Metabolism: Liver (extensive) 1A2, 2D6; minor: 2C19, 3A4: Elimination half-life: 4–5 hours: Excretion: Kidney (<1%) Important information. Azathioprine, sold under the brand name Imuran, among others, is an immunosuppressive medication.
As drug concentration increases, metabolism shifts from first-order to zero-order kinetics.The most important enzyme system of phase I metabolism is cytochrome P-450 (CYP450), a microsomal superfamily of isoenzymes that catalyzes the oxidation of many drugs. Conversion to 6-MP and metabolism of 6-MP may be impaired in patients with liver disease. Lennard, L; Brown, CB; Fox, M; Maddocks, JL 1984-11-01 00:00:00 1 Azathioprine metabolite concentrations were studied in 54 kidney transplant recipients. CYP3A5 is the primary extra-hepatic CYP3A isoform, its polymorphic expression has been implicated in disease risk and the metabolism of endogenous steroids or drug in tissues other than liver. CYP2D6 represents less than 5% of the CYP liver content, but is responsible for the metabolism of up to 25% of common drugs, mainly antidepressants, antipsychotics, beta-blockers, antiretroviral agents, antiarrhythmics, morphine derivatives, and tamoxifen, many of …
Bone-marrow suppression is especially common in people with a genetic deficiency of the enzyme thiopu
These groups are usually defined by the respective number of their functional alleles: ultrarapid (3), extensive (2), intermediate (1), and poor metabolizers (0).
For examples of drugs that interact with specific enzymes, see tables With aging, the liver’s capacity for metabolism through the CYP450 enzyme system is reduced by Glucuronidation, the most common phase II reaction, is the only one that occurs in the liver microsomal enzyme system.
Videos (0) Caution and routine monitoring of blood counts and platelets is recommended. dence that azathioprine is an idiopathic hepato- toxin with the potential for combined cholestatic and hepatocellular injury in humans. Although slow in onset of action, AZA remains a very useful agent in mild to moderately severe SLE. Adverse Reaction: “Azathioprine hypersensitivity syndrome” includes, fever and rigors, arthralgia, myalgia, leukocytosis, cutaneous reactions, gastrointerstinal disturbances, hypotension, liver injury, pancreatitis, interstitial nephritis, pneumonitis, and pulmonary hemorrhage. Monitoring liver function is recommended in these patients.Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.The easiest way to lookup drug information, identify pills, check interactions and set up your own personal medication records. CYP2D6 is an important and complex pharmacogene, the aforementioned technologies enhance characterization and the ability to associate variation with drug-associated phenotypes.A major group of drug-metabolizing enzymes is the microsomal cytochrome P450 (CYP450) family Martis et al. However, in neonates, conversion to glucuronide is slow, potentially resulting in serious effects (eg, as with Conjugation may also occur through acetylation or sulfoconjugation.
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K Rowland's 6 research works with 201 citations and 176 reads, including: In vitro metabolism of 6-mercaptopurine by human liver cytosol
Drug metabolism rates vary among patients. propranolol, verapamil, morphine, nitrates. Study Liver Cirrhosis and Metabolism flashcards from Sarah-Louise Watson's class online, or in Brainscape's iPhone or Android app. Metabolites formed in synthetic reactions are more polar and thus more readily excreted by the kidneys (in urine) and the liver (in bile) than those formed in nonsynthetic reactions. Therapy with azathioprine should be administered cautiously and may need dosage reduction in patients with impaired renal function.Moderate Potential Hazard, Moderate plausibility. In this case, if 500 mg is present in the body at time zero, after metabolism, 450 mg may be present at 1 hour and 400 mg at 2 hours (illustrating a maximal clearance of 50 mg/h and no specific half-life). Last full review/revision May 2019| Content last modified May 2019 By continuing you agree to the Copyright © 2020 Elsevier B.V. or its licensors or contributors. View All Procedures > Azathioprine metabolism in kidney transplant recipients.
This generic drug has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of lupus and is much less expensive than biologic agents such as belimumab or rituximab, which are agents that have not been shown to be more effective than AZA for the control of corticosteroid-resistant nonrenal lupus. Therapy with azathioprine should be administered cautiously in patients with bone marrow depression. Thus, conjugation makes most drugs more soluble and easily excreted by the kidneys. View All News > Click here for the Consumer Version Applies to: Liver DiseaseAzathioprine is metabolically converted to the pharmacologically active 6-mercaptopurine (6-MP).
View All News > Not only has it been shown that AZA crosses the maternal–fetal membranes largely in the form of thiouric acid (an inactive metabolite), but no significant increase in congenital anomalies was documented in case-control studies that compared pregnancies with and without AZA exposure.Among pregnant women treated with AZA for inflammatory bowel disease or after renal transplant, no significant increase in fetal abnormalities has been detected.Azathioprine has been used to treat many immunologic glomerular diseases including lupus, IgA nephropathy, and vasculitis. It is taken by mouth or injected into a vein. While propranolol may not demonstrate consistent efficacy in research, it is a well-tolerated medication.
Available for Android and iOS devices. Azathioprine metabolism in kidney transplant recipients.