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Antifungal Treatment

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Information about Antifungal Treatment

Published on September 2, 2007

Author: girlie

Source: slideshare.net

Description

Antifungal Treatment
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Antifungal Treatment

Fungi for generalists Superficial (skin, nails, oral, vaginal) Very common in otherwise healthy people Frequent episodes suggest interference with immune defenses as in diabetes, antibiotic Rx Systemic rare except in severely immune- compromised

Superficial (skin, nails, oral, vaginal)

Very common in otherwise healthy people

Frequent episodes suggest interference with immune defenses as in diabetes, antibiotic Rx

Systemic

rare except in severely immune- compromised

Antifungals Lamisil Terbinafine Allylamine Triazoles Imidazoles SUBCLASS Griseofulvin Fluconazole Itraconazole Ketoconazole GENERIC Grisactin Fulvicin Gris-PEG Griseofulvin Diflucan Sporanox Nizoral Azoles TRADE CLASS

General Indications Ketaconazole Systemic fungal infections (candidiasis, blastomycosis, coccidioidomycosis, histoplasmosis) Severe recalcitrant dermatophyte infections unresponsive to topical Fluconazole Candidiasis, including vaginal Cryptococcal meningitis Itraconazole Blastomycosis, histoplasmosis, apergillosis Onychomycosis Terbinafine Onychomycosis Griseofulvin Tinea infections of skin, hair, nails unresponsive to topical NOT candidiasis, blastomycosis, coccidioidomycosis, histoplasmosis

Ketaconazole

Systemic fungal infections (candidiasis, blastomycosis, coccidioidomycosis, histoplasmosis)

Severe recalcitrant dermatophyte infections unresponsive to topical

Fluconazole

Candidiasis, including vaginal

Cryptococcal meningitis

Itraconazole

Blastomycosis, histoplasmosis, apergillosis

Onychomycosis

Terbinafine

Onychomycosis

Griseofulvin

Tinea infections of skin, hair, nails unresponsive to topical

NOT candidiasis, blastomycosis, coccidioidomycosis, histoplasmosis

Azoles: Patient Variables Geriatrics More susceptible to hepatotoxicity Require lower dosing in reduced renal function Pediatrics S&E NOT established Pregnancy Category C: Benefit > risk to fetus Lactation Excreted in breast milk. Do NOT use in nursing women.

Geriatrics

More susceptible to hepatotoxicity

Require lower dosing in reduced renal function

Pediatrics

S&E NOT established

Pregnancy

Category C: Benefit > risk to fetus

Lactation

Excreted in breast milk. Do NOT use in nursing women.

Azoles: Monitoring Assess LFTs prior to initiating Tx and periodically (baseline & Q2wk x 2 mo, then Q1-2 mo) Assess for s/s of hepatitis Fatigue, anorexia, N/V, jaundice, dark urine, pale stools Assess for interference with steroidgenesis High-dose ketoconazole: adrenal suppression High-dose itraconazole: hypokalemia & secondary V-fib Assess response to Tx with repeat cultures

Assess LFTs prior to initiating Tx and periodically (baseline & Q2wk x 2 mo, then Q1-2 mo)

Assess for s/s of hepatitis

Fatigue, anorexia, N/V, jaundice, dark urine, pale stools

Assess for interference with steroidgenesis

High-dose ketoconazole: adrenal suppression

High-dose itraconazole: hypokalemia & secondary V-fib

Assess response to Tx with repeat cultures

Azoles: Patient Education Food enhances absorption of itraconazole, variably affects ketoconazole, no effect on fluconazole Administer antacids, H2-blockers, proton pump inhibitors, or anticholinergics at least 2 hours after ketoconazole or itraconazole Immediately report any s/s of hepatitis Fatigue, anorexia, N/V, jaundice, dark urine, pale stools Take as prescribed. Inadequate treatment  poor response or early recurrence of symptoms Women of childbearing age: USE CONTRACEPTION OR ABSTINENCE

Food enhances absorption of itraconazole, variably affects ketoconazole, no effect on fluconazole

Administer antacids, H2-blockers, proton pump inhibitors, or anticholinergics at least 2 hours after ketoconazole or itraconazole

