What Is Caspofungin?

Caspofungin is a semi-synthetic lipopeptide (echinocandin) compound synthesized from the fermentation product of Glarea Lozoyensis.

Caspofungin can inhibit the synthesis of (1,3) -D-glucan, a basic component of many filamentous fungi and yeast cell walls, thereby exerting an antifungal effect.

Carbofuran Basic Information

Chinese name

CAS NO: 162808-62-0

Chemical Structure:

English name: Caspofungin

Molecular formula: C ₅₂ H ₈₈ N ₁₀ O ₁₅

Molecular weight: 1093.31 ^[1]

Caspofungin Caspofungin- related drug labeling profile information

Carprofen net common name

Caspofungin acetate for injection

Indications of carbophene net function

This product is suitable for adult patients and pediatric patients (three months and more): empirical treatment of neutropenia, suspicious fungal infection in patients with fever treatment of invasive aspergillus that is ineffective or intolerable to other treatments disease.

Carboprofen net dosage

· Adult patients are generally recommended for the treatment of adult patients (18 years and older). The infusion solution should be slowly infused intravenously for about 1 hour.
On the first day of empiric therapy, a single 70 mg loading dose was followed by a single 50 mg daily dose. The course of treatment depends on the clinical response of the patient. Empirical treatment needs to be continued until the patient's neutrophils return to normal. Patients diagnosed with a fungal infection require a course of treatment of at least 14 days; treatment needs to continue for at least 7 days after neutrophils return to normal and clinical symptoms have resolved. If the 50 mg dose is well tolerated but lacks an effective clinical response, the daily dose can be increased to 70 mg. Although there is no evidence that a daily dose of 70 mg improves efficacy, the limited safety data available indicate that daily dose increases to 70 mg are well tolerated.
Invasive aspergillosis was given a single 70 mg loading dose of caspofungin acetate for injection on the first day, followed by a daily dose of 50 mg. The course of treatment depends on the severity of the patient's disease, the suppressed recovery of immune function, and the clinical response to the treatment. Although there is no evidence that using larger doses can improve efficacy, the available safety data suggest that patients with no clinical response and well tolerated with this product can consider increasing the daily dose to 70 mg.
No dosage adjustment is required for elderly patients (65 years or older).
There is no need to adjust doses based on gender, race or kidney damage.
Adult patients: When this product is used concurrently with efavirenz, nevirapine, rifampicin, dexamethasone, phenytoin or carbamazepine with metabolic induction drugs, a daily dose of 70 mg should be considered.
Patients with hepatic insufficiency do not need to adjust dosages for adult patients with mild hepatic insufficiency (Child-Pugh scores 5 to 6). However, for adult patients with moderate liver dysfunction (Child-Pugh scores 7 to 9), it is recommended to adjust the daily dose of this product to 35 mg based on pharmacokinetic data after giving the first 70 mg loading dose. There is currently no clinical experience with medications for adult patients with severe liver dysfunction (Child-Pugh score greater than 9) and children with any degree of liver dysfunction.
Pediatric Patients In pediatric patients (3 months to 17 years), this product requires a slow intravenous infusion for about 1 hour. Pediatric patients (3 months to 17 years of age) should be dosed according to the patient's body surface area (see Pediatric Instructions, Mosteller 1 Formula). For all indications, a single loading dose of 70 mg / m2 should be given on the first day (the actual daily dose should not exceed 70 mg), followed by a daily dose of 50 mg / m2 (the actual daily dose should not exceed 70 mg). The course of treatment can be adjusted according to the indication, and the course of treatment for various indications is expressed in adults (see general recommendations for medications for adult patients).
If the daily dose of 50mg / m2 cannot obtain sufficient clinical response, but the patient is well tolerated, the daily dose can be increased to 70 mg / m2 (the actual daily dose does not exceed 70mg). Although there is no evidence that the daily dose of 70 mg / m2 can improve the efficacy, limited safety data show that daily doses up to 70 mg / m2 can still be well tolerated.
In children, the daily dose of this product can be adjusted to 70 mg / m2 when it is used in combination with a metabolic inducer (such as rifampicin, efavirenz, nevirapine, phenytoin, dexamethasone, or carbamazepine). (The actual daily dose does not exceed 70 mg).

