Caspofungin: Formula, Indications, Mechanism of Action, Dosage, Warnings, Side Effects and Interactions

It is an antifungal medicine and belongs to a new class called echinocandins.

Antifungals in the echinocandin class inhibit glucan synthesis in the cell wall, probably through the enzyme 1,3-beta glucan synthase.

There is a potential for the development of resistance, however, the development of in vitro resistance to caspofungin by Aspergillus species has not been studied .

Chemical formula of caspofungin

  • C52H88N10O15.

Presentation

  • Caspofungin in intravenous solution of 50 and 70 mg.

Indications of caspofungin

Caspofungin is used to treat a variety of serious fungal infections .

It is often used in patients who cannot use or do not respond to other antifungal medications such as amphotericin B, itraconazole .

The antifungal effect of echinocandin is used for aspergillosis , candidemia, esophageal candidiasis, and empirical treatment in febrile neutropenia .

Mechanism of action

Caspofungin inhibits the synthesis of a major component of the fungal cell wall, beta (1,3) -D-glucan.

Beta (1,3) -D-glucan is not present in mammalian cells and therefore is an attractive target for antifungal activity.

Caspofungin is fungicidal against Candida sp., And has activity against Aspergillus sp., With hyphae undergoing active cell growth.

The following organisms are generally considered susceptible to caspofungin in vitro:

  • Aspergillus sp., incluyendo Aspergillus flavus, Aspergillus fumigatus y Aspergillus terreus.
  • Candida sp., Including Candida albicans, Candida glabrata, Candida guilliermondii, Candida krusei, Candida Portugal, Xenopus laevis y Candida tropicalis.
  • Activity against Trichosporon beigelii, Fusarium sp., And Rhizopus arrhizus is limited.
  • It has no activity against Cryptococcus neoformans, but in vitro it has shown synergistic activity against C. neoformans when combined with amphotericin B or fluconazole.

Dose

This medication is usually administered intravenously, the doctor prescribes it once a day usually. It should be injected slowly over more than 1 hour.

The maximum dose is 70 mg / day, doses of up to 150 mg / day have been recommended only in cases of cardiovascular infections .

Caspofungin Side Effects

Tell your doctor right away if you have symptoms such as fever, chills, shortness of breath, hot flashes, or dizziness.

May cause inflammation, redness, irritation at the injection site. Effects such as nausea, vomiting, diarrhea, or headache have also been reported.

The doctor should be informed if any serious side effects are observed, including signs of liver disease such as nausea and vomiting that will not stop, loss of appetite, dark colored urine, abdominal pain, yellowish eyes and skin, swelling of the ankles, feet and hands, fast and irregular heartbeat, and muscle cramps.

Serious allergic reactions can present symptoms such as rashes, itching, swelling especially of the face, tongue and throat, severe dizziness and shortness of breath.

Warnings and Contraindications

Allergies

Before using caspofungin, you should inform your doctor if you are allergic to the component of the drug or to other antifungal drugs of echinocandin such as anidulafungin, micafungin, or if you have any other allergies.

Caspofungin is contraindicated for use in patients with hypersensitivity to the drug or any of its components.

Liver problems

Patients with liver disease, or those with cholestasis, hepatitis, or jaundice may require a dose adjustment of caspofungin.

Clinically significant elevations in plasma concentrations of caspofungin have been observed in patients with moderate hepatic impairment.

Newly born

Its safety and efficacy have not been studied in infants less than 3 months of age.

In general, the safety profile of caspofungin in pediatric patients is comparable to that in adult patients.

Pregnancy

Caspofungin is classified in FDA pregnancy risk category C.

Animal data revealed embryotoxic effects with the use of caspofungin, including increased fetal resorption, increased peri-implant implantation loss, and incomplete ossification at multiple fetal sites, including incomplete ossification of the talus, calcaneus, skull, and torso.

Embryotoxic effects have been observed in animals resulting in exposure similar to that observed in humans.

Caspofungin crosses the placenta in animal models and is detected in the plasma of animal fetuses. It should be used during pregnancy only when the benefits clearly outweigh the risks.

Breast-feeding

Data are limited regarding the use of caspofungin during lactation and it is not known whether it is excreted in human milk. Caution is advised when administered to nursing mothers.

No studies have been performed to evaluate the effects of exposure in a breastfed infant, however, based on the oral malabsorption of caspofungin, the risks appear to be low.

Monitor infants potentially exposed to gastrointestinal adverse events and signs of histamine release.

The fluconazole may be a potential alternative to consider during lactation.

Caspofungin interactions

Interactions of caspofungin with other medicines can change how the medicines work or increase the risk of serious side effects.

These medications include carbamazepine , cyclosporine , dexamethasone , certain AIDS medications such as efavirenz, nevirapine, and others such as phenytoin , rifampin, and tacrolimus.