Immediately report any s/s of hepatitis

Fatigue, anorexia, N/V, jaundice, dark urine, pale stools

Take as prescribed. Inadequate treatment  poor response or early recurrence of symptoms

Women of childbearing age: USE CONTRACEPTION OR ABSTINENCE

Ketoconazole Contraindications Hypersensitivity Fungal meningitis (poor CNS penetration) Use with Propulsid  serious cardiac arrhythmias Warnings / Precautions Hepatic toxicity: clinically significant / fatal hepatitis  D/C immediately if s/s, effects usually reversible may take weeks to months Steroidgenesis: directly inhibit adrenal cortisol and testosterone synthesis  low sperm counts, decreased libido, impotence, gynecomastia, menstrual irregularities Hypersensitivity & anaphylaxis Weak bases require gastric acidity for dissolution/absorption  do NOT take with antacids, anticholinergics, or H2-blockers

Contraindications

Hypersensitivity

Fungal meningitis (poor CNS penetration)

Use with Propulsid  serious cardiac arrhythmias

Warnings / Precautions

Hepatic toxicity: clinically significant / fatal hepatitis  D/C immediately if s/s, effects usually reversible may take weeks to months

Steroidgenesis: directly inhibit adrenal cortisol and testosterone synthesis  low sperm counts, decreased libido, impotence, gynecomastia, menstrual irregularities

Hypersensitivity & anaphylaxis

Weak bases require gastric acidity for dissolution/absorption  do NOT take with antacids, anticholinergics, or H2-blockers

Ketoconazole: Pharmacokinetics Bioavailability varies depending on gastric pH Ketoconazole absorption variable with food Itraconazole 2-3 x greater bioavailability with food esp lipids Hypochlohydria in AIDS  decreased bioavailability

Bioavailability varies depending on gastric pH

Ketoconazole absorption variable with food

Itraconazole 2-3 x greater bioavailability with food esp lipids

Hypochlohydria in AIDS  decreased bioavailability

Ketoconazole Adverse Effects Mild / transient – don’t require D/C Most common: N/V Drug Interactions Least favorable toxicity profile Inhibits P450 3A4, also inhibits 1A2, 2C, 3A4 Propulsid  serious cardiac arrhythmias Do NOT take with antacids, anticholinergics, or H2-blockers  decreases bioavailability

Adverse Effects

Mild / transient – don’t require D/C

Most common: N/V

Drug Interactions

Least favorable toxicity profile

Inhibits P450 3A4, also inhibits 1A2, 2C, 3A4

Propulsid  serious cardiac arrhythmias

Do NOT take with antacids, anticholinergics, or H2-blockers  decreases bioavailability

Triazole Indications Oropharyngeal & esophogeal candidiasis Single dose Tx of vulvovaginal candidiasis Contraindications Hypersensitivity Warnings / Precautions Hepatotoxicity Allergic / Dermatologic reaction – anaphylaxis & exfoliative dermatitis (rare) Dose reduction for renal dysfunction Use care in use with elderly

Indications

Oropharyngeal & esophogeal candidiasis

Single dose Tx of vulvovaginal candidiasis

Contraindications

Hypersensitivity

Warnings / Precautions

Hepatotoxicity

Allergic / Dermatologic reaction – anaphylaxis & exfoliative dermatitis (rare)

Dose reduction for renal dysfunction

Use care in use with elderly

Triazoles: Pharmacokinetics Absorption & bioavailability NOT affected by food or gastric pH Excreted renally with therapeutic concentrations achieved in urine UNIQUE among azoles in that it crosses the blood-brain barrier & has good CSF penetration

Absorption & bioavailability NOT affected by food or gastric pH

Excreted renally with therapeutic concentrations achieved in urine

UNIQUE among azoles in that it crosses the blood-brain barrier & has good CSF penetration

Triazoles Pediatrics S&E NOT established Adverse Effects Most Common (single dose): headache, nausea, abdominal pain, diarrhea, dyspepsia, dizziness Most Common (multidose): nausea, headache, skin rash, vomiting, abdominal pain, diarrhea SERIOUS: seizures, exfoliative skin disorders, leukopenia, thrombocytopenia, serious hepatic reactions

