Neoral 100mg/ml Oral Soln 50ml
WARNING: 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.Lymphoma and other cancers have happened in people who take this drug or drugs like it. This has been deadly in some cases. Talk with the doctor.If this drug is given with other drugs that work on the immune system, it can add to the chance of getting an infection or lymphoma or other cancers. Call your doctor right away if you have a change in color or size of a mole; a lump in the armpit, groin, or neck; or any new or changing skin lump or growth. Talk with the doctor.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.This drug may cause kidney problems in some patients. Talk with the doctor. High blood pressure has happened with this drug. Have your blood pressure checked as you have been told by your doctor.Have your blood work and other lab tests checked as you have been told by your doctor.There are different brands and forms of this drug. Do not switch between different brands or forms of this drug without calling the doctor who ordered it.If you are taking this drug for psoriasis AND you have used other drugs or radiation to treat this health problem before, your chance of skin cancer may be higher. @ COMMON USES: It is used to keep the body from harming the organ after an organ transplant.It is used to treat rheumatoid arthritis.It is used to treat psoriasis.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Immunosuppressant
Pharmacologic Class
Calcineurin Inhibitor
Pregnancy Category
C
FDA Approved
Jan 1995
DEA Schedule
Not Controlled
Overview
What is this medicine?
Cyclosporine is a medicine that helps to calm down your body's immune system. This is important for people who have received an organ transplant, to prevent their body from rejecting the new organ. It's also used for certain autoimmune diseases like severe psoriasis or rheumatoid arthritis, where the immune system mistakenly attacks the body's own tissues. By weakening the immune system, it helps your body accept the new organ or stops it from attacking itself.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely. You can take your medication with or without food, but it's essential to take it the same way each time. Choose to always take it with food or always take it on an empty stomach to maintain consistency.
If you are also taking sirolimus, be sure to take it 4 hours after taking this medication. Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well. Establish a routine by taking your medication at the same time every day.
When measuring liquid doses, use the measuring device provided with your medication to ensure accuracy. Do not rinse the syringe before or after taking your dose. If you need to clean the syringe, make sure it is completely dry before using it again.
To mix the solution, combine it with orange or apple juice at room temperature in a glass. Drink the mixture immediately, then rinse the glass with more liquid and drink the rinse solution.
Storing and Disposing of Your Medication
Store your medication at room temperature, avoiding refrigeration or freezing. Keep it in its original container to maintain its potency. Discard any unused portion of the medication 2 months after opening the container.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely. You can take your medication with or without food, but it's essential to take it the same way each time. Choose to always take it with food or always take it on an empty stomach to maintain consistency.
If you are also taking sirolimus, be sure to take it 4 hours after taking this medication. Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well. Establish a routine by taking your medication at the same time every day.
When measuring liquid doses, use the measuring device provided with your medication to ensure accuracy. Do not rinse the syringe before or after taking your dose. If you need to clean the syringe, make sure it is completely dry before using it again.
To mix the solution, combine it with orange or apple juice at room temperature in a glass. Drink the mixture immediately, then rinse the glass with more liquid and drink the rinse solution.
Storing and Disposing of Your Medication
Store your medication at room temperature, avoiding refrigeration or freezing. Keep it in its original container to maintain its potency. Discard any unused portion of the medication 2 months after opening the container.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take this medication exactly as prescribed, at the same time each day, consistently with or without food (but be consistent).
- Do not switch between Neoral and other cyclosporine formulations (e.g., Sandimmune or generic modified cyclosporine) without your doctor's explicit instruction, as they are not interchangeable.
- Do not drink grapefruit juice or eat grapefruit while taking this medication, as it can significantly increase drug levels and side effects.
- Avoid St. John's Wort, as it can decrease drug levels and lead to organ rejection.
- Protect yourself from the sun (wear protective clothing, use sunscreen) as this medication can increase your risk of skin cancer.
- Practice good hygiene and avoid sick people to reduce your risk of infection, as your immune system will be weaker.
- Report any signs of infection (fever, chills, sore throat) immediately to your doctor.
- Do not receive any live vaccines without consulting your doctor.
- Limit potassium-rich foods and avoid potassium supplements unless directed by your doctor, due to risk of high potassium levels.
- Regularly monitor your blood pressure at home if advised by your doctor.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly by indication and patient response, typically initiated at 2-10 mg/kg/day in 2 divided doses, then adjusted based on trough levels.
