Cyclosporine 100mg (mod) Caps
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
Jan 1995
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). It works by weakening your immune system so it doesn't attack the new organ. It's also used to treat severe autoimmune diseases like rheumatoid arthritis or psoriasis by calming down an overactive immune system.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to take it exactly as directed by your doctor. Carefully read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, but be consistent in how you take it each time - either always with food or always on an empty stomach.
If you're 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're feeling 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 in a dry place. Avoid storing it in a bathroom. Keep 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, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To get the most benefit from your medication, it's essential to take it exactly as directed by your doctor. Carefully read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, but be consistent in how you take it each time - either always with food or always on an empty stomach.
If you're 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're feeling 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 in a dry place. Avoid storing it in a bathroom. Keep 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, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Take cyclosporine at the same time each day, consistently with or without food (but be consistent).
- Do not switch between different brands of cyclosporine (e.g., Neoral, Gengraf, or generic modified cyclosporine) without consulting your doctor, as they are not interchangeable on a milligram-for-milligram basis.
- Do not take cyclosporine with grapefruit or grapefruit juice, as this can significantly increase drug levels and lead to serious side effects.
- Avoid St. John's Wort, as it can decrease cyclosporine levels and lead to organ rejection.
- Avoid live vaccines (e.g., MMR, varicella, rotavirus, yellow fever) while on cyclosporine due to weakened immune system.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Limit sun exposure and use sunscreen/protective clothing, as cyclosporine can increase skin cancer risk.
- Maintain good oral hygiene to help prevent gingival hyperplasia (gum overgrowth).
- Do not stop taking cyclosporine suddenly without consulting your doctor, as this can lead to organ rejection or worsening of your condition.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly individualized based on indication, patient response, and therapeutic drug monitoring (TDM).
Condition-Specific Dosing:
renalTransplant:
Initial: 8-10 mg/kg/day orally, given in two divided doses. Maintenance: 2-6 mg/kg/day.
liverTransplant:
Initial: 8-10 mg/kg/day orally, given in two divided doses. Maintenance: 2-6 mg/kg/day.
heartTransplant:
Initial: 10-15 mg/kg/day orally, given in two divided doses. Maintenance: 2-6 mg/kg/day.
rheumatoidArthritis:
Initial: 2.5 mg/kg/day orally, given in two divided doses. May increase by 0.5-0.75 mg/kg/day every 2-4 weeks to a maximum of 4 mg/kg/day.
psoriasis:
Initial: 2.5 mg/kg/day orally, given 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
Infant:
Dosing is typically weight-based and similar to adult mg/kg doses for transplant indications, but requires careful monitoring.
Child:
Dosing is typically weight-based and similar to adult mg/kg doses for transplant indications, but requires careful monitoring.
Adolescent:
Dosing is typically weight-based and similar to adult mg/kg doses for transplant indications, but requires careful monitoring.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment, but monitor cyclosporine levels and renal function closely.
Moderate:
No specific dose adjustment, but monitor cyclosporine levels and renal function closely. Dose reduction may be necessary if renal function deteriorates.
Severe:
Use with caution. Dose reduction may be necessary. Monitor cyclosporine levels and renal function closely. Cyclosporine is nephrotoxic.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis. No supplemental dose needed after dialysis. Monitor levels closely.
Hepatic Impairment:
Mild:
Use with caution. Monitor cyclosporine levels closely. Dose reduction may be necessary.
Moderate:
Use with caution. Significant dose reduction (e.g., 25-50% of usual dose) may be necessary. Monitor cyclosporine levels closely.
Severe:
Use with extreme caution. Significant dose reduction (e.g., 50-75% of usual dose) may be necessary. Monitor cyclosporine levels closely.
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 responsible for dephosphorylating the nuclear factor of activated T-cells (NF-AT). Inhibition of calcineurin prevents the translocation of NF-AT into the nucleus, thereby blocking the transcription of various cytokine genes, most notably interleukin-2 (IL-2). This leads to a decrease in T-lymphocyte activation and proliferation, resulting in immunosuppression.