Pediatrics

S&E NOT established

Adverse Effects

Most Common (single dose): headache, nausea, abdominal pain, diarrhea, dyspepsia, dizziness

Most Common (multidose): nausea, headache, skin rash, vomiting, abdominal pain, diarrhea

SERIOUS: seizures, exfoliative skin disorders, leukopenia, thrombocytopenia, serious hepatic reactions

Triazoles Drug Interactions P450 2C and 3A4 inhibitor Decreases blood levels of OCPs Overdose Gastric lavage & hemodialysis

Drug Interactions

P450 2C and 3A4 inhibitor

Decreases blood levels of OCPs

Overdose

Gastric lavage & hemodialysis

Itraconazole (Sporonox) Indications Wide spectrum of antifungal activity Contraindications Coadministration with propulsid & halcion Use with caution in patients with hypersensitivity to to other azoles Warnings / Precautions Obtain culture prior to Tx Hepatitis – monitor hepatic enzymes HIV – decreased absorption of drug Absorption decreased with decreased gastric acidity

Indications

Wide spectrum of antifungal activity

Contraindications

Coadministration with propulsid & halcion

Use with caution in patients with hypersensitivity to to other azoles

Warnings / Precautions

Obtain culture prior to Tx

Hepatitis – monitor hepatic enzymes

HIV – decreased absorption of drug

Absorption decreased with decreased gastric acidity

Itraconazole (Sporonox) Pharmacokinetics Reduced absorption with decreased stomach acidity Therapeutic concentrations may persist in fingernails & toenails for up to 6 mo after D/C Adverse Effects Greater specificity for P450 3A4 enzyme system Overdose NOT removed by dialysis Gastric lavage & sodium bicarbonate

Pharmacokinetics

Reduced absorption with decreased stomach acidity

Therapeutic concentrations may persist in fingernails & toenails for up to 6 mo after D/C

Adverse Effects

Greater specificity for P450 3A4 enzyme system

Overdose

NOT removed by dialysis

Gastric lavage & sodium bicarbonate

Terbinafine Contraindications Hypersensitivity Warnings Hepatic failure: worse in Hx of liver disease Assess liver function BEFORE prescribing Ophthalmic: changes in ocular lens & retina Neutropenia: reversible if D/C’d Dermatologic: SJS, toxic epidermal necrolysis Renal: do not use with significant renal impairment

Contraindications

Hypersensitivity

Warnings

Hepatic failure: worse in Hx of liver disease Assess liver function BEFORE prescribing

Ophthalmic: changes in ocular lens & retina

Neutropenia: reversible if D/C’d

Dermatologic: SJS, toxic epidermal necrolysis

Renal: do not use with significant renal impairment

Griseofulvin Indications Tinea infections of skin, hair, nails Contraindications Hypersensitivity (5-7%) Hepatocellular failure Porphyria

Indications

Tinea infections of skin, hair, nails

Contraindications

Hypersensitivity (5-7%)

Hepatocellular failure

Porphyria

Griseofulvin: Warnings/Precautions Hypersensitivity (5-7%) Skin rash, urticaria, angioneurotic edema  D/C Prophylaxis S&E NOT established Prolonged therapy Monitor renal, hepatic, hematopietic function periodically PCN cross sensitivity Derived from PCN Lupus erythematosus Exacerbation or lupuslike syndromes Photosensitivity Use sunblock & protective clothing

Hypersensitivity (5-7%)

Skin rash, urticaria, angioneurotic edema  D/C

Prophylaxis

S&E NOT established

Prolonged therapy

Monitor renal, hepatic, hematopietic function periodically

PCN cross sensitivity

Derived from PCN

Lupus erythematosus

Exacerbation or lupuslike syndromes

Photosensitivity

Use sunblock & protective clothing

Griseofulvin Pharmacokinetics Better absorption when taken with meals high in fat content Variable GI absorption Peak: 4 hrs Pediatrics May produce estrogen-like effects in children: enlarged breasts, hyperpigmentation of areola, nipple & external genitalia Pregnancy Category C: embryotoxic & teratogenic Monitor Baseline & periodic: renal, liver, hematopoietic function

