Generic
Cyclosporine
7 brands available in the market
At a glance
Cyclosporine is an immunosuppressant used to prevent organ rejection after liver, kidney or heart transplant, and to treat severe rheumatoid arthritis and psoriasis.
Description
Cyclosporine is an immunosuppressant. It works by suppressing your body's immune response to help accept a newly transplanted organ (e.g., liver, kidney or heart). In rheumatoid arthritis, this immunosuppressive effect reduces inflammation of joints and limits joint damage. In psoriasis, it works by reducing the activity of certain immune cells that cause overproduction of skin cells, thus improving scaling and redness.
Indications
- Prevention of organ rejection in transplant patients
- Rheumatoid arthritis
- Psoriasis
- Atopic dermatitis
- Nephrotic syndrome
Therapeutic class
Immunosuppressants
Pharmacological class
Calcineurin Inhibitor
Pharmacology
Ciclosporin is a strong immunosuppressant that acts mainly on the helper T-cells. It inhibits the activation of calcineurin and production of interleukin-2, thus reducing cell-mediated immune response.
Mechanism of action
Cyclosporine inhibits calcineurin activation and interleukin-2 production in helper T-cells, thereby reducing cell-mediated immune response, which helps prevent organ rejection and reduce inflammation.
Dosage
Adult - Immunosuppression in organ transplantation (Oral): Initially: 10-15 mg/kg/day, starting 4-12 hr before procedure and continued for 1-2 wk; usual maintenance: 2-6 mg/kg/day. Lower doses may be used when combined with other immunosuppressants.
Adult - Psoriasis: Initially: 2.5 mg/kg/day, in 2 divided doses. Reduce to lowest effective dose once remission is achieved. Stop treatment if no sufficient improvement to max dose within 6 wk. Max: 5 mg/kg/day.
Adult - Rheumatoid arthritis: 2.5 mg/kg/day, in 2 divided doses. Treatment should continue for 6-8 wk. If response is insufficient, may increase dose gradually. Max: 4 mg/kg/day.
Adult - Nephrotic syndrome: 5 mg/kg daily, given in 2 divided doses.
Adult - Immunosuppression in organ transplantation (IV): Initially: 5-6 mg/kg/day as a single dose, infuse over 2-6 hr. Switch to oral dosage form as soon as possible.
Child - Nephrotic syndrome: 6 mg/kg daily, given in 2 divided doses.
Administration
Take with or without food. It is better to take it in the same way at the same time every day. Do not chew, crush or break it. Take in the dose and duration as advised by your doctor.
Missed 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 go back to your regular schedule. Do not double the dose.
Side effects
Common Side Effects:
- Headache
- Nausea
- Vomiting
- Increased hair growth
- High blood pressure
- Renal dysfunction
- Loss of appetite
- Diarrhea
- Tremor
- Increased risk of infections
Serious Side Effects:
- Nephrotoxicity
- Hepatotoxicity
- Malignancy (especially skin cancer)
- Hypertension
- Neurotoxicity
Precautions & warnings
- Increased risk of infections due to weakened immune system. Tell your doctor if you develop an infection.
- Increased risk of skin cancer; limit exposure to sunlight.
- May affect your ability to drive.
- Regular blood tests are required to monitor blood pressure, liver and kidney function, and mineral levels.
- Drink 8-10 glasses of water per day.
- Do not stop taking Cyclosporine without talking to your doctor first.
Contraindications
- Hypersensitivity
- Malignant neoplasms
- Uncontrolled hypertension
- Psoriasis (in some cases)
- Lactation
Drug interactions
Drugs that increase cyclosporine levels: Diltiazem, doxycycline, erythromycin, ketoconazole, high-dose methylprednisolone, nicardipine, verapamil, oral contraceptives.
Drugs that decrease cyclosporine levels: Carbamazepine, isoniazid, phenobarbitone, phenytoin and rifampicin.
High-dose methylprednisolone: Increased risk of convulsion.
Potentially Fatal: Additive nephrotoxicity with aminoglycosides, amphotericin B, ciprofloxacin, colchicine, melphalan, co-trimoxazole and NSAIDs.
Food interactions
Consuming alcohol with Cyclosporine does not cause any harmful side effects. Can be taken with or without food.
Use in pregnancy
Cyclosporine may be unsafe during pregnancy. Animal studies have shown harmful effects on the developing baby. Your doctor will weigh the benefits and any potential risks before prescribing it. Please consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Cyclosporine is unsafe during breastfeeding. The drug may cause toxicity to the baby.
Pediatric use
For nephrotic syndrome in children: 6 mg/kg/day in 2 divided doses. Limited information available for other pediatric indications.
Geriatric use
No dosage adjustment is necessary in elderly patients. However, caution should be exercised.
Renal / hepatic impairment
Renal impairment: Use with caution. Dose adjustment may be needed. Please consult your doctor. Regular monitoring of kidney function is advised.
Hepatic impairment: Use with caution. Dose adjustment may be needed. Please consult your doctor. Regular monitoring of liver function is advised.
Overdose effects
No adequate information on overdose is available. Overdose may lead to nephrotoxicity, hepatotoxicity and other toxic effects. Consult your doctor if symptoms appear.
Storage conditions
Store below 30°C temperature, away from light & moisture. Keep out of reach of children.
Chemical structure
Cyclosporine