Neoral 100mg Capsules
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
Category C
FDA Approved
Jun 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 severe autoimmune diseases like rheumatoid arthritis or psoriasis, where the immune system is overactive and attacking the body's own tissues. Because it lowers your immune system, it's very important to take it exactly as prescribed and be aware of potential side effects.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow these guidelines:
Take your medication exactly as directed by your doctor. Read all the information provided with your prescription and follow the instructions carefully.
You can take your medication with or without food, but it's essential to take it the same way each time. Choose to either always take it with food or always take it on an empty stomach.
If you are also taking sirolimus, be sure to take it 4 hours after taking this medication.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel well.
Establish a routine by taking your medication at the same time every day.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it in its original container at room temperature.
Keep it in a dry place, away from the bathroom.
Store all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, follow these steps:
Take the missed dose 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 ensure you get the most benefit from your medication, follow these guidelines:
Take your medication exactly as directed by your doctor. Read all the information provided with your prescription and follow the instructions carefully.
You can take your medication with or without food, but it's essential to take it the same way each time. Choose to either always take it with food or always take it on an empty stomach.
If you are also taking sirolimus, be sure to take it 4 hours after taking this medication.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel well.
Establish a routine by taking your medication at the same time every day.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it in its original container at room temperature.
Keep it in a dry place, away from the bathroom.
Store all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, follow these steps:
Take the missed dose 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 consistently at the same time each day, either with or without food, but always in the same manner.
- Do not switch between different brands of cyclosporine (e.g., Neoral, Gengraf, Sandimmune) without your doctor's explicit instruction, as they are not interchangeable.
- Avoid grapefruit and grapefruit juice, as they can significantly increase cyclosporine levels and lead to toxicity.
- Avoid St. John's Wort, as it can significantly decrease cyclosporine levels and lead to organ rejection.
- Limit sun exposure and use sunscreen/protective clothing due to increased risk of skin cancer.
- Avoid live vaccines while on cyclosporine.
- Maintain good hygiene to reduce infection risk.
- Monitor blood pressure regularly at home if advised by your doctor.
- Report any signs of infection, kidney problems, or other unusual symptoms immediately.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly individualized based on indication and therapeutic drug monitoring (TDM). For transplant prophylaxis, initial oral dose typically 8-10 mg/kg/day (Neoral) given in two divided doses, adjusted based on trough levels. For rheumatoid arthritis or psoriasis, initial doses are lower (e.g., 2.5 mg/kg/day in two divided doses).
Dose Range:
2.5 - 10 mg
Condition-Specific Dosing:
organTransplantProphylaxis:
Initial: 8-10 mg/kg/day orally in two divided doses, adjusted to maintain target trough levels. Maintenance: 2-6 mg/kg/day.
rheumatoidArthritis:
Initial: 2.5 mg/kg/day orally in two divided doses. May increase by 0.5 mg/kg/day every 2-4 weeks to a maximum of 4 mg/kg/day.
psoriasis:
Initial: 2.5 mg/kg/day orally in two divided doses. May increase by 0.5 mg/kg/day every 2 weeks to a maximum of 5 mg/kg/day.
Pediatric Dosing
Neonatal:
Not established for routine use; use with extreme caution and individualized dosing if necessary.
Infant:
Dosing is highly individualized and often similar to adult mg/kg dosing for transplant, but requires careful monitoring.
Child:
Dosing is highly individualized and often similar to adult mg/kg dosing for transplant, but requires careful monitoring. For transplant, initial doses may be higher (e.g., 10-14 mg/kg/day) due to faster clearance.
Adolescent:
Dosing is highly individualized and often similar to adult mg/kg dosing for transplant, but requires careful monitoring.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment, but monitor renal function closely and adjust based on cyclosporine levels and renal function changes.
Moderate:
Reduce dose by 25-50% or adjust based on cyclosporine levels and renal function changes. Avoid if possible in non-transplant indications.
Severe:
Reduce dose significantly (e.g., 50% or more) or adjust based on cyclosporine levels and renal function changes. Avoid if possible in non-transplant indications.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis or peritoneal dialysis. Dose adjustment based on cyclosporine levels and clinical response is necessary. Administer after dialysis.
Hepatic Impairment:
Mild:
Reduce initial dose by 25-50% and monitor cyclosporine levels closely.
Moderate:
Reduce initial dose by 50% or more and monitor cyclosporine levels closely. Use with extreme caution.
Severe:
Contraindicated or use with extreme caution and significant dose reduction (e.g., 75% or more) with intensive monitoring.