Pharmacokinetics
Absorption:
Bioavailability:
20-50% (modified formulation has more consistent and higher bioavailability than original)
Tmax:
1.5-2 hours
FoodEffect:
Food can delay Tmax and decrease Cmax, but the overall AUC (extent of absorption) is generally not significantly affected by food for the modified formulation. However, consistent administration relative to meals is recommended.
Distribution:
Vd:
3.5-5 L/kg
ProteinBinding:
90-98% (primarily to lipoproteins)
CnssPenetration:
Limited
Elimination:
HalfLife:
8-24 hours (highly variable)
Clearance:
0.4-0.7 L/hr/kg
ExcretionRoute:
Primarily biliary/fecal (6% renal)
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
Immunosuppressive effects typically seen within days to weeks, depending on the indication and target levels.
PeakEffect:
Achieved once stable therapeutic trough levels are maintained.
DurationOfAction:
Dependent on continued administration and maintenance of therapeutic levels.
Safety & Warnings
BLACK BOX WARNING
Cyclosporine (modified) should be administered by physicians 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 increased susceptibility to infection and the possible development of lymphoma and other malignancies resulting from immunosuppression are risks of cyclosporine (modified). Cyclosporine (modified) can cause nephrotoxicity and hepatotoxicity. Renal and liver function should be monitored regularly. Hypertension and hirsutism are also common adverse effects.
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 or seek immediate medical attention:
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 may be fatal in some cases. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Fatigue
Decreased appetite
Nausea or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Progressive Multifocal Leukoencephalopathy (PML)
This medication can cause a rare but serious brain problem called PML, which may lead to disability or death. 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 problems
Changes in eyesight
Posterior Reversible Encephalopathy Syndrome (PRES)
This medication can also cause a rare but serious brain problem called PRES. If you experience any of the following symptoms, contact your doctor immediately:
Confusion
Decreased alertness
Changes in eyesight
Loss of eyesight
Seizures
Severe headache
Other Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms, 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 immediate medical attention:
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 may be fatal in some cases. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Fatigue
Decreased appetite
Nausea or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Progressive Multifocal Leukoencephalopathy (PML)
This medication can cause a rare but serious brain problem called PML, which may lead to disability or death. 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 problems
Changes in eyesight
Posterior Reversible Encephalopathy Syndrome (PRES)
This medication can also cause a rare but serious brain problem called PRES. If you experience any of the following symptoms, contact your doctor immediately:
Confusion
Decreased alertness
Changes in eyesight
Loss of eyesight
Seizures
Severe headache
Other Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms, 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, body aches, unusual fatigue, cough, painful urination, skin sores.
- Signs of kidney problems: decreased urine output, swelling in ankles/feet, unusual weight gain, dark urine.
- Signs of liver problems: yellowing of skin or eyes (jaundice), dark urine, persistent nausea or vomiting, severe stomach pain.
- Neurological symptoms: tremor, headache, seizures, confusion, visual disturbances, numbness or tingling.
- High blood pressure: severe headache, blurred vision.
- Gingival hyperplasia (gum overgrowth) or excessive hair growth (hirsutism).
- Unusual bleeding or bruising.
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 these allergies.
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 therapy.
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:
Inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss your health problems with your doctor.
Verify that it is safe to take this medication with your other medications and health conditions.
Do not initiate, stop, or modify the dose 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 these allergies.
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 therapy.
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:
Inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss your health problems with your doctor.
Verify that it is safe to take this medication with your other medications and health conditions.
Do not initiate, stop, or modify the dose 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 engaging in activities that require your full attention, such as driving, wait until you understand how this drug 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 important to discuss this with your doctor.
There may be an increased risk of skin cancer associated with this drug. 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, discuss them with your doctor.
Before receiving any vaccinations, consult 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 ensure the health of your teeth.
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Be aware of the potential for gout attacks and monitor your condition accordingly.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
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, notify your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Before engaging in activities that require your full attention, such as driving, wait until you understand how this drug 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 important to discuss this with your doctor.
There may be an increased risk of skin cancer associated with this drug. 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, discuss them with your doctor.
Before receiving any vaccinations, consult 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 ensure the health of your teeth.
