Generic Name: Cyclosporine Brand Name(s): Generics only. No brands available. Avability: Rx Pregnancy Category: C

Uses

What is Cyclosporine used for?

Cyclosporine is used to prevent organ rejection in people who have received a liver, kidney, or heart transplant. It is usually taken along with other medications to allow your new organ to function normally. Cyclosporine belongs to a class of drugs known as immunosuppressants. It works by weakening the immune system to help your body accept the new organ as if it were your own.

How should I take Cyclosporine?

Take this medication by mouth as directed by your doctor, usually once daily. You may take this medication with or without food, but it is important to choose one way and take this medication the same way with every dose.

The dosage is based on your weight, medical condition, lab tests, and response to treatment.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.

How do I store Cyclosporine?

Cyclosporine is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Cyclosporine in the bathroom or the freezer. There may be different brands of Cyclosporine that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Cyclosporine down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Cyclosporine?

Take this medication by mouth as directed by your doctor, usually once daily. You may take this medication with or without food, but it is important to choose one way and take this medication the same way with every dose.

The dosage is based on your weight, medical condition, lab tests, and response to treatment.

Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Cyclosporine during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Cyclosporine. Cyclosporine is pregnancy risk category C according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Cyclosporine?

Shaking, headache, dizziness, unusual growth of body hair, nausea/vomiting, diarrhea, stomach upset, or flushing may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Unusual growth and swelling of the gums may occur. Brush your teeth and floss daily to reduce this problem. See your dentist regularly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high. Your doctor may control your blood pressure with medication.

Tell your doctor right away if you have any serious side effects, including: signs of kidney problems (such as a change in the amount of urine), signs of liver disease (such as nausea/vomiting that doesn’t stop, dark urine, yellowing eyes/skin, stomach/abdominal pain), easy bruising/bleeding, unusual tiredness, muscle weakness/spasms, slow/irregular heartbeat, numb/tingling skin, severe leg pain.

Get medical help right away if you have any very serious side effects, including: mental/mood changes (such as confusion, difficulty concentrating), vision changes, problems with speech, clumsiness, loss of coordination, weakness on one side of the body, chest pain, seizures.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Cyclosporine?

Some products that may interact with this drug include: coal tar, orlistat, other drugs that weaken the immune system/increase the risk of infection (such as natalizumab, rituximab, tofacitinib), drugs that may increase potassium levels (such as potassium supplements, certain diuretics/”water pills” including amiloride, spironolactone), tacrolimus.

Other medications can affect the removal of cyclosporine from your body, which may affect how cyclosporine works. Examples include boceprevir, bosentan, mifepristone, St. John’s wort, telaprevir, among others.

This medication can slow down the removal of other medications from your body, which may affect how they work. Examples of affected drugs include aliskiren, dabigatran, dronedarone, simeprevir, certain statins (such as pitavastatin, simvastatin), voxilaprevir, among others.

Cyclosporine may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Cyclosporine?

Cyclosporine may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.

What health conditions may interact with Cyclosporine?

Cyclosporine may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Cyclosporine.

What is the dose of Cyclosporine for an adult?

Usual Adult Dose for Organ Transplant – Rejection Prophylaxis

ORAL FORMULATION (MODIFIED):

-Note: The dose is dependent upon type of transplant and formulation; refer to local protocol for specific dosing.

-Initial dose: Give 4 to 12 hours prior to transplantation or postoperatively; the initial dose varies depending on the organ and concomitant immunosuppressives.

NEWLY TRANSPLANTED PATIENTS:

-Renal: 9 mg/kg/day (plus or minus 3 mg/kg/day) orally in 2 divided doses

-Liver: 8 mg/kg/day (plus or minus 4 mg/kg/day) orally in 2 divided doses

-Heart: 7 mg/kg/day (plus or minus 3 mg/kg/day) orally in 2 divided doses

COMMENTS:

-The initial dose of this drug varies depending on the transplanted organ and the other immunosuppressive agents included in the protocol.

-In newly transplanted patients, the initial oral dose is the same as the initial oral dose of the non-modified formulation.

-Titrate the dose based on rejection and tolerability.

-Lower doses of the modified formulation may be sufficient as maintenance therapy.