Pharmacology
Mechanism of Action
Cyclosporine is a calcineurin inhibitor. It forms a complex with cyclophilin (an immunophilin) inside T-lymphocytes. This complex then inhibits calcineurin, a phosphatase that is essential for the activation of nuclear factor of activated T-cells (NF-AT). By inhibiting calcineurin, cyclosporine prevents the dephosphorylation and subsequent nuclear translocation of NF-AT, thereby blocking the transcription of various cytokine genes, including interleukin-2 (IL-2). This leads to a decrease in the production of IL-2 and other cytokines, which are crucial for T-cell activation, proliferation, and differentiation, ultimately suppressing the immune response.
Pharmacokinetics
Absorption:
Bioavailability:
20-50% (Neoral, modified formulation, has more consistent and higher bioavailability than original Sandimmune)
Tmax:
1.5-2 hours
FoodEffect:
Food can delay and decrease absorption, especially high-fat meals. Administer consistently with or without food.
Distribution:
Vd:
3.5-5 L/kg
ProteinBinding:
90-98% (primarily to lipoproteins)
CnssPenetration:
Limited
Elimination:
HalfLife:
8-24 hours (highly variable, depends on age, liver function, and concomitant medications)
Clearance:
0.4-0.7 L/hr/kg
ExcretionRoute:
Primarily biliary (fecal), <6% renal
Unchanged:
<1% in urine
Pharmacodynamics
OnsetOfAction:
Immunosuppressive effects begin within hours to days, but full therapeutic effect and stable blood levels may take several days to weeks.
PeakEffect:
Correlates with peak blood concentrations (Tmax), but clinical immunosuppression is related to sustained trough levels.
DurationOfAction:
Dependent on continued dosing and maintenance of therapeutic blood levels.
Safety & Warnings
BLACK BOX WARNING
Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe cyclosporine. 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 requisite for the follow-up of the patient. Cyclosporine (MODIFIED) has increased bioavailability compared to Sandimmune (cyclosporine). Cyclosporine (MODIFIED) and Sandimmune are not bioequivalent and cannot be used interchangeably without physician supervision. For a given trough concentration, exposure to cyclosporine will be greater with cyclosporine (MODIFIED) than with Sandimmune. Therefore, conversion from Sandimmune to cyclosporine (MODIFIED) requires close monitoring of blood levels and dose adjustment to avoid toxicity. Increased risk of serious infections and development of neoplasms (lymphoma, skin cancer) due to immunosuppression. Nephrotoxicity and hepatotoxicity are major potential toxicities. Hypertension and neurotoxicity (e.g., tremor, convulsions) are also common.
Side Effects
Important Side Effects to Report to Your Doctor Immediately
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, seek medical attention right away:
Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Fainting
+ Changes in eyesight
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of electrolyte problems, including:
+ Mood changes
+ Confusion
+ Muscle pain, cramps, or spasms
+ Weakness
+ Shakiness
+ Balance problems
+ Abnormal heartbeat
+ Seizures
+ Loss of appetite
+ Severe nausea or vomiting
Unexplained bruising or bleeding
Feeling extremely tired or weak
Abnormal sensations, such as burning, numbness, or tingling
Chest pain or pressure, or a 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, seek medical attention 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 but serious brain problem called PML, which can lead to disability or death. If you experience any of the following symptoms, seek medical attention immediately:
Confusion
Memory problems
Depression
Changes in behavior
Weakness on one side of the body
Difficulty speaking or thinking
Balance problems
Changes in eyesight
Posterior Reversible Encephalopathy Syndrome (PRES)
This medication can cause a rare but serious brain problem called PRES, which can lead to disability or death. If you experience any of the following symptoms, seek medical attention immediately:
Confusion
Decreased alertness
Changes in eyesight
Loss of eyesight
Seizures
Severe headache
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to report any concerns to your doctor. If you experience any of the following side effects, seek medical attention 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 or concerns about side effects, 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, seek medical attention right away:
Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Fainting
+ Changes in eyesight
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of electrolyte problems, including:
+ Mood changes
+ Confusion
+ Muscle pain, cramps, or spasms
+ Weakness
+ Shakiness
+ Balance problems
+ Abnormal heartbeat
+ Seizures
+ Loss of appetite
+ Severe nausea or vomiting
Unexplained bruising or bleeding
Feeling extremely tired or weak
Abnormal sensations, such as burning, numbness, or tingling
Chest pain or pressure, or a 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, seek medical attention 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 but serious brain problem called PML, which can lead to disability or death. If you experience any of the following symptoms, seek medical attention immediately:
Confusion
Memory problems
Depression
Changes in behavior
Weakness on one side of the body
Difficulty speaking or thinking
Balance problems
Changes in eyesight
Posterior Reversible Encephalopathy Syndrome (PRES)
This medication can cause a rare but serious brain problem called PRES, which can lead to disability or death. If you experience any of the following symptoms, seek medical attention immediately:
Confusion
Decreased alertness
Changes in eyesight
Loss of eyesight
Seizures
Severe headache
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to report any concerns to your doctor. If you experience any of the following side effects, seek medical attention 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 or concerns about side effects, 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:
- Fever, chills, sore throat, body aches (signs of infection)
- Unusual bruising or bleeding
- Yellowing of skin or eyes (jaundice), dark urine, pale stools (liver problems)
- Swelling in ankles, feet, or hands; decreased urination (kidney problems)
- Severe headache, confusion, seizures, numbness or tingling (neurotoxicity)
- New skin lesions, moles, or changes in existing ones
- Significant increase in blood pressure
- Severe nausea, vomiting, or diarrhea
- Unusual fatigue 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:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the symptoms you experienced with the allergy.
