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Immunomodulating Agents in Gastrointestinal Disease
Published in Thomas F. Kresina, Immune Modulating Agents, 2020
Samir A. Shah, Athos Bousvaros, A. Christopher Stevens
Mycophenolate mofetil is almost completely absorbed from the intestine, and almost completely converted to its active-metabolite mycophenolic acid (MPA) by deesterification in liver and peripheral tissue. Peak serum concentrations of MPA occur approximately 1 hour after ingestion of MMF, with the half-life of MPA ranging from 8 to 12 hours. Mycophenolic acid is eliminated by glucuronidation in the liver, followed by renal excretion of the glucuronide [182]. A high-performance liquid chromatographic assay for measurement of plasma MPA levels has been developed, but the optimal plasma MPA level for transplantation patients is not established [183].
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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Mycophenolate undergoes presystemic metabolism in the liver to active mycophenolic acid (MPA). MPA undergoes enterohepatic recirculation and secondary increases in plasma MPA concentrations are seen; these have been reported at between 6–12 hours after a dose of mycophenolate mofetil, and at between 6–8 hours after a dose of mycophenolate sodium. MPA is metabolised by glucuronidation to the inactive mycophenolic acid glucuronide.
Intestinal Transplantation
Published in John K. DiBaise, Carol Rees Parrish, Jon S. Thompson, Short Bowel Syndrome Practical Approach to Management, 2017
Sherilyn Gordon Burroughs, Douglas G. Farmer
Intermediate and long-term immunosuppressive goals include steroid weaning and a reduction in trough serum levels of tacrolimus to avoid cumulative morbidity. In addition to the universal risk for infection with immunosuppression, the well-known adverse effects of prolonged steroid use such as osteoporosis, adrenal insufficiency, peptic ulcer disease, psychosis, cataracts, growth failure in children, and glucose intolerance are augmented by the toxicities associated with other immunosuppressants used in ITx. For tacrolimus, neurotoxicity, nephrotoxicity, glucose intolerance, and hypertension predominate. With mycophenolic acid, bone marrow depression, mucosal ulcerations, and GI disturbances are problematic. The use of mTORi can result in bone marrow depression, nephrotic syndrome, stomatitis, pneumonitis, and dyslipidemia. Weaning of immunosuppression to avoid these complications must be tempered by the long-term risk for acute and chronic rejection, both significant problems after ITx.
Drugs repurposing for SARS-CoV-2: new insight of COVID-19 druggability
Published in Expert Review of Anti-infective Therapy, 2022
Sujit Kumar Debnath, Monalisha Debnath, Rohit Srivastava, Abdelwahab Omri
Human pluripotent stem cells were used to fabricate colonic organoid and lung models to evaluate the infection target. This cell line is more physiologically relevant than cancer cell lines. Using this model, different FDA-approved drugs were sorted that obstruct the entry of SARS-CoV-2 at physiologically relevant concentrations. Out of them, mycophenolic acid, quinacrine, and imatinib were the most promising candidates [103]. Mycophenolic acid is an immunosuppressant drug used to treat autoimmune conditions like Crohn’s disease and lupus. This drug is also used to prevent rejection during organ transplantations. This drug already showed effectiveness against several viruses like MERS-CoV, human coronavirus (HCoV)-OC43, mouse hepatitis virus, HCoV-NL63, dengue virus, etc. Due to the broad antiviral activity, this drug was explored for COVID-19. An in-vitro antiviral study on VeroE6/TMPRSS2 cells showed a robust cytopathogenic effect (CPE) against COVID-19 [107]. Quinacrine (Qx) is an antimalarial drug that has demonstrated antiviral, antiprion, and anticancer activities. The antiviral activity of Qx is associated with rising pH in acidic organelles, diminishing the enzymatic activity of viral cells, and the ability to bind with viral RNA and DNA. Vero E6 cells line was infected with SARS-CoV-2 to check the antiviral activity of Qx [108]. This study confirmed the reduction of SARS-CoV-2 virus replication and cytotoxicity after 48 h of Qx treatment to the cell line.
Application of Exposure Plus Response Prevention for Obsessive Compulsive Disorder Related to Pediatric Acute-Onset Neuropsychiatric Syndrome
Published in Evidence-Based Practice in Child and Adolescent Mental Health, 2021
Cynthia E. Brown, Kristin M. Hawley
At the beginning of treatment, Jessica was finishing a course of plasmapheresis, a procedure which involves the removal, treatment, and return of plasma into the body. In addition, Jessica received three rounds of inpatient (IVIG) early in treatment. IVIG involves the delivery of immunoglobulin to patients who have immunodeficiencies and suppresses idiotypic antibodies. Another immunosuppressant, mycophenolic acid (500–1000 mg, twice daily) was introduced during the 14th week of treatment and later discontinued. Jessica also received monoclonal antibodies (rituximab) in regular intervals throughout treatment. As a prophylactic against a GAS infection, Jessica received cefadroxil over the course of treatment. Lastly, Jessica took naproxen and an omega-3 supplement daily for anti-inflammatory effects.
Recent advances in the combination delivery of drug for leukemia and other cancers
Published in Expert Opinion on Drug Delivery, 2020
Thikrayat Al-Attar, Sundararajan V. Madihally
Artemisinin, a chemical compound that reacts with iron to produce free radicals, was incorporated in cancer cells treated for free radicals’ ability to kill cells. Electrospun core/shell nanofibers have been designed for targeted delivery and preservation of drug bioavailability [73]. Hyperbranched poly(butylene adipate), which is used as a crystal suppressant for artemisinin, is the core material, and Poly(vinylpyrrolidone) is the shell material. This delivery system effectively reduced prostatic cancer cell viability. Mycophenolic acid (MPA) is shown to inhibit many types of cancer cell growth but degrades quickly due to liver uptake. For the controlled release of MPA, coaxial fibers of PCL core containing MPA and PCL shells were used [74]. This fiber system was tested on glioblastoma multiforme tumor cells, which indicated strong cell suppression.