Cyclosporine 50mg/ml Inj, 5ml
WARNING: You may have more of a chance of getting an infection. Some infections have been severe or deadly. Wash hands often. Stay away from people with infections, colds, or flu.Lymphoma and other cancers have happened in people who take this drug or drugs like it. This has been deadly in some cases. Talk with the doctor.If this drug is given with other drugs that work on the immune system, it can add to the chance of getting an infection or lymphoma or other cancers. Call your doctor right away if you have a change in color or size of a mole; a lump in the armpit, groin, or neck; or any new or changing skin lump or growth. Talk with the doctor.Call your doctor right away if you have any signs of infection like fever, chills, flu-like signs, very bad sore throat, ear or sinus pain, cough, more sputum or change in color of sputum, pain with passing urine, mouth sores, or a wound that will not heal.This drug may cause kidney problems in some patients. Talk with the doctor. High blood pressure has happened with this drug. Have your blood pressure checked as you have been told by your doctor.Have your blood work and other lab tests checked as you have been told by your doctor.There are different brands and forms of this drug. Do not switch between different brands or forms of this drug without calling the doctor who ordered it.This drug may be given with steroid drugs like hydrocortisone. Do not use with other drugs that weaken the immune system. Talk with the doctor. @ COMMON USES: It is used to keep the body from harming the organ after an organ transplant.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Immunosuppressant
Pharmacologic Class
Calcineurin Inhibitor
Pregnancy Category
Not available
FDA Approved
Nov 1983
DEA Schedule
Not Controlled
Overview
What is this medicine?
Cyclosporine is a powerful medicine used to prevent your body from rejecting a transplanted organ (like a kidney, liver, or heart) or to treat severe autoimmune diseases like rheumatoid arthritis or psoriasis. It works by weakening your immune system so it doesn't attack your own body or the new organ. 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
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and be sure to follow all instructions provided. This medication is administered as an intravenous infusion, which means it is given slowly into a vein over a period of time.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
If you miss a dose, contact your doctor immediately to receive guidance on what to do next.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
If you miss a dose, contact your doctor immediately to receive guidance on what to do next.
Lifestyle & Tips
- Take cyclosporine exactly as prescribed, at the same time(s) each day. Do not miss doses.
- Do not change brands or formulations of cyclosporine without consulting your doctor, 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 exposure to sunlight and UV light (tanning beds) and use protective clothing and high SPF sunscreen, as cyclosporine increases the risk of skin cancer.
- Avoid live vaccines while on cyclosporine. Discuss all vaccinations with your doctor.
- Practice good hygiene to reduce the risk of infection (e.g., frequent hand washing).
- Report any signs of infection (fever, chills, sore throat) immediately.
- Monitor blood pressure regularly at home if advised by your doctor.
- Maintain a healthy diet and exercise routine as advised by your doctor to manage potential side effects like high blood pressure, high cholesterol, and weight gain.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly individualized based on indication, patient response, and therapeutic drug monitoring (TDM). IV dose is typically 1/3 of the oral dose.
Condition-Specific Dosing:
Organ Transplant (Prophylaxis of Rejection):
Initial: 2-6 mg/kg/day IV infused over 2-6 hours, given 4-12 hours prior to transplant. Maintenance: Gradually reduce dose based on TDM and clinical response. Often converted to oral therapy as soon as possible.
Rheumatoid Arthritis (Severe, Active):
Not typically used IV for RA. Oral dosing is 2.5 mg/kg/day in 2 divided doses, increasing to max 4 mg/kg/day.
Psoriasis (Severe):
Not typically used IV for Psoriasis. Oral dosing is 2.5 mg/kg/day in 2 divided doses, increasing to max 5 mg/kg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Dosing is highly individualized based on indication, weight, and TDM. Similar principles to adult dosing, often requiring higher mg/kg doses than adults due to faster clearance.
Child:
Dosing is highly individualized based on indication, weight, and TDM. Similar principles to adult dosing, often requiring higher mg/kg doses than adults due to faster clearance.
