Mycophenolate 500mg Inj,1 Vial

Manufacturer MYLAN INSTITUTIONAL Active Ingredient Mycophenolate Mofetil Injection Solution(mye koe FEN oh late MOE fe til) Pronunciation mye koe FEN oh late MOE fe til
WARNING: Use of this drug during pregnancy may cause birth defects or death of the unborn baby. If you are able to become pregnant, you must use birth control that you can trust to prevent pregnancy while taking this drug. Your doctor must talk with you about how to avoid getting pregnant while taking this drug. A pregnancy test will be done right before starting this drug and repeated 8 to 10 days later to show that you are NOT pregnant. If you get pregnant or plan on getting pregnant while taking this drug, call your doctor right away.This drug may raise the chance of getting cancer like lymphoma or skin cancer. Call your doctor right away if you have a change in color or size of a mole, a skin lump or growth, a big weight loss, night sweats, or swollen glands.You may have more of a chance of getting an infection. Some infections have been severe or deadly. Wash hands often. Stay away from people with infections, colds, or flu.Call your doctor right away if you have any signs of infection like fever, chills, flu-like signs, very bad sore throat, ear or sinus pain, cough, more sputum or change in color of sputum, pain with passing urine, mouth sores, or a wound that will not heal. @ COMMON USES: It is used to keep the body from harming the organ after an organ transplant.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Immunosuppressant
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Pharmacologic Class
Inosine Monophosphate Dehydrogenase (IMPDH) Inhibitor
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Pregnancy Category
Category D
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FDA Approved
May 1998
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Mycophenolate is a medicine used to prevent your body from rejecting a transplanted organ (like a kidney, heart, or liver). It works by weakening your immune system so it doesn't attack the new organ. Because it weakens your immune system, it's very important to be careful about infections and to follow your doctor's instructions closely.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to follow the instructions carefully. This medication is administered as an infusion into a vein over a specified period.

Storing and Disposing of Your Medication

If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.

Missing a Dose

If you miss a dose, contact your doctor to receive guidance on the next steps to take.
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Lifestyle & Tips

  • Avoid live vaccines while taking this medication.
  • Practice good hygiene (frequent hand washing) to reduce the risk of infection.
  • Avoid contact with people who are sick or have infections.
  • Use sun protection (sunscreen, protective clothing) as this medication increases the risk of skin cancer.
  • Women of childbearing potential must use two reliable forms of contraception before, during, and for 6 weeks after stopping treatment due to severe birth defect risks.
  • Report any signs of infection, unusual bleeding/bruising, or new skin lesions to your doctor immediately.
  • Do not donate blood during therapy and for at least 6 weeks after stopping therapy. Do not donate semen during therapy and for 90 days after stopping therapy.

Dosing & Administration

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Adult Dosing

Standard Dose: Renal Transplant: 1 g IV twice daily (2 g/day). Cardiac Transplant: 1.5 g IV twice daily (3 g/day). Hepatic Transplant: 1 g IV twice daily (2 g/day).
Dose Range: 2000 - 3000 mg

Condition-Specific Dosing:

renal_transplant: 1 g IV twice daily
cardiac_transplant: 1.5 g IV twice daily
hepatic_transplant: 1 g IV twice daily
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Renal Transplant (โ‰ฅ3 months): 600 mg/mยฒ IV twice daily (maximum 2 g/day).
Adolescent: Renal Transplant: 600 mg/mยฒ IV twice daily (maximum 2 g/day).
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Dose Adjustments

Renal Impairment:

Mild: No dosage adjustment required.
Moderate: No dosage adjustment required.
Severe: For severe chronic renal impairment (GFR < 25 mL/min/1.73 mยฒ), avoid doses exceeding 1 g twice daily. Monitor patients closely.
Dialysis: MPA is not removed by hemodialysis. MPAG is removed. No specific dose adjustment for patients on dialysis, but monitor for adverse effects.

Hepatic Impairment:

Mild: No dosage adjustment required for renal transplant patients with severe hepatic parenchymal disease.
Moderate: No dosage adjustment required for renal transplant patients with severe hepatic parenchymal disease.
Severe: No dosage adjustment required for renal transplant patients with severe hepatic parenchymal disease. Data for other transplant types is limited.

