ITROSPIN-100 Capsules

Itraconazole BP 100 mg

ITROSPIN-100 is a prescription antifungal capsule containing Itraconazole BP 100 mg. Itraconazole is a triazole antifungal medicine used for the treatment of susceptible fungal infections involving the skin, nails and other sites, depending on the infection and the physician’s diagnosis.

The product artwork specifies HPMC capsules, with 100 mg itraconazole per capsule and a pack of 10 × 10 capsules.

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1. Product Information

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2. What is ITROSPIN-100 Used For?

ITROSPIN-100 contains itraconazole, a systemic antifungal agent.

Depending on the diagnosis and the susceptible organism, itraconazole may be used for fungal infections such as:

• Dermatophytosis
• Tinea corporis
• Tinea cruris
• Tinea pedis
• Tinea manuum
• Certain nail fungal infections
• Certain mucocutaneous fungal infections
• Certain systemic fungal infections

The appropriate indication depends on the causative organism, site of infection, severity and current prescribing information.

Itraconazole should not be used simply because a skin lesion appears fungal; appropriate clinical diagnosis is important.

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3. How Does Itraconazole Work?

Itraconazole belongs to the triazole class of antifungal medicines.

It inhibits the fungal enzyme lanosterol 14-alpha-demethylase, which is involved in the synthesis of ergosterol.

Ergosterol is an important component of the fungal cell membrane.

Mechanism:

Itraconazole
↓
Inhibits fungal CYP450-dependent 14-alpha-demethylase
↓
Reduced ergosterol synthesis
↓
Disruption of fungal cell membrane
↓
Inhibition of fungal growth

This mechanism gives itraconazole activity against a range of susceptible fungal organisms.

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4. Therapeutic Role

Itraconazole may be used when systemic antifungal treatment is clinically indicated.

Its therapeutic role includes treatment of susceptible fungal infections involving:

Skin

• Ringworm
• Athlete’s foot
• Jock itch
• Other dermatophyte infections

Nails

Itraconazole is used in selected cases of onychomycosis, where the fungal infection involves the nail.

Mucosal/Other Fungal Infections

Depending on the organism and clinical diagnosis, itraconazole may also be used for certain mucosal and systemic fungal infections.

The exact regimen differs considerably by infection.

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5. Common Clinical Applications

Tinea Corporis

A dermatophyte infection affecting the body, commonly producing circular or spreading lesions.

Systemic itraconazole may be considered when oral antifungal treatment is clinically indicated.

Tinea Cruris

A dermatophyte infection involving the groin.

Treatment selection depends on extent, recurrence and response to topical therapy.

Tinea Pedis

Commonly known as athlete’s foot.

Itraconazole may be considered for selected extensive, recurrent or treatment-resistant infections.

Onychomycosis

Fungal infection of the nails can be difficult to treat because the organism is located within the nail structure.

Itraconazole is one of the systemic antifungal agents used in selected patients.

Important: Itraconazole has specific cardiac warnings when used for onychomycosis. Patients with evidence of ventricular dysfunction such as congestive heart failure or a history of CHF should not receive itraconazole capsules for onychomycosis.

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6. Suggested Use & Dosage

ITROSPIN-100 contains:

Itraconazole BP — 100 mg per capsule

The dosage of itraconazole cannot be determined from the 100 mg capsule strength alone.

The dose and duration depend on:

• Type of fungal infection
• Site of infection
• Severity
• Organism involved
• Patient age
• Liver function
• Kidney function
• Other medicines being used
• Previous antifungal treatment

Therefore:

Take ITROSPIN-100 exactly as prescribed by the physician. Do not self-medicate or determine the duration of treatment based solely on the capsule strength.

Different fungal infections can require substantially different itraconazole regimens.

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7. How to Take ITROSPIN-100

For conventional itraconazole capsules, product information recommends administration immediately after a full meal because food improves absorption.

General administration principles:

• Swallow the capsule whole.
• Do not crush or chew.
• Take immediately after a full meal unless your specific prescribing information says otherwise.
• Take the medicine at the prescribed frequency.
• Complete the prescribed treatment course.
• Do not stop treatment early simply because symptoms improve.

Itraconazole absorption can be reduced when gastric acidity is low, including with acid-suppressing medicines.

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8. Gastric Acid & Absorption

Itraconazole capsules require an acidic gastric environment for optimal absorption.

Absorption may be reduced in patients with:

• Reduced gastric acidity
• Achlorhydria
• Certain gastric disorders
• Use of proton-pump inhibitors
• Use of H2-receptor antagonists
• Other acid-suppressing treatment

The FDA prescribing information notes that itraconazole capsule absorption is reduced with decreased gastric acidity.

Patients taking acid-suppressing medicines should inform their physician or pharmacist.

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9. Possible Side Effects

Possible adverse effects of itraconazole include:

• Nausea
• Abdominal pain
• Diarrhea
• Vomiting
• Headache
• Dizziness
• Indigestion
• Constipation
• Fatigue
• Skin rash

The severity and frequency can vary according to the patient, dose and duration of treatment.

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10. Important Liver Safety Warning

Itraconazole has been associated with rare cases of serious hepatotoxicity, including liver failure and death. Some cases have occurred within the first week of treatment and have occurred in people without previously known liver disease.

