Mechanism of action and target
The action of echinocandins targets the fungal cell wall, which contains chitin, glycoproteins, and glucans. The drugs non-competitively inhibit the enzyme β-(1,3)-D-glucan synthase.
- The addition of glucose to the growing chain is blocked.
- The synthesis of β-(1,3)-D-glucan is disrupted, and wall integrity is lost.
- Osmotic stress develops, leading to cell lysis and death.
These drugs are safe for humans because mammalian cells lack a cell wall and the target of action.
Classification and spectrum of activity
The group includes three main drugs: caspofungin, micafungin, and anidulafungin. Their antimicrobial spectrum covers:
- Genus Candida — exhibits a fungicidal effect. The drugs are active even against strains resistant to other agents, including Candida glabrata and Candida krusei.
- Genus Aspergillus — exhibits a fungistatic effect, halting fungal growth.
General pharmacokinetics and safety
All echinocandins are administered exclusively parenterally, as they have low bioavailability and are not absorbed when taken orally.
- Tolerability: General tolerability is good, comparable to fluconazole.
- Side effects: Headache, fever, altered liver function tests, and rare hemolysis may occur.
- Histamine-like reactions: Due to the peptide chain in the structure, rash, pruritus, and bronchospasm may occur as a result of histamine release.
Clinical use of representatives
Each substance has its own clinical use features:
- Caspofungin: The first representative of the class, used for esophageal candidiasis, candidemia, invasive aspergillosis ("salvage therapy"), and empiric therapy for febrile neutropenia.
- Micafungin: A derivative of Coleophoma empedri, used for esophageal candidiasis and for the prophylaxis of infections after hematopoietic stem cell transplantation.
- Anidulafungin: Derived from Aspergillus nidulans, prescribed for esophageal candidiasis and candidemia. Permits combination therapy with amphotericin B, flucytosine, or azoles.
Echinocandins hit Candida and Aspergillus, destroying the wall via glucan synthase, but are administered IV only!
Class and exam questions
Why are echinocandins not used in tablets?
The drugs have low bioavailability when taken orally and simply are not absorbed in the gastrointestinal tract, which is why they are administered parenterally only.
What effect do echinocandins have on Candida and Aspergillus?
Against fungi of the genus Candida, the drugs exhibit a fungicidal effect (kill them), while against Aspergillus, they exhibit a fungistatic effect (halt growth).
Is dose adjustment of caspofungin required in renal impairment?
No, dose adjustment of caspofungin is not required in renal impairment.
What else to study on this topic
- Biochemical process of β-(1,3)-D-glucan synthesis involving UDP-glucose
- Features of caspofungin metabolism and plasma protein binding
- Drug interactions of caspofungin with cyclosporine and microsomal enzyme inducers
- Caspofungin dose adjustment in moderate hepatic impairment
- Possibilities of anidulafungin combination therapy with other antifungals
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