Bakersfield Mycophenolate Mofetil

Bakersfield Mycophenolate Mofetil

1 Mycophenolate Mofetil Rawan Mohammed Alqahtani Dr. Shaymaa Wagdy Ali 2 Mycophenolate Mofetil Introduction to the drug Mycophenolate mofetil is a medication that healthcare providers mainly use among other types of drugs to prevent the human body from rejecting various organ transplants like the kidney, heart, or even liver. This medication is also considered an inosine monophosphate dehydrogenase inhibitor. It is also referred to as a CellCept (Nickavar, & Sadeghian, 2017). The planted body organ can get attacked by the patient’s immune system, and it belongs to the class of medication referred to as the immunosuppressive agents. Mycophenolate does work by simply weakening the body’s immune system to make it less effective and get no ability to attack or even reject the organ that has been transplanted. Mechanism of the drug This medication, Mycophenolate mofetil, is made from mycophenolic acid (MPA). That is an inhibitor of inosine-5′-monophosphate dehydrogenase. MPA is a significant component that assists in depleting a guanosine nucleotide preferentially. That is in T and B lymphocytes. At the same time, it also inhibits proliferation. As a result, it suppresses the cell-mediated immune responses and antibody formation (Nickavar, & Sadeghian, 2017). Additionally, the MPA also prevents the expression of adhesion molecules and glycosylation in the human body. This medicine is also very active and functions more effectively by depleting tetrahydrobiopterin. At the same time, it also decreases the amount of nitric oxide that gets produced by the inducible NO synthase. That does occur without any interference in the activities of constitutive NO synthases (Bradbury et al., 2021). MPA plays a significant role in the recruitment of both lymphocytes and monocytes into the site of inflammation. 3 After activated, the macrophages produce NO and superoxide, which combine to form tissue-damaging peroxynitrite. MMF can develop an anti-inflammatory activity with the help of these two mechanisms. Contrary to the case of calcineurin inhibitors, MMF does not facilitate the production of TGFbeta, which is fibrogenic. MMF is not nephrotoxic, and it does reduce acute and chronic rejection in allograft recipients. Indication Based on the indication, Mycophenolate mofetil is recommended and has gotten indicated to prevent organ rejection. That is in those patients who are to undergo either hepatic, cardiac, or allogeneic renal transplants. For it to be more effective, it is recommended by healthcare providers to use it alongside cyclosporine and corticosteroids. This medication, Mycophenolate mofetil, can also get used as a second-line treatment for autoimmune hepatitis (Bradbury et al., 2021). That is necessary in case the first-line therapy has failed to respond effectively. Apart from that, this drug has a range of other uses, including dermatitis in children and lupus-associated nephritis. Contraindications Healthcare professionals have managed to observe the allergic reaction of CELLCEPT effectively. It gets contraindicated in patients experiencing hypersensitivity to various components of the drug products. For instance, as the mycophenolate mofetil or even mycophenolic acid. It also gets contraindicated in those patients who are allergic to Polysorbate. Potential toxicities and adverse effect The dosage of Mycophenolate mofetil depends on the type or kind of transplant to be performed. However, just like other drugs, this medication also has side or adverse effects that 4 the patient can experience. That negative effect can sometimes be severe, and they contain a range of factors, as stated below. 1. Mental or mood changes 2. Heartbeat that is fast or even irregular 3. Muscle weaknesses. Tachycardia and palpitation Fatigue 4. A person can also experience eyes that are bleeding or which are bruising 5. This drug can also cause swelling of the feet or even the ankle 6. There might be unusual changes in the amount of human urine 7. Difficulties to fall asleep or even staying asleep 8. A person or the patient can also experience other ill-health conditions such as constipation, headache, dizziness, diarrhoea, vomiting, and even stomach upset. Healthcare professionals recommend that the patient seek advice or consult the doctor or the pharmacist if any of these adverse effects last for so long or even worsen. Pharmacokinetic Parameters Bioavailability bioavailabilit ‫ اول شيء تعرف‬+ ‫راجع اللغه وعالمات الترقيم‬ ‫بعدين تتكلم عن الدواء‬ The bioavailability of the drug, mycophenolate Mofetil, gets affected by pantoprazole in healthy volunteers. The kind of influence on volunteers is caused by 40 mg of pantoprazole. That is taken twice a day and has got on bioavailability on single mycophenolate mofetil. 