CYCLOSPORINE

Background and Date of Approval

Cyclosporine received U.S. Food and Drug Administration (FDA) approval on 13 January 2000 for prevention of organ rejection in transplant recipients.

Uses

Cyclosporine is used in the prevention of organ rejection (Kidney, liver, and heart) and in the treatment of autoimmune diseases like rheumatoid arthritis and psoriasis.

How is it administered?

Cyclosporine is available in the form of capsule, injection and oral solution. Cyclosporine Capsule is available in the doses 25mg, 50mg and 100mg. Your healthcare provider will administer Cyclosporine 50mg Injection if you are unable to tolerate oral capsule or suspension. Your healthcare provider will prescribe the accurate dose based on the organ transplanted, body weight and health condition.

Side Effects

Side effects are unwanted symptoms caused by medicines. Although all drugs can cause side effects, not everyone experiences them. Serious side effects of Cyclosporine: Kidney damage, which may lead to renal dysfunction and elevated serum creatinine levels Liver damage, which may include jaundice, hepatitis, or liver failure Severe allergic reactions (swelling of lips, tongue, or throat, difficulty breathing, or swallowing) Thrombotic Microangiopathy (blood clots affecting small blood vessels, leading to organ damage) Infections (serious bacterial, viral, or fungal infections, including opportunistic infections) Common side effects of Cyclosporine: Hypertension (high blood pressure) Headache Gastrointestinal issues (nausea, vomiting, diarrhoea) Tremors or shaking Hair growth (unwanted body hair) Swelling (oedema, particularly in the ankles and feet) Hyperkalemia (elevated potassium levels) Hyperuricemia (elevated uric acid levels, leading to gout)

Warnings

Immune system suppression : Increases the risk of infections, including serious bacterial, viral, and fungal infections. Kidney damage : This can cause kidney dysfunction and structural damage, requiring regular monitoring of renal function. Liver damage : This may lead to liver injury, including jaundice and hepatitis. Increased blood pressure (Hypertension) : Cyclosporine can elevate blood pressure, requiring monitoring and management. Neurological side effects : May cause tremors, convulsions, or encephalopathy, including rare cases of Posterior Reversible Encephalopathy Syndrome (PRES). Hypersensitivity reactions : Possible allergic reactions, including swelling of lips, tongue, or throat, difficulty breathing, or skin rash. Hematologic changes : These may cause low blood cell counts, leading to anaemia, thrombocytopenia, or leukopenia. Electrolyte imbalances : Can cause changes in potassium (hyperkalemia) and uric acid (hyperuricemia) levels.

Precautions

Cyclosporine has the ability to cause fetal harm, so it is advisable to tell your physician if you are pregnant or planning to have a baby. This medicine also has the tendency to increase blood pressure and blood sugar levels in pregnant women. Avoid breastfeeding your baby while you are on the treatment, as Cyclosporine can impact the growth and development of the baby by passing into the breast milk. It is important to take certain precautions when using Cyclosporine. These include reading and following the recommended dosage instructions provided by the manufacturer, purchasing from reputable sources to ensure quality, being aware of potential interactions with medications or existing health conditions, and monitoring for any allergic reactions or adverse effects.

Word of Advice

Cyclosporine can increase skin sensitivity to sunlight. Apply sunscreen with adequate SPF and wear protective clothing when exposed to the sun. Inform your healthcare provider if you have lactose intolerance before beginning treatment. Cyclosporine contains a small amount of alcohol. While this has minimal impact on driving ability, refrain from driving or operating machinery if you experience dizziness or fatigue. During cyclosporine treatment, monitor for infections, kidney and liver function, blood pressure, and neurological symptoms. Do not stop cyclosporine abruptly, as discontinuation can increase the risk of organ rejection in transplant patients or exacerbate autoimmune conditions. Arrange regular blood tests to assess blood cell counts and electrolyte levels. Exercise careful management of diabetes if you are at risk. Use additional caution when administering cyclosporine to paediatric and geriatric patients. Observe for any psychological effects and maintain regular contact with your healthcare provider to support safe and effective treatment.

References

1. Novartis Pharmaceuticals UK Limited, Electronic Medicines Compendium (EMC), [Revised on May 2022] [Accessed on 15th Sep 2022], https://www.medicines.org.uk/emc/files/pil.1036.pdf 2. AbbVie Inc., [Revised on Feb 2021] [Accessed on 15th Sep 2022], https://www.rxabbvie.com/pdf/gengraf-oral.pdf 3. AbbVie Inc., [Revised on Feb 2021] [Accessed on 15th Sep 2022], https://www.rxabbvie.com/pdf/gengraf-cap.pdf 4. Alan M. Krensky, Jamil R. Azzi, and David A. Hafler, Goodman & Gilman’s Pharmacological Basis of Therapeutics, Immunosuppressants and Tolerogens, 13th Edition, 2018, 637-653. 5. Carolina Tapia; Trevor A. Nessel; Patrick M. Zito, Cyclosporine, StatPearls [Internet], [Revised on 15th Nov 2021] [Accessed on 15th Sep 2022], https://www.ncbi.nlm.nih.gov/books/NBK482450/

Frequently Asked Questions

Who should not use Cyclosporine?

People who have experienced hypersensitivity to Cyclosporine and or any of its ingredients should not use Cyclosporine. Avoid taking Cyclosporine if you have been diagnosed with uncontrolled hypertension, kidney impairment or cancer.

What should you avoid while taking Cyclosporine?

Avoid receiving live attenuated vaccines, and drinking red wine, grapefruit, or grapefruit juice while on treatment with Cyclosporine. Avoid consuming foods high in potassium content. Wear protective clothing and use effective sunscreen to prevent skin damage due to sun exposure.

How long can you take Cyclosporine Injection?

Cyclosporine Injection is prescribed if you are unable to tolerate oral doses. You will be shifted to oral Cyclosporine treatment as soon as possible.

Can I consume grapefruit or grapefruit juice while taking cyclosporine?

Avoiding grapefruit or grapefruit juice while taking cyclosporine is generally advised. Grapefruit can interfere with the metabolism of this medication, leading to increased levels of the medication in the body, which can be potentially harmful.

What will you be monitored for during treatment with Cyclosporine?

Your healthcare provider will your blood pressure, blood glucose, electrolytes, cholesterol and the concentration of Cyclosporine in your blood to check how well your body is tolerating this treatment.

How is Cyclosporine administered?

Cyclosporine is intended for oral administration in the form of injection, capsule or oral suspension. Your healthcare provider will calculate the accurate dose depending on the type of organ transplant and your body weight. You will be prescribed a Cyclosporine injection if you are unable to tolerate oral doses.

Does Cyclosporine affect fertility?

Cyclosporine impairs fertility by lowering sperm count and reducing testicular function in men.

Can cyclosporine increase the risk of developing cancer?

Cyclosporine has been associated with an increased risk of developing certain types of cancer, particularly skin cancers and lymphomas. It is important to undergo regular skin examinations and promptly report any unusual skin growths or changes to your healthcare professional. They can monitor for signs of cancer and provide appropriate management.

Available Brands 50

Written By: Muskan Patel, M.Pharm

Reviewed By: Dr. Vishwa Patel, MBBS