Cyclosporine 25mg (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
Jun 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) by weakening your immune system. It's also used to treat severe autoimmune diseases like rheumatoid arthritis and psoriasis by calming down an overactive immune system. Because it weakens your immune system, it's very important to take it exactly as prescribed and be aware of potential side effects.
How to Use This Medicine
Taking Your Medication Correctly
To 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, away from the 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, away from the 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 (modified vs. non-modified) without your doctor's explicit instruction, as they are not interchangeable.
- Avoid grapefruit and grapefruit juice, as they can significantly increase cyclosporine levels and lead to toxicity.
- Avoid St. John's Wort, as it can significantly decrease cyclosporine levels and lead to rejection.
- Limit sun exposure and use sunscreen/protective clothing due to increased risk of skin cancer.
- Avoid live vaccines while on cyclosporine.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Maintain good oral hygiene to help prevent gingival hyperplasia.
- Regularly monitor blood pressure at home if advised by your doctor.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly individualized based on indication and therapeutic drug monitoring (TDM).
Condition-Specific Dosing:
kidneyTransplantProphylaxis:
Initial: 7 mg/kg/day to 9 mg/kg/day orally, divided into two doses. Taper to 3 mg/kg/day to 6 mg/kg/day maintenance.
liverTransplantProphylaxis:
Initial: 8 mg/kg/day to 10 mg/kg/day orally, divided into two doses. Taper to 4 mg/kg/day to 8 mg/kg/day maintenance.
heartTransplantProphylaxis:
Initial: 10 mg/kg/day to 15 mg/kg/day orally, divided into two doses. Taper to 5 mg/kg/day to 10 mg/kg/day maintenance.
rheumatoidArthritis:
Initial: 2.5 mg/kg/day orally, divided into two doses. May increase by 0.5 mg/kg/day every 2-4 weeks to a maximum of 4 mg/kg/day.
psoriasis:
Initial: 2.5 mg/kg/day orally, divided into two doses. May increase by 0.5 mg/kg/day every 2 weeks to a maximum of 4 mg/kg/day.
Pediatric Dosing
Neonatal:
Not established, use with extreme caution and TDM.
Infant:
Dosing similar to adults on a mg/kg basis, but often requires higher doses due to faster clearance. Individualized based on TDM.
Child:
Dosing similar to adults on a mg/kg basis, but often requires higher doses due to faster clearance. Individualized based on TDM.
Adolescent:
Dosing similar to adults on a mg/kg basis, individualized based on TDM.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment, but monitor renal function closely. Consider lower end of dosing range.
Moderate:
Reduce dose by 25-50% or extend dosing interval. Monitor cyclosporine trough levels and renal function closely.
Severe:
Reduce dose by 50% or more. Monitor cyclosporine trough levels and renal function closely. Avoid if possible.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis. Administer after dialysis. Dose adjustment based on TDM and clinical response.
Hepatic Impairment:
Mild:
Consider lower initial doses and monitor cyclosporine trough levels closely.
Moderate:
Reduce dose by 25-50%. Monitor cyclosporine trough levels and liver function closely.
Severe:
Reduce dose by 50% or more. Monitor cyclosporine trough levels and liver function closely. Avoid if possible.
Pharmacology
Mechanism of Action
Cyclosporine is a calcineurin inhibitor. It forms a complex with cyclophilin, an intracellular immunophilin. This complex then inhibits calcineurin, a phosphatase that is essential for the activation of nuclear factor of activated T-cells (NF-AT). By inhibiting calcineurin, cyclosporine prevents the dephosphorylation and nuclear translocation of NF-AT, thereby blocking the transcription of various cytokine genes, including interleukin-2 (IL-2). This ultimately inhibits the activation and proliferation of T-lymphocytes, leading to immunosuppression.
Pharmacokinetics
Absorption:
Bioavailability:
20-50% (modified formulation has more consistent and higher bioavailability than non-modified)
Tmax:
1.5-2 hours
FoodEffect:
Food can decrease AUC and Cmax, especially high-fat meals. 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, depends on age, liver function, and indication)
Clearance:
0.4-0.7 L/hr/kg
ExcretionRoute:
Primarily biliary (fecal), small amount renal
Unchanged:
<6% in urine
Pharmacodynamics
OnsetOfAction:
Immunosuppressive effects begin within hours to days, but full therapeutic effect may take weeks, especially in autoimmune conditions.
PeakEffect:
Achieved once steady-state trough concentrations are reached (typically 4-7 days).
DurationOfAction:
Dependent on continued dosing and maintenance of therapeutic concentrations.
Safety & Warnings
BLACK BOX WARNING
Cyclosporine (modified) should be administered under the supervision of a physician experienced in immunosuppressive therapy and management of organ transplant patients. Increased risk of serious infections and development of malignancies (especially lymphomas and skin cancer). Increased risk of nephrotoxicity and hepatotoxicity. Hypertension is a common adverse effect. The modified formulation has increased bioavailability compared to the non-modified formulation; therefore, they are not interchangeable on a unit-for-unit basis.