Dose Range:
2 - 10 mg
Condition-Specific Dosing:
Kidney Transplant:
Initial: 8-10 mg/kg/day orally in 2 divided doses, starting 4-12 hours pre-transplant. Maintenance: 2-6 mg/kg/day.
Liver Transplant:
Initial: 8-10 mg/kg/day orally in 2 divided doses, starting 4-12 hours pre-transplant. Maintenance: 2-6 mg/kg/day.
Heart Transplant:
Initial: 10-15 mg/kg/day orally in 2 divided doses, starting 4-12 hours pre-transplant. Maintenance: 2-6 mg/kg/day.
Rheumatoid Arthritis:
Initial: 2.5 mg/kg/day orally in 2 divided doses. May increase by 0.5-0.75 mg/kg/day every 4 weeks to a max of 4 mg/kg/day.
Psoriasis:
Initial: 2.5 mg/kg/day orally in 2 divided doses. May increase by 0.5 mg/kg/day every 2 weeks to a max of 5 mg/kg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Dosing similar to older children/adults on a mg/kg basis, but often requires higher doses due to faster clearance. Close monitoring of trough levels is crucial.
Child:
Dosing similar to adults on a mg/kg basis, often requiring higher doses (e.g., 5-10 mg/kg/day initially for transplant) due to faster clearance. Adjust based on trough levels.
Adolescent:
Dosing similar to adults on a mg/kg basis, adjust based on trough levels.
Dose Adjustments
Renal Impairment:
Mild:
No specific initial dose adjustment, but monitor renal function closely and adjust dose to maintain target trough levels while minimizing nephrotoxicity.
Moderate:
No specific initial dose adjustment, but monitor renal function closely and adjust dose to maintain target trough levels while minimizing nephrotoxicity. Dose reduction may be necessary.
Severe:
Use with caution. Significant dose reduction may be required. Monitor renal function and cyclosporine trough levels frequently.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis or peritoneal dialysis. Dose adjustment based on trough levels and clinical response is necessary.
Hepatic Impairment:
Mild:
Use with caution. Monitor cyclosporine trough levels and liver function tests closely. Dose reduction may be necessary.
Moderate:
Significant dose reduction (e.g., 25-50% of usual dose) is often required. Monitor cyclosporine trough levels and liver function tests frequently.
Severe:
Contraindicated or used with extreme caution and significant dose reduction. Monitor cyclosporine trough levels and liver function tests very frequently. Patients with severe liver impairment may have significantly prolonged half-life and increased exposure.
Pharmacology
Mechanism of Action
Cyclosporine is a calcineurin inhibitor. It forms a complex with cyclophilin, an intracellular immunophilin. This complex then binds to and inhibits calcineurin, a phosphatase that is essential for the activation of T-lymphocytes. By inhibiting calcineurin, cyclosporine prevents the dephosphorylation of the nuclear factor of activated T-cells (NF-AT), which is required for its translocation into the nucleus. This, in turn, inhibits the transcription of various cytokine genes, including interleukin-2 (IL-2), which is crucial for T-cell proliferation and differentiation. The net effect is a potent immunosuppressive action.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable, approximately 20-50% (Neoral has more consistent and higher bioavailability than Sandimmune, ~30-60% for Neoral).
Tmax:
1.5-2 hours (Neoral)
FoodEffect:
Food can delay Tmax and decrease Cmax, but the overall AUC is generally not significantly affected for Neoral. However, consistent administration relative to meals is recommended.
Distribution:
Vd:
3.5-5 L/kg (variable, higher in children)
ProteinBinding:
90-98% (primarily to lipoproteins)
CnssPenetration:
Limited (low concentrations in CSF, but can cause neurotoxicity)
Elimination:
HalfLife:
Approximately 8.4 hours (range 5-18 hours, highly variable)
Clearance:
0.4-0.7 L/hr/kg (variable, higher in children)
ExcretionRoute:
Primarily biliary (fecal, ~6% renal)
Unchanged:
<1% in urine
Pharmacodynamics
OnsetOfAction:
Immunosuppressive effects begin within hours to days, but full therapeutic effect may take weeks.
PeakEffect:
Peak immunosuppression is achieved with stable therapeutic trough levels.
DurationOfAction:
Dependent on drug levels; continuous exposure is required for sustained immunosuppression.
