Cyclosporine 50mg (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 to calm down your body's immune system. It's mainly used to prevent your body from rejecting a transplanted organ (like a kidney or liver) or to treat severe autoimmune diseases like psoriasis or rheumatoid arthritis where your immune system is overactive. By weakening your immune system, it helps your body accept the new organ or reduces the attack on your own tissues.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, but it's essential to take it the same way each time. Choose to take it either always with food or always on an empty stomach to maintain consistency.
If you are also taking sirolimus, be sure to take it 4 hours after taking this medication. Continue taking this medication as directed by your doctor or healthcare provider, even if you start to feel well. Establish a routine by taking your medication at the same time every day.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it in its original container at room temperature. Keep it in a dry place, avoiding storage in a bathroom. It's crucial to 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 the missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, but it's essential to take it the same way each time. Choose to take it either always with food or always on an empty stomach to maintain consistency.
If you are also taking sirolimus, be sure to take it 4 hours after taking this medication. Continue taking this medication as directed by your doctor or healthcare provider, even if you start to feel well. Establish a routine by taking your medication at the same time every day.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it in its original container at room temperature. Keep it in a dry place, avoiding storage in a bathroom. It's crucial to 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 the 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 or formulations of cyclosporine without your doctor's approval, 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 decrease cyclosporine levels and lead to organ rejection or disease flare.
- Protect yourself from the sun (wear protective clothing, use sunscreen) as cyclosporine can increase your risk of skin cancer.
- Avoid live vaccines (e.g., MMR, varicella, rotavirus) while taking cyclosporine due to weakened immune system.
- Report any signs of infection (fever, chills, sore throat, unusual fatigue) immediately to your doctor.
- Maintain good oral hygiene and regular dental check-ups to manage potential gum overgrowth (gingival hyperplasia).
- Monitor your blood pressure regularly as instructed by your doctor.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly individualized based on indication and therapeutic drug monitoring (trough levels).
Dose Range:
2 - 10 mg
Condition-Specific Dosing:
organTransplantProphylaxis:
Initial: 2-4 mg/kg/day orally in 2 divided doses, adjusted to target trough levels. Maintenance: 1-3 mg/kg/day.
rheumatoidArthritis:
Initial: 2.5 mg/kg/day orally in 2 divided doses. Max: 4 mg/kg/day.
psoriasis:
Initial: 2.5 mg/kg/day orally in 2 divided doses. Max: 5 mg/kg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Dosing established, highly individualized based on weight and target trough levels.
Child:
Dosing established, highly individualized based on weight and target trough levels.
Adolescent:
Dosing established, highly individualized based on weight and target trough levels.
Dose Adjustments
Renal Impairment:
Mild:
Monitor renal function closely; dose adjustment may be necessary if renal impairment worsens.
Moderate:
Consider dose reduction (e.g., 25-50%) or discontinuation if renal impairment is significant or progressive.
Severe:
Use with caution; significant dose reduction or discontinuation may be required. Monitor trough levels and renal function frequently.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis. Dosing adjustments are based on residual renal function and trough levels.
Hepatic Impairment:
Mild:
Monitor cyclosporine trough levels and liver function; dose adjustment may be necessary.
Moderate:
Reduce initial dose by 25-50% and monitor trough levels closely.
Severe:
Reduce initial dose by 50% or more; use with extreme caution and frequent monitoring of trough levels and liver function.
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 T-lymphocytes. By inhibiting calcineurin, cyclosporine prevents the dephosphorylation and nuclear translocation of NF-AT (nuclear factor of activated T-cells), thereby blocking the transcription of various cytokine genes, including interleukin-2 (IL-2). This leads to a decrease in T-cell proliferation and activation, resulting in immunosuppression.
Pharmacokinetics
Absorption:
Bioavailability:
20-50% (modified formulation has more consistent and less variable absorption than original)
Tmax:
1.5-3 hours
FoodEffect:
Food (especially high-fat meals) can decrease AUC and Cmax, but the effect is less pronounced with the modified formulation compared to the original. 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:
Days to weeks for full immunosuppressive effect (based on T-cell suppression and clinical response)
PeakEffect:
Not directly applicable as effect is sustained with chronic dosing and monitored by trough levels.
DurationOfAction:
Dependent on continued administration and maintenance of therapeutic trough levels.
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 increased susceptibility to infection and the possible development of lymphoma and other malignancies resulting from immunosuppression are risks of cyclosporine. Cyclosporine can cause nephrotoxicity and hepatotoxicity. Renal and liver function should be monitored regularly. Blood pressure should be monitored regularly as hypertension is a common side effect.
