What drugs does CYP3A5 metabolize?
The geographical distribution of CYP3A5 variants shown has pharmacogenomic relevance for African populations because CYP3A5 is involved in the metabolism of drugs used to treat the three most common infectious diseases: malaria (artemether, lumefantrine, mefloquine, primaquine, chloroquine), HIV/AIDS (efavirenz.
Is tacrolimus metabolized by CYP3A4?
Tacrolimus is a macrolide immunosuppressant used for prevention of allograft rejection in organ transplantation and metabolized in the liver and intestine by cytochrome P450 3A4 (CYP3A4) enzyme.
How does tacrolimus work?
Tacrolimus works by suppressing the immune system to prevent the white blood cells from trying to get rid of the transplanted organ. Tacrolimus is a very strong medicine. It can cause side effects that can be very serious, such as kidney problems. It may also decrease the body’s ability to fight infections.
What is CYP3A5 * 3?
CYP3A5*3 is the most frequent and well-studied variant allele of CYP3A5. Its frequency varies widely across human populations. In White populations, the estimated allele frequency of CYP3A5*3 is 0.82–0.95 [4–8].
What does poor metabolizer of CYP3A5 mean?
Low risk CYP3A5 metabolizer: low risk means there is no recommended change to a medicine based upon the CYP3A5 gene. Poor metabolizer – This means there are two copies of a decreased function CYP3A5 gene which results in poor CYP3A5 enzyme function.
What is the CYP3A5 gene?
CYP3A5 Gene – Cytochrome P450 Family 3 Subfamily A Member 5 This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids.
What drugs interact with tacrolimus?
Some products that may interact with this drug include: aluminum/magnesium antacid, cyclosporine, sirolimus, temsirolimus, ziprasidone, other drugs that may increase the level of potassium in the blood (such as “water pills” including amiloride, spironolactone), other drugs that weaken the immune system/increase the …
What is the side effects of tacrolimus?
Tacrolimus may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- headache.
- diarrhea.
- constipation.
- nausea.
- vomiting.
- heartburn.
- stomach pain.
- loss of appetite.
How long can you use tacrolimus?
Tacrolimus ointment is intended to be used for a short period of time (up to six weeks). It should not be used every day over a long period of time. Some people who frequently have flares may be prescribed the ointment to use on two days of each week to prevent further flares from developing.
What does it mean to be a poor metabolizer of CYP3A5?
Poor metabolizer – This means there are two copies of a decreased function CYP3A5 gene which results in poor CYP3A5 enzyme function. Medicines do not require a change in dose in patients who are poor metabolizers of CYP3A5, because most medicines were developed in CYP3A5 poor metabolizers.
Who should not take tacrolimus?
You should not use this medicine if you are allergic to tacrolimus or hydrogenated castor oil, or if you have used cyclosporine (Neoral, Sandimmune, Gengraf) within the past 24 hours. Using tacrolimus may increase your risk of developing serious infections or certain types of cancer, such as lymphoma or skin cancer.
Does vitamin C interact with tacrolimus?
No interactions were found between tacrolimus and Vitamin C.
How is tacrolimus cleared from the body?
Tacrolimus is excreted primarily via the biliary route [43] and systemic clearance can range from . 6-5.4 L/h/kg [44] though the range greatly depends on the type of transplant the patient underwent as well as several other variables already mentioned.
What is tacrolimus toxicity?
Tacrolimus toxicity commonly presents as acute renal failure. Close monitoring of serum creatinine, GFR, and urine output is necessary for patients on tacrolimus. Toxicity may also present as the development of adverse effects such as tremors, electrolyte disturbances, headaches, and increased SCr.
Is tacrolimus safe to use long term?
Long-term treatment up to 24 months with 0.1% tacrolimus ointment is safe and efficacious in adults with atopic dermatitis. Key words: atopic dermatitis; long-term treatment; tacrolimus ointment.
What is the relationship between CYP3A5 polymorphism and tacrolimus trough concentration?
These studies have shown significantly higher tacrolimus trough concentration divided by daily dose per body weight (Co/D) in patient carrying CYP3A5 (GG or *3/*3) polymorphism i.e., nonexpresser, than expresser CYP3A5 (AA or *1/*1) at various post-transplant time (<1, 3–9, 12–24, 36–60 months).
What is CYP3A5 polymorphism in intron 3?
A polymorphism in intron 3 of the CYP3A5 gene affects the expression of this enzyme and tacrolimus trough blood levels.
What is the CYP3A5 -a reference allele?
Single nucleotide polymorphism in the CYP3A5 gene (rs776746; 6986A>G) results in a change in metabolic activity of CYP3A5 protein which ultimately affects the tacrolimus concentration [ 6 ]. The CYP3A5 -A reference allele (also known as *1) codes for a functional CYP3A5 protein.