Pharmacokinetics

Better absorption when taken with meals high in fat content

Variable GI absorption

Peak: 4 hrs

Pediatrics

May produce estrogen-like effects in children: enlarged breasts, hyperpigmentation of areola, nipple & external genitalia

Pregnancy

Category C: embryotoxic & teratogenic

Monitor

Baseline & periodic: renal, liver, hematopoietic function

Griseofulvin Adverse Effects Common: hypersensitivity – skin rashes, urticaria, angioneurotic edema (rare) Oral thrush, N/V, epigastric distress, diarrhea, headache, fatigue, dizziness, insomnia, mental confusion, impairment of performance of routine acitivities High dose or prolonged Tx: interference with porphyrin metabolism, proteinuria, leukopenia, hepatic toxicity, GI bleed, menstrual irregularities, paresthesias of hands and feet, granulocytopenia Drug Interactions NOT metabolized by P450 Decreases activity of OCPs & anticoagulants

Adverse Effects

Common: hypersensitivity – skin rashes, urticaria, angioneurotic edema (rare)

Oral thrush, N/V, epigastric distress, diarrhea, headache, fatigue, dizziness, insomnia, mental confusion, impairment of performance of routine acitivities

High dose or prolonged Tx: interference with porphyrin metabolism, proteinuria, leukopenia, hepatic toxicity, GI bleed, menstrual irregularities, paresthesias of hands and feet, granulocytopenia

Drug Interactions

NOT metabolized by P450

Decreases activity of OCPs & anticoagulants

Griseofulvin: Pt Education Bioavailability improves when given with food Headaches disappear with continued Tx or taken with food Continue for entire course of Tx – effects not immediately noticeable Photosensitivity – avoid prolonged exposure to sunlight or sunlamps; use sun block and protective clothing Notify provider of rash or sore throat May potentiate effects of alcohol

Bioavailability improves when given with food

Headaches disappear with continued Tx or taken with food

Continue for entire course of Tx – effects not immediately noticeable

Photosensitivity – avoid prolonged exposure to sunlight or sunlamps; use sun block and protective clothing

Notify provider of rash or sore throat

May potentiate effects of alcohol

Fungi Morphology Yeast Unicellular fungi Typically round or oval Reproduce by budding May form pseudohyphae (long chains) Molds Multicellular colonies composed of tubular structures (hyphae) Grow by branching & longitudinal extension Dimorphism Fungi may be yeast or mold depending on env conditions

Yeast

Unicellular fungi

Typically round or oval

Reproduce by budding

May form pseudohyphae (long chains)

Molds

Multicellular colonies composed of tubular structures (hyphae)

Grow by branching & longitudinal extension

Dimorphism

Fungi may be yeast or mold depending on env conditions

Mycosis Presence of parasitic fungi in or on the body Most pathogenic fungi are yeast, are nonmotile, and are nontransmissible May be superficial, subcutaneous, or deeply invasive Fungi are eukaryocytes like mammalian cells Key difference b/w is the sterol used to make the cell membrane Fungi: ergosterol VS. Mammals: cholesterol Mechanism of action = interaction with / inhibition of ergosterol synthesis

Presence of parasitic fungi in or on the body

Most pathogenic fungi are yeast, are nonmotile, and are nontransmissible

May be superficial, subcutaneous, or deeply invasive

Fungi are eukaryocytes like mammalian cells

Key difference b/w is the sterol used to make the cell membrane

Fungi: ergosterol VS. Mammals: cholesterol

Mechanism of action = interaction with / inhibition of ergosterol synthesis

Mechanisms of Action Azoles Fungistatic (vs. fungicidal) Inhibition of ergosterol synthesis  cell membranes becomes more permeable & leak cell contents  inhibits cell growth & replication Griseofulvin Deposited in keratin of diseased tissue making it resistant to fungal infection Diseased tissue gradually exfoliated & replaced with healthy tissue

Azoles

Fungistatic (vs. fungicidal)

Inhibition of ergosterol synthesis  cell membranes becomes more permeable & leak cell contents  inhibits cell growth & replication

Griseofulvin

Deposited in keratin of diseased tissue making it resistant to fungal infection

Diseased tissue gradually exfoliated & replaced with healthy tissue

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