Echinocandins

Last updated: November 01, 2022

Echinocandins

MiBi

MiBi

Bacterial structure and functions
Staphylococcus epidermidis
Staphylococcus aureus
Staphylococcus saprophyticus
Streptococcus viridans
Streptococcus pneumoniae
Streptococcus pyogenes (Group A Strep)
Streptococcus agalactiae (Group B Strep)
Enterococcus
Clostridium perfringens
Clostridium botulinum (Botulism)
Clostridium difficile (Pseudomembranous colitis)
Clostridium tetani (Tetanus)
Bacillus cereus (Food poisoning)
Listeria monocytogenes
Corynebacterium diphtheriae (Diphtheria)
Bacillus anthracis (Anthrax)
Nocardia
Actinomyces israelii
Escherichia coli
Salmonella (non-typhoidal)
Salmonella typhi (typhoid fever)
Pseudomonas aeruginosa
Enterobacter
Klebsiella pneumoniae
Shigella
Proteus mirabilis
Yersinia enterocolitica
Legionella pneumophila (Legionnaires disease and Pontiac fever)
Serratia marcescens
Bacteroides fragilis
Yersinia pestis (Plague)
Vibrio cholerae (Cholera)
Helicobacter pylori
Campylobacter jejuni
Neisseria meningitidis
Neisseria gonorrhoeae
Moraxella catarrhalis
Francisella tularensis (Tularemia)
Bordetella pertussis (Whooping cough)
Brucella
Haemophilus influenzae
Haemophilus ducreyi (Chancroid)
Pasteurella multocida
Mycobacterium tuberculosis (Tuberculosis)
Mycobacterium leprae
Mycobacterium avium complex (NORD)
Mycoplasma pneumoniae
Chlamydia pneumoniae
Chlamydia trachomatis
Borrelia burgdorferi (Lyme disease)
Borrelia species (Relapsing fever)
Leptospira
Treponema pallidum (Syphilis)
Rickettsia rickettsii (Rocky Mountain spotted fever) and other Rickettsia species
Coxiella burnetii (Q fever)
Ehrlichia and Anaplasma
Gardnerella vaginalis (Bacterial vaginosis)
Viral structure and functions
Varicella zoster virus
Cytomegalovirus
Epstein-Barr virus (Infectious mononucleosis)
Human herpesvirus 8 (Kaposi sarcoma)
Herpes simplex virus
Human herpesvirus 6 (Roseola)
Adenovirus
Parvovirus B19
Human papillomavirus
Poxvirus (Smallpox and Molluscum contagiosum)
BK virus (Hemorrhagic cystitis)
JC virus (Progressive multifocal leukoencephalopathy)
Poliovirus
Coxsackievirus
Rhinovirus
Hepatitis A and Hepatitis E virus
Hepatitis D virus
Influenza virus
Mumps virus
Measles virus
Respiratory syncytial virus
Human parainfluenza viruses
Dengue virus
Yellow fever virus
Zika virus
Hepatitis C virus
West Nile virus
Norovirus
Rotavirus
Coronaviruses
HIV (AIDS)
Human T-lymphotropic virus
Ebola virus
Rabies virus
Rubella virus
Eastern and Western equine encephalitis virus
Lymphocytic choriomeningitis virus
Hantavirus
Prions (Spongiform encephalopathy)
Coccidioidomycosis and paracoccidioidomycosis
Histoplasmosis
Blastomycosis
Pneumocystis jirovecii (Pneumocystis pneumonia)
Candida
Mucormycosis
Aspergillus fumigatus
Sporothrix schenckii
Cryptococcus neoformans
Malassezia (Tinea versicolor and Seborrhoeic dermatitis)
Plasmodium species (Malaria)
Babesia
Giardia lamblia
Entamoeba histolytica (Amebiasis)
Cryptosporidium
Acanthamoeba
Naegleria fowleri (Primary amebic meningoencephalitis)
Toxoplasma gondii (Toxoplasmosis)
Trypanosoma brucei
Trypanosoma cruzi (Chagas disease)
Trichomonas vaginalis
Leishmania
Pediculus humanus and Phthirus pubis (Lice)
Sarcoptes scabiei (Scabies)
Protein synthesis inhibitors: Aminoglycosides
Antimetabolites: Sulfonamides and trimethoprim
Antituberculosis medications
Miscellaneous cell wall synthesis inhibitors
Protein synthesis inhibitors: Tetracyclines
Cell wall synthesis inhibitors: Penicillins
Miscellaneous protein synthesis inhibitors
Cell wall synthesis inhibitors: Cephalosporins
DNA synthesis inhibitors: Metronidazole
DNA synthesis inhibitors: Fluoroquinolones
Integrase and entry inhibitors
Nucleoside reverse transcriptase inhibitors (NRTIs)
Protease inhibitors
Hepatitis medications
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Neuraminidase inhibitors
Herpesvirus medications
Azoles
Echinocandins
Miscellaneous antifungal medications
Anthelmintic medications
Antimalarials
Anti-mite and louse medications

