Antifungal p.2

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Questions and Answers

What is the primary function of azole antifungal agents like itraconazole?

Kill bacteria directly

Enhance host immune response

Act as a broad-spectrum antifungal (correct)

Inhibit viral replication

Which of the following conditions is itraconazole considered first-line therapy for?

Bacterial meningitis

Viral pneumonia

Tuberculosis

Blastomycosis (correct)

What serious side effect is associated with itraconazole use?

Severe hypotension

Increased ejection fraction

Hepatic injury (correct)

Hyperkalemia

How does itraconazole exert its antifungal effect?

By inhibiting ergosterol synthesis Signup and view all the answers

Which of the following is NOT a therapeutic use of itraconazole?

Viral infections Signup and view all the answers

What should be monitored in clients taking sulfonylureas with itraconazole?

Blood glucose levels Signup and view all the answers

In which situation should itraconazole NOT be used?

In clients with heart failure Signup and view all the answers

What is the recommended starting dose of itraconazole for most conditions?

200 mg once daily Signup and view all the answers

What effect do proton pump inhibitors have on itraconazole absorption?

They decrease itraconazole absorption Signup and view all the answers

Which of the following is NOT recommended when administering antacids with itraconazole?

Administer antacids with food Signup and view all the answers

What are symptoms of hepatic insufficiency that clients should be educated to recognize?

Persistent nausea and jaundice Signup and view all the answers

Why must coagulation studies be monitored in clients taking warfarin with itraconazole?

Excessive anticoagulation can occur Signup and view all the answers

What is a common drug that itraconazole can increase the levels of, raising concerns about ventricular dysrhythmias?

Cisapride Signup and view all the answers

What is a significant advantage of using itraconazole compared to amphotericin B?

It can be administered orally. Signup and view all the answers

Which of the following systemic fungal infections is itraconazole NOT considered first-line therapy for?

Cryptococcosis Signup and view all the answers

What is one of the key mechanisms by which itraconazole exerts its antifungal effect?

Inhibits ergosterol synthesis. Signup and view all the answers

Which of the following side effects is associated with itraconazole?

Transient decrease in ejection fraction Signup and view all the answers

What is a potential serious consequence of hepatic injury associated with itraconazole?

Hepatic failure resulting in fatalities. Signup and view all the answers

What is a critical reason for using caution with itraconazole in specific clients?

Clients with hepatic dysfunction. Signup and view all the answers

Which drug interaction poses a significant risk for clients taking itraconazole?

Development of fatal ventricular dysrhythmias. Signup and view all the answers

How should proton pump inhibitors be timed in relation to itraconazole administration?

At least 1 hour before or 2 hours after itraconazole. Signup and view all the answers

What is the recommended monthly starting dose of itraconazole for most indications?

200 mg once daily. Signup and view all the answers

Which of the following symptoms indicates hepatic insufficiency that clients should be educated to recognize?

Persistent nausea and dark urine. Signup and view all the answers

What effect do antacids have on the absorption of oral itraconazole?

They reduce the absorption. Signup and view all the answers

Which lab value should be monitored in clients taking sulfonylureas with itraconazole?

Blood glucose levels. Signup and view all the answers

What is the potential impact of itraconazole on coagulation studies for clients on warfarin?

It may cause excessive anticoagulation. Signup and view all the answers

What unique feature of azole antifungal agents like itraconazole sets them apart from amphotericin B?

They can be given orally and have lower toxicity. Signup and view all the answers

Which condition is NOT considered a primary indication for the use of itraconazole?

Hepatitis Signup and view all the answers

What is one of the side effects associated with the use of itraconazole?

Transient decrease in ejection fraction Signup and view all the answers

Which mechanism of action describes how itraconazole works to combat fungal infections?

Inhibits ergosterol synthesis Signup and view all the answers

What common gastrointestinal side effect is associated with itraconazole?

Nausea Signup and view all the answers

In which situation should caution be exercised when prescribing itraconazole?

Clients with hepatic dysfunction Signup and view all the answers

What is the recommended dosing protocol for itraconazole if a clinician deems it necessary?

200 mg once daily, increasing to 200 mg twice daily if needed Signup and view all the answers

Which drug interaction poses a significant risk for clients taking itraconazole?

CYP3A4 substrates Signup and view all the answers

What effect do antacids have on the absorption of itraconazole?

They reduce the absorption of itraconazole Signup and view all the answers

What monitoring is essential for clients taking itraconazole with warfarin?

PT/INR levels Signup and view all the answers

What should clients be taught about potential symptoms of hepatic insufficiency?