Adolescent:
Dosing is highly individualized based on indication, weight, and TDM. Similar principles to adult dosing, often requiring higher mg/kg doses than adults due to faster clearance.
Dose Adjustments
Renal Impairment:
Mild:
Monitor renal function closely. Dose adjustment may not be immediately necessary but monitor cyclosporine levels and renal function.
Moderate:
Monitor renal function closely. Dose reduction may be necessary if renal impairment worsens or cyclosporine levels are elevated. Consider reducing dose by 25-50%.
Severe:
Use with extreme caution. Significant dose reduction (e.g., 50% or more) is typically required. Monitor cyclosporine levels and renal function very closely. May be contraindicated in severe uncontrolled renal impairment.
Dialysis:
Cyclosporine is not significantly removed by hemodialysis or peritoneal dialysis. Dose adjustments are based on residual renal function and TDM, not dialysis schedule.
Hepatic Impairment:
Mild:
Monitor cyclosporine levels and liver function tests. Dose adjustment may not be immediately necessary.
Moderate:
Significant dose reduction (e.g., 25-50%) is often required due to reduced metabolism and clearance. Monitor cyclosporine levels and liver function tests closely.
Severe:
Use with extreme caution. Substantial dose reduction (e.g., 50-75% or more) is typically required. Monitor cyclosporine levels and liver function tests very closely. May be contraindicated in severe uncontrolled hepatic impairment.
Pharmacology
Mechanism of Action
Cyclosporine is a calcineurin inhibitor. It forms a complex with cyclophilin (an intracellular immunophilin). This complex then inhibits the calcium-dependent phosphatase calcineurin. Inhibition of calcineurin prevents the dephosphorylation of the nuclear factor of activated T-cells (NF-AT), which is required for its translocation into the nucleus. This, in turn, inhibits the transcription of various cytokine genes, including interleukin-2 (IL-2), a key cytokine for T-lymphocyte proliferation and activation. The net effect is a potent, selective inhibition of T-lymphocyte activation and proliferation, leading to immunosuppression.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable, especially with oral formulations (e.g., 20-50% for original formulation, higher for microemulsion). IV formulation is 100%.
Tmax:
IV: Immediate (upon completion of infusion). Oral: 1.5-6 hours (variable).
FoodEffect:
Not applicable for IV. For oral, food can affect absorption, especially high-fat meals.
Distribution:
Vd:
3.5-5 L/kg (adults), higher in children.
ProteinBinding:
90-98% (primarily to lipoproteins and albumin).
CnssPenetration:
Limited
Elimination:
HalfLife:
8-24 hours (highly variable, depends on age, liver function, and concomitant medications).
Clearance:
0.4-0.7 L/hr/kg (adults), higher in children.
ExcretionRoute:
Primarily biliary excretion (feces), with a small amount (<6%) excreted renally.
Unchanged:
<1% (renal)
Pharmacodynamics
OnsetOfAction:
Immunosuppressive effects begin shortly after administration, but full therapeutic effect may take days to weeks, guided by TDM.
PeakEffect:
Achieved when steady-state trough concentrations are within the therapeutic range, typically after 4-7 days of consistent dosing.
DurationOfAction:
Dependent on drug concentration; immunosuppression persists as long as therapeutic levels are maintained.
Safety & Warnings
BLACK BOX WARNING
Cyclosporine should be administered by physicians experienced in immunosuppressive therapy. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information for the patient's management. Increased risk of serious infections and malignancies (especially lymphomas and skin cancer). Increased risk of nephrotoxicity and hepatotoxicity. Hypertension and hirsutism are common side effects. Cyclosporine Injection is not bioequivalent to oral cyclosporine formulations and cannot be used interchangeably without physician supervision and monitoring of cyclosporine blood concentrations.