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, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or speaking, 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 conditions have been associated with this medication:
Progressive multifocal leukoencephalopathy (PML): a severe brain problem 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 brain problem 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 mild 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, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or speaking, 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 conditions have been associated with this medication:
Progressive multifocal leukoencephalopathy (PML): a severe brain problem 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 brain problem 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 mild 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 tiredness or weakness
- Swelling in your hands, ankles, or feet (signs of kidney problems)
- Decreased urination
- Yellowing of your skin or eyes (jaundice), dark urine, persistent nausea/vomiting, severe stomach pain (signs of liver problems)
- Headache, tremor, seizures, confusion, numbness or tingling (signs of neurological problems)
- High blood pressure (severe headache, blurred vision)
- Unusual bleeding or bruising
- New lumps or growths on your skin
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 dosage of any medication without consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the symptoms you experienced with 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 dosage of any medication without consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before 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 while taking this medication.
If you are using a salt substitute containing potassium, a potassium-sparing diuretic, or any potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is important to discuss this with your doctor.
There may be an increased risk of skin cancer associated with this 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.
For pediatric patients, this medication should be used with caution, as the risk of certain side effects may be higher in children.
If you are pregnant or become pregnant while taking this medication, it is crucial to contact your doctor immediately, as this drug may harm the unborn baby.
If you are breastfeeding, inform 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 while taking this medication.
If you are using a salt substitute containing potassium, a potassium-sparing diuretic, or any potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is important to discuss this with your doctor.
There may be an increased risk of skin cancer associated with this 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.
For pediatric patients, this medication should be used with caution, as the risk of certain side effects may be higher in children.
If you are pregnant or become pregnant while taking this medication, it is crucial to contact your doctor immediately, as this drug may harm the unborn baby.
If you are breastfeeding, inform 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., tremor, seizures, confusion, coma)
- Nausea, vomiting, abdominal pain
What to Do:
There is no specific antidote for cyclosporine overdose. Treatment is supportive and symptomatic. Induce vomiting if ingestion is recent and patient is conscious. Gastric lavage may be considered. Activated charcoal may be used. Hemodialysis and hemoperfusion are not effective in removing cyclosporine. Closely monitor renal and liver function, blood pressure, and neurological status. Call 1-800-222-1222 (Poison Control Center) immediately for advice.
Drug Interactions
Contraindicated Interactions
- Bosentan (increased cyclosporine levels, hepatotoxicity)
- Aliskiren (increased aliskiren levels, nephrotoxicity)
- Dabigatran (increased dabigatran levels)
- Live attenuated vaccines (due to immunosuppression)
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, diltiazem, verapamil, grapefruit juice) - increased cyclosporine levels
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, St. John's Wort) - decreased cyclosporine levels
- Nephrotoxic agents (e.g., NSAIDs, aminoglycosides, amphotericin B, trimethoprim/sulfamethoxazole, tacrolimus) - increased risk of nephrotoxicity
- Potassium-sparing diuretics, ACE inhibitors, ARBs (increased risk of hyperkalemia)
- Statins (e.g., simvastatin, lovastatin, atorvastatin) - increased statin levels, risk of myopathy/rhabdomyolysis
- Colchicine (increased colchicine levels, toxicity)
- Digoxin (increased digoxin levels)
- Repaglinide (increased repaglinide levels, hypoglycemia)
- Everolimus, Sirolimus (increased levels of both drugs, increased risk of nephrotoxicity)
Moderate Interactions
- Oral contraceptives (may increase cyclosporine levels)
- Metoclopramide (may increase cyclosporine levels)
- Allopurinol (may increase cyclosporine levels)
- Cimetidine (may increase cyclosporine levels)
- Danazol (may increase cyclosporine levels)
- Methotrexate (increased risk of nephrotoxicity)
- Nifedipine (increased risk of gingival hyperplasia)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Renal function (serum creatinine, BUN, GFR)
Rationale: Cyclosporine is nephrotoxic; establish baseline function.
Timing: Prior to initiation
Liver function tests (ALT, AST, ALP, bilirubin)
Rationale: Cyclosporine can cause hepatotoxicity; establish baseline function.
Timing: Prior to initiation
Blood pressure
Rationale: Cyclosporine can cause hypertension.
Timing: Prior to initiation
Lipid profile (total cholesterol, LDL, HDL, triglycerides)
Rationale: Cyclosporine can cause dyslipidemia.
Timing: Prior to initiation
Serum potassium and magnesium
Rationale: Cyclosporine can cause hyperkalemia and hypomagnesemia.
Timing: Prior to initiation
Complete Blood Count (CBC)
Rationale: To assess for potential hematologic abnormalities.
Timing: Prior to initiation
Routine Monitoring
Cyclosporine whole blood trough levels (C0)
Frequency: Initially 2-3 times per week, then weekly, then every 1-2 months once stable (frequency varies by indication and clinical stability)
Target: Highly variable by indication, time post-transplant, and concomitant medications (e.g., 100-400 ng/mL for transplant, lower for autoimmune diseases)
Action Threshold: Levels outside target range require dose adjustment; levels consistently high increase toxicity risk; levels consistently low increase rejection/disease activity risk.
