Cyclosporine 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.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 C
FDA Approved
Nov 1983
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, as it helps prevent their body from rejecting the new organ. It's also used for certain autoimmune diseases like severe 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 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, wait 4 hours after taking this medication before taking sirolimus.
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 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 a missed dose.
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 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, wait 4 hours after taking this medication before taking sirolimus.
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 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 a missed dose.
Lifestyle & Tips
- Take cyclosporine at the same time each day, consistently with or without food (but be consistent).
- Do not switch between different brands or formulations (e.g., Sandimmune, Neoral, Gengraf, or generics) without consulting your doctor, as they are not interchangeable and require dose adjustments and monitoring.
- Do not drink grapefruit juice or eat grapefruit while taking cyclosporine, as it can significantly increase drug levels and lead to toxicity.
- Avoid St. John's Wort, as it can significantly decrease drug levels.
- Avoid live vaccines while on cyclosporine.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Limit sun exposure and use sunscreen/protective clothing due to increased risk of skin cancer.
- Monitor blood pressure regularly at home if advised.
- Maintain good oral hygiene to help prevent gum overgrowth.
- Do not stop taking cyclosporine suddenly without consulting your doctor, as this can lead to organ rejection or disease flare-up.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly individualized based on indication and therapeutic drug monitoring (TDM). Typical initial doses for transplant prophylaxis range from 8-15 mg/kg/day orally in two divided doses, then tapered to 2-6 mg/kg/day maintenance.
Dose Range:
2 - 15 mg
Condition-Specific Dosing:
kidney_transplant_prophylaxis:
Initial: 15 mg/kg/day orally in two divided doses starting 4-12 hours pre-transplant. Maintenance: 5-10 mg/kg/day. Dose adjusted based on trough levels.
liver_transplant_prophylaxis:
Initial: 10-14 mg/kg/day orally in two divided doses starting 4-12 hours pre-transplant. Maintenance: 5-10 mg/kg/day. Dose adjusted based on trough levels.
heart_transplant_prophylaxis:
Initial: 10-15 mg/kg/day orally in two divided doses starting 4-12 hours pre-transplant. Maintenance: 2-6 mg/kg/day. Dose adjusted based on trough levels.
rheumatoid_arthritis:
Initial: 2.5 mg/kg/day orally in two divided doses. May increase by 0.5-0.75 mg/kg/day every 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, but used off-label in specific transplant cases with careful monitoring.
Infant:
Dosing similar to adults on a mg/kg basis, but often requires higher doses due to faster metabolism. Highly individualized based on TDM.
Child:
Dosing similar to adults on a mg/kg basis, but often requires higher doses due to faster metabolism. Highly individualized based on TDM.
Adolescent:
Dosing similar to adults on a mg/kg basis, but often requires higher doses due to faster metabolism. Highly individualized based on TDM.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment for mild impairment, but monitor renal function closely. Dose reduction may be needed if creatinine increases by >25% from baseline.
Moderate:
Dose reduction often required. Monitor cyclosporine trough levels and renal function closely. Consider reducing dose by 25-50% or extending dosing interval.
Severe:
Significant dose reduction required. Contraindicated in severe uncontrolled renal impairment for non-transplant indications. For transplant, dose based on TDM and clinical status. Avoid if possible.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis or peritoneal dialysis. Dose adjustment based on TDM and clinical status, not dialysis schedule.
Hepatic Impairment:
Mild:
Monitor cyclosporine trough levels closely. Dose reduction may be necessary.
Moderate:
Significant dose reduction (e.g., 25-50%) often required. Monitor cyclosporine trough levels and liver function closely.
Severe:
Significant dose reduction (e.g., 50-75%) required. Monitor cyclosporine trough 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 binds to and inhibits calcineurin, a calcium-dependent phosphatase. Inhibition of calcineurin 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), IL-3, IL-4, TNF-alpha, and GM-CSF. The net effect is the inhibition of T-lymphocyte activation and proliferation, leading to immunosuppression.
Pharmacokinetics
Absorption:
Bioavailability:
20-50% (variable, depends on formulation; Neoral/Gengraf microemulsion formulations have more consistent and higher bioavailability than Sandimmune)
Tmax:
1.5-3.5 hours (Neoral/Gengraf); 3-4 hours (Sandimmune)
FoodEffect:
Food can delay and decrease absorption, especially with the original Sandimmune formulation. Microemulsion formulations (Neoral/Gengraf) are less affected by food, but consistent administration relative to meals is recommended.
