Cyclosporine 100mg/ml Mod Oral Soln
Overview
What is this medicine?
How to Use This Medicine
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor. Read all the information provided with your medication and follow the instructions carefully.
You can take your medication with or without food, but be consistent in how you take it each time. Always take it with food or always take it on an empty stomach.
If you are also taking sirolimus, take it 4 hours after taking this medication.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well.
Take your medication at the same time every day to establish a routine.
Measuring and Taking Liquid Doses
Measure your liquid doses carefully using the measuring device provided with your medication.
Do not rinse the syringe before or after taking your dose. If you need to wash it, make sure it is completely dry before using it again.
To take your medication, mix the solution with orange or apple juice at room temperature in a glass. Drink the mixture immediately.
Rinse the glass with more liquid and drink to ensure you get the full dose.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from refrigeration and freezing.
Keep your medication in its original container to maintain its potency.
Discard any unused portion of your medication 2 months after opening the container.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember.
If it is close to the time for your next dose, skip the missed dose and resume your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Take cyclosporine at the same time each day, consistently with or without food, to maintain stable blood levels.
- Do not switch between different 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 organ rejection.
- Limit exposure to sunlight and UV light, and use sunscreen and 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 to your doctor.
- Maintain good oral hygiene to help prevent gingival overgrowth.
- Regularly monitor blood pressure at home if advised by your doctor.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Condition-Specific Dosing:
Pediatric Dosing
Dose Adjustments
Renal Impairment:
Hepatic Impairment:
Pharmacology
Mechanism of Action
Pharmacokinetics
Absorption:
Distribution:
Elimination:
Pharmacodynamics
Safety & Warnings
BLACK BOX WARNING
Side Effects
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 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 burning, numbness, or tingling sensations
Chest pain or pressure, or a rapid heartbeat
Gum changes
Hearing loss
Shortness of breath
Shakiness
Swelling
Mouth irritation or mouth sores
Liver problems: dark urine, fatigue, decreased appetite, nausea, stomach pain, pale stools, vomiting, or yellowing of the skin and eyes (these can be fatal, so seek help immediately)
Progressive multifocal leukoencephalopathy (PML), a severe brain problem: confusion, memory problems, depression, changes in behavior, uneven strength, speech or thinking difficulties, balance problems, or vision changes (can cause disability or be fatal)
Posterior reversible encephalopathy syndrome (PRES), a severe brain problem: confusion, decreased alertness, vision changes, loss of vision, seizures, or severe headache (seek help immediately)
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people experience no side effects or only mild ones, others may have more bothersome symptoms. If you experience any of the following, contact your doctor or seek medical help:
Headache
Dizziness or drowsiness
Stomach pain or diarrhea
Nausea or vomiting
Gas
Hair growth
Acne
Flushing
Common cold symptoms
Joint pain
Leg cramps
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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, sore throat, body aches (signs of infection)
- Unusual tiredness or weakness
- Swelling in hands, feet, or ankles; decreased urination (signs of kidney problems)
- Yellowing of skin or eyes, dark urine, persistent nausea/vomiting, severe stomach pain (signs of liver problems)
- Headache, tremor, seizures, confusion, numbness or tingling (signs of neurotoxicity)
- Unusual bruising or bleeding
- New skin lesions or changes in existing moles
- Significant increase in blood pressure
Before Using This Medicine
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, including medications or radiation therapy.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing treatments and health status.
To ensure your safety, do not start, stop, or modify the dosage of any medication without consulting your doctor. This medication can interact with numerous other drugs, increasing the risk of severe, life-threatening, or fatal side effects. Therefore, it is vital to verify the safety of taking this medication with all your other treatments and health conditions.
Precautions & Cautions
Before operating a vehicle or engaging in activities that require alertness, ensure you understand how this medication affects you.
If you have diabetes (high blood sugar), it is crucial to monitor your blood sugar levels closely while taking this drug.
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 medication. To minimize this risk, limit your exposure to sunlight, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear. Regular skin checks, as advised by your doctor, are also necessary.
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, consult your doctor.
Before receiving any vaccinations, discuss the potential risks and benefits with your doctor, as some vaccines may not be effective or may increase the risk of infection when taken with this medication.
Maintaining good oral hygiene is important; 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.
This medication may harm an unborn baby if taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this medication, contact your doctor immediately.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Severe nephrotoxicity (acute renal failure)
- Hepatotoxicity
- Neurotoxicity (tremor, seizures, coma)
- Severe hypertension
- 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 and symptomatic. Cyclosporine is not dialyzable to a significant extent.
Drug Interactions
Contraindicated Interactions
- Bosentan (increased cyclosporine levels, increased bosentan toxicity)
- Aliskiren (increased cyclosporine levels, increased aliskiren toxicity)
- Dabigatran (increased dabigatran levels, increased bleeding risk)
- Live attenuated vaccines (due to immunosuppression)
Major Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, voriconazole, erythromycin, clarithromycin, diltiazem, verapamil, grapefruit juice) - significantly increase cyclosporine levels.
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, St. John's Wort) - significantly decrease cyclosporine levels.
- Nephrotoxic agents (e.g., NSAIDs, aminoglycosides, amphotericin B, tacrolimus, sirolimus, ACE inhibitors, ARBs) - increased risk of nephrotoxicity.
- Potassium-sparing diuretics, ACE inhibitors, ARBs (increased risk of hyperkalemia).
- Statins (e.g., atorvastatin, simvastatin) - increased risk of myopathy/rhabdomyolysis due to increased statin levels.
- Colchicine (increased colchicine toxicity).
- Digoxin (increased digoxin levels).
- Immunosuppressants (e.g., tacrolimus, sirolimus, everolimus) - increased risk of profound immunosuppression and toxicity.