Certain health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
Other medications you are taking, such as:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
If you have psoriasis and are undergoing other treatments, including medications or radiation.
Please note that this is not an exhaustive list of all potential interactions. This medication can interact with numerous other drugs, which may increase the risk of severe, life-threatening, or fatal side effects. Therefore, it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist to ensure safe use. 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:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the symptoms you experienced with the allergy.
Certain health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
Other medications you are taking, such as:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
If you have psoriasis and are undergoing other treatments, including medications or radiation.
Please note that this is not an exhaustive list of all potential interactions. This medication can interact with numerous other drugs, which may increase the risk of severe, life-threatening, or fatal side effects. Therefore, it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist to ensure safe use. 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 viral infection can lead to kidney loss in transplant patients. 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, as they may interact with the drug.
Be aware of the potential for gout attacks and monitor your condition accordingly.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
When administering this medication to children, exercise caution, as the risk of certain side effects may be higher in this population.
This medication may harm an unborn baby if taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this drug, 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 viral infection can lead to kidney loss in transplant patients. 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, as they may interact with the drug.
Be aware of the potential for gout attacks and monitor your condition accordingly.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
When administering this medication to children, exercise caution, as the risk of certain side effects may be higher in this population.
This medication may harm an unborn baby if taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this drug, contact your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Nephrotoxicity (acute renal failure)
- Hepatotoxicity
- Neurotoxicity (tremor, seizures, confusion)
- Hypertension
- Gastrointestinal upset
What to Do:
There is no specific antidote. Treatment is supportive and symptomatic. Cyclosporine is not dialyzable. Call 1-800-222-1222 (Poison Control) immediately or seek emergency medical attention.
Drug Interactions
Contraindicated Interactions
- Bosentan (increased cyclosporine levels, hepatotoxicity)
- Aliskiren (increased aliskiren levels, nephrotoxicity)
- Dabigatran (increased dabigatran levels)
- St. John's Wort (decreased cyclosporine levels)
- Live attenuated vaccines (risk of infection)
- Potassium-sparing diuretics (risk of hyperkalemia)
- Grapefruit/grapefruit juice (increased cyclosporine levels)
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, diltiazem, verapamil, amiodarone, ritonavir, indinavir, nelfinavir, saquinavir) - increased cyclosporine levels
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, nafcillin, octreotide) - decreased cyclosporine levels
- Nephrotoxic agents (e.g., NSAIDs, aminoglycosides, amphotericin B, tacrolimus, sirolimus, methotrexate, trimethoprim/sulfamethoxazole) - increased risk of nephrotoxicity
- Statins (e.g., atorvastatin, simvastatin) - increased statin levels, risk of myopathy/rhabdomyolysis
- Colchicine - increased colchicine levels, toxicity
- Digoxin - increased digoxin levels
- Repaglinide - increased repaglinide levels, hypoglycemia
- Immunosuppressants (e.g., azathioprine, mycophenolate mofetil) - increased risk of infection and malignancy
Moderate Interactions
- Oral contraceptives (may increase cyclosporine levels)
- Allopurinol (may increase cyclosporine levels)
- Metoclopramide (may increase cyclosporine levels)
- Cimetidine (may increase cyclosporine levels)
- Ranitidine (may increase cyclosporine levels)
- Orlistat (may decrease cyclosporine levels)
- Vaccines (reduced efficacy of vaccines)
Minor Interactions
- Not typically categorized as minor due to narrow therapeutic index and significant interaction potential.
Monitoring
Baseline Monitoring
Renal function (SCr, BUN, eGFR)
Rationale: To establish baseline and assess risk of nephrotoxicity.
Timing: Prior to initiation
Liver function tests (ALT, AST, ALP, bilirubin)
Rationale: To establish baseline and assess risk of hepatotoxicity.
Timing: Prior to initiation
Blood pressure
Rationale: To establish baseline and assess risk of hypertension.
Timing: Prior to initiation
Complete Blood Count (CBC) with differential
Rationale: To establish baseline and monitor for hematologic abnormalities.