1000 mg dose can get experienced on investigated in patients or volunteers (Hedayatfar et al., 2017). High-performance liquid chromatography plays a significant role in measuring the plasma concentrations of mycophenolic acid. Additionally, it is also used to measure the inactive metabolite mycophenolic acid glucuronide. Following the sole administration of punctuation, Not academic language, Need development What is Bioavability?? then the drug 5 pharmacokinetic parameters, concomitant treatment through pantoprazole does assist in lowering the mycophenolic acid exposure (P < .001). That is after administering mycophenolate mofetil. As a result, the concentration does drop by 57%. Additionally, the area under the curve does decrease right from 0 to 12 hours by 27%. However, pantoprazole cannot change the pharmacokinetics of mycophenolate sodium that is enteric-coated. There is a high possibility that these findings or results cause a severe implication since the mycophenolic acid exposure and the incidence of acute rejections in renal transplant recipients are correlated (Hedayatfar et al., 2017). As a result, administering both pantoprazole and mycophenolate mofetil can cause insufficient mycophenolic acid exposure. That can increase the risk of failure in the treatment process. Volume of distribution and distribution phases The recommended distribution volume for the drug, mycophenolate mofetil, is 3.6 (±1.5) to 4.0 (±1.2) L/kg. This dosage contains the protein binding of mycophenolic acid and the drug’s metabolite, which is always 97% 13. This is mainly bound to albumin, and the inactive metabolite is 82% bound to plasma albumin. That is at an average therapeutic concentration. Mycophenolate Mofetil gets distributed in different phases; for instance, at the serum level, the MPA at a steady stage, the same dose gets distributed for two weeks in the range of 1.0 to 3.5 mcg/mL. That is an indication of adequate therapy. Additionally, the distribution level of Mycophenolic acid glucuronide ranges from 35 to 100 mcg/mL. That is a clear indication that the patient has got an average UGT metabolic capacity. MPA-G levels are typically in the range of 100 to 250 mcg/mL during the two weeks following transplantation (Hedayatfar et al., 2017). MPA-G typically decreases after this initial 6 post-transplant phase. According to the low MPA levels and high MPA-G levels, it does indicate that the respective patient has got an active UGT metabolic capability. Additionally, it also indicates that there is a high need for higher doses that are necessary for maintaining therapeutic levels of MPA. A patient with high UGT metabolic capacity requires at least 1 gram or more that is to be administered three times a day. That is to be maintained through serum MPA level in the range of 1.0 mcg/mL to 3.5 mcg/mL. There is the possibility of such a patient having MPA-G levels over 100 mcg/mL. At that point, MPA-G is inactive, though it does describe the metabolic status of the patient. There is a high possibility of patients with low UGT conjugating capability to be over-immunosuppressed. Clearance As indicated by (Nickavar et al., 2017), the plasma clearance of the mycophenolate mofetil is 193 mL/min. After an oral dose is taken and after an intravenous dose of 177 (±31) mL/min. (Nickavar et al., 2017) Half-life As indicated by (Nickavar et al., 2017), the recommended average apparent half-life of the drug, mycophenolate mofetil, is 17.9 (±6.5). That is in hours after oral administration. However, it becomes 16.6 (±5.8) hours after administering intravenous. Generally, mycophenolate mofetil do take an average of one week to be cleared in the human body. Protein and binding issues of drug As indicated in the Chinese Adult Kidney Transplant Recipients, there is a very significant impact of Protein Binding on Exposure of Unbound and Total Mycophenolic Acid. Based on that, the PK of both uMPA and unbound MPAG gets characterized by a two- and onecompartment model. That involves elimination of the first order. A linear protein binding model was adopted in linking the uMPA and tMPA. Through that, the constant protein binding rate got 7 established to be at 851 L/h, 718 L (18.5%) and 53.4/h (2.3%), respectively. It is also very clear through model-based simulation that changes in ALB concentrations has a great impact on tMPA but not uMPA exposure. In kidney transplant recipients, healthcare providers therefore recommend monitoring uMPA instead of tMPA. That is mainly to increase the impact of mycophenolate mofetil, mostly to patients with lower ALB levels. Drug Interactions Mycophenolate Mofetil does interact with many drugs, about 282. Of that number, they get grouped according to the impact of their interaction. In which 45 of them are considered central. At the same time, 209 of them are moderate. The remaining 