Cyclosporine 25mg 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.This drug may be given with steroid drugs like hydrocortisone. Do not use with other drugs that weaken the immune system. Talk with the doctor. @ 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.
Drug Class
Immunosuppressant
Pharmacologic Class
Calcineurin Inhibitor
Pregnancy Category
Category D
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Cyclosporine is a medicine that helps prevent your body from rejecting a transplanted organ (like a kidney, liver, or heart) by weakening your immune system. It can also be used to treat certain severe autoimmune diseases like rheumatoid arthritis or psoriasis by calming down an overactive immune system. Because it weakens 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 out of 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 be consistent in how you take it each time. Choose to either always take it with food or always take it on an empty stomach.
If you are also taking sirolimus, 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 better.
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 your medication in its original container at room temperature.
Keep the container 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 forget to take a dose:
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 a missed dose.
To ensure you get the most out of 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 be consistent in how you take it each time. Choose to either always take it with food or always take it on an empty stomach.
If you are also taking sirolimus, 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 better.
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 your medication in its original container at room temperature.
Keep the container 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 forget to take a dose:
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 a missed dose.
Lifestyle & Tips
- Take cyclosporine at the same time each day, consistently with or without food (but always the same way relative to food).
- Do not switch between different brands or formulations of cyclosporine 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, as cyclosporine can increase your risk of skin cancer.
- Practice good hygiene (frequent hand washing) and avoid sick people to reduce the risk of infection.
- Do not receive live vaccines while on cyclosporine without consulting your doctor.
- Report any new medications, supplements, or herbal products to your doctor or pharmacist, as many can interact with cyclosporine.
- Regularly monitor your blood pressure at home if advised by your doctor.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly individualized based on indication, formulation (modified vs. non-modified), and therapeutic drug monitoring (TDM). For modified cyclosporine (e.g., Neoral, Gengraf) in organ transplant: Initial doses typically 2-10 mg/kg/day orally in 2 divided doses, then tapered based on TDM and clinical response. For autoimmune conditions (e.g., rheumatoid arthritis, psoriasis): Initial doses typically 2.5 mg/kg/day orally in 2 divided doses, increasing by 0.5 mg/kg/day every 2-4 weeks to a maximum of 4 mg/kg/day.
Dose Range:
2 - 10 mg
Condition-Specific Dosing:
renal_transplant_initial:
8-10 mg/kg/day (modified) in 2 divided doses
liver_transplant_initial:
8-10 mg/kg/day (modified) in 2 divided doses
heart_transplant_initial:
10-15 mg/kg/day (modified) in 2 divided doses
rheumatoid_arthritis_initial:
2.5 mg/kg/day (modified) in 2 divided doses
psoriasis_initial:
2.5 mg/kg/day (modified) in 2 divided doses
Pediatric Dosing
Neonatal:
Not established, use with caution and close monitoring.
Infant:
Dosing is individualized and often similar to adult weight-based dosing, but requires careful monitoring of levels and renal function.
Child:
Dosing is individualized and often similar to adult weight-based dosing (e.g., 5-10 mg/kg/day for transplant), but requires careful monitoring of levels and renal function.
Adolescent:
Dosing is individualized and often similar to adult weight-based dosing, but requires careful monitoring of levels and renal function.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment, but monitor cyclosporine levels and renal function closely. Consider lower end of dosing range.
Moderate:
Reduce dose by 25-50% or extend dosing interval. Monitor cyclosporine levels and renal function closely. Avoid if possible in non-life-threatening conditions.
Severe:
Significant dose reduction (e.g., 50% or more) or extended dosing interval. Monitor cyclosporine levels and renal function closely. Avoid if possible in non-life-threatening conditions.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis or peritoneal dialysis. Dosing adjustments are based on residual renal function and cyclosporine levels.
Hepatic Impairment:
Mild:
No specific dose adjustment, but monitor cyclosporine levels and liver function closely.
Moderate:
Reduce dose by 25-50%. Monitor cyclosporine levels and liver function closely.
Severe:
Significant dose reduction (e.g., 50% or more) or extended dosing interval. Monitor cyclosporine levels and liver function closely. Use with extreme caution.
Pharmacology
Mechanism of Action
Cyclosporine is a calcineurin inhibitor. It forms a complex with cyclophilin, an intracellular immunophilin. 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 nuclear translocation of NF-AT, thereby blocking the transcription of various cytokine genes, including interleukin-2 (IL-2). This leads to a decrease in T-lymphocyte proliferation and activation, resulting in immunosuppression.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable (modified formulation: 20-50%; non-modified: 10-60%). Bioavailability of modified formulation is less dependent on bile than non-modified.