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Be aware of the potential for gout attacks and monitor your condition accordingly.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
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, notify your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Severe kidney dysfunction (e.g., acute renal failure)
- Liver dysfunction
- 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. For poison control, call 1-800-222-1222. Treatment is supportive; cyclosporine is not dialyzable to a significant extent.
Drug Interactions
Contraindicated Interactions
- Aliskiren (increased aliskiren levels, renal toxicity)
- Bosentan (increased bosentan levels, hepatotoxicity)
- Dabigatran (increased dabigatran levels)
- Live attenuated vaccines (due to immunosuppression)
- Potassium-sparing diuretics (increased risk of hyperkalemia)
- Potassium supplements (increased risk of hyperkalemia)
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, diltiazem, verapamil, grapefruit juice) - significantly increase cyclosporine levels, increasing toxicity risk.
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, St. John's Wort) - significantly decrease cyclosporine levels, increasing risk of rejection.
- Nephrotoxic drugs (e.g., NSAIDs, aminoglycosides, amphotericin B, trimethoprim/sulfamethoxazole, tacrolimus) - increased risk of nephrotoxicity.
- Statins (e.g., atorvastatin, simvastatin) - increased risk of myopathy/rhabdomyolysis due to increased statin levels.
- Colchicine (increased colchicine levels, toxicity)
- Digoxin (increased digoxin levels, toxicity)
- Sirolimus, Everolimus (increased levels of both drugs, increased risk of nephrotoxicity)
- Immunosuppressants (additive immunosuppression, increased infection/malignancy risk)
Moderate Interactions
- Oral contraceptives (may increase cyclosporine levels)
- Metformin (may increase metformin levels)
- Repaglinide (increased repaglinide levels, hypoglycemia)
- Calcium channel blockers (some may increase cyclosporine levels)
- Diuretics (may exacerbate hyperkalemia or nephrotoxicity)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Renal function (serum creatinine, BUN, GFR)
Rationale: To establish baseline and monitor for nephrotoxicity.
Timing: Prior to initiation
Liver function tests (ALT, AST, ALP, bilirubin)
Rationale: To establish baseline and monitor for hepatotoxicity.
Timing: Prior to initiation
Blood pressure
Rationale: To establish baseline and monitor for hypertension.
Timing: Prior to initiation
Electrolytes (potassium, magnesium)
Rationale: To establish baseline and monitor for hyperkalemia, hypomagnesemia.
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 (total cholesterol, LDL, HDL, triglycerides)
Rationale: To establish baseline and monitor for dyslipidemia.
Timing: Prior to initiation
Uric acid
Rationale: To establish baseline and monitor for hyperuricemia.
Timing: Prior to initiation
Routine Monitoring
Cyclosporine trough levels (C0 or C2)
Frequency: Initially 2-3 times per week, then weekly, then every 2-4 weeks, then monthly once stable.
Target: Highly variable by indication, time post-transplant, and lab assay (e.g., 100-400 ng/mL for C0 in early transplant, lower for maintenance or non-transplant).
Action Threshold: Levels outside target range require dose adjustment and re-monitoring.
Renal function (serum creatinine, BUN)
Frequency: Initially 2-3 times per week, then weekly, then every 2-4 weeks, then monthly.
Target: Stable or within acceptable limits for patient.
Action Threshold: Increase of >25-30% from baseline or progressive increase requires investigation and potential dose reduction.
Blood pressure
Frequency: Daily initially, then weekly, then monthly.
Target: <130/80 mmHg (or as per clinical guidelines).
Action Threshold: Sustained hypertension requires antihypertensive therapy or cyclosporine dose adjustment.
Liver function tests (ALT, AST, ALP, bilirubin)
Frequency: Weekly initially, then monthly.
Target: Within normal limits.
Action Threshold: Significant elevation requires investigation and potential dose reduction.
Electrolytes (potassium, magnesium)
Frequency: Weekly initially, then monthly.
Target: Potassium: 3.5-5.0 mEq/L; Magnesium: 1.5-2.5 mg/dL.
Action Threshold: Hyperkalemia or hypomagnesemia requires intervention.