Dark urine, jaundice, and fatigue Signup and view all the answers

When should proton pump inhibitors be administered in relation to itraconazole?

At least 1 hour before itraconazole or 2 hours after Signup and view all the answers

Which of the following medications may have increased levels due to itraconazole's action?

Cisapride Signup and view all the answers

Which of the following is a distinguishing characteristic of itraconazole compared to amphotericin B?

It can be taken orally. Signup and view all the answers

What is the primary mechanism by which itraconazole disrupts fungal cells?

Blocking ergosterol production. Signup and view all the answers

Which systemic fungal infection is itraconazole recommended as first-line therapy?

Histoplasmosis Signup and view all the answers

What is a notable adverse reaction associated with itraconazole use?

Hepatic injury Signup and view all the answers

In which circumstance should itraconazole be used cautiously?

In patients with hepatitis Signup and view all the answers

What is the recommended approach to administering proton pump inhibitors in relation to itraconazole?

Administer them at least 1 hour before or 2 hours after itraconazole. Signup and view all the answers

Which client condition warrants caution when administering itraconazole?

Hepatic dysfunction. Signup and view all the answers

Which of the following symptoms is indicative of hepatic insufficiency that clients should be educated to recognize?

Jaundice. Signup and view all the answers

What potential risk is associated with combining itraconazole and cisapride?

Heightened risk of fatal ventricular dysrhythmias. Signup and view all the answers

What is the standard recommended dose of itraconazole for most conditions?

200 mg once daily. Signup and view all the answers

Which of the following drugs is affected by the CYP3A4 inhibition caused by itraconazole?

Warfarin. Signup and view all the answers

What should clients taking sulfonylureas with itraconazole be monitored for?

Hypoglycemia. Signup and view all the answers

What is a significant contraindication for using itraconazole?

Use in clients with heart failure. Signup and view all the answers

Study Notes

Azole Antifungal Agents

Itraconazole (Sporanox) is an azole antifungal agent.
Azoles are broad-spectrum antifungal drugs, similar to amphotericin B.
Itraconazole offers an alternative to amphotericin B for systemic mycoses.
Azoles have lower toxicity than amphotericin B and can be administered orally.

Mechanism of Action

Itraconazole inhibits ergosterol synthesis, a sterol crucial for fungal cell membrane integrity.
This inhibition leads to increased membrane permeability and leakage of cellular components, ultimately causing fungal cell death.

Indications and Therapeutic Uses

Itraconazole is effective against a wide range of fungal pathogens causing systemic infections.
It is considered first-line therapy for blastomycosis, histoplasmosis, paracoccidioidomycosis, and sporotrichosis.
It's an alternative to amphotericin B for treating aspergillosis, candidiasis, and coccidioidomycosis.
Itraconazole can also treat superficial mycoses.

Side Effects and Adverse Reactions

Common side effects include gastrointestinal upset, such as nausea, vomiting, and diarrhea.
Itraconazole has a negative inotropic effect, potentially causing a transient decrease in ejection fraction.
Rare but severe adverse reactions include hepatic injury, which can lead to fatalities.

Precautions and Contraindications

Use caution in patients with hepatic dysfunction.
Exercise caution in patients with heart failure, weighing the benefits against the risks.
Black Box Warning: Itraconazole is contraindicated for treating superficial mycoses in patients with heart failure, a history of heart failure, or evidence of ventricular dysfunction.

Drug Interactions

Proton pump inhibitors can reduce itraconazole absorption due to prolonged duration of action and decreased stomach acid content.
Itraconazole is a CYP3A4 inhibitor, which can raise levels of various drugs, including cisapride, pimozide, dofetilide, and quinidine, potentially increasing the risk of fatal ventricular dysrhythmias.
Other drugs affected by CYP3A4 inhibition include cyclosporine, digoxin, warfarin, and sulfonylureas.
Drugs that increase gastric pH, such as antacids, H2 antagonists, and proton pump inhibitors, can decrease oral itraconazole absorption. Administer these agents at least 1 hour before or 2 hours after itraconazole.

Dosing, Administration, & Client Teaching

Dosing varies based on the infection, severity, and patient response.
Check drug dosing guidelines for individualized dosing.
Itraconazole comes in oral suspension (10mg/ml) and capsules (100mg).
Capsules should be taken with food or cola, as cola enhances absorption.
The recommended dose is 200mg once daily, potentially increased to 200mg twice daily if needed.

Administration

Administered orally.

