Tacromus
Generic Name
Tacrolimus
Manufacturer
Various manufacturers globally
Country
Global
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| tacromus 05 mg capsule | ৳ 28.00 | ৳ 280.00 |
Description
Overview of the medicine
Tacrolimus is an immunosuppressant medicine used to prevent organ rejection in people who have received a kidney, liver, or heart transplant. It works by decreasing your body's immune system activity.
Uses & Indications
Dosage
Adults
Highly individualized based on organ type and patient response. Initial doses typically range from 0.1-0.2 mg/kg/day orally in two divided doses for kidney or liver transplants, and 0.075 mg/kg/day for heart transplants, aiming for specific trough levels.
Elderly
No specific dose adjustment for elderly patients, but careful monitoring of renal function, blood pressure, and tacrolimus blood levels is recommended due to potential age-related organ impairment.
Renal_impairment
No dosage adjustment needed for renal impairment, but careful monitoring of tacrolimus blood levels and kidney function is crucial due to potential nephrotoxicity.
How to Take
Take orally, preferably on an empty stomach (1 hour before or 2-3 hours after a meal) to ensure consistent absorption. Swallow the capsules whole with water; do not chew or crush.
Mechanism of Action
Tacrolimus acts as a calcineurin inhibitor. It binds to an intracellular protein (FKBP-12), and this complex then inhibits calcineurin, a phosphatase. Inhibition of calcineurin prevents the dephosphorylation of NF-AT (nuclear factor of activated T-cells), thereby blocking the transcription of genes encoding various lymphokines (e.g., IL-2, IL-3, IFN-gamma) and inhibiting T-lymphocyte activation and proliferation.
Pharmacokinetics
Onset
Immunosuppressive effects develop over several hours to days, depending on the dose and indication. Steady-state concentrations are usually achieved within 2-3 days of consistent dosing.
Excretion
Primarily excreted in the feces (over 90%) after hepatic metabolism, with less than 2% excreted unchanged in urine.
Half life
The elimination half-life is highly variable, ranging from approximately 25 to 60 hours in healthy volunteers and liver transplant patients, but can be shorter in kidney transplant patients.
Absorption
Oral bioavailability is variable and incomplete (approximately 20-25%). Food, especially high-fat meals, can decrease absorption. Peak concentrations typically occur 1-3 hours after oral administration.
Metabolism
Extensively metabolized in the liver and intestinal wall by the cytochrome P450 3A4 (CYP3A4) enzyme system. Many active and inactive metabolites are formed.
Side Effects
Contraindications
- Hypersensitivity to tacrolimus or any excipients in the formulation.
- Hypersensitivity to other macrolides.
Drug Interactions
Live vaccines
Avoid use of live vaccines due to increased risk of infection in immunosuppressed patients.
Nephrotoxic Agents (e.g., NSAIDs, Aminoglycosides)
Increased risk of nephrotoxicity when co-administered with tacrolimus. Monitor renal function closely.
CYP3A4 Inducers (e.g., Rifampin, Phenytoin, St. John's Wort)
Can significantly decrease tacrolimus blood levels, increasing risk of rejection. Dose increase may be necessary.
CYP3A4 Inhibitors (e.g., Ketoconazole, Erythromycin, Grapefruit juice)
Can significantly increase tacrolimus blood levels, increasing risk of toxicity. Dose reduction may be necessary.
Storage
Store at room temperature (20-25°C or 68-77°F). Keep away from moisture, light, and heat. Do not freeze. Keep out of reach of children.
Overdose
Limited experience with overdose. Symptoms may include tremor, headache, nausea, vomiting, and kidney dysfunction. Management is primarily supportive; activated charcoal may be considered if ingested recently. There is no specific antidote.
Pregnancy & Lactation
Pregnancy Category C. Tacrolimus can cross the placenta and has been associated with adverse fetal outcomes. Use only if the potential benefit justifies the potential risk to the fetus. It is excreted in human breast milk; therefore, breastfeeding is not recommended.
Side Effects
Contraindications
- Hypersensitivity to tacrolimus or any excipients in the formulation.
- Hypersensitivity to other macrolides.
Drug Interactions
Live vaccines
Avoid use of live vaccines due to increased risk of infection in immunosuppressed patients.
Nephrotoxic Agents (e.g., NSAIDs, Aminoglycosides)
Increased risk of nephrotoxicity when co-administered with tacrolimus. Monitor renal function closely.
CYP3A4 Inducers (e.g., Rifampin, Phenytoin, St. John's Wort)
Can significantly decrease tacrolimus blood levels, increasing risk of rejection. Dose increase may be necessary.
CYP3A4 Inhibitors (e.g., Ketoconazole, Erythromycin, Grapefruit juice)
Can significantly increase tacrolimus blood levels, increasing risk of toxicity. Dose reduction may be necessary.
Storage
Store at room temperature (20-25°C or 68-77°F). Keep away from moisture, light, and heat. Do not freeze. Keep out of reach of children.
Overdose
Limited experience with overdose. Symptoms may include tremor, headache, nausea, vomiting, and kidney dysfunction. Management is primarily supportive; activated charcoal may be considered if ingested recently. There is no specific antidote.
Pregnancy & Lactation
Pregnancy Category C. Tacrolimus can cross the placenta and has been associated with adverse fetal outcomes. Use only if the potential benefit justifies the potential risk to the fetus. It is excreted in human breast milk; therefore, breastfeeding is not recommended.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 2-3 years from the date of manufacture, consult product packaging for exact expiry.
Availability
Available in pharmacies and hospitals
Approval Status
FDA/DGDA Approved
Patent Status
Off-patent for molecule, variable for specific formulations
WHO Essential Medicine
YesClinical Trials
Tacrolimus has undergone extensive clinical trials demonstrating its efficacy and safety in preventing organ rejection across various transplant types. Ongoing research explores its use in other autoimmune conditions and in optimizing dosing strategies.
Lab Monitoring
- Tacrolimus trough blood levels (regularly to maintain therapeutic range)
- Kidney function tests (serum creatinine, BUN, urine protein)
- Liver function tests (AST, ALT, bilirubin)
- Blood glucose levels
- Electrolytes (potassium, magnesium)
- Complete Blood Count (CBC)
- Blood pressure
Doctor Notes
- Emphasize the critical importance of therapeutic drug monitoring (TDM) to maintain target trough levels and adjust dosage accordingly.
- Educate patients thoroughly about drug-drug and drug-food interactions, especially grapefruit.
- Counsel patients on the increased risk of infections and malignancies, and advise on protective measures (e.g., sun protection, vaccine considerations).
Patient Guidelines
- Take your medicine exactly as prescribed, at the same time each day.
- Do not stop taking tacrolimus abruptly without consulting your doctor, as this can lead to organ rejection.
- Attend all scheduled appointments for blood tests and follow-up.
- Report any unusual symptoms or side effects to your doctor immediately.
Missed Dose Advice
If you miss a dose, take it as soon as you remember, unless it is almost time for your next dose. In that case, skip the missed dose and continue with your regular dosing schedule. Do not double dose to make up for a missed one.
Driving Precautions
Tacrolimus can cause neurological disturbances such as tremor, headache, dizziness, or visual impairment. Exercise caution when driving or operating machinery until you know how the medicine affects you.
Lifestyle Advice
- Avoid grapefruit and grapefruit juice completely during treatment.
- Protect yourself from sun exposure and use sunscreen, as tacrolimus can increase the risk of skin cancer.
- Maintain good hygiene to reduce the risk of infections.
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