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: 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 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 and 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 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 potentially life-threatening brain condition. Contact your doctor immediately if you experience confusion, decreased alertness, vision changes, loss of vision, seizures, or severe headache.
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 or seek immediate 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 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 and 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 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 potentially life-threatening brain condition. Contact your doctor immediately if you experience confusion, decreased alertness, vision changes, loss of vision, seizures, or severe headache.
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
- Severe nausea, vomiting, or abdominal pain
- Swelling in hands, ankles, or feet; decreased urination (kidney problems)
- Severe headache, confusion, seizures, tremors, numbness or tingling
- New skin lesions, moles, or changes in existing ones
- Significant increase in blood pressure
- Unusual fatigue or weakness
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the symptoms you experienced during an allergic reaction.
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, such as using other 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 during an allergic reaction.
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, such as using other 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 alertness, 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. Additionally, if you are using a salt substitute containing potassium, a potassium-sparing diuretic, or a potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is recommended that you discuss this with your doctor. There is an increased risk of skin cancer associated with this drug, so it is vital to limit your exposure to sunlight, sunlamps, and tanning beds. Use protective measures such as sunscreen, clothing, and eyewear to shield yourself from the sun. Follow your doctor's instructions for regular skin checks.
Some individuals treated with this medication have experienced severe kidney problems due to a viral infection (BK virus). If you have undergone a kidney transplant, a BK virus infection can lead to kidney loss. If you have concerns, consult your doctor.
Before receiving any vaccinations, discuss the potential risks and benefits with your doctor, as certain vaccines may not be effective or may increase the risk of infection when used with this medication. Maintain good oral hygiene by visiting your dentist regularly.
Avoid consuming grapefruit and grapefruit juice, as they may interact with this medication. Be aware of the potential for gout attacks and take necessary precautions.
If you are 65 years 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.
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, consult your doctor to discuss the potential risks to your baby.
If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels. Additionally, if you are using a salt substitute containing potassium, a potassium-sparing diuretic, or a potassium product, consult your doctor to discuss potential interactions.
This medication contains alcohol, so it is recommended that you discuss this with your doctor. There is an increased risk of skin cancer associated with this drug, so it is vital to limit your exposure to sunlight, sunlamps, and tanning beds. Use protective measures such as sunscreen, clothing, and eyewear to shield yourself from the sun. Follow your doctor's instructions for regular skin checks.
Some individuals treated with this medication have experienced severe kidney problems due to a viral infection (BK virus). If you have undergone a kidney transplant, a BK virus infection can lead to kidney loss. If you have concerns, consult your doctor.
Before receiving any vaccinations, discuss the potential risks and benefits with your doctor, as certain vaccines may not be effective or may increase the risk of infection when used with this medication. Maintain good oral hygiene by visiting your dentist regularly.
Avoid consuming grapefruit and grapefruit juice, as they may interact with this medication. Be aware of the potential for gout attacks and take necessary precautions.
If you are 65 years 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.
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, consult your doctor to discuss the potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Nephrotoxicity (acute renal failure)
- Hepatotoxicity
- Neurotoxicity (tremors, seizures, confusion)
- Hypertension
- Nausea, vomiting, abdominal pain
What to Do:
There is no specific antidote. Treatment is supportive and symptomatic. Gastric lavage may be performed if ingestion is recent. Cyclosporine is not dialyzable. Call 1-800-222-1222 (Poison Control) immediately.
Drug Interactions
Contraindicated Interactions
- Bosentan (increased cyclosporine levels, hepatotoxicity)
- Aliskiren (increased aliskiren levels, nephrotoxicity)
- Live vaccines (due to immunosuppression)
- St. John's Wort (decreased cyclosporine levels)
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, diltiazem, verapamil, erythromycin, clarithromycin, grapefruit juice) - increased cyclosporine levels
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, nafcillin) - 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 (increased risk of myopathy/rhabdomyolysis)
- Digoxin (increased digoxin levels)
- Colchicine (increased colchicine levels, toxicity)
- Immunosuppressants (e.g., sirolimus, everolimus) - increased risk of immunosuppression and adverse effects
- Vaccines (reduced efficacy of inactivated vaccines, risk of infection with live vaccines)
Moderate Interactions
- Oral contraceptives (may increase cyclosporine levels)
- Metformin (may increase metformin levels)
- Allopurinol (may increase cyclosporine levels)
- Cimetidine (may increase cyclosporine levels)
- Metoclopramide (may increase cyclosporine levels)
- Orlistat (may decrease cyclosporine absorption)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Complete Blood Count (CBC)
Rationale: To establish baseline and monitor for potential hematologic abnormalities (e.g., anemia, leukopenia).
Timing: Prior to initiation
Renal Function (Serum Creatinine, BUN, eGFR)
Rationale: To establish baseline and monitor for nephrotoxicity, a common and serious adverse effect.