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 medical attention immediately:
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 significant weight gain
Signs of electrolyte problems: mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance changes, 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 or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Brain Problems
Two rare but serious brain problems have been associated with this medication:
Progressive Multifocal Leukoencephalopathy (PML): a severe brain condition that can cause disability or be fatal. Seek medical help right away if you experience:
+ Confusion
+ Memory problems
+ Depression
+ Changes in behavior
+ Weakness on one side of the body
+ Speech or thinking difficulties
+ Balance changes
+ Vision changes
Posterior Reversible Encephalopathy Syndrome (PRES): a rare brain condition that can cause serious symptoms. Contact your doctor immediately if you experience:
+ Confusion
+ Decreased alertness
+ Vision changes
+ Loss of vision
+ Seizures
+ Severe headache
Other Side Effects
Most people do not experience significant 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
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 medical attention immediately:
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 significant weight gain
Signs of electrolyte problems: mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance changes, 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 or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Brain Problems
Two rare but serious brain problems have been associated with this medication:
Progressive Multifocal Leukoencephalopathy (PML): a severe brain condition that can cause disability or be fatal. Seek medical help right away if you experience:
+ Confusion
+ Memory problems
+ Depression
+ Changes in behavior
+ Weakness on one side of the body
+ Speech or thinking difficulties
+ Balance changes
+ Vision changes
Posterior Reversible Encephalopathy Syndrome (PRES): a rare brain condition that can cause serious symptoms. Contact your doctor immediately if you experience:
+ Confusion
+ Decreased alertness
+ Vision changes
+ Loss of vision
+ Seizures
+ Severe headache
Other Side Effects
Most people do not experience significant 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
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
- Persistent nausea, vomiting, or severe stomach pain
- Swelling in hands, ankles, or feet; decreased urination (kidney problems)
- Severe headache, confusion, seizures, tremors (neurotoxicity)
- Unusual lumps or growths on your skin or anywhere on your body
- New or changing skin lesions/moles
- Significant increase in blood pressure
- Severe muscle pain 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. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
If you are currently taking any of the following medications:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
Please note that this is not an exhaustive list of all potential interactions. This medication can interact with numerous other drugs, which may increase the risk of severe, life-threatening, or fatal side effects.
To ensure your safety, it is crucial to inform your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your overall health status
Before starting, stopping, or modifying the dose of any medication, including this one, consult with your doctor to confirm that it is safe to do so, given your unique health profile and medication regimen.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Cancer
+ Kidney problems
+ High blood pressure
If you are currently taking any of the following medications:
+ Aliskiren
+ Amiloride
+ Bosentan
+ Dabigatran
+ Orlistat
+ Spironolactone
+ Triamterene
Please note that this is not an exhaustive list of all potential interactions. This medication can interact with numerous other drugs, which may increase the risk of severe, life-threatening, or fatal side effects.
To ensure your safety, it is crucial to inform your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your overall health status
Before starting, stopping, or modifying the dose of any medication, including this one, consult with your doctor to confirm that it is safe to do so, given your unique health profile and medication regimen.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Until you know how this drug affects you, avoid driving and other activities that require you to be alert.
If you have diabetes (high blood sugar), you will need 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.
This medication contains alcohol, so 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.
Some individuals treated with this medication have experienced severe kidney problems due to a viral infection (BK virus). In patients who have undergone a kidney transplant, BK virus 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 certain vaccines may not be effective or may increase the risk of infection when used with this medication.
Maintain good oral hygiene and schedule regular dental check-ups.
Avoid consuming grapefruit and grapefruit juice.
Be aware of the potential for gout attacks.
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 are planning to become pregnant while taking this medication, notify your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Until you know how this drug affects you, avoid driving and other activities that require you to be alert.
If you have diabetes (high blood sugar), you will need 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.
This medication contains alcohol, so 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.
Some individuals treated with this medication have experienced severe kidney problems due to a viral infection (BK virus). In patients who have undergone a kidney transplant, BK virus 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 certain vaccines may not be effective or may increase the risk of infection when used with this medication.
Maintain good oral hygiene and schedule regular dental check-ups.
Avoid consuming grapefruit and grapefruit juice.
Be aware of the potential for gout attacks.
