PANGRAF 5.0 Capsules (Hard Gelatin)

What is PANGRAF 5.0

PANGRAF 5.0 is a prescription medicine containing Tacrolimus, an immunosuppressant primarily used to prevent organ rejection in patients who have undergone a liver, kidney, or heart transplant. It is classified as a calcineurin inhibitor and is typically administered in combination with other immunosuppressive agents such as corticosteroids or mycophenolate mofetil.

• Formulation: Hard gelatin capsules
• Strength: 5.0 mg Tacrolimus per capsule
• Pack size: 100’s (10s blister in box x 6)
• Generic name: Tacrolimus

PANGRAF works by inhibiting the activity of certain white blood cells (T-lymphocytes) that can attack transplanted organs, thereby reducing the immune response and helping the body accept the new organ.

Due to its potent effects on the immune system, it should be used under strict medical supervision with regular blood tests to monitor drug levels and kidney function.

How to use PANGRAF 5.0

Proper use of PANGRAF 5.0 is essential for maximizing its efficacy and minimizing potential risks. Patients should closely follow their healthcare provider’s instructions.

• Administration: Take the capsule orally, preferably on an empty stomach (1 hour before or 2 hours after meals) to enhance absorption.
• Swallow whole: Do not open, crush, or chew the capsule.
• Time of dosing: It should be taken at the same time every day to maintain consistent blood levels.
• With or without food: If taken with food, ensure it is taken the same way each time (e.g., always with food or always without).
• Missed dose: If a dose is missed and it's close to the next scheduled dose, skip the missed dose. Do not double up.
• Monitoring: Regular monitoring of tacrolimus blood levels, kidney function, liver function, and electrolytes (like potassium and magnesium) is essential.

Do not alter the dose or stop the medicine without consulting your doctor, as it can lead to organ rejection or toxicity.

Mode of Action PANGRAF 5.0

Tacrolimus, the active ingredient in PANGRAF 5.0, is a calcineurin inhibitor that functions as a potent immunosuppressive agent.

• Binding target: Tacrolimus binds to an intracellular protein called FK-binding protein 12 (FKBP12).
• Inhibition of calcineurin: The tacrolimus-FKBP12 complex inhibits calcineurin, a calcium-dependent phosphatase crucial for activating T-lymphocytes.
• Reduced cytokine production: Inhibiting calcineurin blocks the transcription of interleukin-2 (IL-2) and other cytokines, which are essential for T-cell proliferation.
• Suppressed immune response: This ultimately suppresses the body’s immune response, preventing the immune system from attacking the transplanted organ.

This mode of action makes PANGRAF particularly effective in preventing acute and chronic rejection of organ transplants. However, the immunosuppressive effect also increases the patient’s susceptibility to infections and certain malignancies, which is why medical supervision is critical.

PANGRAF 5.0 Interactions PANGRAF 5.0

Tacrolimus, the active ingredient in PANGRAF 5.0, is a calcineurin inhibitor that functions as a potent immunosuppressive agent.

• Binding target: Tacrolimus binds to an intracellular protein called FK-binding protein 12 (FKBP12).
• Inhibition of calcineurin: The tacrolimus-FKBP12 complex inhibits calcineurin, a calcium-dependent phosphatase crucial for activating T-lymphocytes.
• Reduced cytokine production: Inhibiting calcineurin blocks the transcription of interleukin-2 (IL-2) and other cytokines, which are essential for T-cell proliferation.
• Suppressed immune response: This ultimately suppresses the body’s immune response, preventing the immune system from attacking the transplanted organ.

This mode of action makes PANGRAF particularly effective in preventing acute and chronic rejection of organ transplants. However, the immunosuppressive effect also increases the patient’s susceptibility to infections and certain malignancies, which is why medical supervision is critical.

Interactions of PANGRAF 5.0 (Tacrolimus)

PANGRAF 5.0 can interact with a wide range of drugs and substances, which may affect its levels in the blood and increase the risk of toxicity or reduce its effectiveness.