Distribution:
Vd:
3.5-5 L/kg
ProteinBinding:
90-98% (primarily to lipoproteins)
CnssPenetration:
Limited (low concentrations in CSF, but can cause neurotoxicity)
Elimination:
HalfLife:
8-24 hours (highly variable, depends on patient population and liver function)
Clearance:
0.4-0.7 L/hr/kg
ExcretionRoute:
Primarily biliary (feces); <6% excreted in urine (mostly as metabolites)
Unchanged:
<1% in urine
Pharmacodynamics
OnsetOfAction:
Immunosuppressive effects begin within hours to days, but full therapeutic effect for transplant prophylaxis is achieved with stable trough levels.
PeakEffect:
Achieved once stable therapeutic trough levels are maintained (typically after 3-7 days of consistent dosing).
DurationOfAction:
Related to drug levels; immunosuppression persists as long as therapeutic levels are maintained.
Safety & Warnings
BLACK BOX WARNING
Cyclosporine 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 risk of serious infections and malignancies (especially lymphomas and skin cancer). Increased risk of nephrotoxicity and hepatotoxicity. Hypertension is a common side effect. Monitoring of blood levels is essential for safe and effective use.
Side Effects
Urgent 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 notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
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 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 may be fatal. If you experience any of the following symptoms, contact your doctor immediately: dark urine, fatigue, decreased appetite, nausea, stomach pain, pale stools, vomiting, or yellowing of the skin or eyes.
Brain Problems
Two rare but serious brain problems have been associated with this medication:
Progressive multifocal leukoencephalopathy (PML): a condition that can cause disability or be fatal. Seek medical help right away if you experience confusion, memory problems, depression, changes in behavior, weakness on one side of the body, speech or thinking difficulties, balance problems, or vision changes.
Posterior reversible encephalopathy syndrome (PRES): a condition that can cause confusion, decreased alertness, vision changes, seizures, or severe headache. Contact your doctor immediately if you experience any of these symptoms.
Other 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 discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or persist:
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 notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
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 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 may be fatal. If you experience any of the following symptoms, contact your doctor immediately: dark urine, fatigue, decreased appetite, nausea, stomach pain, pale stools, vomiting, or yellowing of the skin or eyes.
Brain Problems
Two rare but serious brain problems have been associated with this medication:
Progressive multifocal leukoencephalopathy (PML): a condition that can cause disability or be fatal. Seek medical help right away if you experience confusion, memory problems, depression, changes in behavior, weakness on one side of the body, speech or thinking difficulties, balance problems, or vision changes.
Posterior reversible encephalopathy syndrome (PRES): a condition that can cause confusion, decreased alertness, vision changes, seizures, or severe headache. Contact your doctor immediately if you experience any of these symptoms.
Other 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 discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or persist:
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, body aches, flu-like symptoms (signs of infection)
- Unusual bleeding or bruising
- Yellowing of skin or eyes (jaundice)
- Dark urine, pale stools
- Swelling in hands, ankles, or feet
- Decreased urination
- Severe headache, confusion, seizures, tremors, numbness/tingling
- Vision changes
- Unusual fatigue or weakness
- New skin lesions or changes in existing moles
- Significant increase in blood pressure
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 allergic reaction you experienced, including any symptoms that occurred.
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 inform your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your complete medical history, including all health problems
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
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 allergic reaction you experienced, including any symptoms that occurred.
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 inform your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your complete medical history, including all health problems
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
Precautions & Cautions
Important Warnings and Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other tasks that require alertness.
Diabetes Management
If you have high blood sugar (diabetes), closely monitor your blood sugar levels while taking this medication.
Interactions with Other Medications and Products
If you are taking a salt substitute containing potassium, a potassium-sparing diuretic, or a potassium product, consult your doctor to discuss potential interactions.
Alcohol Content
This medication contains alcohol, so it is crucial to discuss this with your doctor.
Skin Cancer Risk
Prolonged use of this medication may increase the risk of skin cancer. To minimize this risk, avoid excessive sun exposure, sunlamps, and tanning beds. Use sunscreen and wear protective clothing and eyewear when outdoors. Regular skin checks are also recommended, as advised by your doctor.
Kidney Problems and BK Virus Infection
In rare cases, this medication can cause severe kidney problems due to a viral infection (BK virus). If you have had a kidney transplant, BK virus infection can lead to loss of the transplanted kidney. If you have concerns, discuss them with your doctor.
Vaccinations
Before receiving any vaccines, consult your doctor, as some vaccines may not work effectively or may increase the risk of infection when taken with this medication.
Dental Care
Maintain good oral hygiene and schedule regular dental check-ups to prevent potential dental problems.
Grapefruit and Grapefruit Juice
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Gout Attacks
Be aware of the potential for gout attacks and seek medical attention if you experience any symptoms.
Age-Related Precautions
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Similarly, if the patient is a child, use this medication with caution, as the risk of certain side effects may be higher in children.
Pregnancy and Breastfeeding
This medication may harm an unborn baby if taken during pregnancy. If you become pregnant or are planning to become pregnant, inform your doctor immediately. If you are breastfeeding, discuss the potential risks to your baby with your doctor.