Safety & Warnings
BLACK BOX WARNING
Cyclosporine (modified) should be administered by physicians experienced in immunosuppressive therapy. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information for the patient's management. Increased susceptibility to infection and the possible development of lymphoma and other malignancies are complications of immunosuppression. This drug, due to its potential for nephrotoxicity and hepatotoxicity, should be used with caution. Renal and liver function, blood pressure, and cyclosporine blood concentrations should be monitored. Neoral and Sandimmune are not bioequivalent and cannot be used interchangeably without physician supervision. The absorption of Neoral is more consistent and less dependent on the presence of bile than that of Sandimmune.
Side Effects
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: 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
Signs of high blood pressure: severe headache, dizziness, fainting, or changes in vision
Signs of kidney problems: inability to urinate, changes in urine output, blood in the urine, or sudden weight gain
Signs of electrolyte problems: mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance problems, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting
Unexplained bruising or bleeding
Feeling extremely tired or weak
Abnormal sensations such as burning, numbness, or tingling
Chest pain or pressure, or rapid heartbeat
Gum changes
Hearing loss
Shortness of breath
Shakiness
Swelling
Mouth irritation or mouth sores
Liver Problems
This medication can cause liver problems, which can be fatal. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Fatigue
Decreased appetite
Nausea or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Progressive Multifocal Leukoencephalopathy (PML)
This medication can cause a rare and potentially fatal brain problem called PML. If you experience any of the following symptoms, contact your doctor immediately:
Confusion
Memory problems
Depression
Changes in behavior
Weakness on one side of the body
Difficulty speaking or thinking
Balance problems
Changes in vision
Posterior Reversible Encephalopathy Syndrome (PRES)
This medication can cause a rare and potentially fatal brain problem called PRES. If you experience any of the following symptoms, contact your doctor immediately:
Confusion
Decreased alertness
Changes in vision
Loss of vision
Seizures
Severe headache
Other Side Effects
Most people do not experience serious side effects, but some may occur. If you experience any of the following side effects, contact your doctor if they bother you or do not go away:
Headache
Dizziness or drowsiness
Stomach pain or diarrhea
Nausea or vomiting
Gas
Hair growth
Acne
Flushing
Common cold symptoms
Joint pain
Leg cramps
Reporting Side Effects
If you have questions about side effects or want to report a side effect, 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.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: 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
Signs of high blood pressure: severe headache, dizziness, fainting, or changes in vision
Signs of kidney problems: inability to urinate, changes in urine output, blood in the urine, or sudden weight gain
Signs of electrolyte problems: mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance problems, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting
Unexplained bruising or bleeding
Feeling extremely tired or weak
Abnormal sensations such as burning, numbness, or tingling
Chest pain or pressure, or rapid heartbeat
Gum changes
Hearing loss
Shortness of breath
Shakiness
Swelling
Mouth irritation or mouth sores
Liver Problems
This medication can cause liver problems, which can be fatal. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Fatigue
Decreased appetite
Nausea or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Progressive Multifocal Leukoencephalopathy (PML)
This medication can cause a rare and potentially fatal brain problem called PML. If you experience any of the following symptoms, contact your doctor immediately:
Confusion
Memory problems
Depression
Changes in behavior
Weakness on one side of the body
Difficulty speaking or thinking
Balance problems
Changes in vision
Posterior Reversible Encephalopathy Syndrome (PRES)
This medication can cause a rare and potentially fatal brain problem called PRES. If you experience any of the following symptoms, contact your doctor immediately:
Confusion
Decreased alertness
Changes in vision
Loss of vision
Seizures
Severe headache
Other Side Effects
Most people do not experience serious side effects, but some may occur. If you experience any of the following side effects, contact your doctor if they bother you or do not go away:
Headache
Dizziness or drowsiness
Stomach pain or diarrhea
Nausea or vomiting
Gas
Hair growth
Acne
Flushing
Common cold symptoms
Joint pain
Leg cramps
Reporting Side Effects
If you have questions about side effects or want to report a side effect, 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.
Seek Immediate Medical Attention If You Experience:
- Signs of infection: fever, chills, sore throat, body aches, unusual fatigue, painful urination.
- Signs of kidney problems: swelling in your feet or ankles, decreased urination, unusual tiredness.