Dissolution of Caspofungin Acetate for Injection

Do not use any diluent containing dextrose (-D-glucan) because this product is not stable in diluent containing dextrose. Do not mix or infuse this product with any other drug, as there is no information on the compatibility of this product with other intravenous infusions, additives or drugs. The infusion should be visually observed for particulate matter or discoloration.
Medication for adult patients:
The first step is to dissolve the medicine in the medicine bottle. When dissolving the powdered medicine, place the medicine bottle stored in the refrigerator at room temperature, and add 10.5 mL of sterile water for injection or containing para-hydroxybenzoic acid under sterile conditions. Sterile water for injection of methyl ester and propyl paraben, or sterile water for injection containing 0.9% benzyl alcohol. After dissolution, the concentration of the drug solution in the bottle will be 7.2mg / mL (70mg per bottle) or 5.2mg / mL (50mg per bottle).
White to off-white drug powders will completely dissolve. Mix gently until a clear solution is obtained. The dissolved solution should be visually inspected for particulate matter or discoloration. This solution stored at 25 ° C or below can be used within 24 hours.
The second step is to prepare a solution for patient infusion. The diluent prepared as a solution for patient infusion is: sterile saline for injection or lactated Ringer's solution. The standard solution for patient infusion should be prepared under sterile conditions by adding an appropriate amount of the dissolved drug (see the table below) to a 250 mL intravenous infusion bag or bottle. If medically required daily dose is 50mg or 35mg, the volume of the infusion solution can be reduced to 100mL. Do not use the solution if it is cloudy or precipitated. If the infusion solution is stored in an environment of 25 ° C or below, it must be used within 24 hours; if it is stored in a refrigerator at 2 to 8 ° C, it must be used within 48 hours. The infusion solution must be slowly infused intravenously over approximately 1 hour.
Child medication instructions:
The formula for calculating the body surface area (BSA) of the dose administered to children. Before formulating the infusion, use the following formula to calculate the body surface area (BSA) of the patient: (Mosteller formula) Preparation of 70mg / m2 infusion for children over 3 months (Taken from a 70mg vial)
1. Determine the actual loading dose for a pediatric patient using the patient's BSA (calculated according to the above formula) and the following equation:
BSA (m2) × 70 mg / m2 = loading dose Regardless of the patient's calculated dose, the maximum loading dose on day 1 should not exceed 70 mg.
2. Keep the refrigerated bottle at room temperature to rewarm.
3. Under sterile conditions, add 10.5mL of 0.9% sodium chloride injection, sterile water for injection, or bacteriostatic water for injection containing methylparaben and propylparaben. a The dissolved solution should not be allowed to stand for more than 1 hour at 25 ° C (77 ° F). b The final bottled concentration of caspofungin is 7.2 mg / mL.
4. Withdraw the corresponding volume of solution from the vial based on the calculated loading dose (step 1). Under sterile conditions, transfer this volume (mL) of this product solution to an intravenous infusion bag (or bottle) containing 250 mL of 0.9%, 0.45%, or 0.225% sodium chloride injection or lactated Ringer's solution. . In addition, this volume (mL) of this product solution can be added to 0.9%, 0.45%, or 0.225% sodium chloride injection or lactated Ringer's solution after volume reduction under sterile conditions, and the final concentration does not exceed 0.5 mg / mL. When the infusion solution is stored at a temperature of 25 ° C (77 ° F), it must be used within 24 hours or within 48 hours when refrigerated at 2 to 8 ° C (36 to 46 ° F).
5. If the calculated loading dose is less than 50mg, a 50mg vial can be used to prepare the medicament [Refer to the preparation of a 50 mg / m2 infusion solution for children over 3 months (taken from a 50mg vial). 4 steps]. The final concentration of dissolved caspofungin in a 50 mg vial was 5.2 mg / mL.
Preparation of a 50 mg / m2 infusion for pediatric patients over 3 months (taken from a 50 mg vial)
1. Determine the actual daily maintenance dose for a pediatric patient using the patient's BSA (calculated according to the above formula) and the following equation:
BSA (m2) × 50 mg / m2 = daily maintenance dose Regardless of the patient's calculated dose, the daily maintenance dose should not exceed 70 mg.
2. Keep the refrigerated bottle at room temperature to rewarm.
3. Under sterile conditions, add 10.5mL of 0.9% sodium chloride injection, sterile water for injection, or bacteriostatic water for injection containing methylparaben and propylparaben. a The dissolved solution should not be allowed to stand for more than 1 hour at 25 ° C (77 ° F). b The final bottle concentration of caspofungin is 5.2 mg / mL.
4. According to the calculated daily maintenance dose (the first step), draw the corresponding volume of solution from the vial. Under sterile conditions, transfer this volume (mL) of this product solution to an intravenous infusion bag (or bottle) containing 250 mL of 0.9%, 0.45%, or 0.225% sodium chloride injection or lactated Ringer's solution. . In addition, this volume (mL) of this product solution can be added to 0.9%, 0.45%, or 0.225% sodium chloride injection or lactated Ringer's solution after volume reduction under sterile conditions, and the final concentration does not exceed 0.5 mg / mL. When the infusion solution is stored at a temperature of 25 ° C (77 ° F), it must be used within 24 hours or within 48 hours when refrigerated at 2 to 8 ° C (36 to 46 ° F).
5. If the actual daily maintenance dose is greater than 50mg, a 70mg bottle can be used to prepare the drug 4 steps]. The final concentration of dissolved caspofungin in a 70 mg vial was 7.2 mg / mL.