28 are classified as minor interactions. The rate of interactions is affected by various factors such as specific products that affect the body by making it hard to absorb the mycophenolate whenever they get used at the same time along with that medication. However, healthcare professionals advise healthcare professionals to avoid taking this medication simultaneously with various drugs. For example, antacids contain aluminum or even colestipol. Additionally, medicines such as magnesium, cholestyramine, and even calcium-free phosphate binders. The following are some of the most frequently checked interactions for mycophenolate mofetil by the doctors of relevant healthcare providers. • Fish Oil (omega-3 polyunsaturated fatty acids) • Benadryl (diphenhydramine) • Aspir 81 (aspirin) • Eliquis (apixaban) • Bactrim (sulfamethoxazole / trimethoprim) • Aspirin Low Strength (aspirin) 8 • Calcium 600 D (calcium / vitamin d) • Lasix (furosemide) There is only one available alcohol or food interaction with mycophenolate mofetil. That is multivitamins with minerals. It also has got disease interactions with about six diseases which include the following • Vaccination • HGPRT deficiency • GI haemorrhage • Renal dysfunction • Neutropenia • Hepatic dysfunction Therapeutic Drug Monitoring Guidelines Drug half-life in adults As indicated by healthcare professionals, the recommended average apparent half-life of the drug, mycophenolate mofetil, in adults is 17.9 (±6.5). That is concerning hours after oral administration. There is also 16.6 (±5.8) hours which is after intravenous administration. The necessary recommended Plasma clearance of the drug is at 193 mL/min. That is after an oral dose is taken. A 177 (±31) mL/min is also necessary after an intravenous dose (Zhang et al., 2020). The period taken by mycophenolate within the human body do differ depending on certain common factors; for instance, it depends on the body condition or status, which makes people break down medications at a different rate. A healthy adult who is not pregnant can break down mycophenolate and be gone from the body within one week. However, those who are planning to be pregnant or those expecting pregnancy should engage their doctors or healthcare 9 providers to give them the necessary advice on when to stop taking the medication. That assist in preventing unnecessary complication or side effect due to the pregnancy. Target plasma concentrations Based on the Target plasma concentrations, there is a peak and through plasma level average of about 0.9 to 1.2 µg/mL and 0.2 to 0.5 µg/mL. That is mainly on an oral regimen of 1000 mg every 8 hours. Mycophenolate mofetil is a medication that has been proven to be very successful in many patients. Primarily those who are not responsive to other immunosuppressants (“Mycophenolate mofetil,” n.d.). For patients with no recommendation on the optimal dosage of MMF nor data concentration, drug exposure of MMF are available. That result involved the performance with108 through plasma samples. Through the use of EMIT was found to be very effective in most of the patients. Timing of sample Limited sampling strategy (LLS) is a technique that captures the complete characteristics of MPA’s PK. In the timing of the sample, LLS assist in estimating the AUC0–12. That is done through the use of a small number of instances, appropriately three or even less. Facilitating or modelling the kind of relationship that gets created between pharmacokinetic parameters and the drug concentration contributes to the reduction in the number of samples necessary (“Mycophenolate mofetil,” n.d.). The model is significant because it assists in determining the best sampling times concerning parameters in more accurate and precise. In developing this approach, complete pharmacokinetic profiles are necessary. It has to contain sufficient points to ensure it can measure AUC0–12 accurately. Most of the participants prefer the trapezoidal method; however, other common ones that they can also opt for include linear-logarithmic trapezoidal and even linear trapezoidal. The timing group has a significant role in determining 10 the relationship between AUC0–12 and the timed blood concentration data. That is through the use of linear regression. AUC0–12 is considered a dependent variable in which blood concentrations are considered the independent variable at each time point. In the timing sample, an equation is applied in defining AUC0–12 as a function of either one of several concentrations. Below is the equation. AUC0–12=Constant+(M1×C1)+(M2×C2)+(M3×C3)+(Mx×Cx) Time taken for steady state to be established in adults Concerning the expected time for a steady state to get established in an adult patient, it gets defined by the act of eliminating the drug’s half-life. A person can reach a 50% steady-state after