Patients should seek medical advice if they develop symptoms suggestive of liver injury, such as:

• Unusual fatigue
• Loss of appetite
• Persistent nausea or vomiting
• Abdominal discomfort
• Dark urine
• Pale stools
• Yellowing of the skin or eyes
• Unusual itching

If clinical signs or symptoms consistent with liver disease develop, the prescribing information recommends discontinuation and evaluation of liver function.

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11. Important Cardiac Warning

Itraconazole carries an important warning concerning congestive heart failure and cardiac effects.

Itraconazole has demonstrated negative inotropic effects, meaning it can adversely affect the force of cardiac contraction in susceptible situations.

For treatment of onychomycosis, itraconazole capsules should not be used in patients with evidence of ventricular dysfunction such as:

• Congestive heart failure
• Previous history of congestive heart failure

For other indications in patients with ventricular dysfunction, the prescribing information recommends use only when the expected benefit clearly outweighs the risk.

Patients should seek medical attention for symptoms such as:

• Shortness of breath
• Swelling of the legs or feet
• Rapid or unexpected weight gain
• Unusual fatigue
• Difficulty breathing when lying down

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12. Drug Interactions

Itraconazole has extensive drug-interaction potential.

It strongly inhibits CYP3A4, which can increase blood concentrations of many other medicines.

Examples of medicines with important contraindications or major interaction concerns include certain:

• Antiarrhythmics
• Benzodiazepines
• Statins
• Calcium-channel blockers
• Opioids
• Anticoagulants
• Antiepileptic medicines
• Anticancer medicines
• Immunosuppressants
• Antimigraine medicines

Current labeling lists numerous CYP3A4 substrates for which co-administration is contraindicated because of potentially serious or life-threatening adverse effects.

Important examples

Itraconazole capsules are contraindicated with certain medicines including:

• Methadone
• Quinidine
• Dofetilide
• Dronedarone
• Pimozide
• Triazolam
• Oral midazolam
• Lovastatin
• Simvastatin
• Certain ergot alkaloids
• Certain calcium-channel blockers
• Certain other CYP3A4 substrates

This is not a complete interaction list. A complete medication review should be performed before prescribing.

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13. CYP3A4 Interaction

Itraconazole and its active metabolite can inhibit CYP3A4-mediated metabolism.

This can cause:

Itraconazole + CYP3A4 substrate
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Reduced metabolism of the other medicine
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Higher plasma concentration
↓
Potentially increased or prolonged drug effects and toxicity

Some combinations can result in serious cardiac rhythm disturbances, including QT prolongation and potentially fatal ventricular arrhythmias.

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14. Pregnancy & Breastfeeding

Itraconazole should be used during pregnancy only when specifically considered appropriate by the treating physician.

The prescribing information contains important pregnancy precautions, particularly for treatment of onychomycosis.

Women who are pregnant, planning pregnancy or breastfeeding should inform their doctor before starting treatment.

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15. Use in Children

The suitability of itraconazole in children depends on:

• Age
• Body weight
• Type of fungal infection
• Severity
• Organism
• Other medical conditions

Do not administer ITROSPIN-100 to children without specific medical advice.

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16. Elderly Patients

Elderly patients may have:

• Reduced liver function
• Reduced kidney function
• Multiple medicines
• Increased risk of drug interactions

A medication review and appropriate clinical monitoring may therefore be required.

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17. Kidney & Liver Impairment

Liver impairment

Itraconazole is extensively metabolized by the liver. Patients with liver disease require particular caution and medical assessment.

Kidney impairment

The suitability of itraconazole should be assessed in patients with renal impairment, particularly when prolonged treatment is planned or multiple medicines are being used.

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18. When to Seek Immediate Medical Attention

Contact a healthcare professional urgently if the patient develops:

Liver-related symptoms

• Yellow eyes or skin
• Dark urine
• Severe loss of appetite
• Persistent nausea
• Severe abdominal discomfort

Cardiac symptoms

• Shortness of breath
• Leg swelling
• Sudden weight gain
• Difficulty breathing while lying down

Severe allergic reaction

• Facial swelling
• Tongue or throat swelling
• Difficulty breathing
• Severe rash

Cardiac rhythm symptoms

• Fainting
• Severe palpitations
• Unexplained dizziness

Itraconazole-associated cardiac and hepatic adverse effects can be serious and require prompt assessment.

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19. Storage

Store ITROSPIN-100:

• At the temperature specified on the product label.
• In a cool, dry place.
• Protected from excessive heat and moisture.
• Away from direct sunlight.
• Out of reach of children.

Keep the capsules in their original packaging until use.

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20. Key Features of ITROSPIN-100

ITROSPIN-100 Capsules provide:

• Itraconazole BP 100 mg
• Systemic triazole antifungal
• HPMC capsule dosage form
• Oral administration
• Prescription formulation
• Pack of 10 × 10 HPMC capsules
• Suitable for physician-directed treatment of susceptible fungal infections

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21. Why ITROSPIN-100?

ITROSPIN-100 provides Itraconazole 100 mg, a systemic triazole antifungal with activity against a range of susceptible fungal organisms.

Key pharmacological action

Inhibition of ergosterol synthesis

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Disruption of fungal cell membrane

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Inhibition of fungal growth

Its clinical use should be guided by the fungal diagnosis, susceptibility where relevant, infection site, patient-specific factors and potential drug interactions.