Timing: Prior to initiation
Lipid profile
Rationale: To establish baseline and monitor for dyslipidemia.
Timing: Prior to initiation
Serum potassium and magnesium
Rationale: To establish baseline and monitor for electrolyte disturbances.
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 every 2-4 weeks once stable, or as clinically indicated.
Target: Highly variable based on indication, time post-transplant, and concomitant immunosuppression (e.g., 100-400 ng/mL for transplant, lower for autoimmune).
Action Threshold: Levels outside target range require dose adjustment and re-evaluation.
Renal function (SCr, BUN, eGFR)
Frequency: At least twice weekly for first month, then weekly for 2-3 months, then monthly or as clinically indicated.
Target: Stable baseline or within acceptable limits.
Action Threshold: Increase in SCr >30% from baseline on two consecutive measurements requires dose reduction or discontinuation.
Liver function tests (ALT, AST, ALP, bilirubin)
Frequency: Weekly for first month, then monthly or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant elevation requires dose reduction or discontinuation.
Blood pressure
Frequency: Daily initially, then weekly, then monthly.
Target: <130/80 mmHg or individualized.
Action Threshold: Sustained hypertension requires antihypertensive therapy or dose adjustment.
Complete Blood Count (CBC) with differential
Frequency: Monthly or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant cytopenias require investigation and potential dose adjustment.
Serum potassium and magnesium
Frequency: Monthly or as clinically indicated.
Target: Potassium: 3.5-5.0 mEq/L; Magnesium: 1.5-2.5 mg/dL.
Action Threshold: Hyperkalemia or hypomagnesemia requires intervention.
Lipid profile
Frequency: Every 3-6 months.
Target: Within normal limits or target for patient.
Action Threshold: Dyslipidemia requires management.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, unusual fatigue)
- Signs of kidney dysfunction (decreased urine output, swelling, fatigue)
- Signs of liver dysfunction (yellowing of skin/eyes, dark urine, abdominal pain)
- Headache, tremors, seizures, paresthesias (neurotoxicity)
- Gingival hyperplasia (gum overgrowth)
- Hirsutism (excessive hair growth)
- Gastrointestinal upset (nausea, vomiting, diarrhea)
- Muscle pain or weakness
- Skin changes (new moles, lesions, or changes in existing ones)
Special Patient Groups
Pregnancy
Category C. Cyclosporine crosses the placenta. While data suggest it does not increase the overall risk of major birth defects, there is an increased risk of prematurity and low birth weight. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
No clear evidence of increased major congenital malformations, but data are limited.
Second Trimester:
Risk of prematurity and low birth weight observed.
Third Trimester:
Risk of prematurity and low birth weight observed. Potential for neonatal complications related to immunosuppression.
Lactation
Cyclosporine is excreted into breast milk. Due to the potential for serious adverse reactions in the breastfed infant (e.g., immunosuppression, nephrotoxicity, malignancy), breastfeeding is not recommended during cyclosporine therapy.
Infant Risk:
High (L4)
Pediatric Use
Dosing is highly individualized and often requires higher mg/kg doses than adults due to faster drug clearance. Close therapeutic drug monitoring (TDM) is essential. Long-term effects on growth and development, as well as malignancy risk, need careful consideration.
Geriatric Use
No specific dose adjustments based solely on age, but older patients may have reduced renal or hepatic function, requiring dose adjustments and closer monitoring. Increased susceptibility to adverse effects (e.g., nephrotoxicity, hypertension, infections) should be considered.
Clinical Information
Clinical Pearls
- Always specify 'modified' or 'non-modified' cyclosporine when prescribing or discussing, as they are not bioequivalent.
- Therapeutic drug monitoring (TDM) of whole blood trough levels is crucial for safe and effective use.
- Consistency is key: take at the same time daily, and consistently with or without food.
- Educate patients thoroughly on drug interactions, especially grapefruit and St. John's Wort.
- Emphasize the importance of lifelong adherence in transplant patients to prevent rejection.
- Be vigilant for signs of infection, renal dysfunction, and malignancy due to immunosuppression.
- Gingival hyperplasia and hirsutism are common, dose-dependent side effects that can impact patient adherence and quality of life.
Alternative Therapies
- For transplant: Tacrolimus, Sirolimus, Everolimus, Mycophenolate mofetil, Azathioprine, Belatacept.
- For rheumatoid arthritis: Methotrexate, Biologic DMARDs (e.g., TNF inhibitors, IL-6 inhibitors), other conventional DMARDs.
- For psoriasis: Biologic agents (e.g., TNF inhibitors, IL-17 inhibitors, IL-23 inhibitors), Methotrexate, Apremilast, Phototherapy.
Cost & Coverage
Average Cost:
Varies widely, typically $100-$500+ per 30 capsules (100mg)
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 your 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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.