Client Teaching

Educate patients about signs of hepatic insufficiency (persistent nausea, anorexia, fatigue, vomiting, right upper quadrant pain, jaundice, dark urine, pale stools) and advise immediate medical attention if they occur.

Labs to Monitor

Basic Metabolic Panel: Monitor blood glucose levels in patients taking sulfonylureas with itraconazole, as hypoglycemia can occur.
Coagulation Studies: Monitor PT/INR for patients taking warfarin with itraconazole, as excessive anticoagulation can occur.
Serum Drug Levels: Monitor drug levels of cyclosporine and digoxin in patients also taking itraconazole.

Azole Antifungal Agents

Prototype: itraconazole (Sporanox)
Function: Broad-spectrum antifungal drugs, providing an alternative to amphotericin B.
Unique Features: Lower toxicity than amphotericin B and can be administered orally.

Mechanism of Action

Itraconazole: Inhibits the synthesis of ergosterol, a key component of fungal cell membranes. This disrupts membrane integrity, leading to leakage of cellular components.

Indications and Therapeutic Uses

Systemic Fungal Infections: Effective against a range of fungal pathogens, including blastomycosis, histoplasmosis, paracoccidioidomycosis, and sporotrichosis.
Superficial Fungal Infections: Can also treat superficial mycoses.

Side Effects and Adverse Reactions

GI Upset: Nausea, vomiting, and diarrhea are common side effects.
Cardiac Suppression: Transient decrease in ejection fraction due to negative inotropic action.
Hepatic Injury: Rare cases of hepatic failure, potentially fatal.

Precautions and Contraindications

Hepatic Dysfunction: Use with caution in clients with liver issues.
Heart Failure: Use with caution as itraconazole can worsen heart failure.
Black Box Warning: Not recommended for superficial mycoses in clients with heart failure or ventricular dysfunction.

Drug Interactions

Proton Pump Inhibitors: May reduce itraconazole absorption due to decreased gastric acidity.
CYP3A4 Inhibitor: Increases levels of other drugs metabolized by CYP3A4, like cisapride, pimozide, dofetilide, and quinidine, increasing the risk of fatal ventricular dysrhythmias.
Gastric pH Elevators: Antacids, H2 antagonists, and proton pump inhibitors can reduce oral itraconazole absorption. Administer these drugs at least 1 hour before or 2 hours after itraconazole.

Dosing, Administration, & Client Teaching

Dosing: Varies based on the condition, severity, and individual client. Consult drug dosing guidelines for specific dosages.
Administration: Oral administration. Capsules should be taken with food or cola for enhanced absorption.
Client Teaching: Educate clients about signs of hepatic insufficiency (nausea, fatigue, vomiting, abdominal pain, jaundice, dark urine, pale stools) and seek immediate medical attention if these symptoms occur.

Labs to Monitor

Basic Metabolic Panel: Monitor blood glucose levels in clients taking sulfonylureas alongside itraconazole to prevent hypoglycemia.
Coagulation Studies: Monitor PT/INR in clients taking warfarin alongside itraconazole to prevent excessive anticoagulation.
Serum Drug Levels: Monitor cyclosporine and digoxin levels in clients taking itraconazole as well, due to potential drug interactions.

Azole Antifungal Agent

Itraconazole is a broad-spectrum antifungal drug in the Azole class.
Itraconazole is an alternative to amphotericin B for treating systemic mycoses.
Itraconazole is less toxic than amphotericin B and can be taken orally.

Mechanism of Action

Itraconazole inhibits ergosterol synthesis, leading to increased membrane permeability and leakage of cell components.

Indications and Therapeutic Uses

Itraconazole is effective against a wide range of fungal pathogens.
First-line therapy for blastomycosis, histoplasmosis, paracoccidioidomycosis, and sporotrichosis.
Alternative to amphotericin B for aspergillosis, candidiasis, and coccidioidomycosis.
Treats superficial mycoses.

Side Effects and Adverse Reactions

Nausea, vomiting, and diarrhea are common gastrointestinal side effects.
Itraconazole can cause a temporary decrease in left ventricular ejection fraction.
Rare cases of hepatic failure with fatal outcomes have been reported.

Precautions and Contraindications

Use with caution in patients with liver dysfunction.
Use with caution in heart failure, weighing benefits against risks.
Black Box Warning: Do not use for superficial mycoses in patients with heart failure, history of heart failure, or ventricular dysfunction.