-Adjunct therapy with adrenal corticosteroids is recommended initially. Consult local protocol and/or manufacturer product information.

ORAL FORMULATION (NON-MODIFIED):

NOTE: The dosing presented here is to be used as a guideline only. Local protocol should be consulted for specific dosing. Dosing in clinical practice may be very different than the manufacturer labeling. Non-modified formulations have decreased bioavailability in comparison to modified formulations. Modified and non-modified formulations are not bioequivalent and cannot be used interchangeably without physician supervision.

Manufacturer recommendation:

-Initial dose: 15 mg/kg orally 4 to 12 hours prior to transplantation; although a single dose of 14 to 18 mg/kg was used in most clinical trials, most clinicians favor the lower end of the scale; lower initial doses are usually used for renal transplantation in the ranges of 10 to 14 mg/kg/day

-Maintenance dose: The initial single daily dose is continued postoperatively for 1 to 2 weeks and then tapered by 5% per week to a maintenance dose of 5 to 10 mg/kg/day; some clinicians prefer to reduce the maintenance dose to 3 mg/kg/day in some renal transplant patients without an apparent rise in rejection rate

PARENTERAL FORMULATION:

-Note: Local protocol should be consulted for dosing recommendations.

Manufacturer suggested dosing:

-Initial dose: 5 to 6 mg/kg/day IV (or one-third of the oral dose) as a single dose infused over 2 to 6 hours given 4 to 12 hours prior to transplantation

-Maintenance dose: 5 to 6 mg/kg/day IV continued postoperatively until the patient can tolerate capsules or oral solution

COMMENTS:

-Due to the risk of anaphylaxis, the IV formulation should be reserved for patients who are unable to take the oral formulation.

-Adjunct steroid therapy should be used with this drug.

Uses: For the prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants concomitantly with adrenal corticosteroids and in the treatment of chronic rejection in patients previously treated with other immunosuppressive agents

Usual Adult Dose for Rheumatoid Arthritis

ORAL FORMULATION (MODIFIED):

-Initial dose: 1.25 mg/kg orally 2 times a day; onset of action usually occurs between 4 and 8 weeks

-Titration: If insufficient benefit is seen and tolerability is good at the initial dose (including serum creatinine less than 30% above baseline), the dose may be increased by 0.5 to 0.75 mg/kg/day after 8 weeks and again after 12 weeks

-Maximum dose: 4 mg/kg/day orally in 2 divided doses; if no benefit is seen by 16 weeks, therapy should be discontinued

COMMENTS:

-Salicylates, nonsteroidal anti-inflammatory agents, and oral corticosteroids may be continued concomitantly with this drug.

-Dose decreases by 25% to 50% should be made at any time to control adverse events (e.g., hypertension, elevations in serum creatinine 30% above pretreatment level), or significant laboratory abnormalities.

-Most patients can be treated with the modified formulation at doses of 3 mg/kg/day or below when combined with methotrexate doses of up to 15 mg/week.

Use: For severe active, rheumatoid arthritis where the disease has not adequately responded to methotrexate; this drug can be used in combination with methotrexate in rheumatoid arthritis patients who do not respond adequately to methotrexate alone

Usual Adult Dose for Psoriasis

ORAL FORMULATION (MODIFIED):

-Initial dose: 1.25 mg/kg orally 2 times a day for at least 4 weeks

-Titration: If insufficient benefit is seen at 4 weeks and tolerability is good at the initial dose, the dose may be increased by 0.5 mg/kg/day at 2-week intervals based on patient response.

-Maximum dose: 4 mg/kg/day in 2 divided doses

-Note: Doses below 2.5 mg/kg/day may also be effective.

COMMENTS:

-Dose decreases by 25% to 50% should be made at any time for adverse events (e.g., hypertension, elevations in serum creatinine greater than or equal to 25% above pretreatment level), or significant laboratory abnormalities. Discontinue therapy if dose reduction is not effective.

-Improvement is usually seen in 2 weeks; stabilization may take 12 to 16 weeks.

-Discontinue therapy if a satisfactory response cannot be achieved after 6 weeks at 4 mg/kg/day or the maximum tolerated dose.

