Caspofungin

  • C52H88N10O15 ( caspofungin )
  • C52H88N10O15 · 2C2H4O2 ( caspofungin diacetate · )

J02AX04

Antifungal echinocandin

Inhibition of the β (1,3 )-D- glucan

Slightly soluble in water and in methanol, less soluble in ethanol ( caspofungin diacetate · )

Template: Infobox chemical / molecular formula search available

Caspofungin is an antifungal agent from the group of echinocandins and is used in the treatment of fungal infections. It is marketed by Merck under the name CANCIDAS.

Chemistry

Caspofungin is a semisynthetic lipopeptide ( echinocandin ) whose starting material is the Pneumocandin B0. This is derived from the fungus Glarea lozoyensis.

Pharmacology

Mechanism of action

Mushrooms have a consisting of chitin and cell wall polysaccharides. One component of this cell wall β (1,3 )-D- glucan. Caspofungin inhibits the enzyme β (1,3 )-D- glucan synthase, which is responsible in fungi for the construction of this cell wall block. Human cells do not have such a cell wall, and therefore no β (1,3) -D-glucan synthase.

  • Aspergillus spp., Candida spp., Histoplasma capsulatum, Coccidioides immitis

Uptake and distribution in the body ( pharmacokinetics )

Caspofungin is not absorbed in the intestine. It can therefore only be given intravenously. It is bound to 96% to plasma proteins. The degradation of the substance takes place mainly in the liver. Eliminated it is 35% in the faeces and about 41% through the kidneys. The biological half-life is 9-11 hours.

Areas of application (indications )

  • Treatment of invasive Candida infections in adult or pediatric patients.
  • Treatment of invasive aspergillosis in adult or pediatric patients who do not respond to therapy with amphotericin B, lipid formulations of amphotericin B and / or itraconazole or can not tolerate. Refractoriness is defined as progression of infection or failure to improve after at least 7 days of antifungal therapy at therapeutic doses of effective.
  • Empirical treatment of suspected fungal infections ( such as Candida or Aspergillus ) in adult or pediatric patients with fever and neutropenia.

Contraindications ( contraindications)

Hypersensitivity to caspofungin or any other ingredient.

Adverse effects (side effects)

  • Fever, chills
  • Inflammatory reactions at the infusion site ( phlebitis )
  • Abdominal pain, nausea, vomiting
  • Skin rash, itching, sweating
  • Anemia (anemia)
  • Headache

Interactions with other drugs

  • Concomitant administration of cyclosporine, the concentration of ciclosporin increased. Caspofungin remained unchanged.
  • Co-administration of tacrolimus at its minimum plasma concentration lowered.
  • In a few patients, the AUC of caspofungin decreased with concomitant administration of efavirenz
  • Nevirapine
  • Rifampicin
  • Dexamethasone
  • Phenytoin
  • Carbamazepine
CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Candida (fungus) Allergy
168200
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