Drug Interactions

Proton pump inhibitors may reduce itraconazole absorption due to prolonged action and decreased stomach acid.
Itraconazole inhibits CYP3A4 and can increase levels of several drugs including cisapride, pimozide, dofetilide, and quinidine, potentially leading to fatal ventricular dysrhythmias.
Other drugs affected by CYP3A4 inhibition include cyclosporine, digoxin, warfarin, and sulfonylureas.
Antacids, H2 antagonists, and proton pump inhibitors can reduce oral itraconazole absorption. Administer these agents at least 1 hour before or 2 hours after itraconazole.

Dosing, Administration, & Client Teaching

Dosage varies depending on the condition, severity, and patient response.
Itraconazole is available orally as a suspension (10mg/ml) and capsules (100mg).
Capsules should be taken with food or cola (Cola enhances absorption)
Recommended dose is 200mg once daily, increasing to 200mg twice daily if needed.
Educate patients about symptoms of hepatic insufficiency (persistent nausea, anorexia, fatigue, vomiting, RUQ pain, jaundice, dark urine, pale stools), seeking immediate medical attention if these occur.

Labs to Monitor

Basic Metabolic Panel: Monitor blood glucose levels in patients taking sulfonylureas with itraconazole, as hypoglycemia can occur.
Coagulation Studies: Monitor PT/INR in patients taking warfarin with itraconazole to prevent excessive anticoagulation.
Serum Drug Levels: Monitor drug levels of cyclosporine and digoxin in patients taking itraconazole.

Azole Antifungal Agents

Itraconazole (Sporanox) is a prototype drug in the azole antifungal agent class.
Itraconazole is a broad-spectrum antifungal drug that provides an alternative to amphotericin B for treating systemic mycoses.
Azoles have lower toxicity than amphotericin B and can be administered orally.

Mechanism of Action

Itraconazole inhibits the synthesis of ergosterol, a key component of fungal cell membranes.
This inhibition leads to increased membrane permeability and leakage of cellular components, ultimately killing the fungus.

Indications and Therapeutic Uses

Itraconazole is used to treat a broad range of systemic fungal infections including blastomycosis, histoplasmosis, paracoccidioidomycosis, and sporotrichosis.
It is an alternative to amphotericin B for treating aspergillosis, candidiasis, and coccidioidomycosis.
Itraconazole can also be used to treat superficial fungal infections.

Side Effects and Adverse Reactions

GI Upset: Common side effects include nausea, vomiting, and diarrhea.
Cardiac Suppression: Itraconazole can cause a transient decrease in ejection fraction due to its negative inotropic action.
Hepatic Injury: Rare but serious cases of hepatic failure, including fatalities, have been reported.

Precautions and Contraindications

Use caution in clients with hepatic dysfunction.
Use with caution in clients with heart failure, only when the benefit outweighs the risk.
Black Box Warning: Itraconazole should not be used to treat superficial mycoses in clients with heart failure, a history of heart failure, or other indications of ventricular dysfunction.

Drug Interactions

Proton Pump Inhibitors: May reduce itraconazole absorption due to decreased stomach acid content.
CYP3A4 Inhibitors: Itraconazole inhibits CYP3A4, which can increase levels of many other drugs, including cisapride, pimozide, dofetilide, and quinidine, increasing the risk of fatal ventricular dysrhythmias. Other drugs affected by CYP3A4 inhibition include cyclosporine, digoxin, warfarin, and sulfonylureas.
Drugs That Raise Gastric pH: Antacids, H2 antagonists, and proton pump inhibitors can reduce oral itraconazole absorption. Administer these agents at least 1 hour before itraconazole or 2 hours after.

Dosing, Administration, & Client Teaching

Dosing varies based on the condition, severity, and client response.
Consult drug dosing guidelines for individualized dosing.
Available for PO use in suspension (10mg/ml) and capsules (100 mg).
Capsules should be taken with food or cola (cola enhances absorption).
The recommended dose is 200 mg once daily, and can be increased to 200 mg twice daily if needed.
Client Teaching: Educate clients about symptoms of hepatic insufficiency, including persistent nausea, anorexia, fatigue, vomiting, RUQ pain, jaundice, dark urine, and pale stools. Seek medical attention immediately if these symptoms occur.

Labs to Monitor

Basic Metabolic Panel: Monitor blood glucose levels in clients taking sulfonylureas with itraconazole, as hypoglycemia can occur.
Coagulation Studies: Monitor PT/INR for clients taking warfarin with itraconazole, as excessive anticoagulation can occur.
Serum Drug Levels: Monitor drug levels of cyclosporine and digoxin for clients also taking itraconazole.

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