Pharmacology

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Mechanism of Action

Mycophenolate mofetil (MMF) is a prodrug that is rapidly hydrolyzed to its active metabolite, mycophenolic acid (MPA). MPA is a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), an enzyme critical for the de novo synthesis of guanosine nucleotides. Lymphocytes are highly dependent on this pathway for proliferation, whereas other cell types can utilize salvage pathways. By inhibiting IMPDH, MPA effectively depletes guanosine nucleotides, thereby inhibiting lymphocyte proliferation and antibody formation, leading to potent immunosuppression.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (IV)
Tmax: Not applicable (IV administration)
FoodEffect: Not applicable (IV administration)

Distribution:

Vd: Approximately 4 L/kg (for MPA)
ProteinBinding: Approximately 97% (for MPA, primarily to albumin)
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 11-17 hours (for MPA)
Clearance: Approximately 11.6 L/hr (for MPA)
ExcretionRoute: Primarily renal excretion of MPAG (inactive metabolite); a small amount of MPA is excreted in bile via enterohepatic recirculation.
Unchanged: Less than 1% (of MMF)
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Pharmacodynamics

OnsetOfAction: Rapid (immunosuppressive effects are seen shortly after achieving therapeutic concentrations)
PeakEffect: Peak MPA concentrations are achieved shortly after infusion completion. Immunosuppressive effect is sustained with regular dosing.
DurationOfAction: Dependent on maintaining therapeutic concentrations; typically 12 hours with twice-daily dosing.

Safety & Warnings

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BLACK BOX WARNING

Increased risk of serious infections, including opportunistic infections, leading to hospitalizations or death. Increased risk of lymphoma and other malignancies, particularly skin cancer. Increased risk of first trimester pregnancy loss and congenital malformations. Mycophenolate mofetil should not be used in pregnant women unless the benefits clearly outweigh the risks. Women of childbearing potential must use highly effective contraception.
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Side Effects

Serious Side Effects: Seek Medical Help Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:

Allergic reactions: Rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
High blood sugar: Confusion, feeling sleepy, unusual thirst or hunger, frequent urination, flushing, fast breathing, or breath that smells like fruit.
Electrolyte problems: Mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance changes, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting.
High or low blood pressure: Severe headache or dizziness, fainting, or changes in vision.
Kidney problems: Inability to urinate, changes in urine output, blood in the urine, or significant weight gain.
Skin infections: Oozing, heat, swelling, redness, or pain.
Cardiovascular issues: Chest pain or pressure.
Abnormal heart rhythms: Fast, slow, or irregular heartbeat.
Unexplained bleeding: Unusual bruising or bleeding, vomiting blood or coffee ground-like material, or black, tarry, or bloody stools.
Nerve problems: Burning, numbness, or tingling sensations that are not normal.
Muscle issues: Muscle cramps or swelling.
Other symptoms: Pale skin, white patches in the mouth, vaginal itching or discharge, or yellow skin and eyes.

Rare but Serious Conditions

Acute inflammatory syndrome (AIS): This condition can occur within weeks to months after starting this medication or after a dose increase. Seek medical help immediately if you experience fever, joint pain or stiffness, or muscle pain.
Progressive multifocal leukoencephalopathy (PML): This rare brain condition can cause disability or be life-threatening. Contact your doctor right away if you notice confusion, memory problems, depression, changes in behavior, weakness on one side of the body, speech or thinking difficulties, balance changes, or vision changes.
BK virus infection: In people who have had a kidney transplant, this viral infection can cause kidney damage or loss. Seek medical help immediately if you experience changes in urine output, difficulty or pain while urinating, or blood in the urine.
Lung problems: Although rare, this medication can cause lung problems, which can be life-threatening. Contact your doctor right away if you experience shortness of breath, trouble breathing, new or worsening cough, or fever.

Common Side Effects

Not all medications cause side effects, and many people experience only minor or no side effects. However, if you notice any of the following symptoms, contact your doctor or seek medical attention:

Back pain
Constipation, diarrhea, stomach pain, nausea, vomiting, or decreased appetite
Headache
Gas
Dizziness, fatigue, or weakness
Shakiness
Sleep disturbances
Irritation at the injection site

Reporting Side Effects

If you experience any side effects that bother you or do not go away, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Fever, chills, sore throat, body aches (signs of infection)
  • Unusual bleeding or bruising
  • Extreme tiredness or weakness
  • Swollen glands (lymph nodes)
  • New skin lesions or changes in existing moles
  • Severe diarrhea, nausea, or vomiting
  • Yellowing of skin or eyes (jaundice)
  • Dark urine or pale stools
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced.
If you have been diagnosed with Lesch-Nyhan or Kelley-Seegmiller syndrome, or a rare inherited deficiency of hypoxanthine-guanine phosphoribosyltransferase (HGPRT).
If you are currently taking any of the following medications: Azathioprine, cholestyramine, colesevelam, colestipol, norfloxacin with metronidazole, or sevelamer.
If you are taking another medication that contains the same active ingredient as this drug.
If you are able to become pregnant and are not using two forms of birth control.
If you are breastfeeding or plan to breastfeed.