Transcript

Watch video only

Echinocandins are a novel class of medications used to treat mycoses, or fungal infections.

Mycoses can be localized skin infections, or develop into systemic infections in immunodeficient patients.

Antifungals work either through fungistatic action, meaning that they inhibit fungal growth, or through fungicidal action, meaning they kill the fungi.

Now, most fungi have a protective cell wall made of different carbohydrate molecules.

Some fungal species have beta glucans which are polysaccharide polymers that are cross linked with other carbohydrate molecules to make a strong fungal cell wall.

Beta glucans are produced by an enzyme on the cell membrane called beta-1,3-D-glucan synthase.

This enzyme is not found in human cells which makes it a good target for antifungal medications.

Now, echinocandins are a type of medication that noncompetitively bind to and inhibit beta-1,3-D-glucan synthase.

This weakens the cell wall and prevents it from being repaired.

The cell wall gradually deforms more and more until it ruptures, causing the cell to die.

Echinocandins are only available via IV since they are not well absorbed through the GI tract.

Medications in this class include anidulafungin, micafungin, and caspofungin.

They are only effective against fungal species that have beta-1,3-D-glucan synthase, but it’s extremely rare for these organisms to have resistance to these medications.

Because of this, echinocandins are often used to treat fungal infections that are resistant to the more common antifungal medications like amphotericin-B and the “azole” medications like fluconazole.

Echinocandins are used to treat mucocutaneous candidiasis, which affect the skin, nails, and oral mucosa, or disseminated candidiasis, where the infection spreads to multiple organ systems through the blood, causing endocarditis, endophthalmitis, and osteomyelitis.

This is only seen in people with a compromised immune system like those with an HIV infection, or patients undergoing chemotherapy.

Echinocandins are also used to treat invasive aspergillosis.

Normally, aspergillus species cause bronchopulmonary aspergillosis in immunocompetent people with chronic lung diseases like cystic fibrosis, chronic obstructive pulmonary disease, or tuberculosis.

In immunocompromised people, the infection can spread into the blood, causing invasive aspergillosis which can very quickly become fatal.

Key Takeaways

Echinocandins are a class of antifungals, mainly used to treat infections caused by candida species and aspergillus species. They work by disrupting the formation of the fungal cell wall, leading to cell death. They inhibit eta-1,3-D-glucan synthase, an enzyme necessary for the synthesis of major fungal cell components known as Beta glucans. Echinocandins are generally well-tolerated and have a low risk of serious adverse effects.

The most common side effects are facial flushing, nausea, vomiting, and skin rash. Rare but serious side effects include anaphylaxis (a life-threatening allergic reaction) and Stevens-Johnson syndrome (a severe skin reaction).

Sources

  1. "Katzung & Trevor's Pharmacology Examination and Board Review,12th Edition" McGraw-Hill Education / Medical (2018)
  2. "Rang and Dale's Pharmacology" Elsevier (2019)
  3. "Goodman and Gilman's The Pharmacological Basis of Therapeutics, 13th Edition" McGraw-Hill Education / Medical (2017)
  4. "Echinocandins--new antifungal agents" Rev Med Chir Soc Med Nat Iasi (2014)
  5. "Echinocandins in antifungal pharmacotherapy" Journal of Pharmacy and Pharmacology (2017)
  6. "Clinical hepatotoxicity associated with antifungal agents" Expert Opinion on Drug Safety (2016)