- Signs of liver problems: yellowing of your skin or eyes (jaundice), dark urine, persistent nausea or vomiting, severe stomach pain.
- Signs of high blood pressure: severe headache, blurred vision, pounding in your neck or ears.
- Signs of nervous system problems: tremor (shaking), headache, confusion, seizures, numbness or tingling, visual disturbances.
- Unusual bleeding or bruising.
- Muscle pain or weakness.
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 conditions and factors to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reactions you have experienced.
Existing health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
Concurrent medications, such as:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
If you have psoriasis and are undergoing other treatments, including medications or radiation therapy.
This list is not exhaustive, and it is crucial to disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues to your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing treatments and conditions.
To minimize the risk of severe, life-threatening, or fatal side effects, it is vital to be aware of potential interactions between this medication and other substances. Your doctor and pharmacist must be informed about all your medications and health problems to ensure your safety. Do not initiate, discontinue, or modify the dosage of any medication without consulting your doctor.
It is essential to inform your doctor about the following conditions and factors to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reactions you have experienced.
Existing health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
Concurrent medications, such as:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
If you have psoriasis and are undergoing other treatments, including medications or radiation therapy.
This list is not exhaustive, and it is crucial to disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues to your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing treatments and conditions.
To minimize the risk of severe, life-threatening, or fatal side effects, it is vital to be aware of potential interactions between this medication and other substances. Your doctor and pharmacist must be informed about all your medications and health problems to ensure your safety. Do not initiate, discontinue, or modify the dosage of any medication without consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in any activity that requires your full attention, wait until you understand how this medication affects you.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this drug.
If you are using a salt substitute containing potassium, a potassium-sparing diuretic, or any potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is important to discuss this with your doctor.
There may be an increased risk of skin cancer associated with this medication. To minimize this risk, limit your exposure to sunlight, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear. Follow your doctor's recommendations for regular skin checks.
In rare cases, this medication has been linked to severe kidney problems caused by the BK virus, particularly in individuals who have undergone a kidney transplant. This infection can lead to the loss of the transplanted kidney. If you have concerns, discuss them with your doctor.
Before receiving any vaccinations, consult your doctor, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication.
Maintain good oral hygiene and schedule regular dental check-ups to prevent potential complications.
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Be aware of the possibility of gout attacks and monitor your condition accordingly.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
For pediatric patients, this medication should be used with caution, as the risk of certain side effects may be higher in children.
This medication may harm an unborn baby if taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this medication, contact your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Before operating a vehicle or engaging in any activity that requires your full attention, wait until you understand how this medication affects you.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this drug.
If you are using a salt substitute containing potassium, a potassium-sparing diuretic, or any potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is important to discuss this with your doctor.
There may be an increased risk of skin cancer associated with this medication. To minimize this risk, limit your exposure to sunlight, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear. Follow your doctor's recommendations for regular skin checks.
In rare cases, this medication has been linked to severe kidney problems caused by the BK virus, particularly in individuals who have undergone a kidney transplant. This infection can lead to the loss of the transplanted kidney. If you have concerns, discuss them with your doctor.
Before receiving any vaccinations, consult your doctor, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication.
Maintain good oral hygiene and schedule regular dental check-ups to prevent potential complications.
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Be aware of the possibility of gout attacks and monitor your condition accordingly.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
For pediatric patients, this medication should be used with caution, as the risk of certain side effects may be higher in children.
This medication may harm an unborn baby if taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this medication, contact your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Severe kidney problems (e.g., acute renal failure)
- Severe liver problems
- Severe hypertension
- Severe neurological symptoms (e.g., seizures, coma)
- Nausea, vomiting, abdominal pain
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive; there is no specific antidote. Cyclosporine is not dialyzable.
Drug Interactions
Contraindicated Interactions
- Bosentan (increased cyclosporine levels, hepatotoxicity)
- Aliskiren (increased aliskiren levels, nephrotoxicity)
- Dabigatran (increased dabigatran levels)
- Statins (e.g., lovastatin, simvastatin, atorvastatin) at high doses (increased statin levels, rhabdomyolysis risk)
- Live attenuated vaccines (risk of infection in immunosuppressed patients)
- Potassium-sparing diuretics (e.g., amiloride, spironolactone, triamterene) and potassium supplements (risk of hyperkalemia)
- Concomitant use with other nephrotoxic drugs (e.g., aminoglycosides, amphotericin B, NSAIDs, tacrolimus) should be avoided or used with extreme caution.