This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you may have. Your doctor will help you determine whether it is safe to take this medication with your other medications and health conditions. Do not start, stop, or change the dose of any medication without consulting your doctor first.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you.

Regular blood work and laboratory tests, as directed by your doctor, are crucial to monitor your health. If you have diabetes, it is vital to closely monitor your blood sugar levels.

Before receiving any vaccinations, consult with your doctor, as certain vaccines may increase the risk of infection or reduce their effectiveness when taken with this medication.

You may experience increased bleeding tendencies, so it is crucial to be cautious and avoid injuries. To minimize the risk of bleeding, use a soft toothbrush and an electric razor.

Prolonged exposure to sunlight, sunlamps, and tanning beds may increase the risk of skin cancer. To protect yourself, use sunscreen, wear protective clothing, and eyewear that shields you from the sun.

Your doctor may recommend testing for Hepatitis B or C, as this medication may worsen existing infections.

There is a risk of gastrointestinal tract bleeding, holes, and ulcers associated with this medication, which may require hospitalization. Discuss any concerns with your doctor.

This medication may cause diarrhea. If you experience diarrhea, consult with your doctor to explore ways to manage this side effect. Do not stop taking this medication without consulting your doctor.

You may need to avoid donating blood while taking this medication and for a certain period after stopping it. Consult with your doctor for specific guidance.

If you are a male patient, you may need to avoid donating sperm while taking this medication and for a certain period after stopping it. If you have questions or concerns, discuss them with your doctor.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

If you are a female patient of childbearing age, it is essential to use birth control while taking this medication and for at least 6 weeks after your last dose. Note that birth control pills and other hormone-based birth control methods may be less effective during this time. Consider using additional forms of birth control, such as condoms. If you become pregnant, notify your doctor immediately.

If your partner may become pregnant, use birth control while taking this medication and for at least 90 days after your last dose. If your partner becomes pregnant, notify the doctor right away.
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Overdose Information

Overdose Symptoms:

  • Severe myelosuppression (e.g., neutropenia, anemia, thrombocytopenia)
  • Gastrointestinal disturbances (e.g., severe diarrhea, vomiting)

What to Do:

There is no specific antidote. Treatment is supportive. Hemodialysis is not effective in removing MPA. Cholestyramine may remove MPA by interrupting enterohepatic recirculation. Call 1-800-222-1222 (Poison Control Center) or seek immediate medical attention.

Drug Interactions

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Contraindicated Interactions

  • Live attenuated vaccines (due to risk of infection in immunosuppressed patients)
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Major Interactions

  • Acyclovir, Ganciclovir (increased concentrations of both drugs, risk of myelosuppression)
  • Cholestyramine (decreased MPA exposure)
  • Antacids containing magnesium or aluminum hydroxide (decreased MPA absorption if oral, but less relevant for IV)
  • Probenecid (increased MPA and MPAG concentrations)
  • Tacrolimus (potential for altered MPA exposure, monitor levels)
  • Cyclosporine (decreased MPA exposure, monitor levels)
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Moderate Interactions

  • Oral contraceptives (potential for reduced efficacy of oral contraceptives, use alternative birth control)
  • Rifampin (decreased MPA exposure)
  • Sevelamer (decreased MPA exposure)
  • Telmisartan (decreased MPA exposure)
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Complete Blood Count (CBC) with differential

Rationale: To establish baseline hematologic parameters and identify pre-existing cytopenias.

Timing: Prior to initiation of therapy

Liver Function Tests (LFTs)

Rationale: To assess baseline hepatic function.

Timing: Prior to initiation of therapy

Renal Function (BUN, Creatinine, GFR)

Rationale: To assess baseline renal function and guide dosing adjustments if needed.

Timing: Prior to initiation of therapy

Viral Serologies (e.g., CMV, EBV, HBV, HCV)

Rationale: To assess risk of opportunistic infections in immunosuppressed patients.

Timing: Prior to initiation of therapy

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Routine Monitoring

Complete Blood Count (CBC) with differential

Frequency: Weekly for the first month, then twice monthly for the second and third months, then monthly thereafter.