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 are planning to become pregnant while taking this medication, 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 problems (e.g., acute renal failure)
- Severe liver problems
- Severe hypertension
- Neurological symptoms (e.g., tremors, seizures, confusion, 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 primarily supportive; there is no specific antidote. Hemodialysis is not effective in removing cyclosporine.
Drug Interactions
Contraindicated Interactions
- Live attenuated vaccines (during immunosuppression)
- Bosentan (concomitant use with cyclosporine is contraindicated due to increased bosentan levels)
- Dabigatran (concomitant use with cyclosporine is contraindicated due to increased dabigatran levels)
- Aliskiren (concomitant use with cyclosporine is contraindicated due to increased aliskiren levels)
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, diltiazem, verapamil, grapefruit juice) - significantly increase cyclosporine levels, leading to toxicity.
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, St. John's Wort) - significantly decrease cyclosporine levels, leading to rejection.
- Nephrotoxic agents (e.g., aminoglycosides, amphotericin B, NSAIDs, tacrolimus, sirolimus, ACE inhibitors, ARBs) - increased risk of nephrotoxicity.
- Potassium-sparing diuretics, ACE inhibitors, ARBs, potassium supplements - increased risk of hyperkalemia.
- Statins (e.g., simvastatin, lovastatin) - increased risk of myopathy/rhabdomyolysis due to increased statin levels.
- Colchicine - increased risk of colchicine toxicity.
- Digoxin - increased digoxin levels.
- Immunosuppressants (e.g., tacrolimus, sirolimus, everolimus) - increased risk of profound immunosuppression and toxicity.
- Vaccines (inactivated) - reduced immune response to vaccines.
Moderate Interactions
- Oral contraceptives - may increase cyclosporine levels.
- Metformin - may increase metformin levels.
- Repaglinide - increased repaglinide levels.
- Sulfonylureas - increased risk of hypoglycemia.
- Calcium channel blockers (non-dihydropyridine) - may increase cyclosporine levels.
- Corticosteroids - may affect cyclosporine levels (variable).
Minor Interactions
- Magnesium-containing antacids - may decrease cyclosporine absorption (oral formulations).
Monitoring
Baseline Monitoring
Complete Blood Count (CBC)
Rationale: To establish baseline hematologic parameters and monitor for potential bone marrow suppression.
Timing: Prior to initiation
Renal Function (Serum Creatinine, BUN, eGFR)
Rationale: Cyclosporine is nephrotoxic; establish baseline and monitor for impairment.
Timing: Prior to initiation
Liver Function Tests (ALT, AST, ALP, Bilirubin)
Rationale: Cyclosporine is hepatotoxic; establish baseline and monitor for impairment.
Timing: Prior to initiation
Blood Pressure
Rationale: Cyclosporine can cause hypertension.
Timing: Prior to initiation
Serum Electrolytes (Potassium, Magnesium)
Rationale: Cyclosporine can cause hyperkalemia and hypomagnesemia.
Timing: Prior to initiation
Lipid Profile (Total Cholesterol, LDL, HDL, Triglycerides)
Rationale: Cyclosporine can cause hyperlipidemia.
Timing: Prior to initiation
Uric Acid
Rationale: Cyclosporine can cause 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, or as clinically indicated.
Target: Highly variable based on indication, time post-transplant, and assay method (e.g., whole blood C0 100-400 ng/mL for transplant, lower for autoimmune).
Action Threshold: Levels outside target range; adjust dose to maintain therapeutic levels and minimize toxicity.
Renal Function (Serum Creatinine, BUN, eGFR)
Frequency: At least twice weekly initially, then weekly, then every 2-4 weeks, or as clinically indicated.
Target: Maintain within 30% of baseline or within normal limits.
Action Threshold: Significant increase in creatinine (>30% above baseline or rising trend); consider dose reduction or alternative.
Liver Function Tests (ALT, AST, ALP, Bilirubin)
Frequency: Weekly initially, then every 2-4 weeks, or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant elevation (e.g., >2x ULN); consider dose reduction or alternative.
Blood Pressure
Frequency: Daily initially, then weekly, then every 2-4 weeks.
Target: <130/80 mmHg (or target for patient).