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other tasks that require alertness.
Diabetes Management
If you have high blood sugar (diabetes), closely monitor your blood sugar levels while taking this medication.
Interactions with Other Medications and Products
If you are taking a salt substitute containing potassium, a potassium-sparing diuretic, or a potassium product, consult your doctor to discuss potential interactions.
Alcohol Content
This medication contains alcohol, so it is crucial to discuss this with your doctor.
Skin Cancer Risk
Prolonged use of this medication may increase the risk of skin cancer. To minimize this risk, avoid excessive sun exposure, sunlamps, and tanning beds. Use sunscreen and wear protective clothing and eyewear when outdoors. Regular skin checks are also recommended, as advised by your doctor.
Kidney Problems and BK Virus Infection
In rare cases, this medication can cause severe kidney problems due to a viral infection (BK virus). If you have had a kidney transplant, BK virus infection can lead to loss of the transplanted kidney. If you have concerns, discuss them with your doctor.
Vaccinations
Before receiving any vaccines, consult your doctor, as some vaccines may not work effectively or may increase the risk of infection when taken with this medication.
Dental Care
Maintain good oral hygiene and schedule regular dental check-ups to prevent potential dental problems.
Grapefruit and Grapefruit Juice
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Gout Attacks
Be aware of the potential for gout attacks and seek medical attention if you experience any symptoms.
Age-Related Precautions
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Similarly, if the patient is a child, use this medication with caution, as the risk of certain side effects may be higher in children.
Pregnancy and Breastfeeding
This medication may harm an unborn baby if taken during pregnancy. If you become pregnant or are planning to become pregnant, inform your doctor immediately. If you are breastfeeding, discuss the potential risks to your baby with your doctor.
Overdose Information
Overdose Symptoms:
- Severe kidney dysfunction (decreased urine output, swelling)
- Liver dysfunction (jaundice, abdominal pain)
- Severe tremors
- Seizures
- Confusion
- Hypertension
What to Do:
Seek immediate medical attention. There is no specific antidote. Treatment is supportive. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Bosentan (concurrent use increases cyclosporine levels and bosentan levels)
- Dabigatran (increased dabigatran exposure)
- Nelfinavir (significant increase in cyclosporine levels)
- Ritonavir (significant increase in cyclosporine levels)
- St. John's Wort (significant decrease in cyclosporine levels, leading to transplant rejection)
- Live vaccines (due to immunosuppression)
Major Interactions
- CYP3A4 inhibitors (e.g., azole antifungals like ketoconazole, fluconazole, voriconazole; macrolide antibiotics like erythromycin, clarithromycin; diltiazem, verapamil; grapefruit juice) - increase cyclosporine levels, increasing toxicity risk.
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, nafcillin) - decrease cyclosporine levels, increasing risk of rejection.
- Nephrotoxic agents (e.g., aminoglycosides, amphotericin B, NSAIDs, tacrolimus, sirolimus, ACE inhibitors, ARBs) - 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 risk of colchicine toxicity).
- Digoxin (increased digoxin levels).
- Everolimus, Sirolimus (increased levels of both drugs, increased risk of nephrotoxicity and other toxicities).
- Vaccines (reduced efficacy of inactivated vaccines, avoid live vaccines).
Moderate Interactions
- Oral contraceptives (may increase cyclosporine levels slightly).
- Metoclopramide (may increase cyclosporine absorption).
- Cimetidine (may increase cyclosporine levels).
- Allopurinol (may increase cyclosporine levels).
- Danazol (may increase cyclosporine levels).
- Methotrexate (increased risk of nephrotoxicity and hepatotoxicity when used together for psoriasis/RA).
Minor Interactions
- Not available (most interactions are significant due to narrow therapeutic index)
Monitoring
Baseline Monitoring
Renal function (serum creatinine, BUN, GFR)
Rationale: Cyclosporine is nephrotoxic; establish baseline before therapy.
Timing: Prior to initiation
Liver function tests (ALT, AST, ALP, bilirubin)
Rationale: Cyclosporine can cause hepatotoxicity; establish baseline.
Timing: Prior to initiation
Blood pressure
Rationale: Cyclosporine can cause hypertension.
Timing: Prior to initiation
Complete Blood Count (CBC) with differential
Rationale: To assess baseline hematologic status and monitor for myelosuppression.
Timing: Prior to initiation
Lipid profile (total cholesterol, LDL, HDL, triglycerides)
Rationale: Cyclosporine can cause dyslipidemia.
Timing: Prior to initiation
Serum potassium
Rationale: Risk of hyperkalemia.
Timing: Prior to initiation
Serum magnesium
Rationale: Risk of hypomagnesemia.
Timing: Prior to initiation
Uric acid
Rationale: Risk of 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, and concomitant immunosuppression (e.g., 100-400 ng/mL for transplant, 50-200 ng/mL for autoimmune).