Target: Maintain WBC > 2,500/mmยณ, ANC > 1,500/mmยณ, Platelets > 75,000/mmยณ

Action Threshold: Neutropenia (ANC < 1.3 x 10ยณ/ยตL), severe leukopenia, or other significant cytopenias may require dose reduction or interruption.

Liver Function Tests (LFTs)

Frequency: Periodically, or as clinically indicated.

Target: Within normal limits or stable baseline

Action Threshold: Significant elevations may require investigation and dose adjustment.

Renal Function (BUN, Creatinine)

Frequency: Periodically, or as clinically indicated.

Target: Stable baseline

Action Threshold: Significant decline may require dose adjustment.

Mycophenolic Acid (MPA) Trough Levels (Therapeutic Drug Monitoring)

Frequency: Not routinely recommended for all patients, but may be considered in specific situations (e.g., suspected non-adherence, malabsorption, unexplained toxicity, or rejection).

Target: Varies by transplant type and center, typically 1-3.5 mcg/mL (trough) for renal transplant.

Action Threshold: Levels outside target range may warrant dose adjustment.

Signs and Symptoms of Infection

Frequency: Continuously

Target: Absence of fever, chills, malaise, or localized signs of infection.

Action Threshold: Prompt evaluation and treatment for any signs of infection.

Skin Examination

Frequency: Annually

Target: Absence of suspicious skin lesions

Action Threshold: Referral to dermatology for any new or changing skin lesions.

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Symptom Monitoring

  • Signs of infection (fever, chills, sore throat, unusual fatigue, cough, painful urination)
  • Gastrointestinal disturbances (nausea, vomiting, diarrhea, abdominal pain)
  • Unusual bleeding or bruising
  • Skin changes (new moles, skin lesions)
  • Swelling of lymph nodes

Special Patient Groups

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Pregnancy

Mycophenolate mofetil is highly teratogenic and is associated with a significantly increased risk of first trimester pregnancy loss and congenital malformations, including ear, facial, cardiac, and limb abnormalities. It should not be used in pregnant women unless the potential benefits outweigh the risks, and only after careful counseling regarding the significant risks. A Pregnancy Registry is available.

Trimester-Specific Risks:

First Trimester: High risk of spontaneous abortion (45-49%) and major congenital malformations (23-27%).
Second Trimester: Risk of continued exposure is high due to potential for fetal growth restriction and other adverse outcomes.
Third Trimester: Risk of continued exposure is high due to potential for fetal growth restriction and other adverse outcomes.
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Lactation

Mycophenolic acid (MPA) is excreted into breast milk in rats. It is unknown whether MPA is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment with mycophenolate mofetil.

Infant Risk: High risk (L5 - Contraindicated)
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Pediatric Use

Dosing is typically based on body surface area for children โ‰ฅ3 months of age. Safety and efficacy in pediatric renal transplant patients <3 months of age have not been established. Pediatric patients may be at increased risk for certain infections (e.g., EBV-associated lymphoproliferative disease).

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Geriatric Use

No specific dosage adjustment is required based on age. However, elderly patients may be more susceptible to adverse effects, including gastrointestinal, hematologic, and infectious complications. Monitor closely for adverse reactions.

Clinical Information

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Clinical Pearls

  • Mycophenolate mofetil IV is indicated for patients unable to take oral mycophenolate mofetil. Patients should be switched to oral therapy as soon as they can tolerate it.
  • Administer IV infusion over no less than 2 hours to minimize the risk of local adverse reactions.
  • Do not administer by rapid or bolus intravenous injection.
  • Reconstitute and dilute according to manufacturer's instructions; it is incompatible with other IV solutions and should be administered via a separate infusion line.
  • Patients should be educated on the importance of infection prevention and sun protection.
  • Due to the teratogenic risk, ensure strict adherence to contraception guidelines for women of childbearing potential.
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Alternative Therapies

  • Azathioprine
  • Sirolimus
  • Everolimus
  • Belatacept
  • Tacrolimus
  • Cyclosporine
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Cost & Coverage

Average Cost: Varies widely, check current pricing per 500mg vial
Generic Available: Yes
Insurance Coverage: Tier 3 or 4 (Specialty Drug)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication.

This medication is accompanied by a Medication Guide, which is a valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you refill your prescription. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, pharmacist, or other healthcare provider for clarification.

In the event of a suspected overdose, it's crucial to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred.