Brand Name : Tacrograf
Composition : Tacrolimus
Strength availability : 5mg
Manufactured by : Biocon Pharmaceuticals
Dosage Form : capsule
Packing : 10 capsules in 1 strip
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Tacrograf 5mg belongs to macrolide antibiotic originally developed from Streptomyces tsukubaensis. Tacrograf 5mg joints to immunophilins known as FK506-binding proteins (FKBPs). The resulting tacrolimus-immunophilin complex gives the same action and effects as described for cyclosporine. Tacrograf 5mg is authorized for prophylaxis against rejection of allogeneic liver transplants. The drug is also possibly as useful as cyclosporine for other conditions. Tacrograf 5mg has been shown to exert profound antipsoriatic effects, potentially by direct concomitant with keratinocytes.
Tacrograf 5mg is indicated after allogenic organ transplant to decrease the activity of the patient's immune system and so the risk of organ rejection.
Tacrograf 5mg was first approved by the FDA in 1994 for usage in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants.
Tacrograf 5mg has also been indicated for a topical preparation in the treatment of severe atopic dermatitis.
Kidney transplant - Organ Transplant – Rejection prophylaxis :
Dose is depending on body weight and should be described by your doctor. The initial dose is generally 0.1 to 0.2 milligram per kilogram (mg/kg) of body weight per day, divided into 2 doses and have every 12 hours. Your doctor may adjust the dose as needed High dose: 0.1mg/kg/day continuous IV infusion.
Tacrograf combination with azathioprine: initial dose 0.1mg/kg orally every 12hours. Initiate within 24 hours surgery.
In combination with mycophenolate: Initial dose 0.05mg/kg orally every 12hours started with 24hrs of surgery
Children – The prescribed dose is 0.3 mg/kg per day, divided in 2 doses, given every 12 hours
Liver transplant - Organ Transplant – Rejection prophylaxis :
In Adults the Dose is depending on body weight and should be described by your doctor. The initial dose is commonly 0.1 to 0.15 milligram per kilogram (mg/kg) of body weight per day, divided into 2 doses and taken every 12 hours. Your doctor may adjust the dose as needed. Children prescribed Dose is depending on body weight and should be described by your doctor. The initial dose is commonly 0.15 to 0.2 mg/kg of body weight per day, divided into 2 doses and taken every 12 hours.
Heart transplant- Organ Transplant– Rejection prophylaxis : In Adults the Dose is depending on body weight and should be described by your doctor. The initial dose is commonly 0.075 milligram per kilogram (mg/kg) of body weight per day, divided into 2 doses and taken every 12 hours. Your doctor may adjust the dose as needed. Children prescribed dose is 0.3 mg/kg per day, divided in 2 doses, given every 12 hours. Your doctor may adjust your dose as needed.
Graft versus host disease in adult :
Prevention Initial dose: 0.03mg/kg/day, initiate at least 24hrs before to stem cell infusion.
Treatment IV: initial dose 0.03mg/kg/day (continuous infusion)
To convert IV to oral then multiply total daily IV dose 4 times and administer in 2 divided oral dose /day, every 12hrs.
Pediatric dose for organ transplant – Rejection Reversal :
Initial dose: 0.075 to 0.1 mg/kg orally every 12 hrs.
IV, Initial dose: 0.03 to 0.05 mg/kg/day as continuous infusion
Graft versus host disease :
IV, initial dose 0.03 mg/kg/day (continuous IV), started at least 24 hrs. before to stem cell infusion, it used only if oral medication can be tolerated.
IF OVERDOSE OCCURS:
Tacrograf overdose may leads to passing out or breathing trouble. Call emergency medical or poison control for rapid action.
MECHANISM OF ACTION
Tacrograf 5mg prevents the T-lymphocyte activation.
The drug binds to a protein (FKBP- 12) inside the cell and forms complex of Tacrograf 5mg- FKBP-12, calcium, calmodulin, and calcineurin. The alteration of nuclear factor of activated T- cells(NF-AT), a nuclear component which initiate gene transcription for the formation of lymphokines (as interleukin-2, gamma interferon).
Finally, results prevention of T-lymphocyte activation.
Oral slowly absorbed in the GI tract, total bioavailability 20 to 25%, highest blood plasma concentration reached after 1-3hrs. With food slows down resorption and reduces bioavailability.
In the blood Tacrograf 5mg is mainly bound to erythrocytes, plasma 5%, plasma protein binding 98.8%.
Tacrograf 5mg is metabolized in liver, mainly via CYP3A and in the intestinal wall.
Tacrograf 5mg exerted through feces in form of its metabolites. Biological half-life 43 hrs. (healthy), liver transplation person 12hrs, for kidney transplation 16 hrs.
Avoid Tacrograf 5mg, if you allergic to its own or hydrogenated castor oil, cyclosporine with the past 24 hrs.
Discuss with doctor, if Tacrograf 5mg used for longer periods of time, it will develop skin cancer, that weaken immune system and the possible risk.
Inform early to doctor about :
• Have kidney or liver disease;
• Have cardiac disease, hypertension, hyperlipidemia or triglycerides (a type of fat in the blood);
• a cardiac rate disorder or history of long QT syndrome;
• taking heart rhythm medication; or
• usage of other medications that can weaken your immune system
• pregnancy, not known whether harm unborn baby
• while Tacrograf 5mg therapy, avoid breast feed.
Concomitant use of Tacrograf 5mg with
Aluminum/magnesiumantacid, cyclosporine, sirolimus, temsirolimus, ziprasidone, causes increase the level of potassium in the blood and with other drugs ( natalizumab, rituximab) will weaken the immune system and increase the risk of infection.
Cimetidine, danazol, nefazodone, ethinyl estradiol, methylprednisolone, antifungal drugs, rifamycin, anti-seizure will remove tacrolimus from the body and affect its work.
Hypersensitivity reaction by Tacrograf 5mg, the symptoms reported dyspnea, rash, pruritis and acute respiratory distress syndrome.
More common side effects:
Abnormal dreams, Agitation, Chills, Confusion, Cough, Diarrhoea, Dizziness, Fever, Frequent Urination, General Feeling of Discomfort or Illness, Headache, Itching, Skin Rash, Joint Pain, Loss of Appetite, Loss of energy or weakness, Mental depression.
Severe side effects:
Cardiac damage, Liver and kidney problem, Increase in potassium, glucose level, Diabetes mellitus, Hypomagnesemia, Lung damage.
Fungal infection: herpes zoster or polyoma.
Carcinogenesis and mutagenesis: Non- Hodgkin’s lymphoma.
Topical use common: burning or itching sensation; less common flu like symptoms, head pain.
Tacrograf 5mg capsule store at 25℃
Do not keep the drug away from children accessible.
Keep the container at cool and dry place and protect from light.
Dispense the capsule only in original container.
Keep away from spouse or other family members avoid accidently change of medicine.