Renal function (serum creatinine, BUN)
Frequency: Weekly for first month, then every 2-4 weeks, then monthly once stable
Target: Stable and within acceptable limits (e.g., <30% increase from baseline)
Action Threshold: Significant or sustained increase (e.g., >30% above baseline) may indicate nephrotoxicity and require 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 may indicate hepatotoxicity and require dose adjustment.
Blood pressure
Frequency: Weekly for first month, then every 2-4 weeks, then monthly
Target: <140/90 mmHg (or target for patient)
Action Threshold: Sustained hypertension requires antihypertensive therapy or cyclosporine 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 (e.g., dietary changes, supplements, medication adjustment).
Complete Blood Count (CBC)
Frequency: Monthly or as clinically indicated
Target: Within normal limits
Action Threshold: Significant abnormalities (e.g., leukopenia, thrombocytopenia) may require investigation.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, unusual fatigue)
- Signs of kidney problems (decreased urine output, swelling in ankles/feet, unusual fatigue)
- Signs of liver problems (yellowing of skin/eyes, dark urine, persistent nausea/vomiting, abdominal pain)
- Neurological symptoms (tremor, headache, seizures, confusion, paresthesia)
- Hypertension (headache, dizziness)
- Gingival hyperplasia (gum overgrowth)
- Hirsutism (excessive hair growth)
- Gastrointestinal upset (nausea, vomiting, diarrhea)
- Muscle pain or weakness
Special Patient Groups
Pregnancy
Cyclosporine is classified as Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Data from human pregnancies suggest an increased risk of prematurity and low birth weight, but no consistent pattern of major birth defects has been established. Close monitoring of cyclosporine levels and maternal/fetal health is recommended.
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of prematurity and low birth weight, but no clear evidence of teratogenicity.
Second Trimester:
Continued risk of prematurity and low birth weight. Close monitoring of maternal cyclosporine levels and fetal growth.
Third Trimester:
Continued risk of prematurity and low birth weight. Neonatal immunosuppression is possible but rare. Monitor for signs of infection in the neonate.
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 during cyclosporine therapy.
Infant Risk:
Moderate to High (L3-L4)
Pediatric Use
Cyclosporine is used in pediatric patients for organ transplant prophylaxis and certain autoimmune conditions. Dosing is weight-based and highly individualized, requiring careful therapeutic drug monitoring. Pediatric patients may be more susceptible to certain adverse effects, such as hypertension and gingival hyperplasia.
Geriatric Use
Elderly patients may be more susceptible to the adverse effects of cyclosporine, particularly nephrotoxicity, hypertension, and neurotoxicity. Close monitoring of renal function, blood pressure, and cyclosporine trough levels is essential. Lower initial doses or slower titration may be considered.
Clinical Information
Clinical Pearls
- Cyclosporine modified (Neoral, Gengraf) is NOT bioequivalent to non-modified cyclosporine (Sandimmune) and should not be interchanged on a milligram-to-milligram basis. Switching formulations requires careful monitoring and dose adjustment.
- Therapeutic drug monitoring (trough levels) is crucial for safe and effective cyclosporine therapy due to its narrow therapeutic index and highly variable pharmacokinetics.
- Grapefruit and grapefruit juice are absolute contraindications due to significant CYP3A4 inhibition, leading to dangerously high cyclosporine levels.
- Patients on cyclosporine are at increased risk of infections (bacterial, viral, fungal, opportunistic) and malignancies (especially skin cancer and post-transplant lymphoproliferative disorder - PTLD).
- Nephrotoxicity is a major dose-limiting side effect. Differentiate between acute, reversible nephrotoxicity (often dose-dependent) and chronic, irreversible nephrotoxicity (histological changes).
- Hypertension is common and often requires antihypertensive therapy. Calcium channel blockers (e.g., amlodipine) are often preferred as they do not significantly interact with cyclosporine's metabolism (unlike diltiazem/verapamil).
- Gingival hyperplasia and hirsutism are common cosmetic side effects that can impact patient adherence. Good oral hygiene is important for gingival hyperplasia.
Alternative Therapies
- Tacrolimus (another calcineurin inhibitor)
- Sirolimus (mTOR inhibitor)
- Everolimus (mTOR inhibitor)
- Mycophenolate mofetil (antimetabolite)
- Azathioprine (antimetabolite)
- Belatacept (selective T-cell costimulation blocker)
- Corticosteroids (e.g., prednisone)
- Methotrexate (for autoimmune conditions)
- Biologic DMARDs (for autoimmune conditions)
Cost & Coverage
Average Cost:
Price varies widely by pharmacy and formulation (e.g., $100-$500+) per 30 capsules (50mg)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or Tier 4 (Specialty Drug)
General Drug Facts
If your symptoms or health condition do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure your safety and the effectiveness of your treatment, never share your medication with others or take someone else's medication. It is also important to note that some medications may have additional patient information leaflets, so be sure to consult with your pharmacist if you have any questions. If you are unsure about any aspect of your medication, including its use, potential side effects, or interactions, discuss your concerns 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 name of the medication taken, the amount, and the time it was taken, to ensure you receive appropriate and timely care.