Tmax:
1.5-3.5 hours (modified formulation)
FoodEffect:
Food can delay and decrease absorption, especially high-fat meals. Consistent administration relative to meals is important.
Distribution:
Vd:
3.5-5 L/kg
ProteinBinding:
90-98% (primarily to lipoproteins)
CnssPenetration:
Limited, but can cross the blood-brain barrier to some extent, leading to neurotoxicity in some patients.
Elimination:
HalfLife:
Approximately 8.4 hours (range 5-18 hours, highly variable)
Clearance:
0.4-0.7 L/hr/kg
ExcretionRoute:
Primarily biliary/fecal (6% renal)
Unchanged:
<1% (renal)
Pharmacodynamics
OnsetOfAction:
Immunosuppressive effects typically seen within hours to days, but full therapeutic effect may take longer.
PeakEffect:
Correlates with peak blood concentrations, but the overall immunosuppressive effect is related to cumulative exposure.
DurationOfAction:
Related to drug levels; requires twice-daily dosing to maintain therapeutic immunosuppression.
Safety & Warnings
BLACK BOX WARNING
Cyclosporine (modified) should be administered under the supervision of a physician experienced in immunosuppressive therapy and management of organ transplant patients. 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 risk of developing serious infections and malignancies. Renal impairment, including structural kidney damage, is a common and serious consequence of cyclosporine therapy. Hypertension and hirsutism are also common side effects. Cyclosporine (modified) and cyclosporine (non-modified) are not bioequivalent and cannot be used interchangeably without physician supervision.
Side Effects
Urgent 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:
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
+ Passing out
+ Changes in eyesight
Signs of kidney problems, such as:
+ Inability to pass urine
+ 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 changes
+ 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, which can be life-threatening. If you experience any of the following symptoms, contact your doctor immediately:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
A rare but serious brain condition called progressive multifocal leukoencephalopathy (PML) has been associated with this medication. If you notice any of the following symptoms, contact your doctor right away:
+ Confusion
+ Memory problems
+ Depression
+ Changes in behavior
+ Weakness on one side of the body
+ Speech or thinking difficulties
+ Balance changes
+ Vision changes
Another rare but serious brain condition called posterior reversible encephalopathy syndrome (PRES) has been linked to this medication. If you experience any of the following symptoms, seek medical attention immediately:
+ Confusion
+ Decreased alertness
+ Vision changes
+ Loss of vision
+ Seizures
+ Severe headache
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you notice any of the following side effects, contact your doctor or 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
This is not an exhaustive list of possible 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 notice any of the following symptoms, contact your doctor or 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
+ Passing out
+ Changes in eyesight
Signs of kidney problems, such as:
+ Inability to pass urine
+ 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 changes
+ 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, which can be life-threatening. If you experience any of the following symptoms, contact your doctor immediately:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
A rare but serious brain condition called progressive multifocal leukoencephalopathy (PML) has been associated with this medication. If you notice any of the following symptoms, contact your doctor right away:
+ Confusion
+ Memory problems
+ Depression
+ Changes in behavior
+ Weakness on one side of the body
+ Speech or thinking difficulties
+ Balance changes
+ Vision changes
Another rare but serious brain condition called posterior reversible encephalopathy syndrome (PRES) has been linked to this medication. If you experience any of the following symptoms, seek medical attention immediately:
+ Confusion
+ Decreased alertness
+ Vision changes
+ Loss of vision
+ Seizures
+ Severe headache
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you notice any of the following side effects, contact your doctor or 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
This is not an exhaustive list of possible 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:
- Signs of infection: fever, chills, sore throat, cough, unusual fatigue, painful urination.
- Signs of kidney problems: decreased urine output, swelling in ankles/feet, unusual weight gain.
- Signs of liver problems: yellowing of skin or eyes (jaundice), dark urine, persistent nausea/vomiting, severe stomach pain.
- Neurological symptoms: severe headache, tremors, seizures, confusion, numbness or tingling, visual changes.
- Unusual bleeding or bruising.
- Severe or persistent diarrhea, nausea, or vomiting.
- Significant gum overgrowth (gingival hyperplasia).
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. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
* If you are currently taking any of the following medications:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
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.
To ensure your safety, it is crucial to discuss all of your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. Verify that it is safe to take this medication with your existing medications and health conditions before starting, stopping, or changing the dose of any drug. Always consult your doctor before making any changes to your medication regimen.
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. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
* If you are currently taking any of the following medications:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
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.