one half-life. In the two half-lives, the patient would have reached a steady state of 75%, while in the thirst half-life, they would have reached 87.5% of the constant state. According to the rule of the thumb, the steady-state is achieved after five half-lives. That is after getting or completing 97% (“Mycophenolate mofetil,” n.d.). However, it is much possible to achieve a steady-state target level more quickly than expected when a drug with long life like mycophenolate is used. Mycophenolate does not function immediately; however, it takes up to 8 to 12 weeks before experiencing the benefits. However, it is recommended for the patient to continue with treatment all that time. Route of elimination In the general amount of drugs being taken in, a small amount gets excreted as MPA in the urine. That is about 1%. When given orally in a pharmacokinetic study, it was observed at 93% excreted in urine; however, it was at 6% excreted in faeces. Generally, about 87% of the entire administration gets removed in urine in the form of MPAG. A case studies 11 Various studies have been carried out on mycophenolate mofetil. One of them is on a journal of medicine that got documented by Bradbury et al. It is titled “Mycophenolate Mofetil for First-Line Treatment of Immune Thrombocytopenia.” The tough study assignment had 120 adult patients, of which 52.4% were men with a mean age of 54 and a range of 17 to 87. They were suffering from immune thrombocytopenia. They got first-line treatment with glucocorticoid. The second outcome was the response rate, side effects, and adverse events, among other issues such as bleeding and reported quality-of-life measures. There was no apparent difference between the groups concerning bleeding, rescue treatment, and even infection based on the results. However, there were worse quality-of-life outcomes on patients in the mycophenolate mofetil group. That is regarding physical function and fatigue. 12 References Mycophenolate mofetil. (n.d.). DrugBank Online | Database for Drug and Drug Target Info. https://go.drugbank.com/drugs/DB00688 Nickavar, A., & Sadeghian, M. (2017). Mycophenolate mofetil for the treatment of HenochSchönlein purpura nephritis; current knowledge and new concepts. Journal of nephropathology, 6(3), 103. Zhang, H., Zhou, M., Han, X., Yang, Y., & Yu, X. (2020). Mycophenolate mofetil in the treatment of Chinese patients with lupus nephritis: A PRISMA-compliant meta-analysis. Medicine, 99(33). Bradbury, C. A., Pell, J., Hill, Q., Bagot, C., Cooper, N., Ingram, J., … & Greenwood, R. (2021). Mycophenolate Mofetil for First-Line Treatment of Immune Thrombocytopenia. New England Journal of Medicine, 385(10), 885-895. Hackl, A., Becker, J. U., Körner, L. M., Ehren, R., Habbig, S., Nüsken, E., … & Weber, L. T. (2018). Mycophenolate mofetil following glucocorticoid treatment in Henoch-Schönlein purpura nephritis: the role of early initiation and therapeutic drug monitoring. Pediatric Nephrology, 33(4), 619-629. Hedayatfar, A., Falavarjani, K. G., Soheilian, M., Elmi Sadr, N., Modarres, M., Parvaresh, M. M., … & Chee, S. P. (2017). Mycophenolate mofetil for the treatment of multiple sclerosis-associated uveitis. Ocular immunology and inflammation, 25(3), 308-314. The assignments will be discussed under following headings Introduction to the drug o Mechanism of the drug o Indication o Contraindications Potential toxicities and Adverse effect. Pharmacokinetic Parameters o Bioavailability. o Volume of distribution and distribution phases. o Clearance. o Half-life o Protein and binding Tissue of drugs. • Drug Interactions • Therapeutic Drug Monitoring Guidelines o Drug half-life in adults o Target plasma concentrations o Timing of sample o Time taken for steady state to be established in adults o Route of elimination • A Case study (search on internet) • References proper cited in the text. N r Introduction (Main objectives or list of subtopics) Main objectives of the report are very clear and very detailed Information is directly linked to report topic с – 1 r Organization Info orga Information is very organized Visual aids are very creative, clear, and easy to read Report is consistently enhanced by the visual tools C Visual Tools (graphs and images) t E SION 30 Developmen No. Criterion Grammar, spelling & punctuation Exemplary=A (Far Exceeds Standard) Essay is free of distracting spelling, punctuation, and grammatical errors Meets all formal and assignment requirements and evidences attention to detail; all margins, spacing and indentations are correct; essay is neat and correctly assembled with professional look. Student consistently uses appropriate and unified reference styles for the quoted work in text and bibliography Formatting References Quotation and Plagiarism The report showed

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