ITROSPIN-SB 65 Capsules – Itraconazole IP 65 mg

ITROSPIN-SB 65 contains Itraconazole IP 65 mg in a super-bioavailable (SB/SUBA) HPMC capsule formulation. The artwork identifies it as a “Supra Bioavailable Formulation” and shows a pack of 10 × 10 HPMC Capsules.

This formulation is important to distinguish from conventional itraconazole capsules because SB/SUBA itraconazole is not interchangeable mg-for-mg with conventional itraconazole products. CDSCO specifically required this caution for the 65 mg supra-bioavailable formulation.

---

1. Product Information

---

2. Composition

Each HPMC capsule contains:

Itraconazole IP — 65 mg

Excipients — q.s.

Approved colours used in empty capsule shells.

The composition and dosage form above are taken directly from the uploaded product artwork.

---

3. What is ITROSPIN-SB 65?

ITROSPIN-SB 65 is a super-bioavailable itraconazole formulation containing 65 mg of itraconazole.

Itraconazole is a broad-spectrum triazole antifungal used against susceptible fungal organisms.

The SB/SUBA formulation was developed to address some of the absorption variability associated with conventional itraconazole. Pharmacokinetic studies have demonstrated substantially higher and less variable exposure with the super-bioavailable formulation compared with conventional itraconazole.

---

4. What Does “Super Bioavailable” Mean?

Conventional itraconazole absorption can be affected by gastrointestinal conditions, including gastric acidity and food.

The super-bioavailable formulation uses a modified drug-delivery system designed to provide more predictable absorption and reduce dependence on an acidic gastric environment.

Studies have reported that SUBA-itraconazole 65 mg provides exposure comparable to conventional itraconazole 100 mg under specified study conditions. This does not mean that the products can be substituted capsule-for-capsule.

Important:

ITROSPIN-SB 65 should not be substituted or interchanged mg-for-mg with conventional itraconazole capsules.

This distinction is particularly important when changing between formulations. CDSCO specifically included this caution in the approval conditions for supra-bioavailable itraconazole 65 mg.

---

5. Mechanism of Action

Itraconazole inhibits the fungal enzyme lanosterol 14-alpha-demethylase (CYP51).

This enzyme is involved in the production of ergosterol, an essential component of the fungal cell membrane.

Mechanism

Itraconazole
↓
Inhibits fungal CYP51 / 14-alpha-demethylase
↓
Reduced ergosterol synthesis
↓
Disruption of fungal cell membrane
↓
Inhibition of fungal growth

Itraconazole therefore acts primarily by interfering with fungal membrane formation and function.

---

6. Therapeutic Uses

The appropriate indication depends on the approved product indication, formulation and local prescribing information.

For the 65 mg supra-bioavailable itraconazole formulation, CDSCO documentation identifies indications in adult patients for:

• Pulmonary blastomycosis
• Extrapulmonary blastomycosis
• Histoplasmosis
• Chronic cavitary pulmonary histoplasmosis
• Disseminated non-meningeal histoplasmosis
• Pulmonary aspergillosis
• Extrapulmonary aspergillosis in patients intolerant of or refractory to amphotericin B therapy

CDSCO’s 2021 approval documentation also specifically required specialist prescription and a warning that the 65 mg supra-bioavailable formulation is not interchangeable with other itraconazole products.

Important website point

Do not automatically copy the indication list of conventional itraconazole capsules onto ITROSPIN-SB 65. The exact approved indications for the marketed product should be based on its current Indian manufacturing/marketing permission and package insert.

---

7. Dermatological Applications

Itraconazole is also widely used clinically for various superficial fungal infections, including dermatophytosis.

Examples may include:

• Tinea corporis
• Tinea cruris
• Tinea pedis
• Tinea manuum
• Tinea faciei
• Pityriasis versicolor
• Onychomycosis

However, the approved indication of a particular 65 mg SB formulation must be verified from its Indian product licence/package insert before these are presented as official product indications.

The IADVL position statement notes that SUBA-itraconazole has been introduced in India and discusses its use in dermatophytosis, while also noting that evidence for superiority over conventional itraconazole is not definitive across all settings.

---

8. Clinical Evidence in Dermatophytosis

Clinical studies have evaluated super-bioavailable itraconazole in dermatophytosis.

One randomized Indian study comparing conventional itraconazole with super-bioavailable itraconazole in adults with tinea cruris, corporis and/or faciei reported clinical and mycological outcomes with both formulations and found the SB formulation well tolerated.

