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caspofungin (Cancidas)
Tradename: Cancidas.
Indications:
1) HIV antifungal agent
a) treatment of invasive aspergillosis
b) 2nd line agent for patients who do NOT respond to or cannot tolerate amphotericin B or itraconazole
2) treatment of infections due to Candida
a) Candida glabrata
b) esophageal candidiasis
c) oropharyngeal candidiasis [3]
d) candidemia
3) empiric treatment of febrile neutropenia [3]
Contraindications:
- cryptococcosis (lack of antimicrobial activity)
Dosage:
1) 70 mg IV infused over 1 hour, then 50 mg IV QD
2) 70 mg/day if coadministered with rifampin
3) by infusion only (infuse slowly, over 1 hour)
4) do NOT coadminister with other medications
No dosage adjustment with renal failure.
Hepatic failure (Child-Pugh score of 7-9):
- decrease dose to 35 mg/day
Pharmacokinetics:
1) 97% bound to albumin
2) hepatically cleared via hydrolysis & N-acetylation
3) spontaneous degradation
4) elimination
a) 50% in urine (1-9% unchanged; 40% as metabolites)
b) 35% in feces as metabolites
5) poor penetration into the CNS [2]
Antimicrobial activity:
1) Aspergillus
2) Candida
Adverse effects:
1) common (> 10%)
a) headache (11%)
b) fever (3-26%)
c) decreased hemoglobin (3-12%)
d) increased LFTs (alkaline phosphatase, transaminases) 3-13%
e) infusion site reactions/phlebitis (2-16%)
2) not common (1-10%)
a) cardiovascular:
- flushing, hypertension, hypotension, tachycardia
b) central nervous system: dizziness, pain, insomnia
c) gastrointestinal:
- nausea/vomiting, abdominal pain, diarrhea, anorexia
d) hepatic: increased bilirubin
e) renal:
- nephrotoxicity (8%), proteinuria (5%), hematuria, pyruria, increased serum creatinine
f) metabolic: hypokalemia (10%)
g) hematologic:
- eosinophilia, neutropenia, leukocytosis, anemia, thrombocytopenia
h) neuromuscular: myalgia, paresthesia, tremor
i) skin
j) other - flu-like syndrome, diaphoresis
3) uncommon (< 1%
- ARDS, anaphylaxis, hepatic dysfunction, pulmonary edema, renal insufficiency
Drug interactions:
1) coadministration with cyclosporine increases liver toxicity
2) rifampin may diminish caspofungin concentrations
3) caspofungin may diminish tacrolimus concentrations
Mechanism of action:
1) echinocandin
2) inhibits formation of fungal cell walls
3) inhibits synthesis of beta(1,3)-D-glucan*
4) highest activity in regions of active growth
* mammalian cells do not require beta(1,3)-D-glucan
Notes: Manufacturer: Merck
Interactions
drug interactions
General
echinocandin
Properties
MISC-INFO: elimination route LIVER
1/2life 9-11 HOURS
40-50 HOURS
protein-binding 97%
elimination by hemodialysis -
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- Prescriber's Letter 8(3):15 2001
Lexi-Comp Online 2004
- Medical Knowledge Self Assessment Program (MKSAP) 16,
American College of Physicians, Philadelphia 2012
- Deprecated Reference