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, diltiazem, verapamil, grapefruit juice) - significantly increase cyclosporine levels.
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, St. John's Wort) - significantly decrease cyclosporine levels.
- Nephrotoxic agents (e.g., NSAIDs, aminoglycosides, amphotericin B, trimethoprim/sulfamethoxazole) - increased risk of nephrotoxicity.
- Mycophenolate mofetil (decreased mycophenolic acid AUC, increased cyclosporine levels).
- Sirolimus/Everolimus (increased sirolimus/everolimus levels, increased risk of nephrotoxicity).
- Digoxin (increased digoxin levels).
- Colchicine (increased colchicine levels, toxicity).
- Oral contraceptives (increased cyclosporine levels, increased estrogen levels).
- Vaccines (reduced efficacy of vaccines, increased risk with live vaccines).
Moderate Interactions
- Calcium channel blockers (e.g., nifedipine, nicardipine) - may increase cyclosporine levels.
- Metoclopramide (may increase cyclosporine levels).
- Danazol (may increase cyclosporine levels).
- Allopurinol (may increase cyclosporine levels).
- Cimetidine (may increase cyclosporine levels).
- Ranitidine (may increase cyclosporine levels).
- Methotrexate (increased risk of hepatotoxicity and nephrotoxicity).
- Non-depolarizing muscle relaxants (prolonged neuromuscular blockade).
Minor Interactions
- Food (consistent administration relative to meals is important for Neoral).
Monitoring
Baseline Monitoring
Renal function (serum creatinine, BUN, GFR)
Rationale: To establish baseline and monitor for nephrotoxicity.
Timing: Prior to initiation.
Liver function tests (ALT, AST, ALP, bilirubin)
Rationale: To establish baseline and monitor for hepatotoxicity.
Timing: Prior to initiation.
Blood pressure
Rationale: To establish baseline and monitor for hypertension.
Timing: Prior to initiation.
Lipid profile (total cholesterol, LDL, HDL, triglycerides)
Rationale: To establish baseline and monitor for dyslipidemia.
Timing: Prior to initiation.
Electrolytes (potassium, magnesium)
Rationale: To establish baseline and monitor for hyperkalemia and hypomagnesemia.
Timing: Prior to initiation.
Complete Blood Count (CBC) with differential
Rationale: To establish baseline and monitor for hematologic abnormalities.
Timing: Prior to initiation.
Uric acid
Rationale: To establish baseline and monitor for hyperuricemia.
Timing: Prior to initiation.
Routine Monitoring
Cyclosporine whole blood trough levels (C0)
Frequency: Initially 2-3 times per week, then weekly, then monthly once stable. More frequently with dose changes or drug interactions.
Target: Highly variable by indication, time post-transplant, and lab assay (e.g., 100-400 ng/mL for transplant, 50-200 ng/mL for autoimmune diseases).
Action Threshold: Levels outside target range; adjust dose to maintain therapeutic levels while minimizing toxicity.
Renal function (serum creatinine, BUN, GFR)
Frequency: Weekly for first month, then every 2-4 weeks, then monthly once stable.
Target: Within patient's baseline or acceptable limits.
Action Threshold: Increase in serum creatinine >25-30% from baseline or significant decline in GFR; consider dose reduction or alternative.
Liver function tests (ALT, AST, ALP, bilirubin)
Frequency: Weekly for first month, then every 2-4 weeks, then monthly once stable.
Target: Within normal limits.
Action Threshold: Significant elevation; consider dose reduction or alternative.
Blood pressure
Frequency: Daily initially, then weekly, then monthly.
Target: <140/90 mmHg (or patient-specific target).
Action Threshold: Sustained hypertension; initiate or adjust antihypertensive therapy.
Electrolytes (potassium, magnesium)
Frequency: Weekly for first month, then every 2-4 weeks, then monthly once stable.
Target: Potassium 3.5-5.0 mEq/L, Magnesium 1.5-2.5 mg/dL.
Action Threshold: Hyperkalemia or hypomagnesemia; intervene with diet, supplements, or medication adjustment.
Complete Blood Count (CBC) with differential
Frequency: Monthly or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant cytopenias; investigate and manage.
Lipid profile
Frequency: Every 3-6 months.