Another randomized study comparing SB itraconazole 50 mg and 65 mg twice daily in glabrous tinea reported different cure rates between the groups, although this was a relatively small study.

A more recent randomized comparative study also evaluated conventional 100 mg versus SUBA 65 mg and 50 mg formulations in superficial dermatophytosis and found similar short-term clinical responses among groups, while differences in longer-term relapse/recurrence were observed in that study.

Appropriate website claim

It is preferable to state:

“Super-bioavailable itraconazole has been clinically studied in dermatophytosis.”

rather than making an unsupported claim that the formulation is universally superior.

---

9. Dosage and Administration

Important

65 mg of SB/SUBA itraconazole is not equivalent to 65 mg of conventional itraconazole in dosing terms.

The 65 mg SB formulation has specific dosing recommendations and should be prescribed according to its own product information. CDSCO specifically states that the 65 mg supra-bioavailable formulation is not interchangeable or substitutable with other itraconazole products.

For reference, the current U.S. prescribing information for the 65 mg SUBA product TOLSURA uses two 65 mg capsules (130 mg) once daily for blastomycosis/histoplasmosis and for aspergillosis, with higher dosing in selected situations. It also requires administration with food.

For your Indian product page:

Take ITROSPIN-SB 65 exactly as prescribed by the physician. The dose and duration depend on the type and severity of fungal infection and the patient’s clinical condition. Do not substitute ITROSPIN-SB 65 with conventional itraconazole capsules without medical advice.

---

10. How to Take ITROSPIN-SB 65

For the approved SUBA/SB formulation, administration with food is recommended in the prescribing information.

General administration instructions

• Take the capsule as prescribed.
• Take it with food where specified by the product prescribing information.
• Swallow the capsule whole.
• Do not chew, crush or open the capsule.
• Do not independently change from conventional itraconazole to SB itraconazole.
• Complete the prescribed treatment course.

---

11. Why Formulation Matters

Itraconazole has historically demonstrated considerable variability in absorption with conventional capsules.

SUBA itraconazole was developed to improve the consistency of drug exposure.

Published pharmacokinetic research reported approximately 1.8-fold relative bioavailability for SUBA itraconazole compared with conventional itraconazole at steady state under fed conditions, although exposure varies according to study conditions and formulation.

The IADVL position statement notes that SUBA itraconazole provides more controlled release in the upper duodenum and is less dependent on an acidic gastric environment.

---

12. Important Drug Interactions

Itraconazole is a strong inhibitor of CYP3A4 and can interact with numerous medicines.

Potentially important interactions include medicines used for:

• Cardiac conditions
• Hypertension
• Arrhythmias
• Cholesterol management
• Anxiety/sedation
• Immunosuppression
• Anticoagulation
• Diabetes
• Migraine
• Gastrointestinal disorders

Certain CYP3A4 substrates are specifically contraindicated with the 65 mg SUBA formulation because increased drug concentrations can result in serious adverse effects, including QT prolongation and ventricular arrhythmias.

Therefore:

Patients should provide their physician with a complete list of:

• Prescription medicines
• OTC medicines
• Supplements
• Herbal products

before starting treatment.

---

13. Heart Failure Warning

Itraconazole can have negative inotropic effects and may cause or worsen congestive heart failure.

The current TOLSURA label contains a boxed warning regarding congestive heart failure.

Patients should immediately contact their physician if they develop:

• Shortness of breath
• Swelling of feet or legs
• Sudden weight gain
• Unusual fatigue
• Difficulty breathing when lying down
• New or worsening heart symptoms

Itraconazole should be used cautiously in patients with cardiac disease.

---

14. Liver Safety

Serious hepatotoxicity, including liver failure and death, has been reported with itraconazole.

Patients should contact their physician if they develop:

• Yellowing of eyes or skin
• Dark urine
• Persistent nausea
• Loss of appetite
• Severe fatigue
• Abdominal discomfort
• Unusual itching

The prescribing information recommends appropriate clinical assessment and discontinuation if signs of significant liver dysfunction occur.

---

15. Pseudoaldosteronism

Itraconazole, including the SUBA formulation, has been associated with pseudoaldosteronism.

Possible manifestations include:

• Increased blood pressure
• Low potassium
• Swelling/fluid retention
• Fatigue
• Abnormal laboratory findings

The current TOLSURA label recommends monitoring blood pressure and potassium when clinically appropriate.