- Nefazodone (increased cyclosporine levels).
Moderate Interactions
- Oral contraceptives (may increase cyclosporine levels slightly).
- Metoclopramide (may increase cyclosporine levels).
- Allopurinol (may increase cyclosporine levels).
- Cimetidine (may increase cyclosporine levels).
- Danazol (may increase cyclosporine levels).
- Methotrexate (increased risk of hepatotoxicity).
- Vaccines (reduced efficacy of vaccines).
Minor Interactions
- Magnesium-containing antacids (may decrease cyclosporine absorption if taken concurrently).
Monitoring
Baseline Monitoring
Rationale: To establish baseline and monitor for potential hematologic abnormalities (e.g., anemia, leukopenia).
Timing: Prior to initiation
Rationale: To establish baseline renal function and monitor for cyclosporine-induced nephrotoxicity.
Timing: Prior to initiation
Rationale: To establish baseline liver function and monitor for hepatotoxicity.
Timing: Prior to initiation
Rationale: To establish baseline and monitor for hypertension, a common side effect.
Timing: Prior to initiation
Rationale: To establish baseline and monitor for hyperlipidemia.
Timing: Prior to initiation
Rationale: To establish baseline and monitor for hyperkalemia and hypomagnesemia.
Timing: Prior to initiation
Rationale: To establish baseline and monitor for hyperuricemia.
Timing: Prior to initiation
Routine Monitoring
Frequency: Initially 2-3 times per week, then weekly, then every 2-4 weeks, then monthly or as clinically indicated.
Target: Highly variable based on indication, time post-transplant, and concomitant immunosuppression (e.g., 100-400 ng/mL for C0 in transplant, 50-150 ng/mL for C0 in autoimmune diseases). C2 levels may be used in some centers.
Action Threshold: Adjust dose to maintain target range; levels outside range may indicate toxicity or sub-therapeutic dosing.
Frequency: Initially 2-3 times per week, then weekly, then every 2-4 weeks, then monthly or as clinically indicated.
Target: Maintain within acceptable limits for the patient's baseline.
Action Threshold: Increase in serum creatinine >25% from baseline or significant decline in eGFR warrants dose reduction or investigation.
Frequency: Initially weekly, then every 2-4 weeks, then monthly or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant elevation warrants dose reduction or investigation.
Frequency: Daily initially, then weekly, then monthly.
Target: <130/80 mmHg (or as per clinical guidelines).
Action Threshold: Sustained hypertension requires antihypertensive therapy or cyclosporine dose adjustment.
Frequency: Initially weekly, then every 2-4 weeks, then 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., supplementation, dietary changes, medication adjustment).
Frequency: Every 3-6 months.
Target: As per cardiovascular risk guidelines.
Action Threshold: Dyslipidemia requires lifestyle modification or lipid-lowering therapy.
Symptom Monitoring
- Signs of infection (fever, chills, sore throat, unusual fatigue)
- Signs of kidney problems (decreased urine output, swelling in legs/feet, unusual weight gain)
- Signs of liver problems (yellowing of skin/eyes, dark urine, persistent nausea/vomiting, abdominal pain)
- Headache, tremor, seizures, confusion, visual disturbances (neurotoxicity)
- Gingival overgrowth, hirsutism
- Muscle pain or weakness
- Unusual bruising or bleeding
- Skin changes (new moles, lesions, or changes in existing ones)
Special Patient Groups
Pregnancy
Cyclosporine is Pregnancy Category C. It 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 only if the potential benefit justifies the potential risk to the fetus. Close monitoring of cyclosporine levels and maternal/fetal health is essential.
Trimester-Specific Risks:
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.
Pediatric Use
Dosing is weight-based and highly individualized, requiring careful therapeutic drug monitoring (TDM) due to variable pharmacokinetics. Children may require higher mg/kg doses than adults due to faster metabolism. Increased risk of lymphoproliferative disorders and other malignancies in pediatric transplant recipients.
Geriatric Use
No specific dose adjustments are typically required based solely on age, but geriatric patients may have age-related declines in renal or hepatic function, which necessitate dose adjustments and closer monitoring. They may also be more susceptible to adverse effects like hypertension and nephrotoxicity. Start at the lower end of the dosing range and titrate carefully with TDM.
Clinical Information
Clinical Pearls
- Always specify 'modified' or 'non-modified' cyclosporine as they are not bioequivalent and cannot be interchanged without dose adjustment and close monitoring.
- Therapeutic drug monitoring (TDM) of cyclosporine trough levels (C0 or C2) is crucial for safe and effective dosing.
- Grapefruit and St. John's Wort are absolute contraindications due to significant drug interactions.
- Nephrotoxicity is the most common and dose-limiting side effect; monitor renal function closely.
- Hypertension is common and often requires antihypertensive therapy.
- Increased risk of infections and malignancies (especially skin cancer and lymphoproliferative disorders) requires patient education and vigilance.
- Gingival hyperplasia and hirsutism are common cosmetic side effects that can impact adherence.
Alternative Therapies
- Tacrolimus (another calcineurin inhibitor, often preferred due to lower incidence of cosmetic side effects and potentially better efficacy in some settings)
- Sirolimus (mTOR inhibitor)
- Everolimus (mTOR inhibitor)
- Mycophenolate Mofetil (antiproliferative agent)
- Azathioprine (antiproliferative agent)
- Corticosteroids (e.g., Prednisone)
- Belatacept (selective T-cell costimulation blocker)
- Rituximab (anti-CD20 monoclonal antibody for autoimmune conditions)
- Methotrexate (for rheumatoid arthritis, psoriasis)
- Biologic DMARDs (e.g., TNF inhibitors for rheumatoid arthritis, psoriasis)