirubin (8%); decreased serum albumin, decreased serum magnesium (7%); increased blood glucose (6%); increased serum potassium (3%).
Infusion-site pain/pruritus/swelling (less than 5%).
Hypokalemia (8%); anorexia, decreased appetite, fluid overload, hypercalcemia, hyperglycemia, hypomagnesemia (less than 5%).
Back pain (4%).
Cough, pneumonia, respiratory failure (11%); dyspnea, pleural effusion (9%); respiratory distress (8%); rales (7%); epistaxis, hypoxia, tachypnea (less than 5%).
Pyrexia (30%); chills (23%); septic shock (13%); peripheral edema (11%); mucosal inflammation (10%); central line infection (9%); sepsis (5%); edema, graft-versus-host disease (4%); bacteremia (less than 5%); swelling (postmarketing).
Evaluate LFTs prior to treatment and periodically thereafter. If abnormal LFTs are noted, monitor patient's liver function more frequently. If worsening hepatic function is noted, evaluate risk/benefit of continued therapy with caspofungin.
Category C .
Safety and efficacy not established in children younger than 3 mo of age.
Anaphylaxis and possible histamine-mediated symptoms, including rash, facial swelling, pruritus, sensation of warmth, and bronchospasm, have been reported during administration of caspofungin.
No dosage adjustment is needed in patients with renal insufficiency.
LFT abnormalities may occur. Isolated cases of clinically significant hepatic dysfunction, hepatic failure, and hepatitis have been reported.
In clinical studies, single doses of 210 mg were generally well tolerated.
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