---

16. Peripheral Neuropathy

Peripheral neuropathy has been reported during itraconazole treatment, particularly with prolonged therapy.

Patients should report:

• Numbness
• Tingling
• Burning sensations
• Unusual weakness
• Changes in sensation

to their healthcare professional.

---

17. Common Side Effects

Possible adverse effects include:

• Nausea
• Vomiting
• Abdominal discomfort
• Diarrhoea
• Headache
• Dizziness
• Dyspepsia
• Rash
• Fatigue

The frequency and severity depend on the formulation, dose, duration and individual patient factors.

---

18. Serious Adverse Effects

Seek medical attention if symptoms suggest:

Severe allergic reaction

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

Liver injury

• Jaundice
• Dark urine
• Severe fatigue
• Persistent vomiting

Heart failure

• Breathlessness
• Leg swelling
• Rapid weight gain
• Unusual fatigue

Cardiac arrhythmia

• Fainting
• Severe palpitations
• Irregular heartbeat

Severe skin reaction

• Blistering
• Skin peeling
• Extensive rash
• Mouth/eye involvement

---

19. Contraindications and Precautions

ITROSPIN-SB 65 should be avoided in patients with:

• Known hypersensitivity to itraconazole
• Contraindicated interacting medicines
• Certain significant cardiac conditions where itraconazole risk outweighs benefit

Special caution is required in:

• Liver disease
• Kidney disease
• Heart failure
• Arrhythmias
• Patients receiving multiple medicines
• Long-term treatment

The exact contraindication list should follow the final approved package insert.

---

20. Pregnancy

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

Women who are pregnant, planning pregnancy or who become pregnant during treatment should inform their healthcare professional.

For prolonged antifungal treatment, the physician should evaluate:

• Severity of infection
• Alternative treatment options
• Maternal benefit
• Potential fetal risk

---

21. Breastfeeding

Itraconazole can pass into breast milk.

The decision to use ITROSPIN-SB 65 during breastfeeding should be made by the treating physician based on:

• Maternal indication
• Dose
• Treatment duration
• Infant age
• Alternative therapies

---

22. Pediatric Use

The uploaded artwork does not provide a pediatric dose.

Therefore:

ITROSPIN-SB 65 should not be administered to children unless specifically prescribed by a qualified healthcare professional.

The appropriate pediatric antifungal regimen depends on age, body weight, infection and clinical condition.

---

23. Elderly Patients

Elderly patients may have:

• Reduced hepatic function
• Reduced renal function
• Cardiovascular disease
• Multiple concomitant medicines

Therefore, the physician should assess the patient’s medical history and medication profile before prescribing itraconazole.

---

24. Driving and Operating Machinery

Itraconazole may cause dizziness or, in some patients, visual disturbances.

Patients experiencing dizziness, blurred vision or double vision should avoid driving or operating machinery and contact their healthcare professional.

---

25. Storage

Store ITROSPIN-SB 65:

• In a cool, dry place
• Protected from excessive heat
• Protected from moisture
• Away from direct sunlight
• Out of reach of children

Keep the capsules in their original packaging.

Follow the storage instructions printed on the final marketed pack.

---

26. Key Product Features

Itraconazole IP 65 mg

Contains 65 mg itraconazole in a specialized SB/SUBA formulation.

Super-Bioavailable Formulation

Designed to improve the consistency of itraconazole exposure compared with conventional formulations.

HPMC Capsule

The product artwork identifies the dosage form as an HPMC capsule.

Specialist-Directed Antifungal Therapy

The CDSCO documentation for the 65 mg supra-bioavailable formulation specifies specialist prescription.

Non-Interchangeable Formulation

The 65 mg SB formulation should not be substituted mg-for-mg with conventional itraconazole.

---

27. Why ITROSPIN-SB 65?

ITROSPIN-SB 65 combines itraconazole with a super-bioavailable formulation designed to address some of the pharmacokinetic limitations associated with conventional itraconazole.

Product highlights

• Itraconazole IP 65 mg
• Super/Supra Bioavailable formulation
• HPMC capsule
• Systemic triazole antifungal
• Designed for more predictable drug exposure
• Specialist-directed prescription product
• Suitable for selected susceptible fungal infections according to approved indication

The product should not be promoted with unsupported claims such as “100% absorption,” “best itraconazole,” “guaranteed cure,” or “superior to all conventional itraconazole”.