-When a patient appears stable the dose should be lowered, and the patient treated with the lowest dose that maintains an adequate response (not necessarily a complete response).

-Doses at the lower end of the recommended range are effective in maintaining a satisfactory response in 60% of the patients. Doses below 2.5 mg/kg/day may also be effective.

-Most patients will experience relapse of their psoriasis upon cessation of therapy.

-Long term experience in psoriasis patients is limited; therefore, therapy beyond one year is not recommended. Alternating with other forms of therapy should be considered in the long-term management of psoriasis.

Use: For nonimmunocompromised patients with severe (i.e., extensive and/or disabling), recalcitrant, plaque psoriasis who have failed to respond to at least one systemic therapy (e.g., PUVA, retinoids, or methotrexate) or in patients for whom other systemic therapies are contraindicated, or cannot be tolerated

Usual Pediatric Dose for Organ Transplant – Rejection Prophylaxis

The same dose and dosing regimen may be used in children as in adults although in several studies, children have required and tolerated higher doses than adults. Consult the manufacturer product information/and or local protocol.

ORAL FORMULATION (MODIFIED):

1 year and older:

-Note: The dose is dependent upon type of transplant and formulation; refer to local protocol for specific dosing.

-Initial dose: Give 4 to 12 hours prior to transplantation or postoperatively; the initial dose varies depending on the organ and concomitant immunosuppressives.

NEWLY TRANSPLANTED PATIENTS:

-Renal: 9 mg/kg/day (plus or minus 3 mg/kg/day) orally in 2 divided doses

-Liver: 8 mg/kg/day (plus or minus 4 mg/kg/day) orally in 2 divided doses

-Heart: 7 mg/kg/day (plus or minus 3 mg/kg/day) orally in 2 divided doses

COMMENTS:

-The initial dose of this drug varies depending on the transplanted organ and the other immunosuppressive agents included in the protocol.

-In newly transplanted patients, the initial oral dose is the same as the initial oral dose of the non-modified formulation.

-Titrate the dose based on rejection and tolerability.

-Lower doses of the modified formulation may be sufficient as maintenance therapy.

-Adjunct therapy with adrenal corticosteroids is recommended initially. Consult local protocol and/or manufacturer product information.

ORAL FORMULATION (NON-MODIFIED):

6 months and older:

NOTE: The dosing presented here is to be used as a guideline only. Local protocol should be consulted for specific dosing. Dosing in clinical practice may be very different than the manufacturer labeling. Non-modified formulations have decreased bioavailability in comparison to modified formulations. Modified and non-modified formulations are not bioequivalent and cannot be used interchangeably without physician supervision.

Manufacturer recommendation:

-Initial dose: 15 mg/kg orally 4 to 12 hours prior to transplantation; although a single dose of 14 to 18 mg/kg was used in most clinical trials, most clinicians favor the lower end of the scale; lower initial doses are usually used for renal transplantation in the ranges of 10 to 14 mg/kg/day

-Maintenance dose: The initial single daily dose is continued postoperatively for 1 to 2 weeks and then tapered by 5% per week to a maintenance dose of 5 to 10 mg/kg/day; some clinicians prefer to reduce the maintenance dose to 3 mg/kg/day in some renal transplant patients without an apparent rise in rejection rate

PARENTERAL FORMULATION:

6 months and older:

-Note: Local protocol should be consulted for dosing recommendations.

Manufacturer suggested dosing:

-Initial dose: 5 to 6 mg/kg/day IV (or one-third of the oral dose) as a single dose infused over 2 to 6 hours given 4 to 12 hours prior to transplantation

-Maintenance dose: 5 to 6 mg/kg/day IV continued postoperatively until the patient can tolerate capsules or oral solution

COMMENTS:

-Due to the risk of anaphylaxis, the IV formulation should be reserved for patients who are unable to take the oral formulation.

-Adjunct steroid therapy should be used with this drug.

Uses: For the prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants concomitantly with adrenal corticosteroids and in the treatment of chronic rejection in patients previously treated with other immunosuppressive agents

Renal Dose Adjustments

-Rheumatoid arthritis or psoriasis patients with abnormal renal function: Contraindicated

-Careful monitoring of blood or plasma concentrations of this drug is necessary to avoid exacerbation of renal impairment.

