Polyenes are a class of antifungal agents that are primarily used to treat serious fungal infections. They are characterized by their large macrocyclic structures containing multiple conjugated double bonds ("polyene" chains), which is the origin of their name.
The main mechanism of action of polyenes is binding to ergosterol, a key component of fungal cell membranes. This binding disrupts the membrane's integrity, creating pores that lead to leakage of cellular contents and ultimately cell death. Due to their selectivity for ergosterol (which is absent in human cells that contain cholesterol instead), polyenes exhibit fungicidal activity with relatively low toxicity to human cells.
The most well-known polyene antifungal is Amphotericin B, often referred to as the "gold standard" for treating systemic fungal infections. Other examples include Nystatin and Natamycin, which are mainly used for topical infections.
Despite their effectiveness, polyenes can have notable side effects, particularly nephrotoxicity (especially with Amphotericin B), which has led to the development of lipid formulations to reduce toxicity.
Indications:
Used to treat serious systemic fungal infections, including:
Systemic candidiasis
Blastomycosis
Histoplasmosis
Coccidioidomycosis
Invasive fungal infections in immunocompromised patients (e.g., HIV/AIDS, cancer)
---
2. Nystatin (Mycostatin, Nilstat):
Indications:
Used for topical and mucosal fungal infections caused by Candida species, such as:
Oral thrush (oral candidiasis)
Cutaneous candidiasis (skin infections)
Vaginal candidiasis
Note: Nystatin is not absorbed systemically, so it's only used for local infections.
---
3. Natamycin (Natacyn):
Indications:
Used for fungal eye infections, including:
Fungal keratitis (corneal infection)
Fungal conjunctivitis
Effective against fungi like Fusarium and Aspergillus.
1. Amphotericin B
Common Side Effects:
Nephrotoxicity (kidney damage) – most serious and common
Fever, chills, rigors (especially during infusion)
Hypokalemia (low potassium)
Hypomagnesemia (low magnesium)
Anemia (due to decreased erythropoietin production)
Thrombophlebitis (inflammation at IV site)
Hypotension
Note: Lipid formulations (like Ambisome) reduce nephrotoxicity and infusion-related reactions.
---
2. Nystatin
Common Side Effects:
Generally well tolerated because it's not absorbed systemically
Oral form:
Nausea
Vomiting
Diarrhea
Topical form:
Skin irritation
Burning or itching sensation
Allergic reactions (rare)
---
3. Natamycin
Common Side Effects (eye drops):
Eye irritation or discomfort
Blurred vision (temporary)
Redness or tearing
Allergic reactions (rare)
1.Amphotricin B
Precautions:
Monitor renal function closely (serum creatinine, BUN)
Regularly check electrolytes (especially potassium and magnesium)
Monitor for anemia (complete blood count)
Use with caution in patients with renal impairment or those taking other nephrotoxic drugs
Pre-medication with antipyretics, antihistamines, or corticosteroids may be needed to reduce infusion-related reactions
Contraindications:
Known hypersensitivity to Amphotericin B or any component of the formulation
Use with caution during pregnancy (Category B – considered safe if clearly needed)
---
2. Nystatin
Precautions:
Topical use only – do not use systemically
Use oral form carefully in patients with gastrointestinal disorders
Avoid contact with eyes (when used as a cream or ointment)
Prolonged use may lead to fungal resistance
Contraindications:
Known allergy or hypersensitivity to nystatin or any formulation ingredients
---
3. Natamycin
Precautions:
For ophthalmic use only – not for injection or systemic use
May cause temporary blurred vision, so caution is advised when driving or operating machinery
Use with care in patients with hypersensitive eyes or pre-existing ocular conditions
Remove contact lenses before application
Contraindications:
Hypersensitivity to natamycin or any component of the formulation
References:
1. Katzung, B. G., Trevor, A. J. (2021).
Basic and Clinical Pharmacology (15th ed.). McGraw Hill Education.
– Chapter on Antifungal Agents.
2. Goodman & Gilman’s: The Pharmacological Basis of Therapeutics (13th ed.)
– Comprehensive reference for mechanisms, side effects, and pharmacokinetics of antifungals.
3. Lexicomp Drug Monographs
– Up-to-date clinical drug information including indications, side effects, and precautions.
4. Micromedex (IBM Watson)
– Clinical decision support resource for healthcare professionals.
5. AHFS Drug Information (American Society of Health-System Pharmacists)
– Trusted source for evidence-based drug monographs.
6. Drugs.com & Medscape Drug Reference
– Easy-to-access online drug information for students and professionals.
7. World Health Organization (WHO) Model List of Essential Medicines