Caspofungin preparation note

a White to off-white dense powders will completely dissolve. Mix gently until a clear solution is obtained.
b During the dissolution process and before injection, the dissolved solution should be visually observed for particulate matter or discoloration. Do not use when the solution appears cloudy or precipitated.
c The preparation of this product can ensure that the 10mL solution drawn from the vial can obtain the full labeled dose (70mg or 50mg).

Caspofungin adverse reactions

Reported adverse reactions include symptoms that may be mediated by histamine, including rash, facial swelling, itching, warmth, or bronchospasm. Allergic reactions have been reported in patients treated with this product.
Adult patients have had 1865 adults in clinical studies who used single or multiple doses of caspofungin acetate for injection: 564 patients with febrile neutropenia (empirical treatment studies) and 382 patients with invasive candidiasis There were 297 patients with esophageal candidiasis and / or oropharyngeal candidiasis, 228 patients with invasive aspergillosis, and 394 participants in Phase I clinical trials. In empirical treatment studies, patients have received chemotherapy for malignant tumors or hematopoietic stem cell transplants. In studies conducted on patients with a clearly diagnosed Candida infection, most patients are very ill (eg, hematological malignancies or other tumors, recent major surgery, AIDS) and require multiple treatments at the same time. In an uncontrolled study of aspergillosis, the patient's condition is severe and the original disease is complex (such as bone marrow or peripheral blood stem cell transplantation, hematological malignancies, solid tumors or organ transplants), and multiple treatments are required .
Among all adults (989 in total) receiving this product, reported drug-related clinical and laboratory abnormalities are generally mild and rarely cause discontinuation.
Post-marketing experience:
The following post-market adverse events have been reported:
Hepatobiliary: Rare liver dysfunction Cardiovascular: Swelling and peripheral edema Laboratory abnormalities: Laboratory tests of hypercalcemia found:
Other laboratory abnormalities related to the drug have been reported: hypoalbumin, hypokalemia, hypomagnesemia, leukocytopenia, eosinophilia, thrombocytopenia, neutropenia, urinary erythrocytosis, and partial thrombokinase Prolonged time, decreased serum total protein, increased urinary protein, prolonged prothrombin time, low sodium, leukocytosis in the urine, and low calcium.
Pediatric Patients Among pediatric patients, other reported drug-related laboratory abnormalities were hypokalemia, hypomagnesemia, increased blood glucose, decreased phosphorus, increased phosphorus, and eosinophilia.