Tacrolimus Monohydrate (Oral)

Generic Name

Tacrolimus Monohydrate Oral

Other Names

• Prograf
• Advagraf
• Envarsus

Drug Class

• Immunosuppressant

Chemical Formula

C44H69NO12.H2O

Molecular Weight

822.03 g/mol

Mechanism of Action

• Inhibits T-lymphocyte activation

Indications

• Organ transplantation (such as kidney, liver, heart)

Common Dosage Forms

• Capsules
• Extended-release tablets

Typical Dosage

• 0.1-0.2 mg/kg/day in divided doses

Pediatric Dosage

• Dosing based on body weight

Geriatric Dosage

• Adjusted based on renal function

Side Effects

• Nephrotoxicity
• Hypertension
• Tremors
• Diarrhea

Contraindications

• Hypersensitivity to tacrolimus
• Use with sirolimus or live vaccines

Pregnancy Category

• C - Risk cannot be ruled out

Lactation Safety

• Use with caution; may pass into breast milk

Drug Interactions

• Cyclosporine (increased nephrotoxicity)
• Strong CYP3A4 inhibitors/inducers

Overdose Symptoms

• Renal impairment
• Neurotoxicity

Antidote for Overdose

• No specific antidote; supportive care

Storage Conditions

• Store at room temperature below 25°C

Pharmacokinetics

• Absorption: Variable and incomplete
• Distribution: Highly bound to plasma proteins
• Metabolism: Mainly hepatic via CYP3A4
• Excretion: Primarily fecal

Precautions

• Monitor renal function regularly
• Avoid grapefruit juice

Warnings

• Increased risk of infections
• Malignancies

Others

• It is essential to monitor blood levels of tacrolimus regularly to adjust dosage and prevent toxicity.