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, a common adverse effect.
Timing: Prior to initiation
Serum Potassium and Magnesium
Rationale: To establish baseline and monitor for electrolyte disturbances (hyperkalemia, hypomagnesemia).
Timing: Prior to initiation
Uric Acid
Rationale: To establish baseline and monitor for hyperuricemia.
Timing: Prior to initiation
Lipid Panel
Rationale: To establish baseline and monitor for dyslipidemia.
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 based on indication, time post-transplant, concomitant medications, and institutional protocol (e.g., 100-400 ng/mL for C0 in transplant, lower for autoimmune).
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 once stable.
Target: Maintain within 30% of baseline or within normal limits.
Action Threshold: Significant increase (e.g., >30% above baseline) requires dose reduction or discontinuation.
Liver Function Tests (ALT, AST, ALP, Bilirubin)
Frequency: Initially weekly, then every 2-4 weeks, then monthly once stable.
Target: Within normal limits.
Action Threshold: Significant elevation (e.g., >2-3x ULN) requires dose reduction or discontinuation.
Blood Pressure
Frequency: Daily initially, then weekly, then monthly.
Target: <140/90 mmHg (or target per guidelines).
Action Threshold: Sustained hypertension requires antihypertensive therapy or dose adjustment.
Serum Potassium and Magnesium
Frequency: Initially weekly, then every 2-4 weeks, then monthly.
Target: Potassium: 3.5-5.0 mEq/L; Magnesium: 1.7-2.2 mg/dL.
Action Threshold: Hyperkalemia or hypomagnesemia requires intervention (e.g., dietary changes, supplements, medication adjustment).
Complete Blood Count (CBC)
Frequency: Initially weekly, then every 2-4 weeks, then monthly.
Target: Within normal limits.
Action Threshold: Significant abnormalities (e.g., severe leukopenia, anemia) require investigation and potential dose adjustment.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, unusual fatigue)
- Signs of kidney problems (decreased urine output, swelling in ankles/feet, unusual weight gain)
- Signs of liver problems (yellowing of skin/eyes, dark urine, persistent nausea/vomiting, abdominal pain)
- Headache, tremors, seizures, confusion (neurotoxicity)
- Gingival hyperplasia (gum overgrowth)
- Hirsutism (excessive hair growth)
- Nausea, vomiting, diarrhea
- Muscle pain or weakness
- Skin changes (new moles, lesions, or changes in existing ones)
Special Patient Groups
Pregnancy
Category C. Cyclosporine crosses the placenta. 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.
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 and fetal health is essential.
Third Trimester:
Risk of prematurity and low birth weight. Neonatal immunosuppression is possible, though rare. Monitor neonate for signs of infection.
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 not recommended during cyclosporine therapy.
Infant Risk:
High (L5)
Pediatric Use
Dosing is typically higher on a mg/kg basis compared to adults due to faster clearance. Close therapeutic drug monitoring (TDM) is crucial. Children are at similar risks for adverse effects as adults, including nephrotoxicity, hypertension, and increased risk of infection/malignancy.
Geriatric Use
No specific dose adjustment is generally required based on age alone, but older patients may have reduced renal or hepatic function, requiring dose adjustments based on those parameters. More susceptible to adverse effects like hypertension and nephrotoxicity. Start at lower end of dosing range and titrate carefully with TDM.
Clinical Information
Clinical Pearls
- Always specify 'modified' when prescribing or discussing cyclosporine to avoid confusion with the non-modified formulation (Sandimmune), which has different bioavailability and is not interchangeable.
- Therapeutic drug monitoring (TDM) of trough levels is essential for safe and effective use, especially in transplant patients. Target ranges vary widely by indication, time post-transplant, and concomitant immunosuppression.
- Consistency is key: Take cyclosporine at the same time each day, and consistently with or without food. Do not change the timing relative to meals once established.
- Educate patients thoroughly about the importance of avoiding grapefruit/grapefruit juice and St. John's Wort due to significant drug interactions.
- Emphasize lifelong adherence in transplant patients to prevent rejection.
- Monitor for signs of infection and malignancy, and educate patients on sun protection.
- Gingival hyperplasia and hirsutism are common cosmetic side effects that can impact adherence; discuss these with patients.
Alternative Therapies
- Tacrolimus (another calcineurin inhibitor)
- Sirolimus (mTOR inhibitor)
- Everolimus (mTOR inhibitor)
- Mycophenolate mofetil (antiproliferative agent)
- Azathioprine (antiproliferative agent)
- Corticosteroids (e.g., prednisone)
- Belatacept (co-stimulation blocker)
- Rituximab (anti-CD20 monoclonal antibody for autoimmune conditions)
- Methotrexate (for rheumatoid arthritis, psoriasis)
Cost & Coverage
Average Cost:
Varies widely (e.g., $100-$500+) per 30 capsules (25mg)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or 4 (Specialty Drug)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.