Target: Within target for cardiovascular risk.
Action Threshold: Dyslipidemia; initiate or adjust lipid-lowering therapy.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, unusual fatigue)
- Signs of kidney problems (decreased urination, swelling in feet/ankles, unusual tiredness)
- Signs of liver problems (yellowing of skin/eyes, dark urine, persistent nausea/vomiting, abdominal pain)
- Signs of neurotoxicity (headache, tremor, seizures, confusion, visual disturbances)
- Signs of high blood pressure (headache, dizziness, blurred vision)
- Signs of gum overgrowth or hirsutism
- Signs of gastrointestinal upset (nausea, vomiting, diarrhea)
- Muscle pain or weakness
Special Patient Groups
Pregnancy
Cyclosporine crosses the placenta. While it is associated with some risks (e.g., prematurity, low birth weight, hypertension, renal dysfunction in the neonate), it is often continued during pregnancy in transplant recipients due to the high risk of organ rejection if discontinued. The benefits of preventing rejection often outweigh the potential risks to the fetus. Close monitoring of both mother and fetus is essential.
Trimester-Specific Risks:
First Trimester:
Potential for congenital anomalies, though data are conflicting and overall risk appears low compared to general population.
Second Trimester:
Risk of prematurity, low birth weight, and potential for neonatal renal dysfunction or hypertension.
Third Trimester:
Continued risk of prematurity, low birth weight, and potential for neonatal renal dysfunction or hypertension. Neonatal immunosuppression is generally not observed.
Lactation
Cyclosporine is excreted into breast milk. Due to the potential for serious adverse reactions in the breastfed infant (e.g., immunosuppression, nephrotoxicity, increased risk of malignancy), breastfeeding is generally not recommended while taking cyclosporine. The decision to breastfeed should consider the importance of the drug to the mother and the potential risks to the infant.
Infant Risk:
L3 (Moderate risk - evidence of adverse effects in breastfed infants, but risk is not severe; or no controlled studies in breastfeeding women, but the risk of adverse effects is possible).
Pediatric Use
Children generally require higher doses on a mg/kg basis compared to adults due to faster drug clearance. Close monitoring of cyclosporine trough levels, renal function, and blood pressure is crucial. Long-term effects on growth and development should be monitored.
Geriatric Use
Elderly patients may be more susceptible to the adverse effects of cyclosporine, particularly nephrotoxicity, hypertension, and neurotoxicity. Dose selection should be cautious, generally starting at the lower end of the dosing range, and closely monitoring renal function, blood pressure, and cyclosporine levels. Age-related decline in renal function should be considered.
Clinical Information
Clinical Pearls
- Neoral (cyclosporine modified) has improved and more consistent bioavailability compared to the original Sandimmune formulation. Do NOT interchange them on a mg-for-mg basis.
- Always measure cyclosporine whole blood trough levels (C0) to guide dosing, as absorption and metabolism are highly variable among individuals.
- Grapefruit and grapefruit juice are absolute contraindications due to significant CYP3A4 inhibition, leading to dangerously high cyclosporine levels.
- Nephrotoxicity is a major dose-limiting side effect; monitor renal function closely and differentiate between acute reversible nephrotoxicity (due to vasoconstriction) and chronic irreversible nephrotoxicity (due to structural damage).
- Hypertension is common; monitor blood pressure regularly and manage aggressively.
- Increased risk of infections (especially opportunistic infections) and malignancies (e.g., skin cancer, post-transplant lymphoproliferative disorder - PTLD) due to immunosuppression.
- Oral solution should be mixed with orange or apple juice (not grapefruit), or water. Do not mix with milk. Use a glass container and drink immediately. Rinse the glass with more diluent and drink to ensure full dose.
- The oral solution should not be refrigerated, as it may gel. Store at room temperature.
Alternative Therapies
- Mycophenolate mofetil (CellCept, Myfortic)
- Azathioprine (Imuran)
- Sirolimus (Rapamune)
- Everolimus (Zortress, Afinitor)
- Belatacept (Nulojix)
- Corticosteroids (e.g., prednisone)
- Biologic agents (for autoimmune diseases, e.g., TNF inhibitors, IL-17 inhibitors)
Cost & Coverage
Average Cost:
Varies widely, typically $300-$1000+ per 50ml bottle (100mg/ml)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or 4 (Specialty Drug)
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. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.