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Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Antifungal Agents
Chapter 11
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
How Fungus Differs from Bacteria
• Fungus – Composed of a rigid cell wall made up of chitin and
various polysaccharides, and a cell membrane containing ergosterol.
– Protective layers of the fungal cell make the organism resistant to antibiotics.
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Patients Susceptible to Fungal Infections
• Patients with AIDS and AIDS-related complex (ARC)• Patients taking immunosuppressant drugs• Patients who have undergone transplantation surgery or
cancer treatment• Members of growing elderly population no longer
protected from environmental fungi
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Culture• A culture should be obtained prior to prescribing anti-
fungal agents.• Patients on antifungal agents are typically
immunosuppressed.
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Amphotericin B Indications• Aspergillosis• Leishmaniasis• Cryptococcosis• Blastomycosis• Moniliasis • Coccidioidomycosis• Histoplasmosis• Mucormycosis• Candida infections (topically)
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Amphotericin B• Indications - Progressive potential fatal fungal infections • Pharmacokinetics - IV form, excreted in the urine• Contraindications - Kidney disease• Adverse Reaction - Kidney failure
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Systemic Antifungal Agents• Caspofungin (Cancidas) (IV)
– Approved for the treatment of invasive aspergillosis in patients who are refractory to other treatments
• Flucytosine (Ancobon) (Oral)– Less toxic drug used for the treatment of systemic
infections caused by Candida or Cryptococcus • Nystatin (Mycostatin, Nilstat) (Oral)
– Used for the treatment of intestinal candidiasis; also available in a number of topical preparations
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Voriconazole and Terbinafine• Newer Agents• Voriconazole (Vfend)
– Available in oral and IV forms– Treats invasive aspergillosis and serious infections caused by
Scedosporium apiospermum, or Fuscariium species• Terbinafine (Lamisil)
– Blocks the formation of ergosterol– Inhibits a CYP2D6 enzyme system – Oral drug for the treatment of onychomycosis of the toenail or
fingernail
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Azoles• Newer class of drugs used to treat systemic fungal
infections• Less toxic than amphotericin B• Less effective than amphotericin B
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Question
Please answer the following statement as true or false.
Nystatin, taken orally, is used for the treatment of intestinal candidiasis.
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Answer
True
Rationale: Nystatin (Mycostatin, Nilstat) (Oral) – Used for the treatment of intestinal candidiasis; also
available as a topical preparation.
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Ketoconazole (Nizoral)• Used orally to treat many of the same mycoses as
amphotericin B• Works by blocking the activity of a steroid in the fungal
wall• Has side effect of blocking the activity of human steroids,
including testosterone and cortisol
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Ketoconazole (Nizoral) (cont.)• Pharmacokinetics – Absorbed from the GI tract,
metabolized in the liver, excreted in the feces• Contraindications – Not drug of choice for patients with
endocrine or fertility problems• Adverse Reactions – Hepatic toxicity• Drug-Drug Interactions - Many
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Fluconazole (Diflucan)• Not associated with the endocrine problems seen with
ketoconazole• Used to treat candidiasis, cryptococcal meningitis, and
other systemic fungal infections• Prophylactic agent for reducing the incidence of
candidiasis in bone marrow transplant recipients
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Fluconazole (Diflucan) (cont.)• Pharmacokinetics - Available in oral and IV preparations,
excreted unchanged in the urine.• Contraindications – Renal dysfunction• Adverse Reactions – Liver or renal toxicity • Drug-Drug Interactions – Inhibits CYP450 may be
associated with drug–drug interactions
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Itraconazole (Sporanox)• An oral agent used for the treatment of assorted systemic
mycoses• Associated with hepatic failure• Is slowly absorbed from the GI tract and is metabolized in
the liver by the CYP450 system• Is excreted in the urine and feces
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Site of Action of Antifungals
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Overall Contraindications to Systemic Antifungal Agents
• Patient’s with a known allergy• Pregnant or lactating women (with the exception of
terbinafine for life-threatening infections)• Patients with renal or liver disease
– May alter drug metabolism and excretion. Condition may worsen as a result of drug actions.
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Overall Adverse Reactions to Systemic Antifungal Agents
• CNS Effects – Headache, dizziness, fever, shaking, chills
• GI Effects – Nausea, vomiting, dyspepsia, anorexia
• Hepatic Dysfunction• Dermatological Effects
– Rash and pruritus associated with local irritation• Renal Dysfunction
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Question
Which of the following is considered a contraindication of Ketoconazole ?A. Patients with renal problemsB. Patients with fertility problemsC. Patients with hepatic problemsD. Patients with GI problems
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Answer
B. Patients with fertility problems
Rationale: Contraindications – not drug of choice for patients with endocrine or fertility problems.
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Topical Antifungal Infections• Caused by dermatophytes• Tinea Infections (Ringworm)
– Athlete’s foot (tinea pedis)– Jock itch (tinea cruris)
• Candida– Yeast infections of the mouth and vagina
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Topical Antifungal Agents (cont.)
• Action/Indication– Work to alter the cell permeability of the fungus,
causing prevention of replication and fungal death – Indicated only for local treatment of mycoses,
including tinea infections• Contraindication/Cautions
– Limited to known allergy to any of these drugs
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Topical Antifungal Agents (cont.)• Adverse Effects
– Local effects include irritation, burning, rash, and swelling
– When taken as a suppository or troche: nausea, vomiting, hepatic dysfunction, urinary frequency and burning, and change in sexual activity
• Drug-to-Drug Interactions– No reported drug–drug interactions
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Prototype Antifungal Agent
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Prototype Antifungal Agent
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Prototype Antifungal Agent (Continued)
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Use of Antifungals Across the Life Span
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Nursing Considerations for Systemic Antifungal Agents
• Assessment: History and Physical Exam• Nursing Diagnosis• Implementation• Evaluation
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Nursing Considerations for Topical Antifungal Agents
• Assessment: History and Physical Exam• Nursing Diagnosis• Implementation• Evaluation
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Question
The nurse is caring for a patient with a fungal infection. Which of the following would be considered an adverse effect of an antifungal medication?A. Burning or irritation in the sexual partnerB. Abnormal kidney function testsC. Upper abdominal painD. Urinary retention
Copyright © 2013 Wolters Kluwer Health | Lippincott Williams & Wilkins
Answer
A. Burning or irritation in the sexual partner
Rationale: Adverse effects: Troche: nausea, vomiting, abnormal liver function tests; topical: stinging, redness, urticaria, edema; vaginal: lower abdominal pain, urinary frequency, burning or irritation in the sexual partner