CBC with differential
Frequency: Monthly or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant abnormalities (e.g., leukopenia, thrombocytopenia) require investigation.
Lipid profile
Frequency: Every 3-6 months.
Target: As per cardiovascular risk guidelines.
Action Threshold: Dyslipidemia requires management.
Glucose
Frequency: Every 3-6 months.
Target: Fasting <100 mg/dL.
Action Threshold: Hyperglycemia requires management.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, unusual fatigue, cough, painful urination)
- 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 (tremor, headache, seizures, confusion, visual disturbances)
- Gastrointestinal symptoms (nausea, vomiting, diarrhea, abdominal discomfort)
- Cardiovascular symptoms (chest pain, shortness of breath, swelling)
- Skin changes (gingival hyperplasia, hirsutism, skin lesions, increased sun sensitivity)
- Muscle pain or weakness
Special Patient Groups
Pregnancy
Category C. Cyclosporine crosses the placenta. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Data from transplant registries suggest no increased risk of major birth defects, but there is an increased risk of prematurity and low birth weight. Close monitoring of the mother and fetus is essential.
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of prematurity and low birth weight, but no consistent pattern of major malformations.
Second Trimester:
Continued risk of prematurity and low birth weight. Close monitoring of maternal cyclosporine levels and renal function.
Third Trimester:
Continued risk of prematurity and low birth weight. Neonatal immunosuppression is possible, but generally transient.
Lactation
Cyclosporine is excreted into breast milk. Due to the potential for serious adverse reactions in the breastfed infant (e.g., immunosuppression, nephrotoxicity, increased risk of malignancy), breastfeeding is generally not recommended while taking cyclosporine.
Infant Risk:
Risk L3 (Moderately Safe) - Significant amount excreted into milk; potential for adverse effects on infant. Weigh risk vs. benefit. Consider alternative feeding.
Pediatric Use
Dosing is typically weight-based. Children may require higher mg/kg doses than adults due to faster metabolism. Close monitoring of cyclosporine levels, renal function, and blood pressure is crucial. Similar adverse effects as in adults.
Geriatric Use
Use with caution. Elderly patients may be more susceptible to adverse effects, particularly nephrotoxicity and hypertension. Start at the lower end of the dosing range and monitor renal function and cyclosporine levels closely.
Clinical Information
Clinical Pearls
- Always specify 'modified' cyclosporine (e.g., Neoral, Gengraf) when prescribing, as it is not bioequivalent to the original formulation (Sandimmune).
- Therapeutic drug monitoring (TDM) of cyclosporine trough levels (C0) or 2-hour post-dose levels (C2) is essential for safe and effective use, especially in transplant patients. Target levels vary by indication, time post-transplant, and individual patient factors.
- Educate patients thoroughly about the importance of consistent administration (same time, consistent relation to food), avoiding grapefruit products, and reporting any signs of infection or adverse effects.
- Cyclosporine is highly susceptible to drug interactions, particularly with CYP3A4 inhibitors and inducers. A thorough medication review is critical before initiation and with any new medication.
- Nephrotoxicity is a dose-limiting and common side effect. Regular monitoring of renal function is paramount. Dose adjustments may be necessary even with small increases in serum creatinine.
- Hypertension is common and often requires antihypertensive therapy. Monitor blood pressure regularly.
- Patients on cyclosporine are at increased risk for infections and malignancies (especially skin cancer and lymphoproliferative disorders). Emphasize sun protection and regular skin checks.
Alternative Therapies
- Tacrolimus (another calcineurin inhibitor, often preferred due to lower incidence of cosmetic side effects like hirsutism and gingival hyperplasia)
- Sirolimus (mTOR inhibitor)
- Everolimus (mTOR inhibitor)
- Mycophenolate Mofetil (antiproliferative agent)
- Azathioprine (antiproliferative agent)
- Corticosteroids (e.g., Prednisone)
- Belatacept (co-stimulation blocker)
- Rituximab (CD20 monoclonal antibody, for autoimmune diseases)
- Methotrexate (for rheumatoid arthritis, psoriasis)
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 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 for more information. 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 details about the overdose, including the medication taken, the amount, and the time it occurred.