To ensure your safety, it is crucial to discuss all of your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. Verify that it is safe to take this medication with your existing medications and health conditions before starting, stopping, or changing the dose of any drug. Always consult your doctor before making any changes to your medication regimen.
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 medication affects you.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels.
If you are using a salt substitute containing potassium, a potassium-sparing diuretic, or a potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is recommended that you 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 loss of the transplanted kidney. If you have concerns, consult your doctor.
Before receiving any vaccinations, discuss the potential risks and benefits with your doctor, as some 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 potential for gout attacks and seek medical attention if you experience any symptoms.
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, use 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 medication, contact your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Before engaging in activities that require alertness, such as driving, 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.
If you are using a salt substitute containing potassium, a potassium-sparing diuretic, or a potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is recommended that you 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 loss of the transplanted kidney. If you have concerns, consult your doctor.
Before receiving any vaccinations, discuss the potential risks and benefits with your doctor, as some 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 potential for gout attacks and seek medical attention if you experience any symptoms.
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, use 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 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
- Neurological symptoms (e.g., seizures, coma)
- Nausea, vomiting, abdominal pain
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. In the US, you can also call Poison Control at 1-800-222-1222. Treatment is supportive; cyclosporine is not significantly dialyzable.
Drug Interactions
Contraindicated Interactions
- Bosentan (increased cyclosporine levels, increased bosentan hepatotoxicity)
- Aliskiren (increased aliskiren levels, increased risk of nephrotoxicity)
- Dabigatran (increased dabigatran levels)
- Grapefruit or grapefruit juice (increased cyclosporine levels)
- St. John's Wort (decreased cyclosporine levels)
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, diltiazem, verapamil, amiodarone, ritonavir, indinavir, saquinavir) - significantly increase cyclosporine levels, increasing risk of toxicity.
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, nafcillin) - significantly decrease cyclosporine levels, increasing risk of rejection.
- Nephrotoxic agents (e.g., aminoglycosides, amphotericin B, NSAIDs, trimethoprim/sulfamethoxazole, tacrolimus, sirolimus) - increased risk of nephrotoxicity.
- Potassium-sparing diuretics, ACE inhibitors, ARBs (increased risk of hyperkalemia).
- Statins (increased risk of myopathy/rhabdomyolysis due to increased statin levels).
- Colchicine (increased colchicine levels, increased risk of toxicity).
- Digoxin (increased digoxin levels).
- Everolimus/Sirolimus (increased levels of both drugs, increased risk of toxicity).
Moderate Interactions
- Oral contraceptives (may increase cyclosporine levels slightly).
- Vaccines (live attenuated vaccines should be avoided due to immunosuppression).
- Repaglinide (increased repaglinide levels, risk of hypoglycemia).
- Methotrexate (increased methotrexate levels, increased risk of toxicity).
Minor Interactions
- Not typically categorized as minor due to narrow therapeutic index and significant interaction potential.
Monitoring
Baseline Monitoring
Renal function (serum creatinine, BUN, eGFR)
Rationale: To establish baseline kidney function before initiating a nephrotoxic drug.
Timing: Prior to initiation
Liver function tests (ALT, AST, ALP, bilirubin)
Rationale: To establish baseline liver function and identify pre-existing hepatic impairment.
Timing: Prior to initiation
Blood pressure
Rationale: To establish baseline and monitor for hypertension, a common side effect.
Timing: Prior to initiation
Serum potassium
Rationale: To establish baseline and monitor for hyperkalemia.
Timing: Prior to initiation
Serum magnesium
Rationale: To establish baseline and monitor for hypomagnesemia.
Timing: Prior to initiation
Complete Blood Count (CBC)
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 until stable, then weekly for first month, then monthly or as clinically indicated.
Target: Highly variable based on indication, time post-transplant, concomitant immunosuppression, and assay method (e.g., 100-400 ng/mL for transplant, 50-200 ng/mL for autoimmune).
Action Threshold: Levels outside target range require dose adjustment and re-evaluation.
Renal function (serum creatinine, BUN, eGFR)
Frequency: Weekly for first month, then monthly or as clinically indicated.
Target: Stable or within acceptable limits for the patient.
Action Threshold: Increase in serum creatinine >25-30% from baseline or significant decline in eGFR requires dose reduction or discontinuation.
Liver function tests (ALT, AST, ALP, bilirubin)
Frequency: Monthly or as clinically indicated.
Target: Within normal limits or stable.
Action Threshold: Significant elevation requires dose reduction or discontinuation.
Blood pressure
Frequency: Weekly for first month, then monthly or as clinically indicated.