Action Threshold: Levels outside target range require dose adjustment; levels consistently high increase toxicity risk; levels consistently low increase rejection risk.
Renal function (serum creatinine, BUN)
Frequency: Weekly for first month, then monthly or as clinically indicated.
Target: Maintain within acceptable limits for patient's baseline; monitor for >25% increase from baseline.
Action Threshold: Significant increase in creatinine may require 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 intervention (antihypertensives, cyclosporine dose adjustment).
Liver function tests (ALT, AST, ALP, bilirubin)
Frequency: Monthly or as clinically indicated.
Target: Within normal limits
Action Threshold: Significant elevation may require dose reduction or discontinuation.
CBC with differential
Frequency: Monthly or as clinically indicated.
Target: Within normal limits
Action Threshold: Significant cytopenias may require investigation and 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: Patient-specific targets
Action Threshold: Dyslipidemia requires management.
Glucose
Frequency: Every 3-6 months.
Target: Within normal limits
Action Threshold: Hyperglycemia requires management.
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)
- Headache, tremors, seizures, confusion, visual disturbances (neurotoxicity)
- Gingival hyperplasia (gum overgrowth)
- Hirsutism (excessive hair growth)
- Nausea, vomiting, diarrhea, abdominal discomfort
- Muscle pain or weakness
- Skin changes (new moles, skin lesions, increased sun sensitivity)
- Blood pressure changes
Special Patient Groups
Pregnancy
Cyclosporine crosses the placenta. While classified as Category C, its use in pregnant transplant recipients is often continued due to the high risk of organ rejection if discontinued. Risks include prematurity, low birth weight, and potential for renal dysfunction in the neonate. Benefits must outweigh risks.
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.
Third Trimester:
Risk of prematurity, low birth weight, and potential for transient neonatal renal dysfunction or hyperkalemia.
Lactation
Cyclosporine is excreted into breast milk. Due to the potential for serious adverse effects in the nursing infant (e.g., immunosuppression, nephrotoxicity, malignancy), breastfeeding is generally not recommended while taking cyclosporine.
Infant Risk:
High (L5 - contraindicated)
Pediatric Use
Dosing is weight-based and often requires higher mg/kg doses than adults due to faster metabolism. Close therapeutic drug monitoring (TDM) is crucial. Long-term effects on growth and development, as well as malignancy risk, need careful consideration.
Geriatric Use
No specific dose adjustments are typically required based solely on age, but older patients may have age-related decreases in renal or hepatic function, requiring dose adjustments based on individual organ function and TDM. More susceptible to adverse effects like nephrotoxicity, hypertension, and neurotoxicity.
Clinical Information
Clinical Pearls
- Cyclosporine has a narrow therapeutic index; therapeutic drug monitoring (TDM) of whole blood trough levels is essential for efficacy and safety.
- Different cyclosporine formulations (Sandimmune vs. Neoral/Gengraf) are NOT bioequivalent and cannot be interchanged without careful monitoring and dose adjustment.
- Always administer consistently with respect to meals (e.g., always with food or always without food) to minimize variability in absorption.
- Grapefruit and grapefruit juice are absolute contraindications due to significant CYP3A4 inhibition leading to increased cyclosporine levels.
- Patients are at increased risk of infections (bacterial, viral, fungal, opportunistic) and malignancies (especially skin cancer and lymphoma); educate on sun protection and symptom reporting.
- Nephrotoxicity is a dose-limiting and common side effect; monitor renal function closely and adjust dose if creatinine rises significantly.
- Hypertension and hirsutism are common side effects that can impact patient adherence.
- Gingival hyperplasia is a common side effect; emphasize good oral hygiene.
- Many drug interactions exist, especially with CYP3A4 inhibitors/inducers and nephrotoxic agents. Always review concomitant medications carefully.
Alternative Therapies
- Tacrolimus (another calcineurin inhibitor, often preferred due to lower incidence of hirsutism/gingival hyperplasia and potentially better efficacy in some settings)
- Sirolimus (mTOR inhibitor)
- Everolimus (mTOR inhibitor)
- Mycophenolate Mofetil (antiproliferative agent)
- Azathioprine (antiproliferative agent)
- Corticosteroids (e.g., Prednisone)
- Belatacept (co-stimulation blocker, for kidney transplant)
- Rituximab (CD20 inhibitor, for autoimmune diseases)
- Methotrexate (for RA, psoriasis)
- Biologic DMARDs (for RA, psoriasis, e.g., TNF inhibitors, IL-17 inhibitors)
Cost & Coverage
Average Cost:
$100 - $500+ per 30 capsules (100mg)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or Specialty Tier (for brand names); Tier 1 or 2 (for generics)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, 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. If you have any questions or concerns about this medication, don't hesitate to discuss them with 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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.