• CYP3A4 inhibitors: Drugs such as ketoconazole, itraconazole, erythromycin, clarithromycin, and grapefruit juice can increase tacrolimus levels.
• CYP3A4 inducers: Rifampin, phenytoin, carbamazepine, and St. John's Wort can lower tacrolimus levels, potentially leading to organ rejection.
• Nephrotoxic drugs: Concurrent use with NSAIDs (e.g., ibuprofen), aminoglycosides, or amphotericin B increases the risk of kidney damage.
• Hyperkalemia risk: Potassium-sparing diuretics or potassium supplements may elevate potassium levels dangerously.
• Immunosuppressants: Caution should be used when combining with other immunosuppressants due to cumulative immunosuppressive effects.

Always inform your doctor of all medications, herbal supplements, or over-the-counter products you are taking. Blood levels of tacrolimus may need frequent adjustments in the presence of interacting agents.

Dosage of PANGRAF 5.0

The dosage of PANGRAF 5.0 varies based on the type of organ transplant, time since transplantation, patient’s body weight, and clinical condition. Dosage must be individualized and monitored carefully.

• Initial dose:
  • For kidney transplant: 0.15–0.2 mg/kg/day in two divided doses
  • For liver transplant: 0.10–0.15 mg/kg/day in two divided doses
• Maintenance dose: Typically lower than the initial dose and adjusted based on trough blood concentrations (target range usually 5–15 ng/mL).
• Special populations:
  • Renal impairment: Dose adjustments may be necessary.
  • Hepatic impairment: Lower doses may be required due to reduced metabolism.
  • Pediatrics: Often require higher doses on a mg/kg basis due to faster metabolism.

Dosage should always be guided by therapeutic drug monitoring (TDM) and under medical supervision. Never self-adjust the dose based on symptoms or routine labs alone.

Possible side effects of PANGRAF 5.0

As with all immunosuppressants, PANGRAF 5.0 can cause a range of side effects. These may be dose-dependent and vary by individual. Prompt medical attention should be sought for serious reactions.

• Common side effects:
  • Tremors
  • Headache
  • Hypertension
  • Nausea, vomiting, diarrhea
  • Insomnia
• Serious side effects:
  • Nephrotoxicity (kidney dysfunction)
  • Neurotoxicity (seizures, confusion, paresthesia)
  • Infections due to suppressed immunity
  • Hyperglycemia and diabetes mellitus
  • Cardiac arrhythmias
• Rare but severe:
  • Lymphoproliferative disorders
  • Malignancies (e.g., skin cancer)
  • Anaphylaxis (rare with IV form)

Patients should be educated on symptoms of infection, kidney problems, and high blood sugar, and report any unusual signs immediately to their doctor.

PANGRAF 5.0 Contraindications PANGRAF 5.0

PANGRAF 5.0 is contraindicated or should be used with extreme caution in certain populations due to its strong immunosuppressive and nephrotoxic properties.

• Absolute contraindications:
  • Known hypersensitivity to Tacrolimus or any excipients in the formulation
  • Allergy to macrolide antibiotics (due to structural similarity)
• Relative contraindications or caution:
  • Severe liver impairment
  • Pre-existing severe renal dysfunction
  • Uncontrolled infections
  • Patients with congenital or acquired QT prolongation
  • Pregnancy and lactation (use only if benefits outweigh risks)

Due to its narrow therapeutic index, use of PANGRAF should be based on thorough risk-benefit evaluation, especially in vulnerable populations like elderly or pediatric patients.

Storage of PANGRAF 5.0

Proper storage of PANGRAF 5.0 is essential to maintain its potency and ensure safe use.

• Temperature: Store below 25°C (77°F). Avoid freezing.
• Humidity: Keep in a dry place, away from moisture. Do not store in the bathroom.
• Light exposure: Protect from light. Store in original packaging until use.
• Container: Keep capsules in their original blister packs until ready to use. Do not transfer to other containers.
• Keep out of reach of children and pets.
• Do not use: After the expiry date printed on the packaging.
• Disposal: Dispose of unused or expired medication as per local regulations. Do not flush down the toilet.

Always consult a pharmacist or healthcare provider if unsure about the storage or handling of this medication.