Target: <140/90 mmHg (or patient-specific target).
Action Threshold: Sustained hypertension requires antihypertensive therapy or dose adjustment.
Serum potassium
Frequency: Monthly or as clinically indicated.
Target: 3.5-5.0 mEq/L
Action Threshold: >5.5 mEq/L requires intervention.
Serum magnesium
Frequency: Monthly or as clinically indicated.
Target: 1.7-2.2 mg/dL
Action Threshold: <1.7 mg/dL requires supplementation.
Complete Blood Count (CBC)
Frequency: Monthly or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant abnormalities (e.g., leukopenia, thrombocytopenia) require investigation.
Uric acid
Frequency: Periodically or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant elevation may require allopurinol or dose adjustment.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, unusual fatigue)
- Signs of kidney problems (decreased urine output, swelling in ankles/feet, unusual weight gain)
- Signs of liver problems (yellowing of skin/eyes, dark urine, persistent nausea/vomiting, abdominal pain)
- Neurological symptoms (headache, tremor, seizures, confusion, visual disturbances)
- Gingival hyperplasia (gum overgrowth)
- Hirsutism (excessive hair growth)
- Gastrointestinal upset (nausea, vomiting, diarrhea)
- Muscle pain or weakness
- Unusual bleeding or bruising
Special Patient Groups
Pregnancy
Cyclosporine is classified as Pregnancy Category D. It crosses the placenta and has been associated with premature birth and low birth weight. However, in transplant recipients, the benefits of continuing immunosuppression to prevent organ rejection often outweigh the risks to the fetus. Close monitoring of cyclosporine levels and fetal development is essential.
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of congenital anomalies, though data are conflicting and overall risk appears low compared to other immunosuppressants.
Second Trimester:
Risk of prematurity and low birth weight. Close monitoring of maternal cyclosporine levels and fetal growth.
Third Trimester:
Risk of prematurity and low birth weight. Potential for neonatal renal dysfunction or hyperkalemia, though rare.
Lactation
Cyclosporine is excreted into breast milk. Due to the potential for serious adverse effects in the infant (e.g., immunosuppression, nephrotoxicity, increased risk of malignancy), breastfeeding is generally not recommended while taking cyclosporine. The decision should be made considering the importance of the drug to the mother and the potential risks to the infant.
Infant Risk:
L4 (Potentially hazardous)
Pediatric Use
Cyclosporine has been used in pediatric patients for organ transplantation and certain autoimmune conditions. Dosing is typically weight-based and requires careful therapeutic drug monitoring due to variable pharmacokinetics. Children may be more susceptible to certain side effects like hypertension and gingival hyperplasia. Long-term effects on growth and development should be monitored.
Geriatric Use
Elderly patients may have reduced renal function, which can affect cyclosporine clearance and increase the risk of nephrotoxicity. Dosing should be initiated at the lower end of the range and titrated carefully with close monitoring of cyclosporine levels, renal function, and blood pressure. Increased susceptibility to infections and malignancies should also be considered.
Clinical Information
Clinical Pearls
- Cyclosporine (modified) and cyclosporine (non-modified) are NOT bioequivalent. Always ensure the patient receives the correct formulation and brand, and do not interchange without physician supervision and re-titration.
- Therapeutic drug monitoring (TDM) of whole blood trough levels (C0) is crucial for safe and effective use due to high inter- and intra-patient variability in absorption and metabolism.
- Administer consistently relative to meals (e.g., always with food or always without food) to minimize variability in absorption.
- Grapefruit and St. John's Wort are absolute contraindications due to significant drug interactions.
- Nephrotoxicity is a dose-limiting and common side effect; monitor renal function closely and adjust dose as needed.
- Hypertension is common; monitor blood pressure regularly and manage aggressively.
- Increased risk of infections and malignancies (especially skin cancer and post-transplant lymphoproliferative disorder - PTLD) requires patient education on sun protection and symptom awareness.
- Gingival hyperplasia and hirsutism are common cosmetic side effects that can impact adherence.
Alternative Therapies
- Mycophenolate mofetil (CellCept, Myfortic)
- Sirolimus (Rapamune)
- Everolimus (Zortress, Afinitor)
- Azathioprine (Imuran)
- Corticosteroids (e.g., prednisone)
- Belatacept (Nulojix - for kidney transplant)
- Biologic agents (for autoimmune conditions, e.g., TNF inhibitors)
Cost & Coverage
Average Cost:
$100 - $500+ per 30 capsules (25mg)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or 4 (Specialty Drug)
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it's a good idea 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.