Liver Dose Adjustments

-Dose reduction may be necessary in patients with severe liver impairment to maintain blood concentrations within the recommended target range

-Due to decreased plasma clearance of this drug in patients with liver disease, plasma or blood concentrations should be monitored closely and dose adjustments made as necessary.

Dose Adjustments

CONVERSION FROM THE NON-MODIFIED FORMULATION TO THE MODIFIED FORMULATION IN TRANSPLANT PATIENTS:

-Start the modified formulation with the same daily dose as the non-modified formulation. Adjust the dose of the modified formulation to attain the pre-conversion cyclosporine blood trough concentration. Patients who absorb the non-modified formulation poorly require different dosing strategies

-The blood trough concentration should be monitored every 5 to 7 days until the it attains the pre-conversion value.

-Parameters such as serum creatinine and blood pressure should be monitored every 2 weeks during the first 2 months after conversion.

-If blood trough concentrations are outside the desired range and/or if the safety parameters worsen, adjust the dose of the modified formulation accordingly.

TRANSPLANT PATIENTS WHO ABSORB THE NON-MODIFIED FORMULATION POORLY:

-Patients with lower than expected blood trough concentrations in relation to the oral dose of the non-modified formulation may have poor or inconsistent absorption.

-After conversion to the modified formulation, patients tend to have higher cyclosporine concentrations. Due to the increase in bioavailability following conversion to the modified formulation, the cyclosporine blood trough concentration may exceed the target range. Caution should be exercised when converting patients to the modified formulation at doses greater than 10 mg/kg/day; the dose should be titrated individually based on trough concentrations, tolerability, and clinical response. In this population, the blood trough concentration should be measured more frequently, at least 2 times a week (daily, if initial dose exceeds 10 mg/kg/day) until the concentration stabilizes.

Dialysis

Neither dialysis nor renal failure alters the clearance of this drug significantly.

Other Comments

Administration advice:

-The oral formulation should be administered in 2 divided doses, with a mouthful of water, and swallowed whole.

-The oral solution should be diluted and stirred with water, orange juice, squash, or apple juice immediately prior to administration. The measuring device should not come into contact with the diluent and it should not be rinsed with water, alcohol, or any other liquid. The outside of the measuring device may be wiped with a dry tissue. Grapefruit and grapefruit juice should not be used as a diluent for the oral solution or ingested for one hour prior to administration because it increases the bioavailability of this drug.

General:

-The polyoxyethylated castor oil contained in the IV formulation can cause phthalate stripping from PVC.

-Active Herpes simplex infections should be permitted to clear prior to initiating therapy.

-The IV dose is approximately one-third of the recommended oral dose.

-Transferring or switching between different oral formulations of this drug is not recommended; however, if substitution is necessary, appropriate monitoring of drug blood levels, serum creatinine levels, and blood pressure is recommended.

-Modified formulations and non-modified formulations are not bioequivalent and cannot be used interchangeably.

Patient advice:

-Patients should be advised that any change of formulation should be made cautiously and only under physician supervision because it may result in the need for a change in dose.

-Patients should be informed of the necessity of repeated laboratory tests while they are receiving this drug.

-Patients should be given careful dosage instructions, advised of the potential risks during pregnancy, and informed of the increased risk of neoplasia.

-Patients using the oral solution with its accompanying syringe for dosage measurement should be cautioned not to rinse the syringe either before or after use. Introduction of water into the product by any means will cause variation in dose.

What is the dose of Cyclosporine for a child?

The dosage has not been established in pediatric patients. It may be unsafe for your child. It is always important to fully understand the safety of the drug before using. Please consult with your doctor or pharmacist for more information.

How is Cyclosporine available?

Cyclosporine is available in the following dosage forms and strengths:

  • Oral capsule,
  • Oral liquid,
  • Injectable solution,
  • Oral solution,
  • Compounding powder.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Cyclosporine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

 

Hello Health Group does not provide medical advice, diagnosis or treatment.

Sources

Review Date: August 16, 2018 | Last Modified: August 16, 2018

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