Action Threshold: Sustained hypertension; initiate or adjust antihypertensive therapy.
Serum Electrolytes (Potassium, Magnesium)
Frequency: Weekly initially, then every 2-4 weeks, or as clinically indicated.
Target: Potassium: 3.5-5.0 mEq/L; Magnesium: 1.5-2.5 mg/dL.
Action Threshold: Hyperkalemia or hypomagnesemia; intervene with diet, supplements, or medications.
CBC with differential
Frequency: Weekly initially, then every 2-4 weeks, or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant leukopenia, thrombocytopenia, or anemia; investigate and manage.
Lipid Profile
Frequency: Every 3-6 months.
Target: Within target for patient.
Action Threshold: Hyperlipidemia; initiate or adjust lipid-lowering therapy.
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)
- Hypertension (headache, dizziness)
- Muscle pain or weakness
- Nausea, vomiting, diarrhea
- Skin changes (new moles, lesions, or changes in existing ones)
Special Patient Groups
Pregnancy
Cyclosporine crosses the placenta. While data from human pregnancies suggest no increased risk of major birth defects, there is an increased risk of prematurity and low birth weight. Use during pregnancy should only be considered if the potential benefit justifies the potential risk to the fetus, especially in transplant recipients where continued immunosuppression is critical.
Trimester-Specific Risks:
First Trimester:
Limited data, but no clear pattern of major malformations observed. Risk of prematurity and low birth weight may be present.
Second Trimester:
Risk of prematurity and low birth weight continues. Close monitoring of fetal growth is recommended.
Third Trimester:
Risk of prematurity and low birth weight continues. Neonates exposed in utero should be monitored for signs of immunosuppression, hyperkalemia, and renal dysfunction.
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:
L3 (Moderate risk - potential for adverse effects on the infant; weigh benefits of breastfeeding against risks of drug to infant).
Pediatric Use
Children generally require higher mg/kg doses than adults due to faster drug clearance. Dosing must be individualized based on weight, age, indication, and therapeutic drug monitoring. Close monitoring for adverse effects, especially nephrotoxicity, hypertension, and infections, is crucial.
Geriatric Use
Elderly patients may be more susceptible to the adverse effects of cyclosporine, particularly nephrotoxicity, hypertension, and neurotoxicity. Initiate dosing at the lower end of the therapeutic range and monitor closely for adverse effects and drug levels. Renal function often declines with age, necessitating careful dose adjustment.
Clinical Information
Clinical Pearls
- Cyclosporine IV is typically used when oral administration is not feasible (e.g., immediately post-transplant, NPO status). Convert to oral as soon as possible.
- IV cyclosporine should be administered as a slow intravenous infusion over 2-6 hours to minimize the risk of anaphylactoid reactions.
- The IV dose is generally 1/3 of the oral dose due to 100% bioavailability.
- Therapeutic drug monitoring (TDM) of cyclosporine blood levels is essential for safe and effective use, as pharmacokinetics are highly variable.
- Always specify the type of cyclosporine assay (e.g., whole blood, specific vs. non-specific) when ordering and interpreting levels.
- Patients should be educated on the importance of consistent dosing, avoiding grapefruit, and reporting any signs of infection or toxicity.
- Long-term use is associated with increased risks of malignancy (especially skin cancer and post-transplant lymphoproliferative disorder) and chronic nephrotoxicity.
Alternative Therapies
- Tacrolimus (another calcineurin inhibitor, often preferred due to more predictable pharmacokinetics and potentially lower rates of hyperlipidemia and hirsutism)
- Sirolimus (mTOR inhibitor)
- Everolimus (mTOR inhibitor)
- Mycophenolate mofetil (antiproliferative agent)
- Azathioprine (antiproliferative agent)
- Belatacept (co-stimulation blocker)
- Corticosteroids (e.g., prednisone)
Cost & Coverage
Average Cost:
Not available per 50mg/ml, 5ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 3 or 4 (Specialty Drug)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or pour them down the drain. If you are unsure about the proper disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken to ensure prompt and effective treatment.